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b) an aperture in and extending through said bottom cover 1. A battery holder attachment structure, comprising: member into a cell of the housing, said aperture adapted to a battery holder, for holding a button-type battery, provided with communicate gases within the cell to said enclosed area of a flexibly elastic tongue-shaped portion having a locking said cover; projection; and c) an atmospheric vent in said cover adapted to communicate a casing body to which said battery holder is removably gases from within said enclosed area of said cover to atmo- attached, sphere; wherein said casing body includes a fitting opening portion for d) a labyrinth of passages formed by a convoluted arrangement receiving said locking projection therein from below, such of vertical walls extending between said bottom cover mem- that said locking projection is locked therein. ture and said atmospheric vent; and 5,843,596 electrolyte level in said cell when the battery is rotated as METHODS OF FORMING BUTTON TYPE BATTERIES AND TO BUTTON TYPE BATTERY INSULATING AND much as ninety degrees from an upright position, no matter whether said battery is rotated forwardly, rearwardly, or to SEALING GASKETS either side. Mark E. Tuttle, Boise, Id., assignor to Micron Communications, Inc., Boise, Id. Division of Ser. No. 649,925, May 16, 1996, Pat. No. 5,662,718, which is a continuation of Ser. No. 348,543, Dec. 1, 1994, abandoned. This application Oct. 11, 1996, Ser. No. 5,843,594 728,778 GROUP OF WINDING ELECTRODES Int. C1.6 HO1M 2/08 Jin Dong Cheong, Kyungki-do; Jong Wook Lee, and Byoung U.S. CI. 429—185 4 Claims Hyun Kang, both of Suwon, all of Rep. of Korea, assignors to ,16 100 Samsung Display Devices Co., Ltd., Suwon, Rep. of Korea Filed Jun. 9, 1997, Ser. No. 871,249 Claims priority, application Rep. of Korea, Oct. 6, 1996, 1996-20552 Int. C1. HOIM 4700 U.S. Cl. 429_94 10 Claims 22 11 13 d 15 20 20 141 1. A button-type battery insulative sealing gasket, the insulative 114 sealing gasket before being crimped in a battery comprising: "L" cross sectional shape; portion, the “L” base portion being configured to receive an inner sealing portion of a peripheral portion of a button-type 1. A winding electrode assembly, comprising: battery terminal lid, the “L” base portion having a radial a cathode winding electrode; length and an inner radial portion and an outer radial portion; a positive terminal linked to said cathode winding electrode; the “L” cross sectional shape defining an annular “L” stem an anode winding electrode; portion, the “L” stem portion being configured to receive an a negative terminal linked to said anode winding electrode; outer sealing portion of the peripheral portion of the buttona separator between said cathode and said anode winding elec type battery terminal lid, the “L” stem portion having a trodes; transverse length and an inner transverse portion and an outer an electrolyte between said winding electrodes; and transverse portion, the “L” stem portion having a thickness a separator fragment starting substantially at a winding axis of which varies along its transverse length, the stem thickness said winding electrodes and extending to an initial part of said being greater at the inner transverse portion than at the outer cathode winding electrode. transverse portion, the change in the stem portion thickness occurring at a substantially perpendicular step; and the “L” base portion having a thickness which varies along its radial length, the base thickness being greater at the inner 5,843,595 radial portion than at the outer radial portion. BATTERY HOLDER ATTACHMENT STRUCTURE Minoru Kawakatsu, Tokyo, Japan, assignor to Mitsumi Electric Co., Ltd., Tokyo, Japan Filed Jul. 23, 1996, Ser. No. 681,355 5,843,597 Claims priority, application Japan, Jul. 28, 1995, 7-212466 RIBBED GASKET FOR MINIATURE GALVANIC CELL Int. C1. HO1M 2/10 Rose A. Getz, Westlake, Ohio, assignor to Eveready Battery U.S. Cl. 429_97 6 Claims Company, Inc., St. Louis, Mo. 6 1 10 Filed Dec. 1, 1997, Ser. No. 980,508 20 40 12 Int. Cl. HO1M 2/08 U.S. CI. 429—174 13 Claims polarity; 50 b) a second electrode of opposite polarity; 13 c) a separator between said first electrode and said second electrode; d) an electrolyte; 14 15 30 16 12 e) a two-part conductive housing containing said first electrode, said second electrode, said separator and said electrolyte; the Page 3
5,843,612 (5) drying the separated colored resin microparticles. TONER AND DEVELOPER COMPOSITIONS WITH COMPATIBILIZERS 5,843,615 IMAGE-RECORDING TECHNOLOGY U.S. CI. 430—110 34 Claims Ghanshyam H. Popat, Alta Loma; Stephen M. Sharp, Glen1. A toner composition comprised of resin, colorant, wax, and a dora, and Gustav A. Ray, Rancho Cucamonga, all of Calif., compatibilizer of the formula assignors to Avery Dennison Corporation, Pasadena, Calif. Filed Dec. 4, 1995, Ser. No. 566,506 Int. C1.6 G03C 5/56;1/72 23 Claims wherein A is ethylene, B is propylene, C is butene, and D is pentene, and wherein the mol fractions are represented by a, b, c, 20 and d, and wherein a is from about 0.05 to about 0.95, b is from about 0.05 to about 0.95, c is from about 0.05 to about 0.95, and 24 is from about 0.05 to about 0.95, and subject to the provision that the sum of a, b, c, and d are equal to about 1.
5,843,613 LIQUID DEVELOPER Miyamoto, Takatsuki, all of Japan, assignors to Minolta Co., Ltd., Osaka, Japan Filed Feb. 15, 1996, Ser. No. 601,776 Claims priority, application Japan, Feb. 16, 1995, 7-028187; 1. A method of recording images from a portable computer Feb. 16, 1995, 7-028188 screen comprising the steps of: Int. Cl. GO3G 9/125 preparing a thin flexible image-recording assembly including a U.S. Cl. 430—114 24 Claims mechanically developable image sheet and an associated thin 1. A liquid developer comprising: flexible shield, said assembly being less than approximately carrier liquid, and 20 mils thick; toner particles, dispersed in the carrier liquid, formed of binder mounting said assembly on the screen of a portable computer; resin and colorant, wherein said carrier liquid contains acidic removing said shield in the presence of an image on said screen, dispersion resin and basic dispersion resin which are soluble to form an image on said image sheet; in said carrier liquid, replacing said shield to cover said image sheet; said liquid developer having a moisture content of 500-20,000 applying mechanical forces to said assembly to develop the ppm. image on said image sheet; and removing said shield to view the developed image; whereby a copy of an image on a portable computer may be obtained without access to a printer. 10. A method for recording an image displayed on a screen 5,843,614 comprising the steps of: MANUFACTURING METHOD FOR TONER USED IN providing an assembly including: ELECTROPHOTOGRAPHY an opaque sleeve having a slot formed in one side thereof and Kinji Shinzo, Sakura; Hideki Watanabe, Yotsukaido; Seiichi an aperture formed in one face thereof; Uno, Sakura, and Munekazu Hayashi, Ichihara, all of Japan, a plurality of image sheets receivable within the opaque assignors to Dainippon Ink and Chemicals, Inc., Tokyo, sleeve; and Japan a shield receivable within the opaque sleeve and slidable Filed Mar. 20, 1997, Ser. No. 821,054 through the slot of the opaque sleeve; Claims priority, application Japan, Mar. 21, 1996, 8-064930; positioning the assembly in front of a screen on which an image Mar. 17, 1997, 9-062903 is displayable with the aperture of the opaque sleeve facing Int. Cl. G03G 9/09 the screen; U.S. Cl. 430—137 9 Claims opening the aperture by sliding the shield out of the opaque 1. A manufacturing method for a toner used in electrophotogra sleeve through the slot; and phy, the method comprising the steps of: exposing one of the image sheets to an image displayed on the (1) forming a mixture of a colored melted resin (a) and an screen for a predetermined amount of time. aqueous medium (b), wherein the colored melted resin (a) is prepared by heating and melting a kneaded material containing a synthetic resin having an ionic group for use in a toner for electrophotography and a coloring pigment, and the aqueous medium (b) has dissolved therein a substance capable of 5,843,616 neutralizing the ionic group, and is held at a temperature not POSITIVE RESIST COMPOSITION lower than the softening point of the synthetic resin by way of Kunishige Edamatsu, Toyonaka; Yuji Yoshida, Mioo; Kazuhiko heating with application of pressure where necessary; Hashimoto, Ibaraki, and Haruyoshi Osaki, Toyonaka, all of (2) dispersing the colored melted resin (a) in the aqueous Japan, assignors to Sumitomo Chemical Company, Ltd., medium (b) by mechanical means while maintaining said Osaka, Japan mixture of the colored melted resin (a) and the aqueous Filed Apr. 10, 1995, Ser. No. 419,604 medium (b) at a temperature not lower than the softening Claims priority, application Japan, Apr. 11, 1994, 6-072211; point of the synthetic resin; Sep. 9, 1994, 6-215910 (3) producing an aqueous suspension of colored resin micropar Int. Cl. GO3F 7/023 ticles by means of sudden cooling; U.S. CI. 430—192 13 Claims (4) separating the colored resin microparticles from the suspen- 1. A positive resist composition which comprises; sion; and an o-quinonediazide compound; and Page 4
FORWARD ANGLE LIGHT SCATTER
5,843,635 5,843,637 INHIBITION OF APC-MEDIATED APOPTOSIS OF METHODS FOR IDENTIFYING NON-ESSENTIAL GENES ACTIVATED T LYMPHOCYTES OF THE HUMAN CYTOMEGALOVIRUS GENOME AND Stuart F. Schlossman, Newton, and Mei X. Wu, Cambridge, FOR SCREENING FOR INHIBITORS OF HUMAN both of Mass., assignors to Dana-Farber Cancer Institute, CYTOMEGALOVIRUS Inc., Boston, Mass. Thomas R. Jones, Nyack; Viera P. Muzithras, Monroe, both of N.Y., and Yakov Gluzman, Upper Saddle River, N.J., assign- Filed Feb. 27, 1995, Ser. No. 395,149 Int. Cl. C12Q 1/70; GOIN 33/564; C07K 16/00 ors to American Cyanamid Company, Madison, N.J. Division of Ser. No. 291,258, Aug. 16, 1994, abandoned, which U.S. CI. 435/5 8 Claims is a continuation of Ser. No. 906,777, Jun. 30, 1992, abandoned, which is a continuation-in-part of Ser. No. 726,431, Jul. 5, 1991, abandoned. This application Jun. 5, 1995, Ser. No. 463,175 Int. Cl. C12Q 1/70;1768 U.S. Cl. 435/5 7 Claims genome to construct an HCMV recombinant in a manner the insertion of the marker gene prevents the expression of the product of the wild-type gene; (ii) adding to a wild-type HCMV gene, so as to disrupt the wild-type gene, such that the insertion of the marker gene prevents the expression of the product of the wild-type gene; (iii) replacing portions of two or more wild-type HCMV genes, such that the insertion of the B-glucuronidase marker gene prevents the expression of the products of those wild-type genes; and (iv) inserting the B-glucuronidase marker gene between two HCMV genes, such that no HCMV genes are replaced or 1. A method of screening for an inhibitor of antigen presenting disrupted and all HCMV gene products are expressed; cell-mediated priming of resting peripheral blood T lymphocytes to (b) inserting the recombinant HCMV constructed in step (a) into undergo activation induced apoptosis, said method comprising the a suitable mammalian host cell; steps of: (c) growing the host cell under suitable conditions to favor providing first and second samples of components for a T HCMV replication; lymphocyte apoptosis assay, said components comprising (d) measuring the amount of any B-glucuronidase produced; resting peripheral blood T lymphocytes and stimulated anti- (e) repeating steps (c)-d) in the presence of the test compound; gen presenting cells selected from the group consisting of and monocytes, macrophages and dendritic cells, said stimulated (f) comparing the results of (d) and (e), a reduction or inhibition antigen presenting cells being provided for priming said T of the amount of B-glucuronidase produced in the presence of lymphocytes to undergo apoptosis; the test compound indicating that the test compound inhibits causing said first sample of components to react in said apopto- HCMV replication. sis assay, wherein the extent of T lymphocyte apoptosis in said first assay sample is determined; adding a candidate inhibitor to said second sample of compo nents; causing said second sample of components containing said can 5,843,638 NUCLEIC ACIDS AND PEPTIES OF HUMAN didate inhibitor to react in said apoptosis assay, wherein the extent of T lymphocyte apoptosis in said second assay sample Luc Montagnier, Le Plessis Robinson; Bernard Krust; Solange IMMUNODEFICIENCY VIRUS TYPE-1 (HIV-1). is determined; and comparing said extent of T lymphocyte apoptosis in said first Chamaret, both of Paris; François Clavel, Paris; Jean Claude Chermann, Elancourt; Françoise Barre-Sinoussi, assay sample to said extent of T lymphocyte apoptosis in said second assay sample to determine the effect of said candidate Issy les Moulineaux; Marc Alizon; Pierre Sonigo, both of inhibitor. Paris; Stewart Cole, Chatillon; Olivier Danos, Paris, and la Recherche Scientifique, Paris, France Continuation of Ser. No. 130,565, Oct. 1, 1993, abandoned, which is a division of Ser. No. 970,954, Nov. 3, 1992, aban5,843,636 doned, which is a continuation of Ser. No. 747,506, Aug. 20, HEPATITIS C VIRUS EPITOPES 1991, abandoned, which is a continuation of Ser. No. 622,278, Gregory R. Reyes; Jungsuh P. Kim, both of Palo Alto; Ran Dec. 6, 1990, abandoned, which is a continuation of Ser. No. dolph Moeckli, Redwood City, and Christian C. Simonsen, 390,499, Aug. 1, 1989, abandoned, which is a continuation of Saratoga, all of Calif., assignors to Genelabs Technologies, Ser. No. 920,119, Oct. 17, 1986, abandoned, which is a Inc., Redwood City, Calif. continuation-in-part of Ser. No. 771,248, Aug. 30, 1985, abanDivision of Ser. No. 681,703, Apr. 5, 1991, Pat. No. 5,443,965, doned, which is a continuation-in-part of Ser. No. 771,247, which is a continuation-in-part of Ser. No. 594,854, Oct. 10, Sep. 30, 1985, abandoned, which is a continuation-in-part of 1990, abandoned, which is a continuation-in-part of Ser. No. Ser. No. 771,230, Aug. 30, 1985, abandoned, which is a 205,611, Apr. 6, 1990, abandoned. This application Mar. 17, continuation-in-part of Ser. No. 706,562, Feb. 28, 1985, aban1995, Ser. No. 407,410 doned, which is a continuation-in-part of Ser. No. 558,109, Int. Cl. C12Q 1/70; C12P 21/06; C07H 17/00 Dec. 5, 1983, abandoned. This application Jun. 6, 1995, Ser. No. 468,387 U.S. Cl. 435/5 12 Claims Claims priority, application United Kingdom, Nov. 16, 1984, 1. A recombinant polypeptide which is specifically immunoreac- 84 29099; Canada, Oct. 18, 1985, 493377 tive with sera from humans infected with hepatitis C virus (HCV), Int. Cl. C12Q 1/70;1/68; C12N 15749; C07H 21/04 where said polypeptide includes the peptide sequence presented as U.S. CI. 435—5 1 Claim SEQ ID NO:8. 1. A nucleic acid of the genome of a human immunodeficiency Page 5
greater than that of the fluid sample; (ii) a light receiving 5,843,653 edge; and (iii) a reactive surface comprising a plurality of METHOD FOR DETECTING A TARGET MOLECULE IN sites having oligonucleotide immobilized thereon, said sites A SAMPLE USING A NUCLEIC ACID LIGAND defining an array of oligonucleotides, said reactive surface Larry Gold, Boulder, Colo., and Craig Tuerk, Morehead, Ky., assignors to NeXstar Pharmaceuticals, Inc., Boulder, Colo. further comprising other non-situs portions having no oligo Continuation of Ser. No. 714,131, Jun. 10, 1991, Pat. No. nucleotides immobilized thereon; 5,475,096, which is a continuation-in-part of Ser. No. 536,428, (b) contacting the reactive surface under hybridizing conditions Jun. 11, 1990, abandoned. This application Jun. 6, 1995, Ser. with said at least two nucleic acid sequences wherein said No. 469,609 nucleic acid sequences, either directly or through intermediate Int. Cl. C12Q 1/68; C12P 19/34; C07H 21/04;21/02 cognate binding pairs, is labeled with a light scattering label; U.S. Cl. 435—6 57 Claims thereby forming light scattering label complexes attached at those sites of the reactive surface having an oligonucleotide T7 PROD 3 complementary to said nucleic acid sequences immobilized ligation thereon; fronscription (c) illuminating the light receiving edge of the waveguide with variable light effective to create total internal reflection within the waveguide, thereby simultaneously illuminating the entire 3' primer 9P43 ...innealing recognition reactive surface; selection by ap 43 (d) collecting light scattered across the entire reactive surface by 5 said light scattering label; d. CDNA Synthesis of selected (e) comparing the degree of light scattering at each situs with RNAS eluted from filters either (i) the degree of light scattering at a non-situs portion; 17 PRO O or (ii) the degree of light scattering at another situs; Strand Pol synthesis (f) incrementally increasing the stringency conditions at the pol reactive surface of the waveguide device to initiate dissociation of bound nucleic acid from the sites wherein said com f) in vitro transcription to begin the next paring of step (e) is continued during the incremental stringency increase; 1. A method for detecting the presence or absence of a target whereby base differences between the at least two oligonucle- molecule in a sample which may contain said target molecule comprising: otides can be distinguished by differences in dissociation a) exposing said sample which may contain said target molecule properties. to a non-naturally occurring nucleic acid ligand of said target molecule, wherein said nucleic acid ligand is not a nucleic acid having the known physiological function of being bound by said target molecule, under conditions wherein a target molecule; nucleic acid ligand binding pair is formed if said 5,843,652 target molecule is present, wherein said binding is not due to ISOLATION AND CHARACTERIZATION OF AGOUTI: A Watson/Crick base pairing; and DIABETES/OBESITY RELATED GENE b) determining whether said target molecule:nucleic acid ligand Richard P. Woychik, Knoxville, Tenn., assignor to Lockheed binding pair is formed, thereby detecting the presence or Martin Energy Systems, Inc., Oak Ridge, Tenn. absence of the target molecule in the sample. Division of Ser. No. 64,385, May 21, 1993. This application Jun. 5, 1995, Ser. No. 463,387 17 Claims 5,843,654 1. A method for detecting a mammalian Agouti nucleic acid RAPID DETECTION OF MUTATIONS IN THE P53 GENE sequence in a biological sample comprising: Laura M. Heisler, Madison, Wis., Lance Fors, Monrovia, Calif., and Mary Ann D. Brow, Madison, Wis., assignors to a) obtaining a biological sample comprising nucleic acid Third Wave Technologies, Inc., Madison, Wis. sequences from a mammal; Continuation-in-part of Ser. No. 402,601, Mar. 9, 1995, which b) providing a pair of oligonucleotide primers wherein said is a continuation-in-part of Ser. No. 337,164, Nov. 9, 1994, primers are sufficiently complementary to a sequence selected abandoned, which is a continuation-in-part of Ser. No. from the group consisting of: SEQ ID NO: 1, the full comple- 254,359, Jun. 6, 1994, Pat. No. 5,614,402, which is a ment of SEQ ID NO: 1, a mammalian Agouti coding continuation-in-part of Ser. No. 73,384, Jun. 4, 1993, Pat. No. sequence, and the full complement of a mammalian Agouti 5,541,311, which is a continuation-in-part of Ser. No. 986,330, coding sequence, to specifically hybridize to said mammalian Dec. 7, 1992, Pat. No. 5,422,253. This application Jun. 7, Agouti nucleic acid sequence and not to non-Agouti 1995, Ser. No. 484,956 Int. Cl. c12 1768; C12P 19/34 sequences and wherein each member of said pair of primers is U.S. CI. 435—6 25 Claims selected to hybridize to opposite strands of said mammalian 1. A method for treating nucleic acid comprising an oligonucleAgouti sequence; otide containing human p53 gene sequences, comprising: c) treating the biological sample with said pair of primers such a) providing: that each primer will specifically hybridize to said Agouti i) an enzymatic cleavage means; and sequence; ii) a nucleic acid substrate containing human p53 gene d) treating the hybridized primers under conditions such that sequences; b) treating said nucleic acid substrate under conditions such that complementary primer extension products are synthesized said substrate forms one or more cleavage structures, said from the sequences to which each primer is hybridized; cleavage structures formed by intra-strand hydrogen bonding e) repeating steps c) and (d) until the sequences are sufficiently in the absence of a primer oligonucleotide; and amplified to be detected, and; c) reacting said cleavage means with said cleavage structures so f) detecting the amplified sequences. that a plurality of cleavage products are produced. 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5,843,677 factor A, wherein the strain Actinomadura Sp. ATCC 39727 or a METHOD OF ASSAYING ASIALOGLYCOPROTEIN mutant of Actinomadura Sp. ATCC 39727 is cultured under subRECEPTOR AND ASSAY REAGENT THEREFOR merged aerobic conditions in an aqueous nutrient culture medium Yoshiro Niitsu, Sapporo; Yutaka Kohgo, Asahikawa; Junji containing assimilable sources of carbon, nitrogen, and inorganic Kato, Sapporo; Hirokazu Yago, Tokyo; Hisashi Hanada, salts, to provide the A40926 complex, the improvement comprisTokyo, and Koji Ushizawa, Tokyo, all of Japan, assignors to Daiichi Pure Chemicals Co., Ltd., Tokyo, Japan ing: an enrichment in the amount of factor A in the A40926 PCT No. PCT/JP95/00770, $ 371 Date Oct. 18, 1996, § 102(e) complex wherein the enrichment is achieved by cultivating the Date Oct. 18, 1996, PCT Pub. No. W095/29403, PCT Pub. strain in a medium comprised of glucose, meat extract, yeast, Date Nov. 2, 1995 peptone, casein, inorganic salts, and an added amount of a precurPCT Filed Apr. 19, 1995, Ser. No. 722,153 sor, at a temperature between about 27° C. and 33° C., wherein the Claims priority, application Japan, Apr. 20, 1994, 6-081268 amount of precursor in the medium is from about 4 to about 20 Int. Cl. GO1N 33/53: C07K 16/28 mM and the precursor is selected from the group consisting of: U.S. Cl. 435—7.1 15 Claims a) isoleucine, the salt of isoleucine with an acid or a base which 1. A method for detecting the asialoglycoprotein receptor in a is non-toxic to the culture; sample, comprising: b) n-propanol, an ester of n-propanol formed with a linear C,-Co (a) contacting the sample, at a pH from 5 to 7, with an unlabeled alkanoic acid, which ester is non-toxic to the culture; and antibody which is capable of binding the asialoglycoprotein c) 2-methyl-1-butanol, an ester of 2-methyl-1-butanol formed receptor; and with a linear C.-C. alkanoic acid, which ester is non-toxic to (b) contacting the sample from step (a) with a composition comprising an antibody which is capable of binding the until the amount of factor A in the medium is equal to about 47% the culture; asialoglycoprotein receptor and is labeled with an enzyme. 5. A method for detecting the asialoglycoprotein receptor in a to about 59% of the total factors A and B, of the complex as sample, comprising: monitored chromatographically, then recovering the complex from (a) contacting the sample with an unlabeled antibody which is the culture medium by separating the complex enriched in factor A capable of binding the asialoglycoprotein receptor; and from the medium and, isolating the complex via chromatography. (b) contacting the sample from step (a) with a composition 6. A process for preparing antibiotic A40926 complex containing comprising phenol and an antibody which is capable of bind- factor B,, wherein the strain Actinomadura Sp. ATCC 3 9727 or a ing the asialoglycoprotein receptor and is labeled with an mutant of Actinomadura Sp. ATCC 39727 is cultured under subenzyme, wherein the phenol accelerates the binding of the merged aerobic conditions in an aqueous nutrient culture medium antibody which is capable of binding the asialoglycoprotein containing assimilable sources of carbon, nitrogen, and inorganic receptor and the asialoglycoprotein receptor. salts, to provide A40926 complex, the improvement comprising: an 10. A method for detecting the asialoglycoprotein receptor in a enrichment of factor B, in the A40926 complex wherein the sample, comprising: enrichment is achieved by cultivating the strain in a medium (a) contacting the sample, at a pH from 5 to 7, with an unlabeled comprised of glucose, meat extract, yeast, peptone, casein, inor antibody which is capable of binding the asialoglycoprotein ganic salts, and an added amount of a precursor, at a temperature receptor; and (b) contacting the sample from step (a) with a composition between about 27° C. and 33° C., wherein the amount of added comprising phenol and an antibody which is capable of bind- precursor in the medium is from about 4 to about 10 mM and the ing the asialoglycoprotein receptor and is labeled with an precursor is selected from the group consisting of: enzyme. a) valine, the salt of valine formed with an acid or a base which is non-toxic to the culture; and b) isobutanol, an ester of isobutanol formed with a linear C,-C6 alkanoic acid, which ester is non-toxic to the culture; until the amount of factor B, is equal to about 81% to about 97% 5,843,678 of the total of factors A and B, of the complex as monitored OSTEOPROTEGERIN BINDING PROTEINS chromatographically, then recovering the complex from the culture William J. Boyle, Moorpark, Calif., assignor to Amgen Inc., medium by separating the complex from the medium, and isolating Thousand Oaks, Calif. the complex via chromatography. Filed Apr. 16, 1997, Ser. No. 842,842 Int. Cl. C12Q 1/00; C07K 14/00 U.S. Cl. 435—7.1 15 Claims 1. A purified and isolated osteoprotegerin binding protein. 5,843,680 DIFFERENTIAL SEPARATION ASSAY METHODS AND TEST KITS Bala S. Manian, Los Altos Hills; Vartan E. Ghazarossian, 5,843,679 METHOD FOR SELECTIVELY ENHANCING THE Menlo Park, and Paul G. Hayter, Los Altos, all of Calif., PRODUCTION OF FACTORS A OR B, OF ANTIBIOTIC A assignors to Biometric Imaging, Inc., Mountain View, Calif. 40926 COMPLEX Continuation-in-part of Ser. No. 277,161, Jul. 19, 1994, abanEnrico Selva, Via Di Vittorio; Luciano Gastaldo, Via San Mar doned, which is a continuation of Ser. No. 927,928, Aug. 10, tino; Maurizio Denaro, Viale Bligny; Giovanni Cassani, Via 1992, abandoned, which is a continuation-in-part of Ser. No. Vittadini, and Francesco Parenti, Via Benvenuto Cellini, all 828,407, Jan. 31, 1992, Pat. No. 5,137,609. This application of Italy, assignors to Biosearch Italia S.p.A., Varese, Italy Apr. 19, 1995, Ser. No. 425,718 Continuation of Ser. No. 258,907, Jun. 10, 1994, abandoned, Int. C1.6 GOIN 33/558;33/573 which is a continuation of Ser. No. 140,363, Oct. 20, 1993, U.S. Cl. 435—7.4 15 Claims abandoned, which is a continuation of Ser. No. 866,075, Apr. 1. A method for detecting an analyte in a test sample comprising: 1, 1992, abandoned, which is a continuation of Ser. No. a) labeling a specific binding agent with a detectable label, 519,338, May 2, 1990, abandoned, which is a continuation of wherein the labeled binding agent specifically binds to the Ser. No. 95,371, Sep. 10, 1987, abandoned. This application analyte to form a complex; Jun. 2, 1995, Ser. No. 460,024 b) providing a separation medium on which the labeled binding Claims priority, application United Kingdom, Sep. 11, 1988, agent and complex migrate at different velocities during elec8621912 trophoresis; Int. C1.6 C12P 21/04 c) contacting the test sample with an excess amount of labeled U.S. Cl. 435—71.3 9 Claims binding agent to produce a reaction mixture containing the 1. A process for preparing antibiotic A40926 complex containing labeled binding agent and the complex; Page 7
(i) an enzyme donor polypeptide conjugate of the form: 5,843,684 METHOD FOR DETECTING PRE-CANCEROUS OR CANCEROUS CELLS USING P90 ANTIBODIES OR CH3 CH PROBES Hill, N.C., and Carlos Cordon-Cardo, New York, N.Y., N.J. Date Mar. 31, 1995, PCT Pub. No. W094/00603, PCT Pub. Date Jan. 6, 1994 N Continuation-in-part of Ser. No. 18,649, Feb. 17, 1993, aban doned, which is a continuation-in-part of Ser. No. 904,766, R1-COR2+Z Jun. 26, 1992, abandoned, which is a continuation-in-part of Ser. No. 730,185, Jul. 12, 1991, abandoned, which is a wherein Z is an enzyme donor polypeptide of B-galactosidase; continuation-in-part of Ser. No. 543,963, Jun. 27, 1990, abanR,=an alkyl, cycloalkyl or aryl group having 1 to 10 carbon doned. This PCT application Jun. 28, 1993, Ser. No. 362,590 Int. C1.6 GOIN 33/574; CO7K 16/30 atoms; U.S. Cl. 435—7.23 34 Claims Rzra bond or 1. A method of assessing a subject's cancer prognosis, the method comprising: (a) obtaining a biological sample from the subject, (b) determining whether the level of either p53 or dm2 in the -NH-R3-N sample is abnormally elevated; and (c) classifying a biological sample into one of three groups, the first group comprises no abnormal elevation of either the level S of p53 or dm2, the second group comprises abnormal eleva tion of the level of p53 and no abnormal elevation of the level wherein Rz=an alkyl, cycloalkyl, or aryl group having 2 to 10 of dm2 or abnormal elevation of the level of dm2 and no abnormal elevation of the level of p53, and the third group carbon atoms; and comprises abnormal elevation of the level of both p53 and n=1 to p where p=MW of Z/1000; dm2, whereby the first group indicates the best prognosis, the (ii) an enzyme acceptor polypeptide wherein said enzyme second group indicates an intermediate prognosis, and the acceptor polypeptide is characterized by forming with said third group indicates the worst prognosis. enzyme donor polypeptide conjugate an active enzyme complex having B-galactosidase activity in the absence of an antibody to LSD; (iii) an antibody specific for LSD, wherein said enzyme donor 5,843,685 conjugate is capable of competitively binding to said anti PRODUCTION OF CHIMERIC MOUSE-HUMAN body, thereby inhibiting the formation of active enzyme ANTIBODIES WITH SPECIFICITY TO HUMAN TUMOR complex; and ANTIGENS (iv) a substrate for B-galactosidase; and Marc D. Better; Arnold H. Horwitz; Randy R. Robinson; (b) measuring the rate of conversion of said substrate by said Shau-Ping Lei, all of Los Angeles, and Changtung Paul active enzyme complex as a measure of the amount of LSD in Chang, Chatsworth, all of Calif., assignors to Xoma Corposaid sample. ration, Berkeley, Calif. Continuation of Ser. No. 364,001, Dec. 27, 1994, Pat. No. 5,576,184, which is a continuation of Ser. No. 659,401, Jul. 29, 1991, abandoned, which is a continuation-in-part of Ser. No. 240,624, Sep. 6, 1988, abandoned, Ser. No. 241,744, Sep. 8, 5,843,683 1988, abandoned, Ser. No. 243,739, Sep. 13, 1988, abandoned, PAS DOMAIN PROTEINS Ser. No. 367,641, Jun. 19, 1989, abandoned, Ser. No. 382,768, Isaac Edery, Brookline; Zuoshi Josh Huang, Waltham, and Jul. 21, 1989, abandoned, Ser. No. 382,768, Jul. 21, 1989, Michael Rosbash, Newton, all of Mass., assignors to Bran- abandoned, and Ser. No. 253,002, Oct. 4, 1988, abandoned. deis University, Waltham, Mass. This application Jun. 6, 1995, Ser. No. 466,034 Continuation of Ser. No. 531,097, Sep. 20, 1995, abandoned, Int. Cl. A61K 39/395; V07K 16/30; GOIN 33/574 which is a continuation of Ser. No. 91,841, Jul. 14, 1993, U.S. Cl. 435—7.23 19 Claims abandoned. This application Sep. 23, 1996, Ser. No. 716,630 3. A chimeric immunoglobulin comprising two light chains and Int. Cl. GOIN 33/566; C07K 14/705; C12Q 1/68 two heavy chains, each of said heavy chains comprising a variable U.S. Cl. 435—7.8 5 Claims region and a human constant region, and each of said light chains 1. Method for identifying a molecule potentially useful as a comprising a variable region and a human constant region, wherein: therapeutical molecule by altering the interaction of AH receptor (a) said chimeric immunoglobulin recognizes the human tumor protein and Arnt protein through their PAS domains, comprising antigen bound by antibody ING-1; the steps of: (b) the antigen combining site of said chimeric immunoglobulin contacting a test molecule with isolated PAS domains from said of part (a) competitively inhibits the binding of antibody AH receptor protein and Arnt protein; and ING-1 produced by cell line HB9812 as deposited with the assessing the ability of the test molecule to alter the interaction ATCC, and of said PAS domains as an indication of a potentially useful (c) said chimeric immunoglobulin of part (a) mediates therapeutic molecule which alters the interaction of said AH complement-dependent cytolysis or antibody-dependent cellureceptor protein and Arnt protein through their PAS domains. lar cytotoxicity of target cells. Page 8
(a) a DNA encoding a P-selectin ligand protein, said protein 5,843,710 comprising an amino acid sequence selected from the group VACCINES AGAINST ANIMAL PARASITIC NEMATODES consisting of the amino acid sequence set forth in SEQ ID Gary Stewart Cobon, Frenchs Forest; Rosemary Ann Austen, NO:2 from amino acid 1 to amino acid 402, the amino acid East Gosford; Ian Joseph O'Donnell, Gardenvale; Maurice sequence set forth in SEQ ID NO:2 from amino acid 1 to Joseph Frenkel, South Caulfield; William Peter Keith amino acid 310, the amino acid sequence set forth in SEQ ID Kennedy, Willoughby; Keith William Savin, Caulfield South, NO:2 from amino acid 42 to amino acid 402, the amino acid and Barry Maxwell Wagland, Carlingford, all of Australia, assignors to Biotech Australia Pty. Limited and Csiro, Aussequence set forth in SEQ ID NO:2 from amino acid 42 to tralia amino acid 310, and the amino acid sequence set forth in SEQ Division of Ser. No. 353,658, May 2, 1989. This application ID NO:4; and Jun. 7, 1995, Ser. No. 482,547 (b) a DNA capable of hybridizing under stringent conditions to a Claims priority, application Australia, Jul. 7, 1987, PI2940; DNA specified in (a) and encoding a naturally occuring New Zealand, May 7, 1988, 225295; Canada, Jun. 7, 1988, P-selectin ligand protein. 571319 Int. Cl. C08K 14/00; A61K 39/00 U.S. Cl. 435—69.1 17 Claims 1. An isolated parasitic nematode tropomyosin protein capable 5,843,708 of conferring protective immunity against infections of a host by a parasitic nematode species, wherein said tropomyosin protein CHIMERIC ANTIBODIES binds to antibodies raised against a protein isolated from TrichosNorman Hardman; Laura Lee Gill, both of Riehen, Switzer trongylus colubriformis, land; Ronald F.J. de Winter, Milton Ernest, England; Kath wherein said Trichostrongylus colubriformis protein has an rin Wagner, Basel, Switzerland, and Christoph Heusser, approximate molecular weight of 41 kD as determined by Bottmingen, Switzerland, assignors to CIBA-GEIGY Corpo SDS-PAGE, and comprises the amino acid sequence: ration, Tarrytown, N.Y. Division of Ser. No. 307,087, Sep. 16, 1994, which is a con Lys Lys Lys Met Gln Ala Met Lys lle tinuation of Ser. No. 947,897, Sep. 18, 1992, abandoned, Glu Lys Asp Asn Ala Leu Asp Arg Ala Asp Ala Ala Glu Glu Lys Val Arg Gln Tru Glu Lys Leu Glu Arg Val Glu Glu Glu Leu abandoned. This application Jun. 5, 1995, Ser. No. 462,371 Arg Asp Thr Gin Lys Lys Met Met Gln Thr Claims priority, application United Kingdom, Jan. 5, 1988, Glu Asn Asp Leu Asp Lys Ala Gln Glu Asp 8800077; Aug. 24, 1988, 8820099 Leu Ala Ala Ala Thr Ser Gln Leu Glu Glu Glu Val Ala Ala 21 Claims Leu U.S. Cl. 435—69.1 Asn Arg Arg Met Thr Leu Leu Glu Glu Glu Leu Glu Arg Ala Glu 1. A chimeric monoclonal antibody and derivatives thereof con Glu Arg Leu Lys lle Ala Tru Glu Lys Leu sisting of variable regions of mouse origin and human constant Glu Glu Ala Thr His Asn Val Asp Glu Ser regions, which recognize epitopes of CEA not present on non- Glu Arg Val Arg Lys Val Met Glu Asn Gly Phe Gln Asp Glu Glu Arg Ala Asn specific cross-reacting antigen NCAss and NCA9s, on biliary gly- Ser Thr Ile Glu Ala Gln Leu Lys Glu Ala Gln Met coprotein, or on granulocytes. Leu Ala Glu Glu Ala Asp Arg Lys Try Asp Glu Val Ala Arg Lys Leu Ala Met Val Glu Ala Asp Leu Glu Arg Ala Glu Glu Arg Ala Glu Ala Gly Glu Asn Lys Ile Val Glu Leu Glu Glu Glu Leu Arg Val Val Gly Asn Asn 5,843,709 Leu Lys Ser Leu Glu Val Ser Glu Glu Lys Gln lle Arg Thr Ile Ser Ser Arg Leu Lys Glu Ala Glu Thr Arg Ala. both of Germany; Norbert Schnell, Pasadena, Calif.; Johannes Augustin, Tübingen, Germany; Germar Engelke, Frankfurt am Main, Germany; Ralf Rosenstein, Reutlingen, Germany; Cortina Kaletta, München, Germany; Cora Klein, Offenbach, Germany; Bernd Wieland, Rottenburg, 5,843,711 Germany; Thomas Kupke, Tübingen, Germany; Günther DIPHTHERIA TOXIN RECEPTOR-BINDING REGION Jung, Tübingen, Germany, and Roland Kellner, Heppen- R. John Collier, Wellesley Hills, Mass.; David Eisenberg, Los heim, Germany, assignors to Dr. Karl Thomae GmbH, Ger Angeles, Calif.; Haian Fu, Allston, Mass., and Seunghyon many Choe, Reseda, Calif., assignors to The Regents of the UniverDivision of Ser. No. 392,625, Feb. 22, 1995, which is a con sity of California, Oakland, Calif., and The President and tinuation of Ser. No. 876,791, Apr. 30, 1992, abandoned, Fellows of Harvard College, Cambridge, Mass. which is a continuation of Ser. No. 784,234, Oct. 31, 1991, Continuation of Ser. No. 119,316, Sep. 9, 1993, abandoned, abandoned, which is a continuation-in-part of Ser. No. which is a continuation of Ser. No. 881,394, May 6, 1992, 353,590, May 18, 1989, abandoned. This application Jun. 6, abandoned. This application Nov. 2, 1995, Ser. No. 552,248 1995, Ser. No. 466,961 Int. Cl. C12N 15/00 Claims priority, application United Kingdom, May 18, 1988, U.S. CI. 435—69.1 15 Claims 8811761 1. A DNA encoding a polypeptide consisting of: 21 Claims b) amino acids 380–535; nucleotide sequence which codes for a gallidermin precursor, e) amino acids 383-535; wherein f) amino acids 384-535; g) amino acids 385-535; (ii) the host cell comprises an epidermin multi-enzyme com- h) amino acids 386-535; plex; and i) amino acids 496-512; (b) isolating gallidermin. j) amino acids 379-512; Page 9
(a) a nucleotide sequence encoding the polypeptide having the (c) expressing the rep coding region of said second nucleic acid amino acid sequence in FIGS. 1A-1C (SEQ ID NO: 2) from construct, thereby producing an amount of rep expression about amino acid 1 to about amino acid 374 in SEQ ID NO: 2 product under conditions such that an increased frequency of (b) a nucleotide sequence complementary to a nucleotide integration of said nucleotide sequence of said first nucleic sequence encoding the polypeptide having the amino acid acid construct into the genome of said mammalian cell is sequence in FIGS. 1A-1C (SEQ ID NO: 2) from about amino achieved. acid 1 to about amino acid 374 in SEQ ID NO: 2; (c) a nucleotide sequence which hybridizes to the nucleotide sequence in FIGS. 1A-1C (SEQ ID NO: 1) under stringent conditions; and (d) a nucleotide sequence which hybridizes to the nucleotide 5,843,743 sequence that is complementary to the nucleotide sequence in GELS FOR ENCAPSULATION OF BIOLOGICAL FIGS. 1A-1C (SEQ ID NO: 1) under stringent conditions. MATERIALS Waltham; Amarpreet S. Sawhney, Newton, both of Mass.; 5,843,740 Neil P. Desai, Los Angeles, Calif.; Jennifer L. Hill, and Syed F. A. Hossainy, both of Austin, Tex., assignors to Board of Patent Not Issued For This Number Regents, The university of Texas System, Austin, Tex. Division of Ser. No. 024,657, Mar. 1, 1993, Pat. No. 5,573,934, which is a continuation-in-part of Ser. No. 958,870, Oct. 7, 1992, Pat. No. 5,529,914, which is a continuation-in-part of 5,843,741 Ser. No. 870,540, Apr. 20, 1992, abandoned, which is a METHOD FOR ALTERING THE DIFFERENTIATION OF continuation-in-part of Ser. No. 843,485, Feb. 28, 1992, abanANCHORAGE DEPENDENT CELLS ON AN doned. This application Jun. 6, 1995, Ser. No. 467,815 ELECTRICALLY CONDUCTING POLYMER Int. Cl. A61K 9/48; BO5D 7700; C12N 11/00;11/02 Joyce Y. Wong, Cambridge; Donald E. Ingber, Boston, and U.S. CI. 435—177 22 Claims Robert S. Langer, Newton, all of Mass., assignors to Massachusetts Insitute of Technology, Cambridge, and Children's thereon formed by free radical polymerization of a biocompatible, 1. A substrate comprising a surface having a polymeric coating Medical Center Corporation, Boston, both of Mass. Filed Aug. 1, 1994, Ser. No. 283,402 water soluble macromer having covalently linked to it at least two Int. C1. C12N 13/00 free radical polymerizable substituents, U.S. Cl. 435—173.8 26 Claims wherein the coating is formed on the substrate surface by: 1. A method for altering the differentiation of anchorage depen- a) contacting the surface with a solution of a free radical dent cells comprising polymerization initiator; binding cell surface receptor-specific attachment molecules of b) applying to the surface a biocompatible, water-soluble defined types and in a defined density to a surface consisting macromer comprising at least two free radical polymerizof an electrically conducting polymer, able substituents; and attaching anchorage-dependent cells to the cell surface receptor c) exposing the surface to an agent to activate the initiator to specific attachment molecules on the electrically conducting cause the polymerization of the macromers to form the polymer surface, and applying a voltage in an effective amount to change the oxida polymeric coating on the surface. tion state of the electrically conducting polymer thereby to alter the differentiation as a function of the type and density of the attachment molecules and applied voltage, wherein the anchorage dependent cells are selected from the 5,843,744 group consisting of animal cells and plant cells. BACILLUS THURINGIENSIS TN5401 PROTEINS James A. Baum, Doylestown, Pa., assignor to Ecogen Inc., Langhorne, Pa. Continuation-in-part of Ser. No. 89,986, Jul. 8, 1993, Pat. No. 5,843,742 5,441,884. This application Jun. 24, 1994, Ser. No. 266,408 ADENO-ASSOCIATED DERIVED VECTOR SYSTEMS Int. Cl. C12N 9/00;9/16;15/00 FOR GENE DELIVERY AND INTEGRATION INTO TARGET CELLS U.S. CI. 435—183 2 Claims Georges Natsoulis, Berkeley, and Gary Kurtzman, Menlo 1. An isolated Tn5401 resolvase protein having the amino acid Park, both of Calif., assignors to Avigen Incorporated, sequence identified by amino acids 1 through 306 of SEQ ID Alameda, Calif. NO:2. Continuation-in-part of Ser. No. 357,503, Dec. 16, 1994, abandoned. This application Sep. 8, 1995, Ser. No. 525,835 Int. C1.6 C12N 15/10,5/10 U.S. Cl. 435—172.3 40 Claims 1. A method of integrating a selected nucleotide sequence into 5,843,745 the genome of a mammalian cell, comprising: PURIFIED SCYTALIDIUM LACCASES AND NUCLEIC (a) providing: ACIDS ENCODING SAME (i) a mammalian cell; Randy Michael Berka; Sheryl Ann Thompson, both of Davis, (ii) a first virion-free nucleic acid construct comprising a and Feng Xu, Woodland, all of Calif., assignors to Novo nucleotide sequence flanked by a 5' and a 3' adeno Nordisk A/S, Bagsvaerd, Denmark associated virus inverted terminal repeat; and Division of Ser. No. 253,784, Jun. 3, 1994, abandoned. This (iii) a second virion-free nucleic acid construct having a rep coding region operably linked to control elements which application Oct. 4, 1995, Ser. No. 539,134 direct the transcription and translation of the rep coding Int. C1.6 C12N 9/02;1/00 region in said mammalian cell; U.S. Cl. 435—189 5 Claims (b) introducing, in any order, said first and second virion-free 1. A purified laccase obtained from a Scytalidium strain or nucleic acid constructs into said mammalian cell; and strains which have been defined to be equivalent to Scytalidium. Page 10
SDS polyacrylamide gel electrophoresis; (b) functions optimally at 5,843,756 a pH between about 8.0 and 11.0; (c) is at least about 10 times MOUSE MTSI GENE more effective than a metalloprotease obtained from Bacillus Steven Stone, Midvale; Ping Jiang, and Alexander Kamb, both stearothermophilus in converting a proenzyme to an active trypsin- of Salt Lake City, all of Utah, assignors to Myriad Genetics, like protease obtained from a strain of F. oxysporum deposited at Inc., Salt Lake City, Utah the Deutsche Sammlung von Mikroorganismen, Gottingen, Ger- Continuation-in-part of Ser. No. 487,033, Jun. 7, 1995, Pat. many under the number DSM 2672 at a pH between about 6.0 and No. 5,739,027. This application Jul. 28, 1995, Ser. No. 508,735 7.5 at about 250-30° C. for about 30-60 minutes; and (d) is less Int. Cl. C07H 21/04; C12N 15763;1/21 effective than a metalloprotease obtained from Bacillus stearother- U.S. Cl. 435—252.3 5 Claims mophilus in cleaving the primary amino groups from casein. 1. An isolated nucleic acid comprising the sequence shown as SEQ ID NO:44. 2. A replicative cloning vector which comprises the isolated nucleic acid of claim 1. 4. Recombinant host cells transformed with the replicative clon5,843,754 ing vector of claim 2. PARTHENOGENIC BOVINE OOCYTE ACTIVATION Joan L. Susko-Parrish, Monona; David L. Northey; M. Lor raine Leibfried-Rutledge, both of Madison, and Steven L. Stice, DeForest, all of Wis., assignors to ABS Global, Inc., De Forest, Wis. 5,843,757 Division of Ser. No. 16,703, Feb. 10, 1993, Pat. No. 5,496,720. HUMAN JTV1 GENE OVERLAPS PMS2 GENE This application Jun. 6, 1995, Ser. No. 473,794 Bert Vogelstein, Baltimore; Kenneth W. Kinzler, BelAir, and Int. Cl. C12N 5700 Nicholas C. Nicolaides, Baltimore, all of Md., assignors to U.S. Cl. 435—240 19 Claims The John Hopkins University, Baltimore, Md. 1. A method for multiplying bovine embryos in vitro compris Filed Aug. 24, 1995, Ser. No. 518,862 ing: Int. C1.6 C12N 1/21 a. collecting bovine embryonic cells; U.S. Cl. 435—252.3 6 Claims b. isolating individual bovine embryonic cells; 1. A segment of cDNA consisting of the nucleotide sequence c. culturing the individual bovine embryonic cells; shown in SEQ ID NO:1. d. collecting recipient bovine oocytes from donor bovine ani mals in vitro; e. enucleating the recipient bovine oocytes: f. parthenogenically activating the recipient bovine oocytes, wherein the bovine oocytes are activated by a process com 5,843,758 ENZYME BASED BIOREMEDIATION prising the following steps in sequence: i. increasing intracellular levels of divalent cations in the Robyn Joyce Russell, Wanniassa; Richard David Newcomb, bovine oocyte; and Sutton; Geoffrey Charles de Quetteville Robin, Aranda; ii. reducing phosphorylation of cellular proteins in the bovine Thomas Mark Boyce; Peter Malcolm Campbell, both of oocyte; Cook, all of Australia; Anthony Gerard Parker, Davis, g. transferring the nucleus from the cultured bovine embryonic Calif.; John Graham Oakeshott, Wanniassa, and Kerriecell to an enucleated recipient parthenogenically-activated Ann Smyth, Cook, both of Australia, assignors to The Combovine oocyte to form a nuclear transferred oocyte; and monwealth of Australia Commonwealth Scientific and h. forming a single cell bovine embryo from the nuclear trans Industrial Research Organization, Campbell, Australia ferred bovine oocyte. PCT No. PCT/AU95/00016, § 371 Date Oct. 7, 1996, § 102(e) Date Oct. 7, 1996, PCT Pub. No. W095/19440, PCT Pub. Date Jul. 20, 1995 PCT Filed Jan. 13, 1995, Ser. No. 669,524 Claims priority, application Australia, Jan. 13, 1994, PM 5,843,755 3347 GROUP OF ANTITUMOR COMPOUNDS AND METHOD Int. Cl. C12N 1/20;9/16;12/00; B09B 3/00 17 Claims Yoko Obayashi; Toshihiko Yoshimura; Yuka Ikenoue; Ryosuke 1. An isolated and purified organophosphate (OP)-resistant E3 Fudo; Masahiro Murata, and Toshihiko Ando, all of esterase having the amino acid sequence shown in SEQ ID NO: 4 Kawasaki, Japan, assignors to Ajinomoto Co., Inc., Tokyo, or an ortholog thereof, wherein said OP-resistant E3 esterase has a Japan substitution of the amino acid corresponding to the glycine residue PCT No. PCT/JP97/00827, § 371 Date Jun. 10, 1997, § 102(e) at position 137 of the OP-sensitive E3 esterase from Lucilia Date Jun. 10, 1997, PCT Pub. No. W097/44479, PCT Pub. cuprina having the amino acid sequence of SEQ ID NO: 3. Date Nov. 27, 1997 PCT Filed Mar. 14, 1997, Ser. No. 849,220 Claims priority, application Japan, May 20, 1996, 8-124530 Int. Cl. C12N 1/14;1/15; A61K 31/095;31/12 U.S. CI. 435—243 5,843,759 10 Claims HUMAN RAD50 GENE AND METHODS OF USE 1. A compound represented by the following structural formula: THEREOF Gregory Dolganov, San Carlos, and Alexander Novikov, Foster City, both of Calif., assignors to Genelabs Technologies, Inc., application Jul. 17, 1996, Ser. No. 687,080 H Int. C1.6 C07H 21/04; C12N 1/21;15763 N N U.S. Cl. 435—252.3 12 Claims H 4. A protein expression vector containing, as a heterologous gene under the control of suitable control elements, a polynucleS S otide sequence that encodes (i) an hR50 protein encoded by nucleotides 389 to 4324 in SEQ ID NO:44 or (ii) an hRAD50 protein having the sequence identified by SEQ ID NO:47. Page 11
5,843,794 2 TECHNIQUE FOR THE PREVENTION OF FALSE POSITIVE REACTIONS IN IMMUNOLOGICAL TESTING DUE TO CAND C1Q COMPONENTS OF THE COMPLEMENT AND METHOD FOR SCREENING FOR -22 16a N+ RHEUMATIC FACTOR 18a 42 Jacques Singer, Delray Beach, Fla., assignor to Montefiore P-well 42b Medical Center, Bronx, N.Y. Implanted P+ Continuation of Ser. No. 14,549, Feb. 8, 1993, abandoned, which is a continuation-in-part of Ser. No. 857,764, Mar. 26, N+ buffer layer 1992, abandoned. This application Nov. 29, 1995, Ser. No. 14 564,895 -12 Int. C1.6 GOIN 33/546 P+ Substrate U.S. Cl. 436-534 12 Claims -32 Anode SERA + UNCOATED LATEX forming the second well by ion implanting a first dopant, of said one conductivity type into an inner surface area of the first NO CURVE well exposed within said inner periphery of said polycrystalline silicon layer, the said ion implanting being done at a first energy at which said first dopant does not penetrate said polycrystalline silicon layer, whereby said second well is self-aligned with said inner periphery of said polycrystalline silicon layer, said second well having a bottom; completing formation of the second well by activating said first dopant without noticeably diffusing said first dopant vertically NO CURVE or horizontally, whereby said second well has an outer periphery that remains registered with said inner periphery of said polycrystalline silicon layer; NEW ALIQUOT HEAT 56°C 30 MIN + SALT forming a subsurface plate-like area of said opposite conductiv ity type having a higher dopant concentration than said first well in said first well below said bottom of said second well by ion implanting a second dopant of said opposite conducNO CURVE CURVE NEW ALIQUOT + SALT + HEAT 63°C -3 MIN NO DETECTABLE tivity type into said inner surface area exposed within said CIQ OR RF inner periphery of said polycrystalline silicon layer, said ion NO CURVE CURVE implanting of said second dopant being done at a second RF NEGATIVE RF POSITIVE energy which is higher than said first energy but at which said (CIQ BY INFERENCE) 1. A method for preventing interference caused by C or Cl, in second dopant does not penetrate said polycrystalline silicon an immunoassay of a body fluid for an antigen or an antibody, said layer, whereby said plate-like area in said first well is selfmethod comprising heating a sample of said body fluid, which is aligned with said inner periphery of said polycrystalline silidiluted sufficiently to permit an immunoassay, to a temperature of con layer and said outer periphery of said second well; 59° C. to 64° C. with a neutral salt for a period of time sufficient completing formation of the plate-like area by activating said for said neutral salt to prevent said interference caused by said C second dopant without noticeably diffusing said second or Cıq without affecting said antigen or said antibody in said dopant vertically or horizontally, whereby said second well immunoassay. remains substantially registered with said inner periphery of said polycrystalline silicon layer and said outer periphery of said second well; etching through a central area of said second well into said plate-like area, effective to form a surface recess; 5,843,795 implanting a third dopant of said opposite conductivity type into said surface recess at an energy at which said third dopant is Patent Not Issued For This Number targeted to lodge at said surface recess in said first well, and activating the third dopant without noticeably diffusing said third dopant of vertically or horizontally, effective to increase punch through voltage of said first well; and forming an electrode in said surface recess that is in electrical 5,843,796 contact with each of said second well and said plate-like area METHOD OF MAKING AN INSULATED GATE BIPOLAR in said first well. TRANSISTOR WITH HIGH-ENERGY P+ IMPLANT AND SILICON-ETCH CONTACT Donald Ray Disney, Kokomo, Ind., assignor to Delco Electron- ics Corporation, Kokomo, Id. Filed Sep. 11, 1995, Ser. No. 526,427 5,843,797 METHOD OF REDUCING OFFSET FOR IONU.S. Cl. 4376 2 Claims IMPLANTATION IN SEMICONDUCTOR DEVICES 1. In a method of making an insulated gate switching transistor Makoto Iuchi, Tokyo, Japan, assignor to NEC Corporation, having a layer of one conductivity type, with a surface, a first well Tokyo, Japan of opposite conductivity type to said one conductivity type in said Filed Mar. 18, 1996, Ser. No. 617,112 surface, an annular second well of said one conductivity type Claims priority, application Japan, Mar. 17, 1995, 7-057851 disposed in said surface concentrically within said first well, and Int. Cl.O HO1L 21/266 an insulated gate electrode disposed on a generally annular periph- U.S. Cl. 437–45 7 Claims eral surface portion of said first well, said insulated gate electrode 1. A method for manufacturing on a wafer a plurality of semihaving a polycrystalline silicon layer with an inner periphery that conductor devices having a common designed structure, said is used for self-aligned formation of said first well, the improve- method comprising the steps of: ment comprising: grouping the semiconductor devices in a plurality of groups providing said polycrystalline silicon layer with a thickness that including a first group and a second group, each group includwill mask ion implants of dopants; ing at least one semiconductor device, Page 12
providing a polyimide with a pre-laminated thin copper layer on encapsulating said die, said internal lead frame and said each of two sides thereof as a substrate; thermally conductive internal element to form a protective laminating, exposing and developing a plurality of first dry film casing, such that a plurality of said circuit conductors layers on both surfaces of said polyimide substrate, while extend through a first end of said casing to form leads and defining a plurality of predetermined openings in an upper wherein an end portion of said thermally conductive intersurface of said polyimide substrate; nal element extends through a second end of said casing, sequentially applying a multi-layer electroplating operation of opposite said first end; electro-coppering, electronickelling, gold plating and elec- mounting a thin, warp-resistant metal layer to a first major tronickelling again on the exposed surface of the upper first surface of said casing; dry film layer; mounting a substantially planar external thermally conductive forming a plurality of electroplated multi-layer protrusions after element to a second major surface of said casing; and removing said first dry film layers; vertically orienting a plurality of said packages and mounting laminating, etching and developing a plurality of second dry film said packages adjacent one another to form an ultra-high layers on two surfaces of a laminate, while defining predeter- density memory module. mined openings on a lower surface of said laminate; serving said second dry film layers as a mask for etching the bottom thin copper layer on a lower side of said laminate; serving said bottom thin copper layer on the lower side as a 5,843,808 mask for applying a laser etching operation to said polyimide STRUCTURE AND METHOD FOR AUTOMATED substrate to form a pattern of holes without totally penetrating ASSEMBLY OF A TAB GRID ARRAY PACKAGE said polyimide substrate by the control of laser energy; laminating a third dry film layer on the upper surface of the Marcos Karnezos, Menlo Park, Calif., assignor to ASAT, Limlaminate for protecting the pattern previously formed; ited, Tsuen Wan, Hong Kong applying an electrolytic plating operation to each hole in said Filed Jan. 11, 1996, Ser. No. 585,134 Int. CI. HO1L 21/44 polyimide substrate for forming electrolytic contacts by filling 9 Claims each hole with an electrolyte and the outer surface thereof U.S. Cl. 438—121 being in a protruding form; removing said third dry film layer; etching the exposed top thin copper layer between said electro plated multi-layer protrusions to separate the adjacent electroplated layers from each other, and removing a nickel 5 F7 electroplated layer on the top of the multi-layer electroplated 75 layer by etching to expose a gold plated layer; and TOP respectively defining a chip installation hole and a plurality of through holes in a central position and other predetermined 1. A method for forming a TGA package, comprising the steps positions on the two sides of the polyimide substrate by of: performing a laser drilling operation for defining a structure forming a plurality of stiffeners on a carrier strip, each stiffener for mounting a chip between the two electroplated multi-layer having a cavity formed on one side of said strip; protrusions beside the chip installation hole. singulating a plurality of tape frames from a tape, each tape frame including (i) a first plurality of conductive wire bonding pads, (ii) a plurality of solder ball bonding pads for attaching solder balls and (iii) a plurality of conductive traces each for 5,843,807 routing a signal from one of said first plurality of wire METHOD OF MANUFACTURING AN ULTRA-HIGH bonding pads to a corresponding solder ball bonding pad; DENSITY WARP-RESISTANT MEMORY MODULE attaching each of said tape frame to one of said plurality of Carmen D. Burns, Austin, Tex., assignor to Staktek Corpora stiffeners via a tape adhesive; tion, Austin, Tex. attaching a plurality of solder balls to said tape at said plurality Division of Ser. No. 473,593, Jun. 7, 1995, Pat. No. 5,644,161, of conductive bond pads using a reflow procedure; which is a continuation-in-part of Ser. No. 280,968, Jul. 27, attaching a semiconductor die to said cavity of said stiffener 1994, Pat. No. 5,581,121, which is a division of Ser. No. using a die attach epoxy, said semiconductor die having 37,830, Mar. 29, 1993, Pat. No. 5,369,056. This application formed thereon a second plurality of wire bonding pads; Jul. 25, 1996, Ser. No. 686,985 using a plurality of bond wires, coupling selected ones of said Int. Cl. HOLL 21/58,31/024 second plurality of wire bonding pads on said semiconductor U.S. Cl. 438—109 14 Claims die to corresponding ones of said first plurality of wire bond ing pads; -20 encapsulating said semiconductor die and said bond wires with a resin encapsulation; and singulating each of said stiffeners from said carrier strip.
44 26 -32 50 24 5,843,809 LEAD FRAMES FOR TRENCH DRAMS 35 38 Michael D. Rostoker, Boulder Creek, Calif., assignor to LSI 1. A method of manufacturing an ultra-high density memory Logic Corporation, Milpitas, Calif. module, comprising the steps of: Filed Jan. 24, 1996, Ser. No. 590,527 forming a high density memory package by: Int. Cl. HO1L 21/60 mounting a substantially planar internal lead frame, com- U.S. Cl. 438—123 10 Claims prised of a plurality of circuit conductors, to an integrated 1. A method of packaging a trench-type DRAM integrated circuit die so said lead frame overlays and is in thermal circuit die having a plurality of trench capacitors and a plurality of contact with at least a portion of said die; input and output pads aligned generally along a single line, a mounting a substantially planar thermally conductive internal method comprising the following steps: element so it overlays and is in thermal contact with at least providing a DIP lead frame having two halves aligned in parallel a portion of said die; with and on opposite sides of said line of input and output Page 13
5,843,816 INTEGRATED SELF-ALIGNED BUTT CONTACT PROCESS FLOW AND STRUCTURE FOR SLX TRANSISTOR FULL COMPLEMENTARY METAL OXIDE SEMICONDUCTOR STATIC RANDOM ACCESS MEMORY CELL Jhon-Jhy Liaw, Taipei, and Jin-Yuan Lee, Hsin-Chu, both of 24FOX FOX Taiwan, assignors to Taiwan Semiconductor Manufacturing Company, Ltd., Hsin-Chu, Taiwan Filed Jul. 28, 1997, Ser. No. 901,646 Int. Cl.“ HO1L 21/8244 6 3 4 5 9 (N+) 8 9(N+) 13(P) 7(N) U.S. Cl. 438238 18 Claims 42 42 42. PL1(ILD38 PL238/ILD PL3 38 (ILD PL 4 depositing a first metal silicide layer on said first polysilicon layer; 40 depositing a first insulator layer on said first metal silicide layer; 40 -38 38patterning of said first insulator layer, of said first metal silicide OX3 layer, and of said first polysilicon layer, to form polycide gate G3 structures, on said gate insulator layer; -350 ion implanting a first conductivity imparting dopant into said semiconductor substrate, in regions not covered by said poly P 31 cide gate structures, to form a lightly doped source and drain region; 32 35B 32 33A38 350 32 30 depositing a second insulator layer; G2 anisotropic etching of said second insulator layer to form insu 1. A method of forming a contact between a conductor and a lator spacers on the sides of said polycide gate structures; substrate region in a MOSFET device comprising: ion implanting a second conductivity imparting dopant into said forming a semiconductor substrate with a silicon oxide layer semiconductor substrate, in regions not covered by said poly- formed on the surface thereof, cide gate structures, or not covered by said insulator spacers, forming a stack of a conductor material upon the surface of the · to form a heavily doped source and drain region; silicon oxide layer and forming a first dielectric layer upon the conductor material, depositing a third insulator layer; patterning the conductor stack into conductors, opening a hole in said third insulator layer, creating a self forming a butted contact pattern in the first dielectric layer by aligned contact, (SAC), opening, exposing said heavily doped removal of the dielectric layer in at least one butted contact source and drain region, in said semiconductor substrate, in region, the space between said polycide gate structures, with said forming doped regions in the substrate self-aligned with the insulator spacers; conductors, ion implanting a third conductivity imparting dopant into said forming a second dielectric layer over the device and patterning SAC opening, to create said SAC halo implant region, in said the second dielectric layer with contact openings therethrough semiconductor substrate, in space between said polycide down to the substrate and to the butted contact region, structures; forming contacts to the substrate and the butted contact regions depositing a second polysilicon layer, including deposition on on the conductor through the contact openings. said heavily doped source and drain region, and on said SAC halo implant region, in said SAC opening, in space between said polycide gate structures; depositing a second metal silicide layer on said second polysili 5,843,817 con layer; PROCESS FOR INTEGRATING STACKED CAPACITOR patterning of said second metal silicide layer, and of said second DRAM DEVICES WITH MOSFET DEVICES USED FOR polysilicon layer, to create a polycide, self- aligned contact, HIGH PERFORMANCE LOGIC CIRCUITS (SAC), structure, completely overlying said SAC opening, Jin-Yuan Lee, and Mong-Song Liang, both of Hsin-Chu, Taiand with said polycide SAC structure partially overlying a wan, assignors to Taiwan Semiconductor Manufacturing Company, Ltd., Hsin-Chu, Taiwan portion of said polysilicon gate structures, in regions where Filed Sep. 19, 1997, Ser. No. 933,371 said polycide gate structures are adjacent to said SAC open Int. CI. HO1L 21/8242 ing; U.S. Cl. 438239 20 Claims depositing a fourth insulator layer; 1 2 depositing a third polysilicon layer; patterning of said third polysilicon layer to create polysilicon load resistors; 24 21 0 20 16 17 depositing a composite interlevel dielectric layer on said semi 14 conductor substrate, including deposition on said polycide 21b 24 SAC structure, and on said polysilicon load resistors; annealing of said composite interlevel dielectric layer; opening contact holes in said composite interlevel dielectric FOX FOX layer, and in said fourth insulator layer, to expose top surface of said polycide SAC structure, and top surface of said polysilicon load resistors; and 11 5 6 13(N+) 20 25 (N+) forming an interconnect metallization structures, overlying and 10(N) 23(N) contacting, said polycide SAC structure, and said polysilicon 1. A method for fabricating a memory device, and a logic device, load resistors, in said contact holes, in said composite inter- on the same single semiconductor chip, using an integrated fabrilevel dielectric layer. cation process, comprising the steps of: Page 14
photolithographic processing to create a second photoresist 5,843,841 shape, on said first metal interconnect layer, directly overlying FABRICATION PROCESS OF A SEMICONDUCTOR said raised metal plug structure; INTEGRATED CIRCUIT DEVICE HAVING A LOCAL anisotropic etching of said first metal interconnect layer, to form INTERCONNECT PATTERN AND A SEMICONDUCTOR a first level interconnect metallization structure, directly over- INTEGRATED CIRCUIT DEVICE FABRICATED lying said raised metal plug structure; ACCORDING TO SUCH A FABRICATION PROCESS removal of said second photoresist shape; Tetsuo Izawa; Hiroshi Goto, and Koichi Hashimoto, all of deposition of a first interlevel dielectric layer on said first level Kawasaki, Japan, assignors to Fujitsu Limited, Kawasaki, interconnect metallization structure, on exposed sidewalls of Japan underlying said raised metal plug structures and on said Division of Ser. No. 394,347, Feb. 23, 1995. This application insulator layer, not covered by said raised metal plug struc Jun. 10, 1996, Ser. No. 661,011 ture; Claims priority, application Japan, Feb. 25, 1994, 6-027146; application of a spin on glass layer, on said underlying first Aug. 4, 1994, 6-183159; Dec. 14, 1994, 6-311020 interlevel dielectric layer, partially filling the spaces between Int. Cl.HOL 21/441 said first level interconnect metallization structures, and U.S. Cl. 438—666 5 Claims between said raised metal plug structures; bake out of said spin on glass layer; IIIC curing of said spin on glass layer; IIIC IIIC deposition of a second interlevel dielectric layer, on said spin on Head glass layer, completely filling spaces between said first level interconnect metallization structures, and between said raised metal plug structures; IIIB chemical mechanical polishing to expose top surface of said first level interconnect metallization structure, and planarizing top 30 surface of said first interlevel dielectric layer, top surface of said spin on glass layer, and top surface of said second IIIA interlevel dielectric layer; deposition of a second metal interconnect layer on exposed top 1. A method for fabricating a semiconductor integrated circuit surface of said first level interconnect metallization structure, device, comprising the steps of: on top surface of said first interlevel dielectric layer, on top (a) forming a conductor film on a substrate; surface of said spin on glass layer, and on top surface of said (b) forming an insulator film on said conductor film to form a second interlevel dielectric layer; and layered structure including said conductor film and said insupatterning of said second metal interconnect layer, to form lator film on said substrate; second level interconnect metallization structure, contacting (c) removing said insulator film selectively from a first part underlying, said first level interconnect metallization struc thereof corresponding to a first conductor pattern to be ture. formed, while leaving said insulator film on a second part thereof corresponding to a second conductor pattern to be formed; (d) patterning said layered structure to form said conductor 5,843,840 patterns; SEMICONDUCTOR DEVICE HAVING A WIRING LAYER (e) providing a side wall insulator to each of side walls of said AND METHOD FOR MANUFACTURING SAME conductor patterns; Kazuki Miyazaki; Kazunobu Shigehara, and Masanobu Zenke, (f) providing a first local interconnect pattern on said first part to all of Tokyo, Japan, assignors to NEC Corporation, Tokyo, establish an electrical connection with said first conductor Japan pattern at said first part; and Filed Mar. 4, 1996, Ser. No. 610,349 (g) providing a second local interconnect pattern on said second Claims priority, application Japan, Mar. 3, 1995, 7-044613 part across said second conductor pattern at said second part, Int. Cl. HOIL 21/28 without establishing electrical connection therewith. U.S. Cl. 438-659 4 Claims
4 TUNGSTEN FILM 3 ADHESION LAYER 2 SILICON OXIDE
4 TUNGSTEN FILM 3 ADHESION LAYER 2 SILICON OXIDE
5,843,842 PRODUCING SILICON PRECIPITATES Koyang-gun, all of Rep. of Korea, assignors to Samsung 5,355,020. This application Sep. 3, 1996, Ser. No. 697,880 Claims priority, application Rep. of Korea, Jul. 8, 1991, 1991 11543 Int. Cl.“ HO1L 21/441 U.S. Cl. 438—688 31 Claims tor substrate: forming an opening in said insulating layer, said opening expos ing a portion of said major surface of said semiconductor substrate; forming a first metal layer on an inner surface of said opening, on said insulating layer, and on said exposed portion of said
1. A method for forming a semiconductor device having a wiring conductor formed of tungsten, the method including the steps of forming a tungsten film by a low pressure chemical vapor deposition, injecting ions into said tungsten film, and patterning said ion-injected tungsten film so as to form a wiring conductor composed of said ion-injected tungsten film. Page 15
5,843,858 a green body moulded from a finely dispersed powder mixture OXYGEN SENSORS MADE OF ALKALINE-EARTH of aluminum, Al2O3, and a material containing Si. DOPED LANTHANUM FERRITES Karl-Heinz Hardtl, Hagenbach; Ulrich Schonauer, Karlsruhe, and Andreas Krug, Igersheim, all of Germany, assignors to Roth-Technik GmbH & Co. Forschung Fur-Automobil-Und Umwelttechnik, Gaggenau, Germany 5,843,860 PCT No. PCT/EP95/01755, $ 371 Date Mar. 3, 1997, § 102(e) CERAMIC COMPOSITION FOR HIGH-FREQUENCY Date Mar. 3, 1997, PCT Pub. No. W095/32418, PCT Pub. Ho-Gi Kim, and Yung Park, both of Seoul, Rep. of Korea, DIELECTRICS Date Nov. 30, 1995 PCT Filed May 9, 1995, Ser. No. 737,623 assignors to Korea Advanced Institute of Science and TechClaims priority, application Germany, May 24, 1994, 44 18 nology, Taejon, Rep. of Korea 054.3 Filed Aug. 13, 1997, Ser. No. 911,466 Claims priority, application Rep. of Korea, Aug. 13, 1996, U.S. Cl. 501—126 1 Claim 96-33523 Int. Cl. L04B 35/49 U.S. Cl. 501-134 19 Claims 1. A ceramic composition for high-frequency dielectrics which 2.0 La0,75Sr0,25Fe03 comprises ZrO2, SnO2 and TiO2 in the following molar ratio: 1.5 1.0 (ZrO2)--(SnO2),(TiO2) 1+y 0.5 wherein. log (o/Scm-1) 0.0 O T = 1000°C - T = 950°C 0.1MSX $0.4M and OM&y=0.1M, -0.5 T= 900°C T = 850°C -1.0 and a sintering aid component consisting essentially of 1% or T = 800°C less of Mn(NO3)2.4H2O by total weight of MnO. -1.5 12. A process for preparing a ceramic composition for high-20 -15 -10 -5 0 frequency dielectrics, the process comprising: log (pO2/ bar) adding ZrO2, SnO2 and TiO2 in the following molar ratio: 1. Method for producing an oxygen sensor measuring resistance (Z02)-(SnO2),(TiO2)1+y as a function of oxygen partial pressure, made of alkaline-earthdoped perovskitic lanthanum ferrites with the general formula wherein, 0.1Mex$0.4M and OM&y=0.1M; melting and grinding the mixture at 1900° C. or above; and La - Me, FeO3-8 adding a sintering aid component consisting essentially of 1% or less of Mn(NO3)2.4H20 by total weight of Mno. where Me is one of the alkaline earth metals, Mg, Ca, Sr, and Ba, x is the degree of doping, the oxygen deficit of anion 8=0 to 0.25, and the degree of doping of the lanthanum ferrites is x=0.1 to 0.3 and is selected to provide a temperature independent resistance property to the oxygen sensor in a lean range comprising the steps 5,843,861 of applying said alkaline-earth-doped perovskitic lanthanum fer- PROCESS FOR THE SYNTHESIS OF KAOLIN CLAYS rites, using thick film technology to a carrier and stoving or HAVING VARYING MORPHOLOGICAL PROPERTIES tempering; or stoving and tempering said alkaline-earth-doped Prakash B. Malla, Dublin, Ga., assignor to Thiele Kaolin Comperovskitic lanthanum ferrites applied to said carrier material, pany, Sandersville, Ga. wherein said carrier is a non-metal oxide substrate, and said Filed Dec. 23, 1996, Ser. No. 779,964 stoving step comprises drying said thick film on said substrate Int. Cl. C04B 14/04;33/04; C09C 1/42 holding for 15 minutes at 120° C., increasing a stoving temperature U.S. CI. 501-146 18 Claims at 20K/min to 350° C. and holding for 10 minutes at 350° C.; 1. A process for the synthesis of a crystalline kaolin clay, increasing said stoving temperature at 20K/min to 1200° C. and wherein the process comprises the sequential steps of: holding for 25 minutes at 1200° C., and cooling at 20K/min to (a) placing a amorphous calcined kaolin clay into a vessel which ambient temperature. contains an acidic media; (b) mixing the contents of the vessel at a temperature within the range of about 150° to about 350° C., for a time period of about 1 to about 20 days, to obtain a homogeneous slurry having a solids content of about 1 to about 50 percent by 5,843,859 weight; and REACTION-FORMED MOULDED CERAMIC BODY (c) cooling the slurry. CONTAINING MULLITE, ITS PRODUCTION AND ITS USE Nils Claussen, Auf den Schwarzen Bergen 15, W-2107 Rosen- garten, Germany 5,843,862 Date Nov. 25, 1992, PCT Pub. No. W091/18846, PCT Pub. PROCESS FOR MANUFACTURING AN ABSORBENT Date Dec. 12, 1991 COMPOSITION PCT Filed May 28, 1991, Ser. No. 108,563 Alakananda Bhattacharyya, Wheaton, Ill., assignor to Amoco Claims priority, application Germany, May 29, 1990, 40 17 Corporation, Chicago, Ill. 262.7; Dec. 11, 1990, 40 39 530.8 Continuation-in-part of Ser. No. 488,872, Jun. 9, 1995, Pat. Int. Cl. C04B 35/185;35/65 No. 5,591,418, which is a division of Ser. No. 252,175, Jun. 1, U.S. Cl. 501-128 1994, Pat. No. 5,426,083. This application Oct. 25, 1996, Ser. 1. Reaction-formed molded ceramic body having a mullite No. 736,949 matrix that is virtually free of intergranular phases, comprising Int. Cl. B01J 20/10:20/00 (a) from 20–100 vol. % mullite and from 0 to 80 vol. % of at U.S. Cl. 502—411 13 Claims least one oxide selected from the group consisting of A1,03, 1. A process for manufacturing a composition which comprises: ZrOz, zircon, cordierite and MgAl2O4, wherein said mullite is blending water; about two molar parts of a divalent metal formed by heat treating, in an oxygen containing atmosphere, compound which is not a salt and includes a divalent metal Page 16
selected from the group consisting of magnesium, calcium, zinc, strontium and barium; and about one molar part in sum of an aluminum compound which is not a salt and a trivalent metal compound which is not a salt and includes a trivalent metal selected from the group consisting of cerium, lanthanum, iron, chromium, vanadium, and cobalt; and about onehalf to about one molar part of a water soluble interstitial anion precursor to produce a mixture; heating the mixture to a temperature in the range of about 50° to about 100° C. for at least about one hour; recovering from the mixture an anionic layered mixed hydrox
calcining the recovered layered mixed hydroxide for not less than about one hour at a temperature of about 450° C. or hotter, to produce a dehydrated material which is essentially devoid of interstitial anions; mixing the dehydrated material with an aqueous solution includ ing about 0.01 to less than two molar parts of a metalate salt containing vanadate, tungstenate, or molybdate anions to produce a slurry, the solution also including an amount of an alkalinity control agent appropriate to stabilize the vanadate, tungstenate, or molybdate anions in monometalate, dimete late, trimetalate or tetrametalate form; and recovering solids from the slurry and calcining the solids to produce an at least partially collapsed composition suitable for use as a sulfur oxide absorbent which is substantially composed of solid solution microcrystallites having aluminum oxide dispersed in an oxide of the divalent metal and of spinel base microcrystallites, each of the microcrystallites having the greatest linear dimension in the range of about 0.1 to about 30 nanometers.
providing a thermally imageable document having a base sheet, a thermal imaging layer and an overlying protective top coating resistant to the intrusion of moisture and solvents thereby protecting the thermal imaging layer from moisture and solvents, and applying a non-blocking coating receptive to alcohols, glycols and water on a zone of said top coating to provide a Bekk smoothness of at least 50 seconds in the zone of the receptive coating, an optical image density of at least 1.00, when imaged, in the zone of the receptive coating, said receptive coating being absorptive of moisture and solvents such that an ink stamp image applied to said receptive coating from an ink stamp pad will dry to a smudge-resistant state within no more than about thirty seconds of its application to the receptive coating.
5,843,863 PROCESS FOR IMPROVING FLOW CHARACTERISTICS 5,843,865 OF CRYSTALLINE IBUPROFEN SYNERGISTIC ANTIMICROBIAL COMPOSITIONS CONTAINING AN IONENE POLYMER AND A SALT OF Lloyd E. Goddard, Orangeburg, and George A. Knesel, DODECYLAMINE AND METHODS OF USING THE Columbia, both of S.C., assignors to Albemarle Corporation, Richmond, Va. SAME Continuation of Ser. No. 963,939, Oct. 20, 1992, abandoned, Fernando Del Corral, Memphis; Percy Jaquess, Tigrett, and which is a continuation of Ser. No. 734,910, Jul. 24, 1991, David Oppong, Memphis, all of Tenn., assignors to Buckman abandoned, which is a continuation-in-part of Ser. No. Laboratories International, Inc., Memphis, Tenn. 615,348, Nov. 19, 1990, abandoned. This application Sep. 3, Filed Feb. 6, 1997, Ser. No. 796,575 1993, Ser. No. 115,836 Int. Cl. A01N 33/00;33/02;33/08; A61K 31/74 34 Claims U.S. Cl. 562-493 2 Claims 1. A composition comprising (a) an ionene polymer and (b) a 1. A process for preparing crystalline ibuprofen having a crystal salt of dodecylamine, wherein components (a) and (b) are present habit characterized by having a particle length larger than 150 in a synergistically microbicidally effective combined amount to microns average and a length to width aspect ratio of from about 4 control the growth of at least one microorganism, wherein the to 1 to about 5 to 1 comprising ionene polymer comprises the repeating unit of formula I: (a) forming a saturated solution of ibuprofen in a liquid hydro carbon solvent at a temperature from about 20° C. to about 60° C.; R1 R3 (b) seeding said saturated solution with solid ibuprofen; 1 . (c) cooling said saturated solution to a temperature of about 0° -A-N+-B-N+. | | C. to about —20° C. at a rate to retard primary nucleation and R2 R4 promote secondary nucleation to obtain a slurry; and (d) separating the crystalline ibuprofen from the liquid phase of wherein the slurry R', R?, R3, and R4 are identical or different, and are selected from hydrogen, C.-C20 alkyl optionally substituted with at least one hydroxyl group, or benzyl optionally substituted on the benzene moiety with at least one C-C20 alkyl group; A is a divalent radical selected from C, C10 alkylene, C2-C10 5,843,864 alkenylene, C2-C10 alkynylene, C7-C10 hydroxyalkylene, NON-SMUDGING THERMALLY IMAGEABLE symmetric or asymmetric di-C, -C10-alkylenether, arylene, DOCUMENTS, METHOD OF MAKING SAME AND arylene-C,-C10-alkylene, or C.-C10-alkylenearyl-C, C10 SYSTEM FOR REDUCING THE SMUDGING OF INK alkylene; STAMP PAD IMAGES APPLIED TO SUCH DOCUMENTS B is a divalent radical selected from C, C10 alkylene, C2-C10 Mark R. Popp, Mount Juliet, Tenn., and Ora W. Jones, Hud alkenylene, C2-C10 alkynylene, C7-C10 hydroxyalkylene, son, Fla., assignors to DocuSystems, Inc., Morton Grove, Il. arylene, arylene-C,-C10-alkylene, or C-C10-alkylenearylFiled Feb. 24, 1997, Ser. No. 806,539 Ci-C10-alkylene; and X2- is a divalent counter ion, two monovalent counter ions, or a U.S. Cl. 503—201 21 Claims fraction of a polyvalent counter ion sufficient to balance the 1. A method of making a thermally imageable document which cationic charge in the repeating unit which forms the ionene resists smudging of stamp ink images, comprising the steps of polymer backbone. Page 17
5,843,888 conformational change in the ICAM-1 molecule, and the blocking LOW OXYGEN AFFINITY MUTANT HEMOGLOBIN peptide, when bound to the ICAM-1 molecule, inhibits the binding Chien Ho; Hyun-Won Kim, and Tong-Jian Shen, all of Pittsof the ICAM-1 molecule to a human LFA-1 molecule, burgh, Pa., assignors to Carnegie Mellon University, Pittswherein the modulator peptide comprises an amino acid burgh, Pa. sequence included in the amino acid sequence of the extracel Filed May 1, 1995, Ser. No. 432,071 lular segment of the LFA-1 molecule and has a molecular Int. Cl. C07K 14/805; C07H 21/06 weight under 20 kilodaltons, U.S. Cl. 514-6 15 Claims wherein the modulator peptide is prepared by a method compris- 1. A non-naturally occurring mutant human hemoglobin wherein ing the steps of: the valine residue at position 96 of the a chain (SEQ ID NO: 1) is (a) identifying a protein domain of the LFA-1 molecule replaced by a tryptophan residue. wherein the protein domain is capable of binding to the ICAM-1 molecule; and (b) synthesizing the modulator peptide comprising an amino acid sequence included in the protein domain, wherein, in the binding assay of Example 2, the fluorescence 5,843,889 GLYCOPEPTIDE ANTIBIOTIC DERIVATIVES intensity value calculated using a first sample lacking the modulator peptide is at least 10% lower than the fluores- Robin D. G. Cooper, Indianapolis; Bret E. Huff, Mooresville; cence intensity value calculated using a second sample Thalia I. Nicas, Indianapolis; John T. Quatroche, Indianapoincluding the modulator peptide. lis; Michael J. Rodriguez, Indianapolis; Nancy J. Snyder, Lilly and Company, Indianapolis, Ind. 5,843,886 Division of Ser. No. 356,413, Dec. 15, 1994, abandoned, which METHOD OF TREATING OR PREVENTING TYPE 1 is a continuation-in-part of Ser. No. 189,393, Jan. 28, 1994, DIABETES BY ORAL ADMINISTRATION OF INSULIN abandoned. This application Mar. 12, 1997, Ser. No. 816,224 Howard L. Weiner, Brookline; George Eisenbarth, Wellesley; Int. Cl. C07K 7750;9/00; A61K 37/02 David Allen Hafler, West Newton, and Zhengi Zhang, U.S. Cl. 5148 9 Claims Walden, all of Mass., assignors to Autoimmune, Inc., Lexing- 1. A compound of the formula: ton, Mass. Continuation of Ser. No. 235,121, Apr. 28, 1994, abandoned, HO OH which is a continuation of Ser. No. 70,020, May 28, 1993, abandoned, which is a continuation of Ser. No. 896,484, Jun. R7-R6-0 2, 1992, abandoned, which is a continuation of Ser. No. CH OH 595,468, Oct. 10, 1990, abandoned. This application Jun. 2, O 1995, Ser. No. 461,588 CI Int. Cl. A61K 38/28 U.S. Cl. 514-3 32 Claims OH 1. A method for suppressing an autoimmune response against H СІ pancreatic beta cells in a mammal in need of suppression of said H Н NH 0 OH autoimmune response, comprising nasally or by mouth administer HO HH, NH NHCH ing to said mammal an effective amount of a composition compris H UN N ing insulin or a fragment of insulin having the property of sup HN Ο Η H pressing said autoimmune response, wherein said composition is N H Ο Η H CH2 CH effective to suppress said autoimmune response without causing a CH2 CH decrease in the blood sugar level of said mammal within four hours O C-NH2 after said administration. OH CH3 OH OH
or salt thereof, wherein: R is vancosaminyl; and of R ;
5,843,887 AND METHODS Persan, both of France, by Jacqueline Bourland, legal rep- resentative, assignors to Allied Medical Research Associates, Washington, D.C. Continuation of Ser. No. 412,347, Mar. 31, 1995, abandoned. This application Oct. 16, 1997, Ser. No. 951,308 Claims priority, application France, Sep. 1, 1994, 94 10673 Int. Cl. A61K 38/28;38/00, CO7K 5/00;1/00 U.S. Cl. 5143 6 Claims 1. A method of delivering an insulin-containing composition to the circulation system of a host in need of insulin comprising: administering orally to said host a pharmaceutical composition comprising: c) a physiologically acceptable carrier, diluent, excipient or adjuvant; wherein said IF is non covalently bound to said insulin, and wherein after oral administration, said insulin enters the circulation system.
wherein q is 0 to 4; (i) halo, (ii) nitro, (iii) (C,C)alkyl, (iv) (C,C)alkoxy, (v) halo-(C,C)alkyl, (vi) halo-(C,C)alkoxy, (vii) hydroxy, and (vii) (C,C)thioalkyl; Page 18
5,843,898 5,843,901 TRANSFORMATION VECTORS ALLOWING LHRH ANTAGONIST PEPTIDES Roger W. Roeske, Indianapolis, Ind., assignor to Advanced Research & Technology Institute, Bloomington, Ind. Henri Marcel Jozef De Greve, Brussels, Belgium; Maria Benita Leonor Fernandez Salgado, Iguala, Mexico; Marc Charles Filed Jun. 7, 1995, Ser. No. 480,494 Ernest Van Montagu, Brussels, Belgium; Mark Albert Int. Cl. A61K 38/00;38/04;38/08 Vaeck, Zemst, Belgium; Marcus Florent Oscar Zabeau, U.S. Cl. 51415 5 Claims Gent, Belgium; Jan Jozef August Leemans, Heusden, Bel 1. A peptide compound comprising a structure: gium, and Hermanus Fransiscus Paulus Hofte, Gent, Belgium, assignors to Plant Genetic Systems, N.V., Gent, Bel- . A-B-C-D-E-F-G-H-I-J gium Division of Ser. No. 446,486, May 22, 1995, Pat. No. wherein 5,545,565, which is a continuation of Ser. No. 133,965, Oct. 8, A is pyro-Glu, Ac-D-Nal, Ac-D-Qal, Ac-Sar, or Ac-D-Pal; 1993, abandoned, which is a division of Ser. No. 14,148, Feb. B is His or 4-CI-D-Phe; 5, 1993, Pat. No. 5,317,096, which is a division of Ser. No. 555,828, Jul. 23, 1990, Pat. No. 5,254,799, which is a continu- C is Trp, D-Pal, D-Nal, L-Nal-D-Pal(N-O), or D-Trp; ation of Ser. No. 821,582, Jan. 22, 1986, abandoned, which is D is Ser; a continuation-in-part of Ser. No. 692,759, Jan. 18, 1985, E is N-Me-Ala, Tyr, N-Me-Tyr, Ser, Lys(iPr), 4-Cl-Phe, His, abandoned. This application Jun. 5, 1995, Ser. No. 463,510 Asn, Met, Ala, Arg or Ile; F is D-Asn or D-Gln; U.S. Cl. 51412 1 Claim G is Leu or Trp; H is Lys(iPr), Gln, Met, or Arg; I is Pro; and J is Gly-NH2 or D-Ala-NH2; or a pharmaceutically acceptable salt thereof. 5,843,899 USE OF INSULIN-LIKE GROWTH FACTORS I AND II FOR INHIBITION OF INFLAMMATORY RESPONSE Philip F. Halloran, Edmonton, Canada, assignor to Ciba-Geigy Corporation, Ardsley, N.Y. tion May 16, 1997, Ser. No. 857,774 5,843,902 U.S. Cl. 514-12 8 Claims METHODS FOR TREATING PROSTATE CANCER WITH 1. A method for inhibition of an inflammatory response in a LHRH ANTAGONISTS mammal that has an inflammatory condition, wherein said inflam- Marc B. Garnick; Christopher J. Molineaux, both of matory condition causes degeneration of cartilage, pancreatic cells, Brookline, Mass., and Malcolm L. Gefter, Lincoln, Mass., brain cells or gastrointestinal cells, said method comprising admin assignors to Praecis Pharmaceuticals Incorporated, Camistering thereto an inflammatory response inhibitory dose of IGF sufficient to inhibit degeneration of said cartilage, pancreatic cells, bridge, Mass. brain cells or gastrointestinal cells. Continuation-in-part of Ser. No. 573,109, Dec. 15, 1995. This application Nov. 25, 1996, Ser. No. 755,593 Int. Cl. A61K 37/24 U.S. Cl. 514/15 77 Claims 5,843,900 1. A method for treating prostate cancer in a subject in need of BRADYKININ ANTAGONISTS such treatment, comprising: John C. Cheronis, Lakewood; Albert Gyorkos, Westminster; administering to the subject an LHRH antagonist for a period of Lyle W. Spruce, Arvada, and Eric T. Whalley, Golden, all of at least 14 days; and Colo., assignors to Cortech, Inc., Denver, Colo. Continuation-in-part of Ser. No. 296,185, Aug. 8, 1994, which simultaneously or subsequently administering to the subject an is a continuation of Ser. No. 974,000, Oct. 10, 1992, aban LHRH agonist such that the LHRH antagonist completely doned, which is a continuation-in-part of Ser. No. 859,582, suppresses agonist-induced hormone surge in the subject. Mar. 27, 1992, abandoned, which is a continuation-in-part of Ser. No. 677,391, Apr. 1, 1991, abandoned. This application Jun. 5, 1995, Ser. No. 465,672 Int. Cl. A61K 38/08; CO7K 7/18 U.S. Cl. 514/15 21 Claims 1. A heterodimer of the formula:
where BKAn is a bradykinin antagonist peptide selected from: DArgo-Argʻ-Pro2-Hyp3-Gly4-Iglb-Ser®-DIglb7-Oic8-Argo; DArgo-Arg'-Pro2-Hyp-Gly4-Thi®-Ser®-DIglb?-Oic®-Argo; DArgo-Arg'-Pro2-Hypo-Gly4-Iglb?-Ser®-D-Tic”-NChg8-Argo; Y is dihydromorphine or morphine; and 6 position amino acid residue of said peptide; wherein said heterodimer retains bradykinin antagonist activity. Page 19
% RECOVERY OF 5 FLUOROURACIL DOSE = 25mg/kg
% RECOVERY OF 5-FLUOROURACIL IN 0-24 5,843,920 HOUR URINE VERSUS DOSE OF NUCLEOSIDE ANIONIC SACCHARIDES FOR EXTRACTION OF ANTI ANGIOGENIC PROTEIN FROM CARTILAGE Paul B. Weisz, State College, Pa., assignor to BioCell Technology, LLC, Newtown, Pa. Filed Sep. 16, 1996, Ser. No. 710,375 Int. Cl. A61K 31/715:35/34 U.S. CI. 51458 20 Claims 1. A method of extracting an anti-angiogenic protein from carti lage comprising the steps of: 0.03 0.3 3 contacting particles of cartilage with (a) a saccharide having a DOSE EQUIVALENT OF 5-ETHY NYLURACIL (mg/kg) suitable degree of intramolecular density of anionic substitu5-ETHYNYLURACIL-BASE ents and (b) an aqueous medium containing between 0.2 and 21,31-DIDEOXY RIBOSIDE 4.0 molar concentration of inorganic cations for a time suffiARABINOSIDE cient for anti-angiogenic protein transfer from the cartilage to 2 21-DEOXY RIBO-51-MONOPHOSPHATE the saccharide to form a composition, and 2-DEOXY RIBOSIDE RIBOSIDE separating said composition containing extracted anti angiogenic protein. 5-fluoro-5"-(1-propynyl)-2',2'"-O-succinylbis(1-B-D arabinofuranosyl)uracil); and 5-chloro-2'-5'-dideoxy-5-fluorouridine-2''-deoxy-5"ethynyluridine (3-5')diphosphate. 5,843,921 THERAPEUTIC FOOD COMPOSITION AND METHOD TO DIMINISH BLOOD SUGAR FLUCTUATIONS Francine R. Kaufman, Los Angles, Calif., assignor to Childrens 5,843,918 ANTI-ENDOTOXIN COMPOUNDS Hospital of Los Angeles, Los Angeles, Calif. William J. Christ, Andover; Lynn D. Hawkins, Haverhill; Tsu Continuation-in-part of Ser. No. 418,210, Apr. 7, 1995, Pat. tomu Kawata; Daniel P. Rossignol, both of Andover, all of No. 5,605,893, which is a continuation-in-part of Ser. No. Mass.; Seiichi Kobayashi, Tsuchiurashi, and Osamu Asano, 213,542, Mar. 15, 1994, abandoned. This application Oct. 21, Tsukuba, both of Japan, assignors to Eisai Co., Ltd., Tokyo, 1996, Ser. No. 733,959 Japan Int. Cl. A61K 31/715 Division of Ser. No. 935,050, Aug. 25, 1992, Pat. No. U.S. Cl. 51460 31 Claims 5,530,113, which is a continuation-in-part of Ser. No. 776,100, Oct. 11, 1991, abandoned. This application Jun. 7, 1995, Ser. 1. A therapeutic food composition for treatment of diabetic No. 472,820 patients to diminish fluctuations in blood sugar levels and prevent Int. Cl. A61K 31/715;31/72;31/73 hypoglycemic episodes, comprising per serving or unit about U.S. Cl. 51453 1 Claim 20–50 grams of nutrients, including: 1. A method for treating sepsis in a mammal, said method a) about 5-15 g of slowly absorbed complex carbohydrate; comprising administering to said mammal a therapeutic composi- b) about 7–20 g of rapidly absorbed complex carbohydrate; tion containing a compound having the formula: c) about 3-20 g of protein; OPO(OH)2 d) about 2–7 g of fat; and e) at least one sweetening agent, CH301 0 wherein the amount of simple sugars other than fructose in said composition is less than about 3 grams per unit. НО" ' (HO)2OPO N NH (CH2)10CH H CH3(CH2)6 (CH2CH3
(CH2)10CH OH 5,843,922 PREPARATION OF OLIGOSACCHARIDES AND (CH2)SCH PRODUCTS THEREFROM ette, Ind., assignors to Fuisz Technologies Ltd., Chantilly, Va. or a pharmaceutically-acceptable salt thereof. Continuation of Ser. No. 282,807, Jul. 29, 1994, abandoned. This application Jun. 11, 1996, Ser. No. 662,201 Int. Cl. A61K 31/715; G07H 3/06; C12N 1/20 U.S. Cl. 51461 37 Claims 5,843,919 1. A method of preparing a bifidobacteria-nourishing medium, COMPOSITION AND METHOD FOR THE TREATMENT comprising: OF ARTHRITIS subjecting an essentially anhydrous saccharide-based feedstock John A. Burger, 220 10th St., Huntington Beach, Calif. 92648 having fructosyl units contained therein to flash flow processFiled Oct. 22, 1997, Ser. No. 955,098 Int. C1.6 A61K 31/70:31/20 ing under essentially to provide a substantially amorphous and U.S. Cl. 514-62 28 Claims essentially anhydrous shearform matrix, and 1. A composition for the treatment of arthritis comprising glu reacting said shearform matrix with an acid catalyst under acid cosamine, or a polymer or copolymer thereof, and omega-3-fatty thermolysis conditions to provide a fructosyl-containing oliacid, in amounts effective to elicit a synergistic response. gosaccharide. Page 20
or a phenyl radical of formula It wherein: R and R? may be the same or different and are each selected (It) from the group consisting of hydrogen and lower alkyl; X is selected from the group consisting of Ge, Si and Sn; Y' and Y2 are the same and are either CH2 or C=0; m is zero or one; Z is CH2 when m is 1 and CH, or C=0 when m is zero; alkylene and 3 to 6 inclusive when R3 is alkenylene; and R4 and Rare independently selected from the group consisting 5,843,934 USES OF ESTROGEN COMPOUNDS FOR THE of lower alkyl or lower alkenyl, or are linked together to form TREATMENT OF DISEASE a heterocyclic group selected from morpholino, pyrrolidino, James W. Simpkins, Gainesville, Fla., assignor to University of piperidino and lower alkyl substituted piperazino in which the Florida Research Foundation, Inc., Gainesville, Fla. lower alkyl group is attached to a terminal nitrogen atom, Continuation-in-part of Ser. No. 149,175, Nov. 5, 1993, aban or a pharmaceutically acceptable acid addition salt thereof, doned, and a division of Ser. No. 318,042, Oct. 4, 1994, Pat. wherein the effective amount of the active agent represents less No. 5,554,601. This application May 16, 1996, Ser. No. than approximately 1.0 wt. % of the composition, 648,857 Int. Cl. A61K 31/56 and further wherein the composition is in the form of an ointU.S. Cl. 514182 6 Claims ment, lotion, cream, gel or shampoo. 1. A method for conferring a cytoprotective effect on a population of cells in a male or female subject, comprising: (a) providing an estrogen compound having insubstantial sex related activity, in a pharmaceutical formulation; and 5,843,937 DNA-BINDING INDOLE DERIVATIVES, THEIR PRODRUGS AND IMMUNOCONJUGATES AS ANTICANCER AGENTS Yuqiang Wang, Mountain View; Susan C. Wright, Saratoga, and James W. Larrick, Woodside, all of Calif., assignors to 5,843,935 PROTEIN KINASE C INHIBITORS Panorama Research, Inc., Mountain View, Calif. William F. Heath, Jr., Fishers; Michael R. Jirousek, Indianapo Filed May 23, 1996, Ser. No. 652,883 lis; John H. McDonald, III, Carmel, and Christopher J. Rito, Int. Cl. A61K 31/40;31/545; C07D 487/04,501/22 Mooresville, all of Ind., assignors to Eli Lilly and Company, U.S. Cl. 514202 41 Claims Indianapolis, Ind. 1. A compound of the formula: Continuation of Ser. No. 643,707, May 6, 1996, abandoned, which is a continuation of Ser. No. 413,735, Mar. 30, 1995, R, (C(O)-R2-R3-NH).-C(O)-R3-NH),-R4 cation Jul. 12, 1997, Ser. No. 903,236 CICH U.S. Cl. 514183 7 Claims 1. A method for treating restenosis comprising administering a therapeutically effective amount of a PKC inhibitor. N-, N-,
5,843,936 TOPICAL ADMINISTRATION OF AZASPIRANES TO PREVENT OR TREAT SKIN CONDITIONS ASSOCIATED WITH HYPERPROLIFERATION OF KERATINOCYTES Lawrence R. Bernstein, 380 Willow Rd., Menlo Park, Calif. 94025 Filed Jun. 28, 1996, Ser. No. 672,728 Int. Cl. A61K 31/555 U.S. Cl. 514188 29 Claims 1. A locally administrable topical pharmaceutical composition comprising a carrier suitable for topical administration and an amount of an active agent effective to prevent or treat skin conditions associated with hyperproliferation of keratinocytes and/or an immunologically mediated hyperproliferative skin disorder, wherein the active agent is an azaspirane compound having the structure of formula (I) Page 21
Co-C12-aryl-C,-Cg-alkyl where the aryl group is unsubstituted NR24—C(=0)0—RS, or substituted with one to three of the groups selected from NR24_C(=O)S—RS, (CH)-4-NR24_C(=O)-R25, nitro, NR2_CH(OH)-R25, halo(F, a, Br, I), and NR24_CH-R25 C,-C4-alkoxy; NR24_S(O)-R25 where u is 0,1, or 2, R13 is selected from the group CHR24_0_R25 hydrogen, CHR24—CH,R25, C, Coalkyl, CHR24_R25 halo(F, CI, Br, I)-C,-C6 alkyl, CR24=CHR25 (E or Z), phenyl, (CH2)2-4-C(=O)-R25, benzyl, and Co-Cloaryl-R25, CH2–0-COCHZ; heterocyle-R25, R15 is selected from the group C, C alkyl-Co-Cigaryl-R25, and Co-C14aryl, CZ-Calkyl-heterocycle-R25, heteroaryl, where the heteroaryl is a 5- or 6-member aromatic where any heterocycle is a 5- or 6-member saturated or unsaturated ring containing 1 to 3 heteroatoms selected from O, N, and S ring containing 1 to 3 heteroatoms selected from O, N, and S; and where the heteroaryl is unsubstituted or substituted with R24 is selected from the group one or two substituents selected from the group hydrogen, ОН, benzyl, SH, halo(F, a, Br, I)benzyl, CC_alky, Ci-Coalkyl, and C, C alkoxy, halo(F, CI, Br, I)C,-Coalkyl; CF3, R25 is selected from R25, halo(F, CI, Br, I), s S COOH, COO—C,-C alkyl), N NH, 1 1 NH(CC alkyl), and N(C1-C alkyl)2, C3-C4-cycloalkyl, R25 is selected from the group C,-C4-alkyl, unsubstituted or substituted with a substituent selected from the group Co-C14aryl, heteroaryl as defined above, NOR26, ОН. C, Coalkyl, SH C2-Cgalkenyl, CZ-C alkyl, Ci-Coalkylamine, C, C alkoxy, C2-Coalkenylamine, and Ci-C alkylthio, halo(F, CI, Br, IC,-Coalkyl, where any alkyl or alkenyl moiety is optionally substituted halo(F, CI, Br, I), with one to three NO2, CO,H, SSR26, CO2-C, Cd-alkyl, NH, NOR26, and N[(C,C4)-alkyl]2, NR27R28, NH[(C,-C4)-alkyl], where any amine moiety is optionally substituted with POZH, R27 or R28 R26 is selected from the group hydrogen, CN, C, Coalkyl, halo(F, CI, Br, IC,-Coalkyl, and NO2, COOR13, C,Co alkanoyl; R27 and R28 are independently selected from the group C-Co-perfluoroalkyl, and hydrogen, R19 is selected from the group C,-Coalkyl, hydrogen, phenyl, C, Co-alkyl napthyl, C2-C/-alkenyl, benzyl, C-Co-alkoxy, CH2napthyl (a or B) Cz-Co-alkoxyalkyl, C,Coalkanoyl, CH2-0_COCH3, and C.-C.cycloalkanoyl, benzyl, where the phenyl moiety is unsubstituted or substituted Co-Claroyl, with a group selected from the group Co-Cigary1C,-Coalkanoyl, CZ-Coalkylsulfonyl, NH2, Co-Cigarylsulfonyl, OH, and Co-Cigary1C, Coalkylcarbamoyl, OCH3; cinnamoyl, X is selected from the group heterocyclecarbonyl, NR24_C(=0)-R25, -Coalkoxycarbonyl, -C(=O)-R8, Co-Caryloxycarbonyl, NR24_C(=O)-NR7'R, Co-Clary1C,-C alkoxycarbonyl, and Page 22
wherein Pl represents alkoxycarbonyl, aralkoxycarbonyl, alkanoyl, the pyridine system cycloalkylcarbonyl, cycloalkylalkoxycarbonyl, cycloalkylalkanoyl, aralkanoyl, aroyl, aryloxycarbonyl, heterocyclylcarbonyl, hetero- cyclyloxycarbonyl, heterocyclylalkoxycarbonyl, heteroaralkoxy- N carbonyl, heteroaryloxycarbonyl or heteroaroyl radicals; P2 represents hydrogen; R? represents alkyl, aryl, cycloalkyl, cycloalkylalkyl or aralkyl radicals, which radicals are optionally substituted with alkyl, (O)m halogen, -NO2, CN, CF3, -OR'or-SRo radicals, wherein Ro represents hydrogen or alkyl radicals; being connected to the group Ro represents hydrogen, alkyl, alkenyl, alkynyl, hydroxyalkyl, alkoxyalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, het -Neroaryl, heterocyclylalkyl, aryl, aralkyl or heteroaralkyl radicals; and R R4 represents represents alkyl, haloalkyl, alkenyl, alkynyl, cycloalkyl, heterocycloalkyl, heteroaryl, aryl or aralkyl radi- which bears it either in the 2-position or in the 3-position cals; and wherein alkyl, alone or in combination, is a straight-chain or of the pyridine ring; branched-chain hydrocarbon radical having from 1 to 8 car- R, and R2, which may be identical or different, are chosen, bon atoms; alkenyl, alone or in combination, means a straight- independently of each other, from hydrogen, amino, alkychain or branched-chain hydrocarbon radial having one or lamino, dialkylamino, alkyl, hydroxy, alkoxy, nitro, and halomore double bonds and from 2 to 8 carbon atoms; alkynyl, gen, alone or in combination, means a straight-chain hydrocarbon Rz and Rd, which may be identical or different, are chosen, radical having one or more triple bonds and from 2 to 10 carbon atoms; cycloalkyl, alone or in combination, is a hydro independently of each other, from amino, alkylamino, dialkycarbon ring containing from 3 to 8 carbon atoms; aryl, alone lamino, alkyl, hydroxy, alkoxy, nitro, and halogen, or in combination, means a phenyl or naphthyl radical option R represents hydrogen or alkyl, ally substituted with alkyl, alkoxy, halogen, hydroxy, amino, A represents a single bond; and in this case Het represents a nitro, cyano or haloalkyl radicals; heterocyclyl or heterocy group chosen from pyrazine and substituted pyrazine, or altercloalkyl means a saturated or partially unsaturated monocy natively A represents alkylene which is unsubstituted or subclic, bicyclic or tricyclic heterocycle having one or more stituted with one or more alkyl, or alkenylene which is unsubnitrogen, oxygen or sulphur heteroatoms, which is optionally substituted on one or more carbon atoms by halogen, alkyl, stituted or substituted with one or more alkyl; and in this case alkoxy or oxo radicals, or on a secondary nitrogen atom by Het also represents a group chosen from pyrazine and substialkyl, aralkoxycarbonyl, alkanoyl, phenyl or phenylalkyl radi tuted pyrazine, cals, or on a tertiary nitrogen atom by oxido radical; and X represents oxygen, imino, or imino substituted with a group heteroaryl means an aromatic heterocyclyl radical which is chosen from alkyl, alkoxy, hydroxy, amino, arylalkyloxy, and optionally substituted as defined above with respect to the definition of heterocyclyl. aryloxy, an enantiomer and a diastereoisomer thereof and an addition salt thereof with a pharmaceutically-acceptable acid or base, it being understood that, except where otherwise mentioned: the term "substituted" relating to the pyrazine system means 5,843,947 that it is substituted with one or more groups chosen from N-PYRIDYL CARBOXAMIDES AND DERIVATIVES alkyl, alkoxy, trifluoromethyl, hydroxy, halogen, thio, and Jean-Michel Robert; Odile Rideau; Sylvie Robert-Piessard; alkylthio, Jacqueline Courant, all of Nantes; Guillaume Le Baut, Saint Sebatien sur Loire; Daniel-Henri Caignard, Paris; Pierre the terms “alkyl”, "alkoxy", and "alkylene" denote linear or Renard, Versailles, and Gérard Adam, Le Mesnil le Roi, all branched groups containing 1 to 6 carbon atoms, inclusive, of France, assignors to Adir et Compagnie, Courbevoie, the term “aryl” denotes phenyl or naphthyl, France the term “alkenylene” denotes a linear or branched unsaturDivision of Ser. No. 450,346, May 25, 1995, Pat. No. ated chain containing 2 to 6 carbon atoms, inclusive. 5,712,294. This application Mar. 26, 1997, Ser. No. 827,344 Claims priority, application France, May 27, 1994, 94 06412 Int. Cl. A61K 31/495; C07D 401/12 U.S. Cl. 514252 15 Claims 1. A compound selected from those of formula (I): 5,843,948 PIPERAZINOPHENYL- AND RI PIPERAZINOPHENYLOXYCARBOXYLIC ACID R2 DERIVATIVES, AND PROCESSES AND INTERMEDIATES Het-A-C-N N FOR THEIR PREPARATION AND PHARMACEUTICAL 11 | COMPOSITIONS COMPRISING THEM X R Wolfgang Kehrbach, Hanover; Uwe Schoen, Burgdorf, both of (O)m R4 Germany; Jack A. J. den Hartog, Weesp, Netherlands; Jan in which H. van Maarseveen; Chris G. Kruse, both of Amersfoort, m is equal to 0 or 1, Netherlands; Jochen Antel, Bad Muender, Germany; Janthe symbol Hendrik Reinders, Hilversum, Netherlands; Dieter Ziegler, Hemmingen, and Gerhard-Wilhelm Bielenberg, Alfeld/ Leine, both of Germany, assignors to Solvay Pharmaceuti- N cals GmbH, Hanover, Germany Filed Dec. 19, 1997, Ser. No. 994,754 Claims priority, application Germany, Dec. 19, 1996, 196 52 (O)m 919.0 Int. Cl. A61K 31/495; CO7D 401/04;295/135 representing the pyridine ring when m is equal to 0 and U.S. Cl. 514252 12 Claims pyridine N-oxide when m is equal to 1, 1. A compound corresponding to the formula I: Page 23
5,843,960 R4 I INHIBITORS OF ROTAMASE ENZYME ACTIVITY Joseph P. Steiner, Hampstead; Solomon Snyder, Baltimore; Gregory S. Hamilton, Catonsville, and Ted Dawson, Balti more, all of Md., assignors to GPI Nil Holdings, Inc., WilmN - N R2 ington, Del., and Johns Hopkins University School of Medicine, Baltimore, Md. Continuation of Ser. No. 653,905, May 28, 1996, Pat. No. 5,696,135, which is a continuation-in-part of Ser. No. 474,072, Jun. 7, 1995, Pat. No. 5,798,355. This application Jan. 23, 1997, Ser. No. 787,162 R1 Int. Cl. A61K 31/445;38/18 wherein: U.S. Cl. 514317 6 Claims R1, R2, R3, and R4 are selected from the group consisting of 1. A method for preventing neurodegenerative effects of a neu hydrogen, C-salkyl, C-salkoxy, phenyl, halo, hydroxy, rological disorder in an animal in need thereof, comprising: Cl-salkylsulfonyl, C-salkylthio, trihaloC -salkyl, amino, nitro administering to an animal an effective amount of a nonimmuand 2-quinolinylmethoxy; nosuppressive pipecolic acid derivative having an affinity for Rs is selected from the group consisting of C-salkyl and R, FKBP-type immunophilins to prevent neurodegeneration, where R, is (CH),Rg or (CH2),CHROR, where wherein the FKBP-type immunophilin exhibits rotamase n is 1 or 2; activity and the nonimmunosuppressive pipecolic acid derivaRg is halo, oxy, carbonyl, hydroxy, oximino, carboxy, tive inhibits said rotamase activity of the immunophilin. C-salkoxycarbonyl, N-C-salkyl-N-hydroxy-amido; 5,843,961 with the proviso that if R, is present, R1, R2, R3, and R4 are METHOD AND COMPOSITION FOR TREATING other than 2-quinolinylmethoxy; ERECTILE DYSFUNCTION with the further proviso that if R, is absent one of R1, R2, Rz, Nils G. Kock, Apotekaregatan 3, S-413 19 Göteborg, and Gerand R4 is 2-quinolinylmethoxy; hard Lycke, Annikas gata 4, S-421 67 Västra Frölunda, both and pharmaceutically acceptable salts thereof. of Sweden Division of Ser. No. 317,910, Oct. 4, 1994, abandoned, which is a continuation of Ser. No. 965,688, Oct. 22, 1992, aban doned, which is a continuation of Ser. No. 244,407, Sep. 14, 5,843,959 1988, abandoned. This application Jun. 7, 1995, Ser. No. METHODS AND BICYCLIC POLYAMINE 484,546 COMPOSITIONS FOR THE TREATMENT OF Claims priority, application Sweden, Sep. 14, 1988, 8803097 INFLAMMATION Int. Cl. A61K 31/445;31/47;31/31;31/19 Raymond J. Bergeron, Jr., Gainesville, Fla., assignor to Univer- U.S. Cl. 514321 27 Claims sity of Florida Research Foundation, Inc., Gainesville, Fla. 1. A pharmaceutical composition for administration to the ureFiled Mar. 19, 1997, Ser. No. 820,027 thra of a male individual to produce penile erection, comprising an Int. Cl. A61K 31/445;31/33;31/55;31/40 effective amount of a lipophilic active agent dispersed in a hydroU.S. Cl. 514-316 4 Claims philic vehicle, wherein; 1. A method for treating inflammation in a human or non-human (a) the hydrophilic vehicle is suitable for urethral administration mammal suffering therefrom comprising administering to said and effective to facilitate passage of the lipophilic active agent mammal an amount of a polyamine or a pharmaceutically accept- through the urethral membrane so that the active agent able acid salt thereof sufficient to exert an anti-inflammatory activ- reaches the corpora cavernosa; and ity in said mammal, said polyamine having the formula: (b) the lipophilic active agent comprises an a,-receptor blocking agent present in the composition at a concentration effective (CH2) R2 R3 (CH2) to produce penile erection following administration of the 1 . RI-N CH+CH2tyN+CH2tyN+CH2tz CH N-R4 composition to the urethra of the male individual.
or a salt thereof with a pharmaceutically acceptable acid wherein: 5,843,962 R1, R2, Rz and R4 may be the same or different and represent H, METHODS OF INHIBITING OVARIAN DYSGENESIS, straight- or branched-chain alkyl, aryl, aryl alkyl or cycloalkyl DELAYED PUBERTY, OR SEXUAL INFANTILISM of 1-12 carbon atoms; Jeffrey A. Dodge, Indianapolis, Ind., assignor to Eli Lilly and a, b, c and d may be the same or different and are integers from Company, Indianapolis, Ind. 0 to 8, except that when a or c is zero, b or d is greater than or Division of Ser. No. 170,946, Dec. 21, 1993, Pat. No. equal to 3 and when a or c is one, b or d is greater than or 5,541,589. This application May 17, 1995, Ser. No. 442,919 equal to 2; and Int. Cl. A61K 31/445;31/358 X, Y and Z may be the same or different; X and Z are integers U.S. Cl. 514—324 6 Claims from 0 to 10; and Y is an integer from 1 to 10, excluding the 1. A method of inhibiting sexual infantilism comprising adminpolyamine of the formula wherein a=b=c=d=2, X=Z=2 and istering to a human in need thereof an effective amount of a Y=4. compound having the formula Page 24
the racemic-enantiomeric mixtures and optical isomers of said 5,843,971 compounds or a pharmaceutically acceptable salt or prodrug 1, 1-BIS (HETEROAZOLYL) ALKANE DERIVATIVES thereof, AND THEIR USE AS NEUROPROTECTIVE AGENTS wherein Robin Bernard Boar, Hertfordshire; Duncan Alastair Gray, Powys, and Dennis Mark O'Shea, Hertfordshire, all of Great R! is an optionally substituted phenyl, optionally substituted Britain, assignors to Astra Aktiebolag, Sodertalje, Sweden phenoxyalkyl having 1 to 4 carbons in the alkoxy portion, PCT No. PCT/SE95/00604, § 371 Date Jan. 29, 1996, § 102(e) optionally substituted pyridinyl, optionally substituted pyrim Date Jan. 29, 1996, PCT Pub. No. W095/33747, PCT Pub. idyl, optionally substituted thiazolyl or optionally substituted Date Dec. 14, 1995 oxazolyl; PCT Filed May 29, 1995, Ser. No. 448,411 where the optionally substituted moieties of R' are optionally Claims priority, application Sweden, Jun. 7, 1994, 9401965 substituted with one to three substituents, each substituent Int. Cl. A61K 31/425; C07D 417/06 is independently selected from the group consisting of U.S. Cl. 514-365 7 Claims hydroxy, fluoro, chloro, iodo, bromo, CF3, sulfonamide, 1. A compound having the general formula (1) (C1-C4)alkyl, (C1-C4)alkoxy, carboxy, hydroxyalkyl, (C,C4)alkoxycarbonyl, (C,CA)thioalkyl, sulfonyl, sulfiY3 R2 (1) nyl, amino, -NH-C0—(CH2)a-(phenyl), -NH-CO- Y1 Y4 ( C1-C10)alkyl, -NH-S02(CH2)2-(phenyl) and -NH-S02—(C1-C10)alkyl; X1 X2 R2 is hydrogen or (C,-Co)alkyl; wherein: R’ is hydrogen or (C.-C.)alkyl; X, and X2 are independently 0, S or Se; R4 and RS are each independently selected form the group Y and Y2 are independently C or N with the proviso that at consisting of hydrogen, CO2H, -CO2R", -CO2NROR", least one of Y, and Y2 is N; -CHO, COR", -CH2OH, CH 2OCH,CO2R and Y3 and Y4 are independently C or N with the proviso that at -CHOCH_CH_OR; least one of Y3 and Y4 is N; R® for each occurrence is independently selected form the R, and R2 each represent one or more groups independently group consisting of hydrogen and (CZ-C4) alkyl; selected from H, lower alkyl, lower alkoxy-lower alkyl, Y is oxygen or sulfur; hydroxy-lower alkyl, lower acyloxy-lower alkyl or CFz; and Z is-(CH2)- n is 1; WR3 R5 R? is hydrogen, (C,-C1o)alkyl, (C,-C 10)alkenyl, –(CH2) (optionally substituted phenyl), -CH2)-(optionally subC=C stituted pyridinyl), C0—(CH2)-(optionally substituted R4 Ro phenyl), -C0—C, C10)alkyl, --S02(CH2), (optionally substituted phenyl) or -S02—(C,-C10)alkyl; wherein W is O, S, NH or N-lower alkyl, where the optionally substituted moieties in the definition Rz is H, lower alkyl or lower acyl, of R7 are optionally substituted with one to three subor WR3 is H, stituents, each independently selected form the group R4 is lower alkyl or lower perfluoroalkyl, consisting of hydroxy, fluoro, chloro, iodo, bromo, CF3, or Rz and R, together form a ring sulfonamide, (C,-C4)alkyl, (C-C4)alkoxy, carboxy, hydroxyalkyl, (C, C4)alkoxycarbonyl, (C,-C)thioalkyl, W sulfonyl, sulfinyl, amino, -NH-C0—(CH2)-(phenyl), -NH-C0—(C-C10)allyl, -NH-S02—(CH2) (phenyl) and -NH-S02—(C,C10)allyl; (CH2), a is 0, 1, 2, 3 or 4 provided that R4 and Rare not both hydrogen at the same time. wherein n is 2, 3 or 4, R, and Rindependently are H or lower alkyl; geometrical and optical isomers and racemates thereof where such isomers exist, as well as pharmaceutically acceptable acid addition 5,843,973 salts thereof and solvates thereof; with the proviso that 1,1-di(2thiazolyl)ethanol is excluded. THIAZOLIDINONE COMPOUNDS AND COMPOSITION FOR ANGINA PECTORIS COMPRISING THE COMPOUNDS AS AN ACTIVE INGREDIENT Sadao Ishihara, Saitama-ken; Fujio Saito, Urayasu; Yasuo Ohhata, Tokyo; Shigeki Miyake, Mitaka; Ryosuke Yorikane, 5,843,972 Toda, and Norio Fukuda, Tokyo, all of Japan, assignors to HETEROCYCLIC B-ADRENERGIC AGONISTS Robert L. Dow, and Stephen W. Wright, both of Groton, Sankyo Company, Limited, Tokyo, Japan Conn., assignors to Pfizer Inc., New York, N.Y. Filed Jun. 10, 1997, Ser. No. 872,770 Filed Mar. 28, 1997, Ser. No. 827,289 Claims priority, application Japan, Dec. 15, 1994, 6-311511 Int. Cl. A61K 31/38;31/425; C07D 307/02;277760 Int. Cl. A61K 31/42;31/425; CO7D 263/24;277/14 U.S. CI. 514367 15 Claims U.S. Cl. 514-369 74 Claims 1. A compound of the formula (I) 1. A thiazolidinone compound having the general formula: Page 25
R, and R=H, lower alkoxy, hydroxy, lower straight and 5,843,997 branched chain alkyl or halogen; EXCITATORY AMINO ACID RECEPTOR ANTAGONISTS Rz and R=H, lower alkoxy, lower straight and branched chain Lawrence J. Heinz, Pittsboro; William H.W. Lunn, and Daralkyl or halogen; and ryle Darwin Schoepp, both of Indianapolis, all of Ind., n=an integer from 0 to 2; assignors to Eli Lilly and Company, Indianapolis, Ind. salts thereof; stereoisomers thereof; and mixtures thereof. Division of Ser. No. 322,632, Oct. 13, 1994, Pat. No. 5,576,323, which is a continuation-in-part of Ser. No. 161,830, Dec. 3, 1993, abandoned. This application Apr. 2, 1996, Ser. No. 626,447 13 Claims 5,843,995 1. A compound of the formula INHIBITION OF HIV-1 REPLICATION USING COR4 I OLIGOCARBAMATE DERIVATIVES (R'), (R2)p Tariq M. Rana, Piscataway, and Ikramul Huq, Highland Park, (CH2) Wm H2N COR Filed Jul. 7, 1997, Ser. No. 888,865 wherein: Z is NRS, O, or S; U.S. Cl. 514-551 21 Claims W is CH 3-p), –(CH),-,-(CH2),CH(3-p), — (CH),CO—, 1. An oligocarbamate derivative of the formula (CH2),0, -(CH),CH=CH(CH2),– -(CH2),CH=CH-CH=CHCO—, -CH=CHCOR, –(CH2),CHOHR“, –(CH2),CHOH—, -(CH2),COR”, -O(CH2),—, NR”, O, S, SO, or SO2; H N n is 0 or 1; m is 0 or 1; p is 0, 1, 2, or 3; q is 0–6; r is 1 or 2; s N is 0 or 1, provided that the sum of n, m, p and s is at least 1, H2N N R2 H R4 H and that p is 1 if n is 1, s is 0 and m is 0 or if m is 1 and W is –(CH2), -, -(CH2),CO—, -(CH2),0—, -(CH2), CH=CH(CH2),—, -CH2),CH=CH-, -CH=CHCO—, H R3 -(CH2),CHOH—, -O(CH2), -, NR5, O, S, SO or SO2; N R and R2 are independently aryl, substituted aryl, heterocycle, or substituted heterocycle; R3 H O R5 R3 is hydrogen or a carboxy protecting group; R4 is hydrogen or a carboxy protecting group; R3 R$ is hydrogen, C,-C10 alkyl, acyl, or H R3 N OH CO2(C,-C4 alkyl); N Ris C,-C10 alkyl; R3 H provided that when n is 0 and s is 1, then R' is selected from the group consisting of tetrazolyl, triazolyl, pyridazinyl, pyrimidi nyl, pteridinyl, 1,2,4-triazine-3,5-dionyl, pyrazolonyl, wherein 7H-purinyl, xanthinyl, 3-ethyl-5-hydroxy-1,2,4-thiadiazolyl, R' is a p-hydroxybenzyl or benzyl group; 3-hydroxy- 1,2,4-thiadiazolyl, rhodaninyl, hydantoinyl, and R2 is hydrogen or methyl; pseudothiohydantoinyl; further provided that when n is 1, m is 1, and W is NRS, O, S, R3 is guanidinopropyl; SO, or SO2, then s is 1; and when n is 0 and s is 0, then m is R* is aminobutyl or guanidino propyl; and Ris amidomethyl or amidoethyl; and analogs thereof, and the 1 and W is –(CH2),C0—, -(CH2),0—, -CH=CHCO—, -CH=CHCOR, (CH2),CHOHR“, –(CH2),CHOH—, biologically and pharmaceutically acceptable salts thereof. -(CH2),CORO, -O(CH2),–, NR, O, S, SO, or SO2; or a pharmaceutically-acceptable salt thereof.
5,843,996 INTRAVENOUS MAGNESIUM GLUCONATE FOR TREATMENT OF CONDITIONS CAUSED BY EXCESSIVE OXIDATIVE STRESS DUE TO FREE RADICALDISTRIBUTION William B. Weglicki, 8404 Coach St., Potomac, Md. 20850 Filed Jan. 24, 1997, Ser. No. 787,731 Int. Cl. A61K 31/19 U.S. Cl. 514-557 7 Claims 1. A method of treating ischemia/reperfusion injury due to oxidative stress in a patent in need thereof comprising administering intravenously to the patient an amount of magnesium gluconate effective to substantially reduce an excess free radical surge.
5,843,998 SKIN BLEMISH TREATMENT Jin Song, 2316 Woodfield Way, Bedford, Tex. 76021; John Koch, 8343 Deep Green Dr., Dallas, Tex. 75249, and Marilyn Squier, 614 Reinosa, Garland, Tex. 75043 Filed Jun. 30, 1997, Ser. No. 884,801 Int. Cl. A61K 31/17:31/60;31/19 U.S. CI. 514588 22 Claims 1. A composition suitable for treating acne vulgaris in humans comprising: (a) a therapeutically effective amount of carbamide peroxide; hydroxy acids; and Page 26
5,844,012 FOAM RI R1 (IIb) 1 Robert Gabriel Petrella, Allentown; John Joseph Koch, A-S10-SiO-Z-Si-A, Coplay, and Thomas William Bodnar, Macungie, all of Pa., 1 assignors to Air Products and Chemicals, Inc., Allentown, R1 Pa. Int. Cl. C08J 9/04 U.S. Cl. 521—128 16 Claims D=a group of the formula 1. In a method for producing water-blown molded flexible polyurethane foam which comprises reacting and foaming in one step in a mold a reaction mixture comprising a polyol, an organic polyisocyanate, a urethane catalyst composition comprising a gel ling catalyst and a blowing catalyst, and water as a blowing agent, -0-2-Si-A the improvement for enhancing the surface cure of the molded foam which comprises adding to the reaction mixture an isocyanate trimerization catalyst in an amount from about 0.005 to 0.04 gram milliequivalents per 100 grams of polyol, the trimerization catalyst being a quaternary ammonium salt or an alkali metal or alkaline earth metal salt of a Brönsted acid having a pKa of >1, R'=an unsubstituted or substituted alkyl group having from 1 to wherein the compound is other than (a) an inorganic alkaline earth 30 carbon atoms, an unsubstituted or substituted aryl group or metal salt that has a water solubility of <1 gram of salt per 100 an unsubstituted or substituted alkaryl group, but with at least milliliters of water at 25° C., (b) alkali metal dihydrogen phos80% of the R' groups being methyl groups, phate, (c) alkali metal sulfate and (d) an alkali metal or alkaline a is from 3 to 200, earth metal hydroxide or alkoxide. b is from 0 to 50, c is from 0 to 10, d is from 0 to 5 and e is from 0 to 4, 5,844,013 where the values of a, b, c, d and e in the individual segments A, B, HYDROPHILIC POLYURETHANE GEL FOAMS, D and Z can be different and at least one of b or c is not equal to PARTICULARLY FOR TREATING DEEP WOUNDS, 0, WOUND DRESSING BASED ON HYDROPHILIC E=a group of the general formula; POLYURETHANE GEL FOAMS AND METHOD OF MANUFACTURE Jochen Kenndoff; Vadim Lenuck, both of Hamburg, and -R,2–0–C„H2m0—),R3 Günther Sachau, Quickborn, all of Germany, assignors to Beiersdorf AG, Hamburg, Germany where PCT No. PCT/EP93/02686, $ 371 Date May 30, 1995, $ 102(e) R2 is a divalent alkyl group which may also be branched Date May 30, 1995, PCT Pub. No. W094/07935, PCT Pub. f is 0 or 1; Date Apr. 14, 1994 m has an average value of from 2 to 4; PCT Filed Oct. 1, 1993, Ser. No. 406,926 n is from 0 to 100; Claims priority, application Germany, Oct. 2, 1992, 42 33 R3 is hydrogen, an unsubstituted or substituted alkyl group Int. Cl. C08J 9/04;9/12; CO8L 75/04; A61F 13/02;13/15; A61L 289.3; Mar. 17, 1993, 43 08 445.1; Mar. 17, 1993, 43 08 347.1 having from 1 to 6 carbon atoms, an acyl group or a 15/20;15/26;15/58 o co-NH-R4 group in which R* is an unsubstituted or U.S. Cl. 521—137 46 Claims substituted alkyl or aryl group; and 1. Self-adhesive, hydrophilic polyurethane gel foams formed by X=a polyvalent organic group. mixing covalently crosslinked polyurethane as a matrix and (B) 85–38% by weight, based on the total of (A) and (B), of 5,844,011 one or more polyhydroxyl compounds which are bound in COMPOSITION AND METHOD FOR SELECTIVELY the matrix by secondary valence forces and have an averABSORBING LIQUID HYDROCARBON FROM A FLOOR age molecular weight between 1000 and 12000, and an OR OTHER HARD SURFACE average OH number between 20 and 112, as liquid dispersRaymond J. Gaudin, 203 Medinah, St. Simons Island, Ga. ant, the dispersant being free of hydroxyl compounds with 31522 a molecular weight below 800, and, where appropriate, Filed Apr. 9, 1997, Ser. No. 833,735 (C) 0–100% by weight, based on the total of (A) and (B), of Int. Cl. B08B 7/00; C08G 18/00 fillers and/or additives, U.S. Cl. 521-122 14 Claims and which is prepared by reacting a mixture of 1. Composition for removing liquid hydrocarbon from floors and a) one or more polyisocyanates other hard surfaces comprising: b) one or more polyhydroxyl compounds with an average molecular weight between 1000 and 12000, and with an absorbent granular polyisocyanurate foam having a first bulk average OH number between 20 and 112, density for absorbing the liquid hydrocarbon; and c) optionally, catalysts or accelerators for the reaction a particulate abrasive material having a second bulk density between isocyanate groups and hydroxyl groups and, greater than the first bulk density for imparting slip-resistance optionally, to the floor or hard surface, wherein the granular polyisocya- d) fillers and additives, nurate foam and the particulate abrasive material are blended this mixture being free of hydroxyl compounds with a molecular together to form a mixture. weight below 800, the average functionality of the polyisocy |
How many formula units of nis are contained in a 430. g sample of the compound?
Pos Terkait
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