Patents Examined by Philip I. Datlow
  • Patent number: 5604221
    Abstract: The present invention relates to certain novel indane-2-mercaptoacetylamide disulfide derivatives of the formula ##STR1## useful as inhibitors of enkephalinase.
    Type: Grant
    Filed: December 12, 1995
    Date of Patent: February 18, 1997
    Assignee: Merrell Pharmaceuticals Inc.
    Inventors: Gary A. Flynn, Douglas W. Beight, Alan M. Warshawsky, Shujaath Mehdi, John H. Kehne
  • Patent number: 5604218
    Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
    Type: Grant
    Filed: March 30, 1995
    Date of Patent: February 18, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Scott Hecker, In-Seop Cho, Burton Christensen, Tomasz Glinka, Ving J. Lee
  • Patent number: 5602113
    Abstract: Disclosed are novel pyrido[2,3,-b][1,5]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: February 11, 1997
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
  • Patent number: 5602120
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from CH and N;Z is cyanoR.sub.1 represents C.sub.1-4 alkyl;m is 0, 1, 2 or 3;n is 0, 1 or 2;q is 1 or 2; andD is a 5, 6 or 7-membered, saturated or unsaturated, homo- or heterocyclic ring; and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Jian-Min Fu, Ashok Tehim, Robert A. Kirby
  • Patent number: 5602121
    Abstract: Described herein are D4 receptor-selective compounds of the general formula: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 . . . is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;Y is selected from N and CH;R.sub.1 represents C.sub.1-4 alkyl;n is 0, 1 or 2;q is 1 or 2; andZ is C.sub.5-10 alkyl optionally substituted with OH, halo, C.sub.1-4 alkyl or C.sub.1-4 alkoxy and optionally incorporating a heteroatom selected from O, N and S;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the D4 receptor is implicated, such as schizophrenia, is also described.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventor: Jian-Min Fu
  • Patent number: 5602124
    Abstract: Described herein are 5-HT2 receptor-selective compounds of Formula I: ##STR1## wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5- or 6-membered, homo- or heterocyclic rings;X.sub.1 is selected from CH.sub.2, O, NH, S, C.dbd.O, CH--OH, CH--N(C.sub.1-4 alkyl).sub.2, C.dbd.CHCl, C.dbd.CHCN, N--C.sub.1-4 alkyl, N-acetyl, SO.sub.2 and SO;X.sub.2 - - - is selected from N.dbd., CH.sub.2 --, CH.dbd., C(O)--, O--, and S--;R.sub.1 is C.sub.1-6 alkyl optionally substituted with a substituent selected from OH, halo, C.sub.1-4 alkyl and C.sub.1-4 alkoxy; andR.sub.2, R.sub.3 and R.sub.4 are independently selected from H and R.sub.1 ;and acid addition salts, solvates and hydrates thereof.
    Type: Grant
    Filed: December 12, 1994
    Date of Patent: February 11, 1997
    Assignee: Allelix Biopharmaceuticals, Inc.
    Inventors: Ashok Tehim, Jian-Min Fu, Sumanas Rakhit
  • Patent number: 5599843
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle 2-phenyllactic acid or a topically effective salt thereof.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: February 4, 1997
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5599810
    Abstract: Alpha-adrenergic receptor antagonsists having the formula (I) as set forth below which are useful to produce alpha-adrenergic antagonism, pharmaceutical compositions thereof, and methods of treatment therewith are disclosed: ##STR1## The variables X, R, Y, Het and A are as defined in the specification.
    Type: Grant
    Filed: October 20, 1995
    Date of Patent: February 4, 1997
    Assignee: SmithKline Beecham Corporation
    Inventors: William E. Bondinell, Robert M. Demarinis, Thomas W. Ku, Francis R. Pfeiffer, Dinubhai H. Shah, Joseph W. Venslavsky
  • Patent number: 5597820
    Abstract: A 1,4-benzoxazine derivative of the following formula (I): ##STR1## or a pharmaceutically acceptable salt thereof is disclosed. The compound of the present invention is useful as a medicament for preventing or treating disorders induced by intracellular acidosis during myocardial ischemia, such as cardiac dysfunction, myocardial necrosis, arrhythmia, reperfusion injury, and the like, which are observed in ischemic heart diseases (e.g. myocardial infarction, angina pectoris, etc.).
    Type: Grant
    Filed: December 22, 1995
    Date of Patent: January 28, 1997
    Assignee: Kanebo, Ltd.
    Inventors: Manabu Hori, Ikuo Watanabe, Hiroshi Ohtaka, Kengo Harada, Joji Maruo, Tominori Morita, Takeshi Yamamoto, Hisayoshi Tsutsui
  • Patent number: 5595999
    Abstract: Compounds of the formula ##STR1## wherein L, M, R, T and X are set forth in the description, as well as hydrates or solvates thereof, which inhibit thrombin-induced platelet aggregation and clotting of fibrinogen in plasma, are described. The compounds of formula I are prepared by amidination or, depending on whether L is NH or O, by amide formation or esterification.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: January 21, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Jean Ackermann, David Banner, Klaus Gubernator, Paul Hadvary, Kurt Hilpert, Klaus M uller, Ludvik Labler, G erard Schmid, Thomas B. Tschopp, Hans P. Wessel, Beat Wirz
  • Patent number: 5595988
    Abstract: Antiallergic triazolo(pyrrolo, thieno or furano)azepines of formula ##STR1## the pharmaceutically acceptable addition salts and stereochemically isomeric forms thereof, whereineach of the dotted lines independently represents an optional bond;-E-G- is a bivalent radical of formula--X--C(R.sup.1).dbd.CH-- (a-1); or--CH.dbd.C(R.sup.2)--X-- (a-2);X represents O, S or NR.sup.3 ;R.sup.3 represents hydrogen, C.sub.1-6 alkyl or C.sub.1-4 alkylcarbonyl;-B.dbd.D- is a bivalent radical of formula--C(R.sup.4).dbd.N-- (b-1); or--N.dbd.C(R.sup.5)-- (b-2);L represents hydrogen; C.sub.1-6 alkyl; substituted C.sub.1-6 alkyl; C.sub.3-6 alkenyl; C.sub.3-6 alkenyl substituted with aryl; or,L represents a radical of formula -Alk-Y-Het.sup.1 (c-1), -Alk-NH--CO-Het.sup.2 (c-2) or -Alk-Het.sup.3 (c-3). Compositions comprising said compounds, processes of preparing the same and intermediates in the preparation thereof.
    Type: Grant
    Filed: May 8, 1995
    Date of Patent: January 21, 1997
    Assignee: Janssen Pharmaceutica N.V.
    Inventors: Frans E. Janssens, Jean F. A. Lacrampe, Isabelle N. C. Pilatte
  • Patent number: 5593989
    Abstract: New compounds of formula: ##STR1## wherein A--B, X, Y, R and n are as defined in the description. The geometric isomers, racemate and optical isomers thereof and the addition salts with pharmaceutically acceptable acids, and medicinal products containing the same are useful for treating psychotic disorders, depression, Parkinson's disease, memory disorders and disorders associated with drug abuse.
    Type: Grant
    Filed: June 1, 1995
    Date of Patent: January 14, 1997
    Assignee: Adir et Compagnie
    Inventors: Jean-Louis Peglion, Joel Vian, Bertrand Goument, Mark Millan, Val erie Audinot, Jean-Charles Schwartz, Pierre Sokoloff
  • Patent number: 5593986
    Abstract: The present invention includes novel (7R)-7-(acylamino)-3-(arylthio)-3-cephem-4-carboxylic acids or their pharmacologically acceptable salts which exhibit antibiotic activity against a wide spectrum of organisms including organisms which are resistant to .beta.-lactam antibiotics and are useful as antibacterial agents. The invention also relates to novel intermediates useful for making the novel compounds of the present invention and to novel methods for producing the novel compounds and intermediate compounds.
    Type: Grant
    Filed: March 29, 1995
    Date of Patent: January 14, 1997
    Assignee: Microcide Pharmaceuticals, Inc.
    Inventors: Burton G. Christensen, In-Seop Cho, Tomasz W. Glinka, Scott J. Hecker
  • Patent number: 5593979
    Abstract: Disclosed are novel pyrido[2,3-b][1,4]benzodiazepines. These compounds are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.
    Type: Grant
    Filed: December 29, 1994
    Date of Patent: January 14, 1997
    Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.
    Inventors: Karl D. Hargrave, Ernest Cullen, John R. Proudfoot, Karl G. Grozinger, Kollol Pal, Julian Adams
  • Patent number: 5594135
    Abstract: The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
    Type: Grant
    Filed: October 11, 1995
    Date of Patent: January 14, 1997
    Assignee: Hoffmann-La Roche Inc.
    Inventors: J urgen Geiwiz, Erwin G otschi, Paul Hebeisen, Helmut Link, Thomas L ubbers
  • Patent number: 5591774
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle malic acid or a topically effective salt thereof.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: January 7, 1997
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5589505
    Abstract: A method for visibly reducing a facial wrinkle by topically applying to the wrinkle quinic acid or a topically effective salt thereof, or quinolactone.
    Type: Grant
    Filed: June 5, 1995
    Date of Patent: December 31, 1996
    Assignee: Tristrata Technology, Inc.
    Inventors: Ruey J. Yu, Eugene J. Van Scott
  • Patent number: 5589473
    Abstract: The present invention relates to a compound of the formula ##STR1## wherein X.sup.1, R.sup.1, R.sup.2, OP, R.sup.3, R.sup.4, R.sup.5, R.sup.6, and R.sup.0 are as described herein, and their pharmaceutically acceptable salts thereof carrying an acidic and/or basic substituent.The compound of formula I as well as their pharmaceutically acceptable salts inhibit DNA gyrase activity in bacteria and possess antibiotic, especially antibacterial activity against microorganisms and can be used in the control or prevention of infectious diseases.
    Type: Grant
    Filed: March 20, 1995
    Date of Patent: December 31, 1996
    Assignee: Hoffmann-La Roche Inc.
    Inventors: J urgen Geiwiz, Erwin G otschi, Paul Hebeisen, Helmut Link, Thomas L ubbers
  • Patent number: 5587463
    Abstract: The present invention involves a novel tripyrrole dimethine-derived "expanded porphyrin" (texaphyrin), the synthesis of such compounds, their analogs or derivatives and their uses. These expanded porphyrin-like macrocycles are efficient chelators of divalent and trivalent metal ions. Metal complexes of these compounds are active as photosensitizers for the generation of singlet oxygen and thus potentially for inactivation or destruction of human immunodeficiency virus (HIV-1), mononuclear or other cells infected with such virus and tumor cells as well. A variety of texaphyrin derivatives have been produced and many more are readily obtainable. Various metal (e.g., transition, main group, and lanthanide) complexes with the texaphyrin and texaphyrin derivatives of the present invention have unusual water solubility and stability which render them particularly useful. These metallotexaphyrin complexes have optical properties making them unique as compared to existing porphyrin-like or other macrocycles.
    Type: Grant
    Filed: March 8, 1994
    Date of Patent: December 24, 1996
    Assignee: Board of Regents, The University of Texas System
    Inventors: Jonathan L. Sessler, Gregory W. Hemmi, Toshiaki Murai
  • Patent number: 5587476
    Abstract: The invention relates to an addition compound which is obtainable by reaction of a diamine of the formula I, ##STR1## where R.sup.1 is (C.sub.2 -C.sub.4)-alkylene or 1,2- or 1,3-cyclo-(C.sub.3 -C.sub.7)-alkylene andR.sup.2 and R.sup.3, which are identical or different, are (C.sub.1 -C.sub.3)-alkyl or hydrogen orR.sup.2 and R.sup.3 together are (C.sub.2 -C.sub.4)-alkylene, with fullerenes C.sub.60 and/or C.sub.70. The fullerene derivatives are useful as electrically conducting materials.
    Type: Grant
    Filed: February 15, 1995
    Date of Patent: December 24, 1996
    Assignee: Hoechst Aktiengesellschaft
    Inventors: Klaus-Dieter Kampe, Hans-Ulrich ter Meer, Norbert K. Egger, Martin A. Vogel