Bicyclo Ring System Which Contains The Hetero Ring As One Of The Cyclos Patents (Class 540/593)
  • Patent number: 5929069
    Abstract: A compound represented by the formula (I) or (II) or a salt thereof wherein R.sup.1 represents hydrogen atom or a C.sub.1-6 alkyl group; R.sup.2 and R.sup.3 independently represent a hydrogen atom or a C.sub.1-6 alkyl group, or R.sup.2 and R.sup.3 may combine together to represent a 5- or 6-membered cycloalkyl group; R.sup.4 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.5 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; R.sup.6 represents a hydrogen atom or a C.sub.1-6 alkyl group; x represents --NR.sup.7 --, --O--, --CHR.sup.7 -- or --S-- in which R.sup.7 represents, for example, a hydrogen atom or a C.sub.1-6 alkyl group; and Y represents a phenylene group or a pyridinediyl group. The compounds are useful as agents for enhancing the activities of retinoid compounds.
    Type: Grant
    Filed: September 20, 1996
    Date of Patent: July 27, 1999
    Assignee: Institute of Medicinal Molecular Design, Inc.
    Inventor: Koichi Shudo
  • Patent number: 5914319
    Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: June 22, 1999
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5885967
    Abstract: This invention relates to peptide derivatives, pharmaceutical formulations containing those compound and methods of their use as thrombin inhibitors.
    Type: Grant
    Filed: March 4, 1994
    Date of Patent: March 23, 1999
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5874427
    Abstract: This invention provides novel 5-HT.sub.1F agonists of the Formula ##STR1## in which X, Y, E, R, A, B, and n are as defined in the specification, which are useful for the treatment of migraine and associated disorders.
    Type: Grant
    Filed: April 14, 1998
    Date of Patent: February 23, 1999
    Assignee: Eli Lilly and Company
    Inventors: Sandra A. Filla, Joseph H. Krushinski, Jr., John Mehnert Schaus
  • Patent number: 5863924
    Abstract: The disclosed pyrimidine derivatives, and pharmaceutically acceptable salts and N-oxides thereof, exhibit useful pharmacological properties, in particular use as selective 5HT.sub.2B -antagonists. The invention is also directed to formulations and methods for treatment.
    Type: Grant
    Filed: May 20, 1997
    Date of Patent: January 26, 1999
    Assignee: Syntex (U.S.A.) Inc.
    Inventors: Jacob Berger, Lee Allen Flippin, Robert Greenhouse, Saul Jaime-Figueroa, Yanzhou Liu, Aubry Kern Miller, David George Putman, Klaus Kurt Weinhardt, Shu-Hai Zhao
  • Patent number: 5814642
    Abstract: A novel compound of the formula ##STR1## wherein Ar represents a tetracyclic fused heterocyclic group which may be substituted; R.sup.1 represents H or a hydrocarbon group which may be substituted; Y represents an amino acid or nitrogen-containing saturated heterocyclic group which may be substituted, its salt, inhibiting excellent cholinesterase inhibitory activity and monoamine uptake inhibitory activity, thus being useful as therapeutic and/or prophylactic medicaments of senile dementia.
    Type: Grant
    Filed: July 30, 1996
    Date of Patent: September 29, 1998
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto
  • Patent number: 5811374
    Abstract: New 3-arylpyrrolidine-2,4-dione derivatives of the formula (I): ##STR1## in which the variables A, B, E, R, X, Y, Z and n are set forth in the specification, are useful as insecticides, acaricides, and herbicides.
    Type: Grant
    Filed: June 7, 1995
    Date of Patent: September 22, 1998
    Assignee: Bayer Aktiengesellschaft
    Inventors: Heinz-Jurgen Bertram, Reiner Fischer, Bernd-Wieland Kruger, Christoph Erdelen, Klaus Lurssen, Robert R. Schmidt, Hans-Joachim Santel
  • Patent number: 5792761
    Abstract: A compound which inhibits human thrombin and where has the structure ##STR1##
    Type: Grant
    Filed: August 8, 1997
    Date of Patent: August 11, 1998
    Assignee: Merck & Co., Inc.
    Inventors: Mark E. Fraley, Adel M. Naylor-Olsen, Randall W. Hungate, Joseph P. Vacca
  • Patent number: 5789402
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: August 4, 1998
    Assignee: Eli Lilly Company
    Inventors: James E. Audia, David J. Hibschman, Joseph H. Krushinski, Jr., Thomas E. Mabry, Jeffrey S. Nissen, Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson, David T. Wong
  • Patent number: 5753644
    Abstract: An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist.The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.
    Type: Grant
    Filed: October 15, 1996
    Date of Patent: May 19, 1998
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Kazuyoshi Kitano, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5741789
    Abstract: A series of hetero-oxy alkanamines are effective pharmaceuticals for the treatment of conditions related to or affected by the reuptake of serotonin and by the serotonin 1.sub.A receptor. The compounds are particularly useful for alleviating the symptoms of nicotine and tobacco withdrawal, and for the treatment of depression and other conditions for which serotonin reuptake inhibitors are used.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: April 21, 1998
    Assignee: Eli Lilly and Company
    Inventors: David J. Hibschman, Joseph H. Krushinski, Jr., Kurt Rasmussen, Vincent P. Rocco, John M. Schaus, Dennis C. Thompson
  • Patent number: 5726159
    Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: March 10, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Robert T. Shuman, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5723633
    Abstract: A pyran derivative has a structure ofR.sup.2 R.sup.3 C.dbd.(C.sub.5 H.sub.2 R.sup.1 O)--(CH.dbd.CH).sub.n --C.sub.6 H.sub.2 R.sup.6 R.sup.7 --NR.sup.4 R.sup.5wherein n is 3 or 4; R.sup.1 is a proton, alkyl or phenyl group; each of R.sup.2 and R.sup.3 is independently a cyano, alkoxycarbonyl having an alkyl, acyl having an alkyl, aracyl having phenyl, sulfonyl, aryl, or aryloxy; each of R.sup.4 and R.sup.5 is an alkyl group; and each of R.sup.6 and R.sup.7 is a proton, provided that R.sup.4 and R.sup.5 are alkyl groups, and a pair of R.sup.4 and R.sup.6 as well as a pair of R.sup.5 and R.sup.7 can be bonded to each other to form a heterocycle.A photosensitive composition comprises a polymerizable compound, a polymerization initiator and a photosensitizer which is the pyran derivative. A photosensitive resin composition comprises a crosslinkable polymer, a crosslinking agent and the photosensitizer.
    Type: Grant
    Filed: December 20, 1995
    Date of Patent: March 3, 1998
    Assignee: Canon Kabushiki Kaisha
    Inventors: Shin Kobayashi, Susumu Matsumura, Naosato Taniguchi, Yoko Yoshinaga, Toshiyuki Sudo, Hideki Morishima, Tadashi Kaneko
  • Patent number: 5719156
    Abstract: The invention relates to compounds of the formulas ##STR1## wherein Z, R.sub.c, y, x, l.sub.1, l.sub.2, l.sub.3, u, R.sub.4,R.sub.c', n, R.sub.1, R.sub.2, and R.sub.3, are as described herein. These compounds are neurokinin antagonists. These compounds are useful in the treatment of chronic airway diseases such as asthma.
    Type: Grant
    Filed: May 2, 1995
    Date of Patent: February 17, 1998
    Assignee: Schering Corporation
    Inventors: Ho-Jane Shue, Neng-Yang Shih, John Piwinski, Xiao Chen, David J. Blythin
  • Patent number: 5719141
    Abstract: Compounds of the formula I ##STR1## in which R.sub.1 is arylamino, N-aryl-N-(lower alkoxy-lower alkyl)-amino, N-aryl-N-aryl-lower alkyl-amino or heterocyclyl bonded via a ring carbon atom, X is a carbonyl or methylene group, R.sub.2 and R.sub.3 independently of one another are hydrogen or lower alkyl or, together with the carbon atom with which they are bonded, are a cycloalkylidene radical, R.sub.4 is hydrogen, lower alkyl, lower alkanoyl or lower alkoxycarbonyl, R.sub.5 is hydroxyl, lower alkanoyloxy or lower alkoxycarbonyloxy, R.sub.6 is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl, cycloalkyl-lower alkyl, aryl-lower alkyl or heteroaryl-lower alkyl having 5 to 7 ring atoms in the heteroaryl ring and R.sub.7 is hydrogen or lower alkyl, or R.sub.6 and R.sub.7, together with the carbon atom with which they are bonded, are a cydoalkylidene radical and R.sub.
    Type: Grant
    Filed: September 8, 1995
    Date of Patent: February 17, 1998
    Assignee: Novartis Corporation
    Inventors: Vittorio Rasetti, Heinrich Rueger, Jurgen Klaus Maibaum, Robert Mah, Markus Grutter, Nissim Claude Cohen
  • Patent number: 5710150
    Abstract: Benzazepine derivatives represented by the following general formula (I) useful as arginine vasopressin antagonists or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and difluorobenzazepinone derivatives represented by the following general formulae (II) and (III) which are useful as production intermediates of the compound (I).
    Type: Grant
    Filed: February 26, 1996
    Date of Patent: January 20, 1998
    Assignee: Yamanouchi Pharmaceutical Co., Ltd.
    Inventors: Nobuaki Taniguchi, Akihiro Tanaka, Akira Matsuhisa, Ken-ichiro Sakamoto, Hiroyuki Koshio, Takeyuki Yatsu
  • Patent number: 5710130
    Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: January 20, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5707966
    Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: January 13, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5708174
    Abstract: Compounds of formula (I), wherein formula I consists of formulae (I-1) to (I-4), which are defined in the specification, and pharmaceutically acceptable salts thereof, and the use of a compound of formula I or a pharmaceutically acceptable salt thereof, and their use as pharmaceuticals in the treatment of gastrointestinal disorders, cardiovascular disorders and CNS disorder.
    Type: Grant
    Filed: April 11, 1995
    Date of Patent: January 13, 1998
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis David King, Laramie Mary Gaster, Graham Francis Joiner, Keith Raymond Mulholland, Shirley Katherine Rahman
  • Patent number: 5705487
    Abstract: This invention relates to thrombin inhibiting compounds having the Formula IX--Y--NH--(CH.sub.2).sub.r --G Iwhere X, Y, r and G have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: September 1, 1995
    Date of Patent: January 6, 1998
    Assignee: Eli Lilly and Company
    Inventors: Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5698692
    Abstract: A compound represented by the general formula (I) and a pharmaceutically acceptable salt and solvate thereof having an effect for inhibiting the agglutination of platelets is disclosed: ##STR1## wherein R.sup.1 represents a group --W--(CH.sub.2).sub.i --COOR.sup.3,R.sup.2 represents a hydrogen atom or a group --W--(CH.sub.2).sub.i --COOR.sup.3 or --OR.sup.4,X represents --CH.dbd. or --N.dbd.,Y represents(i) a group --(CO).sub.k --N(R.sup.5)--Z--, wherein Z represents a bond or a group --(CH.sub.2).sub.m --CO-- or a group --(CH.sub.2).sub.m --CHR.sup.6 --,(ii) a group --(CH.sub.2).sub.m --N(R.sup.5)--(CO).sub.k --, or(iii) a group --(CO).sub.k --Het, wherein Het represents a five- or six-membered heterocyclic ring comprising a nitrogen atom,A represents(i) the following groups (II), (III) or (IV) ##STR2## B represents a bond, C.sub.1-6 alkylene or C.sub.2-6 alkenylen.
    Type: Grant
    Filed: October 18, 1996
    Date of Patent: December 16, 1997
    Assignee: Meiji Seika Kabushiki Kaisha
    Inventors: Kiyoaki Katano, Shokichi Ohuchi, Eiki Shitara, Masaro Shimizu, Kazue Yaegashi, Tomoaki Miura, Yasuko Isomura, Hiroyuki Iida, Midori Ishikawa, Kenji Asai, Emiko Hatsushiba, Mami Kawaguchi, Takashi Tsuruoka
  • Patent number: 5696112
    Abstract: This invention relates to bicyclic non-peptide vasopressin antagonists useful in treating conditions where decreased vasopressin levels are desired, in conditions with excess renal water reabsorption and in conditions with increased vascular resistance and coronary vasoconstriction, the compounds of this invention having the core structure of ##STR1## wherein: E--Y is selected from the moieties --CH.dbd.CH--, --CH.sub.2 CH.sub.2 --, and ##STR2## the moiety ##STR3## includes an optionally substituted, fused 6-membered heterocyclic aromatic ring containing two nitrogen atoms, a fused 5-membered heterocyclic aromatic ring containing either a) one heteroatom selected from O, S or N; b) two N atoms; or one N atom and one O or S atom;and R.sup.1, R.sup.2, R.sup.3 and R.sub.b are as defined herein.
    Type: Grant
    Filed: January 17, 1995
    Date of Patent: December 9, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Efren G. Delos Santos
  • Patent number: 5688790
    Abstract: This invention relates to compounds of formula (I): ##STR1## wherein R.sup.1 represents C.sub.1-4 alkyl; andR.sup.2, R.sup.3, R.sup.4 and R.sup.5 each independently represent hydrogen, halogen, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, C.sub.1-4 alkoxyC.sub.1-4 alkyl, C.sub.1-4 alkylsulphonyl, trifluoromethylsulphonyl; optionally substituted arylsulphonyl, optionally substituted heteroarylsulphonyl, optionally substituted aralkylsulphonyl, optionally substituted heteroaralkylsulphonyl, nitro, cyano, amino, mono- or di-alkylamino, trifluoromethyl, trifluoromethoxy, hydroxyl, hydroxyC.sub.1-4 alkyl, C.sub.1-4 alkylthio, C.sub.1-4 alkanoyl, C.sub.1-4 alkoxycarbonyl, aminosulphonyl, or mono- or diC.sub.1-4 alkylaminosulphonyl; orR.sup.1 and R.sup.2 together form a linking chain --(CH.sub.2).sub.m Op; (wherein m is 2 to 4 and p is zero or 1) which chain may be optionally substituted by one or two C.sub.1-4 alkyl groups;and Y represents a group of formula (.alpha.
    Type: Grant
    Filed: September 28, 1995
    Date of Patent: November 18, 1997
    Assignee: SmithKline Beecham Plc
    Inventors: Michael Stewart Hadley, Christopher Norbert Johnson, Geoffrey Stemp
  • Patent number: 5677299
    Abstract: Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin antagonist.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: October 14, 1997
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Keizo Kan, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5674863
    Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: October 7, 1997
    Assignee: Genentech, Inc.
    Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
  • Patent number: 5674879
    Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders.
    Type: Grant
    Filed: March 3, 1995
    Date of Patent: October 7, 1997
    Assignee: G.D. Searle & Co.
    Inventors: Robert E. Manning, Horng-Chih Huang
  • Patent number: 5674865
    Abstract: A benzodiazepinedione derivative which acts as a nonpeptidyl platelet aggregation inhibitor is provided. This inhibitor potently inhibits fibrinogen binding to the GPII.sub.b III.sub.a receptor and is provided in therapeutic compositions for the treatment of diseases for which blocking platelet aggregation is indicated. These nonpeptidyl inhibitors are provided in combination with thrombolytics and anticoagulants.
    Type: Grant
    Filed: May 26, 1995
    Date of Patent: October 7, 1997
    Assignee: Genentech, Inc.
    Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
  • Patent number: 5656627
    Abstract: The present invention relates to novel classes of compounds which are inhibitors of interleukin-1.beta. converting enzyme. The ICE inhibitors of this invention are characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting ICE activity and consequently, may be advantageously used as agents against interleukin-1 mediated diseases, including inflammatory diseases, autoimmune diseases and neurodegenerative diseases. This invention also relates to methods for inhibiting ICE activity and methods for treating interleukin-1 mediated diseases using the compounds and compositions of this invention.
    Type: Grant
    Filed: March 17, 1995
    Date of Patent: August 12, 1997
    Assignee: Vertex Pharmaceuticals, Inc.
    Inventors: Guy W. Bemis, Julian M. C. Golec, David J. Lauffer, Michael D. Mullican, Mark A. Murcko, David J. Livingston
  • Patent number: 5654297
    Abstract: This invention relates to new bicyclic non-peptide vasopressin antagonists which are useful in treating conditions where decreased vasopressin levels are desired, such as in congestive heart failure, in disease conditions with excess renal water reabsorption and in conditions with increased vascular resistance and coronary vasoconstriction.
    Type: Grant
    Filed: June 2, 1995
    Date of Patent: August 5, 1997
    Assignee: American Cyanamid Company
    Inventors: Jay D. Albright, Efren G. Delos Santos
  • Patent number: 5654296
    Abstract: The compound ##STR1## wherein ring A represents a benzene ring;Ar represents an aromatic group;R.sup.1 and R.sup.2 independently represent hydrogen, acyl or hydrocarbon group or R.sup.1 and R.sup.2 taken together with the adjacent nitrogen atom represent a nitrogen-containing heterocyclic group;m represents an integer of 1 to 6;n represents an integer of 2 to 3;- - - - - represents a single bond or a double bond;X stands for --O-- or --NR.sup.3 -- in which R.sup.3 represents hydrogen, acyl or hydrocarbon group where - - - - - is a single bond or .dbd.N-- where - - - - - is a double bond has excellent GnRH receptor antagonizing activity, calcium antagonizing and monoamine-uptake inhibiting activities and and value as a prophylactic/therapeutic drug for sex hormone-dependent diseases and for central nervous system diseases.
    Type: Grant
    Filed: December 6, 1996
    Date of Patent: August 5, 1997
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Kaneyoshi Kato, Yoshihiro Sugiura, Koichi Kato, Yasuo Nagai
  • Patent number: 5650406
    Abstract: A compound represented by general formula (1) or an innocuous salt thereof, a process for producing the same, and a schizophrenia remedy containing the same as the active ingredient (wherein the nitrogeneous ring B represents 3-azabicyclo [3.2.2] nonan-3-yl or 4-azatricyclo [4.3.1.1.sup.3.8 ] undecan-4-yl; and R represents hydrogen, lower alkyl, lower alkoxy, hydroxy or halogen). The above compound and salt have a high affinity for sigma-binding sites and are useful as an antischizophrenic drug.
    Type: Grant
    Filed: October 8, 1996
    Date of Patent: July 22, 1997
    Assignee: Asahi Kasei Kogyo Kabushiki Kaisha
    Inventors: Nobuyuki Takahashi, Daisuke Mochizuki
  • Patent number: 5639745
    Abstract: Disclosed are compounds, compositions and methods for inhibiting interleukin-1.beta. protease activity. The compounds, bicyclic derivatives of aldehydes and .alpha.-substituted methyl ketones, have the formula (A) set out herein.
    Type: Grant
    Filed: May 25, 1995
    Date of Patent: June 17, 1997
    Assignee: Sanofi
    Inventors: Roland E. Dolle, Prasad V. Chaturvedula, Tina Morgan Ross, Stanley J. Schmidt
  • Patent number: 5622947
    Abstract: An object of the present invention is to provide a vasopressin antagonist and oxytocin antagonist.The vasopressing antagonist and oxytocin antagonist according to the present invention contain, as the active ingredient, a benzoheterocyclic compound represented by the general formula (1): ##STR1## (wherein R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and the carbon-carbon bond between 4- and 5-positions in the benzoazepine skeleton are the same as defined in claims 1, 2 and 3.) or salt thereof.
    Type: Grant
    Filed: May 25, 1994
    Date of Patent: April 22, 1997
    Assignee: Otsuka Pharmaceutical Co., Ltd.
    Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Kazuyoshi Kitano, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5607944
    Abstract: The invention relates to bicyclic heterocyclic compounds of general formula ##STR1## wherein A to F, Y.sub.1 and Y.sub.2 are defined as in claim 1, the tautomers thereof, the stereoisomers thereof including their mixtures, and salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable pharmacological properties, preferably aggregation-inhibiting effects, pharmaceutical compositions containing the compounds and processes for preparing them as well as new intermediate products of general formula Ia.
    Type: Grant
    Filed: July 31, 1995
    Date of Patent: March 4, 1997
    Assignee: Karl Thomae GmbH
    Inventors: G unter Linz, Frank Himmelsbach, Helmut Pieper, Volkhard Austel, Thomas M uller, Johannes Weisenberger, Brian Guth
  • Patent number: 5599793
    Abstract: This invention relates to L-arginine aldehyde derivatives, having the Formula I ##STR1## where X and Y have the values defined in the description, as well as pharmaceutical formulations containing those compounds and methods of their use as thrombin inhibitors, coagulation inhibitors, and thromboembolic disorder agents.
    Type: Grant
    Filed: March 2, 1995
    Date of Patent: February 4, 1997
    Assignee: Eli Lilly and Company
    Inventors: Nickolay Y. Chirgadze, Aaron L. Schacht, Gerald F. Smith, Michael R. Wiley
  • Patent number: 5597816
    Abstract: Pyrazoloazepino-substituted oximes, having the formula ##STR1## wherein R is ##STR2## where R.sup.5 is --(CH.sub.2).sub.c -- and c is 3-6 are disclosed. These compounds are useful for the treatment of atherosclerosis and hypercholesterolemia.
    Type: Grant
    Filed: June 6, 1995
    Date of Patent: January 28, 1997
    Assignee: The Upjohn Company
    Inventors: Scott D. Larsen, Charles H. Spilman
  • Patent number: 5552398
    Abstract: Compounds of formula (I), ##STR1## wherein L is N or CR.sub.c, wherein R.sub.c is hydrogen, alkoxy, halo, alkyl or cyano; Q is NR.sub.1, CH.sub.2, O, or S; R.sub.a is hydrogen, halo, alkyl, amino, nitro or alkoxy; R.sub.b is hydrogen, halo, alkyl or alkoxy; R.sub.1 is hydrogen, alkyl, alkenyl, aralkyl, alkanoyl, or alkanoylalkyl; R.sub.2 is alkoxy; R.sub.3 is hydrogen, chloro or fluoro; R.sub.4 is hydrogen, alkyl, amino optionally substituted by alkyl, halo, hydroxy or alkoxy; R.sub.5 is hydrogen, halo, alkyl, alkoxy, nitro, amino or alkylthio; R.sub.6 is hydrogen, halo, alkyl, alkoxy or amino; n is 0, 1, 2, 3, or 4; p and m are independently 0, 1 or 2; and R.sub.q is hydrogen or C.sub.1-6 are 5-HT.sub.4 receptor antagonists.
    Type: Grant
    Filed: November 14, 1994
    Date of Patent: September 3, 1996
    Assignee: SmithKline Beecham p.l.c.
    Inventors: Francis D. King, Laramie M. Gaster, Paul A. Wyman
  • Patent number: 5550162
    Abstract: Compounds of the formula: ##STR1## in which R.sub.1 represents a hydrogen or halogen atom or a methyl or C.sub.1 -C.sub.4 alkoxy group, R'.sub.1 represents a hydrogen or halogen atom, R".sub.1 represents a hydrogen atom or a methoxy group, R.sub.3 represents a C.sub.1 -C.sub.3 alkyl group, R.sub.4 represents a 2,3-dihydro-1H-inden-2-yl, 2,3-dihydro-1H-inden-1-yl or 1,2,3,4-tetrahydronaphthalen-1-yl group, or R.sub.3 and R.sub.4 together form, with the adjacent nitrogen atom, a 1,2,3,4-tetrahydroisoquinol-2-yl, 6,7-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 5,8-dimethoxy-1,2,3,4-tetrahydroisoquinol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[3,4-b]indol-2-yl, 1,2,3,4-tetrahydro-9H-pyrido[4,3-b]indol-3-yl, 4,5,6,7-tetrahydrothieno[2,3-c]pyrid-6-yl, 2,3-dihydro-1H-isoindol-2-yl or 2,3,4,5-tetra-hydro-1H-3-benzazepin-3-yl, group are useful in the treatment of cerebral disorders.
    Type: Grant
    Filed: February 20, 1995
    Date of Patent: August 27, 1996
    Assignee: SYNTHELABO
    Inventors: Jonathan Frost, Pascal George, Patrick Pasau, R egine Bartsch, Corinne Rousselle, Paul H. Williams, Jean C. Muller
  • Patent number: 5532240
    Abstract: A condensed thiophene compound represented by general formula: ##STR1## or a pharmaceutically acceptable salt thereof, wherein ring S represents a thiophene ring; R.sup.1 represents hydrogen, halogen, alkyl, etc.; R.sup.2 represents hydrogen, alkyl, acyl, etc.; G represents --CH.sub.2 --, --CH(OH)--, --CO--, etc.; Q represents alkylene; T represents --N(Rb)(Rc) (wherein Rb, Rc represents each alkyl etc.; or alternatively Rb and Rc are combined together to form cyclic amino); D represents --CH.sub.2 -- or --S--; A and B represent each carbonyl or thiocarbonyl, or are null; and m and n represent each 0, 1 to 4, provided that m+n represents an integer of 4 or less.This compound is useful as an antipsychotic drug having a reduced extrapyramidal side effect.
    Type: Grant
    Filed: July 8, 1994
    Date of Patent: July 2, 1996
    Assignee: Yoshitomi Pharmaceutical Industries, Ltd.
    Inventors: Tohru Nakao, Yuji Ono, Masahiro Bougauchi, Yasuto Morimoto
  • Patent number: 5498609
    Abstract: Novel benzoheterocyclic compound of the formula (1): ##STR1## and pharmaceutically acceptable salts thereof, which show excellent anti-vasopressin activity and oxytocin antagonistic activity, and are useful as a vasopressin antagonist or oxytocin antagonist.
    Type: Grant
    Filed: April 20, 1994
    Date of Patent: March 12, 1996
    Assignee: Otsuka Pharmaceutical Company, Limited
    Inventors: Hidenori Ogawa, Kazumi Kondo, Hiroshi Yamashita, Keizo Kan, Michiaki Tominaga, Yoichi Yabuuchi
  • Patent number: 5478822
    Abstract: Compounds of the formula ##STR1## wherein n is 1 to 5 and R is hydrogen, C.sub.1 to C.sub.4 alkyl, arylalkyl having from one to four carbon atoms in the alkyl moiety or arylalkyl substituted with one or more substituents selected independently from the group consisting of halogen, nitro, cyano, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, C.sub.1 to C.sub.6 halosubstituted alkyl, C.sub.1 to C.sub.6 hydroxysubstituted alkyl, C.sub.2 to C.sub.7 alkoxycarbonyl and aminocarbonyl, and the pharmaceutically acceptable salts thereof, inhibit the enzyme lipoxygenase and are useful in treating allergy and inflammatory and cardiovascular conditions for which the action of lipoxygenase has been implicated. These compounds form the active ingredient in pharmaceutical compositions for treating such conditions.
    Type: Grant
    Filed: December 17, 1993
    Date of Patent: December 26, 1995
    Assignee: Pfizer Inc.
    Inventors: Yoko Hoshino, Takafumi Ikeda
  • Patent number: 5462934
    Abstract: A compound of the formula: ##STR1## wherein R.sup.1 is H or an optionally substituted hydrocarbon or acyl group; ring A is an optionally further substituted benzene ring; n is an integer of 1 to 10; R.sup.2, R.sup.3 and R.sup.4 are H or an optionally substituted hydrocarbon group; R.sup.3 and R.sup.4 may form an optionally substituted heterocyclic group, taken together with the adjacent nitrogen atom; k is an integer of 0 to 3; and m is an integer of 1 to 8; provided that when k=0 and m=2, n is an integer of not less than 2 or a pharmaceutically acceptable salt thereof, exhibiting excellent cholinesterase inhibitory activity and monoamine reuptake inhibitory activity, thus being useful as therapeutic/prophylactic medicaments of senile dementia.
    Type: Grant
    Filed: March 4, 1993
    Date of Patent: October 31, 1995
    Assignee: Takeda Chemical Industries
    Inventors: Giichi Goto, Masaomi Miyamoto, Yuji Ishihara
  • Patent number: 5461063
    Abstract: Compounds of formula (I), and salts and prodrugs thereof: ##STR1## wherein X represents O or S;Y represents (CH.sub.2).sub.m, where m is 0 or 1;Z represents (CH.sub.2).sub.n, where n is 0 or 1;R.sup.1 represents optionally substituted phenyl;R.sup.2 is phenyl, naphthyl, indazolyl, thienyl, furyl, pyridyl, thiazolyl, tetrazolyl, quinolyl, benzhydryl or benzyl;R.sup.3 is H, COR.sup.a, CO.sub.2 R.sup.a C(COOR).sub.2, C(CONR.sup.a R.sup.b).sub.2, COCONR.sup.a R.sup.b, COCO.sub.2 R.sup.a, C.sub.1-6 alkyl optionally substituted by a group selected from (CO.sub.2 R.sup.a, CONR.sup.a R.sup.b, hydroxy, cyano, COR.sup.a, NR.sup.a R.sup.b, C(NOH)NR.sup.a R.sup.b, CONHphenyl(C.sub.1-4 alkyl), COCO.sub.2 R.sup.a, C(.dbd.NR.sup.a)NR.sup.b NR.sup.c CO.sub.2 R.sup.d, CONHNR.sup.a R.sup.b, C(S)NR.sup.a R.sup.b, CONR.sup.a C.sub.1-6 alkylR.sup.12, CONR.sup.13 C.sub.2-6 alkynyl, CONR.sup.13 C.sub.2-6 alkenyl, COCONR.sup.a R.sup.b, CONR.sup.a C(NR.sup.b)NR.sup.c R.sup.d, CONR.sup.13 SO.sub.2 R.sup.a, SO.sub.2 R.sup.13 COR.sup.
    Type: Grant
    Filed: August 5, 1993
    Date of Patent: October 24, 1995
    Assignee: Merck Sharp & Dohme Limited
    Inventors: Fintan Kelleher, Richard T. Lewis
  • Patent number: 5446040
    Abstract: Compounds of the formula ##STR1## wherein the variables R.sub.1 and p and the rings A and B are as defined in claim 1, and, where appropriate, tautomers thereof, in each case in free form or in the form of a salt, can be used as agrochemical active ingredients and can be prepared in a manner known per se.
    Type: Grant
    Filed: November 29, 1993
    Date of Patent: August 29, 1995
    Assignee: Ciba-Geigy Corporation
    Inventor: Harald Walter
  • Patent number: 5426105
    Abstract: Conformationally restricted compounds are described which are therapeutically effective as angiotensin II antagonists for the treatment of circulatory disorders. Compounds of particular interest are of Formula I ##STR1## wherein W is N or CH.sub.2 ; wherein X is N or CR.sup.2 ; wherein Y is (CH.sub.2).sub.n and n is 1 to 3; wherein Z is C.dbd.R.sup.3 or CR.sup.4 R.sup.5, or wherein Y and Z together forms --CR.sup.6 .dbd.CR.sup.7 --, --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 or --CR.sup.6 .dbd.CR.sup.7 --CH.sub.2 --CH.sup.2 --; wherein the remainder of the variables are as defined in the specification; or a pharmaceutically suitable salt or tautomer thereof.
    Type: Grant
    Filed: September 24, 1993
    Date of Patent: June 20, 1995
    Assignee: G.D. Searle & Co.
    Inventors: Robert E. Manning, Horng-Chih Huang
  • Patent number: 5384318
    Abstract: Compounds of the formula ##STR1## and pharmaceutical compositions comprising them, wherein R.sup.1, R.sup.2, R.sup.3, W, X and Z are as defined below. The compounds are inhibitors of 5-lipoxygenase enzyme and antagonists of leukotriene B4, leukotriene C4, leukotriene D4 and leukotriene E4.
    Type: Grant
    Filed: February 21, 1992
    Date of Patent: January 24, 1995
    Assignee: Pfizer Inc.
    Inventors: James F. Eggler, Anthony Marfat, Lawrence S. Melvin, Jr., Hiroko Masamune
  • Patent number: 5378702
    Abstract: Thiadiazinones of the formula I ##STR1## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5 and n have the meaning given in claim 1, show antiarrhythmic action and are suitable for the control of cardiovascular disorders.
    Type: Grant
    Filed: July 16, 1993
    Date of Patent: January 3, 1995
    Assignee: Merck Patent Gesellschaft Mit Beschrankter Haftung
    Inventors: Rochus Jonas, Ingeborg Lues, Klaus-Otto Minck, Michael Klockow
  • Patent number: 5369084
    Abstract: Isonicotinic acid derivatives and related furo-, thieno- and pyrrolo[3,4-c]pyridin-1(3H)-one, -thione and -imine compounds having the formula ##STR1## wherein R is ##STR2## Q is O, S or NR.sup.7 ; Y is O, S or NR.sup.8 ; L is COOR.sup.9, CONR.sup.10 R.sup.11, C(.dbd.S)NR.sup.10 R.sup.11, CN, or a radical of formula ##STR3## the acceptable addition salts, the stereochemically isomeric forms and the N-oxides thereof, having herbicidal properties, compositions containing the same and methods for controlling weeds.
    Type: Grant
    Filed: May 6, 1993
    Date of Patent: November 29, 1994
    Assignee: Janssen Pharmaceutical N.V.
    Inventors: Hans-Rudolf Waespe, Guy R. E. Van Lommen, Victor K. Sipido
  • Patent number: 5292746
    Abstract: The present invention is directed to a new class of cyclic nitrones and their use as spin trapping agents.
    Type: Grant
    Filed: August 5, 1992
    Date of Patent: March 8, 1994
    Assignee: Merrell Dow Pharmaceuticals Inc.
    Inventors: Albert A. Carr, Craig E. Thomas, Ronald C. Bernotas, George Ku
  • Patent number: 5273974
    Abstract: A condensed heterocyclic derivative of the formula (I): ##STR1## wherein X is an oxygen atom, a sulfur atom or R.sup.1 --N< wherein R.sup.1 is a hydrogen atom, a hydrocarbon group which may be substituted or an acyl group which may be substituted; R.sup.2 is a hydrogen atom or a hydrocarbon group which may be substituted; ring A is a benzene ring which may be substituted, k is a whole number of 0 to 3; m is a whole number of 1 to 8; and n is a whole number of 1 to 6, or a pharmaceutically acceptable salt thereof exhibiting high colinesterase inhibitory activity, and a method for producing the same.
    Type: Grant
    Filed: November 22, 1991
    Date of Patent: December 28, 1993
    Assignee: Takeda Chemical Industries, Ltd.
    Inventors: Giichi Goto, Yuji Ishihara, Masaomi Miyamoto