Tricyclo Ring System Having The Hetero Ring As One Of The Cyclos Patents (Class 540/495)
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Patent number: 6218387Abstract: The present invention relates to compounds of the formula I, A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: October 5, 1999Date of Patent: April 17, 2001Assignees: Hoechst Aktiengesellschaft, Genetech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Karlheinz Scheunemann, Jean-Marie Ruxer, Denis Carniato, Jean-Michel Lefrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 6207663Abstract: Vitronectin receptor antagonists, their preparation and their use The present invention relates to compounds of the formula I A—B—D—E—F—G (I) in which A, B, D, E, F and G have the meanings given in the patent claims, to their preparation and to their use as medicaments. The compounds of the invention are used as vitronectin receptor antagonists and as inhibitors of bone resorption.Type: GrantFiled: October 5, 1999Date of Patent: March 27, 2001Assignees: Hoechst Atkiengesellschaft, Genentech, Inc.Inventors: Volkmar Wehner, Hans Ulrich Stilz, Anuschirwan Peyman, Jochen Knolle, Jean-Marie Ruxer, Denis Carniato, Jean-Michel LeFrancois, Thomas Richard Gadek, Robert McDowell
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Patent number: 6028081Abstract: Substituted quinolone derivatives represented by the following formula: ##STR1## wherein R.sup.1 represents a substituted or unsubstituted (hetero)aryl group, R.sup.2 represents H or an alkoxycarbonyl, substituted aminocarbonyl, cyano or like group, and R.sup.3 and R.sup.4 each independently represent H or a substituted alkyl, aryl, amino or like group, and salts thereof; pharmaceuticals containing the same. These derivatives and salts have excellent anti-ulcer activities.Type: GrantFiled: August 27, 1998Date of Patent: February 22, 2000Assignee: SSP Co., Ltd.Inventors: Yoshihisa Sada, Shigeru Adegawa, Kinichi Mogi, Haruyoshi Honda, Hiromichi Eto, Shinichi Morimoto, Junji Okawa, Norimitsu Umehara, Susumu Sato
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Patent number: 6015791Abstract: The present invention relates to certain substituted oxadiazole, thiadiazole, and triazoles, in particular those including a cycloheptane structure, that are useful as serine protease inhibitors, including inhibitors for human neutrophil elastase. Compounds of the invention are useful in treating conditions such as adult respiratory distress syndrome, septic shock, and multiple organ failure.Type: GrantFiled: December 4, 1997Date of Patent: January 18, 2000Assignee: Cortech Inc.Inventors: Albert Gyorkos, Lyle W. Spruce
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Patent number: 5985869Abstract: Novel benzoheterocyclic compounds of the formula: ##STR1## wherein R.sup.1 is H, halogen, alkyl, optionally substituted amino, alkoxy; R.sup.2 is H, halogen, alkoxy, phenylalkoxy, OH, alkyl, optionally substituted amino, carbamoyl-alkoxy, optionally substituted amino-alkoxy, optionally substituted benzoyloxy; R.sup.3 is a group: --NR.sup.4 R.sup.5 or --CO--NR.sup.11 R.sup.12 ; R.sup.4 is H, optionally substitued benzoyl, alkyl; R.sup.5 is a group: ##STR2## [R.sup.16 is halogen, optionally substituted alkyl, OH, alkoxy, alkanoyloxy, alkylthio, alkanoyl, carboxy, alkoxycarbonyl, CN, NO.sub.2, optionally substituted amino, phenyl, cycloalkyl, etc., or a group: --O--A--NR.sup.6 R.sup.7 ; m is 0 to 3], phenyl-alkoxycarbonyl, alkanoyl, phenylalkanoyl, etc.; R.sup.11 is H or alkyl; R.sup.12 is cycloalkyl or optionally substituted phenyl; and W is a group: --(CH.sub.2).sub.p (p is 3 to 5) or --CH.dbd.CH--(CH.sub.2).sub.q (q is 1 to 3), the carbon atom of these groups beign optionally replaced by O, S, SO, SO.sub.Type: GrantFiled: July 15, 1997Date of Patent: November 16, 1999Assignee: Otsuka Pharmaceutical Company, LimitedInventors: Hidenori Ogawa, Hisashi Miyamoto, Kazumi Kondo, Hiroshi Yamashita, Kenji Nakaya, Hajime Komatsu, Michinori Tanaka, Shinya Kora, Michiaki Tominaga, Yoichi Yabuuchi
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Patent number: 5917033Abstract: The present invention pertains to a method for designing inhibitors of enzyme human immunodeficiency virus type 1 reverse transcriptase which comprises the steps of:(a) providing a three dimensional model of the receptor site in the prepolymerization complex of the p66 subunit of enzyme human immunodeficiency virus type 1 reverse transcriptase and a known nonnucleoside inhibitor;(b) locating the conserved residues in the p66 subunit which constitute the nonnucleoside inhibitor binding pocket; and(c) designing a new nonnucleoside inhibitor which possesses complementary structural features and binding forces to the residues in the p66 subunit nonnucleoside inhibitor binding pocket.Type: GrantFiled: October 31, 1995Date of Patent: June 29, 1999Assignee: University of Medicine & Dentistry of New JerseyInventors: Mukund J. Modak, Prem N. S. Yadav, Janardan S. Yadav
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Patent number: 5891872Abstract: Novel compounds of Formula ##STR1## are disclosed. Also disclosed is a method of inhibiting Ras function and therefore inhibiting the abnormal growth of cells. The method comprises administering a compound of the formula to a biological system. In particular, the method inhibits the abnormal growth of cells in a mammal such as a human being.Type: GrantFiled: May 22, 1995Date of Patent: April 6, 1999Assignee: Schering CorporationInventors: Ronald J. Doll, Alan K. Mallams, Adriano Afonso, Dinanath F. Rane, F. George Njoroge, Randall R. Rossman
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Patent number: 5891871Abstract: The invention relates to substituted 2,3-benzodiazepin-4-ones which are antagonists or positive modulators of AMPA receptors, and the use thereof for treating, preventing or ameliorating neuronal loss associated with stroke, global and focal ischemia, CNS trauma, hypoglycemia and surgery, as well as treating or ameliorating neurodegenerative diseases including Alzheimer's disease, amyotrophic lateral sclerosis, Huntington's disease, Parkinson's disease and Down's syndrome, treating, preventing or ameliorating the adverse consequences of the overstimulation of the excitatory amino acids, treating or ameliorating anxiety, psychosis, convulsions, chronic pain, glaucoma, CMV retinitis, urinary incontinence, muscular spasm and inducing anesthesia, as well as for treating or ameliorating the adverse consequences of excitatory amino acid deficiency such as schizophrenia, Alzheimer's disease and malnutrition and neural maldevelopment, and as cognition enhancers.Type: GrantFiled: March 20, 1997Date of Patent: April 6, 1999Assignee: CoCensys, Inc.Inventors: Haiji Xia, Sui Xiong Cai, George Field, Nancy C. Lan, Yan Wang
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Patent number: 5877312Abstract: This invention relates to methods for preparing alkylating agents and use of the agents prepared. In particular, this invention relates to preparation methods for hydroxy halide and organooxy halide alkylating agents and their use for alkylating cyclic urea compounds.Type: GrantFiled: December 31, 1996Date of Patent: March 2, 1999Assignee: DuPont Pharmaceuticals CompanyInventors: Prabhakar Kondaji Jadhav, George Clautice Emmett, Michael Ernest Pierce
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Patent number: 5874424Abstract: 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 an IL-1 mediated disease, an apoptosis mediated disease, AML, CML, melanoma, myeloma, Kaposi's sarcoma, graft vs host disease, rheumatoid arthritis, inflammatory bowel disorder, psoriasis, osteoarthritis, myeloma, apoptosis, sepsis, rheumatoid arthritis, asthma, Alzheimer's disease, Parkinson's disease, and ischemic heart disease 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: GrantFiled: February 8, 1996Date of Patent: February 23, 1999Assignee: Vertex Pharmaceuticals IncorporatedInventors: Mark James Batchelor, David Bebbington, Guy W. Bemis, Wolf Herman Fridman, Roger John Gillespie, Julian M. C. Golec, David J. Lauffer, David J. Livingston, Saroop Singh Matharu, Michael D. Mullican, Mark A. Murcko, Robert Murdoch, Robert E. Zelle
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Patent number: 5866567Abstract: A compound of the general formula ##STR1## wherein A represents a benzene ring, B represents a 6-membered hydrocarbon ring; X represents a lower alkylene, carbonyl or sulfonyl; Y represents a bond, oxygen or >N--R.sup.1, R.sup.1 represents H or an alkyl group, R represents H, an aromatic group, or an alkyl group optionally substituted by an aromatic group; m and n each represents 1-3, or a salt thereof has potent GnRH receptor antagonizing activity.Type: GrantFiled: June 25, 1996Date of Patent: February 2, 1999Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato
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Patent number: 5837704Abstract: Novel compounds for the treatment of HIV-1 infection. These are 2-heteroary-5,11-dihydro-6H-dipyrido?3,2-b:2',3'-e!?1,4!diazepines of the formula ##STR1## wherein Z is oxygen, sulfur, .dbd.NCN or .dbd.NOR.sup.Type: GrantFiled: August 1, 1996Date of Patent: November 17, 1998Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl Hargrave, John Proudfoot, Usha Patel, Suresh Kapadia, Terence Kelly, Daniel McNeil, Mario Cardozo
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Patent number: 5834462Abstract: Novel tricyclic heterocyclic sulfonamide derivatives and sulfonic ester derivatives which have each an antitumor action and are represented by the following general formula (I) and processes for producing the same are provided. These compounds have each an excellent antitumor activity.A sulfonamide derivative or a sulfonic ester derivative represented by the following general formula (I): ##STR1## {G represents an aromatic 5- or 6-membered ring; L represents 0 or --N(R.sup.1)-- (R.sup.1 represents hydrogen or lower alky); and M represents a tricyclic structure selected from among the following ones; ##STR2## ?rings A and B represent each an unsaturated 5- or 6-membered ring; X represents N(R.sup.2), (wherein R.sup.2 represents hydrogen or lower alkyl), or NHCO;Y represents O, S(O).sub.n, C(R.sup.3)(R.sup.4), C(O), N(R.sup.5), CH(R.sup.6)CH(R.sup.7), C(R.sup.8).dbd.C(R.sup.9), N(R.sup.10)C(O), N.dbd.C(R.sup.11), OCH(R.sup.12), S(O).sub.n CH(R.sup.13) or N(R.sup.14)CH(R.sup.15);Z represents nitrogen or C(R.sup.Type: GrantFiled: March 23, 1995Date of Patent: November 10, 1998Assignee: Eisai Co., Ltd.Inventors: Hiroshi Yoshino, Norihiro Ueda, Jun Niijima, Toru Haneda, Yoshihiko Kotake, Kentaro Yoshimatsu, Tatsuo Watanabe, Takeshi Nagasu, Naoko Tsukahara, Nozomu Koyanagi, Kyosuke Kitoh
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Patent number: 5834463Abstract: Compounds represented by the formula: ##STR1## wherein ring A is benzene; Ar is aromatic group; R.sup.1, R.sup.2 and R.sup.3 each stands for H, acyl, hydrocarbon or heterocyclic, or R.sup.2 and R.sup.3, taken together, may form non-aromatic cyclic hydrocarbon; X is methylene or carbonyl; ......... is single bond or double bond; when ......... is single bond, Y is --NR.sup.4 -- (R.sup.4 is H, acyl, hydrocarbon or heterocyclic), when ......... is double bond, Y is N; n is 1-3, provided that, X is carbonyl and, at the same time, R.sup.2 and R.sup.3, taken together, form non-aromatic cyclic hydrocarbon, ......... is double bond or R.sup.4 is a heterocyclic or --Z(CH.sub.2).sub.m --W (Z is methylene or carbonyl, W is optionally substituted amino, and m denotes 0-5), or salts thereof have an excellent GnRH receptor antagonistic action and/or an action of improving sleep disturbances.Type: GrantFiled: June 26, 1995Date of Patent: November 10, 1998Assignee: Takeda Chemical Industries, Ltd.Inventors: Shigenori Ohkawa, Nobuhiro Fujii, Koichi Kato, Masaomi Miyamoto
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Patent number: 5811546Abstract: The synthesis and the application of new dyes is described. In particular said new dyes can be incorporated in non-migratory state in hydrophilic colloid layers of photographic materials wherefrom they can be rapidly removed after being quickly decolorized in alkaline aqueous liquids used in the processing of said materials. In photographic applications dyes of the general formula (I) are provided with at least one ionisable group which permits solubilization in aqueous and/or alkaline medium. ##STR1## The meanings of the symbols are as defined in the claims and in the description.Type: GrantFiled: December 26, 1996Date of Patent: September 22, 1998Assignee: Agfa-Gevaert, N.V.Inventors: Eric Kiekens, Paul Callant
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Patent number: 5811545Abstract: The synthesis and the application of new dyes is described. In particular said new dyes can be incorporated in non-migratory state in hydrophilic colloid layers of photographic materials wherefrom they can be rapidly removed after being quickly decolorised in alkaline aqueous liquids used in the processing of said materials. In photographic applications dyes of the general formula (I) are provided with at least one ionisable group which permits solubilization in aqueous and/or alkaline medium. ##STR1## The meanings of the symbols are as defined in the claims and in the description.Type: GrantFiled: December 9, 1996Date of Patent: September 22, 1998Assignee: AGFA-Gevaert, N.V.Inventors: Eric Kiekens, Paul Callant
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Patent number: 5712269Abstract: Muscarinic M.sub.2 receptor ligands are described which are suitable for the treatment of neurological disorders, and which may be administered with minimal side-effects. A method of synthesis of these compounds is also described.Type: GrantFiled: January 24, 1995Date of Patent: January 27, 1998Assignee: Pharmaceutical Discovery CorporationInventors: R. Tyler McCabe, Bryan R. Wilson, Christopher A. Rhodes
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Patent number: 5703069Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.Type: GrantFiled: September 11, 1996Date of Patent: December 30, 1997Assignee: Warner-Lambert CompanyInventors: David Thomas Connor, Stephen Joseph Gracheck
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Patent number: 5698551Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 29, 1996Date of Patent: December 16, 1997Assignee: Novo Nordisk A/SInventors: Tine Krogh J.o slashed.rgensen, Knud Erik Andersen, Henrik Sune Andersen, Rolf Hohlweg, Peter Madsen, Uffe Bang Olsen
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Patent number: 5693649Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: October 18, 1995Date of Patent: December 2, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5688788Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: May 18, 1995Date of Patent: November 18, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5674865Abstract: 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: GrantFiled: May 26, 1995Date of Patent: October 7, 1997Assignee: Genentech, Inc.Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
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Patent number: 5674863Abstract: 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: GrantFiled: May 26, 1995Date of Patent: October 7, 1997Assignee: Genentech, Inc.Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
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Patent number: 5668129Abstract: The present invention relates to novel N-substituted azaheterocyclic carboxylic acids and esters thereof in which a substituted alkyl chain forms part of the N-substituent or salts thereof, to methods for their preparation, to compositions containing them, and to their use for the clinical treatment of painful, hyperalgesic and/or inflammatory conditions in which C-fibers play a pathophysiological role by eliciting neurogenic pain or inflammation.Type: GrantFiled: March 27, 1996Date of Patent: September 16, 1997Assignee: Novo Nordisk A/SInventors: Knud Erik Andersen, Uffe Bang Olsen, Hans Petersen, Frederik Christian Gr.o slashed.nvald, Ursula Sonnewald, Tine Krogh J.o slashed.rgensen, Henrik Sune Andersen
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Patent number: 5641772Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.Type: GrantFiled: April 13, 1995Date of Patent: June 24, 1997Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
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Patent number: 5620974Abstract: Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.Type: GrantFiled: July 22, 1994Date of Patent: April 15, 1997Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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Patent number: 5612330Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones, and diazepinones are effective therapeutic agents for treating viral diseases, including those caused by herpesvirus and HIV.Type: GrantFiled: March 22, 1995Date of Patent: March 18, 1997Assignee: Warner-Lambert CompanyInventors: David T. Connor, Stephen J. Gracheck
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Patent number: 5610155Abstract: New condensed diazepinones of general formula I ##STR1## wherein B represents one of the divalent groups ##STR2## and X, l, m, n and R.sup.1 to R.sup.7 are as defined herein, as well as the salts thereof with inorganic or organic acids and processes for preparing them.These compounds are useful for improving or normalising arteriosclerotically induced disorders of cerebral blood flow, for treating diseases of the central nervous system, particularly Alzheimer's disease and Parkinson's disease, and as vagal pacemakers for treating bradycardia and bradyarrhythmia, and also for improving memory performance.Type: GrantFiled: June 1, 1995Date of Patent: March 11, 1997Assignee: Dr. Karl Thomae GmbHInventors: Wolfgang Eberlein, Gerhard Mihm, Wolfhard Engel, Klaus Rudolf, Henri Doods, Harald Ziegler, Michael Entzeroth
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Patent number: 5571912Abstract: This invention relates to a novel method for preparing certain dipyrido-diazepines.Type: GrantFiled: August 14, 1995Date of Patent: November 5, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl G. Grozinger, Karl D. Hargrave, Julian Adams
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Patent number: 5571809Abstract: Disclosed are novel pyridodiazepines. These compounds, as well certain known 6,11-dihydro-5H-pyrido[2,3-b][1,5]benzodiazepin-5-ones are useful in the treatment of AIDS, ARC and related disorders associated with HIV infection.Type: GrantFiled: August 17, 1994Date of Patent: November 5, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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Patent number: 5569760Abstract: A process for preparing nevirapine which comprises reacting 2-chloro-N-(2-chloro-4-methyl-3-pyridyl)-3-pyridine carboxamide with cyclopropylamine followed by cyclisation of the product, wherein the reaction with cyclopropylamine is carried out in the presence of an oxide or hydroxide of an element of the second main or sub-group of the periodic table of elements.Type: GrantFiled: January 12, 1995Date of Patent: October 29, 1996Assignee: Boehringer Ingelheim KGInventors: Heinrich Schneider, Albrecht Christmann
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Patent number: 5565449Abstract: 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: GrantFiled: May 26, 1995Date of Patent: October 15, 1996Assignee: Genentech, Inc.Inventors: Brent Blackburn, Peter Barker, Thomas Gadek, Robert McDowell, Lawrence McGee, Todd Somers, Rob Webb, Kirk Robarge
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Patent number: 5565446Abstract: Benzothiophene, benzofuran and indolethiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases; these compounds also inhibit the activation of human immunodeficiency virus (HIV).Type: GrantFiled: May 19, 1995Date of Patent: October 15, 1996Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, James B. Kramer, Paul C. Unangst
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Patent number: 5554632Abstract: The present patent application discloses compounds having the formula ##STR1## or a pharmaceutically acceptable salt thereof wherein R.sup.3, R.sup.4, R.sup.6 and R.sup.7 each have the meanings set forth in the specification.The compounds are useful for the treatment of various central nervous system disorders such as epilepsy and other convulsive disorders, anxiety, sleep disorders and memory disorders.Type: GrantFiled: December 9, 1994Date of Patent: September 10, 1996Assignees: NeuroSearch A/S, Meiji Seika Kaisha, Ltd.Inventors: Lene Teuber, Oskar Axelsson, Frank Watjen
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Patent number: 5541181Abstract: Disclosed is the novel compound BU-4664L and derivatives thereof. The compound is produced by fermentation of Micromonospora sp. M990-6. The compound possesses anti-inflammatory and/or anti-tumor cell activities.Type: GrantFiled: May 26, 1994Date of Patent: July 30, 1996Assignee: Bristol-Myers Squibb CompanyInventors: Hiroaki Ohkuma, Seikichi Kobaru
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Patent number: 5532358Abstract: A method for preparing certain 4-alkyl-5,11-dihydro-6H-dipyrido[3,2-b:2',3'-e][1,4]diazepin-6-ones, which employs the following reaction scheme: ##STR1##Type: GrantFiled: October 12, 1994Date of Patent: July 2, 1996Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventor: Terence A. Kelly
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Patent number: 5489586Abstract: Benzothiophene, benzofuran and indole-thiazepinones, oxazepinones and diazepinones as well as methods of preparation thereof are described as agents which inhibit leukocyte adherence to vascular endothelium and, as such, are effective therapeutic agents for treating inflammatory diseases.Type: GrantFiled: December 12, 1994Date of Patent: February 6, 1996Assignee: Warner-Lambert CompanyInventors: Diane H. Boschelli, David T. Connor, James B. Kramer, Paul C. Unangst
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Patent number: 5439905Abstract: Thienodiazepine compounds of the formula ##STR1## wherein each symbol is as defined in the specification, their pharmaceutically acceptable salts, and pharmaceutical compositions containing said compound.Since the compounds possess excellent antagonistic actions on cholecystokinin and gastrin, and exhibit potent and durable suppressive actions on pancreatic enzyme secretion and gastric acid secretion, they are useful as medicaments acting on the central nervous system and the peripheral nervous system, as well as prophylactic and therapeutic medicines for pancreatic disorders and gastrointestinal ulcers. Furthermore, they are expected to exhibit anti-dementia actions based on their antagonistic actions on cholecystokinin, and are useful as an anti-dementia.Type: GrantFiled: May 27, 1993Date of Patent: August 8, 1995Assignee: Yoshitomi Pharmaceutical Industries, Ltd.Inventors: Yoichi Naka, Keiichiro Haga, Masahiro Hosoya
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Patent number: 5420123Abstract: Endothelin-inhibiting compounds of the formula ##STR1## wherein: one of R.sup.1 and R.sup.2 is Y.sup.2 -CO.sub.2 H and the other is R;R is(a) hydrogen,(b) alkyl,(c) alkenyl,(d) alkynyl,(e) cycloalkyl,(f) cycloalkenyl,(g) aryl,(h) cycloalkylalkyl,(i) cycloalkenylalkyl, or(j) aralkyl;R.sup.3 is aryl or heteroaryl;X.sup.1 and X.sup.2 are each independently(a) hydrogen,(b) halo or haloalkyl,(c) hydroxy,(d) alkoxy(e) cyano,(f) nitro, or(g) amino, alkylamino, or dialkylamino;and the remaining symbols are as defined in the specification.Type: GrantFiled: December 21, 1992Date of Patent: May 30, 1995Assignee: Bristol-Myers Squibb CompanyInventor: Natesan Murugesan
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Patent number: 5418229Abstract: A compound of the formula ##STR1## wherein X, R.sup.1, R.sup.2, R.sup.3, R.sup..sup.4, Y, m and n are defined herein are useful as muscarinic receptor antagonists.Type: GrantFiled: May 31, 1994Date of Patent: May 23, 1995Inventors: David Alker, Peter E. Cross
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Benzazepine platelet aggregation inhibitors having specificity for the GPII.sub.b III.sub.a receptor
Patent number: 5403836Abstract: A benzazepine derivative that 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: GrantFiled: May 6, 1993Date of Patent: April 4, 1995Assignee: Genentech, Inc.Inventors: Brent Blackburn, Robert McDowell, Thomas Gadek, Rob Webb -
Patent number: 5366972Abstract: Disclosed are novel 5,11-dihydro-6H-dipyrido[3,2-b; 2',3'-e][1,4]diazepines. These are useful in the prevention or treatment of HIV infection.Type: GrantFiled: July 13, 1993Date of Patent: November 22, 1994Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Karl D. Hargrave, John R. Proudfoot, Julian Adams, Karl G. Grozinger, Gunther Schmidt, deceased, Wolfhard Engel, Gunther Trummlitz, Wolfgang Eberlein
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Patent number: 5324832Abstract: Muscarinic antagonists formed by substitution of the distal N-methyl group of pirenzepine or telenzepine. The group used for substitution can be, for example, a propargyl group, a benzyl group, a substituted benzyl group, a hydroxyethyl group, a chloroethyl group, an aminoethyl group, an .omega.-amino alkyl group, or an N-substituted .omega.-amino alkyl group.Type: GrantFiled: July 3, 1991Date of Patent: June 28, 1994Assignee: The United States of America as represented by the Department of Health and Human ServicesInventors: Kenneth A. Jacobson, Barton J. Bradbury, Yishai Karton
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Patent number: 5317101Abstract: The invention relates to tricyclic heterocycles of the formula I ##STR1## wherein X is oxy, thio, sulphinyl, sulphonyl, amino, (1-4C)alkylamino or methylene;Y is carbonyl or methylene;each R.sup.1 includes hydrogen, halogeno and various other substituents;each of m and n is 1 or 2;A.sup.1, alkylene, alkenylene or alkynylene;Het is a 5 or 6 membered heteroaryl group optionally bearing particular substituents; andG is carboxy, 1H-tetrazol-5-yl or a group of the formula:--CONH--SO.sub.2 R.sup.2wherein R.sup.2 is (1-4C)alkyl, benzyl or phenyl;and pharmaceutically-acceptable salts thereof, which possess anti-hyperalgesic properties. The invention also relates to processes for the manufacture of said tricyclic heterocycles; and to novel pharmaceutical compositions containing them.Type: GrantFiled: September 25, 1992Date of Patent: May 31, 1994Assignee: Imperial Chemical Industries PLCInventors: John Oldfield, Howard Tucker
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Patent number: 5264432Abstract: 5-(w-Aminoacyl)-5,10-dihydro-11H-dibenzo(b,e)(1,4)-diazepine-11-ones, and their preparation are disclosed for treatment of antiarrhythmia and as an anticholinergic drug.Type: GrantFiled: November 4, 1992Date of Patent: November 23, 1993Assignee: Arzneimittelwerk Dresden G.m.b.HInventors: Carla Ruger, Wolfgang Sauer, Dieter Lohmann, Hildegard Poppe, Reni Bartsch, Arkadij M. Lichoserstov, Natalja V. Kaverina, Alexandr P. Skoldinov, Yekaterina K. Grigoryeva, Yekaterina A. Talmachova, Valentin V. Lyskovzev, Alwina W. Stawrowskaya, Gennadi G. Chichkanov
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Patent number: 5250679Abstract: 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: GrantFiled: April 10, 1992Date of Patent: October 5, 1993Assignee: Genentech, Inc.Inventors: Brent Blackburn, Robert McDowell, Thomas Gadek, Peter Barker, Lawrence McGee, Rob Webb
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Patent number: 5238936Abstract: The compounds are trisubstituted triazines and pyrimidines useful for the suppressing the resistance of tumour cells to anti-cancer agents and for suppressing the resistance of parasites to anti-parasitic agents.A compound disclosed is 2,4-diallylamino-6-{4-[(10,11-dihydro-5H-dibenzo[a,d]cyclohepten-5-yl) methylamino]piperidin-1-yl}-1,3,5-triazine.Type: GrantFiled: March 6, 1992Date of Patent: August 24, 1993Assignee: Adir et CompagnieInventors: Gilbert Regnier, Alain Dhainaut, Ghanem Atassi, Alain Pierre, Stephane Leonce
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Patent number: 5225557Abstract: A process for preparing optically active naphtho[1.2-b][1,4]thiazepin-4(5H)-ones comprising resolution of rac-.beta.-[(2-amino-1-naphthalenyl)thio]-.alpha.-hydroxy-4-methoxybenzene propanoic acid and converting the optically active acids so obtained into final products is described. The end product naphtho[1,2-b][1,4]thiazepin-4(5H)-ones have activity as calcium channel blockers and accordingly are useful as agents for lowering blood pressure, and as agents for treating ischemia.Type: GrantFiled: December 10, 1990Date of Patent: July 6, 1993Assignee: Hoffmann-La Roche Inc.Inventor: Erno Mohacsi
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Patent number: 5179090Abstract: Condensed diazepinones of general formula I ##STR1## in which]B represents one of the divalent groups ##STR2## X is a .dbd.CH-- group or a nitrogen atom,R represents a lower alkyl radical, which may optionally be further substituted by a phenyl optionally carrying halogen, methyl or methoxy,R.sup.4 and R.sup.5 represent hydrogen, halogen or lower alkyl,R.sup.6 is hydrogen, chlorine or methyl,R.sup.7 and R.sup.8 denote lower alkyl, R.sup.8 also additionally denotes halogen, andm, n, o and p represent the numbers 0, 1, 2 or 3 with the following limitations: the sum of m+n and the sum of o+p each denote the numbers 1, 2 or 3, the sum of n+o and the sum of m+p each denote the numbers 1, 2, 3, 4 or 5, wherein, however, the sum of m+n+o+p must always be greater than 2, andA.sup.1, A.sup.2, A.sup.3 and A.sup.4 denote hydrogen, or, for the case where m, n, o and p each denote the number 1, A.sup.1 and A.sup.2 together or A.sup.3 and A.sup.Type: GrantFiled: October 18, 1991Date of Patent: January 12, 1993Inventors: Klaus Rudolf, Wolfhard Engel, Wolfgang Eberlein, Gunter Trummlitz, Gerhard Mihm, Henri Doods, Norbert Mayer
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Patent number: 5175157Abstract: Disclosed are new cyclic amine derivatives of the formula I ##STR1## wherein the substituents are defined in the specification. These compounds are useful as for treating sinus tachycardia.Type: GrantFiled: July 3, 1991Date of Patent: December 29, 1992Assignee: Boehringer Ingelheim GmbHInventors: Manfred Psiorz, Joachim Heider, Andreas Bomhard, Manfred Reiffen, Norbert Hauel, Klaus Noll, Berthold Narr, Christian Lillie, Walter Kobinger, Jurgen Dammgen