Bicyclo Ring System Which Is Isoindole (including Hydrogenated) Patents (Class 546/277.1)
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Patent number: 6559174Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: GrantFiled: March 13, 2002Date of Patent: May 6, 2003Assignee: Merck & Co., Inc.Inventors: Linus S. Lin, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
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Patent number: 6552065Abstract: The present invention provides hydroxamate compounds which are deacetylase inhibitors. The compounds are suitable for pharmaceutical compositions having anti-proliferative properties.Type: GrantFiled: August 31, 2001Date of Patent: April 22, 2003Assignee: Novartis AGInventors: Stacy William Remiszewski, Kenneth Walter Bair, Richard William Versace, Lawrence Blas Perez, Michael Alan Green, Lidia Cristina Sambucetti, Sushil Sharma
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Patent number: 6541503Abstract: Compounds of formula (I): wherein X is N, CH, CCF3, or C(C1-12 aliphatic); R4 is sulfonic acid, C1-12 aliphatic-sulfonyl, sulfonyl-C1-12 aliphatic, C1-12 aliphatic-sulfonyl-C1-6 aliphatic, C1-6 aliphatic-amino, R7-sulfonyl, R7 sulfonyl-C1-12 aliphatic, R7-aminosulfonyl, R7-aminosulfonyl-C1-12 aliphatic, R7-sulfonylamino, R7-sulfonylamino-C1-12 aliphatic, aminosulfonylamino, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl, di-C1-12 aliphatic amino, di-C1-12 aliphatic aminocarbonyl, di-C1-12 aliphatic aminosulfonyl-C1-12 aliphatic, (R8)1-3-Arylamino, (R8)1-3-Arylsulfonyl, (R8)1-3-Aryl-aminosulfonyl, (R8)1-3-Aryl-sulfonylamino, Het-amino, Het-sulfonyl, Het-aminosulfonyl, aminoiminoamino, or aminoiminoaminosulfonyl, R5 is hydrogen; and further wherein R4 and R5 are optionally joined to form a fused ring, pharmaceutical formulations comprising them and their use in therapy, especially in the treatment of diseases mediated by CDK2 activity, such as alopecia induced by caType: GrantFiled: August 8, 2001Date of Patent: April 1, 2003Assignee: SmithKline Beecham CorporationInventors: Stephen Thomas Davis, Scott Howard Dickerson, Stephen Vernon Frye, Philip Anthony Harris, Robert Neil Hunter, III, Lee Frederick Kuyper, Karen Elizabeth Lackey, Michael Joseph Luzzio, James Marvin Veal, Duncan Herrick Walker
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Publication number: 20030004153Abstract: The present invention relates to novel heteroaryl-diazabicycloalkanes which are found to be cholinergic ligands at the nicotinic Acetyl Choline Receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neurodegeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: May 14, 2002Publication date: January 2, 2003Inventors: Dan Peters, Gunnar M Olsen, Elsebet Ostergaard Nielsen, Philip K Ahring, Simon Feldbaek Nielsen, Tino Dyhring Jorgensen
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Publication number: 20020193399Abstract: Compounds of Formula I are antagonists of VLA-4 and/or alpha4/beta7, and as such are useful in the inhibition or prevention of cell adhesion and cell-adhesion mediated pathologies. These compounds may be formulated into pharmaceutical compositions and are suitable for use in the treatment of AIDS-related dementia, allergic conjunctivitis, allergic rhinitis, Alzheimer's disease, asthma, atherosclerosis, autologous bone marrow transplantation, certain types of toxic and immune-based nephritis, contact dermal hypersensitivity, inflammatory bowel disease including ulcerative colitis and Crohn's disease, inflammatory lung diseases, inflammatory sequelae of viral infections, meningitis, multiple sclerosis, multiple myeloma, myocarditis, organ transplantation, psoriasis, pulmonary fibrosis, restenosis, retinitis, rheumatoid arthritis, septic arthritis, stroke, tumor metastasis, uveititis, and type I diabetes.Type: ApplicationFiled: March 13, 2002Publication date: December 19, 2002Inventors: Linus S. Lin, Shrenik K. Shah, Linda L. Chang, William K. Hagmann, Richard A. Mumford
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Patent number: 6492374Abstract: The present invention relates to benzofuran derivatives having general Formula (I) wherein A is selected from (1), (2), (3), (4) wherein Z is O or S; s is 0 or 1; q is 0 or 1; R4 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C26-alkynyl, C1-6-alkyl-aryl, or C1-6-alkyl-O-aryl; D is a spacer group selected from branched or straight chain C1-6-alkylene, C2-6-alkenylene and C2-6-alkynylene; its enantiomers, and pharmaceutically acceptable acid addition salt thereof. The compounds are potently binding to the 5-HT1A receptor.Type: GrantFiled: June 4, 2001Date of Patent: December 10, 2002Assignee: H. Lundbeck A/SInventors: Kim Andersen, Mario Rottländer, Klaus Peter Bøgesø, Henrik Pedersen, Thomas Ruhland, Robert Dancer
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Patent number: 6482951Abstract: Isoindolin-1-one-substituted propionamide glucokinase activators which increase insulin secretion in the treatment of type II diabetes.Type: GrantFiled: December 6, 2001Date of Patent: November 19, 2002Assignee: Hoffmann-La Roche Inc.Inventor: Kevin Richard Guertin
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Patent number: 6476028Abstract: A method of treating a CCR5-mediated disease state in mammals which comprises administering to a mammal in need of such treatment, an effective amount of a compound of formula (I) or a pharmaceutically acceptable salt thereof.Type: GrantFiled: August 8, 2000Date of Patent: November 5, 2002Assignees: SmithKline Beecham Corporation, SmithKline Beecham p.l.c.Inventors: William E. Bondinell, James Chan, Roderick A. Porter, Joseph W. Venslavsky, Steven Dabbs, David T. Davies
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Publication number: 20020072616Abstract: Compounds of formula (I), their salts and prodrugs thereof, where the substituents are as defined herein are disclosed as opiate binding agents useful in the treatment of opiate-mediated conditions. Also described are processes for making such substances.Type: ApplicationFiled: October 30, 2001Publication date: June 13, 2002Applicant: Pfizer Inc.Inventors: Bernard Joseph Banks, Robert James Crook, Stephen Paul Gibson, Graham Lunn, Alan John Pettman
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Patent number: 6391896Abstract: The invention is related to the following compounds: wherein all variables are as defined in the specification. The compounds are useful for treating psychotic disorders.Type: GrantFiled: July 3, 2001Date of Patent: May 21, 2002Assignee: Duphar International Research BVInventors: Roelof Van Hes, Johannes A. M. Van Der Heijden, Cornelis G. Kruse, Jacobus Tipker, Martinus T. M. Tulp, Gerben M. Visser, Bernard J. Van Vliet
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Patent number: 6365617Abstract: The invention is directed to novel indole and indazole urea-peptoid compounds which are useful as thrombin receptor antagonists for the treatment of diseases associated with thrombosis, restenosis, hypertension, heart failure, arrhythmia, inflammation, angina, stroke, atherosclerosis, ischemic conditions, Angiogenesis related disorders, cancer, and neurodegenerative disorders. Pharmaceutical compositions comprising the substituted indole and indazole urea-peptoid compounds of the present invention and methods of treating conditions mediated by the thrombin receptor are also disclosed.Type: GrantFiled: June 26, 2000Date of Patent: April 2, 2002Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: David F. McComsey, William J. Hoekstra, Bruce E. Maryanoff, Han-Cheng Zhang
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Patent number: 6365606Abstract: Novel compounds which are effective PDE IV inhibitors are disclosed. The compounds possess improved PDE IV inhibition compared to theophylline or rolipram, with improved selectivity with regard to, e.g., PDE V inhibition. The present invention includes compounds of Formula I: wherein the substituents are as disclosed herein.Type: GrantFiled: February 18, 2000Date of Patent: April 2, 2002Assignee: Euro-Celtique, S.A.Inventors: David Cavalla, Peter Hofer, Andre Gehrig, Peter Wintergerst, Mark Chasin
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Patent number: 6344468Abstract: The present invention relates to substituted isoindolone derivatives of the formula I, in which R1, R2, R3, R4, R5, R6 and R7 are as defined in the claims, which are useful pharmaceutically active compounds for the therapy and prophylaxis of illnesses, for example cardiovascular diseases such as hypertension, angina pectoris, cardiac insufficiency, thromboses or atherosclerosis. The compounds of the formula I are capable of modulating the body's production of cyclic guanosine monophosphate (cGMP) and are generally suitable for the therapy and prophylaxis of illnesses which are associated with a disturbed cGMP balance. The invention furthermore relates to processes for preparing compounds of the formula I, to their use for the therapy and prophylaxis of the abovementioned illnesses and for preparing pharmaceuticals for these, and also pharmaceutical preparations which comprise compounds of the formula I.Type: GrantFiled: October 6, 2000Date of Patent: February 5, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Ursula Schindler, Karl Schoenafinger, Hartmut Strobel, Viola Groehn
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Patent number: 6337344Abstract: The present invention relates to the inhibition of blood clotting proteins, and more particularly, to indole derivatives of formula (I), in which R1a, R1b, R1c R1d, R2, R3, R4 and A are defined as indicated in the claims. The compounds of formula (I) are inhibitors of the blood clotting enzyme factor Xa. The invention also relates to processes for the preparation of the compounds of formula (I), to methods of inhibiting factor Xa activity and of inhibiting blood clotting, to use of the compounds of formula (I) in the treatment and prophylaxis of diseases which can be cured or prevented by the inhibition of factor Xa activity such as thromboembolic diseases, and to the use of the compounds of formula (I) in the preparation of medicaments to be applied in such diseases.Type: GrantFiled: August 14, 2000Date of Patent: January 8, 2002Assignee: Aventis Pharma Deutschland GmbHInventors: Elisabeth Defossa, Uwe Heinelt, Otmar Klingler, Gerhard Zoller, Fahad A. Al-Obeidi, Armin Walser, Peter Wildgoose, Hans Matter
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Patent number: 6262080Abstract: The present invention provides novel thio-substitutedamido lactam derivatives of the formula useful in as inhibitors of matrix metallo-proteinases (MMPs).Type: GrantFiled: December 17, 1999Date of Patent: July 17, 2001Assignee: Avantis Pharmaceuticals Inc.Inventors: Alan M. Warshawsky, Michael J. Janusz
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Patent number: 6262268Abstract: A novel process is provided for the preparation of 3-(5,6,7,8-tetrahydro-[1,8]-naphthyridin-2-yl)-propylamine which is useful in the synthesis of &agr;v integrin receptor antagonists. Also provided are useful intermediates obtained from the process.Type: GrantFiled: November 9, 2000Date of Patent: July 17, 2001Assignee: Merck & Co., Inc.Inventors: Michael Palucki, David L. Hughes, Chunhua Yang, Nobuyoshi Yasuda
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Patent number: 6245768Abstract: Disclosed are compounds of the formula or the pharmaceutically acceptable salts thereof wherein the 6-membered A ring may be optionally substituted with up to four groups independently selected from halogen, hydroxy, lower alkyl, or lower alkoxy; Ar represents optionally substituted aryl or heteroaryl Z represents carbon or nitrogen provided that where Z is carbon, R11 represents hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy, or phenyl optionally substituted with one or two groups selected from hydrogen, halogen, hydroxy, lower alkyl, or lower alkoxy; and where Z is nitrogen, R11 represents an electron pair; R5 is hydrogen or lower alkyl, L and m represent integers; n is 0, or an integer; R12 and R13 independently represent lower alkyl; or together may together form an optionally substituted 5-11 membered ring with the nitrogen atoms to which they are bonded;CR′R″ represents a methylene group optionally substituted with lower alkyl;and k is an integer of from 1Type: GrantFiled: August 3, 1999Date of Patent: June 12, 2001Assignee: Neurogen CorporationInventors: Xiao-shu He, Brian de Costa, Jan W. F. Wasley
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Patent number: 6245774Abstract: Compounds of general formula (1) are described: wherein ═W— is (1) ═C(Y)— where Y is a halogen atom, or an alkyl or —XRa group where X is —O—, —S(O)m— [where m is zero or an integer of value 1 or 2], or —N(Rb)— [where Rb is a hydrogen atom or an optionally substituted alkyl group] and Ra is a hydrogen atom or an optionally substituted alkyl group or, (2) ═N—; L is (1) a —C(R)═C(R1)(R2) or [—CH(R)]nCH(R1)(R2) group; is (2) a —(Xa)nAlk′Ar′, or Alk′XaAr′ group; or is (3) XaR1; Z is a group (A), (B), (C) or (D): wherein Ar is a monocyclic or bicyclic aryl group optionally containing one or more heteroatoms selected from oxygen, sulphur or nitrogen atoms; Z1is a group —NR12C(O)— [where R12 is a hydrogen atom or an optionally substituted alkyl or (Alk)tAr group], —C(O)NR12—, —NR12Type: GrantFiled: June 20, 1995Date of Patent: June 12, 2001Assignee: Celltech Therapeutics LimitedInventors: Graham John Warrellow, Ewan Campbell Boyd, Rikki Peter Alexander
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Patent number: 6239129Abstract: Compound of formula (I): wherein: R1 and R2 each independently of the other represents hydrogen or alkyl, A represents alkylene, alkenylene or alkynylene, G1 represents wherein R3 and R4 each independently of the other represents hydrogen, alkyl, cycloalkyl, cycloalkylalkyl, optionally substituted aryl or optionally substituted arylalkyl, or G1 represents heterocycloalkyl optionally substituted by alkyl, cycloalkyl, cycloalkylalkyl, nitrile, carboxy, alkoxycarbonyl, carbamoyl, optionally substituted aryl, optionally substituted arylalkyl, optionally substituted heteroaryl or optionally substituted heteroarylalkyl, and which medicinal products containing the same/are useful as serotonin-reuptake inhibitors.Type: GrantFiled: January 25, 2000Date of Patent: May 29, 2001Assignee: Adir et CompagnieInventors: Gilbert Lavielle, Olivier Muller, Bernard Cimetiere, Mark Millan, Alain Gobert, Jean-Michel Rivet
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Patent number: 6235758Abstract: A compound of formula (I) or a salt thereof: wherein: P1 is pyridiyl; P2 is phenyl; A is a bond or a chain of 1 to 5 atoms optionally substituted by C1-6 alkyl; R1 and R2 groups are each independently hydrogen, C1-6alkyl optionally substituted by NR12R13, C2-6alkenyl, C2-6alkynyl, cyano, halogen, CF3, NR12R13, CHO, OCF3, COR14, CH2OR14 or OR14 where R12, R13 and R14 are independently hydrogen or C1-6alkyl; n and m are independently 0, 1 or 2; R3 is hydrogen or C1-6 alkyl; R4 is a group of formula (i): in which: R6 and R7 are independently hydrogen, C1-6 alkyl optionally substituted by one or more fluorine atoms, C1-6alkylthio, C1-6alkoxy or halogen.Type: GrantFiled: July 23, 1999Date of Patent: May 22, 2001Assignee: SmithKline Beecham p.l.c.Inventors: Laramie Mary Gaster, Paul Adrian Wyman, Keith Raymond Mulholland, David Thomas Davies, David Malcolm Duckworth, Ian Thomson Forbes, Graham Elgin Jones
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Patent number: 6194581Abstract: In accordance with the present invention, there is provided a class of pyridine compounds which are modulators of acetylcholine receptors. The compounds of the invention displace acetylcholine receptor ligands from their binding sites.Type: GrantFiled: December 22, 1998Date of Patent: February 27, 2001Assignee: Merck & Co., Inc.Inventors: Nicholas D. Cosford, Jean-Michel Vernier