Bicyclo Ring System Which Is Indole (including Hydrogenated) Patents (Class 546/201)
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Patent number: 7119090Abstract: The present invention relates to novel pyrrole substituted 2-indolinone compounds and physiologically acceptable salts and prodrugs thereof which modulate the activity of protein kinases and therefore are expected to be useful in the prevention and treatment of protein kinase related cellular disorders such as cancer.Type: GrantFiled: February 25, 2002Date of Patent: October 10, 2006Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Li Sun, Gerald McMahon
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Patent number: 7119106Abstract: Substituted 2-(2,6-dioxopiperidin-3-yl)phthalimides and 1-oxo-2-(2,6-dioxopiperidin-3-yl)isoindolines reduce the levels of TNF? in a mammal. Typical embodiments are 1-oxo-2-(2,6-dioxo-3-methylpiperidin-3-yl)-4,5,6,7-tetrafuoroisoindoline and 1,3-dioxo-2-(2,6-dioxo-3 -methylpiperidin-3-yl)-4-aminoisoindoline.Type: GrantFiled: January 6, 2003Date of Patent: October 10, 2006Assignee: Celgene CorporationInventors: George W. Muller, David I. Stirling, Roger Shen-Chu Chen
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Patent number: 7115635Abstract: The object of the present invention is to provide a compound having a treatment effect based on a chemokine inhibitory activity, which is satisfactory as a pharmaceutical product for oral administration. The present inventors have found that the following benzylpiperidine derivative (the formula (1)) has a chemokine inhibitory activity. Further intensive studies have resulted in successful enhancement of the chemokine inhibitory activity and stability in blood of the present compound, as well as the completion of the present invention. wherein each symbol is as defined in the specification.Type: GrantFiled: April 26, 2002Date of Patent: October 3, 2006Assignee: Mitsubishi Pharma CorporationInventors: Masatoshi Kiuchi, Takanobu Kuroita, Hideo Tomozane, Shuuzou Takeda, Yoshihito Tanaka, Hidemitsu Higashi, Shigeki Kuwahara
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Patent number: 7105516Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.Type: GrantFiled: September 15, 2003Date of Patent: September 12, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Derek John Denhart, Jonathan L. Ditta, Dalton King, John E. Macor, Lawrence R. Marcin, Ronald J. Mattson, Zhaoxing Meng
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Patent number: 7105543Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent seleceted from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C 1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: September 1, 2005Date of Patent: September 12, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 7105515Abstract: The present invention relates to new derivatives of sulphonamides, with the general formula (I), as well as to their physiologically acceptable salts, the processes for their preparation, their application as medicaments in human and/or veterinary therapy and the pharmaceutical compositions that contain them.Type: GrantFiled: November 13, 2002Date of Patent: September 12, 2006Assignee: Laboratories Del Dr. Esteve, S.A.Inventors: Ramón Merce-Vidal, Blas Andaluz-Mataro, Jordi Frigola-Constansa
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Patent number: 7091353Abstract: The invention relates to isoindole-imide compounds and pharmaceutically acceptable salts, hydrates, solvates, clathrates, enantiomers, diastereomers, racemates, or mixtures of stereoisomers thereof, pharmaceutical compositions comprising these isoindole-imide compounds, and methods for reducing the level of cytokines and their precursors in mammals. In particular, the invention pertains to isoindole-imide compounds that are potent inhibitors of the production of TNF-? in mammals. The isoindole-imides described herein are useful for treating or preventing diseases or disorders in mammals, for example, cancers, such as solid tumors and blood-born tumors; heart disease, such as congestive heart failure; osteoporosis; and genetic, inflammatory; allergic; and autoimmune diseases.Type: GrantFiled: December 21, 2001Date of Patent: August 15, 2006Assignee: Celgene CorporationInventors: Michael J. Robarge, Roger Shen-Chu Chen, George W. Muller, Hon-Wah Man
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Patent number: 7091220Abstract: The present invention relates to substituted indole Mannich bases, processes of preparing substituted indole Mannich base, a medicament containing the same, and a pharmaceutical composition containing the same.Type: GrantFiled: December 20, 2000Date of Patent: August 15, 2006Assignee: Gruenenthal GmbHInventors: Matthias Gerlach, Corinna Maul
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Patent number: 7074796Abstract: The present invention relates to substituted 4-phenyl-1-piperazinyl derivatives having the formula I wherein W is C, CH or N, and the dotted line emanating from W indicates a bond when W is C and no bond when W is N or CH; R1 and R2 are independently selected from hydrogen and halogen, provided at least one of R1 and R2 is a halogen atom; R3 is selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, aryloxy, aralkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6 alkyl)amino, nitro and cyano n is 2, 3, 4 or 5; X is CH2, O, S, CO, CS, SO or SO2; and Q is a group of formula wherein Z is a chain of 3 to 4 chain members; wherein the chain members are selected from C, CH, CH2, CO, N and NH, provided that only one of the chain members may be N or NH, and said chain optionally containing one or two double bonds; hvad med acyl?? R4, R5, R6, R7, R8, R9 and R10 are independently selected from hydrogen, halogen, C1-6 alkyl, trifluoromethyl, C1-6 alkoxy, hydroxy, amino, C1-6 alkylamino, di(C1-6Type: GrantFiled: June 27, 2002Date of Patent: July 11, 2006Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler, Jakob Felding
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Patent number: 7071201Abstract: A novel compound of the formula: wherein A, B, C, D, T, Y, and Z represent each methine or nitrogen; R1, R2, R3, R4, and R5 represent each a substituent; n represents 0 or an integer of 1 to 3; m represents 0 or an integer of 1 to 6; and p represents an integer of 1 to 3; and pharmacologically acceptable salts thereof. The compound has a serotonin antagonism and is clinically useful as medicament, in particular, for treating, ameliorating and preventing spastic paralysis or central muscle relaxants for ameliorating myotonia.Type: GrantFiled: May 2, 2001Date of Patent: July 4, 2006Assignee: Eisai Co., Ltd.Inventors: Noritaka Kitazawa, Kohshi Ueno, Keiko Takahashi, Teiji Kimura, Atsushi Sasaki, Koki Kawano, Tadashi Okabe, Makoto Komatsu, Manabu Matsunaga, Atsuhiko Kubota
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Patent number: 7071213Abstract: There are disclosed compounds of the formula I: or a pharmaceutically acceptable salt of the compound, which exhibit anti-inflammatory and immunomodulatory activity. Also disclosed are pharmaceutical compositions containing said compounds.Type: GrantFiled: November 12, 2002Date of Patent: July 4, 2006Assignee: Schering CorporationInventors: Richard J. Friary, Joseph A. Kozlowski, Bandarpalle B. Shankar, Michael K. C. Wong, Guowei Zhou, Brian J. Lavey, Neng-Yang Shih, Ling Tong, Lei Chen, Youheng Shu
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Patent number: 7071177Abstract: This invention relates to anti-inflammatory and analgesic compounds, especially to certain p-(sulfonyl)phenyl amino derivatives, pharmaceutical compositions containing them, methods for their use, and methods for preparing these compounds.Type: GrantFiled: April 26, 2001Date of Patent: July 4, 2006Assignee: Syntex (U.S.A.) LLCInventors: Nancy Elisabeth Krauss, Taraneh Mirzadegan, David Bernard Smith, Keith Adrian Walker
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Patent number: 7067534Abstract: This invention is directed to compounds which are selective antagonists for melanin concentrating hormone-1 (MCH1) receptors. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier. This invention provides a pharmaceutical composition made by combining a therapeutically effective amount of the compound of this invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of the compound of the invention and a pharmaceutically acceptable carrier.Type: GrantFiled: November 21, 2003Date of Patent: June 27, 2006Assignee: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, John Wetzel, John E. DeLeon, Yu Jiang, Chien-An Chen, Kai Lu
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Patent number: 7056932Abstract: The invention is concerned with novel heterocyclyl substituted 1-alkoxy acetic acid derivatives of formula (I) wherein R1 to R6 and A are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds inhibit the formation of coagulation factors Xa, IXa and thrombin induced by factor VIIa and tissue factor and can be used as medicaments.Type: GrantFiled: December 10, 2004Date of Patent: June 6, 2006Assignee: Hoffman-La Roche Inc.Inventors: Luca Claudio Gobbi, Katrin Groebke Zbinden, Peter Mohr, Ulrike Obst
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Patent number: 7053078Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: June 12, 2001Date of Patent: May 30, 2006Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 7053086Abstract: The present invention relates to certain 4-heteroaryl-3-heteroarylidenyl-2-indolinones compounds and their physiologically acceptable salts which modulate the activity of protein kinases (“PKs”), in particular CDK2. The compounds of the present invention are therefore useful in treating disorders related to abnormal PK activity. Pharmaceutical composition containing these compounds and methods of preparing these compounds are also described.Type: GrantFiled: August 27, 2003Date of Patent: May 30, 2006Assignee: Sugen, Inc.Inventors: Peng Cho Tang, Chung Chen Wei, Ping Huang, Jingrong Cui
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Patent number: 7049314Abstract: The present invention relates to compounds of Formula (I) and pharmaceutically acceptable salts or solvates thereof and pharmaceutically acceptable formulations comprising said compounds useful for the treatment of premature ejaculation, depression, attention deficit hyperactivity disorder, obsessive-compulsive disorder, post-traumatic stress disorder and substance abuse disorders.Type: GrantFiled: September 15, 2003Date of Patent: May 23, 2006Assignee: Bristol-Myers Squibb CompanyInventors: Dalton King, Jeffrey A. Deskus, John E. Macor, Ronald J. Mattson, Zhaoxing Meng, Charles P. Sloan
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Patent number: 7041668Abstract: The present invention discloses and claims benzimidazole compounds of formula (I): in which A is aryl or heteroaryl; R1 is selected from optionally substituted alkyl, alkoxy, aryl or heteroaryl, NH-lower alkyl or NH-cycloalkyl, or halogen, NH2; 1-imidazolyl or SO2Me; R2 is selected from optionally substituted —CO-alkyl, —CO-cycloalkyl, —CO-aralkyl, —CO-aryl, —CO-alkoxy, aryl or aralkyl, or —CO-amino, CO—NHR3 or CO—R3R4 wherein R3 and R4 are selecteded independently from hydrogen, alkyl, hydroxyalkyl, alkoxyalkyl, fluoroalkyl, alkynyl, heteroalkyl, alkylheteroalkyl, aryl, aralkyl or together form an alkylene chain optionally containing one to 4 heteroatoms; a pharmaceutically acceptable salt or a prodrug thereof; the use of compounds of formula (I) for the treatment of cancer, and pharmaceutical compositions comprising a compound of formula (I) and one or more pharmaceutically acceptable adjuvants or diluents.Type: GrantFiled: March 25, 2004Date of Patent: May 9, 2006Assignee: Aventis Pharma S.A.Inventors: Francois Clerc, Francois Hamy, Isabelle Depaty, Odile Angouillant-Boniface, Stéphanie Deprets, Chantal Carrez, Manfred Roesner
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Patent number: 7034029Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptorType: GrantFiled: January 16, 2004Date of Patent: April 25, 2006Assignee: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7019004Abstract: The invention provides compounds of formula (I) wherein X, Y, R1, R2, R3 and R4 are as defined in the description, and the preparation thereof.Type: GrantFiled: May 7, 2001Date of Patent: March 28, 2006Assignee: Novartis AGInventors: Daniel Berney, Robin Breckenridge, Peter Neumann, Gideon Shapiro, Max Peter Seiler, Thomas J. Troxler
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Patent number: 7005438Abstract: Isoindolin-1-one and Isoindoline-1,3-dione substituted in the 2-position with a 2,6-dioxo-3-hydroxypiperidin-5-yl group, which may be further substituted in the 5-position with alkyl or halogeno, and in the 4-position with alkyl or a nitrogen-containing group are inhibitors of, and thus useful in the treatment of disease states mediated by, TNF?. A typical embodiment is 2-(2,6-dioxo-3-hydroxy-5-fluoropiperidin-5-yl)-4-aminoisoindolin-1-one.Type: GrantFiled: December 9, 2003Date of Patent: February 28, 2006Assignee: Celgene CorporationInventors: George Muller, Hon-Wah Man, David I. Stirling
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Patent number: 6998401Abstract: There is provided an aminophenoxyacetic acid derivative of the following formula (I): wherein, R1, R2, R3 and R4 are, independent from each other, alkoxy group, alkyl group or aryl group, etc.; E1 and E2 are oxygen atom, sulfur atom, etc.; n is 0 to 5; X and Y are alkylene group, cycloalkylen group, or alkenylen group; Q is pheny group which may be substituted or benzoyl group, etc, or a pharmaceutically acceptable salt thereof. These compounds have neuroprotective effects by inducing calbindin D28Kd, one of Ca2+-binding proteins.Type: GrantFiled: March 24, 2003Date of Patent: February 14, 2006Assignee: Suntory LimitedInventors: Hirokazu Annoura, Naohiro Takemoto, Hiroshi Uramoto
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Patent number: 6995176Abstract: The present invention provides a compound of formula I and the use thereof for the treatment of a central nervous system disorder related to or affected by the 5-HT6 receptor.Type: GrantFiled: July 17, 2003Date of Patent: February 7, 2006Assignee: WyethInventors: Ronald Charles Bernotas, Steven Edward Lenicek
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Patent number: 6984637Abstract: This invention relates to certain cyclic amine derivatives of Formula (I) that are CCR-3 receptor antagonists, pharmaceutical compositions containing them, methods for their use and methods for preparing these compounds.Type: GrantFiled: November 21, 2003Date of Patent: January 10, 2006Assignee: Syntex (U.S.A.) LLCInventors: Leyi Gong, Denis John Kertesz, David Bernard Smith, Francisco Xavier Talamas, Robert Stephen Wilhelm
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Patent number: 6969729Abstract: The present invention relates to ion channel activating agents. More particularly, the present invention relates to a particular class of chemical compounds that has proven useful as openers of SKCa and IKCa channels. In further aspects, the present invention relates to the use of these SK/IK channel activating agents for the manufacture of medicaments and pharmaceutical compositions comprising the SK/IK channel activating agents.Type: GrantFiled: October 16, 2002Date of Patent: November 29, 2005Assignee: Neurosearch A/SInventors: Bo Skaaning Jensen, Tino Dyhring Jørgensen, Philip K. Ahring, Palle Christophersen, Dorte Strøbaek, Lene Teuber, Søren Peter Olesen
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Patent number: 6967252Abstract: Novel flame retarding compounds that comprise at least one sterically hindered nitroxyl, hydroxylamine or hydrocarbyloxyamine moiety and at least one conventional organohalogen or organophosphorus flame retardant moiety, represented by where HA is independently of each other a sterically hindered nitroxyl, sterically hindered hydroxylamine or sterically hindered hydrocarbyloxyamine moiety, L is independently of each other a direct bond or chemical linking group, FRM is independently of each other an organohalogen or an organophosphorus flame reatardant moiety, and x, y and z are each independently greater than or equal to 1, are especially effective towards providing flame retardancy to organic polymer substrates.Type: GrantFiled: December 16, 2002Date of Patent: November 22, 2005Assignee: Ciba Specialty Chemicals CorporationInventors: Malisa V. Troutman, Ramanathan Ravichandran, Redina Kote, Roswell E. King
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Patent number: 6958338Abstract: The present invention relates to 4-, 5-, 6- or 7-methylene substituted indolyl derivatives of formula I wherein R is aryl or heteroaryl, where said aryl or heteroaryl groups may be substituted one or more times with a substituent selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, C1-6-alkoxy, C1-6-alkylthio, hydroxy, hydroxy-C1-6-alkyl trifluoromethyl, trifluoromethylsulfonyl, C1-6-alkylsulfonyl, amino, C1-6-alkylamino, di-(C1-6-alkyl)amino, acyl, aminocarbonyl and a methylene dioxy group; X is N, C or CH; provided that the dotted line indicates a bond when X is C and no bond when X is N or CH; R1 is hydrogen, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyl, C3-8-cycloalkyl-C1-6-alkyl, aryl, aryl-C1-6-alkyl, acyl, thioacyl, C1-6-alkylsulfonyl, trifluoromethylsulfonyl or arylsulfonyl; and R2 and R3 are independently selected from hydrogen, halogen, cyano, nitro, C1-6-alkyl, C2-6-alkenyl, C2-6-alkynyl, C3-8-cycloalkyType: GrantFiled: February 4, 2003Date of Patent: October 25, 2005Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jan Kehler
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Patent number: 6951874Abstract: The invention provides compounds of general formula (I) wherein Q, R, R2, R4, R5, R6, R7 and R8 are as defined in the specification, processes for their preparation, pharmaceutical compositions containing them and their use in therapyType: GrantFiled: February 23, 2001Date of Patent: October 4, 2005Assignee: AstraZeneca ABInventors: Peter Hansen, Lars Pettersson
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Patent number: 6951849Abstract: Benzimidazolidinone derivative compounds, which increase acetylcholine signaling or effect in the brain, and highly selective muscarinic agonists, particularly for the M1 and/or M4 receptor subtypes, pharmaceutical compositions comprising the same, as well as methods of treating psychosis using these compounds are disclosed.Type: GrantFiled: April 3, 2003Date of Patent: October 4, 2005Assignee: ACADIA Pharmaceuticals Inc.Inventors: Nicholas Michael Kelly, Kristian Norup Koch, Bo-Ragnar Tolf
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Patent number: 6949540Abstract: Substituted pyrazoles, methods of manufacturing them, compositions containing them, and methods of using them to treat, for example, autoimmune diseases mediated by cathepsin S are described.Type: GrantFiled: March 28, 2003Date of Patent: September 27, 2005Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Hui Cai, James P. Edwards, Steven P. Meduna, Barbara A. Pio, Jianmei Wei
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Patent number: 6908922Abstract: Compound of formula (I): wherein: V represents a single bond or an alkylene chain, M represents a single bond or an alkylene chain, A and E each represents nitrogen or CH, but at least one of the two groups A or E represents nitrogen, W represents a group of formula (i), (ii) or (iii): Medicinal products containing the same which are useful in the treatment of diseases or pathological conditions ins which endothelial dysfunction is known.Type: GrantFiled: November 12, 2002Date of Patent: June 21, 2005Assignee: Les Laboratoires ServierInventors: Jean-Louis Peglion, Christophe Poitevin, Jean-Paul Vilaine, Nicole Villeneuve, Marie-Pierre Bourguignon, Catherine Thollon
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Patent number: 6906084Abstract: The present invention relates to compounds of formula I, in which R0; R1; R2; R3; R4; R5; R6; R7; Q; V, G and M have the meanings indicated in the claims. The compounds of formula I are valuable pharmacologically active compounds. They exhibit a strong antithrombotic effect and are suitable, for example, for the therapy and prophylaxis of cardiovascular disorders like thromboembolic diseases or restenoses. They are reversible inhibitors of the blood clotting enzymes factor Xa (FXa) and/or factor VIIa (FVIIa), and can in general be applied in conditions in which an undesired activity of factor Xa and/or factor VIIa is present or for the cure or prevention of which an inhibition of factor Xa and/or factor VIIa is indicated. The invention furthermore relates to processes for the preparation of compounds of formula I, their use, in particular as pharmaceuticals for treating the foregoing conditions, and pharmaceutical preparations comprising them.Type: GrantFiled: November 21, 2002Date of Patent: June 14, 2005Assignee: Aventis Pharma Deutschland GmbHInventors: Marc Nazaré, Melanie Essrich, David William Will, Hans Matter, Kurt Ritter, Volkmar Wehner
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Patent number: 6906090Abstract: The invention provides the use of certain isatin and oxindole derivatives in the preparation of a medicament for use in the treatment of mycobacterial disease.Type: GrantFiled: March 4, 1999Date of Patent: June 14, 2005Assignee: AstraZeneca ABInventor: Ramachandran Janakiraman
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Patent number: 6906075Abstract: Melanin concentrating hormone receptor ligands (especially substituted benzoimidazole analogues), capable of modulating MCH receptor activity, are provided. Such ligands may be used to modulate MCH binding to MCH receptors in vivo or in vitro, and are particularly useful in the treatment of a variety of metabolic, feeding and sexual disorders in humans, domesticated companion animals and livestock animals. Pharmaceutical compositions and methods for treating such disorders are provided, as are methods for using such ligands for detecting MCH receptors (e.g., receptor localization studies).Type: GrantFiled: January 9, 2003Date of Patent: June 14, 2005Assignee: Neurogen Corp.Inventors: Robert W. DeSimone, Cheryl Steenstra, Linda Gustavson, Rajagopal Bakthavatchalam, Alan Hutchison
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Patent number: 6903112Abstract: The present invention provides a compound of formula I and the use thereof in the therapeutic treatment of disorders related to or affected by the 5-HT6 receptor.Type: GrantFiled: October 23, 2003Date of Patent: June 7, 2005Assignee: WyethInventors: Ping Zhou, Derek Cecil Cole, Michael Gerard Kelly, William Joseph Lennox
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Patent number: 6903117Abstract: A compound of formula (I): or a salt thereof, or a solvate thereof, wherein Ra represents a group R5 which is hydrogen, alkyl or optionally substituted aryl and Rb represents a moiety of formula (a): wherein X represents a hydroxy or an alkoxy group wherein the alkyl group may be substitued or unsubstituted or X represents a group NRsRt wherein Rs and Rt each independently represent hydrogen, alkyl, substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, optionally substituted arylalkyl, an optionally substituted heterocyclic group or an optionally substituted heterocyclylalkyl group, or Rs and Rt together with the nitrogen to which they are attached form a heterocyclic group; R1 represents an alkyl or a substituted or unsubstituted aryl group; and R2, R3 and R4 each independently represent hydrogen, alkyl, aryl or substituted aryl; R6 and R7 each independently represent hydrogen, hydroxy, amino, alkoxy, optionally substituted aryloxy, optionally substituted benzyloxy, alkylamiType: GrantFiled: November 20, 2002Date of Patent: June 7, 2005Assignee: Nikem Research S.R.L.Inventors: Carlo Farina, Stefania Gagliardi, Guy Marguerite Marie Gerard Nadler
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Patent number: 6903104Abstract: The invention is based on the discovery that certain 3-oxoacetamideindolyl compounds have potent anticancer and anti-angiogenic activity. The 3-oxoacetamideindolyl compounds are of the following formula. In this formula, each R1 is independently isoxazolyl, thiazolyl, isothiazolyl, 1,3,4-thiadiazolyl, 1,3-benzothiazolyl, quinolyl, isoquinolyl, thionaphthenyl, or benzofuranyl, each being optionally substituted with 1-6 independent R5; or when taken together with R2 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5. Each R2 is independently H, C1-C10 alkyl, or aryl, each being optionally substituted with 1-4 independent R5; or when taken together with R1 and the nitrogen atom to which they are attached form a 5-8 membered ring comprising C, N, S, or O atoms wherein any atom is optionally substituted with an independent R5.Type: GrantFiled: December 5, 2002Date of Patent: June 7, 2005Assignee: National Health Research InstitutesInventors: Chiung-Tong Chen, Shu-Jen Chen, Ming-Chu Hsu, Der-Ren Hwang, Wen-Tai Li, Chu-Chung Lin
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Patent number: 6900196Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: July 6, 2004Date of Patent: May 31, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6890938Abstract: Compound with an indole linked through an aliphatic ring system to an aromatic moiety are useful in treating conditions associated with enhanced P38? kinase activity.Type: GrantFiled: November 20, 2001Date of Patent: May 10, 2005Assignee: Scios, Inc.Inventors: Gregory Luedtke, Richland Tester, Sundeep Dugar, Qing Lu, John Perumattam, Xuefei Tan
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Patent number: 6890916Abstract: The present invention relates to dopamine D4 ligands having the general formula I wherein R1—R10, W, X, Y1—Y4, and n are as described herein. The compounds of the invention are potent dopamine D4 receptor ligands.Type: GrantFiled: December 9, 2002Date of Patent: May 10, 2005Assignee: H. Lundbeck A/SInventors: Benny Bang-Andersen, Jakob Felding, Jan Kehler, Kim Andersen
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Patent number: 6887870Abstract: Heterocyclic are provided which are sodium/proton exchange (NHE) inhibitors which have the structure wherein n is 1 to 5; X is N or C—R5 wherein R5 is H, halo, alkenyl, alkynyl, alkoxy, alkyl, aryl or heteroaryl; Z is a heteroaryl gorup, R1, R2, R3 and R4 are as defined herein, and where X is N. R1 is preferably aryl or heteroaryl, and are useful as antianginal and cardioprotective agents. In addition, a method is provided for preventing or treating angina pectoris, cardiac dysfunction, myocardial necrosis, and arrhythmia employing the above heterocyclic derivatives.Type: GrantFiled: September 25, 2000Date of Patent: May 3, 2005Assignee: Bristol-Myers Squibb CompanyInventors: Saleem Ahmad, Shung C. Wu, Steven V. O'Neil, Khehyong Ngu, Karnail S. Atwal, David S. Weinstein
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Patent number: 6881844Abstract: The present invention provides glucokinase activators of formula I: wherein R1, R2 and R3 are defined in the specification. Glucokinase activators are useful for increasing insulin secretion in the treatment of type II diabetes.Type: GrantFiled: September 30, 2003Date of Patent: April 19, 2005Assignee: Hoffman-La Roche Inc.Inventor: Wendy Lea Corbett
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Patent number: 6878725Abstract: Compounds of formula (I) in which R2, X, Y, Cy, L and Lp(D)n have the meanings given in the specification, are inhibitors of the serine protease, Factor Xa and are useful in the treatment of cardiovascular disorders.Type: GrantFiled: June 12, 2001Date of Patent: April 12, 2005Assignee: Eli Lilly and CompanyInventors: John Walter Liebeschuetz, Christopher William Murray, Stephen Clinton Young, Nicholas Paul Camp, Stuart Donald Jones, William Alexander Wylie, John Joseph Masters, Michael Robert Wiley, Scott Martin Sheehan, David Birenbaum Engel, Brian Morgan Watson
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Patent number: 6869957Abstract: This invention provides a novel series of non-peptidyl compounds which are useful in the treatment or prevention of a physiological disorder associated with an excess of tachykinins. This invention also provides methods for the treatment of such physiological disorders as well as pharmaceutical formulations which employ these novel compounds.Type: GrantFiled: September 23, 2003Date of Patent: March 22, 2005Assignee: Eli Lilly and CompanyInventors: Sung Y. Cho, Thomas A. Crowell, Bruce D. Gitter, Philip A. Hipskind, J. Jeffry Howbert, Joseph H. Krushinski, Jr., Karen L. Lobb, Brian S. Muehl, James A. Nixon
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Patent number: 6869971Abstract: UCS 1025 derivatives having antitumor activity or antibacterial activity which are represented by formula (I): wherein R1 represents hydrogen, lower alkyl, etc.; R2 represents hydrogen, or is combined with R3 to represent a bond, etc., or is combined with R4 to represent —O(C?O)—, etc.; R3 represents hydrogen, etc., or is combined with R2 to represent a bond, etc.; R4 represents hydrogen, etc., or is combined with R2 to represent —(C?O)O—, etc.; R5 represents hydrogen or is combined with R6 to represent a bond; R6 represents hydrogen, etc., or is combined with R5 to represent a bond; R7 represents hydrogen or is combined with R8 to represent ?O; R8 represents hydroxy or is combined with R7 to represent ?O; ---- represents a single bond or a double bond, and a represents a single bond (two carbon atoms to which a is bound are combined to form a single bond) or an oxygen atom, or pharmaceutically acceptable salts thereof.Type: GrantFiled: October 19, 2000Date of Patent: March 22, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Tsutomu Akama, Akira Asai, Tsutomu Agatsuma, Shinji Nara, Yoshinori Yamashita, Tamio Mizukami, Shun-ichi Ikeda, Yutaka Saitoh, Yutaka Kanda
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Patent number: 6861418Abstract: The present invention relates to 4-arylindolinones, as well as pharmaceutical compositions thereof, capable of modulating protein kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation. The present invention also relates to methods for treating protein kinase related disorders.Type: GrantFiled: December 16, 2003Date of Patent: March 1, 2005Assignee: Sugen, Inc.Inventors: Jingrong Cui, Ruofei Zhang, Hong Shen, Ji Yu Chu, Fang-Jie Zhang, Marcel Koenig, Steven Huy Do, Xiaoyuan Li, Chung Chen Wei, Peng Cho Tang
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Patent number: 6861530Abstract: This invention relates to substituted piperidine derivatives having at least one six-membered ring substituent. The piperidine derivatives exhibit antitumor activity and are useful as pharmaceuticals such as an antitumor agent.Type: GrantFiled: July 6, 2001Date of Patent: March 1, 2005Assignee: Kyowa Hakko Kogyo Co., Ltd.Inventors: Shinji Nara, Rieko Nakatsu, Yutaka Kanda, Shiro Akinaga, Mitsunobu Hara, Jun Eishima, Timothy A. Grese, Douglas L. Gernert
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Patent number: 6855710Abstract: The present invention relates to new substituted indolinones of general formula wherein X and R1 to R5 are defined as in claim 1, the isomers and the salts thereof which have valuable properties. The above compounds of general formula I wherein R1 denotes a hydrogen atom, a C1-3-alkyl group or a prodrug group have valuable pharmacological properties, particularly an inhibiting effect on various kinases, on viral cyclin and on receptor tyrosine kinases, and the other compounds of the above general formula I wherein R1 does not represent a hydrogen atom, a C1-3-alkyl group or a prodrug group are valuable intermediate products for the preparation of the abovementioned compounds.Type: GrantFiled: September 19, 2003Date of Patent: February 15, 2005Assignee: Boehringer Ingelheim Pharma KGInventors: Rainer Walter, Wolfgang Grell, Armin Heckel, Frank Himmelsbach, Wolfgang Eberlein, Gerald Roth, Jacobus C.A. van Meel, Norbert Redemann, Walter Spevak, Ulrike Tontsch-Grunt, Thomas von Rueden
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Patent number: 6844344Abstract: The present invention provides compounds of formula (I) which are useful for treating depression, anxiety, and alleviating the symptoms caused by withdrawal or partial withdrawal from the use of tobacco or of nicotineType: GrantFiled: December 6, 2000Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Xiaoqiang He, Nicholas Allan Honigschmidt, Todd Jonathan Kohn, Vincent Patrick Rocco, Patrick Gianpietro Spinazze, Kumiko Takeuchi
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Patent number: 6844338Abstract: A pharmaceutical compound of the formula (I) in which R1 and R2 are each hydrogen or C1-6 alkyl, R3 is —SR10, —SOR10, —SO2R10, —COR10, —CH2OH or —CONHR11, where R10 is C1-6 alkyl and R11 is hydrogen or C1-6 alkyl, R4, R5, R6 and R7 are each hydrogen or C1-6alkyl, provided that at least one of R4, R5, R6 and R7 is C1-6alkyl, R8 and R9 are each hydrogen, halo, C1-6 alkyl or cyano, n is 0 or 1 and m is 2 or 3, x is a (a) or (b), and y is (c) or (d), wherein R12 and R13 are each hydrogen, C1- alkyl, cyclopropyl or cyclopropyl-C1-6 alkyl; and salts thereof.Type: GrantFiled: May 4, 2001Date of Patent: January 18, 2005Assignee: Eli Lilly and CompanyInventors: John Fairhurst, Peter Gallagher