The Additional Ring Is A Hetero Ring Patents (Class 546/207)
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Patent number: 7435824Abstract: Compounds useful as prodrugs of potassium channel inhibitor compounds, in particular as prodrugs of Kv1.5 channel inhibitors.Type: GrantFiled: January 3, 2005Date of Patent: October 14, 2008Assignees: Bristol-Myers Squibb Company, Icagen Inc.Inventors: Michael F. Gross, John Lloyd
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Patent number: 7419990Abstract: Certain novel piperidine derivatives are agonists of the human melanocortin receptor(s) and, in particular, are selective agonists of the human melanocortin-4 receptor (MC-4R). They are therefore useful for the treatment, control, or prevention of diseases and disorders responsive to the activation of MC-4R, such as obesity, diabetes, sexual dysfunction, including erectile dysfunction and female sexual dysfunction.Type: GrantFiled: July 16, 2004Date of Patent: September 2, 2008Assignee: Merck & Co., Inc.Inventors: Heather Sings, Feroze Ujjainwalla
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Patent number: 7417042Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: GrantFiled: August 8, 2005Date of Patent: August 26, 2008Assignee: Proteolix, Inc.Inventors: Mark S. Smyth, Guy J. Laidig
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Publication number: 20080194629Abstract: The invention relates to 3,5-piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,5-piperidine compound, and/or a method of treatment comprising administering a 3,5-piperidine compound, a method for the manufacture of a 3,5-piperidine compound, and novel intermediates and partial steps for their synthesis. Especially, the 3,5-piperidine compounds have the formula I, wherein the symbols have the meanings described in the specification.Type: ApplicationFiled: May 2, 2006Publication date: August 14, 2008Inventors: Daniel Kaspar Baeschlin, Werner Breitenstein, Claus Ehrhardt, Juergen Klaus Maibaum, Nils Ostermann, Juerg Zimmermann, Simon Rudisser, Eric Vangrevelinghe, Osamu Irie, Ichiro Umemura, Masaki Suzuki, Muneto Mogi, Takanori Kanazawa, Fumiaki Yokokawa, Atsuko Nihonyanagi
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Publication number: 20080176841Abstract: Provided herein are novel epoxide inhibitors of cysteine proteases, compositions comprising the epoxide inhibitors, and packaged pharmaceuticals. Also provided are methods of inhibiting a papain-family cysteine protease and methods of treating or preventing a disease by administering a composition containing an epoxide inhibitor of the invention. The compositions may be administered in combination with another therapeutic agent.Type: ApplicationFiled: June 13, 2007Publication date: July 24, 2008Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Matthew S. Bogyo, Amir M. Sadaghiani, Steven Verhelst
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Patent number: 7393849Abstract: Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:Type: GrantFiled: April 23, 2007Date of Patent: July 1, 2008Assignee: Aventis Pharmaceuticals Inc.Inventors: Pavel Safar, Armin Walser, Stephen James Shimshock
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Patent number: 7390803Abstract: The present invention is directed to compounds of the formula (I) (wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R27, R28, R29, R30, R31, X, m, n and the dashed line are defined herein) which are useful as modulators of chemokine receptor activity.Type: GrantFiled: October 24, 2003Date of Patent: June 24, 2008Assignee: Merck & Co., Inc.Inventors: Gabor Butora, Sander G. Mills, Alexander Pasternak, Kothandaraman Shankaran, Lihu Yang, Changyou Zhou, Stephen D. Goble
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Publication number: 20080139556Abstract: A composition for binding FKBP proteins is disclosed, along with a method of treating conditions associated with neuronal degeneration, wherein said composition comprises a compound of formula I, wherein, R, R1, R2, R3 and X are as defined herein.Type: ApplicationFiled: December 6, 2006Publication date: June 12, 2008Applicant: AVENTIS PHARMACEUTICALS INC.Inventors: Raymond W. KOSLEY, Bruce Baron, Patrick Jimonet, John G. Jurcak, Stephen J. Shimshock, Xu-yang Zhao, Rosy Sher, Paul J. Mueller, Jennifer Beall, Matthieu Barrague, Joseph W. Guiles
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Patent number: 7381727Abstract: The invention concerns compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7, R8 and R9 are as defined herein. The invention also concerns the method for preparing said compounds and their therapeutic use.Type: GrantFiled: January 22, 2007Date of Patent: June 3, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Christian Congy, Laurent Hortala, Murielle Rinaldi-Carmona
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Patent number: 7375115Abstract: There are provided novel 4(2-furoyl)aminopiperidines represented by the general formula (I), their synthetic intermediates, processes for their preparation and medicaments containing them. In the above formula, X is OH or N, and Y is a group of the following general formula (II), formula (II-a) or formula (III): wherein a, b and c are each an integer of 0-6; Z is CH2 or NH; W is O or S; T is O or N—R15 wherein R15 is H, a C1-C6 alkyl group, a benzyl group or a phenethyl group; and R1 is H, a C1-C6 alkoxycarbonyl group, a benzyloxy-carbonyl group, or the like. The 4-(2-furoyl)aminopiperidine derivatives according to this invention possess opioid ? antagonistic activity and are useful for the treatment or prevention of side effects which are caused by ? receptors agonist and which are selected from constipation, nausea/emesis or itch, or for the treatment or prevention of idiopathic constipation, postoperative ileus, paralytic ileus, irritable bowel syndrome or chronic pruritus.Type: GrantFiled: October 8, 2002Date of Patent: May 20, 2008Assignees: Kyorin Pharmaceutical Co., Ltd., Nisshin Pharma Inc.Inventors: Ryuuta Fukutomi, Hitoshi Inoue, Koji Kawamura, Takuya Kishimoto, Masashi Suzuki, Rie Shibayama, Kazuko Kojima, Kouichirou Hagihara
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Patent number: 7361658Abstract: 2-Acylaminothiazole derivatives or salts thereof which have a platelet increasing activity based on an excellent human c-mpl-Ba/F3 cell growth function and a function of accelerating formation of megakaryocytic colonies and which are useful for treating thrombocytopenia are provided.Type: GrantFiled: July 15, 2004Date of Patent: April 22, 2008Assignee: Astellas Pharma Inc.Inventors: Keizo Sugasawa, Yuji Koga, Kazuyoshi Obitsu, Takao Okuda, Koichiro Harada, Hideki Kubota, Fukushi Hirayama, Masaki Abe, Ken-ichi Suzuki
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Publication number: 20080081824Abstract: The present application describes modulators of CCR3 of formula (I): or stereoisomers or prodrugs or pharmaceutically acceptable salts thereof, wherein m, n, Q1, R1, R2, R3, R4, R5, R6, R7, T1, T2, W1, W2, W3 and Z1 are as defined herein. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and atherosclerosis using said modulators are disclosed.Type: ApplicationFiled: September 29, 2006Publication date: April 3, 2008Inventors: Changsheng Zheng, Dean A. Wacker
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Publication number: 20080081813Abstract: Biphenylcarboxamide compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: ApplicationFiled: March 27, 2002Publication date: April 3, 2008Inventors: Lieven Meerpoel, Marcel Viellevoye
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Patent number: 7348440Abstract: The present invention relates to dihydropyrrole compounds that are useful for treating cellular proliferative diseases, for treating disorders associated with KSP kinesin activity, and for inhibiting KSP kinesin. The invention also related to compositions which comprise these compounds, and methods of using them to treat cancer in mammals.Type: GrantFiled: June 12, 2003Date of Patent: March 25, 2008Assignee: Merck & Co., Inc.Inventors: Kenneth L. Arrington, Paul J. Coleman, Christopher D. Cox, Mark E. Fraley, Robert M. Garbaccio, George D. Hartman, William F. Hoffman, Edward S. Tasber
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Patent number: 7329656Abstract: This invention is directed to Arylthiobenzylpiperidine derivatives which are ligands at the MCH1 receptor. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a pharmaceutical composition made by admixing a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention further provides a process for making a pharmaceutical composition comprising combining a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. This invention also provides a method of treating a subject suffering from depression and/or anxiety which comprises administering to the subject a therapeutically effective amount of a compound of the subject invention.Type: GrantFiled: September 21, 2005Date of Patent: February 12, 2008Assignee: H. Lundbeck A/SInventors: Mohammad R. Marzabadi, Yu Jiang, Chien-An Chen, Kai Lu, Kim Andersen
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Patent number: 7326722Abstract: The present invention discloses and claims a compound of general formula (I) wherein A, X and R2 are as described herein. Also disclosed and claimed is application of this compound in a variety of therapeutic applications.Type: GrantFiled: April 17, 2003Date of Patent: February 5, 2008Assignee: Sanofi-AventisInventors: Gihad Dargazanli, Geneviève Estenne-Bouhtou, Pascale Magat, Benoît Marabout, Florence Medaisko, Pierre Roger, Mireille Sevrin, Corinne Veronique
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Patent number: 7320978Abstract: This invention relates to compounds of formula (I): Wherein R1, R2, R3, R4, R5, R6, R7 and R8 are as described herein. The invention further relates to a method for prevention and therapeutic use thereof.Type: GrantFiled: August 1, 2006Date of Patent: January 22, 2008Assignee: Sanofi-AventisInventors: Francis Barth, Joelle Arnaud-Taillades, Christian Congy, Murielle Rinaldi-Carmona
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Patent number: 7312336Abstract: Compounds of general formula (I) are disclosed and claimed in the present application, as well as their pharmaceutically acceptable salts, pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain.Type: GrantFiled: December 9, 2003Date of Patent: December 25, 2007Assignee: AstraZeneca Canada Inc.Inventors: Daniel Delorme, Edward Roberts, Zhongyong Wei
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Patent number: 7309709Abstract: The present invention relates to compounds of the Formula: wherein R1 to R6, X, Z and A are as defined. These compounds have activity inhibiting production of A?-peptide. The invention also relates to pharmaceutical compositions and methods for treating diseases, for example, neurodegenerative diseases, e.g., Alzheimer's disease, in a mammal comprising compounds of the present Formula.Type: GrantFiled: March 11, 2005Date of Patent: December 18, 2007Assignee: Pfizer Inc.Inventor: Lei Zhang
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Publication number: 20070270398Abstract: The present invention relates to new compounds of formula I, to pharmaceutical compositions comprising said compounds, and to the use of said compounds in therapy. The present invention further relates to processes for the preparation of compounds of formula I.Type: ApplicationFiled: May 11, 2007Publication date: November 22, 2007Inventors: Anders Johansson, Johan Johansson, Carl-Gustav Sigfridsson
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Patent number: 7294637Abstract: One aspect of the present invention relates to a method of treating of drug addiction or drug dependence in a mammal, comprising the step of administering to a mammal in need thereof a therapuetically effective amount of a heterocyclic compound, e.g., a 3-substituted piperidine. In a preferred embodiment, the method of the present invention treats cocaine addiction or methamphetamine addiction.Type: GrantFiled: February 4, 2004Date of Patent: November 13, 2007Assignee: Sepracor, Inc.Inventors: Brian M. Aquila, Thomas D. Bannister, Gregory D. Cuny, James R. Hauske, Joanne M. Holland, Paul E. Persons, Heike S. Radeke, Fengjiang Wang, Liming Shao
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Patent number: 7285568Abstract: Novel biaromatic compounds having the structural formula (I) below: are formulated into pharmaceutical compositions suited for administration in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively, into cosmetic compositions.Type: GrantFiled: May 24, 2005Date of Patent: October 23, 2007Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Claire Bouix-Peter, Michel Rivier, Pascal Collette, Andre Jomard
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Patent number: 7282519Abstract: The invention describes novel nitrosated and/or nitrosylated diuretic compounds or pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated and/or nitrosylated diuretic compound, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent. The invention also provides novel compositions and kits comprising at least one diuretic compound of the invention, that is optionally nitrosated and/or nitrosylated, and, optionally, at least one nitric oxide donor compound and/or at least one therapeutic agent.Type: GrantFiled: August 20, 2004Date of Patent: October 16, 2007Assignee: NitroMed, Inc.Inventors: David S. Garvey, L. Gordon Letts, Manuel Worcel, Richard A. Earl, Maiko Ezawa, Xinqin Fang, Subhash P. Khanapure, Chia-En Lin, Ramani R. Ranatunge, Cheri A. Stevenson
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Publication number: 20070208056Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: January 23, 2007Publication date: September 6, 2007Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Patent number: 7265110Abstract: The present invention relates compounds of the formula (I); wherein R1, R2, R3, R4, R5, R6, R7, R8, and R10 represent a variety of substituents; A represents NR9 or O; B represents a bond, CH2, NR9 or O, wherein one or both hydrogen atoms in said CH2 moiety may be replaced with one or both of R7 and R8, or alternatively, one of the hydrogen atoms in said CH2 moiety together with a hydrogen atom from an adjacent carbon are replaced by a double bond; with the proviso that when A is O, then B is NR9; n is zero, 1 or 2; and pharmaceutically acceptable salts thereof.Type: GrantFiled: September 6, 2002Date of Patent: September 4, 2007Assignee: Merck Sharp & Dohme LimitedInventors: Jose Luis Castro Pineiro, Duncan Edward Shaw, Brian John Williams
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Patent number: 7265133Abstract: This invention provides compounds of formula I: wherein a, b, c, m, p, s, t, W, Ar1, X1, R1, R2, R3, R4, R6, and R7 are as defined specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: GrantFiled: March 10, 2005Date of Patent: September 4, 2007Assignee: Theravance, Inc.Inventors: Mathai Mammen, Yu-Hua Ji, YongQi Mu, Craig Husfeld, Li Li
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Patent number: 7259157Abstract: Compounds represented by Formula (I): or pharmaceutically acceptable salts thereof, are effective as NMDA NR2B antagonists useful for relieving pain.Type: GrantFiled: April 2, 2002Date of Patent: August 21, 2007Assignee: Merck & Co., Inc.Inventors: Nigel J. Liverton, John W. Butcher, Charles McIntyre, Christopher F. Claiborne, David A. Claremon, John A. McCauley, Joseph J. Romano, Wayne Thompson, Peter M. Munson
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Patent number: 7253186Abstract: Disclosed herein are compounds of Formula I, or a pharmaceutically acceptable salt, amide, ester, or prodrug thereof. Also disclosed are methods of inhibiting an activity of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Disclosed are also methods of inhibiting an activation of a monoamine receptor comprising contacting the monoamine receptor or a system containing the monoamine receptor with an effective amount of one or more of the compounds of Formula I. Furthermore, methods of treating psychotic disease using a compound of Formula I are disclosed.Type: GrantFiled: June 20, 2003Date of Patent: August 7, 2007Inventors: Carl-Magnus Andersson, Nathalie Schlienger, Alma Fejzic, Eva Louise Hansen, Jan Pawlas
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Patent number: 7241760Abstract: The present invention relates to imidazole derivatives of the general formula wherein R1, R2, R3 and R4 are described hereinbelow. These compounds can be used in the treatment or prevention of mGluR5 receptor mediated disorders. These compounds are useful, interalia, in the treatment or prevention of acute and/or chronic neurological disorders such as psychosis, epilepsy, schizophrenia, Alzheimer's disease, cognitive disorders and memory deficits, as well as chronic and acute pain.Type: GrantFiled: June 12, 2004Date of Patent: July 10, 2007Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Simona Maria Ceccarelli, Georg Jaeschke, Sabine Kolczewski, Richard Hugh Philip Porter, Eric Vieira
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Patent number: 7235544Abstract: The invention relates to compounds of formula (I): wherein substituents are as defined.Type: GrantFiled: June 17, 2004Date of Patent: June 26, 2007Assignee: Glaxo Group LimitedInventors: Alan David Borthwick, John David Harling, Wendy Rebecca Irving, Savvas Kleanthous, Nigel Stephen Watson, Robert John Young
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Publication number: 20070142432Abstract: The present invention relates to a chemical genus of biaryl substituted nitrogen-attached heterocycles that are inhibitors of LTA4H (leukotriene A4 hydrolase). The compounds have the general formula: They are useful for the treatment and prevention and prophylaxis of inflammatory diseases and disorders.Type: ApplicationFiled: August 3, 2006Publication date: June 21, 2007Applicant: deCODE Chemistry, Inc.Inventors: Vincent Sandanayaka, Jasbir Singh, Mahnaz Keyvan, Michael David Krohn, Mark E. Gurney
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Patent number: 7232818Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases. The activities of those Ntn having multiple activities can be differentially inhibited by the compounds described. For example, the chymotrypsin-like activity of the 20S proteasome may be selectively inhibited with the inventive compounds. The peptide-based compounds include at least three peptide units, an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation.Type: GrantFiled: April 14, 2005Date of Patent: June 19, 2007Assignee: Proteolix, Inc.Inventors: Mark S. Smyth, Guy J. Laidig, Ronald T. Borchardt, Barry A. Bunin, Craig M. Crews, John H. Musser
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Patent number: 7223763Abstract: Sulfonamide and urea compounds having an inhibitory effect on Src kinase including enantiomers, stereoisomers and tautomers thereof, as well as pharmaceutically acceptable salts or solvates of said compound, said compound having the general structure shown in Formula II are disclosed and claimed:Type: GrantFiled: April 30, 2004Date of Patent: May 29, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: Pavel Safar, Armin Walser, Stephen James Shimshock
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Patent number: 7223867Abstract: Diastereoselective and enantioselective synthetic routes for the preparation of compounds of formula (I): or derivatives thereof, wherein: R is C1-6alkyl, C3-7cycloalkyl, C1-6alkoxy, hydroxy, halo, C1-6alkenyl, C1-6alkynyl, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, arylC1-6alkoxy, heteroarylC1-6alkoxy, aminoC1-6alkyl, (C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, arylC1-6alkylamino, heteroarylC1-6alkyamino; R1 is hydrogen or R; R2 is hydroxy, C1-6alkoxy, amino, C1-6alkylamino, di(C1-6alkyl)amino; R3 and R4 are each independently selected from the list consisting of perhaloC1-6alkyl, hydrogen, halo, C1-6alkyl, C1-6alkoxy, hydroxy, amino, C1-6alkylamino, di(C1-6alkyl)amino, hydroxyC1-6alkyl, C1-6alkoxyC1-6alkyl, aminoC1-6alkyl,(C1-6alkyl)aminoC1-6alkyl, di(C1-6alkyl)aminoC1-6alkyl, aryl, and COX wherein X may be hydroxy, C1-6 alkoxy, C1-6alkyl, amino, C1-6alkylamino, or di(C1-6alkyl)amino; and wherein any alkyl group or the alkyl moiety of any group contType: GrantFiled: November 5, 2002Date of Patent: May 29, 2007Assignee: GlaxoSmithKline S.P.A.Inventors: Giovanni Palombi, Silvano Ronzoni
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Patent number: 7217823Abstract: One aspect of the present invention relates to heterocyclic compounds. A second aspect of the present invention relates to the use of the heterocyclic compounds as ligands for various mammalian cellular receptors, including dopamine transporters. The compounds of the present invention will find use in the treatment of numerous ailments, conditions and diseases which afflict mammals, including but not limited to addiction, anxiety, depression, sexual dysfunction, hypertension, migraine, Alzheimer's disease, obesity, emesis, psychosis, analgesia, schizophrenia, Parkinson's disease, restless leg syndrome, sleeping disorders, attention deficit hyperactivity disorder, irritable bowel syndrome, premature ejaculation, menstrual dysphoria syndrome, urinary incontinence, inflammatory pain, neuropathic pain, Lesche-Nyhane disease, Wilson's disease, and Tourette's syndrome.Type: GrantFiled: November 25, 2003Date of Patent: May 15, 2007Assignee: Sepracor Inc.Inventor: Michael Z. Hoemann
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Patent number: 7217706Abstract: This invention relates to new propanolamine derivatives or salts thereof represented by the following formula [I]: Wherein each symbol is as defined in the specification or salts thereof which have gut selective sympathomimetic, anti-ulcerous, anti-pancreatitis, lipolytic, anti-urinary incontinence and anti-pollakiuria activities, to processes for the preparation thereof, to a pharmaceutical composition comprising the same and to a method for the prevention and/or treatment diseases indicated in the specification to a human being or an animal.Type: GrantFiled: February 14, 2002Date of Patent: May 15, 2007Assignee: Astellas Pharma Inc.Inventors: Kiyoshi Taniguchi, Minoru Sakurai, Naoaki Fujii, Kumi Hosoi, Yasuyo Tomishima, Hisashi Takasugi, Hajime Sogabe, Hirofumi Ishikawa, Naomi Hanioka
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Patent number: 7205410Abstract: The present invention of compounds of formula (I) a stereochemically isomeric form thereof, an N-oxide form thereof or a pharmaceutically acceptable acid addition salt thereof, —R1—R2— is a bivalent radical of formula wherein in said bivalent radicals one or two hydrogen atoms may be substituted with C1-6alkyl or hydroxy; R3 is hydrogen or halo; R4 is hydrogen or C1-6alkyl; R5 is hydrogen or C1-6alkyl; L is C3-6cycloalkyl, oxoC5-6cycloalkyl, C2-6alkenyl, or L is a radical of formula -Alk-R6—, Alk-X—R7, -Alk-Y—C(?O)—R9, or -Alk-Y—C(?O)—NR11R12 wherein each Alk is C1-12alkanediyl; and R6 is hydrogen, amino, cyano, C1-6alkylsulfonylamino, C3-6cycloalkyl, oxoC5-6cycloalkyl, aryl or a heterocyclic ringsystem; R7 is hydrogen, C1-6alkyl, hydroxyC1-6alkyl, C3-6cycloalkyl, aryl or a heterocyclic ringsystem; X is O, S, SO2 or NR8; said R8 being hydrogen or C1-6alkyl; R9 is hydrogen, C1-6alkyl, C3-6cycloalkyl, C1-6alkyloxy, hydroxy or aryl; Y is a direct bond or NR10; said R10 being hydrogen, or C1-6alkyl; R11 and RType: GrantFiled: January 29, 2003Date of Patent: April 17, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Jean-Paul René Marie André Bosmans, Ann Louise Gabriëlle Meulemans, Michel Anna Jozef De Cleyn, Henricus Jacobus Maria Gijsen
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Patent number: 7205318Abstract: The present application describes lactam-containing cyclic diamines and derivatives thereof of Formula I: P4-M-M4I or pharmaceutically acceptable salt forms thereof, wherein M is a non-aromatic carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: GrantFiled: March 16, 2004Date of Patent: April 17, 2007Assignee: Bristol-Myers Squibb CompanyInventors: Jennifer X. Qiao, Tammy C. Wang, Gren Z. Wang, Timur Gungor
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Patent number: 7205319Abstract: This invention discloses and claims a compound of general formula (I) in which R1 represents either a hydrogen atom, or an optionally substituted alkyl group, or a cycloalkylalkyl group, or an optionally substituted phenylalkyl group, or an alkenyl group, X represents a hydrogen atom or one or more substituents chosen from halogen atoms and trifluoromethyl, alkyl and alkoxy groups, R2 represents one or more substituents chosen from halogen atoms, optionally substituted alkoxy and optionally substituted amino. The compounds of this invention exhibit therapeutic utility.Type: GrantFiled: January 28, 2005Date of Patent: April 17, 2007Assignee: Sanofi-aventisInventors: Gihad Dargazanli, Geneviève Estenne-Bouhtou, Benoît Marabout, Pierre Roger, Mireille Sevrin
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Patent number: 7186733Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, thienyl, furanyl, imidazolyl, pyrrolyl, triazolyl, thiazolyl, and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6alkyl, NO2, CF3, C1–C6alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety or functional gastrointestinal disorders.Type: GrantFiled: May 16, 2002Date of Patent: March 6, 2007Assignee: Astrazeneca ABInventors: William Brown, Andrew Griffin, Christopher Walpole
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Patent number: 7186719Abstract: Compounds of formula (II) are antibacterial agents wherein Q represents a radical of the formula: —N(OH)CH(?O) or the formula: —C(?O)NH(OH); R1 represents hydrogen, C1–C6 alkyl or C1–C6 alkyl substituted by one or more halogen atoms, or, except when Q is a radical of the formula: —N(OH)CH(?O), a hydroxy, C1–C6 alkoxy, C1–C6 alkenyloxy, amino, C1–C6 alkylamino, or di-(C1–C6 alkyl)amino group; R2 represents a substituted or unsubstituted C1–C6 alkyl, cycloalkyl(C1–C6 alkyl)- or aryl(C1–C6 alkyl)-group; and A represents a group of formula (IIA), or (IIB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 when taken together with the nitrogen atom to which they are attached form a saturated heterocyclic first ring of 5 to 7 atoms as specified in the description.Type: GrantFiled: September 30, 2004Date of Patent: March 6, 2007Assignee: British Biotech PharmaceuticalsInventors: Lisa Marie Pratt, Kenneth Noel Keavey, Gilles Denis Pain, Laurent Mounier
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Patent number: 7176326Abstract: Novel ?-lactams finding utility as intermediates in the preparation of sidechain-bearing taxanes such as taxol and taxol derivatives. The present invention also relates to novel methods of coupling ?-lactams to form such sidechain-bearing taxanes, and to novel sidechain-bearing taxanes.Type: GrantFiled: October 20, 2004Date of Patent: February 13, 2007Assignee: Bristol-Myers Squibb CompanyInventors: John K. Thottathil, Ivan D. Trifunovich, David J. Kucera, Wen-Sen Li
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Patent number: 7166586Abstract: Sulfonamide lactams of the following formula wherein X, R1, R2, R3, R4, R4a, R5, R5a, R6, R6a, R7 and R8 are as described herein, are provided which inhibitors of Factor Xa and are useful as anticoagulants in the treatment of cardiovascular diseases associated with thromboses.Type: GrantFiled: February 26, 2003Date of Patent: January 23, 2007Assignee: Bristol Myers Squibb Co.Inventors: Stephen P. O'Connor, Michael Lawrence, Yan Shi, Philip D. Stein
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Patent number: 7160902Abstract: Amide derivatives of the general formulae Ia and Ib: are disclosed. Pharmaceutical compositions containing these compounds, and methods for their use, inter alia, for treating and/or preventing gastrointestinal disorders, pain, and pruritus are also disclosed.Type: GrantFiled: November 14, 2003Date of Patent: January 9, 2007Assignee: Adolor CorporationInventors: Roland E. Dolle, Guo-Hua Chu, Minghua Gu
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Patent number: 7153857Abstract: Compounds of the formula I useful as metalloproteinase inhibitors, especially as inhibitors of MMP 13.Type: GrantFiled: August 8, 2002Date of Patent: December 26, 2006Assignee: AstraZeneca ABInventors: Maurice Raymond Verschoyle Finlay, Howard Tucker, David Waterson
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Patent number: 7153868Abstract: The present invention provides a method of treatment of a subject suffering from a disease, such as schizophrenia, for which the administration of an NK-3 antagonist is indicated which comprises administering to that subject a therapeutically effective amount of a compound of formula I: wherein, generally, Q is R1 is benzyl, phenyl, thiophene or imidazolyl optionally substituted with C1-4alkyl or halogen, such as methyl, fluorine or bromine; R2 is hydrogen or C1-4alkyl such as methyl; R3 is phenyl; R4 is hydrogen; R5 is hydrogen or C1-6alkylcarbonyl such as methylcarbonyl; X is —SO2— or —C(O)N(R2)SO2— where R2 is preferably hydrogen; Y is a bond, CH2 or Z1 where Z1 is —N(Rf)— in which Rf is C1-6alkylcarbonyl such as ethylcarbonyl; and R6 is phenyl, pyrazolyl, pyridyl, pyrimidinyl or benzimidazolonyl optionally substituted with one or two groups chosen from C1-6alkyl and benzyl, such as methyl, ethyl and benzyl; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: April 16, 2003Date of Patent: December 26, 2006Assignee: Merck Sharp & Dohme Ltd.Inventors: Mark Stuart Chambers, Philip Jones, Helen Jane Szekeres
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Patent number: 7119203Abstract: This invention is directed generally to proteinase (also known as “protease”) inhibitors, and, more particularly, to piperidinyl- and piperazinyl-sulfonylmethyl hydroxamic acids that, inter alia, inhibit matrix metalloproteinase (also known as “matrix metalloprotease” or “MMP”) activity and/or aggrecanase activity. Such hydroxamic acids generally correspond in structure to the following formula: (wherein A1, A2, Y, E1, E2, E3, and Rx are as defined in this specification), and further include salts of such compounds. This invention also is directed to compositions of such hydroxamic acids, intermediates for the syntheses of such hydroxamic acids, methods for making such hydroxamic acids, and methods for treating conditions (particularly pathological conditions) associated with MMP activity and/or aggrecanase activity.Type: GrantFiled: April 25, 2003Date of Patent: October 10, 2006Assignee: Pharmacia CorporationInventors: Thomas E. Barta, Daniel P. Becker, Louis J. Bedell, Terri L. Boehm, David L. Brown, Jeffery N. Carroll, Yiyuan Chen, Yvette M. Fobian, John N. Freskos, Alan F. Gasiecki, Margaret L. Grapperhaus, Robert M. Heintz, Susan L. Hockerman, Darren J. Kassab, Ish K. Khanna, Stephen A. Kolodziej, Mark A. Massa, Joseph J. McDonald, Brent V. Mischke, Deborah A. Mischke, Patrick B. Mullins, Mark A. Nagy, Monica B. Norton, Joseph G. Rico, Michelle A. Schmidt, Nathan W. Stehle, John J. Talley, William F. Vernier, Clara I. Villamil, Lijuan J. Wang, Thomas A. Wynn
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Patent number: 7115632Abstract: A sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound that inter alia inhibits matrix metalloprotease activity is disclosed as are a treatment process that comprises administering a contemplated sulfonyl aromatic or heteroaromatic ring hydroxamic acid compound in a MMP enzyme-inhibiting effective amount to a host having a condition associated with pathological matrix metalloprotease activity. A contemplated compound corresponds in structure to the formula wherein W and the R groups are defined elsewhere.Type: GrantFiled: May 11, 2000Date of Patent: October 3, 2006Assignee: G. D. Searle & Co.Inventors: Louis J Bedell, Joseph J McDonald, Thomas E Barta, Daniel P Becker, Rao N Shashidhar, John N Freskos, Brent V Mischke, Daniel P Getman, Gary A DeCrescenzo, Clara I Villamil
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Patent number: 7091199Abstract: The compounds are of the class of thienoisoxazole phenoxy unsubstituted ethyl and propyl derivatives, useful as D4 antagonists. Said compounds are useful for the treatment of medical conditions mediated by inhibition of D4 receptor. These conditions comprise, for example, Attention Deficit Hyperactivity Disorder, Obsessive-Compulsive Disorder, Psychoses, Substance Abuse, Substance Dependence, Parkinson's Disease, Parkinsonism, Tardive Diskinesia, Gilles de la Tourette Syndrome, Conduct Disorder, and Oppositional Defiant Disorder. A further aspect of the invention is to provide a pharmaceutical composition, intermediates, and a method of making said class of compounds.Type: GrantFiled: September 13, 2000Date of Patent: August 15, 2006Assignee: Aventis Pharmaceuticals Inc.Inventors: George E. Lee, John G. Jurcak, Timothy A. Ayers
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Patent number: 7074808Abstract: Compounds of general formula I R1 is selected from any one of phenyl, pyridinyl, pyrroloyl, thienyl, furanyl, imidazolyl, triazolyl, thiazolyl and pyridine N-oxide; where each R1 phenyl ring and R1 heteroaromatic ring may optionally and independently be further substituted by 1, 2 or 3 substituents selected from straight and branched C1–C6 alkyl, NO2, CF3, C1–C6 alkoxy, chloro, fluoro, bromo, and iodo. The substitutions on the phenyl ring and on the heteroaromatic ring may take place in any position on said ring systems; are disclosed and claimed in the present application, as well as salts and pharmaceutical compositions comprising the novel compounds and their use in therapy, in particular in the management of pain, anxiety and functional gastrointestinal disorders.Type: GrantFiled: May 16, 2002Date of Patent: July 11, 2006Assignee: AstraZeneca ABInventors: Zhongyong Wei, William Brown, Christopher Walpole