1,3-diazole Ring (including Hydrogenated) Patents (Class 544/370)
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Patent number: 7420057Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.Type: GrantFiled: October 12, 2006Date of Patent: September 2, 2008Assignee: Boehringer Ingelheim Pharma KGInventors: Carlo Bombarda, Enrica Dubini, Antoine Ezhaya, Margarete Schneider, legal representative, Heinrich Schneider
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Publication number: 20080207589Abstract: The present invention relates to new substituted imidazole compounds have the following Formula (I) and to the pharmaceutically acceptable salts, esters, or prodrugs thereof, to compositions of the compounds together with pharmaceutically acceptable carriers, and to uses of the compounds:Type: ApplicationFiled: January 3, 2008Publication date: August 28, 2008Inventors: Rustum Boyce, Eric Martin, Weibo Wang, Hong Yang, Paul A. Barsanti
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Publication number: 20080200455Abstract: 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: ApplicationFiled: August 20, 2007Publication date: August 21, 2008Applicant: WyethInventors: Michael Gerard Kelly, Derek Cecil Cole
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Patent number: 7414058Abstract: There is disclosed a method for the treatment of Extra Pyramidal syndrome (EPS) comprising the administration of an adenosine A2a receptor antagonist, alone or in combination with other agents useful for treating EPS.Type: GrantFiled: December 17, 2003Date of Patent: August 19, 2008Assignee: Schering CorporationInventors: Michael Grzelak, John Hunter, Annamarie Pond, Geoffrey Varty
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Publication number: 20080188486Abstract: The present invention relates to compounds of formula I wherein one of R1 and R2 is hydrogen and the other one is and wherein A and R1 to R4 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are useful for the treatment and/or prevention of diseases which are associated with the modulation of H3 receptors.Type: ApplicationFiled: January 23, 2008Publication date: August 7, 2008Inventors: Matthias Nettekoven, Olivier Roche
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Patent number: 7396834Abstract: Compounds of general formula: wherein R1 and R2 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared. They are useful in therapy, in particular in the management of pain.Type: GrantFiled: November 5, 2003Date of Patent: July 8, 2008Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Niklas Plobeck, Christopher Walpole
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Publication number: 20080139534Abstract: Disclosed are bisbenzamidine and bisbenzamidoxime compounds useful for treatment of treatment of trypanosomiasis. The compounds disclosed are useful for treating mammals infected with parasitic hemoflagellates, in particular Trypanosoma brucei gambiense and Trypanosoma brucei rhodesiense.Type: ApplicationFiled: December 7, 2007Publication date: June 12, 2008Applicant: XAVIER UNIVERSITY OF LOUISIANAInventors: Tien L. HUANG, Jean Jacques VANDEN EYNDE, Annie MAYENCE, Cyrus BACCHI, Isaac O. DONKOR, Nageswara R. KODE
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Publication number: 20080132495Abstract: The invention provides a compound of the formula (I): or a salt, solvate, tautomer or N-oxide thereof, wherein M is selected from a group D1 and a group D2: and R?, E, A and X are as defined in the claims. Also provided are pharmaceutical compositions containing the compounds, processes for making the compounds and the use of the compounds in the prophylaxis or treatment of a disease state mediated by a CDK kinase, GSK-3 kinase or Aurora kinase.Type: ApplicationFiled: December 30, 2005Publication date: June 5, 2008Applicant: ASTEX THERAPEUTICS LIMITEDInventors: Valerio Berdini, Maria Grazia Carr, Adrian Liam Gill, Steven Howard, Eva Figueroa Navarro, Gary Trewartha, David Charles Rees, Mladen Vinkovic, Paul Graham Wyatt
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Publication number: 20080132496Abstract: Substituted carboxylic acid amides of general formula wherein A, B, and R1 to R5 are as defined herein, and the tautomers and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties, such as antithrombotic activity and factor Xa-inhibiting activity.Type: ApplicationFiled: November 30, 2007Publication date: June 5, 2008Applicant: Boehringer Ingelheim Pharma GmbH & Co. KGInventors: James Gillard, Sandra Ruth Handschuh, Herbert Nar, Roland Pfau, Henning Priepke, Wolfgang Wienen, Annette Mario Schuler-Metz, Eckhart Bauer, Georg Dahmann, Kai Gerlach
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Patent number: 7381726Abstract: The invention relates to new crystalline modifications of the hydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine, crystalline modification of the dihydrochloride of 1-[4-(5-cyanoindol-3-yl)butyl]-4-(2-carbamoyl-benzofuran-5-yl)-piperazine and amorphous 1-[4-(5-cyanoindol-3-yl)butyl]4-(2-carbamoyl-benzofuran-5-yl)-piperazine hydrochloride which are suitable in particular for the preparation of solid medicaments for the treatment or prevention of depressive disorders, anxiety disorders, bipolar disorders, mania, dementia, substance-related disorders, sexual dysfunctions, eating disorders, obesity, fibromyalgia, sleeping disorders, psychiatric disorders, cerebral infarct, tension, for the therapy of side-effects in the treatment of hypogonadism, secondary amenorrhea, premenstrual syndrome and undesired puerperal lactation.Type: GrantFiled: June 5, 2002Date of Patent: June 3, 2008Assignee: Merck Patentgesellschaft mit Beschrankter HaftungInventors: Andreas Bathe, Bernd Helfert, Steffen Neuenfeld, Heike Kniel, Matthias Bartels, Susanne Rudolph, Henning Böttcher
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Patent number: 7361657Abstract: This invention concerns the use of compounds of formula (I) wherein ?a1=a2?a3=a4—is a radical of formula —CH?CH—CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N—wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections.Type: GrantFiled: January 12, 2006Date of Patent: April 22, 2008Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7351822Abstract: 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: March 18, 2004Date of Patent: April 1, 2008Assignee: 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, Peter Robert Guzzo, Michael John Mayer
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Patent number: 7351828Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction.Type: GrantFiled: October 31, 2003Date of Patent: April 1, 2008Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Pramila A. Bhatia, Jerome F. Daanen, Andrew O. Stewart, Meena V. Patel, Teodozyj Kolasa, Jorge D. Brioni, Jeffrey Rohde
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Publication number: 20080058297Abstract: This invention relates to pyrimidine compounds of formula (I), formula (I?), and formula (I?): and pharmaceutically acceptable salts, solvates, clathrates, and prodrugs thereof, wherein R1, R2, R3, R4, R5, U, V, W, X, Y, Z, and n are defined herein. This invention also relates to compositions comprising these compounds and methods for using them. The compounds and compositions of this invention are useful to treat or prevent disorders associated with excessive bone loss, including, without limitation periodontal disease, non-malignant bone disorders (such as osteoporosis, Pagers-disease of bone, osteogenesis imperfecta, fibrous dysplasia, and primary hyperparathyroidism) estrogen deficiency, inflammatory bone loss, bone malignancy, arthritis, osteopetrosis, and certain cancer-related disorders (such as hypercalcemia of malignancy (HCM), osteolytic bone lesions of multiple myeloma and osteolytic bone metastases of breast cancer and other metastatic cancers).Type: ApplicationFiled: May 28, 2004Publication date: March 6, 2008Applicant: Synta Pharmaceuticals Corp.Inventors: Mitsunori Ono, Lijun Sun, Yumiko Wada, Keizo Koya, Masazumi Nagai
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Patent number: 7335660Abstract: This invention relates to compounds of formula (I) where R1 to R12, —W—V—, —X—Y—, p and n have the values defined in claim 1, their preparation and use as pharmaceuticals for the treatment of central nervous system disorders, such as depression, bipolar disorder, and anxiety.Type: GrantFiled: December 6, 2002Date of Patent: February 26, 2008Assignee: Eli Lilly and CompanyInventors: Javier Agejas-Chicharro, Graham Henry Timms, Andrew Caerwyn Williams, Nicholas Paul Camp, Jeremy Gilmore, Ana Belen Bueno Melendo, Carlos Lamas-Peteira
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Patent number: 7329749Abstract: Compound of the formula (I) in which R1, R2 and alk are as defined in Claim 1, are potent 5-HT2A antagonist and are suitable for the treatment of psychoses, schizophrenia, depression, neurological disorders, memory disorders, Parkinson's disease, amyotrophic lateral sclerosis, Alzheimer's disease, Hutington's disease, eating disorders, such as bulimia, anorexia nervosa, premenstrual syndrome and/or for positively influencing obsessive-compulsive disorder (OCD).Type: GrantFiled: December 24, 2001Date of Patent: February 12, 2008Assignee: Merck Patent GesellschaftInventors: Henning Boettcher, Gerd Bartoszyk, Juergen Harting, Christoph van Amsterdam, Christoph Seyfried
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Publication number: 20080032994Abstract: The present invention relates to the compounds of formula (I), their preparation and use as antifungal and/or antibacterial agents. where the values for R1, R2, R3, R4, R5 and A are as defined herein.Type: ApplicationFiled: November 2, 2006Publication date: February 7, 2008Inventors: Marcel Borgers, Maarten van Geffen, Jannie Ausma
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Publication number: 20080027053Abstract: This invention includes oxazolidinone prodrug compounds of Formula (I) and Formula (II) as defined herein. The prodrugs are convertible by natural biological processes into an active ingredient possessed of antimicrobial properties useful in treating bacterial infections in mammals.Type: ApplicationFiled: July 9, 2007Publication date: January 31, 2008Inventors: Mark J. Macielag, Manomi A. Tennakoon
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Patent number: 7309703Abstract: 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: August 10, 2001Date of Patent: December 18, 2007Assignee: Ortho McNeil Pharmaceutical, Inc.Inventors: Mary Pat Beavers, J. Guy Breitenbucher, Hui Cai, James P. Edwards, Cheryl A. Grice, Darin J. Gustin, Haripada Khatuya, Steven P. Meduna, Barbara A. Pio, Kevin L. Tays, Jianmei Wei
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Patent number: 7291642Abstract: The present invention provides bradykinin-B1 antagonists of the formula in which A, Ar, G, Q, R1 and R4 are as defined in claim 1, their enantiomers, their diastereomers, their mixtures and their salts, in particular their physiologically acceptable salts with organic or inorganic acids or bases having useful properties, their preparation, medicaments comprising the pharmacologically effective compounds, their preparation and their use.Type: GrantFiled: October 21, 2005Date of Patent: November 6, 2007Assignee: Boehringer Ingelheim International GmbHInventors: Iris Kauffmann-Hefner, Norbert Hauel, Henri Doods, Angelo Ceci, Stefan Peters
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Publication number: 20070249608Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: ApplicationFiled: April 18, 2007Publication date: October 25, 2007Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 7271261Abstract: 2-Aryl substituted benzimidazoles and imidazo[4,5]pyridines are disclosed as inhibitors of Cds1 and useful as adjuvants to chemotherapy or radiation therapy in the treatment of cancer.Type: GrantFiled: October 18, 2002Date of Patent: September 18, 2007Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Kristen L. Arienti, Frank U. Axe, J. Guy Breitenbucher, Liming Huang, Alice Lee, Kelly J. McClure
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Patent number: 7253173Abstract: Compounds of general formula (I) wherein R1, R2 and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.Type: GrantFiled: November 5, 2003Date of Patent: August 7, 2007Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin, Paul Jones, Daniel Pagé, Niklas Plobeck, Christopher Walpole
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Patent number: 7244847Abstract: The present invention is directed to novel benzimidazoles according to representative structures I and II, and their derivatives that possess antibacterial activity. This invention is also directed to compositions including the benzimidazole derivatives, and methods for using the same.Type: GrantFiled: February 6, 2002Date of Patent: July 17, 2007Assignee: Isis Pharmaceuticals, Inc.Inventors: Eric E. Swayze, Yun He, Punit P. Seth, Elizabeth Anne Jefferson
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Patent number: 7241787Abstract: The invention relates to substituted N-cyclohexylheterocycles and to the physiologically tolerated salts and physiologically functional derivatives thereof, to processes for their preparation and to their use as medicaments. Compounds of the formula I, in which the radicals have the stated meanings, and the physiologically tolerated salts thereof, and process for their preparation are described. The compounds bring about for example a weight reduction in mammals and are suitable for example for the prevention and treatment of obesity and diabetes.Type: GrantFiled: January 25, 2005Date of Patent: July 10, 2007Assignee: Sanofi-Aventis Deutschland GmbHInventors: Lothar Schwink, Thomas Boehme, Matthias Gossel, Siegfried Stengelin
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Patent number: 7241764Abstract: Compounds of general formula:[Chemical formula should be inserted here. Please see paper copy] wherein R1, R2, and R3 are as defined in the specification, as well as salts, enantiomers thereof and pharmaceutical compositions including the compounds are prepared.Type: GrantFiled: November 5, 2003Date of Patent: July 10, 2007Assignee: AstraZeneca ABInventors: William Brown, Andrew Griffin
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Patent number: 7238695Abstract: The present invention is directed to imidazolyl derivatives or pharmaceutically acceptable salts thereof which are useful as agonists or antagonists of somatostatin receptors, having the following formula (I), wherein the substituents are defined in the specification.Type: GrantFiled: February 4, 2004Date of Patent: July 3, 2007Assignee: Societe de Conseils de Recherches et d'Applications Scientifiques, SASInventors: Christophe Alain Thurieau, Lydie Francine Poitout, Marie-Odile Galcera, Christophe Philippe Moinet, Thomas D. Gordon, Barry A. Morgan
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Patent number: 7238712Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds of the formula and the pharmaceutically acceptable salts thereof, or a pharmaceutical composition thereof, wherein represents a single or double bond; one Z2 is CA or CR8A and the other is CR1, CR12, NR6 or N wherein each R1, R6 and R8 is independently hydrogen or noninterfering substituent; A is —Wi—COXjY wherein Y is COR2 or an isostere thereof and R2 is hydrogen or a noninterfering substituent, each of W and X is a spacer of 2–6 ?, and each of i and j is independently 0 or 1; Z3 is NR7 or O; each R3 is independently a noninterfering substituent; n is 0–3; each of L1 and L2 is a linker; each R4 is independently a noninterfering substituent; m is 0–4; Z1 is CR5 or N wherein R5 is hydrogen or a noninterfering substituent; each of l and k is an integer from 0–2 wherein the sum of l and k is 0–3; Ar is an aryl group substituted with 0–5 noninterfering substituents, wherein two noninterfering substituents can form a fused ring; aType: GrantFiled: May 28, 2002Date of Patent: July 3, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 7235661Abstract: The present invention relates to the use of compounds of formula (I) for the treatment of sexual dysfunction and to compositions containing compounds of formula (I) for the treatment of sexual dysfunction, wherein A, L, D and B1, are as described in the specification.Type: GrantFiled: March 31, 2006Date of Patent: June 26, 2007Assignee: Abbott LaboratoriesInventors: Marlon D. Cowart, Steven P. Latshaw, Sherry L. Nelson, Andrew O. Stewart
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Patent number: 7223764Abstract: The present invention is directed to a 2,4-bis(trifluoroethoxy)pyridine compound represented by formula (1): (wherein X1 represents a fluorine atom or a hydrogen atom) or a salt thereof, and to a drug containing the compound or the salt as an active ingredient. The compound has metabolic resistance in human liver microsome, good absorbability upon oral administration, and excellent ACAT inhibitory activity.Type: GrantFiled: July 6, 2004Date of Patent: May 29, 2007Assignee: Kowa Co., Ltd.Inventors: Kimiyuki Shibuya, Tadaaki Ohgiya, Takayuki Matsuda, Toru Miura
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Patent number: 7214796Abstract: This invention relates to a method for producing 1-[2-(benzimidazol-2-ylthio)ethyl]piperazine (5) or its salt by the following reaction scheme: This invention enables efficient production of 1-[2-(benzimidazol-2-ylthio) ethyl]piperazine or its salt which is an intermediate in the production of a cyclic diamine compound which is useful as a ACAT inhibitor.Type: GrantFiled: November 27, 2003Date of Patent: May 8, 2007Assignee: Kowa Co., Ltd.Inventors: Kimiyuki Shibuya, Yukihiro Sato
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Patent number: 7214679Abstract: Compounds of the formula: wherein the substituents are as defined herein are useful for treating conditions mediated by p38 kinase.Type: GrantFiled: January 13, 2004Date of Patent: May 8, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sundeep Dugar, Gregory R. Luedtke, Xuefei Tan, Glen McEnroe
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Patent number: 7214802Abstract: Disclosed compounds of formula (I) which inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease. Also disclosed are processes for preparing these compounds and pharmaceutical compositions comprising these compounds.Type: GrantFiled: March 7, 2005Date of Patent: May 8, 2007Assignee: Boehringer Ingelheim Pharmaceuticals, Inc.Inventors: Derek Cogan, Ming-Hong Hao, Victor Marc Kamhi, Craig Andrew Miller, Matthew Russell Netherton, Alan David Swinamer
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Patent number: 7202233Abstract: A pharmaceutical composition an inclusion complex and methods for treating patients and preparing said complex disclosed for transmucosal delivery comprising an inclusion complex of (a) alprazolam and (b) a water soluble 2-hydroxypropyl-beta-cyclodextrin, and a pharmaceutically acceptable carrier therefor, wherein all the alprazolam is present in ring-closed form.Type: GrantFiled: June 3, 2005Date of Patent: April 10, 2007Assignee: Farmarc Nederland BVInventor: Lawrence John Penkler
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Patent number: 7189726Abstract: The invention is directed to methods to inhibit p38-? kinase using compounds which contain an aromatic residue coupled to an benzofuran moiety through a piperidine.Type: GrantFiled: May 14, 2002Date of Patent: March 13, 2007Assignee: Scios, Inc.Inventors: Babu J. Mavunkel, Sarvajit Chakravarty, John J. Perumattam, Sundeep Dugar, Qing Lu, Xi Liang
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Patent number: 7186724Abstract: The invention relates to heterocyclic substituted carbonyl derivatives that display selective binding to dopamine D3 receptors. In another aspect, the invention relates to a method for treating central nervous system disorders associated with the dopamine D3 receptor activity in a patient in need of such treatment comprising administering to the subject a therapeutically effective amount of said compounds for alleviation of such disorder. The central nervous system disorders that may be treated with these compounds include Psychotic Disorders, Substance Dependence, Substance Abuse, Dyskinetic Disorders (e.g. Parkinson's Disease, Parkinsonism, Neuroleptic-Induced Tardive Dyskinesia, Gilles de la Tourette Syndrome and Huntington's Disease), Dementia, Anxiety Disorders, Sleep Disorders, Circadian Rhythm Disorders and Mood Disorders.Type: GrantFiled: April 6, 2004Date of Patent: March 6, 2007Assignee: Aventis Pharmaceuticals Inc.Inventors: James A Hendrix, Horst Hemmerle, Matthias Urmann, Gregory M Shutske, Jospeh T Strupczewski, Kenneth J Bordeau, John G Jurcak, Thaddeus Nieduzak, Sharon A Jackson, Paul Angell, James P Carey, George Lee, David Fink, Jean-Fancois Sabuco, Yulin Chiang, Nicola Collar
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Patent number: 7183410Abstract: The invention relates to the polymorph A of flibanserin, to a technical process for the preparation thereof, as well as to the use thereof for preparing medicaments.Type: GrantFiled: August 1, 2002Date of Patent: February 27, 2007Assignee: Bidachem S.p.A.Inventors: Carlo Bombarda, Enrica Dubini, Antoine Ezhaya, Margarete Schneider, legal representative, Heinrich Schneider, deceased
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Patent number: 7173034Abstract: This invention concerns the use of compounds of formula (I) wherein -a1=a2-a3=a4- is a radical of for CH?CH—, —N?CH—CH?CH—, —CH?N—CH?CH—, —CH?CH—N?CH—, —CH?CH—CH?N— wherein each hydrogen atom may optionally be substituted; Q is a radical of formulas (b-1), (b-2), (b-3), (b-4), (b-5), (b-6), (b-7), (b-8), G is a direct bond or C1-10alkanediyl; R1 is an optionally substituted monocyclic heterocycle; for the manufacture of a medicament for the treatment of viral infections, in particular RSV infections. Certain compounds of formula (I) are new.Type: GrantFiled: June 3, 2005Date of Patent: February 6, 2007Assignee: Janssen Pharmaceutica, N.V.Inventors: Frans Eduard Janssens, Kathleen Petrus Marie-José Meersman, François Maria Sommen, Jérôme Emile Georges Guillemont, Jean Fernand Armand Lacrampe, Koenraad Jozef Lodewijk Marcel Andries
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Patent number: 7169775Abstract: Amino methyl imidazoles of Formula I are provided: wherein R, R1, R2, R3, R4, R5, and R6 are defined herein. Such compounds are ligands of C5a receptors. Preferred compounds of Formula I bind to C5a receptors with high affinity and exhibit neutral antagonist or inverse agonist activity at C5a receptors. This invention also relates to pharmaceutical compositions comprising such compounds. It further relates to the use of such compounds in treating a variety of inflammatory, cardiovascular, and immune system disorders. Additionally, this invention provides labeled amino methyl imidazoles compounds, which are useful as probes for the localization of C5a receptors.Type: GrantFiled: August 21, 2003Date of Patent: January 30, 2007Assignee: Neurogen CorporationInventors: Andrew Thurkauf, He Zhao, Suoming Zhang, Yang Gao
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Patent number: 7160912Abstract: The present invention relates to novel oxazolidinone compounds of formula (I), their stereoisomers, their salts and pharmaceutical compositions containing them. The present invention also relates to a process for the preparation of the above said novel compounds, their stereoisomers, their salts and pharmaceutical compositions.Type: GrantFiled: July 3, 2003Date of Patent: January 9, 2007Assignees: Dr.Reddy's Laboratories Ltd., Dr. Reddy's Laboratories, Inc.Inventors: Natesan Selvakumar, Jagattaran Das, Sanjay Trehan, Javed Iqbal, Magadi Sitaram Kumar, Ramanujam Rajagopalan, Mamidi Naga Venkata Srinivasa Rao
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Patent number: 7160886Abstract: Certain novel N-acylated piperazine 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: February 27, 2004Date of Patent: January 9, 2007Assignee: Merck & Co., Inc.Inventors: Raman K. Bakshi, Liangqin Guo, Qingmei Hong, Ravi P. Nargund, Patrick G. Pollard, Iyassu K. Sebhat, Feroze Ujjainwalla, Zhixiong Ye
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Patent number: 7157464Abstract: Compounds are provided that act as potent antagonists of the CCR1 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR1. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.Type: GrantFiled: June 11, 2003Date of Patent: January 2, 2007Assignee: Chemocentryx, Inc.Inventors: Andrew M. K. Pennell, James B. Aggen, J.J. Kim Wright, Subrabrata Sen, Brian E. McMaster, Daniel Joseph Dairaghi
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Patent number: 7144883Abstract: The present invention relates to substituted sulfonamide compounds of the general formula (I), wherein P is sulfonamide or amide-substituted sulfonic acid, which compounds are potentially useful for the prophylaxis and treatment of medical conditions relating to obesity, type II diabetes and/or disorders of the central nervous systemType: GrantFiled: June 11, 2002Date of Patent: December 5, 2006Assignee: Biovitrum ABInventors: Patrizia Caldirola, Gary Johansson, Andrew Mott, Katarina Beierlien, Markus Thor, Lars Tedenborg, Ulf Bremberg, Annika Jenmalm Jensen
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Patent number: 7138420Abstract: Disclosed are substituted benzimidazole compounds of formula (I): wherein R1, R2, R3, R4 and Xa are defined herein. The compounds of the invention inhibit Itk kinase and are therefore useful for treating diseases and pathological conditions involving inflammation, immunological disorders and allergic disorders. Also disclosed are processes for preparing these compounds and to pharmaceutical compositions comprising these compounds.Type: GrantFiled: August 1, 2003Date of Patent: November 21, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Joerg Martin Bentzien, Brian Nicholas Cook, Charles Cywin, Roman Wolfgang Fleck, Ho Yin Lo, Peter Allen Nemoto, Steven S. Pullen, Gregory Paul Roth, Roger John Snow, Hidenori Takahashi, Ji Wang, Kevin J. Moriarty, Lei Qiao, Michael Winters
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Patent number: 7135473Abstract: A cyclic diamine compound of formula (1): wherein R1 and R2 are individually a hydrogen atom or a methoxy group, provided R1 is a methoxy group when R2 is a hydrogen atom, or a hydrogen atom when R2 is a methoxy group; A is an oxygen atom, a sulfur atom, CH?CH, CH?N or NR3, in which R3 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; B is a nitrogen atom, CH or CR4, in which R4 is a hydrogen atom, or a lower alkyl, hydroxy lower alkyl, lower alkoxy lower alkyl, aryl or aryl lower alkyl group; m is 1 or 2; and n is a number of 1 to 5, an acid-addition salt thereof, or a hydrate thereof. The compound has inhibitory effects on cell adhesion and is useful for treatment of allergy, asthma, rheumatism, arteriosclerosis, and inflammation.Type: GrantFiled: August 13, 2003Date of Patent: November 14, 2006Assignee: Kowa Co., Ltd.Inventors: Tatsuhiko Kodama, Masahiro Tamura, Toshiaki Oda, Yukiyoshi Yamazaki, Masahiro Nishikawa, Takeshi Doi, Yoshinori Kyotani
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Patent number: 7132421Abstract: The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activityType: GrantFiled: June 15, 2004Date of Patent: November 7, 2006Assignee: Hoffmann-La Roche Inc.Inventors: Nader Fotouhi, Emily Aijun Liu, Binh Thanh Vu
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Patent number: 7125877Abstract: This invention provides compounds which are represented by a general formula [I] [in which X stands for hydrogen or halogen; B stands for halogen, cyano or optionally fluorine-substituted lower alkyl; D stands for a 3–10 membered aliphatic nitrogen-containing heterocyclic group; R3, R4 and R5 may be same or different, and each stands for hydrogen, lower alkyl optionally having substituent group(s) and the like; and a is 0 or 1]. These compounds exhibit high affinity to nociceptin receptors and whereby inhibit actions of nociceptin, and are useful as an analgesic, antiobestic, agent for ameliorating brain function, treating agents for Alzheimer's disease and dementia, and therapeutic agents for schizophrenia, neurodegenerative diseases, depression, diabetes insipidus, polyuria, hypotension and the like.Type: GrantFiled: May 14, 2003Date of Patent: October 24, 2006Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Kensuke Kobayashi, Hirobumi Takahashi, Hiroshi Kawamoto, Tetsuya Kato, Satoru Itoh, Takashi Yoshizumi, Osamu Okamoto
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Patent number: 7119086Abstract: The invention relates to compounds of formula: and also to the salts thereof with mineral or organic acids, and the solvates and/or hydrates thereof, with affinity for and selectivity towards the arginine-vasopressin V1b receptors and/or for the ocytocin receptors and, furthermore, for certain compounds, affinity for the V1a receptors. The invention also relates to the process for preparing them, to the intermediate compounds of formula (IV) that are useful for preparing them, to pharmaceutical compositions containing them and to their use for preparing medicinal products.Type: GrantFiled: July 15, 2002Date of Patent: October 10, 2006Assignee: Sanofi-AventisInventors: Alain Di Malta, Georges Garcia, Richard Roux, Bruno Schoentjes, Claudine Serradeil-Le Gal, Bernard Tonnerre, Jean Wagnon
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Patent number: 7115644Abstract: Disclosed are benzimidazolone compounds of formulas (I) & (II): wherein R1, R2, R3, R4, R5, X, L, m, n and t are defined herein. The compounds inhibit production of cytokines involved in inflammatory processes and are thus useful for treating diseases and pathological conditions involving inflammation such as chronic inflammatory disease.Type: GrantFiled: September 3, 2003Date of Patent: October 3, 2006Assignee: Boehringer Ingelheim Pharmaceuticals Inc.Inventors: Antonio Jose del Moral Barbosa, Jr., Daniel R. Goldberg, Abdelhakim Hammach, Pingrong Liu, Neil Moss, Mark Stephen Ralph, Gregory Paul Roth, Christopher Ronald Sarko, Fariba Soleymanzadeh, Andre White
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Patent number: RE39608Abstract: Compounds of the formula Ia or IB where A is a saturated or monounsaturated heterocyclic, 4 - to 8-membered ring which contains one or two nitrogen atoms, and their tautomeric forms, possible enantiomeric and diastereomeric forms, their prodrugs and possible physiologically tolerated salts are useful as inhibitors of the enzyme poly(ADP-ribose)polymerase.Type: GrantFiled: November 23, 1999Date of Patent: May 1, 2007Assignee: Abbott GmbH & Co. KGInventors: Wilfried Lubisch, Michael Kock, Thomas Höger, Sabine Schult, Roland Grandel, Reinhold Müller