The Additional Hetero Ring Contains Ring Nitrogen Patents (Class 514/210.2)
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Publication number: 20110105454Abstract: The present invention relates to novel substituted oxindole derivatives of the formula (I), pharmaceutical agents containing said derivatives, and the use thereof for the treatment of vasopressin-dependent illnesses.Type: ApplicationFiled: December 23, 2008Publication date: May 5, 2011Applicant: Abbott GmbH & Co. KGInventors: Wilfried Braje, Astrid Netz, Thorsten Oost, Wolfgang Wernet, Andrea Hager-Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
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Publication number: 20110105456Abstract: The present invention relates to certain 3-phenyl-pyrazole derivatives of Formula (Ia) and pharmaceutical compositions thereof that modulate the activity of the 5-HT2A serotonin receptor. Compounds and pharmaceutical compositions thereof are directed to methods useful in the treatment of platelet aggreagation, coronary artery disease, myocardial infarction, transient ischemic attack, angina, stroke, atrial fibrillation, reducing the risk of blood clot formation, asthma or symptoms thereof, agitation or a symptom, behavioral disorders, drug induced psychosis, excitative psychosis, Gilles de la Tourette's syndrome, manic disorder, organic or NOS psychosis, psychotic disorder, psychosis, acute schizophrenia, chronic schizophrenia, NOS schizophrenia and related disorders, and sleep disorders, sleep disorders, diabetic-related disorders, progressive multifocal leukoencephalopathy and the like.Type: ApplicationFiled: December 22, 2010Publication date: May 5, 2011Inventors: Bradley Teegarden, Yifeng Xiong, Sonja Strah-Pleynet, Honnappa Jayakumar, Peter I. Dosa, Konrad Feichtinger, Matin Casper, Juerg Lehmann, Robert M. Jones, David J. Unett, Jin Sun Karoline Choi
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Publication number: 20110105455Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: ApplicationFiled: October 28, 2010Publication date: May 5, 2011Inventors: STEVEN J. COATS, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Publication number: 20110098269Abstract: The present invention provides compounds according to Formulas I, II, III, IV, V, VI, VII or VIII: their use as H3 antagonists/inverse agonists, processes for their preparation, and pharmaceutical compositions thereof.Type: ApplicationFiled: November 17, 2010Publication date: April 28, 2011Applicant: Cephalon, Inc.Inventors: Nadine C. Becknell, Reddeppa reddy Dandu, Derek D. Dunn, Robert L. Hudkins, Kurt A. Josef, Babu G. Sundar, Allison L. Zulli
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Publication number: 20110098268Abstract: The present invention relates to a novel class of substituted spirocyclic compounds. These compounds can inhibit histone deacetylase and are suitable for use in selectively inducing terminal differentiation, and arresting cell growth and/or apoptosis of neoplastic cells, thereby inhibiting proliferation of such cells. Thus, the compounds of the present invention are useful in treating a patient having a tumor characterized by proliferation of neoplastic cells. The compounds of the invention may also be useful in the prevention and treatment of TRX-mediated diseases, such as autoimmune, allergic and inflammatory diseases, and in the prevention and/or treatment of diseases of the central nervous system (CNS), such as neurodegenerative diseases.Type: ApplicationFiled: October 26, 2010Publication date: April 28, 2011Applicant: MERCK & CO., IncInventors: Dawn M. Mampreian, Joey L. Methot, Thomas Miller, Paul Tempest, Anna A. Zabierek
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Publication number: 20110098267Abstract: The invention relates to a topical composition and a method for treating psoriasis. The topical composition comprises one or more compound that inhibits the production of IL-12 and IL-23.Type: ApplicationFiled: February 6, 2009Publication date: April 28, 2011Applicant: Synta Pharmaceuticals CorporationInventors: Suresh R. Babu, Yumiko Wada, Jianhua Shen, Nhung Nguyen
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Patent number: 7932246Abstract: Compounds of formula: (I), and salts, N-oxides, hydrates and solvates thereof are histone deacetylase inhibitors and are useful in the treatment of cell proliferative diseases, including cancers: (I) wherein Q, V and W independently represent —N? or —C?; B is a divalent radical selected from: (IIA), (IIB), (IIC), (IID), and (IIE). Wherein the bond marked * is linked to the ring containing Q, V and W through -[Linker1]- and the bond marked ** is linked to A through -[Linker2]-; A is an optionally substituted mono-, bi- or tri-cyclic carbocyclic or heterocyclic ring system; and -[Linker1]- and -[Linker2]- independently represent a bond, or a divalent linker radical.Type: GrantFiled: May 15, 2006Date of Patent: April 26, 2011Assignee: Chroma Therapeutics Ltd.Inventors: David Festus Charles Moffat, Sanjay Ratilal Patel, Francesca Ann Mazzei, Andrew James Belfield, Sandra Van Meurs
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Publication number: 20110092474Abstract: Diamino-pyridine, pyrimidine and pyridazine compounds which may be used as H4 receptor modulators, and in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, such as allergy, asthma, autoimmune diseases, and pruritis.Type: ApplicationFiled: June 11, 2009Publication date: April 21, 2011Inventors: Hui Cai, Frank Chavez, Paul J. Dunford, Andrew J. Greenspan, Steven P. Meduna, Jorge A. Quiroz, Brad M. Savall, Kevin L. Tays, Robin L. Thurmond, Jianmei Wei, Ronald L. Wolin, Xiaohu Zhang
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Publication number: 20110086836Abstract: The present invention relates to substituted phenylpiperidine derivatives as melanocortin-4 receptor modulators. Depending on the structure and the stereochemistry the compounds of the invention are either selective agonists or selective antagonists of the human melanocortin-4 receptor (MC-4R). The agonists can be used for the treatment of disorders and diseases such as obesity, diabetes and sexual dysfunction, whereas the antagonists are useful for the treatment of disorders and diseases such as cancer cachexia, muscle wasting, anorexia, anxiety and depression. Generally all diseases and disorders where the regulation of the MC-4R is involved can be treated with the compounds of the invention.Type: ApplicationFiled: April 5, 2007Publication date: April 14, 2011Applicant: Santhera Pharmaceuticals (Schweiz) AGInventors: Michael Soeberdt, Holger Deppe, Philipp Weyermann, Stephan Bulat, Andreas Von Sprecher, Achim Feurer, Cyrille Lescop, Marco Hennebohle, Sonja Nordhoff
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Publication number: 20110086832Abstract: The present application relates to thiazolylidene containing compounds of formula (I) wherein R1, R2, R3, R4, L2 and A are as defined in the specification. Compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions are also disclosed.Type: ApplicationFiled: December 16, 2010Publication date: April 14, 2011Applicant: ABBOTT LABORATORIESInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez-Medrano, Xueqing Wang, Sridhar Peddi, William A. Carroll, Michael J. Dart
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Patent number: 7919488Abstract: The present invention provides compounds of formula (I), or pharmaceutically acceptable salts or solvates thereof, methods for their preparation, methods for their use, and pharmaceutical formulations comprising them.Type: GrantFiled: June 28, 2007Date of Patent: April 5, 2011Assignee: Pfizer Inc.Inventors: Simon Paul Planken, Scott Channing Sutton, Rongliang Chen
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Publication number: 20110071125Abstract: This invention relates to novel substituted phenylamino-benzene compounds, pharmaceutical compositions containing such compounds and the use of those compounds or compositions for treating hyper-proliferative and/or angiogenesis disorders, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: May 9, 2008Publication date: March 24, 2011Inventors: Joachim Rudolph, Jaques Dumas, Li Yingfu, Daniel Auclair, Mario Lobell, Marion Hitchcock, Ingo Hartung, Marcus Koppitz, Dominic Brittain, Florian Puehler, Kirstin Petersen, Judith Guenther, Benjamin Bader
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Publication number: 20110071127Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: November 30, 2010Publication date: March 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Malcolm TAYLOR, Chandana CHOWDHURY, Christopher Francis PALMER, Nigel BLUMIRE
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Publication number: 20110071126Abstract: The present invention is directed to a compound represented by the following structural formula or a pharmaceutically acceptable salt thereof. Pharmaceutical compositions and method of use of the compounds are also described.Type: ApplicationFiled: March 12, 2010Publication date: March 24, 2011Inventors: Salvacion CACATIAN, David A. CLAREMON, Lawrence W. DILLARD, Klaus FUCHS, Niklas HEINE, Lanqi JIA, Katerina LEFTHERIS, Brian McKEEVER, Angel MORALES-RAMOS, Suresh B. SINGH, Shankar VENKATRAMAN, Guosheng WU, Zhongren WU, Zhenrong XU, Jing YUAN, Yajun ZHENG
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Patent number: 7906503Abstract: Novel compounds of the structural formula (I) are antagonists and/or inverse agonists of the Cannabinoid-1 (CB1) receptor and are useful in the treatment, prevention and suppression of diseases mediated by the CB1 receptor. The compounds of the present invention are useful as centrally acting drugs in the treatment of psychosis, memory deficits, cognitive disorders, migraine, neuropathy, neuro-inflammatory disorders including multiple sclerosis and Guillain-Barre syndrome and the inflammatory sequelae of viral encephalitis, cerebral vascular accidents, and head trauma, anxiety disorders, stress, epilepsy, Parkinson's disease, movement disorders, and schizophrenia. The compounds are also useful for the treatment of substance abuse disorders, the treatment of obesity or eating disorders, as well as the treatment of asthma, constipation, chronic intestinal pseudo-obstruction, and cirrhosis of the liver.Type: GrantFiled: October 21, 2008Date of Patent: March 15, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Robert K. Baker, Jianming Bao, Shouwu Miao, Kathleen M. Rupprecht
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Publication number: 20110059938Abstract: The present invention encompasses compounds of general formula (1) wherein the groups R2 to R4, L, Q and n are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof for preparing a medicament having the above-mentioned properties.Type: ApplicationFiled: November 15, 2010Publication date: March 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen STEURER, Peter ETTMAYER, Andreas MANTOULIDIS, Ioannis SAPOUNTZIS, Martin STEEGMAIER
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Publication number: 20110059944Abstract: Compounds of Formula I that inhibit Btk are described herein. Pharmaceutical compositions comprising at least one compound of Formula I, together with at least one pharmaceutically acceptable vehicle chosen from carriers, adjuvants, and excipients, are described. Methods of treating patients suffering from certain diseases responsive to inhibition of Btk activity and/or B-cell activity are described. Methods for determining the presence of Btk in a sample are described.Type: ApplicationFiled: November 4, 2010Publication date: March 10, 2011Inventors: Peter A. Blomgren, Kevin S. Currie, Seung H. Lee, Scott A. Mitchell, Jianjun Xu, Aaron C. Schmitt, Zhongdong Zhao, Pavel E. Zhichkin, Douglas G. Stafford, Jeffrey E. Kropf
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Publication number: 20110059937Abstract: This invention relates to novel compounds and compositions thereof, useful in the treatment of disease states mediated by the chemokine, Interleukin-8 (IL-8).Type: ApplicationFiled: November 12, 2010Publication date: March 10, 2011Inventor: Jakob Busch-Petersen
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Publication number: 20110059942Abstract: Compounds of formula (I): or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.Type: ApplicationFiled: October 20, 2008Publication date: March 10, 2011Inventors: Matthew ColinThor Fyfe, William Gattrell, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Patent number: 7902181Abstract: The present invention provides compounds of formula (I) in which n, y, X1, X2, A, B, R1, R2, R3, R4 and R5 are as defined in the specification, a process for their preparation, pharmaceutical compositions containing them and their use in therapy.Type: GrantFiled: December 10, 2008Date of Patent: March 8, 2011Assignee: AstraZeneca ABInventors: Mark Furber, Christopher Andrew Luckhurst, Hitesh Jayantilal Sanganee, Linda Anne Stein, Peter Alan Cage
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Publication number: 20110053907Abstract: Provided herein are substituted pyrimidine and triazine derivatives, including bicyclic pyrimidine derivatives, their pharmaceutical compositions, their preparation, and their use as agents or drugs for cancer therapy, either alone or in combination with radiation and/or other anticancer drugs. In one embodiment, the pyrimidine and triazine derivatives are morpholino-pyrimidine, morpholino-triazine, pyridyl-pyrimidine, and pyridyl-triazine derivatives which are selective irreversible inhibitors of the p110? isoform of PI3K.Type: ApplicationFiled: March 26, 2009Publication date: March 3, 2011Applicant: Auckland UniServices LimitedInventors: Gordon William Rewcastle, Peter Robin Shepherd, Glaire Chaussade, William Alexander Denny, Swarnalatha Akuratiya Gamage
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Publication number: 20110046106Abstract: The present invention relates to compounds of general formula I wherein A, B, R1, R2 and R3 are defined as in claim 1, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: February 5, 2009Publication date: February 24, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Norbert Hauel, Angelo Ceci, Henri Doods, Iris Kauffmann-Hefner, Ingo Konetzki, Annette Schuler-Metz, Rainer Walter
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Publication number: 20110046104Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: October 30, 2009Publication date: February 24, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Paul Mortimore, Julian M.C. Golec, Daniel David Robinson, John Studley
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Publication number: 20110039819Abstract: The present invention relates to substituted phenoxybenzamide compounds of general formula (I): in which R1, R2, R3, R4, R5, X, R6 and q are as defined in the claims, to methods of preparing said compounds, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of a hyper-proliferative and/or angiogenesis disorder, as a sole agent or in combination with other active ingredients.Type: ApplicationFiled: April 9, 2009Publication date: February 17, 2011Inventors: Marion Hitchcock, Ingo Hartung
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Publication number: 20110039817Abstract: 4-Aminopyrimidine derivatives of formula (I) that are useful as histamine H4 receptor antagonists.Type: ApplicationFiled: December 18, 2008Publication date: February 17, 2011Inventors: Elena Carceller González, Eva María Medina Fuentes, Robert Soliva Soliva, Marina Virgili Bernadó, Josep Martí Via
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Publication number: 20110039821Abstract: The present invention relates to a compound of formula (I): or a pharmaceutically acceptable salt or solvate thereof, wherein: Ring A is (4-12)-membered heterocyclyl; Ring B is a fused benzene ring selected from the group consisting of: Ring A, ring B, ring C, R1, R1a, R2, R3, R4, L2, n, t, w, and z are as defined in the specification. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and methods of treating a condition that is mediated by the modulation of glucokinase, the method comprising administering to a mammal an effective amount of a compound of formula (I).Type: ApplicationFiled: October 27, 2010Publication date: February 17, 2011Inventors: Hao Bai, Simon Bailey, Dilip Ramakant Bhumralkar, Feng C. Bi, Fengli Guo, Mingying He, Paul Stuart Humphries, Anthony Lai Ling, Jihong Lou, Seiji Nukui, Ru Zhou
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Patent number: 7888354Abstract: The present invention provides a prophylactic or therapeutic agent for dementia, Alzheimer's disease, attention-deficit hyperactivity disorder, schizophrenia, eating disorders, obesity, diabetes, hyperlipidemia, sleep disorders, narcolepsy, sleep apnea syndrome, circadian rhythm disorder, depression, allergic rhinitis or other diseases. A phenylpyrazole derivative represented by formula (1) or a pharmaceutically acceptable salt thereof: {wherein R1 and R2, which may be the same or different, each represent C1-C6 alkyl or C3-C8 cycloalkyl, or R1 and R2 are attached to each other together with their adjacent nitrogen atom to form a 4- to 7-membered saturated heterocyclic ring (wherein said saturated heterocyclic ring may be substituted with halogen or C1-C6 alkyl), n represents an integer of 0 to 2, T represents a hydrogen atom, halogen or C1-C6 alkyl, and R represents formula (I): or the like}.Type: GrantFiled: November 13, 2008Date of Patent: February 15, 2011Assignee: Taisho Pharmaceutical Co., LtdInventors: Toshio Nakamura, Makoto Tatsuzuki, Dai Nozawa, Tomoko Tamita, Seiji Masuda, Hiroshi Ohta, Shuhei Kashiwa, Aya Fujino, Shigeyuki Chaki, Toshiharu Shimazaki
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Patent number: 7879839Abstract: The present invention relates to compounds having the structure useful as potassium channel inhibitors to treat cardiac arrhythmias, and the like.Type: GrantFiled: July 27, 2005Date of Patent: February 1, 2011Assignee: Merck Sharp & Dohme Corp.Inventors: Christopher J. Dinsmore, Jeffrey M. Bergman, Douglas C. Beshore, B. Wesley Trotter, Kausik K. Nanda, Richard Isaacs, Linda S. Payne, Lou Anne Neilson, Zhicai Wu, Mark T. Bilodeau, Peter J. Manley, Adrienne E. Balitza
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Patent number: 7879838Abstract: The present application discloses a compound, or enantiomers, stereoisomers, rotamers, tautomers, racemates or prodrug of said compound, or pharmaceutically acceptable salts or solvates of said compound, or of said prodrug, said compound having the general structure shown in Formula 1: and the pharmaceutically acceptable salts, solvates or esters thereof. Also disclosed is a method of treating chemokine mediated diseases, such as, palliative therapy, curative therapy, prophylactic therapy of certain diseases and conditions such as inflammatory diseases (non-limiting example(s) include, psoriasis), autoimmune diseases (non-limiting example(s) include, rheumatoid arthritis, multiple sclerosis), graft rejection (non-limiting example(s) include, allograft rejection, xenograft rejection), infectious diseases (e.g, tuberculoid leprosy), fixed drug eruptions, cutaneous delayed-type hypersensitivity responses, ophthalmic inflammation, type I diabetes, viral meningitis and tumors using a compound of Formula 1.Type: GrantFiled: February 14, 2006Date of Patent: February 1, 2011Assignees: Schering Corporation, Pharmacopeia Drug Discovery, Inc.Inventors: Qingbei Zeng, De-Yi Yang, Stuart B. Rosenblum, Michael K. C. Wong, Gopinadhan N. Anilkumar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Neng-Yang Shih, Brian F. McGuinness, Lisa Guise Zawacki, Doublas W. Hobbs
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Publication number: 20110021492Abstract: The present invention provides compounds of Formula (I): or stereoisomers, tautomers, or pharmaceutically acceptable salts thereof, wherein the variables A, L1, L2, R2, R11, and M are as defined herein. These compounds are selective factor XIa inhibitors or dual inhibitors of fXIa and plasma kallikrein. This invention also relates to pharmaceutical compositions comprising these compounds and methods of treating thromboembolic and/or inflammatory disorders using the same.Type: ApplicationFiled: March 12, 2009Publication date: January 27, 2011Inventors: James R. Corte, Zilun HU, Mimi L. Quan
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Publication number: 20110021487Abstract: The present application relates to novel cycloalkoxy-substituted 4-phenyl-3,5-dicyanopyridine derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, preferably for the treatment and/or prevention of cardiovascular and metabolic disorders.Type: ApplicationFiled: January 31, 2009Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Walter Hübsch, Peter Nell, Frank Süssmeier, Alexandros Vakalopoulos, Daniel Meibom, Barbara Albrecht-Küpper, Katja Zimmermann
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Publication number: 20110021486Abstract: Compounds of formula I: wherein X, R2, R3, R3a, R3b, R5 and R6 are defined herein, are useful as inhibitors of the hepatitis C virus NS5B polymerase.Type: ApplicationFiled: December 3, 2008Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. Beaulieu, Pasquale Forgione, Alexandre Gagnon, Cedrickx Godbout, Marc-Andre Terrebonne, Montse Llinas-Brunet, Julie Naud, Martin Poirier, Jean Rancourt
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Publication number: 20110020469Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: September 30, 2010Publication date: January 27, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Michael Mortimore, Damien Fraysse, Alistair Rutherford
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Publication number: 20110021488Abstract: The present invention relates to compounds of general formula I wherein A, B, D, Y, R1, R2, R3, R4 and R5 are defined as in the specification, the enantiomers, the diastereomers, the mixtures and the salts thereof, particularly the physiologically acceptable salts thereof with organic or inorganic acids or bases, which have valuable properties, the preparation thereof, the pharmaceutical compositions containing the pharmacologically effective compounds, the preparation thereof and the use thereof.Type: ApplicationFiled: October 5, 2010Publication date: January 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Iris KAUFFMANN-HEFNER, Norbert HAUEL, Rainer WALTER, Heiner EBEL, Henri DOODS, Angelo CECI, Annette SCHULER-METZ, Ingo KONETZKI
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Publication number: 20110015157Abstract: This invention relates to novel compounds of the Formula (I), (Ia), (Ib), (Ic), (Id), (Ie), (If), (Ig), (Ih); (Ii); (Ij), (Ik), (II) pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are useful for the therapeutic treatment of diseases associated with the modulation or inhibition of 11 ?-HSD1 in mammals. The invention further relates to pharmaceutical compositions of the novel compounds and methods for their use in the reduction or control of the production of cortisol in a cell or the inhibition of the conversion of cortisone to cortisol in a cell.Type: ApplicationFiled: July 25, 2008Publication date: January 20, 2011Inventors: David A. Claremon, Wei He, Gerard McGeehan, Suresh B. Singh, Colin M. Tice, Zhenrong Xu, Yuanjie Ye, Wei Zhao, Linghang Zhuang, Salvacion Cacatian, Katerina Leftheris
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Patent number: 7871999Abstract: The present invention relates to substituted thiazoles, to methods for the production thereof, to medicaments containing these compounds and to the use thereof for producing medicaments.Type: GrantFiled: June 26, 2008Date of Patent: January 18, 2011Assignee: Gruenenthal GmbHInventors: Michael Haurand, Klaus Schiene, Sven Kühnert, Melanie Reich
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Publication number: 20110009377Abstract: The invention relates to azetidine derivatives having the formula (I): Wherein R?, R1, R2, R3, R6, R7, R, Y, A and B are as defined herein. The invention also relates to a method for preparing the same and therapeutic use thereof.Type: ApplicationFiled: June 18, 2010Publication date: January 13, 2011Applicant: SANOFI-AVENTISInventor: Jean-Francois Sabuco
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Publication number: 20110003787Abstract: The present invention relates to a compound or a pharmacologically acceptable salt thereof having superior glucokinase activating activity, and is a compound represented by general formula (I), or pharmacologically acceptable salt thereof: [wherein, A represents, for example, an oxygen atom or sulfur atom, R1 represents, for example, a C1-C6 alkyl group, a C1-C6 alkoxy group or a C1-C6 halogenated alkyl group, A and R1 together with the carbon atom bonded thereto form a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R2 represents a phenyl group that may be substituted with 1 to 5 group(s) independently selected from Substituent Group ? or a heterocyclic group that may be substituted with 1 to 3 group(s) independently selected from Substituent Group ?, R3 represents a hydroxy group or a C1-C6 alkoxy group, and Substituent Group ? consists of, for example, a halogen atom, a C1-C6 alkyl group, a C1-C6 alkyl group substituted with 1 or 2 hydType: ApplicationFiled: July 26, 2010Publication date: January 6, 2011Inventors: Akihiro Furukawa, Takehiro Fukuzaki, Yukari Onishi, Hideki Kobayashi, Takeshi Honda, Yumi Matsui, Masahiro Konishi, Kenjiro Ueda, Tetsuyoshi Matsufuji
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Publication number: 20100331294Abstract: Compounds of the formula wherein R1 and R2 are as disclosed herein, are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor full or partial agonists. Also disclosed are pharmaceutical compositions, methods for using such compounds and compositions, and processes for preparing the compounds.Type: ApplicationFiled: June 30, 2010Publication date: December 30, 2010Applicant: ABBOTT LABORATORIESInventors: Lawrence A. Black, Gregory A. Gfesser, Marlon D. Cowart
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Publication number: 20100331304Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: October 30, 2008Publication date: December 30, 2010Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Doris Riether, Renee M. Zindell, Nigel James Blumire
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Publication number: 20100324009Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 23, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100317644Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.Type: ApplicationFiled: August 24, 2010Publication date: December 16, 2010Applicant: Gruenenthal GmbHInventors: Stefan OBERBOERSCH, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
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Publication number: 20100317641Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: October 30, 2009Publication date: December 16, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
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Publication number: 20100317647Abstract: The invention relates to a compound of formula (I) wherein A1 and R1 to R5 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: June 2, 2010Publication date: December 16, 2010Inventors: David Banner, Simona M. Ceccarelli, Uwe Grether, Wolfgang Haap, Hans Hilpert, Holger Kuehne, Harald Mauser, Jean-Marc Plancher, Rubén Alvarez Sánchez
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Patent number: 7851463Abstract: The invention relates to compounds of the formula (I). The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: GrantFiled: October 14, 2005Date of Patent: December 14, 2010Assignee: Abbott GmbH & Co. KGInventors: Karla Drescher, Andreas Haupt, Liliane Unger, Sean C. Turner, Wilfried Braje, Roland Grandel, Christophe Henry, Gisela Backfisch, Armin Beyerbach, Wilfried Lubisch
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Publication number: 20100310675Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: June 8, 2010Publication date: December 9, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Hayley Binch, Michael Mortimore, Chris Davis, Dean Boyall, Simon Everitt, Daniel Robinson, Sharn Ramaya, Damien Fraysse, John Studley, Andrew Miller, Michael O'Donnell, Alistair Rutherford, Joanne Pinder
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Publication number: 20100305088Abstract: This invention is directed to a 3-(amido or sulphamido)-4-(4-substituted-azinyl)benzamide or benzsulphonamide compound as defined herein. The 3-(amido or sulphamido)-(4-substituted-azinyl)benzamide or benzsulphonamide compound is useful as a inhibitor of the chemokine receptor CxCR3, and for preventing or treating a CxCR3 chemokine receptor mediated disease or condition related thereto in a patient in need of such.Type: ApplicationFiled: August 6, 2010Publication date: December 2, 2010Applicant: SANOFI-AVENTISInventors: David S. Thorpe, Martin Smrcina, Dagmar D. Cabel
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Publication number: 20100305085Abstract: The invention relates to dihydropyrazolon-derivatives of formula (I), to methods for their production, to their use for treating and/or for preventing diseases and their use for producing medicaments for treating and/or for preventing diseases, in particular cardiovascular and haematological diseases, kidney diseases and for promoting the healing of wounds.Type: ApplicationFiled: October 12, 2007Publication date: December 2, 2010Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Kai Thede, Ingo Flamme, Felix Oehme, Jens-Kerim Ergüden, Friederike Stoll, Joachim Schuhmacher, Hanno Wild, Peter Kolkhof, Hartmut Beck, Jörg Keldenich, Metin Akbaba, Mario Jeske
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Publication number: 20100305092Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, X have the meanings given in claim 16. The compounds are useful e.g. in the treatment of autoimmune disorders, such as multiple sclerosis.Type: ApplicationFiled: December 17, 2008Publication date: December 2, 2010Applicant: MERCK SERONO SAInventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin
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Publication number: 20100305086Abstract: This invention discloses a method of treatment of osteoarthritis pain by administration of a composition containing a nicotinic acetylcholine receptor ligand and a nicotinic acetylcholine receptor subtype ?4?2 allosteric modulator. The present application also relates to compositions comprising such compounds for use in treating pain and related disorders mediated by controlling neurotransmitter release in a subject.Type: ApplicationFiled: May 26, 2010Publication date: December 2, 2010Applicant: ABBOTT LABORATORIESInventors: Murali Gopalakrishnan, Chih-Hung Lee, Jianguo Ji, Tao Li, Kevin B. Sippy