Oxadiazoles (including Hydrogenated) Patents (Class 546/269.1)
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Publication number: 20110312930Abstract: The present application relates to novel aryl compounds with aminoalkyl substituents, to processes for their preparation, to their use for treatment and/or prevention of diseases and to their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 22, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch
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Publication number: 20110311593Abstract: The invention relates to N-hydroxylated amidines, guanidines and aminohydrazones for application on the skin. In particular, the invention relates to transdermal therapeutic systems containing N-hydroxylated amidines, guanidines and aminohydrazones as a prodrug, and to methods for producing and using such systems.Type: ApplicationFiled: February 5, 2010Publication date: December 22, 2011Inventors: Rudolf Matusch, Hans-Rainer Hoffmann, Bodo Asmussen, Andreas Koch
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Publication number: 20110301122Abstract: The present application relates to novel substituted aryl compounds, processes for their preparation, their use for treatment and/or prevention of diseases and their use for the preparation of medicaments for treatment and/or prevention of diseases, in particular for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be carried out as monotherapy or also in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: October 31, 2009Publication date: December 8, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Michael Härter, Hartmut Beck, Peter Ellinghaus, Kerstin Berhörster, Susanne Greschat, Karl-Heinz Thierauch, Frank Süssmeier
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Publication number: 20110301161Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salt thereof, wherein R1-R7 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: December 1, 2010Publication date: December 8, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Zhidong CHEN, Ming-Hong HAO, Weimin LIU, Ho-Yin LO, Pui Leng LOKE, Chuk Chui MAN, Tina Marie MORWICK, Peter Allen NEMOTO, Hidenori TAKAHASHI, Heather TYE, Lifen WU
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Publication number: 20110294829Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: December 8, 2009Publication date: December 1, 2011Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20110275631Abstract: Disclosed are compounds and compositions of the formula I as described herein which are inhibitors of MMP-13. Also disclosed are methods of using and making compounds of the formula I.Type: ApplicationFiled: October 13, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Bennett Farmer, II, Neil Alexander Farrow, Donghong Amy Gao, Alexander Heim-Riether, Lana Louise Smith Keenan, Ingo Andreas Mugge, Steven John Taylor, Zhaoming Xiong, Yang Yu, Qiang Zhang
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Publication number: 20110275610Abstract: Disclosed are compounds of Formula (I) or a pharmaceutically acceptable salt thereof, wherein: n is zero or an integer selected from 1 through 4; R1 is cycloalkyl, aryl, heteroaryl, or heterocyclyl, each optionally substituted with one to five substituents independently selected from C1 to C6 alkyl, C1 to C4 haloalkyl, benzyl, —OR4, and/or halogen; and R2, R3, R4, and n are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and vascular disease.Type: ApplicationFiled: January 22, 2010Publication date: November 10, 2011Inventors: Alaric J. Dyckman, William J. Pitts, Scott Hunter Watterson
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Publication number: 20110269769Abstract: The present invention is directed to certain imidazole derivatives which are useful as inhibitors of Fatty Acid Amide Hydrolase (FAAH). The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzeimer Disease, and Parkinson's Disease.Type: ApplicationFiled: June 4, 2009Publication date: November 3, 2011Inventors: Linus S. Lin, Marc D. Chioda, Ping Liu, Ravi P. Nargund
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Patent number: 8034953Abstract: The present invention is directed to modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.Type: GrantFiled: May 9, 2006Date of Patent: October 11, 2011Assignee: Incyte CorporationInventors: Andrew P. Combs, Eddy W. Yue
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Publication number: 20110245227Abstract: Novel compounds are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. These novel compounds have the structure Formula I or Formula IA.Type: ApplicationFiled: June 14, 2011Publication date: October 6, 2011Inventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Patent number: 8030309Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: GrantFiled: September 27, 2010Date of Patent: October 4, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Youla S. Tsantrizos, Catherine Chabot, Pierre Beaulieu, Christian Brochu, Martin Poirier, Timothy A. Stammers, Bounkham Thavonekham, Jean Rancourt
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Publication number: 20110237576Abstract: The present invention provides a compound which has an effect of inhibiting amyloid-? production and is useful as a therapeutic agent for diseases induced by production, secretion and/or deposition of amyloid-? proteins. The present invention relates to a compound represented by formula (I) or a pharmaceutically acceptable salt or solvate thereof: wherein A is optionally substituted carbocyclic diyl or optionally substituted heterocyclic diyl; B is an optionally substituted carbocyclic group or an optionally substituted heterocyclic group; R1 is a group such as optionally substituted lower alkyl; R2 is a group such as hydrogen; and R3a and R3b are each independently a group such as hydrogen, provided that the following compound is excluded.Type: ApplicationFiled: October 22, 2009Publication date: September 29, 2011Applicant: SHIONOGI & CO., LTD.Inventors: Shuji Yonezawa, Yuusuke Tamura, Yuuji Kooriyama, Gaku Sakaguchi
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Publication number: 20110230498Abstract: This invention provides compounds of Formula (I) which are PAFR antagonists: Formula (I) and the pharmaceutically acceptable salts thereof. The compounds are useful for treating PAF-mediated disorders, and can be used in methods for treating atherosclerosis and preventing or reducing risk for atherosclerotic disease events. The compounds are also useful for treating or ameliorating pain, e.g. inflammatory pain and/or nociceptive pain, and for treating or ameliorating autoimmune and/or inflammatory diseases, among other conditions.Type: ApplicationFiled: December 8, 2009Publication date: September 22, 2011Inventors: Anthony Ogawa, Hyun O. Ok, Debra Ondeyka, Feroze Ujjainwalla, Ellen Vande Bunte
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Publication number: 20110224259Abstract: The invention relates to novel heterocyclic derivatives as inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5). QC catalyzes the intramolecular cyclization of N-terminal glutamine residues into pyroglutamic acid (5-oxo-prolyl, pGlu*) under liberation of ammonia and the intramolecular cyclization of N-terminal glutamate residues into pyroglutamic acid under liberation of water.Type: ApplicationFiled: March 3, 2011Publication date: September 15, 2011Applicant: PROBIODRUG AGInventors: Ulrich HEISER, Daniel RAMSBECK, Torsten HOFFMANN, Livia BOEHME, Hans-Ulrich DEMUTH
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Patent number: 8017631Abstract: This invention relates to novel oxadiazole derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: GrantFiled: April 24, 2006Date of Patent: September 13, 2011Assignee: Neurosearch A/SInventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jørgensen
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Publication number: 20110212945Abstract: The present disclosure relates to new azabiphenylaminobenzoic acid derivatives of formula (I); as well as processes for their preparation, pharmaceutical compositions comprising them, and their use in therapy as inhibitors of the dehydroorotate dihydrogenase (DHODH).Type: ApplicationFiled: August 8, 2008Publication date: September 1, 2011Applicant: ALMIRALL, S.A.Inventors: Julio Cesar Castro Palomino Laria, Emma Terricabras Belart, Montserrat Erra Sola, Eloisa Navarro Romero, Silvia Fonquerna Pou, Aranzazu Cardus Figueras, Maria Estrella Lozoya Toribio
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Publication number: 20110207738Abstract: The invention relates to annelated pyrrolidin sulfonamides with oxadiazolone headgroup and to their physiologically acceptable salts and physiologically functional derivatives showing PPARdelta or PPARdelta and PPARalpha agonist activity. What is described are compounds of the formula (I), in which the radicals are as defined, and their physiologically acceptable salts and processes for their preparations. The compounds are suitable for the treatment and/or prevention of disorders of fatty acid metabolism and glucose utilization disorders as well as of disorders in which insulin resistance is involved and demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: ApplicationFiled: May 22, 2009Publication date: August 25, 2011Applicant: SANOFI-AVENTISInventors: Stefanie Keil, Matthias Urmann, Wolfgang Wendler, Maike Glien, Hans Matter, Eugen Falk
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Publication number: 20110206783Abstract: The subject invention relates to novel P2X3 receptor antagonists that play a critical role in treating disease states associated with pain, in particular peripheral pain, inflammatory pain, or tissue injury pain that can be treated using a P2X3 receptor subunit modulator.Type: ApplicationFiled: October 21, 2009Publication date: August 25, 2011Inventors: Christopher S. Burgey, Zhengwu J. Deng, Diem N. Nguyen, Daniel V. Paone, Anthony W. Shaw
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Publication number: 20110196150Abstract: Provided are 4?-arylmethoxy isoindoline compounds, and pharmaceutically acceptable salts, solvates, clathrates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.Type: ApplicationFiled: February 10, 2011Publication date: August 11, 2011Inventors: Hon-Wah Man, George W. Muller, Alexander L. Ruchelman, Ehab M. Khalil, Roger Shen-Chu Chen, Weihong Zhang
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Publication number: 20110190346Abstract: The instant invention provides compounds of formula I which are 5-lipoxygenase activating protein inhibitors. Compounds of formula I are useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: February 7, 2011Publication date: August 4, 2011Applicant: Merck Sharp & Dohme Corp.Inventors: Lin Chu, Ihor E. Kopka, Bing Li, Anthony K. Ogawa, Feroze Ujjainwalla
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Patent number: 7968552Abstract: A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided. It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.Type: GrantFiled: April 23, 2007Date of Patent: June 28, 2011Assignee: Astellas Pharma Inc.Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Yasuhiro Yonetoku, Norio Asai, Shigeru Yoshida, Takatoshi Soga
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Publication number: 20110118282Abstract: A compound having the structure useful for treatment or prevention of cardiovascular diseases, endothelial dysfunction, diastolic dysfunction, atherosclerosis, hypertension, angina pectoris, thromboses, restenoses, myocardial infarction, strokes, cardiac insufficiency, pulmonary hypertonia, erectile dysfunction, asthma bronchiale, chronic kidney insufficiency, diabetes, or cirrhosis of the liver in a human or animal patient.Type: ApplicationFiled: September 2, 2008Publication date: May 19, 2011Inventors: Amy R. Bittner, Christopher Joseph Sinz, Jiang Chang, Ronald M. Kim, J.W. Mirc, Emma R. Parmee, Qiang Tan
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Publication number: 20110118290Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to use thereof for controlling animal pests, in particular arthropods and especially insects.Type: ApplicationFiled: October 12, 2010Publication date: May 19, 2011Applicant: Bayer CropScience AGInventors: Thomas BRETSCHNEIDER, Arnd VOERSTE, Martin FÜßLEIN, Adeline KÖHLER, Ulrich GÖRGENS
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Publication number: 20110105530Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Publication number: 20110098273Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.Type: ApplicationFiled: September 3, 2008Publication date: April 28, 2011Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
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Publication number: 20110098287Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to use thereof for controlling animal pests, in particular arthropods and especially insects.Type: ApplicationFiled: June 4, 2009Publication date: April 28, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Fusslein, Achim Hense, Joachim Kluth
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Publication number: 20110092547Abstract: Compounds of formula (I), or pharmaceutically-acceptable salts and/or pro-drugs thereof, which inhibit acetyl CoA(acetyl coenzyme A):diacylglycerol acyltransferase (DGAT1) activity are provided, wherein n is 0 to 3; p is 0 or 1; q is 0 to 2; R1 and R2 are, for example, independently fluoro, chloro, bromo, cyano or (1-4C)alkyl; X is —O—, —S— or —NRa— wherein Ra is hydrogen or (1-4C)alkyl; RA1 and RA2 are, for example, independently hydrogen or (1-4C)alkyl; Ring A is a di-linked ring or ring system chosen from (4-6C)cycloalkane, (7-10C)bicycloalkane and (8-12C)tricycloalkane each optionally substituted, for example, by one substituent selected from (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; or Ring A is phenylene optionally substituted, for example, by up to four substituents selected from fluoro, chloro, bromo, cyano, (1-4C)alkyl, (1-4C)alkoxy and (1-4C)alkoxy(1-4C)alkyl; together with processes for their preparation, pharmaceutical compositions containing them and their use as medicamentsType: ApplicationFiled: August 15, 2008Publication date: April 21, 2011Inventors: Alan Martin Birch, Roger John Butlin, Adrian Liam Gill, Samuel David Groombridge, Alleyn Thomas Plowright, Michael James Waring
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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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Patent number: 7915263Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1? is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: August 29, 2007Date of Patent: March 29, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Kato, Nobuhiko Kawanishi, Kouta Masutani, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20110028509Abstract: The invention relates to compounds of formula I wherein R1, R2, R4, Ra, Rb, Rc, Re, A*, W1, W2 and W3 are as defined in claim 16, for the treatment of CXCR3 related diseases.Type: ApplicationFiled: April 8, 2009Publication date: February 3, 2011Applicant: MERCK SERONO SAInventors: Stefano Crosignani, Christophe Cleva, Christos Tsaklakidis, Lars Burgdorf
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Publication number: 20110028463Abstract: [Problems] To provide a compound that is useful as an agent for treating chronic renal insufficiency or an agent for treating diabetic nephropathy. [Means for Solving Problems] The present inventors have conducted extensive studies on a compound having an EP4 receptor antagonistic action, and as a result, they have found that various amide derivatives having a carboxylic group or an equivalent thereof exhibit an excellent EP4 receptor antagonistic action, thereby completing the present invention. Since the compound of the present invention has an excellent EP4 receptor antagonistic action, it is useful as an agent for preventing and/or treating chronic renal insufficiency or diabetic nephropathy.Type: ApplicationFiled: July 2, 2008Publication date: February 3, 2011Applicant: Astellas Pharma Inc.Inventors: Eisuke Nozawa, Ryotaro Ibuka, Kazuhiro Ikegai, Keisuke Matsuura, Tatsuya Zenkoh, Ryushi Seo
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Publication number: 20110015203Abstract: An enantiomer, diastereoisomer or tautomer of a compound, represented by formula I: wherein A, B, R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are as defined herein, or a salt or ester thereof, as an inhibitor of HCV NS5B polymerase.Type: ApplicationFiled: September 27, 2010Publication date: January 20, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Youla S. TSANTRIZOS, Catherine CHABOT, Pierre BEAULIEU, Christian BROCHU, Martin POIRIER, Timothy A. STAMMERS, Bounkham THAVONEKHAM, Jean RANCOURT
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Publication number: 20110009421Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaki Setoh, Toshitake Kobayashi, Toshio Tanaka, Atsuo Baba
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Publication number: 20110003815Abstract: The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: October 6, 2008Publication date: January 6, 2011Inventors: Anthony Ogawa, Feroze Ujjainwalla, Bing Li, Lin Chu, Minal Patel, Helen M. Armstrong, Hyun O. Ok, Rosemary Sisco, Dwight MacDonald, John Hutchinson, Helene Perrier
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Publication number: 20110003806Abstract: This invention provides compounds of formula IA or IB: wherein R1, R2, G1 and HY are as described in the specification. The compounds are inhibitors of PI3K and/or mTor and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: January 28, 2010Publication date: January 6, 2011Applicants: Millennium Pharmaceuticals, Inc., Takeda Pharmaceutical Company LimitedInventors: Masaaki Hirose, Steven P. Langston, Hirotake Mizutani, Stepan Vyskocil
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Patent number: 7858649Abstract: This invention relates to novel imidazole derivatives, pharmaceutical compositions containing these compounds, and methods of treatment therewith. The compounds of the invention are of the general formula (I) and include any of its stereoisomers, any mixture of its stereoisomers, and pharmaceutically acceptable salts thereof. The compounds of the invention are useful in the treatment of central nervous system diseases and disorders, which are responsive to modulation of the GABAA receptor complex, and in particular for combating anxiety and related diseases.Type: GrantFiled: October 12, 2006Date of Patent: December 28, 2010Assignee: Neurosearch A/SInventors: William Dalby Brown, Janus S. Larsen, Lene Teuber, David Tristram Brown, Philip K. Ahring, Naheed Mirza, Elsebet Østergaard Nielsen
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Publication number: 20100305104Abstract: The invention relates to compounds of formula (I): wherein R1, R2, Ra, Rb, Rc and W, 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: October 1, 2008Publication date: December 2, 2010Inventors: Cyril Montagne, Anna Quattropani, Wolfgang Sauer, Agnes Bombrun
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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: 20100298384Abstract: The present invention relates to novel oxazolidinone compounds of formula (I) with antibacterial activity, their pharmaceutically acceptable salts, their stereoisomers, their prodrugs, pharmaceutical compositions comprising the same and to their use as therapeutic agentsType: ApplicationFiled: December 4, 2007Publication date: November 25, 2010Inventors: Mohamed Takhi, Jagattaran Das, Javed Iqbal, Natesan Selvakumar, Sreenivas Kandepu, M. Sitaram Kumar
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Publication number: 20100286110Abstract: 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 10, 2008Publication date: November 11, 2010Inventors: Matthew Colin Thor Fyfe, William Gattrell, Colin Peter Sambrook-Smith
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Publication number: 20100273805Abstract: The present invention is directed to novel compounds, to a process for their preparation, their use in therapy and pharmaceutical compositions comprising the novel compounds.Type: ApplicationFiled: April 21, 2010Publication date: October 28, 2010Applicant: AstraZeneca ABInventors: Kenneth Granberg, Bjorn Holm
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Publication number: 20100267775Abstract: A pharmaceutical agent having GPR40 receptor agonistic action, particularly a compound which is useful as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus. The present inventors have examined a compound having GPR40 receptor agonistic action, confirmed that an oxadiazolidinedione compound which has a substituent such as a benzyl group, etc. linked with a substituent such as a phenyl group, etc. through a linker at the 2-position of an oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof has an excellent GPR40 agonistic activity, and thus completed the invention. The oxadiazolidinedione compound has excellent insulin secretagogue action and anti-hyperglycemic action, and therefore can be used as an insulin secretagogue or an agent for preventing and/or treating diabetes mellitus.Type: ApplicationFiled: October 22, 2008Publication date: October 21, 2010Inventors: Kenji Negoro, Fumiyoshi Iwasaki, Kei Ohnuki, Toshio Kurosaki, Kazuyuki Tsuchiya, Kazuyuki Kuramoto, Shigeru Yoshida, Takatoshi Soga
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Patent number: 7816380Abstract: ?-Hydroxycycloalkanecarboxamide derivatives of formula (I) or a pharmaceutically acceptable salt thereof, wherein formula (a) is a single or double bond; R1, R2 and R3 are each independently selected from H, halogen and OH; or R1 and R2 attached to the same carbon atom together represent oxo; R4 is H or methyl; R5 is Cl or I2; R6 is selected from —CO2—C1-4alkyl, —O—C1-4alkyl, —O—C1-4haloalkyl, 2-methyltetrazol-5-yl, 5-methyl-1,2,4-oxadiazol-3-yl, 3-methyl-1,2,4-oxadiazol-5-yl, 5-halomethyl-1,2,4-oxadiazol-3-yl, 3-halomethyl-1,2,4-oxadiazol-5-yl, tetrazol-5-yl, 5-halomethyl-1,2,3-triazolyl, and 5-methyl-1,2,3-triazolyl; R7 and R8 are each independently Cl or I2; and n is 0 or 1, are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway.Type: GrantFiled: May 30, 2006Date of Patent: October 19, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Scott D. Kuduk, Michael R. Wood
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Publication number: 20100261673Abstract: Embodiments of the present invention provide novel antibacterials that target penicillin-binding proteins or other important cellular targets. Methods for inhibiting growth (reproduction, etc.) of bacteria using compounds described herein are also provided. Various embodiments exhibit activity against gram positive bacteria, such as certain strains of Entercoccus and Staphylococcus aureus.Type: ApplicationFiled: December 21, 2007Publication date: October 14, 2010Applicant: UNIVERSITY OF NOTRE DAME DU LACInventors: Shahriar Mobashery, Peter I. O'Daniel, Mayland Chang
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Publication number: 20100249139Abstract: The present invention relates to compounds of formula I wherein R1a to R1e and R2 to R5 are as defined in the description and claims, and pharmaceutically acceptable salts thereof. The compounds are glucocorticoid receptor antagonists useful for the treatment and/or prevention of diseases such as diabetes, dyslipidemia, obesity, hypertension, cardiovascular diseases, adrenal imbalance or depression.Type: ApplicationFiled: March 19, 2010Publication date: September 30, 2010Inventors: Daniel Hunziker, Christian Lerner, Werner Mueller, Ulrike Obst Sander, Philippe Pflieger, Pius Waldmeier
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Publication number: 20100240658Abstract: The invention relates to compounds of formula I: wherein R1, R2, Ra, Rb, W, Q and S 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: October 1, 2008Publication date: September 23, 2010Applicant: MERCK SERONO SAInventors: Anna Quattropani, Cyril Montagne, Wolfgang Sauer, Stefano Crosignani, Agnes Bombrun, Mathilde Muzerelle, Jerome Dorbais, Delphine Marin, Jerome Gonzalez, Patrick Gerber
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Publication number: 20100240708Abstract: Disclosed are compounds, pharmaceutical compositions containing the compounds, methods for using the compounds and processes for making the compounds. More specifically, the disclosure relates to alpha-(N-benzenesulfonamido)cycloalkyl compounds that may inhibit one or both of: (i) the functioning of a ?-secretase enzyme; or (ii) the production of ?-amyloid. Such compounds may be beneficial in the treatment of Alzheimer's disease and other conditions. Representative compounds have the following formula I: wherein: A, R1, and R2 are described herein.Type: ApplicationFiled: March 17, 2010Publication date: September 23, 2010Inventors: Dalton King, Zhaoxing Meng, Ivar M. McDonald, Richard E. Olson, John E. Macor
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Patent number: 7790754Abstract: ?-Hydroxy amide derivatives of the general formula (I) are bradykinin B1 antagonists or inverse agonists useful in the treatment or prevention of symptoms such as pain and inflammation associated with the bradykinin B1 pathway. R2a is selected from (1) a group selected from Ra. (2) (CH2)nNRbC(O)Ra. (3) (CH2)nNRbSO2Rd. (4) (CH2)nNRbCO2Ra. (5) (CH2)k-heterocycle optionally substituted with 1 to 3 groups independently selected from halogen.nitro, cyano.ORa.SRa.C1-4 alkyl and C1-3 haloakyl wherein said heterocycle is (a) a 5-membered heteroaromatic ring having a ring heteroatom selected from N.O and S. and optionally having up to 3 additional ring nitrogen atoms wherein said ring is optionally benzo-fused; or (b) a 6-membered heteromatic ring containing from 1 to 3 ring nitrogen atoms and N-oxydes thereof. Wherein said ring is optionally benzo-fused. (6) (CH2)kCO2Ra. and (7) (CH2)C(O)NRbRc.Type: GrantFiled: December 17, 2004Date of Patent: September 7, 2010Assignee: Merck Sharp & Dohme Corp.Inventors: Michael R. Wood, Neville J. Anthony, Mark G. Bock, Scott D. Kuduk
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Publication number: 20100210603Abstract: The present invention relates to a novel class of sulfonamides which are aspartyl protease inhibitors. In one embodiment, this invention relates to a novel class of HIV aspartyl protease inhibitors characterized by specific structural and physicochemical features. This invention also relates to pharmaceutical compositions comprising these compounds. The compounds and pharmaceutical compositions of this invention are particularly well suited for inhibiting HIV-1 and HIV-2 protease activity and consequently, may be advantageously used as anti-viral agents against the HIV-1 and HIV-2 viruses. This invention also relates to methods for inhibiting the activity of HIV aspartyl protease using the compounds of this invention and methods for screening compounds for anti-HIV activity.Type: ApplicationFiled: September 11, 2009Publication date: August 19, 2010Inventors: Roger D. Tung, Mark A. Murcko, Govinda R. Bhisetti