Carbocyclic Ring Containing Patents (Class 546/194)
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Patent number: 8268894Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis.Type: GrantFiled: November 11, 2010Date of Patent: September 18, 2012Assignees: The United States of America as Represented by the Secretary, Department of Health and Human Services, Sequella, Inc.Inventors: Marina Nikolaevna Protopopova, Elena Bogatcheva, Leo Einck, Richard Edward Lee, Richard Allan Slayden, Clifton E. Barry, III
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Publication number: 20120232049Abstract: A pyridine or pyrimidine derivative represented by the formula (I) has an excellent HGFR inhibitory activity and exhibits strong cell proliferation inhibitory effect and anti-tumor effect against cancer cell lines with amplified HGFR gene. wherein R1 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; R2 and R3 represent hydrogen; R4, R5, R6, and R7 may be the same or different and each represents hydrogen, halogen, C1-6 alkyl or the like; R8 represents hydrogen or the like; R9 represents a 3- to 10-membered non-aromatic heterocyclic group or the like; n represents an integer of 1 or 2; X represents —CH?, nitrogen.Type: ApplicationFiled: February 22, 2008Publication date: September 13, 2012Applicant: Eisai R&D Management Co., Ltd.Inventors: Hiroshi Obaishi, Takayuki Nakagawa, Tomohiro Matsushima, Setsuo Funasaka, Shuji Shirotori, Keiko Takahashi
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Publication number: 20120232109Abstract: [Problem] There is provided a compound useful as a preventive or remedy for cardiovascular disease, neurologic disease, metabolic disease, reproductive disease, and digestive disease. [Means for Resolution] A compound or a pharmaceutically acceptable salt thereof represented by the following Formula (I) wherein Z represents wherein n1, n2, and n3 are 0, 1, or 2, respectively; R1 represents C1-6 alkyl, C3-8 cycloalkyl, or the like; R2 represents aryl or heteroaryl; R3 represents a hydrogen atom, C1-6 alkyl, or the like; and M1, M2, M3, and M4 independently represent a hydrogen atom, C1-6 alkyl, or the like, or M1, together with M2, M3, or M4, forms —CH2— or the like.Type: ApplicationFiled: May 23, 2012Publication date: September 13, 2012Inventors: Tsuyoshi Nagase, Takahide Sasaki, Toshiyuki Takahashi
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Publication number: 20120232052Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
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Publication number: 20120225861Abstract: Benzoxazole and benzothiazole compounds and the stereoisomers, tautomers, solvates, oxides, esters, and prodrugs thereof and pharmaceutically acceptable salts thereof are disclosed. Compositions of the compounds, either alone or in combination with at least one additional therapeutic agent, with a pharmaceutically acceptable carrier, and uses of the compounds, either alone or in combination with at least one additional therapeutic agent are also disclosed. The embodiments are useful for inhibiting cellular proliferation, inhibiting the growth and/or metathesis of tumors, treating or preventing cancer, treating or preventing degenerating bone diseases such as rheumatoid arthritis, and/or inhibiting molecules such as CSF-1R.Type: ApplicationFiled: April 23, 2012Publication date: September 6, 2012Inventors: James C. Sutton, Marion Wiesmann, Weibo Wang, Mika Lindvall, Jiong Lan, Savithri Ramurthy, Anu Sharma, Elizabeth J. Mieuli, Liana M Klivansky, William Lenahan, Susan Kaufman, Hong Yang, Simon C. Ng, Keith Pfister, Allan S. Wagman, Victoria Sung, Martin Sendzik
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Publication number: 20120225868Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceuticals.Type: ApplicationFiled: February 27, 2012Publication date: September 6, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120226033Abstract: The present invention relates to novel benzene-carboxamide compounds having a structure that corresponds to the general formula (I) below: and also to their method of synthesis and to their use in pharmaceutical compositions intended for use in human or veterinary medicine or else to their use in cosmetic compositions.Type: ApplicationFiled: September 16, 2010Publication date: September 6, 2012Applicant: GALDERMA RESEARCH & DEVELOPMENTInventors: Laurence Clary, Jean-Claude Pascal
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Publication number: 20120225062Abstract: The present invention provides compounds of Formula I: and related compounds as further described herein, and pharmaceutical compositions comprising these compounds. The invention further provides methods to use these compounds and compositions for treating disorders associated with undesired levels of Pim kinase activity, including cancers and autoimmune disorders.Type: ApplicationFiled: March 2, 2012Publication date: September 6, 2012Inventors: Matthew Burger, Gisele Nishiguchi, Timothy D. Machajewski, Alice Rico, Robert Lowell Simmons, Aaron R. Smith, Victoriano Tamez, JR., Huw Tanner, Lifeng Wan
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Patent number: 8258304Abstract: N-aryl piperidine substituted biphenylcarboxamides compounds of formula (I) methods for preparing such compounds, pharmaceutical compositions comprising said compounds as well as the use of said compounds as a medicine for the treatment of hyperlipidemia, obesity and type II diabetes.Type: GrantFiled: January 9, 2009Date of Patent: September 4, 2012Assignee: Janssen Pharmaceutica N.V.Inventors: Lieven Meerpoel, Leo Jacobus Jozef Backx, Peter Walter Maria Roevens
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Publication number: 20120220561Abstract: The present invention relates to compound of formula (I): or pharmaceutically acceptable salts thereof, wherein R1-R5 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: August 12, 2011Publication date: August 30, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra BARTOLOZZI, Todd BOSANAC, Zhidong CHEN, Stephane DE LOMBAERT, John D. HUBER, Ho Yin LO, Pui Leng LOKE, Weimin LIU, Tina Marie MORWICK, Alan OLAGUE, Doris RIETHER, Heather TYE, Lifen WU, Renee M. ZINDELL
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Publication number: 20120220564Abstract: Methods and compounds effective in ameliorating conditions characterized by unwanted calcium channel activity, particularly unwanted T-type calcium channel activity are disclosed using a series of compounds containing N-acylated cyclic amines linked to an a?l ring as shown in formula (I).Type: ApplicationFiled: September 17, 2010Publication date: August 30, 2012Applicant: Zalicus Pharmaceuticals Ltd.Inventors: Hassan Pajouhesh, Yongbao Zhu, Yuanxi Zhou, Michael E. Grimwood, Eric Simonson
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Patent number: 8252793Abstract: The invention provides compositions and methods for treating and/or preventing ocular disorders associated with increased intraocular pressure. In particular, the compounds are bradykinin agonists.Type: GrantFiled: August 17, 2011Date of Patent: August 28, 2012Assignees: Alcon Research, Ltd., Astellas Pharma Inc.Inventors: Keith D. Combrink, Suchismita Mohapatra, Mark R. Hellberg, Najam A. Sharif, Ganesh Prasanna, Iok-Hou Pang, Bryon Severns, Hwang-Hsing Chen, Abdelmoula Namil
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Publication number: 20120214809Abstract: The present application provides novel aminoindane compounds and methods for preparing and using these compounds. These compounds are useful in treating pain and/or itch in patients by administering one or more of the compounds to a patient. The methods include administering a compound of formula (I) or (II) and a TRPV 1 receptor activator. In one embodiment, the TRPV 1 receptor activator is lidocaine.Type: ApplicationFiled: February 18, 2012Publication date: August 23, 2012Inventors: Scott Kevin Thompson, Tony Priestley, Roger Astbury Smith, Ashis K. Saha, Sonali Rudra, Arun Kuma Hajra, Dipanwita Chatterjee, Carl Henry Behrens, Yigang He, Hui-Yin Li
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Publication number: 20120214783Abstract: 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: May 3, 2012Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Pierre L. BEAULIEU, Pasquale FORGIONE, Alexandre GAGNON, Cedrickx GODBOUT, Marc-Andre JOLY, Montse LLINAS-BRUNET, Julie NAUD, Martin POIRIER, Jean RANCOURT
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Publication number: 20120214823Abstract: Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1.Type: ApplicationFiled: September 20, 2010Publication date: August 23, 2012Inventors: Hugh Y. Zhu, Jagdish A. Desai, Alan B. Cooper, Ronald J. Doll
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Publication number: 20120213758Abstract: The present invention relates to a genus of biaryl compounds containing at least one further ring. The compounds are PDE4 inhibitors useful for the treatment and prevention of stroke, myocardial infarct and cardiovascular inflammatory diseases and disorders.Type: ApplicationFiled: April 27, 2012Publication date: August 23, 2012Applicant: DeCODE Genetics enfInventors: Jasbir SINGH, Mark E. GURNEY, Alex BURGIN, Alexander KISELYOV, Munagala RAO, Timothy HAGEN
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Publication number: 20120214991Abstract: An indenone derivative of formula (1) is effective in enhancing the activity of osteoblastic cells and inhibiting bone resorption by osteoclastic cells, and a pharmaceutical composition comprising the indenone derivative or a pharmaceutically acceptable salt thereof is useful for preventing or treating bone diseases such as osteoporosis.Type: ApplicationFiled: October 21, 2009Publication date: August 23, 2012Applicant: Korea Research Institute of Chemical TechnologyInventors: Jung Nyoung Heo, Myung Ae Bae, Nack Jeong Kim, Sung Youn Chang, Nam Sook Kang, Sung Eun Yoo, Eun Sook Hwang
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Publication number: 20120208815Abstract: New compounds, compositions and methods of inhibition of kinase activity associated with tumorigenesis in a human or animal subject are provided. In certain embodiments, the compounds and compositions are effective to inhibit the activity of at least one serine/threonine kinase or receptor tyrosine kinase. The new compounds and compositions may be used either alone or in combination with at least one additional agent for the treatment of a serine/threonine kinase- or receptor tyrosine kinase-mediated disorder, such as cancer.Type: ApplicationFiled: March 3, 2008Publication date: August 16, 2012Inventors: Matthew Burger, Mika Lindvall, Wooseok Han, Jiong Lan, Gisele Nishiguchi, Cynthia Shafer, Comelia Bellamacina, Kay Huh, Gordana Atallah, Christopher Mcbride, William Antonios-Mccrea, JR., Tatiana Zavorotinskaya, Annette Walter, Pablo Garcia
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Patent number: 8242278Abstract: A process for producing a biaryl compound, characterized by reacting an arylhydrazine compound, hydrogen peroxide and an aryl compound. When the reaction is conducted in the presence of a given metal or a compound of the metal or in the presence of a metal oxide obtained by reacting the given metal or a compound of the metal with hydrogen peroxide, then the yield of the biaryl compound is improved.Type: GrantFiled: May 1, 2009Date of Patent: August 14, 2012Assignee: Sumitomo Chemical Company, LimitedInventor: Koji Hagiya
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Publication number: 20120202775Abstract: Compounds having drug and bio-affecting properties are described herein, including their properties, pharmaceutical compositions and methods of use. In particular, tricyclic aryl or heteroaryl piperazine diamide derivatives that possess unique antiviral activity are set forth. These compounds are useful for the treatment of HIV and AIDS.Type: ApplicationFiled: August 4, 2011Publication date: August 9, 2012Inventors: Tao Wang, Zhongxing Zhang, Zhiwei Yin, John F. Kadow, Nicholas A. Meanwell
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Publication number: 20120201816Abstract: The present application describes lactam-containing compounds and derivatives thereof of Formula I: P4—P-M-M4??I or pharmaceutically acceptable salt forms thereof, wherein ring P, if present is a 5-7 membered carbocycle or heterocycle and ring M is a 5-7 membered carbocycle or heterocycle. Compounds of the present invention are useful as inhibitors of trypsin-like serine proteases, specifically factor Xa.Type: ApplicationFiled: April 12, 2012Publication date: August 9, 2012Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Donald J. P. Pinto, Mimi L. Quan, Michael J. Orwat, Yun-Long Li, Wei Han, Jennifer X. Qiao, Patrick Y. S. Lam, Stephanie L. Koch
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Patent number: 8232404Abstract: 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: GrantFiled: June 14, 2011Date of Patent: July 31, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Dean A. Wacker, Karen A. Rossi, Ying Wang
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Publication number: 20120190699Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing the compounds of the invention and intermediate compounds useful in these processes.Type: ApplicationFiled: December 14, 2011Publication date: July 26, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Jean-Damien Charrier, Steven Durrant, Sharn Ramaya, Juan-Miguel Jimenez, Alistair Rutherford
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Patent number: 8227613Abstract: The invention is concerned with novel heteroaryl carboxamide derivatives of formula (I), wherein m, X, Y, R1, R2, R3 and R4 are as defined in the description and in the claims, as well as physiologically acceptable salts thereof. These compounds are antagonists of CCR-2 receptor, CCR-5 receptor and/or CCR-3 receptor and can be used as medicaments.Type: GrantFiled: June 15, 2009Date of Patent: July 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Jean-Michel Adam, Johannes Aebi, Alfred Binggeli, Luke Green, Guido Hartmann, Hans P. Maerki, Patrizio Mattei, Fabienne Ricklin, Olivier Roche
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Patent number: 8227506Abstract: Compounds represented by formula (1) and pharmaceutically acceptable salt thereofs: wherein each symbol is as defined in the specification, are useful as inhibitors of an activated blood coagulation factor X. Compositions which contain, as an active ingredient, an FXa selective low-molecular weight FXa inhibitor having a short serum half-life are particularly useful as anticoagulants for an extracorporeal blood circuit.Type: GrantFiled: August 2, 2007Date of Patent: July 24, 2012Assignee: Ajinomoto., Inc.Inventors: Masaru Takayanagi, Shunji Takehana, Kayo Otani, Yuki Saitou
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Publication number: 20120184553Abstract: The present invention relates to novel compounds that inhibit LRRK2 kinase activity, processes for their preparation, to compositions containing them and to their use in the treatment of diseases characterised by LRRK2 kinase activity, particularly Parkinson's disease and Alzheimer's disease.Type: ApplicationFiled: September 27, 2010Publication date: July 19, 2012Inventors: Paula Louise Nichols, Andrew John Eatherton, Paul Bamborough, Karamjit Singh Jandu, Oliver James Philps, Daniele Andreotti
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Publication number: 20120184520Abstract: [Problem] The present invention provides a compound which is useful as an active ingredient of a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases. [Means for Solution] The present inventors have conducted intensive studies on a compound having a VAP-1 inhibitory activity, and as a result, they have found that a compound of the present invention or a salt thereof exhibits an excellent VAP-1 inhibitory activity and is useful for preventing and/or treating VAP-1-related diseases, in particular, diabetic nephropathy or diabetic macular edema, thereby completing the present invention. The present invention further relates to a pharmaceutical composition, in particular, a pharmaceutical composition for preventing and/or treating VAP-1-related diseases, which comprises the compound of the present invention or a salt thereof, and an excipient.Type: ApplicationFiled: September 15, 2010Publication date: July 19, 2012Applicant: Astellas Pharma Inc.Inventors: Kousei Yoshihara, Daisuke Suzuki, Susumu Yamaki, Yuji Koga, Norio Seki, Jiro Fujiyasu, Masahiro Neya
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Publication number: 20120184572Abstract: Aryl GPR119 agonists are provided. These compounds are useful for the treatment of diabetic diseases, including Type II diabetes and other diseases associated with poor glycemic control.Type: ApplicationFiled: January 13, 2011Publication date: July 19, 2012Inventors: Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
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Publication number: 20120184556Abstract: Disclosed are substituted benzoimidazolesulfonamides and substituted indolesulfonamides as mGluR4 potentiators.Type: ApplicationFiled: July 23, 2010Publication date: July 19, 2012Inventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Charles David Weaver, Colleen M. Niswender, Yiu-Yin Cheung
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Publication number: 20120184538Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 10, 2012Publication date: July 19, 2012Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Patent number: 8222418Abstract: Compounds of formula I: modulate the action of gamma secretase, and hence find use in treatment of Alzheimer's disease and related conditions.Type: GrantFiled: March 27, 2007Date of Patent: July 17, 2012Assignee: Merck Sharp + Dohme Corp.Inventors: Joanne Clare Hannam, Sascha Hartmann, Andrew Madin, Mark Peter Ridgill
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Publication number: 20120178723Abstract: This invention provides compounds of formula IA-a or IB-a and subsets thereof: wherein Z, HY, R1, R2, G1, W, n, and A and subsets thereof are as described in the specification. The compounds are inhibitors of PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 11, 2011Publication date: July 12, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Masaaki Hirose, Zhigen Hu, Yongbo Hu, Hong Myung Lee, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120178741Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y, Z and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: ApplicationFiled: March 21, 2012Publication date: July 12, 2012Applicant: JANSSEN PHARMACEUTICA N.V.Inventors: Kristof Van Emelen, Leo Jacobus Jozel Backx, Sven Franciscus Anna Van Brandt, Patrick René Angibaud, Isabelle Noélle Constance Pilatte, Marc Gustaaf Celine Verdonck, Hans Louis Jos De Winter, Jimmy Arnold Viviane Van heusden
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Publication number: 20120177570Abstract: The invention relates to compounds of formula IA? and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula IA? or a pharmaceutically acceptable derivative thereof.Type: ApplicationFiled: February 14, 2012Publication date: July 12, 2012Applicant: Purdue Pharma L.P.Inventor: Laykea TAFESSE
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Publication number: 20120178734Abstract: Derivatives of 6,7-dihydro-5H-imidazo[1,2-a]imidazole-3-carboxylic acid amide exhibit good inhibitory effect upon the interaction of CAMs and Leukointegrins and are thus useful in the treatment of inflammatory disease.Type: ApplicationFiled: May 28, 2010Publication date: July 12, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Jennifer A. Kowalski, Matt Aaron Tschantz
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Patent number: 8217028Abstract: The present invention relates to novel oxadiazole derivatives having pharmacological activity, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of various disorders.Type: GrantFiled: June 18, 2009Date of Patent: July 10, 2012Assignee: Glaxo Group LimitedInventors: Jose Luis Castro Pineiro, Xichen Lin, Qian Liu, Kevin Meng, Feng Ren, David R Vesey, Baowei Zhao
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Publication number: 20120172369Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (DGAT) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.Type: ApplicationFiled: September 3, 2010Publication date: July 5, 2012Inventors: Pauline C. Ting, Joe F. Lee, Robert G. Aslanian
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Publication number: 20120165333Abstract: The present invention relates to compounds of formula I useful in the inhibition of c-Met protein kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative disorders.Type: ApplicationFiled: April 20, 2011Publication date: June 28, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Pan Li, Kira McGinty, Steven M. Ronkin, Qing Tang, Anne-Laure Grillot, Nathan D. Waal
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Publication number: 20120164103Abstract: Compounds represented by formula I: or pharmaceutically acceptable salts and solvates thereof, wherein R1, X, Y, Y1, and Z are as defined herein, are useful for treating flaviviridae viral infections.Type: ApplicationFiled: March 9, 2012Publication date: June 28, 2012Applicant: Vertex Pharmaceuticals (Canada) IncorporatedInventors: Real Denis, Carl Poisson, Sanjoy Kumar Das, Irina Motorina, Rabindra Rej, Constantin G. Yannopoulos, Laval Chan Chun Kong
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Patent number: 8207199Abstract: A compound which is useful as an active ingredient of a pharmaceutical composition for treating neuropathic pain is provided. The present inventors have made extensive studies on compounds having an FAAH inhibitory activity, and as a result, have found that an azole compound substituted with an N-(pyridine-3-yl)oxycarbonyl-piperidin-4-yl group and a phenyl group or a pharmaceutically acceptable salt thereof has an excellent FAAH inhibitory activity, thereby completing the present invention. The compound of the present invention is confirmed to have an excellent FAAH inhibitory activity and an antiallodynic effect in rat models with neuropathic pain, and thus is useful as an agent for preventing and/or an agent for treating neuropathic pain.Type: GrantFiled: July 13, 2009Date of Patent: June 26, 2012Assignee: Astellas Pharma Inc.Inventors: Satoshi Aoki, Ryosuke Munakata, Noriyuki Kawano, Kiyohiro Samizu, Hiromasa Oka, Takahiro Ishii, Takashi Sugane
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Patent number: 8207198Abstract: The present invention relates to substituted triazoles of formula (I), uses thereof, processes for the preparation thereof and compositions containing said compounds. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction.Type: GrantFiled: May 15, 2009Date of Patent: June 26, 2012Assignee: Pfizer Inc.Inventors: Alan Daniel Brown, Andrew Antony Calabrese, David Ellis
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Patent number: 8207166Abstract: The present invention relates to compounds of formula (I), pharmaceutical compositions which contain them and methods for treating cancer using compounds of formula (I).Type: GrantFiled: November 8, 2010Date of Patent: June 26, 2012Assignee: Bayer Healthcare LLCInventors: Wendy Lee, Gaetan Ladouceur, Jacques Dumas, Roger Smith, Shihong Ying, Gan Wang, Zhi Chen, Qingjie Liu, Holia Mokdad
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Publication number: 20120157433Abstract: The present invention provides a compound of Formula (I): and pharmaceutically acceptable salts thereof. Also provided is a method of using a compound of Formula I for treating a disease or condition mediated by a CDK inhibitor.Type: ApplicationFiled: September 2, 2010Publication date: June 21, 2012Inventors: Keith B. Pfister, Martin Sendzik
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Publication number: 20120157432Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and method of using the same in the treatment or prevention of diseases mediated by the activation of ?3-adrenoceptor.Type: ApplicationFiled: August 17, 2010Publication date: June 21, 2012Applicant: Merck Sharp & Dohme, Corp.Inventors: Scott D. Edmondson, Richard Berger, Lehua Chang, Vincent j. Colandrea, Jeffrey J. Hale, Bart Harper, Nam Fung Kar, Bing Li, Greg J. Morriello, Christopher R. Moyes, Deyou Sha, Dong-Ming Shen, Liping Wang, Harvey Wendt, Cheng Zhu
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Publication number: 20120157449Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, x, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: ApplicationFiled: December 7, 2011Publication date: June 21, 2012Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20120157494Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein the variables are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of diseases associated with the P2X7 purinergic receptor.Type: ApplicationFiled: December 14, 2011Publication date: June 21, 2012Inventors: Ralph New Harris, III, David Bruce Repke, Keith A.M. Walker
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Publication number: 20120157425Abstract: The invention relates to new piperidine derivatives of the formula I to their use as medicaments, to methods for their therapeutic use and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 21, 2011Publication date: June 21, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Gerald Juergen ROTH, Martin FLECK, Thorsten LEHMANN-LINTZ, Heike NEUBAUER, Bernd NOSSE
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Patent number: 8202910Abstract: Methods and compositions for treating disease caused by infectious agents, particularly tuberculosis. In particular, methods and compositions comprising substituted ethylene diamines for the treatment of infectious diseases are provided. In one embodiment, these methods and compositions are used for the treatment of mycobacterial infections, including, but not limited to, tuberculosis. In certain embodiments, the present invention comprises compositions comprising novel substituted ethylene diamine compounds further comprising antitubercular agents such as rifampicin, isoniazid, pyrazinamide and ethambutol.Type: GrantFiled: October 22, 2008Date of Patent: June 19, 2012Assignee: Sequella, Inc.Inventors: Marina Nikolaena Protopopova, Leo Einck, Boris Nikonenko, Ping Chen
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Patent number: 8202856Abstract: 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: GrantFiled: December 17, 2008Date of Patent: June 19, 2012Assignee: Merck Serono SAInventors: Anna Quattropani, Christophe Cleva, Eric Sebille, Matthias Schwarz, Delphine Marin, Agnes Bombrun, Wesley Blackaby, Charles Baker-Glenn, Chris Knight, Craig Rouse
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Patent number: 8202871Abstract: The present application discloses compounds of the formula: and pharmaceutical compositions containing same and their use for treating and preventing various pathologies, including obesity, appetite disorders, excess weight and diabetes.Type: GrantFiled: January 24, 2011Date of Patent: June 19, 2012Assignee: Sanofi-AventisInventors: Marco Baroni, Letizia Puleo