Carbocyclic Ring Containing Patents (Class 546/194)
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Publication number: 20110312963Abstract: The present disclosure relates to compounds of formula (I): which are inhibitors of p38 mitogen-activated protein kinase enzymes, particularly the alpha and gamma kinase sub-types thereof, and their use in therapy, including in pharmaceutical combinations, especially in the treatment of inflammatory diseases, including inflammatory diseases of the lung, such as COPDType: ApplicationFiled: December 11, 2009Publication date: December 22, 2011Inventors: Kazuhiro Ito, Peter Strong, William Garth Rapeport, Peter John Murray, John King-Underwood, Jonathan Gareth Williams, Stuart Thomas Onions, Kevin Joly, Catherine Elisabeth Charron
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Publication number: 20110312944Abstract: Compounds which modulate the CB2 receptor 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: February 16, 2010Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20110312995Abstract: This invention provides for certain bridged and fused heterocyclic compounds of the formula (I) or a pharmaceutically acceptable salt, ester solvate or prodrug thereof wherein: L is: (II) and the other variables are defined herein; the inventive compounds are agonists of the G-protein coupled receptor 40 (GPR40, also known as free fatty acid receptor FFAR). This invention further relates to pharmaceutical compositions containing these compounds, and the use of these compounds to regulate insulin levels in a mammal. The compounds may be used, for example in the prevention and treatment of Type 2 diabetes mellitus and in the prevention and treatment of conditions related to Type 2 diabetes mellitus, such as insulin resistance, obesity and lipid disorders.Type: ApplicationFiled: January 21, 2010Publication date: December 22, 2011Applicant: Schering CorporationInventors: Hubert B. Josien, John W. Clader, William J. Greenlee, Michael John Mayer, Robert Jason Herr, Jason L. Davis, Kai Deng, Ming Min Hsia, Shuangyi Wan
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Publication number: 20110306606Abstract: The present invention relates to a novel 2,6-substituted-3-nitropyridine derivative compound, a method for preparing the same, and a pharmaceutical composition including the same for prevention and treatment of osteoporosis. The 2,6-substituted-3-nitropyridine derivative compound of the present invention increases osteoblast activity and effectively inhibits the differentiation of osteoclasts, and thus can be usefully used for the prevention and treatment of osteoporosis.Type: ApplicationFiled: December 4, 2009Publication date: December 15, 2011Inventors: Jei Man Ryu, Jin Soo Lee, Whui Jung Park, Yun Ha Hwang, Ki Yoon Kim
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Publication number: 20110306587Abstract: Unsaturated nitrogen heterocyclic compounds of formula (I): as defined in the specification, compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, Huntington's Disease, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. ALLEN, Jian J. Chen, Michael J. Frohn, Essa Hu, Qingyian Liu, Alexander J. Pickrell, Shannon Rumfelt, Robert M. Rzasa, Wenge Zhong
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Publication number: 20110306591Abstract: Heteroaryloxycarbocyclyl compounds, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, Huntington's Disease, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: May 11, 2011Publication date: December 15, 2011Inventors: Jennifer R. Allen, Michael J. Frohn, Paul E. Harrington, Essa Hu, Alexander J. Pickrell, Robert M. Rzasa, Kelvin K. C. Sham
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Publication number: 20110306636Abstract: The present invention provides oxadiazole pyridine derivatives of Formula (I), their use as medicaments and their use for treating multiple sclerosis and other diseases.Type: ApplicationFiled: March 2, 2010Publication date: December 15, 2011Applicant: Merck Serono SAInventors: Anna Quattropani, Patrick Gerber, Jerome Dorbais
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Patent number: 8076329Abstract: The present patent application concerns compounds of formula (I) with R1 and R2 taken together with the nitrogen atom to which they are attached, form a mono or bicyclic saturated nitrogen-containing ring; their preparation and their use as a H3 receptor ligand for treating e.g. CNS disorders like Alzheimer's disease.Type: GrantFiled: April 25, 2006Date of Patent: December 13, 2011Assignee: BioprojetInventors: Isabelle Bertrand, Marc Capet, Jeanne-Marie Lecomte, Nicolas Levoin, Xavier Ligneau, Olivia Poupardin-Olivier, Philippe Robert, Jean-Charles Schwartz, Olivier Labeeuw
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Patent number: 8076359Abstract: The present invention relates to disubstituted piperidinyl renin inhibitor compounds having the structure (Formula I) and their use in treating cardiovascular events and renal insufficiency.Type: GrantFiled: November 14, 2007Date of Patent: December 13, 2011Assignee: Merck Canada Inc.Inventors: Daniel Dube, Michel Gallant, Erich L. Grimm, Helene Juteau, Sebastien Laliberte, Tom Yao-Hsiang Wu
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Publication number: 20110301156Abstract: Vanilloid receptor ligand compounds corresponding to formula I: pharmaceutical compositions containing such compounds, a process for producing such compounds, and methods of using such compounds for treating or inhibiting pain and various other disorders or conditions.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: Gruenenthal GmbHInventors: Robert Frank, Gregor Bahrenberg, Thomas Christoph, Klaus Schiene, Jean De Vry, Derek Saunders, Bernd Sundermann, Jeewoo Lee
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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: 20110301196Abstract: The invention provides compounds that are effective as inhibitors of human plasmin and plasma kallikrein, and that are useful for the prevention of blood loss and as components of fibrin adhesives. The invention further provides methods of making and using the compounds.Type: ApplicationFiled: January 28, 2011Publication date: December 8, 2011Applicant: The Medicines Company (Leipzig) GmbHInventors: Peter HEROLD, Mohammed DAGHISH, Stjepan JELAKOVIC, Friedrich-Alexander LUDWIG, Claudia REICHELT, Alexander SCHULZE, Andrea SCHWEINITZ
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Patent number: 8071615Abstract: This invention comprises the novel compounds of formula (I) wherein n, m, t, R1, R2, R3, R4, R5, L, Q, X, Y and have defined meanings, having histone deacetylase inhibiting enzymatic activity; their preparation, compositions containing them and their use as a medicine.Type: GrantFiled: September 19, 2008Date of Patent: December 6, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Kristof Van Emelen, Marc Gustaaf Celine Verdonck, Sven Franciscus Anna Van Brandt, Leo Jacobus Jozef Backx
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Patent number: 8071778Abstract: The invention encompasses compounds of Formula I, including pharmaceutically acceptable salts, their pharmaceutical compositions, and their use in treating CNS disorders.Type: GrantFiled: January 25, 2008Date of Patent: December 6, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Michael F. Parker, Joanne J. Bronson, Mark V. Silva, Kevin W. Gillman
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Patent number: 8071593Abstract: Described are compounds which inhibit, regulate and/or modulate kinase signal transduction, for example of Met kinase. The compounds are of the formulae A1 to A148 and B1 described herein, including 2-oxobenzoxazol-3-ylmethyl]phenyl}carbamate and 2-oxooxazolo[4,5-b]pyridin-3-ylmethyl)phenyl]carbamate compounds, and pharmaceutically usable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. Also described are compositions containing these compounds. Also described are methods for the treatment of diseases in which the inhibition, regulation and/or modulation of kinase signal transduction plays a role by administering these compounds.Type: GrantFiled: May 8, 2008Date of Patent: December 6, 2011Assignee: Merck Patent Gesellschaft mit beschrankter HaftungInventors: Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
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Publication number: 20110294793Abstract: The present invention provides compound of Formula (I): or a stereoisomer, tautomer, salt or solvate thereof, wherein the variables are defined herein. The compounds of formula (I) are inhibitors of Bcl-2 family antiapoptotic proteins, compositions containing the compounds and methods of treating diseases using the compounds.Type: ApplicationFiled: June 8, 2009Publication date: December 1, 2011Inventors: kyoung S Kim, Robert M. Borzilleri, Zhen-Wei Cai, Kap-Sun Yeung
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Publication number: 20110294836Abstract: 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: June 16, 2009Publication date: December 1, 2011Applicant: METABOLEX, INC.Inventors: Jiangao Song, Jingyuan Ma, Christopher J. Rabbat, Imad Nashashibi, Xin Chen, Zuchun Zhao
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Publication number: 20110294788Abstract: The present invention relates to novel substituted dihydropyrazolone derivatives, to their preparation and to their therapeutic use as activators of the transcription factor HIF.Type: ApplicationFiled: June 29, 2011Publication date: December 1, 2011Applicant: SANOFIInventors: Jean-Michel ALTENBURGER, Valérie FOSSEY, Stéphane ILLIANO, Géraldine MANETTE
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Patent number: 8063068Abstract: Novel vinylazacycloalkane compounds of Formula (I) are disclosed. The compounds are ligands of various nAChRs. The compounds and their pharmaceutically acceptable salts can be used to prepare pharmaceutical compositions and/or medicaments intended to prevent or treat disorders associated with dysfunction of nAChRs, especially within the central nervous system or the gastrointestinal system. Examples of types of disorders that can be treated include neurodegenerative disorders, including central nervous system disorders such as Alzheimer's disease, cognitive disorders, motor disorders such as Parkinson's disease, drug addiction, behavioral disorders and inflammatory disorders within the gastrointestinal system. The compounds can also serve as analgesics in the treatment of acute, chronic or recurrent pain.Type: GrantFiled: January 5, 2009Date of Patent: November 22, 2011Assignee: Targacept, Inc.Inventors: Jeffrey Daniel Schmitt, Gary Maurice Dull, Craig Harrison Miller, Arielle Genevois-Borella, Marc Capet, Michel Cheve
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Publication number: 20110281874Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: July 27, 2011Publication date: November 17, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. AICHER, Steven Armen BOYD, Mark Joseph CHICARELLI, Kevin Ronald CONDROSKI, Ronald Jay HINKLIN, Ajay SINGH
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Publication number: 20110281840Abstract: This invention relates to compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein X, R1, R2, R3, R4, R5, R6, R7, k, m, n, p, q, r and s are each as described herein, and compositions containing such compounds, and the use of such compounds in the treatment of a condition mediated by CB2 receptor activity.Type: ApplicationFiled: January 22, 2010Publication date: November 17, 2011Inventors: Kazuo Ando, Yasuhiro Iwata
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Publication number: 20110281872Abstract: The invention relates to compositions and methods for the treatment and prevention of cancer and other cell proliferative disorders.Type: ApplicationFiled: March 11, 2011Publication date: November 17, 2011Applicant: Kinex Pharmaceuticals, LLCInventors: David G. Hangauer, JR., Michael J. Ciesielski, Robert A. Fenstermaker
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Publication number: 20110280808Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 18, 2011Publication date: November 17, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Publication number: 20110281851Abstract: The invention provides compounds of formula I: wherein a, b, c, m, s, t, W, Z, Ar, R1, R2, R3, R6, and R7 are as defined in the specification. The compounds of formula I are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes and intermediates for preparing such compounds and methods of using such compounds to treat pulmonary disorders.Type: ApplicationFiled: July 29, 2011Publication date: November 17, 2011Applicant: THERAVANCE, INC.Inventors: Yu-Hua JI, Mathai MAMMEN, Craig HUSFELD, Li LI, YongQi MU, Aaron KUSHNER, Eric STANGELAND, Trevor MISCHKI, Adam HUGHES, Sarah DUNHAM
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Publication number: 20110281871Abstract: The invention relates to a compound of formula wherein R1, R2, X, L, W, n, and o are defined herein and to pharmaceutically suitable acid addition salts thereof, with the exception of the following compounds 6-(4-methyl-piperazin-1-yl)-N-phenethyl-nicotinamide (CAS 199478-31-4), N-(3,4-dichloro-benzyl)-3-fluoro-benzamide (CAS 424815-98-5), N-(4-chloro-benzyl)-3-fluoro-benzamide (CAS 544661-83-8), N-(3-chloro-benzyl)-3-fluoro-benzamide (CAS 796051-07-5), and N-phenethyl-6-phenylamino-nicotinamide (CAS 571913-74-1). The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1 and are useful for the treatment of CNS disorders.Type: ApplicationFiled: July 26, 2011Publication date: November 17, 2011Inventors: Guido Galley, Katrin Groebke Zbinden, Roger Norcross, Henri Stalder
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Patent number: 8058271Abstract: Described herein are compounds that are useful as ROCK inhibitors. These compounds, and pharmaceutically acceptable compositions thereof, are useful for treating or lessening the severity of a variety of disorders, including cardiovascular, inflammatory, neurological, or proliferative diseases or disorders.Type: GrantFiled: May 10, 2007Date of Patent: November 15, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Jeremy Green, Jingrong Cao, Upul Bandarage, Jon Come, Craig Marhefka
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Publication number: 20110275639Abstract: Compounds are provided that are modulators of the C5a receptor. The compounds are substituted piperidines and are useful in pharmaceutical compositions, methods for the treatment of diseases and disorders involving the pathologic activation of C5a receptors.Type: ApplicationFiled: March 25, 2011Publication date: November 10, 2011Applicant: ChemoCentryx, Inc.Inventors: Pingchen Fan, Kevin Lloyd Greenman, Manmohan Reddy Leleti, Yandong Li, Jay P. Powers, Hiroko Tanaka, Ju Yang, Yibin Zeng
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Publication number: 20110275608Abstract: A method for preventing and/or treating a metabolic disease, cerebrovascular disease, etc. which comprises administering to a mammal an effective amount of the compound of the formula (I): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof. And a novel compound of the formula (I-1): wherein all symbols have the same meanings as defined in the specification; a salt thereof, an N-oxide thereof, a solvate thereof, or a prodrug thereof has an anti-diabetic effect and a neuroprotective effect. Accordingly, the compound of the formula (I) and the compound of the formula (I-1) are useful in a method for preventing and/or treating for a metabolic disease such as diabetes, cerebrovascular disease such as stroke, etc.Type: ApplicationFiled: January 7, 2010Publication date: November 10, 2011Applicant: ARRAY BIOPHARMA INC.Inventors: Martha E. Rodriguez, David A. Mareska, Jeremy J. Hans, Darren M. Harvey, Robert D. Groneberg, Michael O'Sullivan
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Publication number: 20110275615Abstract: An amide of the formula I and its tautomeric forms, possible enantiomeric and diastereomeric forms, E and Z forms, and possible physiologically tolerated salts, in which the variables have the following meanings: A —(CH2)p—R1, where R1 can be pyrrolidine, morpholine, piperidine, —NR5R6 and and R5, R6 and R7 can, independently of one another, be hydrogen, C1-C4-alkyl, CH2Ph, Ph, CH2CH2Ph, it also being possible for the phenyl rings to be substituted by R6, and p can be 1 and 2, and B can be phenyl, pyridyl, pyrimidyl and pyridazyl, it also being possible for the rings to be substituted by up to 2 R8 radicals, and D can be a bond, —(CH2)m—, —CH?CH—, —C?C—, and R2 is chlorine, bromine, fluorine, C1-C6-alkyl, NHCO—C1-C4-alkyl, NHSO2—C1-C4-alkyl, NO2, —O—C1-C4-alkyl and NH2, and R3 is —C1-C6-alkyl, branched or unbranched, and which may also carry a phenyl ring, indolyl ring or cyclohexyl ring which is in turn substituted by a maximum of two R8 radicals, where R8 is hydrogen, C1-C4-alkyl, branched or unType: ApplicationFiled: October 29, 2010Publication date: November 10, 2011Inventors: Hans-Jörg Treiber, Monika Knopp, Wilfried Lubisch, Achim Moeller
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Publication number: 20110275797Abstract: An N-acyl anthranilic acid derivative represented by general formula (1) or a salt thereof is useful for prevention or treatment of diseases associated with excessive production of collagen. (In the formula, R1 represents a carboxyl group or the like; R2 represents a hydrogen atom or the like; R3 represents an optionally substituted aryl group or the like; X1 represents a carbonyl group; X2 represents a bonding hand; X3 represents a bonding hand; X4 represents a bonding hand or the like; and A represents an optionally substituted phenyl group or the like.Type: ApplicationFiled: January 29, 2010Publication date: November 10, 2011Applicant: Toyama Chemical Co., Ltd.Inventors: Junichi Yokotani, Arihiro Takatori, Yukie Tada, Minori Yanai, Hiroshi Kato, Yoichi Taniguchi, Chiharu Tanabe
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Publication number: 20110275612Abstract: Disclosed is a compound of formula (I). Wherein R1, R2Ar and Cy are as defined herein, or a pharmaceutically acceptable salt thereof. Also disclosed are pharmaceutical compositions of the compound of formula (I), methods of making the compounds of formula I, and methods of using the compounds of formula (I) to treat a disorder associated with activation of CCR10.Type: ApplicationFiled: May 14, 2009Publication date: November 10, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Alexander Heim-Riether, Wang Mao, Craig Andrew Miller, Philip Dean Ramsden, Lana Louise Smith Keenan, Roger John Snow, Jiang-Ping Wu, Yu Yang
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Publication number: 20110269734Abstract: Compounds of formula (I):or pharmaceutically acceptable salts thereof, are GPCR agonists and are useful as for the treatment of diabetes and obesity.Type: ApplicationFiled: July 10, 2009Publication date: November 3, 2011Applicant: Prosidion LimitedInventors: Lisa Sarah Bertram, Matthew Colin Thor Fyfe, Revathy Perpetua Jeevaratnam, John Keily, Thomas Martin Krulle, Chrystelle Marie Rasamison, Colin Peter Sambrook-Smith, Simon Andrew Swain
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Publication number: 20110269742Abstract: Disclosed are Serotonin 5-HT2B receptor inhibitors of the formula I. Also disclosed are methods of making and methods of using these compounds.Type: ApplicationFiled: December 14, 2009Publication date: November 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Derek Cogan, Neil Moss, Christopher Ronald Sarko, Samantha Jayne Bamford, Pui Leng Loke, Spencer Charles R. Napier, Heather Tye, Mark Whittaker
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Publication number: 20110269712Abstract: This invention is directed to compounds of Formula (1) including all geometric and stereoisomers, N oxides, and agriculturally suitable salts thereof, agricultural compositions containing them and their use as fungicides, (1) provided that the compound of Formula 1 is other than 2-[1-[(2-chlorophenyl)acetyl]-4-piperidinyl]-N-methyl-N-[(1R)-1-phenylethyl]-4-thiazolecarboxamide and R1 is other than 4-fluorophenyl; wherein R1, R2, A, G, Q, W1, W2, X and n are otherwise as defined in the disclosure, Also disclosed are compositions containing the a compound having a formula corresponding to Formula (1) where the provisos are both omitted; and methods for controlling plant diseases caused by fungal plant pathogens which involves applying an effective amount of a compound having a formula corresponding to Formula (1) where the provisos are both omitted.Type: ApplicationFiled: July 26, 2006Publication date: November 3, 2011Inventors: John Joseph Bisaha, Patrick Ryan Kovacs, Renne M. Lett, Jeffrey Keith Long, Robert James Pasteris, Boris Abramovich Klyashchitsky, Bruce Lawrence Finkelstein, Brenton Todd Smith
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Publication number: 20110269747Abstract: Polyarylcarboxamide compounds of formula (I) are useful as lipid lowering agents.Type: ApplicationFiled: July 13, 2011Publication date: November 3, 2011Inventors: Lieven Meerpoel, Peter Walter Maria Roevens, Leo Jacobus Jozef Backx, Louis Jozef Elisabeth Van der Veken, Marcel Viellevoye
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Publication number: 20110263643Abstract: The present invention is directed to 2,3-disubstituted piperidine amide compounds which are antagonists of orexin receptors, and which are useful in the treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which orexin receptors are involved.Type: ApplicationFiled: October 15, 2009Publication date: October 27, 2011Inventors: Christopher D. Cox, Broc Flores, John D. Schreier
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Publication number: 20110263560Abstract: 3,4-substituted piperidine compounds, these compounds for use in the diagnostic and therapeutic treatment of a warm-blooded animal, especially for the treatment of a disease (=disorder) that depends on activity of renin; the use of a compound of that class for the preparation of a pharmaceutical formulation for the treatment of a disease that depends on activity of renin; the use of a compound of that class in the treatment of a disease that depends on activity of renin; pharmaceutical formulations comprising a 3,4-substituted piperidine compound, and/or a method of treatment comprising administering a 3,4substituted piperidine compound, a method for the manufacture of a 3,4-substituted piperidine compound, and novel intermediates and partial steps for their synthesis are disclosed. The 3,4-disubstituted piperidine compounds have the formula (I), wherein the symbols have the meanings defined in the specification.Type: ApplicationFiled: July 6, 2011Publication date: October 27, 2011Applicant: NOVARTIS AGInventors: Werner BREITENSTEIN, Takeru EHARA, Claus EHRHARDT, Philipp GROSCHE, Yuko HITOMI, Yuki IWAKI, Takanori KANAZAWA, Kazuhide KONISHI, Juergen Klaus MAIBAUM, Keiichi MASUYA, Atsuko Nihonyanagi, Nils OSTERMANN, Masaki SUZUKI, Atsushi TOYAO, Fumiaki YOKOKAWA
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Publication number: 20110263628Abstract: The present invention is related to N-hydroxyamide derivatives of Formula (I) and use thereof in particular for the treatment and/or prophylaxis of autoimmune disorders, inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, cancer, respiratory diseases and fibrosis, including multiple sclerosis, arthritis, emphysema, chronic obstructive pulmonary disease, liver and pulmonary fibrosis.Type: ApplicationFiled: June 8, 2011Publication date: October 27, 2011Applicant: APPLIED RESEARCH SYSTEMS ARS HOLDING N.V.Inventors: Dominique Swinnen, Agnes Bombrun, Jerome Gonzalez, Stefano Crosignani, Patrick Gerber, Catherine Jorand-Lebrun
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Publication number: 20110263548Abstract: Novel compounds of structure Formula (I) or an enantiomer, a diastereomer, or a pharmaceutically acceptable salt thereof, wherein Z, R1, R2, R21, T1, T2, T3 and T4 are defined herein, 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. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: July 15, 2009Publication date: October 27, 2011Applicant: BRISTOL-MYERS SQUIBB COMPANYInventors: Dean A. Wacker, Karen A. Rossi, Ying Wang, Gang Wu
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Publication number: 20110263571Abstract: Provided are a novel low-molecular-weight compound that suppresses production of induction type MMPs, particularly MMP-9, rather than production of hemostatic type MMP-2, as well as a prophylactic/therapeutic drug for autoimmune diseases or osteoarthritis. An amide derivative represented by the following formula (I) wherein each symbol is as defined in the specification, a pharmacologically acceptable salt thereof, or a hydrate or solvate thereof.Type: ApplicationFiled: October 27, 2009Publication date: October 27, 2011Applicant: MITSUBISHI TANABE PHARMA CORPORATIONInventors: Seigo Ishibuchi, Hidemasa Hikawa, Akiko Tarao, Jun-ichi Endoh, Kunitomo Adachi, Kazuhiro Maeda, Kaoru Tashiro
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Publication number: 20110263428Abstract: Compounds of formula (I), wherein the substituents are as defined in claim 1, are suitable for use as herbicides.Type: ApplicationFiled: July 1, 2009Publication date: October 27, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Stephane Andre Marie Jeanmart, Russell Colin Viner, John Benjamin Taylor, William Guy Whittingham, Jeffrey Steven Wailes, Sarah Margaret Targett, Christopher John Mathews, Mangala Govenkar, Matthew Robert Cordingley, Claire Janet Russell, Melloney Tyte
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Publication number: 20110256064Abstract: The present invention relates to novel compounds that can be employed in the treatment of a group of disorders and abnormalities associated with amyloid protein, such as Alzheimer's disease, and of diseases or conditions associated with amyloid-like proteins. The compounds of the present invention can also be used in the treatment of ocular diseases associated with pathological abnormalities/changes in the tissues of the visual system. The present invention further relates to pharmaceutical compositions comprising these compounds and to the use of these compounds for the preparation of medicaments for treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins. A method of treating or preventing diseases or conditions associated with amyloid and/or amyloid-like proteins is also disclosed.Type: ApplicationFiled: April 15, 2011Publication date: October 20, 2011Applicant: AC Immune, S.A.Inventors: Heiko Kroth, Cotinica Hamel, Pascal Benderitter, Wolfgang Froestl, Nampally Sreenivasachary, Andreas Muhs
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Patent number: 8039490Abstract: The present invention relates to compounds of the general formula as dual modulators of the 5-HT2a and D3 receptors useful against CNS disorders, wherein A, R1, R2, n, p, q and r are as defined in the specification.Type: GrantFiled: February 13, 2007Date of Patent: October 18, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Georg Jaeschke, Thomas Luebbers, Olivier Roche, Rosa Maria Rodriguez Sarmiento, Lucinda Steward
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Publication number: 20110251190Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and other related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, R2, R7, X and Y of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.Type: ApplicationFiled: March 14, 2011Publication date: October 13, 2011Applicant: Amgen Inc.Inventors: Yuan CHENG, Ryan White, Albert Amegadzie, James Brown, Alan C. Cheng, Erin F. Dimauro, Thomas Dineen, Oleg Epstein, Vijay Keshav Gore, Jason Brooks Human, Ted Judd, Charles Kreiman, Qingyian Liu, Patricia Lopez, Vu Van Ma, Isaac Marx, Ana Minatti, Hanh Nho Nguyen, Nick A. Paras, Vinod F. Patel, Wenyuan Qian, Matthew Weiss, Qiufen Xue, Xiao Mei Zheng, Wenge Zhong
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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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Publication number: 20110243865Abstract: Disclosed is a melanin production inhibitor which has an excellent inhibitory activity on the production of melanin and is highly safe. The melanin production inhibitor comprises a compound represented by general formula (1) (excluding clotrimazole), and/or a pharmacologically acceptable salt thereof.Type: ApplicationFiled: December 22, 2009Publication date: October 6, 2011Applicant: POLA CHEMICAL INDUSTRIES INC.Inventors: Kouji Yokoyama, Makoto Kimura, Masashi Tamai, Yuko Saitoh, Tomomi Kato, Yu Ikeda
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Publication number: 20110245220Abstract: The invention provides compounds, pharmaceutical compositions comprising such compounds and methods of using such compounds to treat or prevent diseases or disorders associated with the activity of GPR119.Type: ApplicationFiled: October 1, 2010Publication date: October 6, 2011Applicant: IRM LLCInventors: Mihai Azimioara, Christopher Cow, Robert Epple, Gerald Lelais, John Mecom, Victor Nikulin
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Publication number: 20110245223Abstract: The present invention provides a compound represented by the following formula [1?] or a salt thereof: wherein ring A, R2, R3, R4 and X are as defined in the description, and an agent for the treatment or prophylaxis of a pathology involving glucocorticoid, or a 11?HSD1 inhibitor, containing the compound or a salt thereof.Type: ApplicationFiled: December 1, 2010Publication date: October 6, 2011Applicant: Japan Tobacco Inc.Inventors: Hiroshi Yamamoto, Yasuhiro Ohe, Hiroyuki Goto, Kazuhito Harada, Shinji Yata, Takashi Ito, Jun Nishiu, Makoto Kakutani, Shunsuke Fujii, Kota Asahina
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Publication number: 20110245226Abstract: The present application describes substituted piperidinyl modulators of MIP-1? or CCR-1 or stereoisomers or pharmaceutically acceptable salts thereof. In addition, methods of treating and preventing inflammatory diseases such as asthma and allergic diseases, as well as autoimmune pathologies such as rheumatoid arthritis and transplant rejection using said modulators are disclosed.Type: ApplicationFiled: June 8, 2011Publication date: October 6, 2011Inventors: Percy H. Carter, Cullen L. Cavallaro, John V. Duncia, Daniel S. Gardner, John Hynes, Rui-Qin Liu, Joseph B. Santella, Dharmpal S. Dodd
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Publication number: 20110237590Abstract: To provide a novel JAK3 inhibitor that is useful as a preventive and/or therapeutic agent for rejection and graft versus host disease (GvHD) in organ transplantation, rheumatoid arthritis, multiple sclerosis, systemic lupus erythematosus, Sjögren syndrome, Behcet's disease, type I diabetes mellitus, autoimmune thyroiditis, idiopathic thrombocytopenic purpura, ulcerative colitis, Crohn's disease, asthma, allergic rhinitis, atopic dermatitis, contact dermatitis, urticaria, eczema, psoriasis, allergic conjunctivitis, uveitis, cancer, leukemia and the like. The pyridine-3-carboxyamide derivative represented by the general formula (1): or its salt or a solvate thereof.Type: ApplicationFiled: November 27, 2009Publication date: September 29, 2011Inventors: Takahiro Kitamura, Hajime Yamada, Shunji Takemura, Masanori Ashikawa, Tetsuya Ishikawa, Yoshiharu Miyake, Akiyasu Kouketsu, Seiichi Sato, Hiroyuki Ishiwata, Yuichiro Tabunoki, Manabu Shibasaki, Takatoshi Ozawa, Ryota Shigemi, Takeshi Doi, Masahiro Tamura