Ring Chalcogen In The Additional Hetero Ring (e.g., Oxazole, Etc.) Patents (Class 514/236.8)
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Publication number: 20120283255Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 27, 2012Publication date: November 8, 2012Inventors: Pierre DEPREZ, Hélène Jary, Taoues Temal
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Patent number: 8304412Abstract: The present application relates to novel 4-cycloalkyl- and 4-heterocycloalkyl-3,5-dicyano-2-thio-pyridine derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: November 17, 2007Date of Patent: November 6, 2012Assignee: Bayer Intellectual Property GmbHInventors: Peter Nell, Walter Hübsch, Barbara Albrecht-Küpper, Alexandros Vakalopoulos, Frank Süssmeier, Jörg Keldenich, Joachim Telser
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Publication number: 20120277150Abstract: [Object] To provide a GPR40 activating agent containing, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the compound or the salt, or the like, particularly, an insulin secretagogue and a prophylactic and/or therapeutic agent against diabetes, obesity, or other diseases. [Means of Solving the Problem] A compound of Formula (I): (where p is 0 to 4; j is 0 to 2; k is 0 to 1; a ring A is an aryl group, a heterocyclic group, a cycroalkyl group, a cycroalkenyl group, a spirocyclic group; a ring B is an aryl group, a heteroaryl group; X is 0 or —NR7—; and R1 to R7 and L are specific groups), a salt of the compound, or a solvate of the compound or the salt.Type: ApplicationFiled: April 11, 2012Publication date: November 1, 2012Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Munetaka OHKOUCHI
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Publication number: 20120270877Abstract: The invention provides compounds which directly inhibit IRE-1? activity in vitro, prodrugs, and pharmaceutically acceptable salts thereof. Such compounds and prodrugs are useful for treating diseases associated with the unfolded protein response and can be used as single agents or in combination therapies.Type: ApplicationFiled: November 1, 2010Publication date: October 25, 2012Applicant: MannKind CorporationInventors: Qingping Zeng, Warren S. Wade, John Bruce Patterson
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Publication number: 20120252796Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: September 29, 2010Publication date: October 4, 2012Inventors: Harikishore Pingali, V.V.M. Sairam Kalapatapu, Pankaj Makadia, Mukul R. Jain
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Publication number: 20120252814Abstract: Compounds of the following formula are provided for use with glucokinase: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: March 21, 2012Publication date: October 4, 2012Applicant: TAKEDA CALIFORNIA, INC.Inventors: Zacharia Cheruvallath, Jun Feng, Prasuna Guntupalli, Stephen L. Gwaltney, Joanne Miura, Mark Sabat, Mingnam Tang, Haxia Wang
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Publication number: 20120252815Abstract: The present invention relates to compounds of the formula (I), in which R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, M1, M2, M3, Y1, Y2, V, W, n, m and o have the gleanings given herein, and physiologically acceptable salts, derivatives, prodrugs, solvates, tautomers and stereoisomers thereof, including mixtures thereof in all ratios, for use in the treatment of diseases which are influenced by inhibition of Sph kinase 1.Type: ApplicationFiled: November 18, 2010Publication date: October 4, 2012Applicant: Merck Patent Gesellschaft MIT Beschrankter HaftungInventors: Frank Stieber, Dirk Wienke
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Publication number: 20120252797Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20120238561Abstract: The present invention relates to morpholinothiazole derivatives and pharmaceutically acceptable salts thereof, processes for preparing them, pharmaceutical compositions containing them and their use in therapy. The invention particularly relates to positive allosteric modulators of nicotinic acetylcholine receptors, such positive allosteric modulators having the capability to increase the efficacy of nicotinic receptor agonists.Type: ApplicationFiled: November 25, 2010Publication date: September 20, 2012Inventors: Gregor James Macdonald, Benoît Christian Albert Ghislain De Boeck, Joseph Elisabeth Leenaerts
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Publication number: 20120237478Abstract: The present application provides for a compound of Formula IV, or a pharmaceutically acceptable salt, solvate, and/or ester thereof, compositions containing such compounds, therapeutic methods that include the administration of such compounds, and therapeutic methods and include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: November 21, 2011Publication date: September 20, 2012Applicant: Gilead Sciences, Inc.Inventors: Manoj C. Desai, Allen Y. Hong, Hon C. Hui, Hongtao Liu, Randall W. Vivian, Lianhong Xu
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Patent number: 8268818Abstract: The present invention relates to compounds useful as inhibitors of PI3K, particularly of PI3K?. 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.Type: GrantFiled: September 4, 2007Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
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Publication number: 20120231995Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Publication number: 20120231076Abstract: The invention relates to pharmaceutical compositions comprising rivaroxaban, suitable for immediate release, and processes of preparing such compositions, preferably by a melt-granulation process or by a specific direct-compression process.Type: ApplicationFiled: October 5, 2010Publication date: September 13, 2012Applicant: Ratiopharm GmbHInventors: Ralph Stefan, Jana Paetz
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Publication number: 20120225880Abstract: A compound of formula (I): wherein A, B, D, X, Y, R1, R2, R3, m, p, and q are defined herein. Also disclosed is a method for inhibiting FMS-like tyrosine kinase 3, aurora kinase, or vascular endothelial growth factor receptor.Type: ApplicationFiled: March 1, 2012Publication date: September 6, 2012Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Tsu-An Hsu, Wen-Hsing Lin, Yu-Sheng Chao
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Publication number: 20120214802Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: October 9, 2009Publication date: August 23, 2012Inventors: Geoffrey M. Bilcer, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
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Publication number: 20120214788Abstract: The invention relates to novel heteroaryl-substituted piperidines, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of cardiovascular diseases and tumour diseases.Type: ApplicationFiled: February 20, 2012Publication date: August 23, 2012Applicant: Bayer Pharma AktiengesellschaftInventors: Dirk Heimbach, Susanne Röhrig, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Yolanda Cancho Grande, Mario Jeske, Kersten Matthias Gericke
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Publication number: 20120214813Abstract: The use of 5-(2,4-Dihydroxy-5-isopropyl-phenyl)-4-(4-morpholin-4-ylmethyl-phenyl)-isoxazole-3-carboxylic acid ethylamide or a tautomer thereof or a pharmaceutically acceptable salt or a hydrate or a solvate for the treatment of cancer of the bladder, the colon, the liver, the lung, the breast, the vagina, the ovaries, the pancreas, the kidney, the stomach, the gastrointestinal tract, the prostate, the head and neck, the peritoneal cavity, the thyroid, the bone, the brain, the central nervous system and/or the blood and/or for the treatment of myelodysplastic syndrome, systemic mastocytosis, von Hippel-Lindau syndrome, multicentric Castleman disease and/or psioriasis.Type: ApplicationFiled: May 2, 2012Publication date: August 23, 2012Applicant: NOVARTIS AGInventors: Patrick Chene, Carlos Garcia-Echeverria, Michael Rugaard Jensen, Cornelia Quadt, Thomas Radimerski, Joseph Schoepfer
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Patent number: 8247412Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, Y and G have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: GrantFiled: April 24, 2006Date of Patent: August 21, 2012Assignee: Galapagos SasuInventors: Pierre Deprez, Hélène Jary, Taoues Temal
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Publication number: 20120202786Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: ApplicationFiled: April 16, 2012Publication date: August 9, 2012Applicant: Dart Neuroscience (Cayman) Ltd.Inventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120196863Abstract: The present invention provides 1,4 Oxazines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.Type: ApplicationFiled: January 25, 2012Publication date: August 2, 2012Inventors: Matteo Andreini, Emanuele Gabellieri, Robert Narquizian, Massimiliano Travagli, Wolfgang Wostl
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Publication number: 20120196864Abstract: A compound represented by the formula (I): wherein each symbol is as described in the specification, or a salt thereof has a superior activity as an estrogen-related receptor-? modulator, and is useful as a prophylactic or therapeutic agent for cancer.Type: ApplicationFiled: August 4, 2010Publication date: August 2, 2012Inventors: Atsushi Hasuoka, Koji Ono, Masanori Kawasaki
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Publication number: 20120189579Abstract: The present invention concerns a substituted pyrrolidinone of the following formula I or a salt, solvate, tautomer, isotope, enantiomer, diastereoisomer or racemic mixture thereof: (I), for the treatment of hepatitis C.Type: ApplicationFiled: July 9, 2010Publication date: July 26, 2012Applicant: VIVALISInventors: Amaya Berecibar, Philippe Guedat, Isabelle Valarche, Céline Mohamed-Arab, Christophe Matt
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Patent number: 8227605Abstract: The present invention relates to novel Anilinopiperazine Derivatives of formula (I), compositions comprising the Anilinopiperazine Derivatives, and methods for using the Anilinopiperazine Derivatives for treating or preventing a proliferative disorder, an anti-proliferative disorder, inflammation, arthritis, a central nervous system disorder, a cardiovascular disease, alopecia, a neuronal disease, an ischemic injury, a viral disease, a fungal infection, or a disorder related to the activity of a protein kinase.Type: GrantFiled: October 29, 2007Date of Patent: July 24, 2012Assignee: Schering CorporationInventors: Gerald W. Shipps, Jr., Cliff C. Cheng, Xiaohua Huang, Thierry O. Fischmann, Jose S. Duca, Matthew Richards
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Patent number: 8227464Abstract: This invention relates to novel compounds that are substituted oxazolidinones derivatives and pharmaceutically acceptable salts thereof. More specifically, this invention relates to novel oxazolidinones compounds that are derivatives of rivaroxaban. The invention also provides pyrogen-free compositions comprising one or more compounds of the invention and a carrier, and the use of the disclosed compounds and compositions in methods of treating diseases and condition that are beneficially treated by administering a selective inhibitor of factor Xa, such as rivaroxaban.Type: GrantFiled: July 22, 2011Date of Patent: July 24, 2012Assignee: Concert Pharmaceuticals, Inc.Inventor: Craig E. Masse
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Patent number: 8227461Abstract: The present invention is concerned with novel isoxazole derivatives of formula I wherein X, R1, R2, R3, R4 and R5 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceuticals.Type: GrantFiled: April 23, 2010Date of Patent: July 24, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120184554Abstract: Provided are an agent for the treatment and/or prophylaxis of a mood disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: September 2, 2010Publication date: July 19, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Koji Yamada, Tomoyuki Kanda
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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: 8222243Abstract: The invention provides a compound of formula I: wherein A1, A2, A3, R1, X, Y, and B have any of the values described herein, as well as salts of such compounds, compositions comprising such compounds, and therapeutic methods that comprise the administration of such compounds. The compounds are inhibitors of monoamine oxidase B (MAO-B) enzyme function and are useful for improving cognitive function and for treating psychiatric disorders in animals.Type: GrantFiled: August 26, 2008Date of Patent: July 17, 2012Assignee: Dart NeuroScience (Cayman) LtdInventors: Alan P. Kaplan, Terence P. Keenan, Andrew J. McRiner
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Publication number: 20120178713Abstract: The present invention relates to phenyl sulfonamides useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including for example the treatment of pain.Type: ApplicationFiled: March 14, 2012Publication date: July 12, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Esther Martinborough, Lev T.D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
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Publication number: 20120178733Abstract: The present invention is directed to compounds represented by Formula I and pharmaceutically acceptable salts, solvates, hydrates, and prodrugs thereof which are inhibitors of Factor Xa. The present invention is also directed to and intermediates used in making such compounds, pharmaceutical compositions containing such compounds, methods to prevent or treat a number of conditions characterized by undesired thrombosis and methods of inhibiting the coagulation of a blood sample.Type: ApplicationFiled: August 19, 2011Publication date: July 12, 2012Inventors: Bing-Yan Zhu, Shawn M. Bauer, Zhaozhong J. Jia, Gary D. Probst, Yanchen Zhang, Robert M. Scarborough
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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: 20120172345Abstract: This invention provides compounds of formula IA-i-a or IB-i-a and subsets thereof: wherein Z, HY, R1, R2, R3, 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 5, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Brian S. Freeze, Masaaki Hirose, Yongbo Hu, Todd B. Sells, Zhan Shi, Stepan Vyskocil, Tianlin Xu
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Publication number: 20120172362Abstract: Provided are an agent for the treatment and/or prophylaxis of an anxiety disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: September 2, 2010Publication date: July 5, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junya Kase, Tomoyuki Kanda
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Patent number: 8207164Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, in free form or in salt form, to their preparation, to their medical use and to medicaments comprising them.Type: GrantFiled: July 23, 2010Date of Patent: June 26, 2012Assignee: Novartis AGInventors: Philipp Holzer, Rainer Machauer, Marina Tintelnot-Blomley
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Publication number: 20120157457Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.Type: ApplicationFiled: January 23, 2012Publication date: June 21, 2012Applicants: The Salk Institute for Biological Studies, The Scripps Research InstituteInventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter G. Schultz, Sheng Ding, Tomoko Kuwabara
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Publication number: 20120149706Abstract: This invention relates to the use of a group of aryl ureas in treating cytokine mediated diseases, other than cancer and proteolytic enzyme mediated diseases, other than cancer, and pharmaceutical compositions for use in such therapy.Type: ApplicationFiled: February 21, 2012Publication date: June 14, 2012Inventors: Jacques DUMAS, Uday KHIRE, Timothy B. Lowinger, Holger PAULSEN, Bernd RIEDL, Willian J. SCOTT, Roger A. SMITH, Jill WOOD, Holia HATOUM-MOKDAD, Wendy LEE, Aniko REDMAN, Jeffrey JOHNSON, Robert SIBLEY
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Publication number: 20120142677Abstract: 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: December 15, 2009Publication date: June 7, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela Berry, Rajashekhar Betageri, Eugene Richard Hickey, Someina Khok, Doris Riether, Lifen Wu, Renee M. Zindell
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Publication number: 20120129843Abstract: This invention relates to thiazole I and its therapeutic and prophylactic uses, wherein the variables Rz, Q, J, R1, R3, R5, and R6 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Yan ZHANG, Brett Andrew Tounge, Aihua Wang, Michael Hawkins, Kristi Anne Leonard, Joseph Kent Barbay, Umar S.M. Maharoof
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Publication number: 20120129842Abstract: This invention relates to bisthiazole I and its therapeutic and prophylactic uses, wherein the variables A, R5, R6, and R7 are defined in the specification. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: November 16, 2011Publication date: May 24, 2012Inventors: Paul Francis JACKSON, Brett Andrew Tounge, Kristi Anne Leonard, Yan Zhang, Aihua Wang, Michael Hawkins, Umar S.M. Maharoof, Joseph Kent Barbay
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Publication number: 20120122870Abstract: Ischemia-reperfusion injury remains a primary cause of morbidity and mortality in individuals who experience disruption of normal blood flow to one or more major organs. For example, there are no clinically proven strategies that prevent acute renal failure following cardiac surgery. The present invention provides a variety of methods for the treatment or prevention of ischemia-reperfusion injury. In one aspect of the invention, a method for treating or preventing ischemia-reperfusion injury includes administering to a subject an effective amount of a sphingosine kinase inhibitor. Sphingosine kinase inhibitors are very effective in the protection against IR-induced acute renal failure and liver failure. Moreover, the effects occur very early after administration, requiring only a very short time of treatment. Toxicology studies with sphingosine kinase inhibitors demonstrate that they have low toxicity, even in long-term treatment.Type: ApplicationFiled: May 10, 2010Publication date: May 17, 2012Applicants: MUSC FOUNDATION FOR RESEARCH DEVELOPMENT, APOGEE BIOTECHNOLOGY CORPORATIONInventors: Charles D. Smith, Zhi Zhong, Lynn W. Maines
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Patent number: 8178522Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: May 15, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120115839Abstract: The present invention relates to the pharmaceutical use of selective GABA A ?5 negative allosteric modulators for the treatment, prevention and/or delay of progression of central nervous system (CNS) conditions related to excessive GABAergic inhibition in the brain.Type: ApplicationFiled: November 1, 2011Publication date: May 10, 2012Inventors: Rodolfo Gasser, Maria-Clemencia Hernandez, Andrew Thomas
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Patent number: 8173652Abstract: The present invention is concerned with isoxazole-isoxazoles and isoxazole-isothiazoles of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as cognitive enhancers or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: February 12, 2010Date of Patent: May 8, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Maria-Clemencia Hernandez, Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120108576Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: ApplicationFiled: November 30, 2011Publication date: May 3, 2012Applicant: ACHILLION PHARMACEUTICALS, INC.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Publication number: 20120108571Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: ApplicationFiled: January 10, 2012Publication date: May 3, 2012Inventors: Michael Gaul, Lily Lee Searle, Dionisios Rentzeperis
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Publication number: 20120108591Abstract: A new class of alkylsulfinyl thiazolides is described. These compounds show strong activity against hepatitis viruses.Type: ApplicationFiled: October 28, 2011Publication date: May 3, 2012Inventors: J. Edward Semple, Jean-Francois Rossignol
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Patent number: 8168634Abstract: A series of thiazole derivatives which are substituted in the 2-position by a substituted morpholin-4-yl moiety, being selective inhibitors of P13 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: October 16, 2007Date of Patent: May 1, 2012Assignee: UCB Pharma S.A.Inventors: Rikki Peter Alexander, Julien Alistair Brown, Karen Viviane Lucile Crépy, Stephen Robert Mack
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Publication number: 20120101100Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 25, 2009Publication date: April 26, 2012Inventors: Shanta Bist, Brian Dangel, Brian Sherer
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Publication number: 20120101101Abstract: Provided are an agent for the treatment and/or prophylaxis of a movement disorder, the agent for the treatment and/or prophylaxis wherein the movement disorder is extrapyramidal syndrome, the agent for the treatment and/or prophylaxis wherein the movement disorder is bradykinesia, gait disturbance, dystonia, dyskinesia or tardive dyskinesia, the agent for the treatment and/or prophylaxis wherein the movement disorder is a side effect of L-DOPA and/or dopamine agonist therapy, and the like, each containing a thiazole derivative represented by the formula (I) wherein R1 represents aryl and the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof as an active ingredient.Type: ApplicationFiled: April 28, 2010Publication date: April 26, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Noriaki Uesaka, Takashi Sawada, Tomoyuki Kanda