Thiadiazoles (including Hydrogenated) Patents (Class 546/268.7)
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Publication number: 20110172276Abstract: A carboxamide compound represented by the formula (I): [wherein Q represents a nitrogen-containing 5-membered heterocyclic group optionally fused with a benzene ring, R1 represents a C1-C3 alkyl group or the like, R2 represents a hydrogen atom or the like, and R3 represents a hydrogen atom.] has an excellent plant disease controlling effect.Type: ApplicationFiled: March 25, 2011Publication date: July 14, 2011Inventors: Sadayuki Arimori, Yoshiharu Kinoshita
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Publication number: 20110152295Abstract: Heteroaromatic compounds of structural formula I are selective inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD1) relative to other known stearoyl-coenzyme A desaturases. The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease, such as atherosclerosis; obesity; diabetes; neurological disease; metabolic syndrome; insulin resistance; and liver steatosis.Type: ApplicationFiled: September 2, 2009Publication date: June 23, 2011Inventors: Jean-Philippe Leclerc, Chun Sing Li, Yeeman K. Ramtohul
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Publication number: 20110130396Abstract: Novel imidazo[2,1-b][1,3,4]thiadiazole derivatives of formula (I) wherein R1 and R2 have the meaning according to claim 1, are inhibitors of TGF-beta receptor I kinase, and can be employed, inter alia, for the treatment of tumors.Type: ApplicationFiled: July 1, 2009Publication date: June 2, 2011Inventors: Guenter Hoelzemann, Hartmut Greiner, Emilie Rossignol, Dominique Swinnen
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Publication number: 20110105447Abstract: Disclosed are novel calcium release-activated calcium (CRAC) channel inhibitors, methods for preparing them, pharmaceutical compositions containing them, and methods of treatment using them. The present disclosure also relates to methods for treating non-small cell lung cancer (NSCLC) with CRAC inhibitors, and to methods for identifying therapeutics for treating and of diagnosing cancer.Type: ApplicationFiled: October 6, 2010Publication date: May 5, 2011Applicants: Incozen Therapeutics Pvt. Ltd., Rhizen Pharmaceuticals SAInventors: Meyyappan Muthuppalaniappan, Srikant Viswanadha, Gayatri S. Merikapudi, Swaroop Kumar V.S. Vakkalanka
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Publication number: 20110104110Abstract: The present invention relates to Substituted Indole Derivatives, compositions comprising at least one Substituted Indole Derivative, and methods of using these Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: May 5, 2011Inventors: Gopinadhan N. Anikumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih
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Publication number: 20110105530Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: ApplicationFiled: June 25, 2009Publication date: May 5, 2011Inventors: Natalie Dales, Zaihui Zhang, Jianmin Fu, Duanjie Hou, Shaoyi Sun, Vishnumurthy Kodumuru, Natalia Pokrovskaia
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Publication number: 20110098287Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to use thereof for controlling animal pests, in particular arthropods and especially insects.Type: ApplicationFiled: June 4, 2009Publication date: April 28, 2011Applicant: Bayer CropScience AGInventors: Thomas Bretschneider, Eva-Maria Franken, Ulrich Görgens, Martin Fusslein, Achim Hense, Joachim Kluth
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Publication number: 20110098273Abstract: The invention provides small molecule drugs that are chemically modified by covalent attachment of a water soluble oligomer. A conjugate of the invention, when administered by any of a number of administration routes, exhibits characteristics that are different from the characteristics of the small molecule drug not attached to the water soluble oligomer.Type: ApplicationFiled: September 3, 2008Publication date: April 28, 2011Applicant: Nektar TherapeuticsInventors: Zhongxu Ren, Bo-Liang Deng, Jennifer Riggs-Sauthier, Micah Harvey
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Patent number: 7915263Abstract: The present invention relates to a compound of formula I: wherein: R1 is a hydrogen atom, F, CN, etc.; R1? is a hydrogen atom or lower alkyl which may be substituted; R2 is O, S, SO, SO2, etc.; R3 is a phenyl which may be substituted; X1, X2, and X3 each independently CH, N, etc. provided, however, that among X1, X2 and X3, the number of nitrogen is 0 or 1; W is the following residue: wherein: W1, W2, and W3 each independently CH, N, etc., or a pharmaceutically acceptable salt or ester thereof.Type: GrantFiled: August 29, 2007Date of Patent: March 29, 2011Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Yoshikazu Iwasawa, Tetsuya Kato, Nobuhiko Kawanishi, Kouta Masutani, Takashi Mita, Katsumasa Nonoshita, Mitsuru Ohkubo
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Patent number: 7910743Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: GrantFiled: May 20, 2009Date of Patent: March 22, 2011Assignee: Cytokinetics, Inc.Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, Jr.
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Publication number: 20110033417Abstract: The present invention relates to 2,3-Substituted Indole Derivatives, compositions comprising at least one 2,3-Substituted Indole Derivative, and methods of using the 2,3-Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: August 27, 2008Publication date: February 10, 2011Inventors: Gopinadhan N. Anilkumar, Frank Bennett, Tin-Yau Chan, Kevin X. Chen, Mousumi Sannigrahi, Francisco Velazquez, Srikanth Venkatraman, Qingbei Zeng, Jose S. Duca, Charles A. Lesburg, Joseph A. Kozlowski, F. George Njoroge, Stuart B. Rosenblum, Neng-Yang Shih, Stephen J. Gavalas, Yueheng Jiang, Patrick A. Pinto, Haiyan Pu, Oleg B. Selyutin, Bancha Vibulbhan, Li Wang, Wanli Wu, Weiying Yang, Yuhua Huang, Hsueh-Cheng Huang, Robert Palermo, Boris Feld
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Publication number: 20110009421Abstract: An object of the present invention is to provide an agent for preventing or treating schizophrenia or the like, wherein the compound of the present invention has GPRS2 agonist activity.Type: ApplicationFiled: February 27, 2009Publication date: January 13, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Masaki Setoh, Toshitake Kobayashi, Toshio Tanaka, Atsuo Baba
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Publication number: 20110003815Abstract: The present invention provides compounds of Formula I which are FLAP inhibitors useful as anti-atherosclerotic, anti-asthmatic, anti-allergic, anti-inflammatory and cytoprotective agents.Type: ApplicationFiled: October 6, 2008Publication date: January 6, 2011Inventors: Anthony Ogawa, Feroze Ujjainwalla, Bing Li, Lin Chu, Minal Patel, Helen M. Armstrong, Hyun O. Ok, Rosemary Sisco, Dwight MacDonald, John Hutchinson, Helene Perrier
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Publication number: 20100331283Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.Type: ApplicationFiled: June 23, 2010Publication date: December 30, 2010Applicant: Array BioPharma Inc.Inventors: Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robisnson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtti
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Publication number: 20100331346Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R2?, R2?, R3, R4, R5, R6, R7 and R8 have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: ApplicationFiled: December 23, 2008Publication date: December 30, 2010Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Stefan Bender, Lars Thore Burgdorf, Ulrich Emde, Norbert Beier, Johannes Gleitz, Christine Charon
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Patent number: 7858647Abstract: The present invention comprises N-[1,3,4]-thiadiazol-2-yl-benzene sulfonamides, their physiologically acceptable salts and functional derivatives that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, And the isomers thereof wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the compounds preparation are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: April 4, 2008Date of Patent: December 28, 2010Assignee: Sanofi-AventisInventors: Stefanie Keil, Hans Matter, Karl Schoenafinger, Matthias Urmann, Maike Glien, Wolfgang Wendler, Hans-Ludwig Schaefer, Eugen Falk
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Publication number: 20100316605Abstract: 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: ApplicationFiled: June 9, 2010Publication date: December 16, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith
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Publication number: 20100317670Abstract: The present invention discloses a compound of formula: where Ar1, Ar2, X, Z1, Z2, R3, and m are as disclosed herein or a pharmaceutically acceptable salt thereof (a “Pyridylene Compound”); compositions comprising an effective amount of a Pyridylene Compound; and methods for treating or preventing pain or other conditions in an animal comprising administering to an animal in need thereof an effective amount of a Pyridylene Compound.Type: ApplicationFiled: July 21, 2010Publication date: December 16, 2010Applicant: PURDUE PHARMA L.P.Inventor: QUN SUN
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Publication number: 20100292227Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: May 11, 2010Publication date: November 18, 2010Applicant: BOEHRINGER INGLEHEIM INTERNATIONAL GMBHInventors: CHRISTIANE YOAKIM, MURRAY BAILEY, FRANCOIS BILODEAU, REBEKAH CARSON, LEE FADER, STEPHEN KAWAI, SEBASTIEN MORIN, CARL THIBEAULT, BRUNO SIMONEAU, SIMON SURPRENANT, YOULA TSANTRIZOS, STEVEN LAPLANTE
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Publication number: 20100286110Abstract: Compounds of formula (I) or pharmaceutically acceptable salts thereof, are agonists of GPR119 and are useful for the treatment of diabetes and as peripheral regulators of satiety, e.g. for the treatment of obesity and metabolic syndrome.Type: ApplicationFiled: October 10, 2008Publication date: November 11, 2010Inventors: Matthew Colin Thor Fyfe, William Gattrell, Colin Peter Sambrook-Smith
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Publication number: 20100260711Abstract: The present invention relates to 3-Aminosulfonyl Substituted Indole Derivatives, compositions comprising at least one 3-Aminosulfonyl Substituted Indole Derivative, and methods of using the 3-Aminosulfonyl Substituted Indole Derivatives for treating or preventing a viral infection or a virus-related disorder in a patient.Type: ApplicationFiled: November 13, 2008Publication date: October 14, 2010Applicant: Schering CorporationInventors: Kevin X. Chen, Stuart B. Rosenblum, F. George Njoroge, Joseph A. Kozlowski
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Publication number: 20100256115Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein X, Y, A, R1, R2, R3, R4, R4?, R5, R5?, R6 and R6? are as described herein.Type: ApplicationFiled: March 18, 2010Publication date: October 7, 2010Inventors: Frederick Cohen, Kurt Deshayes, Wayne J. Fairbrother, Bainian Feng, John A. Flygare, Lewis J. Gazzard, Vickie Hsiao-Wei Tsui
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Publication number: 20100249071Abstract: The invention is directed to Compounds of Formula I: as well as methods of making and using the compounds.Type: ApplicationFiled: March 25, 2010Publication date: September 30, 2010Applicant: Exelixis, Inc.Inventors: Lynne Canne Bannen, Diva Sze-Ming Chan, Morrison B. Mac, Stephanie Ng, John M. Nuss, Yong Wang, Wei Xu
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Patent number: 7795249Abstract: The present invention provides certain pyrazoline compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutical compositions and methods of using the compositions in the treatment of various diseases.Type: GrantFiled: December 19, 2007Date of Patent: September 14, 2010Assignee: Millennium Pharmaceuticals, Inc.Inventors: Ruth S. Adams, Matthew Duffey, Alexandra E. Gould, Paul D. Greenspan, Bheemashankar A. Kulkarni, Tricia J. Vos
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Publication number: 20100204219Abstract: The invention relates to novel compounds of formula (I) wherein X, Y, Z represent independently from one another C or N, n stands for 1, 2, 3, m is 0 or 1, p stands for 0 or an integer from 1 to 6, R1, R2 represent independently from one another hydrogen, a halogen atom, a hydroxyl group, a C1-C3 alkyl group and a C1-C3 alkoxy group, R3 represents, independently from one another if p is not 0, hydrogen, halogen, a C1-C5 linear or branched alkyl, a carboxylyl, a carbomethoxyl, carboethoxyl, a benzyl, an acyl, a hydroxyl, a C1-C4 linear or branched alkoxyl, a trifluoromethyl, a cyano, a morpholino, a 1,3-dioxolyl, an N-acetylamidyl or an amidoyl group, a saturated 5-8 membered ring, a heterocyclic ring, optionally substituted by a C1-C3 alkyl, a hydroxyl or a benzyl group, a C1-C6 alkylsulfonyl, a mono or disubstituted C1-C5 alkyl group, a branched or a cyclic amine, R6 is H or part of a alicyclic, heteroalicyclic ring system, if m is 0 then C represents CF3 or a branched or unbranched C1-C4 alkyl group, if m=1Type: ApplicationFiled: December 11, 2007Publication date: August 12, 2010Inventors: Gabriel Garcia, Pierre Daram, Barbara Froesch, Guy Lemaillet, Leonardo Scapozza
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Patent number: 7772257Abstract: The present invention comprises bicyclic aryl-sulfonic acid [1,3,4]-thiadiazol-2-yl-amides, their functional derivatives thereof as well as their physiologically acceptable salts and pharmaceutical compositions thereof that exhibit peroxisome proliferator activated receptor (PPAR) PPARdelta and PPARgamma agonist activity. The structure of the compounds of the invention are defined by Formula I below, wherein the various substituents are defined herein, including their physiologically acceptable salts. Processes for the preparation of compounds are also disclosed. The compounds are suitable for the treatment of fatty acid metabolism and glucose utilization disorders, disorders relating to insulin resistance are involved as well as demyelinating and other neurodegenerative disorders of the central and peripheral nervous system.Type: GrantFiled: September 24, 2009Date of Patent: August 10, 2010Assignee: Sanofi-AventisInventors: Karl Schoenafinger, Stefanie Keil, Matthias Urmann, Hans Matter, Maike Glien, Wolfgang Wendler
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Publication number: 20100197655Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: January 12, 2010Publication date: August 5, 2010Inventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20100190774Abstract: The present invention provides compounds useful as inhibitors of c-Met tyrosine kinase. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various proliferative disorders.Type: ApplicationFiled: April 8, 2010Publication date: July 29, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: David J. Lauffer, Alexander Aronov, Pan Li, David D. Deininger, Kira McGinty, Dean Stamos, Jon H. Come, Michelle Stewart
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Publication number: 20100179172Abstract: A novel pesticide is provided. The present invention provides a pesticide containing, as an active ingredient, an N-phenyl-methanamine derivative represented by the formula (I) or its salt: wherein R1 is alkyl which may be substituted, etc.; each of R2, R3, R4 and R6 which are independent of one another, is hydrogen, halogen, alkyl which may be substituted, etc.; R5 is haloalkyl or halogen; each of R7 and R8 which are independent of each other, is hydrogen, cyano, alkyl, etc.; R9 is alkyl, cycloalkyl, etc.; m is from 0 to 1 and n is from 0 to 4.Type: ApplicationFiled: June 20, 2008Publication date: July 15, 2010Applicant: Ishihara Sangyo Kaisha , Ltd.Inventors: Masayuki Morita, Kazuhiro Yamamoto, Toshihiko Ueki, Kumiko Azuma, Taku Hamamoto
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Publication number: 20100168005Abstract: The invention relates to pyridin-3-yl derivatives of Formula (I) wherein R1, R2, R3, R4, R5; R6 and A are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: September 6, 2007Publication date: July 1, 2010Applicant: ACTELION PHARMACEUTICALS LTD.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
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Publication number: 20100144756Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 10, 2008Publication date: June 10, 2010Inventors: Christelle Boléa, Sylvain Calanire
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Publication number: 20100099713Abstract: Provided are compounds having the Formula I or salts thereof, wherein R2, L, R3, R11, D2 and R13 are as defined herein, 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: January 16, 2008Publication date: April 22, 2010Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas Daniel Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Publication number: 20100093689Abstract: The present invention provides novel heteroaryl compounds and analogues thereof, which are selective inhibitors of the human P2Y1 receptor. The invention also provides for various pharmaceutical compositions of the same and methods for treating diseases responsive to modulation of P2Y1 receptor activity.Type: ApplicationFiled: November 17, 2009Publication date: April 15, 2010Inventors: James C. Sutton, Zulan Pi, Rejean Ruel, Alexandre L'Heureux, Carl Thibeault, Patrick Y.S. Lam
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Publication number: 20100087417Abstract: The invention relates to novel amino-pyridine derivatives, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: February 29, 2008Publication date: April 8, 2010Inventors: Martin Bolli, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
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Publication number: 20100063108Abstract: The invention relates to pyridine derivatives of Formula (I) wherein A, R1, R2, R3, R4, R5, and R6 are as described in the description, their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents.Type: ApplicationFiled: September 6, 2007Publication date: March 11, 2010Applicant: Actelion Pharmaceuticals Ltd.Inventors: Martin Bolli, David Lehmann, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner, Jorg Velker
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Publication number: 20100063109Abstract: The present invention relates to compounds of the formulae herein, their acceptable salts, solvates, hydrates and polymorphs thereof. The compounds of this invention are useful in treatment of disease, particularly leukemia. The invention also provides compositions comprising a compound of this invention and the use of such compositions in methods of treating disease, disorders, or symptoms thereof in a subject.Type: ApplicationFiled: July 18, 2007Publication date: March 11, 2010Applicant: University of RochesterInventors: Craig Jordan, Monica Guzman
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Publication number: 20100041660Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: October 23, 2009Publication date: February 18, 2010Inventors: MORIHIRO MITSUYA, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20100029625Abstract: A therapeutic and/or prophylactic agent for restenosis, which comprises a thiadiazoline derivative represented by the general formula (0), or a pharmaceutically acceptable salt thereof: [wherein, n represents an integer of 1 to 3, R0 represents aryl, —NR1CONR2 (wherein R1 represents a hydrogen atom or the like, and R2 represents lower alkyl or the like) or the like, R3 represents lower alkyl, R4 represents a hydrogen atom or the like, and R5 represents aryl or the like].Type: ApplicationFiled: June 22, 2006Publication date: February 4, 2010Applicants: KYOWA HAKKO KIRIN CO., LTD., FUJIFILM CORPORATIONInventors: Ryuichiro Nakai, Emi Shimoike, Hideaki Kusaka, Chikara Murakata, Yoshinori Yamashita
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Publication number: 20100029685Abstract: This invention relates to oxadiazolyl and thiadiazolyl derivatives, which are found to be modulators of the nicotinic acetylcholine receptors. Due to their pharmacological profile the compounds of the invention may be useful for the treatment of diseases or disorders as diverse as those related to the cholinergic system of the central nervous system (CNS), the peripheral nervous system (PNS), diseases or disorders related to smooth muscle contraction, endocrine diseases or disorders, diseases or disorders related to neuro-degeneration, diseases or disorders related to inflammation, pain, and withdrawal symptoms caused by the termination of abuse of chemical substances.Type: ApplicationFiled: October 24, 2007Publication date: February 4, 2010Applicant: NeuroSearch A/SInventors: Bjarne H. Dahl, Dan Peters, Gunnar M. Olsen, Daniel B. Timmermann, Susanne Jorgensen
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Publication number: 20100004219Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity, including metabolic and inflammatory or immune associated diseases or disorders having the structure of formula I or an enantiomer, diastereomer, tautomer, or a pharmaceutically-acceptable salt, thereof, wherein: A is a 5-, 6-, or 7-membered heterocyclo or heteroaryl, each containing 1, 2, or 3 heteroatoms selected from N, O, and S and substituted with one to four groups, R1, R2, R3, and/or R4, provided that (i) A is not tetrazole or (ii) if A is thienyl or furanyl then Z is selected from a group other than succinimido or thalimido; M is selected from alkyl, cycloalkyl, aryl, heterocyclo, and heteroaryl; Ma is a linker between C and M and is selected from a bond and C1-C3alkylene; Q is selected from (i) hydrogen, halogen, nitro, cyano, hydroxy, C1-4alkyl, and substituted C1-4 alkyl; or (ii) Q is combined with R6 and with the carbon atoms to whType: ApplicationFiled: October 31, 2007Publication date: January 7, 2010Inventors: Bingwei Vera Yang, Lidia M. Doweyko
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Publication number: 20090325981Abstract: 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 liver X receptors (LXRs).Type: ApplicationFiled: February 11, 2005Publication date: December 31, 2009Applicant: IRM LLCInventors: Valentina Molteni, Xiaolin Li, Juliet Nabakka, David Archer Ellis, Beth Anaclerio, Enrique Saez, John Wityak
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Publication number: 20090324511Abstract: Certain substituted urea derivatives selectively modulate the cardiac sarcomere, for example by potentiating cardiac myosin, and are useful in the treatment of systolic heart failure including congestive heart failure.Type: ApplicationFiled: May 20, 2009Publication date: December 31, 2009Inventors: Bradley P. Morgan, Alex Muci, Erica Kraynack, Pu-Ping Lu, Todd Tochimoto, David J. Morgans, JR.
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Patent number: 7629362Abstract: The present invention relates to a compound which has a glucokinase-activating effect and is useful as a therapeutic agent for diabetes mellitus, being represented by a formula (I): [wherein X1 represents a nitrogen atom, sulfur atom, oxygen atom or the like; R1 represents a 6- to 10-membered aryl group, 5- to 7-membered heteroaryl group or the like; D represents an oxygen atom or sulfur atom; R2 and R3 are the same or different, each representing a hydrogen atom, lower alkyl group or the like; a formula (II) represents an optionally substituted 5- to 7-membered heteroaryl group or the like; a formula (III) represents a monocyclic or bicyclic heteroaryl group] or a pharmaceutically acceptable salt thereof.Type: GrantFiled: February 13, 2004Date of Patent: December 8, 2009Assignee: Banyu Pharmaceutical Co., Ltd.Inventors: Morihiro Mitsuya, Makoto Bamba, Fumiko Sakai, Hitomi Watanabe, Yasuhiro Sasaki, Teruyuki Nishimura, Jun-ichi Eiki
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Publication number: 20090298836Abstract: The invention relates to thiazole compounds of Formula I and Formula II and compositions thereof useful for treating diseases mediated by protein kinase B (PKB) where the variables have the definitions provided herein. The invention also relates to the therapeutic use of such thiazole compounds and compositions thereof in treating disease states associated with abnormal cell growth, cancer, inflammation, and metabolic disorders.Type: ApplicationFiled: July 15, 2008Publication date: December 3, 2009Applicant: Amgen Inc.Inventors: Qingping Zeng, Chester Chenguang Yuan, Guomin Yao, Xianghong Wang, Seifu Tadesse, Andreas Reichelt, Qingyian Liu, Matthew R. Lee, Xin Huang, Fang-Tsao Hong, Nianhe Han, Christopher H. Fotsch, Celia Dominguez, Matthew P. Bourbeau, John G. Allen
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Publication number: 20090298885Abstract: The present invention relates to methylene urea derivatives of formula (I), the use of the compounds of formula (I) as inhibitors of raf-kinase, the use of the compounds of formula (I) for the manufacture of a pharmaceutical composition and a method of treatment, comprising administering said pharmaceutical composition to a patient.Type: ApplicationFiled: June 19, 2009Publication date: December 3, 2009Applicant: Merck Patent GmbHInventors: Hans-Peter Buchstaller, Matthias Wiesner, Oliver Schadt, Christiane Amendt, Frank Zenke, Christian Sirrenberg, Matthias Grell, Dirk Finsinger
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Publication number: 20090247526Abstract: Provided are compounds of formula I wherein R2, L, Z, Y, G and R1 are as defined herein, that are useful in the treatment and/or prevention of diseases or disorders mediated by deficient levels of glucokinase activity or which can be treated by activating glucokinase including, but not limited to, diabetes mellitus, impaired glucose tolerance, IFG (impaired fasting glucose) and IFG (impaired fasting glycemia), as well as other diseases and disorders such as those discussed herein.Type: ApplicationFiled: January 24, 2007Publication date: October 1, 2009Applicant: ARRAY BIOPHARMA INC.Inventors: Thomas D. Aicher, Steven Armen Boyd, Mark Joseph Chicarelli, Kevin Ronald Condroski, Rustam Ferdinand Garrey, Ronald Jay Hinklin, Ajay Singh, Timothy M. Turner
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Patent number: 7585880Abstract: The present invention provides a novel compound having a GPR40 receptor function modulating action, which is useful as an insulin secretagogue, a drug for the prophylaxis or treatment of diabetes and the like. A compound represented by the formula (I) wherein each symbol is as defined in the specification, a salt thereof and a prodrug thereof have unexpectedly superior GPR40 receptor agonist activity and also show superior properties as a pharmaceutical product, such as stability and the like. Thus, they can be safe and useful drugs for the prophylaxis or treatment of GPR40 receptor related conditions or diseases in mammals.Type: GrantFiled: December 24, 2004Date of Patent: September 8, 2009Assignee: Takeda Pharmaceutical Company LimitedInventors: Tsuneo Yasuma, Shinobu Sasaki, Nozomu Sakai
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Publication number: 20090221587Abstract: Compounds of formula (I), wherein the substituents are as defined in claim (1), and the agrochemically acceptable salts and all stereoisomers and tautomeric forms of the compounds of formula (I) can be used as agrochemical active ingredients and can be prepared in a manner known per se.Type: ApplicationFiled: August 14, 2006Publication date: September 3, 2009Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Andre Jeanguenat, Roger Graham Hall, Olivier Loiseleur, Stephan Trah, Patricia Durieux, Andrew Edmunds, Andrew Edmunds, Andre Stoller
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Patent number: 7582366Abstract: A difluoropyridine-based compound includes at least one difluoropyridine group in its molecule. The difluoropyridine-based compound may be used as an electron injection material, an electron transport material, or a hole blocking material in full-color fluorescent or phosphorescent devices. The difluoropyridine-based compound has good electrical characteristics and a high charge transport capability. The difluoropyridine-based compound may be used to produce an organic electroluminescent device with high efficiency, low voltage, improved brightness, and a long life expectancy.Type: GrantFiled: March 16, 2006Date of Patent: September 1, 2009Assignee: Samsung Mobile Display Co., Ltd.Inventors: Seok-Hwan Hwang, Young-Kook Kim, Chang-Ho Lee, Seok-Jong Lee, Seung-Gak Yang, Hee-Yeon Kim, Jung-Han Shin
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Publication number: 20090192196Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 6-membered heterocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: July 12, 2007Publication date: July 30, 2009Inventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal