Ring Sulfur Or Ring Oxygen In The Additional Hetero Ring Patents (Class 546/209)
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Publication number: 20130274254Abstract: The present application provides for a compound of formula I, and related compounds, 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 that include the administration of such compounds with at least one additional therapeutic agent.Type: ApplicationFiled: December 20, 2011Publication date: October 17, 2013Applicant: Gilead Sciences, Inc.Inventors: Carina Cannizzaro, Manoj C. Desai, Hon Chung Hui, Melody S. Lee, Hongtao Liu, Jianyu Sun, Lianhong Xu
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Publication number: 20130274292Abstract: Ketoheteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols A, L1, G, X, Y, T and R1 have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: ApplicationFiled: March 13, 2013Publication date: October 17, 2013Inventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Thomas Seitz, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Ulrike Wachendorff-Neumann
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Patent number: 8557821Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity, as well as methods of using the compounds of formula (I) to control microbes.Type: GrantFiled: August 5, 2010Date of Patent: October 15, 2013Assignee: Syngenta Crop Protection, LLCInventors: Sarah Sulzer-Mosse, Clemens Lamberth, Mathias Stephan Respondek, Laura Quaranta
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Patent number: 8557824Abstract: Compounds of the formula (I), in which R1, R2, R3, R4, K, G, E and WType: GrantFiled: September 19, 2008Date of Patent: October 15, 2013Assignee: Merck Patent GmbHInventors: Kai Schiemann, Melanie Schultz, Andree Blaukat, Ingo Kober, Wolfgang Staehle
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Publication number: 20130261155Abstract: The present invention relates to fungicidal 1-(heterocyclic carbonyl) piperidines and their thiocarbonyl derivatives, their process of preparation and intermediate compounds for their preparation, their use as fungicides, particularly in the form of fungicidal compositions and methods for the control of phytopathogenic fungi of plants using these compounds or their compositions.Type: ApplicationFiled: October 20, 2011Publication date: October 3, 2013Inventors: Jurgen Benting, Peter Dahmen, Philippe Desbordes, Stephanie Gary, Jean-Pierre Vors, Ulrike Wachendorff-Neumann
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Publication number: 20130261154Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, J, Z, and Q are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 12, 2011Publication date: October 3, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Mary Ann Hanagan, Gilles Seburyamo
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Patent number: 8546375Abstract: Disclosed herein are azetidinyl compounds of formula I, as described herein, pharmaceutical compositions comprising an azetidinyl compound, and a method of using an azetidinyl compound in the treatment or prophylaxis of a melanin-concentrating hormone related disease or condition.Type: GrantFiled: July 5, 2011Date of Patent: October 1, 2013Assignee: AstraZeneca ABInventors: Susanne Doris Margit Bökman-Winiwarter, Marlene Fredenwall, Carl Anders Hogner, Lars Anders Mikael Johansson, Robert Andrew Judkins, Lanna Li, Björn Christian Ingvar Löfberg, Sverker Von Unge
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Patent number: 8546588Abstract: This invention provides compounds of formula (I): wherein X1, X2, X3, R2, R4b, R1, and G have values as described in the specification, useful as inhibitors of HDAC6. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of proliferative, inflammatory, infectious, neurological or cardiovascular diseases or disorders.Type: GrantFiled: February 25, 2011Date of Patent: October 1, 2013Assignee: Millennium Pharmaceuticals, Inc.Inventors: Christopher Blackburn, Kenneth M. Gigstad, He Xu
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Patent number: 8546583Abstract: The present invention relates to compounds of formula (I), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1, R2, R3, R4, and L1 are defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions. The present invention also relates to compounds of formula (II), or pharmaceutical salts, prodrugs, salts of prodrugs, or combinations thereof, wherein R1a, R2a and (Rx)n are as defined in the specification, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: May 30, 2007Date of Patent: October 1, 2013Assignee: AbbVie Inc.Inventors: Alan S. Florjancic, Michael J. Dart, Keith B. Ryther, Arturo Perez-Medrano, William A. Carroll, Meena V. Patel, Karin Rosemarie Tietje, Tongmei Li, Teodozyj Kolasa, Megan E. Gallagher, Sridhar Peddi, Jennifer M. Frost, Derek W. Nelson
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Patent number: 8541592Abstract: The present invention relates to thiazolinones and also to pharmaceutical compositions comprising the compounds, as well as methods of use of the compounds for treatment of disorders associated with human 11-?-hydroxysteroid dehydrogenase type 1 enzyme and for the preparation of a medicament which acts on the human 11-?-hydroxysteroid dehydrogenase type 1 enzyme.Type: GrantFiled: November 13, 2006Date of Patent: September 24, 2013Assignees: Amgen Inc., Biovitrum ABInventors: Martin Henriksson, Evert Homan, Lars Johansson, Jerk Vallgarda, Meredith Williams, Eric A. Bercot, Christopher H. Fotsch, Aiwen Li, Guolin Cai, Randall W. Hungate, Chester Chenguang Yuan, Christopher Tegley, David J. St. Jean, Jr., Nianhe Han, Qi Huang, Qingyian Liu, Michael D. Bartberger, George A. Moniz, Matthew J. Frizzle, Teresa L. Marshall
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Publication number: 20130244998Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds, and enantiomers, diastereomers, and pharmaceutically acceptable salts thereof, are represented by Formula (I) as follows: wherein Y, Z, and R are defined herein.Type: ApplicationFiled: May 2, 2013Publication date: September 19, 2013Applicant: Janssen Pharmaceutica, NVInventors: Peter J. Connolly, Haiyan Bian, Xun Li, Li Liu, Mark J. Macielag, Mark E. McDonnell
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Publication number: 20130231326Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: ApplicationFiled: January 14, 2013Publication date: September 5, 2013Applicant: RECEPTOS, INC.Inventors: Esther Martinborough, Marcus F. Boehm, Adam Richard Yeager, Junko Tamiya, Liming Huang, Enugurthi Brahmachary, Manisha Moorjani, Gregg Alan Timony, Jennifer L. Brooks, Robert Peach, Fiona Lorraine Scott, Michael Allen Hanson
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Publication number: 20130231340Abstract: The invention provides a method of inhibiting a TYK2 kinase, which method comprises bringing into contact with the TYK2 kinase an effective TYK2 kinase-inhibiting amount of a compound having the formula (0): or a salt or stereoisomer thereof. The invention also provides a novel subset of compounds within formula (0) as well as pharmaceutical compositions containing them and their use in medicine.Type: ApplicationFiled: March 1, 2013Publication date: September 5, 2013Applicant: SAREUM LIMITEDInventor: John Charles READER
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Publication number: 20130231321Abstract: The present invention provides 2-substituted-ethynylthiazole derivatives of formula (I): wherein R1, R2 and X are as defined herein, or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and methods of using same.Type: ApplicationFiled: April 16, 2013Publication date: September 5, 2013Applicant: H. LUNDBECK A/SInventors: Mathivanan Packiarajan, Allen Hopper, Anette Graven Sams, Gitte Kobberoee Mikkelsen, Michel Grenon
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Patent number: 8524743Abstract: Bis(difluoromethyl)pyrazole derivatives of the formula (I) in which the symbols R1, X and G are each as defined in the description, and agrochemically active salts, metal complexes and N-oxides thereof, and use thereof for controlling phytopathogenic harmful fungi, and also processes for preparing compounds of the formula (I).Type: GrantFiled: December 21, 2010Date of Patent: September 3, 2013Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Sebastian Hoffmann, Joachim Kluth, Tomoki Tsuchiya, Pierre Wasnaire, Jürgen Benting, Daniela Portz, Ulrike Wachendorff-Neumann
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Publication number: 20130217663Abstract: An object of the present invention is to provide a compound having a modulating activity at an S1P receptor which is useful for preventing and treating autoimmune diseases, allergic diseases, and the like. According to the present invention, a compound represented by formula (I) or a pharmaceutically acceptable salt thereof is provided.Type: ApplicationFiled: December 21, 2012Publication date: August 22, 2013Applicant: MEIJI SEIKA PHARMA CO., LTD.Inventor: MEIJI SEIKA PHARMA CO., LTD.
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Publication number: 20130217690Abstract: [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 O 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: March 15, 2013Publication date: August 22, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: Mochida Pharmaceutical Co., Ltd.
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Publication number: 20130217665Abstract: The invention relates to a compound of formula (I) wherein A1 to A3 and R1 to R3 are defined as in the description and in the claims. The compound of formula (I) can be used as a medicament.Type: ApplicationFiled: February 14, 2013Publication date: August 22, 2013Applicant: HOFFMANN-LA ROCHE INC.Inventor: HOFFMANN-LA ROCHE INC.
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Publication number: 20130203729Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1-R5 and n are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: August 9, 2012Publication date: August 8, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Todd BOSANAC, Angela BERRY, John David GINN, Tamara Denise HOPKINS, Sabine SCHLYER, Fariba SOLEYMANZADEH, John WESTBROOK, Maolin YU, Zhonghua ZHANG
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Patent number: 8501794Abstract: The present application relates to isothiazolylidene containing compounds of Formula (I) wherein R1, R2, R3, R4, and L are as defined in the specification, compositions comprising such compounds, and methods for treating conditions and disorders using such compounds and compositions.Type: GrantFiled: November 4, 2009Date of Patent: August 6, 2013Assignee: AbbVie Inc.Inventors: William A. Carroll, Michael J. Dart, Teodozyj Kolasa, Tongmei Li, Derek W. Nelson, Meena V. Patel, Sridhar Peddi, Arturo Perez-Medrano, Xueqing Wang
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Patent number: 8501781Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I), in which the symbols have the meanings given in the description and agrochemically active salts thereof and their use for controlling phytopathogenic harmful fungi and also processes for preparing compounds of the formula (I).Type: GrantFiled: October 27, 2010Date of Patent: August 6, 2013Assignee: Bayer Cropscience AGInventors: Pierre Cristau, Nicola Rahn, Tomoki Tsuchiya, Joachim Kluth, Pierre Wasnaire, Sebastian Hoffmann, Jürgen Benting, Ulrike Wachendorff-Neumann, Thomas Seitz
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Publication number: 20130196996Abstract: One embodiment provides a method, comprising treating or preventing at least one disease selected from the group consisting of bladder cancer, weight loss accompanying bladder cancer, bone pain accompanying bladder cancer, bladder cancer carcinoma in-situ (CIS), TA stage bladder cancer, T1 stage bladder cancer, T2 stage bladder cancer, T3 stage bladder cancer, T4 stage bladder cancer, lymph node metastasis therefrom, solid organ metastasis therefrom, bony metastasis therefrom, cachexia/anorexia associated with bladder cancer, generalized wasting syndrome associated with bladder cancer, or a combination thereof, by administering to a subject in need thereof one or more compounds described herein, prodrug thereof, salt thereof, or a combination thereof.Type: ApplicationFiled: January 19, 2011Publication date: August 1, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: John Arthur Taylor, III, Thais Sielecki-Dzurdz
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Publication number: 20130196966Abstract: Compounds that selectively modulate the sphingosine 1 phosphate receptor are provided including compounds which modulate subtype 1 of the S1P receptor. Methods of chiral synthesis of such compounds are provided. Uses, methods of treatment or prevention and methods of preparing inventive compositions including inventive compounds are provided in connection with the treatment or prevention of diseases, malconditions, and disorders for which modulation of the sphingosine 1 phosphate receptor is medically indicated.Type: ApplicationFiled: January 14, 2013Publication date: August 1, 2013Applicant: RECEPTOS, INC.Inventor: RECEPTOS, INC.
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Publication number: 20130196964Abstract: The present application relates to novel aryl compounds with heterocyclic substituents, 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: August 1, 2013Applicant: 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: 20130184249Abstract: The present invention relates to compounds of formula wherein R1, R2, R3, R4, Z, and n are as defined herein or to a pharmaceutically active salt thereof. Compounds of the invention are high potential NK-3 receptor antagonists for the treatment of depression, pain, psychosis, Parkinson's disease, schizophrenia, anxiety and attention deficit hyperactivity disorder (ADHD).Type: ApplicationFiled: February 28, 2013Publication date: July 18, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130184258Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium 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.Type: ApplicationFiled: October 26, 2012Publication date: July 18, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventor: Vertex Pharmaceuticals Incorporated
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Publication number: 20130184284Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu, Scott A. Bolton, Laxman Pasunoori, Sunil Kumar Mandal, Philip M. Sher
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Publication number: 20130184262Abstract: The present invention provides compounds of Formula (I): or a stereoisomer, or a pharmaceutically acceptable salt thereof, wherein all of the variables are as defined herein. These compounds are agonists, partial agonists and modulators of the NPY Y4 receptor and may be used for the treatment and prophylaxis of various diseases and conditions.Type: ApplicationFiled: July 16, 2012Publication date: July 18, 2013Inventors: William R. Ewing, Yeheng Zhu, Chongqing Sun, Yanting Huang, Maheswaran Sivasamban Karatholuvhu
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Publication number: 20130184257Abstract: Compounds of Formula (I) and pharmaceutically acceptable salts thereof in which X1, X2, L, R3, R4, R5, R7 and n have the meanings given in the specification, are modulators of GPR119 and are useful in the treatment or prevention of diseases such as such as, but not limited to, type 2 diabetes, diabetic complications, symptoms of diabetes, metabolic syndrome, obesity, dyslipidemia, and related conditions.Type: ApplicationFiled: September 15, 2011Publication date: July 18, 2013Inventors: Thomas Daniel Aicher, Josef R. Bencsik, Steven Armen Boyd, Kevin Ronald Condroski, Jay Bradford Fell, John P. Fischer, Ronald Jay Hinklin, Scott Alan Pratt
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Publication number: 20130178420Abstract: The invention relates to compounds that modulate the glucagon-like peptide 1 (GLP-1) receptor, methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds are act as modulators or potentiators of GLP-1 receptor on their own, or with receptor ligands including GLP-1 peptides GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.Type: ApplicationFiled: December 12, 2012Publication date: July 11, 2013Applicant: RECEPTOS, INC.Inventor: RECEPTOS, INC.
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Publication number: 20130177844Abstract: The present invention provides a positive-charge control agent containing, as an active substance(s), one or two or more rhodanine compounds represented by the following formula (1). wherein R1 represents a hydrogen atom, etc.; R2 represents a hydrogen atom, etc.; and R3 to R7, which may be identical to or different from each other, represent a hydrogen atom, a cyano group, a trifluoromethyl group, a nitro group, etc. R2 to R7 may be joined to each other to form a ring. V, W, X, Y and Z represent a carbon atom or a nitrogen atom and 0 to 3 of V, W, X, Y and Z are nitrogen atoms, with the proviso that at least one of R3 to R7 is a linear or branched alkyl group having 1 to 4 carbon atoms substituted with three or more fluorine atoms etc.Type: ApplicationFiled: November 22, 2011Publication date: July 11, 2013Applicant: HODOGAYA CHEMICAL CO., LTD.Inventors: Masateru Yasumura, Masami Ito, Ikuo Kimura, Masaya Tojo, Kanae Hiraishi, Masaki Okubo
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Publication number: 20130178505Abstract: Compositions and methods for inhibiting translation are provided. Compositions, methods and kits for treating (1) cellular proliferative disorders, (2) non-proliferative, degenerative disorders, (3) viral infections, (4) disorders associated with viral infections, and/or (5) non-proliferative metabolic disorders such as type II diabetes where inhibition of translation initiation is beneficial using the compounds disclosed herein.Type: ApplicationFiled: June 28, 2011Publication date: July 11, 2013Applicant: PRESIDENT AND FELLOWS OF HARVARD COLLEGEInventors: Michael Chorev, Bertal Huseyin Aktas, Jose A. Halperin, Gerhard Wagner
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Patent number: 8481564Abstract: The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, prostate cancer, lung cancer, colon cancer, stomach cancer, hairy cell leukemia; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including rheumatoid arthritis, and other forms of inflammatory arthritis, osteoarthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.Type: GrantFiled: April 6, 2011Date of Patent: July 9, 2013Assignee: Janssen Pharmaceutica, N.V.Inventors: Carl R. Illig, Shelley K. Ballentine, Jinsheng Chen, Renee Louise DesJarlais, Sanath K. Meegalla, Mark Wall, Kenneth Wilson
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Patent number: 8481574Abstract: The present invention relates to compounds of formula (I) wherein A, E, L2, R1, R3, R4 and R5 are as defined in the herein, compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and compositions.Type: GrantFiled: October 12, 2007Date of Patent: July 9, 2013Assignee: Abbott LaboratoriesInventors: Michael D. Meyer, Michael J. Dart, William A. Carroll, Meena V. Patel, Tedozyi Kolasa, Xueqing Wang
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Publication number: 20130172311Abstract: The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly 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 effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: ApplicationFiled: May 3, 2011Publication date: July 4, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Härter, Hartmut Beck, Susanne Greschat-Schade, Peter Ellinghaus, Kerstin Unterschemmann, Joachim Schuhmacher
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Publication number: 20130172553Abstract: Processes for the chiral syntheses of isoxazolines and intermediates are described. Compounds prepared thereby, and methods of using the compounds are also described.Type: ApplicationFiled: November 26, 2010Publication date: July 4, 2013Applicant: CPSI STOCKHOLDER TRUSTInventors: Thais Sielecki-Dzurdz, James Pruitt
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Patent number: 8476287Abstract: [Problem] To provide a GPR40 activating agent having, as an active ingredient, a novel compound having a GPR40 agonist action, a salt of the compound, a solvate of the salt or the compound, 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 n is 0 to 2; p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is an aryl group which is optionally substituted with L or a heterocyclic group which is optionally substituted with L; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is O, S, —NR7—; and R1 to R7 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: December 24, 2010Date of Patent: July 2, 2013Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Publication number: 20130165450Abstract: This invention relates to certain thiazole carboxamide derivatives of Formula (I) as inhibitors of 3-phosphoinositide-dependent protein kinase (PDK-1). The compounds can be useful in inhibiting the proliferation of cancer cells, and other aberrant conditions where the PDK-1 signaling pathway is overstimulated.Type: ApplicationFiled: September 9, 2011Publication date: June 27, 2013Inventors: Hon-Chung Tsui, Sunil Paliwal, Thierry Oliver Fischmann
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Publication number: 20130165422Abstract: The disclosure relates to hexafluoroisopropyl carbamate derivatives of general formula (I): in which: R, Z, A, m, and n are as defined in the disclosure; in the form of the base or of an addition salt with an acid, and to the preparation process and therapeutic application thereof.Type: ApplicationFiled: November 29, 2012Publication date: June 27, 2013Applicant: SANOFIInventor: SANOFI
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Publication number: 20130165438Abstract: The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro Urade, Makoto Kitade, Keiko Yamane, Shinichi Aoki, Hiroyoshi Yamanaka
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Publication number: 20130165444Abstract: Piperidine derivatives of which the following is exemplary and their use in the treatment of obesity, diabetes or dyslipidemia.Type: ApplicationFiled: December 14, 2012Publication date: June 27, 2013Inventors: Gerald Juergen ROTH, Martin FLECK, Bernd NOSSE, Thorsten LEHMANN-LINTZ
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Patent number: 8470811Abstract: The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly 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 effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.Type: GrantFiled: May 9, 2011Date of Patent: June 25, 2013Assignee: Bayer Intellectual Property GmbHInventors: Michael Härter, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Kerstin Berhörster, Joachim Schuhmacher
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Publication number: 20130158075Abstract: The present invention relates to heterocyclic compounds of formula 1, in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, solvates, polymorphs, prodrugs, carboxylic acid isosteres and N-oxides. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: August 31, 2011Publication date: June 20, 2013Applicant: PIRAMAL ENTERPRISES LIMITEDInventors: Rajiv Sharma, Kishorkumar Shivajirao Kadam, Ravindra Dnyandev Jadhav, Shivaji Sadashiv Kandre, Amol Gupte
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Publication number: 20130158001Abstract: Disclosed are compounds of Formula (I): (I) or stereoisomers, salts, or prodrugs thereof, wherein: (i) R1 and R2 are independently C1-C4 alkyl, or (ii) R1 and R2 together with the carbon atom to which they are attached, form a cyclic group; and Q is H, C1-6alkyl, phenyl or 5- to 6-membered heteroaryl substituted with zero to 3 substituents, and G is defined herein. Also disclosed are method of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. There compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as autoimmune diseases and chronic inflammatory disease.Type: ApplicationFiled: July 20, 2011Publication date: June 20, 2013Inventors: Jagabandhu Das, Soo S. Koo, Anurag S. Srivastava, Robert V. Moquin
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Publication number: 20130150341Abstract: This invention relates to compounds of formula I their use as positive allosteric modulators of mGlu5 receptor activity, pharmaceutical compositions containing the same, and methods of using the same as agents for treatment and/or prevention of neurological and psychiatric disorders associated with glutamate dysfunction such as schizophrenia or cognitive decline such as dementia or cognitive impairment. A, B, X, R1, R2, R3 have meanings given in the description.Type: ApplicationFiled: December 3, 2012Publication date: June 13, 2013Inventors: Matthias GRAUERT, Daniel BISCHOFF, Georg DAHMANN, Raimund KUELZER, Klaus RUDOLF, Bernd WELLENZOHN
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Publication number: 20130150366Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use in the treatment of bacterial infections are also described.Type: ApplicationFiled: February 5, 2013Publication date: June 13, 2013Applicant: ASTRAZENECA, INTELLECTUAL PROPERTYInventor: AstraZeneca, Intellectual Property
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Publication number: 20130143892Abstract: The present invention relates to compounds of general formula I, wherein R1, LP, HetAr, Ar, and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR119 receptor and modulate its activity.Type: ApplicationFiled: June 6, 2012Publication date: June 6, 2013Applicants: NEUROCRINE BIOSCIENCES, INC., BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Armin HECKEL, Frank HIMMELSBACH, Elke LANGKOPF, Bernd NOSSE, Neil J. ASHWEEK, Nicole HARRIOTT
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Patent number: 8455521Abstract: Diaminoalkanes of below Formula I have now been found which are orally active and bind to aspartic proteases to inhibit their activity: They are useful in the treatment or amelioration of diseases associated with elevated levels of aspartic protease activity. The invention also relates to a method for the use of the compounds of Formula I in ameliorating or treating aspartic protease related disorders in a subject in need thereof comprising administering to said subject an effective amount of a compound of Formula I.Type: GrantFiled: May 28, 2010Date of Patent: June 4, 2013Assignee: Vitae Pharmaceuticals, Inc.Inventors: John J. Baldwin, David A. Claremon, Colin M. Tice, Salvacion Cacatian, Lawrence W. Dillard, Alexey V. Ishchenko, Jing Yuan, Zhenrong Xu, Gerard McGeehan, Wei Zhao, Robert D. Simpson, Suresh B. Singh, Patrick T. Flaherty, Jean-Pierre Wery
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Patent number: 8455520Abstract: Compounds of the Formula: (I) as well as pharmaceutically acceptable salts and hydrates thereof, that are useful for treating hypertension, diabetes, inflammation, atherosclerosis, pain, and the like are disclosed. Pharmaceutical compositions and methods of use are also included.Type: GrantFiled: July 11, 2008Date of Patent: June 4, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Steven L. Colletti, Hong Shen, Fa-Xiang Ding
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Patent number: 8450323Abstract: Disclosed are compounds of the following formula: in which R1, R2, R6, R7, R12, X, and q are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: GrantFiled: January 18, 2012Date of Patent: May 28, 2013Assignee: Takeda Pharmaceutical Company LimitedInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov