1,2-thiazoles (including Hydrogenated) Patents (Class 546/271.1)
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Patent number: 8975235Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: GrantFiled: August 14, 2012Date of Patent: March 10, 2015Assignee: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8937083Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: GrantFiled: October 24, 2012Date of Patent: January 20, 2015Assignee: DowAgroSciences, LLCInventors: Noormohamed M. Niyaz, Negar Garizi, Yu Zhang, Tony K. Trullinger, Ricky Hunter, Ann M. Buysse, Asako Kubota, Paul Renee LePlae, Jr., Daniel Knueppel, Christian T. Lowe, Dan Pernich, David A. Demeter, Timothy C. Johnson
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Publication number: 20150005165Abstract: The invention relates to a carboxylic acid derivatives of benzoheterocyclyl pyridines and benzoheterocyclyl pyrimidines of general formula (I) and to the use thereof as herbicides.Type: ApplicationFiled: July 24, 2012Publication date: January 1, 2015Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Michael Gerhard Hoffmann, Marco Bruenjes, Uwe Doeller, Hans-Joerg Dietrich, Isolde Haeuser-Hahn, Christopher Hugh Rosinger, Elmar Gatzweiler, Ines Heinemann
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Publication number: 20140378415Abstract: The present invention provides compounds of formula (I) wherein P is P0, heterocyclyl or heterocyclyl substituted by one to five Z formula (II); Y1, Y2, Y3 and Y4 are independently of each other C—H, C—R5, or nitrogen; G1 is oxygen or sulfur; X4 is C1-C8 haloalkyl; R4 is aryl or aryl substituted by one to five R9, or heteroaryl or heteroaryl substituted by one to five R9; and R1, R2, R4, R5, R9 and Z are as defined in the claims. The invention also provides compositions comprising the compounds of formula (I), intermediates useful in the preparation of compounds of formula (I) and methods of using the compounds of formula (I) to control insects, acarines, nematodes or molluscs.Type: ApplicationFiled: August 27, 2012Publication date: December 25, 2014Applicant: SYNGENTA PARTICIPATIONS AGInventors: Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20140275179Abstract: Disclosed are compounds, compositions and methods for treating of disorders that are affected by the modulation of the GPR120 receptor. Such compounds are represented by Formula (I) and Formula (II) as follows: wherein Y, R1, G, and Q are defined herein; and wherein R11, R21, R41, RB1 and G1, are defined herein.Type: ApplicationFiled: March 7, 2014Publication date: September 18, 2014Applicant: Janssen Pharmaceutica NVInventors: Zhihua Sui, Chaozhong Cai, Xuqing Zhang
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Publication number: 20140256745Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: October 19, 2012Publication date: September 11, 2014Applicant: CalciMedica, Inc.Inventors: Jianguo Cao, Jeffrey P. Whitten, Zhijun Wang, Evan Rogers, Jonathan Grey
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Patent number: 8809378Abstract: The instant invention describes compounds having metalloenzyme modulating activity, and methods of treating diseases, disorders or symptoms thereof mediated by such metalloenzymes.Type: GrantFiled: June 19, 2012Date of Patent: August 19, 2014Assignee: Viamet Pharmaceuticals, Inc.Inventors: William J. Hoekstra, Stephen W. Rafferty, Christopher M. Yates, Robert J. Schotzinger, Michael R. Loso, Michael T. Sullenberger, Gary D. Gustafson
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Patent number: 8765752Abstract: [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: GrantFiled: March 15, 2013Date of Patent: July 1, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Publication number: 20140162998Abstract: A Pim kinase inhibitor compound having the structure represented by Formula I, and isomers, diastereomers, enantiomers, tautomers, and pharmaceutically acceptable salts thereof. The compounds significantly inhibit Pim kinase activity and can be used to prepare drugs for treating Pim kinase mediated diseases, such as cancers, autoimmune diseases, allergic reactions, or organ transplant rejection. Also provided are methods for preparing the compounds represented by Formula I.Type: ApplicationFiled: February 10, 2014Publication date: June 12, 2014Applicant: Jikai Biosciences, Inc.Inventor: Yu GE
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Publication number: 20140135215Abstract: A compound of the formula I where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as pesticidal agents.Type: ApplicationFiled: December 17, 2013Publication date: May 15, 2014Applicant: Syngenta Crop Protection LLCInventors: Ottmar Franz HUETER, Peter RENOLD, Werner ZAMBACH, Thomas PITTERNA, Peter MAIENFISCH
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Publication number: 20140113931Abstract: Provided are picolinamide compounds for inhibiting of Syk kinase, intermediates used in making such compounds, methods for their preparation, pharmaceutical compositions thereof, methods for inhibiting Syk kinase activity, and methods for treating conditions mediated at least in part by Syk kinase activity.Type: ApplicationFiled: March 15, 2013Publication date: April 24, 2014Applicant: Portola Pharmaceuticals, Inc.Inventor: Portola Pharmaceuticals, Inc.
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Publication number: 20140057871Abstract: [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 secretagogues and a prophylactic and/or therapeutic agent against diabetes, obesity, or the like. [Means of solving the problem] A compound of Formula (III): (where f is 0 to 2; g is 1 to 4; j is 0 to 3; k is 0 to 2; n is 0 to 2; p is 0 to 4; h is 0 to 3; q1 id 0 to 3; q2 is 0 or 1; r1 is 0 to 2 (with the proviso that q1+q2+r1 is 0 to 5); J1a is —CR11a—, N; J2 is —CR12aR12b—, —CR12c—; T is —CH2—, O, —S(O)i— (i is an integer of 0 to 2) or —NR7—; X is O, S, or —NR7—; ring A?? is a benzene ring, a pyridine ring; ring B? is a benzene ring, a pyridine ring, a pyrimidine ring; and R1 to R14 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: April 11, 2012Publication date: February 27, 2014Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventors: Akihiro Okano, Munetaka Ohkouchi, Muneyoshi Makabe
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Patent number: 8653259Abstract: The invention provides the process illustrated in scheme 1 for synthesizing heterocyclic compounds of formula I. In the process, an isothiocyanate of formula II is initially reacted with a primary amine or formula III to give a thiourea of formula IV. Subsequently, the thiourea of formula IV is converted to the corresponding heterocycle of formula I using a base and a sulfonyl chloride.Type: GrantFiled: February 6, 2008Date of Patent: February 18, 2014Assignee: Sanofi-Aventis Deutschland GmbHInventors: Uwe Heinelt, Hans-Jochen Lang
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Publication number: 20140038936Abstract: 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: May 7, 2013Publication date: February 6, 2014Inventors: Alex Aronov, Jon H. Come, Robert J. Davies, Albert Charles Pierce, Philip N. Collier, Ronald Lee Grey, Hardwin O'Dowd, James A. Henderson, Elaine B. Krueger, Anne-Laure Grillot, Arnaud Le Tiran, Yusheng Liao, David Messersmith, Jian Wang, Jingrong Cao, Upul Keerthi Bandarage, Suganthini S. Nanthakumar
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Patent number: 8629102Abstract: [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: GrantFiled: March 15, 2013Date of Patent: January 14, 2014Assignee: Mochida Pharmaceutical Co., Ltd.Inventor: Munetaka Ohkouchi
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Patent number: 8629284Abstract: A compound of the formula I or where W, X and Y are for example each CH; R1 is H; R2 is halogen; and R6 is, for formula I, for example, OH, CN, C3-C8-cycloalkyl, C3-C8-cycloalkyl-C1-C6-alkyl, C2-C6-alkenyl, C2-C6-haloalkenyl, C2-C6-alkenyloxy, C2-C6-alkynyl, C2-C6-haloalkynyl, C2-C6-alkynyloxy, optionally substituted C1 to C3-alkyl, or optionally substituted C1-C6-alkoxy, or R6 is, for formula II, for example, CN, C3-C8-cycloalkyl, or optionally substituted C3-C6-alkyl; and/or salts thereof; and their use as as pesticidal agents.Type: GrantFiled: October 27, 2009Date of Patent: January 14, 2014Assignee: Syngenta Crop Protection, LLCInventors: Ottmar Franz Hueter, Peter Renold, Werner Zambach, Thomas Pitterna, Peter Maienfisch
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Publication number: 20140005150Abstract: 3,4-diarylpyrazole derivatives of formula (I) as defined in the specification, and pharmaceutically acceptable salts thereof, process for their preparation and pharmaceutical compositions comprising them are disclosed; the compounds of the invention may be useful, in therapy, in the treatment of diseases associated with a disregulated protein kinase activity, like cancer.Type: ApplicationFiled: August 20, 2013Publication date: January 2, 2014Applicant: NERVIANO MEDICAL SCIENCES S.R.L.Inventors: Maurizio Pulici, Fabio Zuccotto, Gabriella Traquandi, Sonia Biondaro, Paolo Trifiro', Alessandra Badari, Stefano Nuvoloni, Giovanni Cervi, Chiara Marchionni, Michele Modugno
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Publication number: 20130296309Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: July 11, 2013Publication date: November 7, 2013Inventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Publication number: 20130296369Abstract: The present invention relates to cyanoenamine derivatives, their process of preparation, intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants and in material protection, using these compounds or compositions.Type: ApplicationFiled: November 11, 2011Publication date: November 7, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Jürgen Benting, Ulrike Wachendorff-Neumann, Philippe Desbordes, Christophe Dubost, Pierre Genix, Shinichi Narabu, Jean-Pierre Vors
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Publication number: 20130252972Abstract: The present invention relates to a compound of formula I: (I) wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.Type: ApplicationFiled: July 19, 2011Publication date: September 26, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wendeborn
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Patent number: 8524745Abstract: The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: GrantFiled: December 11, 2012Date of Patent: September 3, 2013Assignee: Allergan, Inc.Inventors: Haiqing Yuan, Richard L. Beard, Xiaoxia Liu, John E. Donello, Veena Viswanath
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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: 20130210836Abstract: The present invention relates to a compound of formula (I): wherein the substituents have the definitions as defined in claim 1 or a salt or a N-oxide thereof, their use and methods for the control and/or prevention of microbial infection, particularly fungal infection, in plants and to processes for the preparation of these compounds.Type: ApplicationFiled: July 19, 2011Publication date: August 15, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Carla Bobbio, Camilla Corsi, Stephane Andre Marie Jeanmart, Sebastian Volker Wenderborn
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Publication number: 20130210721Abstract: [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 15, 2013Applicant: MOCHIDA PHARMACEUTICAL CO., LTD.Inventor: MOCHIDA PHARMACEUTICAL CO., LTD.
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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: 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: 20130150413Abstract: The present invention relates to novel benzisothiazol-3(1H)-one-5-sulfonyl derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of chemokine receptors.Type: ApplicationFiled: December 11, 2012Publication date: June 13, 2013Applicant: ALLERGAN, INC.Inventor: ALLERGAN, INC.
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Publication number: 20130109566Abstract: This document discloses molecules having the following formula (“Formula One”): and processes related thereto.Type: ApplicationFiled: October 24, 2012Publication date: May 2, 2013Applicant: Dow Agrosciences LLCInventor: Dow AgroSciences LLC
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Publication number: 20130072449Abstract: Compounds, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds to treat, prevent or diagnose diseases, disorders, or conditions associated with one or more of the lysophosphatidic acid receptors are provided.Type: ApplicationFiled: August 14, 2012Publication date: March 21, 2013Applicant: InterMune, Inc.Inventors: Brad O. Buckman, John B. Nicholas, Kumaraswamy Emayan, Scott D. Seiwert
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Patent number: 8399451Abstract: Disclosed are compounds of Formula (I) or a stereoisomer or a pharmaceutically acceptable salt thereof, wherein: A is Q is a substituted 5-membered monocyclic heteroaryl group; W is CH2, O, or NH; and R1, R2, R3, R4, R5, R6, m, n, t, and x are defined herein. Also disclosed are methods of using such compounds as selective agonists for G protein-coupled receptor S1P1, and pharmaceutical compositions comprising such compounds. These 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 vascular disease.Type: GrantFiled: August 5, 2010Date of Patent: March 19, 2013Assignee: Bristol-Myers Squibb CompanyInventors: John L. Gilmore, James E. Sheppeck
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Patent number: 8338459Abstract: Compounds, compositions and methods are provided for stabilizing transthyretin and for treating, preventing, or ameliorating one or more symptoms of transthyretin mediated diseases. In one embodiment, the compounds are benzoxazoles and related compounds.Type: GrantFiled: December 28, 2010Date of Patent: December 25, 2012Assignee: FoldRx Pharmaceuticals, Inc.Inventor: Richard Labaudinière
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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: 20120232052Abstract: The present invention relates to aryl carboxamide derivatives of formula (I), wherein Ar1 is phenyl; Ar2 is aryl; n is 1-4; X is —O—, —S—, —SO— or —SO2—, a prodrug thereof or a pharmaceutically acceptable salt thereof, which have blocking activities of voltage gated sodium channels as the TTX-S channels, and which are useful in the treatment or prevention of such disorders and diseases as pain in which voltage gated sodium channels are involved. The invention also relates to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases as pain in which voltage gated sodium channels are involved.Type: ApplicationFiled: November 16, 2010Publication date: September 13, 2012Inventors: Tatsuya Yamagishi, Yoshimasa Arano, Mikio Morita, Tadashi Inoue
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Publication number: 20120184748Abstract: A compound is useful as a recyclable catalyst for esterification or acylation of alcohols and consists of saccharine and a compound comprising a pyridine moiety. In addition, also a method of preparing the compound and an ester synthesis method using the compound are introduced.Type: ApplicationFiled: May 25, 2011Publication date: July 19, 2012Applicant: NATIONAL TAIPEI UNIVERSITY OF TECHNOLOGYInventors: NORMAN LU, WEN-HAN TU, CHIEH-KENG LI
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Patent number: 8212048Abstract: A method of producing an aromatic compound of the following formula (3) comprising reacting a compound of the following formula (1) with an olefin compound of the following formula (2) in the presence of a transition metal complex: (wherein, an Ar1 ring represents an aromatic hydrocarbon ring or aromatic heterocyclic ring, an Ar2 ring represents a heterocyclic ring containing X1 and N*, and the X1 represents a nitrogen atom or carbon atom and the N represents a nitrogen atom connecting via a double bond to either one of two adjacent atoms in the Ar2 ring.) (wherein, R1, R2, R3 and R4 represent each independently a hydrogen atom, an alkyl group having 1 to 10 carbon atoms or an aryl group having 6 to 18 carbon atoms.) (wherein, Ar1, Ar2, X1, N*, R1, R2 and R3 represent the same meanings as described above.).Type: GrantFiled: February 2, 2007Date of Patent: July 3, 2012Assignees: Sumitomo Chemical Company, Limited, Osaka UniversityInventors: Fumitoshi Kakiuchi, Yusuke Matsuura, Masato Ueda
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Publication number: 20120157403Abstract: Heterocyclic-substituted tricyclics of the formula or a pharmaceutically acceptable salt or solvate of said compound, isomer or racemic mixture wherein represents an optional double bond, the dotted line is optionally a bond or no bond, resulting in a double bond or a single bond, as permitted by the valency requirement and wherein E, A, G M, Het, B, X, R3, R10, R11, R32 and R33 are herein defined and the remaining substituents are as defined in the specification, are disclosed, as well as pharmaceutical compositions containing them and a method of treating diseases associated with thrombosis, atherosclerosis, restenosis, hypertension, angina pectoris, arrhythmia, heart failure, and cancer by administering said compounds. Combination therapy with other cardiovascular agents is also claimed.Type: ApplicationFiled: February 24, 2012Publication date: June 21, 2012Inventors: Samuel Chackalamannil, Mariappan V. Chelliah, Yuguang Wang, Yan Xia
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Publication number: 20120157459Abstract: [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: ApplicationFiled: December 24, 2010Publication date: June 21, 2012Inventors: Akihiro Okano, Naoto Kosuga, Munetaka Ohkouchi, Daido Hotta, Muneyoshi Makabe
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Publication number: 20120142732Abstract: This invention provides compounds of formula IA or IB: wherein HY, R1, R2, and G1, are as described in the specification. The compounds are inhibitors of VPS34 and/or PI3K and are thus useful for treating proliferative, inflammatory, or cardiovascular disorders.Type: ApplicationFiled: August 10, 2011Publication date: June 7, 2012Applicant: Millennium Pharmaceuticals, Inc.Inventors: Courtney A. Cullis, Krista E. Granger, Jianping Guo, Masaaki Hirose, Gang Li, Miho Mizutani, Tricia J. Vos
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Publication number: 20120142671Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.Type: ApplicationFiled: November 1, 2011Publication date: June 7, 2012Applicant: Portola Pharmaceuticals, Inc.Inventors: Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
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Patent number: 8168798Abstract: This invention relates to prodrugs of caspase inhibitors comprising of a furo[3,2-d]oxazolin-5-one moiety which, under specific conditions, can convert into biologically active compounds, particularly caspase inhibitors. This invention also relates to the processes for preparing these prodrugs of caspase inhibitors. This invention further relates to pharmaceutical compositions comprising said prodrugs and to the use thereof for the treatment of diseases related to inflammatory or degenerative conditions.Type: GrantFiled: December 17, 2010Date of Patent: May 1, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Steven Durrant, Jean-Damien Charrier, John Studley
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Publication number: 20120094993Abstract: The present invention relates to compounds of formula I, wherein A, R1 to R7 are defined in the description, and to pharmaceutically acceptable salts thereof. The present invention also relates to the manufacture of such compounds or their pharmaceutically acceptable salts, pharmaceutical compositions containing them and their use as medicaments for the treatment and/or prophylaxis of diseases which can be treated with HDL-cholesterol raising agents, such as dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: October 7, 2011Publication date: April 19, 2012Inventors: Uwe Grether, Paul Hebeisen, Torsten Hoffmann, Stephan Roever
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Patent number: 8143293Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant, melanomas, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, leukemias, papillary thyroid carcinoma, non small cell lung cancer, mesothelioma, hypereosinophilic syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocyclosis, mast cell leukemia, a disease caused by c-Abl kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof, or a disease caused by c-Kit kinase, oncogenic forms thereof, aberrant fusion proteins thereof and polymorphs thereof.Type: GrantFiled: April 18, 2008Date of Patent: March 27, 2012Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20120040937Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.Type: ApplicationFiled: October 7, 2011Publication date: February 16, 2012Inventors: Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
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Publication number: 20120022255Abstract: This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.Type: ApplicationFiled: March 23, 2010Publication date: January 26, 2012Inventors: Toshio Fujishita, Minako Mikamiyama, Makoto Kawai, Toshiyuki Akiyama
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Publication number: 20110318266Abstract: Disclosed are mGluR4 positive allosteric modulator ligands of general formula (I) and radiolabeled derivates, their use as therapeutic agents for the treatment of central nervous system disorders modulated by mGluR4 and as ligands for the labeling and diagnostic imaging of mGluR4 in mammals.Type: ApplicationFiled: August 24, 2009Publication date: December 29, 2011Inventor: John A. McCauley
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Publication number: 20110312976Abstract: The present invention relates to a compound represented by formula (I): (wherein R, R2, R3 and R4 each independently represent a hydrogen or halogen atom; R5 and R6 each independently represent a hydrogen atom or lower alkyl or together represent oxo; X represents C(O) or the like; Y represents an oxygen atom or the like; Z represents a hydrogen atom or the like; R represents 5- or 6-membered heteroaryl having 1-3 hetero atoms selected from the group consisting of nitrogen, sulfur and oxygen atoms, contained within a ring, or the like) or to a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: March 9, 2010Publication date: December 22, 2011Applicant: MSD K.K.Inventors: Keisuke Arakawa, Teruyuki Nishimura, Yuichi Sugimoto, Hiroyuki Takahashi, Tadashi Shimamura
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Publication number: 20110306493Abstract: The invention relates to sulfoximinamid compounds of formula (I), to the enantiomers, diastereomers and salts thereof and to compositions comprising such compounds. The invention also relates to the use of the sulfoximinamid compounds, of their salts or of compositions comprising them for combating animal pests. Furthermore the invention relates also to methods of applying such sulfoximine compounds. The sulfoximinamid compounds of the present invention are defined by the following formula I: wherein Q, Het, R1, R2, R3, R4 and n are defined as in the description.Type: ApplicationFiled: June 19, 2009Publication date: December 15, 2011Applicant: BASF SEInventors: Ralph Paulini, Delphine Breuninger, Wolfgang Von Deyn, Henricus Maria Martinus Bastiaans, Carsten Beyer, Douglas D. Anspaugh, Hassan Oloumi-Sadeghi, Faraneh Oloumi
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Publication number: 20110301034Abstract: The present invention relates to isothiazole and pyrazole compounds of formula (I) having plant growth regulating properties, to agricultural compositions comprising them, and to the use of said compounds for regulating plant growth.Type: ApplicationFiled: December 11, 2009Publication date: December 8, 2011Applicant: SYNGENTA CROP PROTECTION LLCInventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Ulrich Johannes Haas
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Patent number: 8067611Abstract: The invention relates to 1-(thiazolyl)- and 1-(isothiazolyl)pyrazol-4-ylacetic acid derivatives of the general formula (I) and salts thereof in which Het, R1, R2, R3, R4, R5, R6 and n are as defined in claim 1. The compounds (I) or salts thereof are suitable for use as herbicides and plant growth regulators, in particular as herbicides for the selective control of harmful plants in crops of useful plants and can be prepared by processes as described in claim 9.Type: GrantFiled: December 3, 2009Date of Patent: November 29, 2011Assignee: Bayer CropScience AGInventors: Arianna Martelletti, Harald Jakobi, Jan Dittgen, Isolde Haeuser-Hahn, Dieter Feucht, Christopher Hugh Rosinger
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Publication number: 20110224241Abstract: The present invention relates to compounds of Formula (I) wherein R1, R2, R3 or R4 are as defined in claim 1 or a salt or N-oxide thereof and their use in methods for the control and/or prevention of fungal infection, particularly in plants. The compounds claimed are isothiazole and pyrazole derivatives.Type: ApplicationFiled: July 9, 2008Publication date: September 15, 2011Applicant: SYNGENTA CROP PROTECTION, INC.Inventors: Peter Ackermann, Carla Bobbio, Camilla Corsi, Josef Ehrenfreund, Ann Monica McGinley, Andreas Verras, Ruud Titulaer