1,2-oxazoles (including Hydrogenated) Patents (Class 546/272.1)
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Publication number: 20130196952Abstract: The invention relates to compounds of Formula (1) and to processes for the preparation of intermediates used in the preparation of compositions containing and the uses of such derivatives. The compounds according to the present invention are useful in numerous diseases in which ALK protein is involved or in which inhibition of ALK activity may induce benefit, especially for the treatment of cancer mediated by a mutated EML4-ALK fusion protein.Type: ApplicationFiled: May 4, 2011Publication date: August 1, 2013Applicant: PFIZER INC.Inventors: Mark Edward Bunnage, Andrew Simon Cook, Jingrong Jean Cui, Kevin Nell Dack, Judith Gail Deal, Danlin Gu, Mingying He, Patrick Stephen Johnson, Ted William Johnson, Phuong Thi Quy Le, Cynthia Louise Palmer, Hong Shen
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Patent number: 8497263Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.Type: GrantFiled: September 23, 2011Date of Patent: July 30, 2013Assignee: Shionogi & Co., Ltd.Inventors: Hiroyuki Kai, Shunji Shinohara, Takayuki Kameyama
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Publication number: 20130190355Abstract: Many GTPases such as Ras, Ral and Rho require post-translational farnestylation or geranylgeranylation for mediating malignant transformation. Dual farnesyltransferase (FT) (FTI) and geranylgeranyltransferase-I (GGT-1) inhibitors (GGTI) were developed as anticancer agents from based on an ethylenediamine scaffold. On the basis of a 4-fold substituted ethylenediamine scaffold, the inhibitors are structurally simple and readily derivatized, facilitating extensive structure-activity relationship studies. The most potent inhibitor is compound exhibited an in vitro hFTase IC50 value of 25 nM and a whole cell H-Ras processing IC50 value of 90 nM. Several of the inhibitors proved highly selective for hFTase over the related prenyltransferase enzyme geranylgeranyltransferase-I (GGTase-I).Type: ApplicationFiled: March 11, 2013Publication date: July 25, 2013Applicants: Yale University, H. Lee Moffitt Cancer Center and Research Institute, Inc.Inventors: H. Lee Moffitt Cancer Center and Research Institute, Inc., Yale University
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Publication number: 20130190286Abstract: The present invention encompasses compounds of general formula (1) where in the groups R0to R3 and L are defined as in claim 1, which are suitable for the 5 treatment of diseases characterised by excessive or abnormal cell proliferation, pharmaceutical preparations which contain compounds of this kind and their use as medicaments.Type: ApplicationFiled: March 25, 2011Publication date: July 25, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Patent number: 8486951Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: GrantFiled: August 21, 2012Date of Patent: July 16, 2013Assignee: Deciphera Pharmaceuticals, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Patent number: 8476446Abstract: The present invention relates to isoxazole compounds of formula (I) having fungicidal activity, to agricultural compositions comprising them, and to the use of said compounds and compositions in agriculture for the control of microbial pests, particularly fungal pests, on plants.Type: GrantFiled: December 11, 2009Date of Patent: July 2, 2013Assignee: Syngenta Crop Protection LLCInventors: Camilla Corsi, Sebastian Volker Wendeborn, Carla Bobbio, Jilali Kessabi, Peter Schneiter, Valeria Grasso, Shy-Fuh Lee, Ulrich Johannes Haas, Micah Gliedt
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Publication number: 20130158034Abstract: Compounds of Formula I are useful as antagonists of TRPM8. Such compounds are useful in treating a number of TRPM8 mediated disorders and conditions and may be used to prepare medicaments and pharmaceutical compositions useful for treating such disorders and conditions. Examples of such disorders include, but are not limited to, migraines and neuropathic pain. Compounds of Formula I have the following structure: where the definitions of the variables are provided herein.Type: ApplicationFiled: June 21, 2012Publication date: June 20, 2013Applicant: Amgen Inc.Inventors: James BROWN, Jian J. CHEN, Vijay Keshav GORE, Scott HARRIED, Daniel B. Horne, Matthew R. KALLER, Qingyian LIU, Holger MONENSCHEIN, Thomas T. NGUYEN, Nobuko NISHIMURA, Wenge ZHONG
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Publication number: 20130158076Abstract: 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: February 15, 2013Publication date: June 20, 2013Applicant: MERCK PATENT GMBHInventor: Merck Patent GmbH
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Patent number: 8455500Abstract: [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 p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: GrantFiled: October 29, 2010Date of Patent: June 4, 2013Assignee: Mochida Pharmaceutical Co., Ltd.Inventors: Akihiro Okano, Munetaka Ohkouchi
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Publication number: 20130137865Abstract: A compound represented by formula [I] and a pharmaceutically accepted salt of said compound are a novel compound and a pharmaceutically accepted salt thereof which exert antagonistic activity against group II metabotropic glutamate (mGlu) receptors, and are effective as a novel preventive or therapeutic agent for disorders such as mood disorders (depressive disorder, bipolar disorder, etc.), anxiety disorders (generalized anxiety disorder, panic disorder, obsessive-compulsive disorder, social anxiety disorder, posttraumatic stress disorder, a specific phobic disorder, acute stress disorder, etc.), schizophrenia, Alzheimer's disease, cognitive impairment, dementia, drug dependence, convulsions, shivering, pain, sleep disorders, and the like.Type: ApplicationFiled: August 11, 2011Publication date: May 30, 2013Applicant: TAISHO PHARMACEUTICAL CO., LTD.Inventors: Toshio Nakamura, Kazunari Sakagami, Kazuhide Konishi, Kanako Yamamoto, Seiji Masuda, Yohei Matsuda, Kumiko Okada, Tsuyoshi Shibata, Hiroshi Ohta, Akito Yasuhara, Hiroshi Kawamoto, Hideaki Amada, Hiroki Urabe, Rie Nishikawa, Shuhei Kashiwa ASHIWA
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Publication number: 20130137876Abstract: The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R1 and R2 indicate respectively independent hydrogen atoms, or the like; R1 and R2 may be bonded, and may form a heterocycle together with the nitrogen atom between R1 and R2).Type: ApplicationFiled: January 25, 2013Publication date: May 30, 2013Applicant: Nippon Soda Co., Ltd.Inventor: Nippon Soda Co., Ltd.
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Publication number: 20130131115Abstract: A pest control composition comprising a hydrazide compound shown by formula (1) below (in the formula, G, M, Q1, Q2, Q3, Q4, R2, R4, R5, R6 and m have the same meanings described in the specification) and etofenprox and a method for controlling pests whereby an effective dose of the hydrazide compound represented by formula (1) and etofenprox is applied to a pest or a pest habitat.Type: ApplicationFiled: July 25, 2011Publication date: May 23, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Kaori Ikari
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Patent number: 8445692Abstract: The present invention relates to the discovery that specific human taste receptors in the T2R taste receptor family respond to particular bitter compounds present in, e.g., coffee. Also, the invention relates to the discovery of specific compounds and compositions containing that function as bitter taste blockers and the use thereof as bitter taste blockers or flavor modulators in, e.g., coffee and coffee flavored foods, beverages and medicaments. Also, the present invention relates to the discovery of a compound that antagonizes numerous different human T2Rs and the use thereof in assays and as a bitter taste blocker in compositions for ingestion by humans and animals.Type: GrantFiled: November 4, 2011Date of Patent: May 21, 2013Assignee: Senomyx Inc.Inventors: Donald S Karanewsky, Joseph R. Fotsing, Catherine Tachdjian, Melissa Arellano
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Publication number: 20130123260Abstract: The disclosure relates to compounds of formula (I) for use in the treatment or prophylaxis of rhinovirus infection, methods of treating or preventing rhinovirus infection employing said compounds or pharmaceutical composition comprising the same. The disclosure also relates to compounds of formula (I) for use in the treatment or prophylaxis of exacerbation of respiratory disorders (such as asthma, COPD, bronchitis and/or cystic fibrosis) by rhinovirus infection.Type: ApplicationFiled: June 17, 2011Publication date: May 16, 2013Applicant: RESPIVERT LIMITEDInventors: Catherine Elisabeth Charron, Kazuhiro Ito, William Garth Rapeport
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Patent number: 8436023Abstract: The present invention comprises compounds of Formula (I). wherein: R1, R2, X, and Z are as defined in the specification. The invention also comprises a method of preventing, treating or ameliorating a syndrome, disorder or disease, wherein said syndrome, disorder or disease is type II diabetes, obesity and asthma. The invention also comprises a method of inhibiting CCR2 activity in a mammal by administration of a therapeutically effective amount of at least one compound of Formula (I).Type: GrantFiled: June 9, 2011Date of Patent: May 7, 2013Assignee: Janssen Pharmaceutica N.V.Inventors: Xuqing Zhang, Zhihua Sui, James C. Lanter
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Publication number: 20130102778Abstract: The present invention relates to a process for the preparation of a compound of formula (I) wherein R1 and R2 are as defined herein, which is useful as an intermediate in the preparation of active pharmaceutical compounds.Type: ApplicationFiled: October 12, 2012Publication date: April 25, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130102462Abstract: The present invention relates to a process for producing aromatic carbonyl compounds of formula I and aromatic imine compounds of formula III comprising the step of reacting a (hetero)aromatic halogen or sulfonate compound II wherein the variables are as defined in the claims and description, with a mixture of carbon monoxide and hydrogen in the presence of a transition metal complex catalyst. The invention also relates to specific compounds III, to compositions comprising them and to their use for combating invertebrate pests.Type: ApplicationFiled: June 22, 2011Publication date: April 25, 2013Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Christian Rein, Joachim Schmidt-Leithoff, Wolfgang Von Deyn, Prashant Deshmukh, Arun Narine, Joachim Dickhaut, Nina Gertrud Bandur, Juergen Langewald
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Publication number: 20130096124Abstract: The present invention relates to new isoxazoline compounds of formula wherein the variables have the meaning as indicated in the claims; in free form and in salt form; and optionally the enantiomers and geometrical isomers thereof. The compounds of formula (I) are useful in the control of parasites, in particular ectoparasites, in and on vertebrates.Type: ApplicationFiled: June 11, 2011Publication date: April 18, 2013Inventors: Steve Nanchen, Noelle Gauvry, Thomas Goebel
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Publication number: 20130079362Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: ApplicationFiled: August 21, 2012Publication date: March 28, 2013Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20130072490Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: September 29, 2010Publication date: March 21, 2013Applicant: Amira Pharmaceuticals INC.Inventors: Ryan Clark, Brian Andrew Stearns, Jill Melissa Scott, Heather Renee Coate, Lucy Zhao, Thomas Jon Seiders, Deborah Volkots, Jeannie Arruda, Nicholas Simon Stock, Yen Pham Truong, David Nathan Zalatan
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Publication number: 20130065907Abstract: The present invention relates to compounds of the formula wherein R1 to R4 are defined in the description, and to pharmaceutically acceptable salts thereof, their manufacture, 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 particularly dyslipidemia, atherosclerosis and cardiovascular diseases.Type: ApplicationFiled: September 11, 2012Publication date: March 14, 2013Inventors: Stephan Roever, Uwe Grether
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Publication number: 20130065923Abstract: The present disclosure relates to a series of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I). wherein R1, R2, R3, R4, Q1, Q2, Q3, Q4, X, m and p are as described herein. More specifically, the compounds of this invention are modulators of H3 receptors and are, therefore, useful as pharmaceutical agents, especially in the treatment and/or prevention of a variety of diseases modulated by H3 receptors including diseases associated with the central nervous system. Additionally, this disclosure also relates to methods of preparation of substituted N-heteroaryl bipyrrolidine carboxamides of formula (I) and intermediates therefor.Type: ApplicationFiled: November 6, 2012Publication date: March 14, 2013Applicant: SANOFIInventor: Sanofi
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Patent number: 8389550Abstract: The present invention is concerned with novel isoxazole-pyridines of formula I wherein R1, R2, R3 and L are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: GrantFiled: February 17, 2010Date of Patent: March 5, 2013Assignees: Hoffmann-La Roche Inc., Roche Palo Alto LLCInventors: Bernd Buettelmann, Matthew C. Lucas, Andrew Thomas
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Publication number: 20130053376Abstract: Provided are compounds of the formula (I): or a stereoisomer, tautomer, salt, hydrate or prodrug thereof that modulate tyrosine kinase activity, compositions comprising the compounds and methods of their use.Type: ApplicationFiled: March 18, 2009Publication date: February 28, 2013Inventors: Yahua Liu, Alexey Vyacheslavovich Anikin, Charles Chamchoumis Mikel, Douglas Eric McGrath, Goverdhan Reddy Vavilala, Jason Conrad Pickens, Aleksander Kadushkin, Luyong Jiang, Mohan Santhanam Thiruvazhi, Sergey Zozulya, Rajendran Vairagoundar, Tong Zhu, Alexander Chucholowski, Zheng Yan, Alisher Khasanov, Christina Gregor
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Patent number: 8383615Abstract: Compounds of the formula (I), (II) and (III) which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: June 8, 2010Date of Patent: February 26, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Eugene Richard Hickey, Doris Riether, David Smith Thomson, Lifen Wu, Renee M. Zindell
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Patent number: 8377942Abstract: Novel isoxazoline compounds, compositions containing the compounds and methods for making the compounds are disclosed. The compounds and compositions have pesticidal properties and are suitable for controlling ectoparasites on non-human animals.Type: GrantFiled: December 17, 2009Date of Patent: February 19, 2013Assignee: Novartis AGInventors: Steve Nanchen, Noëlle Gauvry, Francois Pautrat
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Publication number: 20130039944Abstract: Disclosed herein are compounds and related compositions for the treatment of viral infection, including RNA viral infection, and compounds that can modulate the RIG-I pathway in vertebrate cells, including compounds that can activate the RIG-I pathway.Type: ApplicationFiled: April 20, 2011Publication date: February 14, 2013Applicant: Kineta, Inc.Inventors: Shawn P. Iadonato, Kristin Bedard
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Patent number: 8372867Abstract: The present invention relates to novel aryl isoxazoline derivatives having excellent insecticidal activity as insecticides and represented by the formula: and their use as insecticides and acarizides.Type: GrantFiled: March 28, 2008Date of Patent: February 12, 2013Assignee: Bayer CropScience AGInventors: Jun Mihara, Tetsuya Murata, Daiei Yamazaki, Yasushi Yoneta, Katsuhiko Shibuya, Eiichi Shimojo, Ulrich Görgens, Andreas Turberg, Thomas Bach
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Publication number: 20130035326Abstract: Provided herein are compounds for treatment of KIT, CSF-1R and/or FLT3 kinase mediated diseases. Also provided are pharmaceutical compositions comprising the compounds and methods of using the compounds and compositions.Type: ApplicationFiled: August 18, 2010Publication date: February 7, 2013Applicant: AMBIT BIOSCIENCES CORPORATIONInventors: Sunny Abraham, Mark W. Holladay, Gang Liu, Shimin Xu
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Publication number: 20130029845Abstract: Disclosed are compounds of Formula 1, including all geometric and stereoisomers, N-oxides, and salts thereof, wherein A1, A2, A3, A4, A5 and A6 are independently selected from the group consisting of CR3 and N; provided that at most 3 of A1, A2, A3, A4, A5 and A6 is N; B1, B2 and B3 are independently selected from the group consisting of CR2 and N; each R3 is independently H, halogen, C1-C6 alkyl, C1-C6 haloalkyl, C3-C6 cycloalkyl, C3-C6 halocycloalkyl, C1-C6 alkoxy, C1-C6 haloalkoxy, C1-C6 alkylthio, C1-C6 haloalkylthio, C1-C6 alkylsulfinyl, C1-C6 haloalkylsulfinyl, C1-C6 alkylsulfonyl, C1-C6 haloalkylsulfonyl, C1-C6 alkylamino, C2-C6 dialkylamino, —CN or —NO2; and R1, R2, R4, R5, W and n are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling an invertebrate pest comprising contacting the invertebrate pest or its environment with a biologically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: July 30, 2012Publication date: January 31, 2013Applicant: E.I. du Pont de Nemours and CompanyInventors: George Philip LAHM, Wesley Lawrence SHOOP, Ming XU
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Patent number: 8362257Abstract: The present invention offers compounds or their salts expressed by formula (I) (in the formula, X indicates an alkyl group, or the like; Y indicates an alkyl group; Z indicates a respectively independent nitro group, or the like; n indicates any integer from 0 to 3; A indicates carbon atom, or the like, and hydrogen atom is bonded thereto in the case where the carbon atom is not substituted with Z; D indicates oxygen atom, or the like; W indicates hydrogen atom, or the like; R1 and R2 indicate respectively independent hydrogen atoms, or the like; R1 and R2 may be bonded, and may form a heterocycle together with the nitrogen atom between R1 and R2).Type: GrantFiled: September 15, 2009Date of Patent: January 29, 2013Assignee: Nippon Soda Co., Ltd.Inventors: Jyun Iwata, Masahiro Kawaguchi
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Publication number: 20130023566Abstract: The invention relates to 2-(1,2-benzisoxazol-3-yl)benzylamine derivatives having the general Formula (I) wherein R1 represents the group CONR2R3 which is present at one of the positions 5-, 6- or 7- on the 1,2-benzisoxazole ring; R2 and R3 are independently H or (C1-4)alkyl; and R4 is cyclopropyl, 2-pyridyl or phenyl, optionally substituted with one or more halogens; or a pharmaceutically acceptable salt thereof, to pharmaceutical compositions comprising the same, as well as to the use of these derivatives for the treatment of pain, such as neuropathic pain or inflammatory pain.Type: ApplicationFiled: July 6, 2010Publication date: January 24, 2013Applicant: N.V. OrganonInventor: Simon James Anthony Grove
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Patent number: 8357703Abstract: The present invention is concerned with novel isoxazoles of formula I wherein X, R1, R2, R3 and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. The active compounds of the present invention have affinity and selectivity for GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the active compounds of formula I, pharmaceutical compositions containing them and their use as therapeutics.Type: GrantFiled: May 3, 2010Date of Patent: January 22, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Patent number: 8354436Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: January 15, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
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Publication number: 20130005735Abstract: The present invention relates to compounds of formula (I) wherein X, R1, R2, R3, R4 and R5 are as defined herein, which are useful for treating diseases which respond to CXCR2 receptor mediators. Pharmaceutical compositions that contain the compounds and processes for preparing the compounds are also described.Type: ApplicationFiled: September 12, 2012Publication date: January 3, 2013Inventors: Urs Baettig, Anne-Marie D'souza, Peter Hunt, Neil John Press, Simon James Watson
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Publication number: 20120329812Abstract: Certain chemical entities are provided herein. Also provided are pharmaceutical compositions comprising at least one chemical entity and one or more pharmaceutically acceptable vehicle. Methods of treating patients suffering from certain diseases and disorders responsive to the inhibition of KMO activity are described, which comprise administering to such patients an amount of at least one chemical entity effective to reduce signs or symptoms of the disease or disorder are disclosed. These diseases include neurodegenerative disorders such as Huntington's disease. Also described are methods of treatment include administering at least one chemical entity as a single active agent or administering at least one chemical entity in combination with one or more other therapeutic agents. Also provided are methods for screening compounds capable of inhibiting KMO activity.Type: ApplicationFiled: August 3, 2009Publication date: December 27, 2012Inventors: John Wityak, Leticia M. Toledo-Sherman, Celia Dominguez, Stephen Martin Courtney, Christopher John Yarnold, Paula C. De Aguiar Pena, Andreas Scheel, Dirk Winkler
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Publication number: 20120316124Abstract: The present invention relates to compounds formula (I), wherein P is P1, P2, heterocyclyl or heterocyclyl substituted by one to five Z; and wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5, R6, R17, R18, R19 and R20 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to processes and intermediates for preparing compounds of formula (I), to insecticidal, acaricidal, nematicidal and molluscicidal compositions comprising the compounds of formula (I) and to methods of using the compounds of formula (I) to control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: February 17, 2011Publication date: December 13, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Thomas Pitterna, Myriem El Qacemi, Jerome Yves Cassayre, Peter Renold, Vladimir Bobosik
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Publication number: 20120291159Abstract: The present invention relates to azoline compounds which are useful for combating or controlling invertebrate pests, in particular arthropod pests and nematodes. The invention also relates to a method for controlling invertebrate pests by using these compounds and to plant propagation material and to an agricultural and a veterinary composition comprising said compounds.Type: ApplicationFiled: December 20, 2010Publication date: November 15, 2012Applicant: BASF SEInventors: Karsten Koerber, Florian Kaiser, Wolfgang von Deyn, Steffen Gross, Prashant Deshmukh, Joachim Dickhaut, Nina Gertrud Bandur, Arun Narine, Carsten Beyer, Deborah L. Culbertson, Douglas D. Anspaugh, Franz Josef Braun, Ronan Le Vezouet
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Publication number: 20120289483Abstract: 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: July 26, 2012Publication date: November 15, 2012Applicant: SYNTA PHARMACEUTICALS CORPORATIONInventors: Lijun Sun, Christopher Borella, Hao Li, Jun Jiang, Shoujun Chen, Keizo Koya, Takayo Inoue, Zhenjian Du, Kevin Foley, Yaming Wu, Mei Zhang, Weiwen Ying
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Publication number: 20120289522Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: October 1, 2010Publication date: November 15, 2012Inventors: Thomas J. Seiders, Lucy Zhao, Jeannie Arruda, Bowei Wang, Brian Andrew Stearns, Yen Pham Truong, Jill Melissa Scott, John Howard Hutchinson, Ryan Clark, Heather Renee Coate, Nicholas Simon Stock, Deborah Volkots
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Publication number: 20120289505Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. 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: December 30, 2010Publication date: November 15, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Publication number: 20120258987Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.Type: ApplicationFiled: April 4, 2012Publication date: October 11, 2012Applicant: AMIRA PHARMACEUTICALS, INC.Inventors: Thomas Jon Seiders, Jeffrey Roger Roppe, Timothy Andrew Parr
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Publication number: 20120252797Abstract: Isoxazoles of formula (A) or (B) wherein R1 is a group of formula (IB) The isoxazoles are inhibitors of HSP90 activity, and useful for the treatment of, for example, cancers.Type: ApplicationFiled: June 18, 2012Publication date: October 4, 2012Applicants: Vernalis (Cambridge) Limited, The Institute of Cancer Research, Cancer Research Technology Ltd.Inventors: Martin James Drysdale, Brian William Dymock, Harry Finch, Paul Webb, Edward McDonald, Karen Elizabeth James, Kwai Ming Cheung, Thomas Peter Matthews
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Publication number: 20120238517Abstract: The present invention relates to compounds of formula (I): Wherein A1, A2, A3, A4, G1, L, Y1, Y2, Y3, Y4, R1, R2, R3 and R4 are as defined in claim 1; or a salt or N-oxide thereof. Furthermore, the present invention relates to intermediates for preparing compounds of formula (I), to compositions comprising them and to methods of using them to combat and control insect, acarine, nematode and mollusc pests.Type: ApplicationFiled: December 1, 2010Publication date: September 20, 2012Applicant: SYNGENTA CROP PROTECTION LLCInventors: Jerome Yves Cassayre, Peter Renold, Myriem El Qacemi, Thomas Pitterna, Julie Clementine Toueg
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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: 20120232116Abstract: The present invention relates to compounds which bind to the NR1 H4 receptor (FXR) and act as agonists of the NR1 H4 receptor (FXR). The invention further relates to the use of the compounds for the preparation of a medicament for the treatment of diseases and/or conditions through binding of said nuclear receptor by said compounds, and to a process for the synthesis of said compounds.Type: ApplicationFiled: August 19, 2010Publication date: September 13, 2012Applicant: PHENEX PHARMACEUTICALS AGInventors: Claus Kremoser, Ulrich Abel, Christoph Steeneck, Olaf Kinzel
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Patent number: 8258161Abstract: A novel crystalline anhydrous toluenesulfonic acid salt form of a selective PPAR gamma partial agonist which has a fused bicyclic aromatic group attached to an oxypropanoic acid moiety is stable and non-hygroscopic. The crystalline salt form is useful for making pharmaceutical formulations for the treatment of type 2 diabetes, hyperglycemia, obesity, and dyslipidemia.Type: GrantFiled: February 28, 2008Date of Patent: September 4, 2012Assignee: Merck Sharp & Dohme Corp.Inventor: Aquiles E. Leyes
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Publication number: 20120220772Abstract: [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 p is 0 to 4; j is 0 to 3; k is 0 to 2; a ring A is a specific cyclic group; a ring B is a benzene ring, a pyridine ring, or a pyrimidine ring; X is —CH2—, O, —S(O)i— (i is 0 to 2), or —NR7—; R1 to R6 are specific groups), a salt of the compound, or a solvate of the salt or the compound.Type: ApplicationFiled: October 29, 2010Publication date: August 30, 2012Inventors: Akihiro Okano, Munetaka Ohkouchi
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Patent number: 8242283Abstract: A pesticide, particularly an insecticide or an acaricide, including a substituted isoxazoline compound of formula (1) or a salt thereof: wherein A1, A2 and A3 independently of one another are carbon atom or nitrogen atom, G is benzene ring, etc., L is —N(R2c)—, or —CH(R2a)N(R2c)—, etc., X is halogen atom, C1-C6 haloalkyl, etc., Y is halogen atom, C1-C6alkyl, etc., R1 is —C(O)R1a, —C(O)OR1a, —C(O)NHR1a, etc., R2 is hydrogen atom, C1-C6haloalkyl, —C1-C4alkoxy C1-C4alkyl, cyano C1-C6alkyl, C3-C6alkenyl, C3-C6alkynyl, —C(O)R15, —C(O)OR15, etc., R3 is C1-C6haloalkyl, etc., m is an integer of 0 to 5, n is an integer of 0 to 4. The pesticide containing these compounds.Type: GrantFiled: March 28, 2011Date of Patent: August 14, 2012Assignee: Nissan Chemical Industries, Ltd.Inventors: Takeshi Mita, Kazushige Maeda, Mitsuaki Komoda, Eitatsu Ikeda, Ken-ichi Toyama, Motoyoshi Iwasa
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Publication number: 20120196902Abstract: The present invention relates to organic molecules capable of modulating tyrosine kinase signal transduction in order to regulate, modulate and/or inhibit abnormal cell proliferation.Type: ApplicationFiled: October 20, 2011Publication date: August 2, 2012Inventors: Sougato Boral, Shimiao Wang, JULIE A. WURSTER