Nitrogen Attached Directly To The 1,3-thiazole Ring By Nonionic Bonding Patents (Class 546/270.7)
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Patent number: 8778929Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.Type: GrantFiled: September 28, 2009Date of Patent: July 15, 2014Assignee: Boehringer Ingelheim International GmbHInventors: Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
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Publication number: 20140179663Abstract: The present invention relates to compounds of Formula (I): Wherein variables are as defined above. The compounds have apoptosis signal-regulating kinase (“ASK1”) inhibitory activity, and are thus useful in the treatment of ASK1-mediated conditions, including autoimmune disorders, inflammatory diseases, cardiovascular diseases, diabetes, diabetic nephropathy, cardio-renal diseases, including kidney disease, fibrotic diseases, respiratory diseases, COPD, idiopathic pulmonary fibrosis, acute lung injury, acute and chronic liver diseases, and neurodegenerative diseases.Type: ApplicationFiled: December 20, 2013Publication date: June 26, 2014Applicant: Gilead Sciences, Inc.Inventor: Gregory Notte
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Publication number: 20140171639Abstract: 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: February 24, 2014Publication date: June 19, 2014Applicant: AMGEN INC.Inventors: Kaustav Biswas, James Brown, Jian J. Chen, Vijay Keshav Gore, Scott Harried, Daniel B. Horne, Matthew R. Kaller, Qingyian Liu, Vu Van Ma, Holger Monenschein, Thomas T. Nguyen, David J. St. Jean, JR., Chester Chenguang Yuan, Wenge Zhong
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Publication number: 20140158956Abstract: The coloring matter compound is represented by the following general formula (1): wherein R1, R2, R6 represent an alkyl group; R3 to R5 represent an alkyl group, or satisfy either of the following conditions i) and ii): i) R3 and R4 are bonded to each other, so as to form a cyclic organic functional group containing R3, R4 and a carbon atom bonded to R3 and R4, and R5 represents an alkyl group; ii) R3 to R5 are bonded to one another, so as to form a cyclic organic functional group containing R3, R4, R5 and a carbon atom bonded to R3 to R5; and R7, R8 represent an alkyl group or an acyl group, or R7 and R8 are bonded to each other, so as to form a cyclic organic functional group containing R7, R8 and a nitrogen atom bonded simultaneously to R7 and R8.Type: ApplicationFiled: February 18, 2014Publication date: June 12, 2014Applicant: CANON KABUSHIKI KAISHAInventors: Taichi Shintou, Yuko Katsumoto, Akiko Kitao, Takeshi Miyazaki
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Publication number: 20140158955Abstract: The coloring matter compound is represented by the following general formula (1): wherein R1 and R2 each independently represent an alkyl group or an acyl group, or R1 and R2 may be bonded to each other so as to form a cyclic organic functional group containing, as a hetero atom, a nitrogen atom to which R1 and R2 are bonded; R3 and R4 each independently represent an alkyl group; R5 and R6 each independently represent an alkyl group or an alkoxy group; R7 represents a hydrogen atom, an alkyl group or an alkoxy group; and R8 represents an alkyl group.Type: ApplicationFiled: February 14, 2014Publication date: June 12, 2014Applicant: CANON KABUSHIKI KAISHAInventors: Yuko Katsumoto, Taichi Shintou, Akiko Kitao, Takeshi Miyazaki
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Patent number: 8741934Abstract: The invention is directed to compounds of Formula I in which: R5, R6, B and Z are defined supra.Type: GrantFiled: November 15, 2012Date of Patent: June 3, 2014Assignees: Pfizer Limited, Icagen, Inc.Inventors: Brian Edward Marron, Paul Christopher Fritch, Christopher John Markworth, Andrew Thomas Maynard, Nigel Alan Swain
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Patent number: 8691820Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer.Type: GrantFiled: June 23, 2011Date of Patent: April 8, 2014Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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Patent number: 8691850Abstract: The present application relates to novel phenylaminothiazole derivatives, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, preferably for the treatment and/or prevention of hypertension and other cardiovascular disorders.Type: GrantFiled: August 30, 2005Date of Patent: April 8, 2014Assignee: Bayer Intellectual Property GmbHInventors: Jens-Kerim Ergüden, Gunter Karig, Ulrich Rosentreter, Barbara Albrecht, Kerstin Henninger, Joachim Hütter, Nicole Diedrichs, Peter Nell, Sabine Arndt, Walter Hübsch, Andreas Knorr, Karl-Heinz Schlemmer, Dirk Brohm
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Patent number: 8691573Abstract: The present invention relates compounds for stabilizing cells and methods of their use.Type: GrantFiled: December 3, 2009Date of Patent: April 8, 2014Assignee: The Scripps Research InstituteInventors: Yue Xu, Sheng Ding
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Publication number: 20140066466Abstract: Described herein are compositions that inhibit the production of TNF? downstream of CD40 activation. As such, also described are various methods of using compositions exhibiting this activity for the treatment or prevention of inflammatory diseases associated with TNF? production or CD40 activation.Type: ApplicationFiled: March 12, 2012Publication date: March 6, 2014Applicant: President and Fellows of Harvard CollegeInventor: Junying Yuan
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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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Publication number: 20140038948Abstract: Compounds active on protein kinases are described, as well as methods of using such compounds to treat diseases and conditions associated with aberrant activity of protein kinases.Type: ApplicationFiled: June 25, 2013Publication date: February 6, 2014Applicant: Plexxikon Inc.Inventors: Guoxian Wu, Jiazhong Zhang, Yong-Liang Zhu, Chao Zhang, Prabha N. Ibrahim, Songyuan Shi, Wayne Spevak, Dean R. Artis, James Tsai
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Publication number: 20140031348Abstract: Compounds are provided that act as potent antagonists of the CCR2 receptor. Animal testing demonstrates that these compounds are useful for treating inflammation, a hallmark disease for CCR2. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR2-mediated diseases, and as controls in assays for the identification of CCR2 antagonists.Type: ApplicationFiled: July 9, 2013Publication date: January 30, 2014Inventors: Solomon Ungashe, Zheng Wei, Arindrajit Basak, Trevor T. Charvat, Wei Chen, Jeff Jin, Jimmie Moore, Yibin Zeng, Sreenivas Punna, Daniel Dairaghi, Derek Hansen, Andrew M.K. Pennell, John J. Wright
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Publication number: 20140024657Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I)-(VIII) and by Compounds (1)-(7), (13)-(26), (27)-(33), (48)-(57), and (58)-(70). These necrostatins are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring necrostatins. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: September 20, 2013Publication date: January 23, 2014Applicant: President and Fellows of Harvard CollegeInventors: Junying YUAN, Emily S. Hsu
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Publication number: 20140004155Abstract: 2-aminothiazole derivatives represented by formula (I), where R1 and R2 represent cycloalkyls, respectively; or R1 represents a substituted aromatic group, and R2 represents H, a C1-C11 alkyl, —CH2Ph (benzyl), or a methyl ether including a C1-C11 alkyl. R3 is a substituent including an amino group. X represents a carbonyl or a methylene and n is an integer from 0 to 5.Type: ApplicationFiled: September 1, 2013Publication date: January 2, 2014Applicants: Hangzhou Zhongmei Huadong Pharmaceutical Co., Ltd., Huazhong University of Science & TechnologyInventors: Fengchao JIANG, Ping ZHOU, Jianguo CHEN, Yue WANG, Baoshuai CAO, Jia YAN
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Publication number: 20130338111Abstract: The present invention relates to compounds of the formula and pharmaceutically acceptable salts, solvates or tautomers thereof, to processes for the preparation of, intermediates used in the preparation of, and compositions containing such compounds, and the uses of such compounds, in particular for the treatment of pain.Type: ApplicationFiled: August 16, 2013Publication date: December 19, 2013Applicants: Icagen, Inc., Pfizer LimitedInventors: Serge Beaudoin, Michael Christopher Laufersweiler, Christopher John Markworth, Brian Edward Marron, David Simon Millan, David James Rawson, Steven Michael Reister, Kosuke Sasaki, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130336965Abstract: The present invention provides a compound of formula (A): as described herein, and pharmaceutically acceptable salts, enantiomers, rotamers, tautomers, or racemates thereof. Also provided are methods of treating a disease or condition mediated by PIM kinase using the compounds of Formula I, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: May 20, 2013Publication date: December 19, 2013Applicant: Novartis AGInventors: Matthew Burger, Joseph E. Drumm, III, Gisele Nishiguchi, Alice Rico, Robert Lowell Simmons, Benjamin Taft, Huw Tanner
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Patent number: 8604033Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, X, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: GrantFiled: January 14, 2011Date of Patent: December 10, 2013Assignee: Addex Pharma S.A.Inventor: Christelle Boléa
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Publication number: 20130324737Abstract: The invention disclosed in this document is related to the field of processes to produce certain 2-(pyridine-3-yl)thiazoles as intermediates for the synthesis of pesticidal thiazole amides.Type: ApplicationFiled: May 30, 2013Publication date: December 5, 2013Applicant: DOW AGROSCIENCES LLCInventors: Ronald Ross, JR., Carl DeAmicis, Yuanming Zhu, Noormohamed M. Niyaz, Kim E. Arndt, Scott P. West, Gary Roth
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Patent number: 8598361Abstract: The present invention relates to a process for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine in high yield and purity. The present invention also relates to processes for the synthesis of 5-fluoro-1H-pyrazolo[3,4-b]pyridin-3-amine derivatives. These processes are useful for preparing biologically active compounds, particularly certain GSK-3 inhibitors, or derivatives thereof.Type: GrantFiled: January 11, 2012Date of Patent: December 3, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Juan-Miguel Jimenez, Andrew Miller, Philip Collier, Jeremy Green, Albert Dros, Huai Gao, Sylvain Hamon
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Publication number: 20130317070Abstract: The invention provides for the use of antimicrobial chemical entities based on a nitrothiazolide backbone that exhibit anti-mycobacteria activity, including the mycobacterium causing tuberculosis. Multiple compounds were synthesized and screened for anti-tuberculosis activity. Disclosed herein are a series of compounds with anti-tuberculosis activity, including six leads that completely inhibited bacterial growth at 5 micrograms per ml or less. Three of these compounds were tested to determine MIC and these ranged between 1 and 4 micrograms per ml against both drug susceptible Mycobacterium tuberculosis strains and strains that are multi-drug resistant (MDR) including XDR strains. The compounds developed are derived from parent compound nitazoxanide, which had no inhibitory activity in the stringent testing format used herein.Type: ApplicationFiled: September 20, 2011Publication date: November 28, 2013Applicant: UNIVERSITY OF VIRGINIA PATENT FOUNDATION D/B/A UNIVERSITY OF VIRGINIA LICENSING & VENTURES GROUPInventors: Paul S. Hoffman, Timothy L. MacDonald, Eric R. Houpt, Thomas E. Ballard
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Publication number: 20130317218Abstract: The present invention relates to novel bicyclic thiazole compounds that inhibit Traf2- and Nck-interacting kinase (TNIK), and as such are useful as TNIK inhibitors administered to cancer patients, especially to solid cancer patients such as colorectal cancer, pancreatic cancer, non-small cell lung cancer, prostate cancer or breast cancer. The bicyclic thiazole compounds are showed by a next formula (I). (wherein R1, R2, R3 and Q are as defined in the specification), or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: May 24, 2012Publication date: November 28, 2013Inventors: Masaaki Sawa, Hideki Moriyama, Tesshi Yamada, Miki Shitashige, Yusuke Kawase, Yuko Uno
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Publication number: 20130310375Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
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Publication number: 20130310393Abstract: Disclosed are heteroaryl compounds of Formula (I), (I), or pharmaceutically acceptable salts thereof, wherein Z is CH or N; W is CR3 or N; and R1, R2, and R3 are defined herein. Also disclosed are methods of using such compounds in the treatment of at least one CYP17 associated condition, such as, for example, cancer, and pharmaceutical compositions comprising such compounds.Type: ApplicationFiled: September 23, 2011Publication date: November 21, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Audris Huang
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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: 20130288250Abstract: A method for in vitro predicting survival and/or metastatic outcome of gastrointestinal stromal tumors (GISTs), characterized in that it comprises the measure of the level, in a patient-derived biological sample of GIST, of a pool of polypeptides or polynucleotides consisting in Aurora kinase A (AURKA); a kit for the in vitro prediction of the survival outcome of a patient suffering from GIST, and/or the development of metastases in a patient treated for or suffering from GIST, and/or the prediction of the efficacy of a treatment for GIST, characterized in that it comprises means for detecting and/or quantify, in a sample, AURKA expression or level, and means for the calculation of the GI; and a method for screening for compounds for the use in the treatment of GISTs and to an AURKA inhibitor for its use in the treatment of GISTs.Type: ApplicationFiled: October 20, 2011Publication date: October 31, 2013Applicants: UNIVERSITE BORDEAUX SEGALEN, INSTITUE CURIE, INSTITUT BERGONIE, INSERMInventors: Frédéric Chibon, Jean-Michel Coindre, Alain Aurias
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Patent number: 8563741Abstract: The present invention relates to CDK inhibitors and their use in the treatment of cell proliferative diseases such as cancer. The compounds of the invention may further act as HDAC inhibitors.Type: GrantFiled: September 10, 2008Date of Patent: October 22, 2013Assignee: Curis, Inc.Inventors: Changgeng Qian, Xiong Cai, Haixiao Zhai
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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: 8541453Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: GrantFiled: May 20, 2011Date of Patent: September 24, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20130245273Abstract: The present invention relates to compounds useful as inhibitors of protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Juan-Miguel Jimenez, Philip Collier, Jeremy Green, Gregory Henkel, Michael Liu, Timothy Neuberger
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Publication number: 20130231342Abstract: The invention relates to (hetero)aryl cyclopropylamine compounds, including particularly the compounds of formula (I) as described and defined herein, and their use in therapy, including, e.g., in the treatment or prevention of cancer, a neurological disease or condition, or a viral infection. Thus, in one specific aspect the invention relates to formulas (II), (III), (IV), (V), (VI), (VII), (VIII), (IX).Type: ApplicationFiled: July 27, 2011Publication date: September 5, 2013Applicant: Oryzon Fenomics S.A.Inventors: Alberto Ortega Muñoz, Matthew Colin Thor Fyfe, Marc Martinell Pedemonte, Iñigo Tirapu Fernandez de la Cuesta, Maria de los Ángeles Estirate-Martinez
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Publication number: 20130225587Abstract: The compound of Formula (I), pharmaceutically acceptable salts thereof, solvates thereof, chelates thereof, non-covalent complexes thereof or produgs of compounds mentioned above or the mixture of any form above mentioned are provided. The use of the compounds in manufacturing a medicament for the treatment and/or prevention of diabetes, obesity and related disorders.Type: ApplicationFiled: November 9, 2011Publication date: August 29, 2013Applicants: Zhejiang Beta Pharma Incorporation, Fujian Haixi Pharmaceuticals, Inc.Inventors: Xinshan Kang, Wei Long, Cunbo Ma, Yanping Wang, Xiaoyan Shen, Yunyan Hu, Fenlai Tan, Yinxiang Wang
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Patent number: 8518948Abstract: Compounds of general Formula (I): wherein R1, R2, R3, Ra, A, B and x are as defined herein are inhibitors of protein kinases in particular members of the cyclin-dependent kinase family and/or the glycogen synthase kinase 3 family and are useful in preventing and/or treating any type of pain, inflammatory disorders, cancer, immunological diseases, proliferative diseases, infectious diseases, cardiovascular diseases, metabolic disorders, renal diseases, neurologic and neuropsychiatric diseases and neurodegenerative diseases.Type: GrantFiled: March 10, 2011Date of Patent: August 27, 2013Assignee: Ingenium Pharmaceuticals GmbHInventors: Lutz Zeitlmann, Andre Niestroj, Ulrich Heiser
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Patent number: 8513430Abstract: The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11?HSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.Type: GrantFiled: July 25, 2011Date of Patent: August 20, 2013Assignee: High Point Pharmaceuticals, LLCInventors: Dharma Rao Polisetti, Suparna Gupta
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Publication number: 20130210809Abstract: The present invention relates to novel compounds of Formula (1), wherein M, A and B are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors-subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: July 12, 2011Publication date: August 15, 2013Inventors: Christelle Boléa, Sylvain Celanire, Cédric Boudou, Lam Tang, Jean-Philippe Rocher, Nigel John Liverton
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Publication number: 20130190312Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Such compounds disrupt Nek2/Hec1 binding and may be useful as chemotherapeutic agents for neoplastic diseases.Type: ApplicationFiled: November 29, 2012Publication date: July 25, 2013Inventors: Jiann-Jyh HUANG, Shih-Hsien CHUANG, Ying-Shuan Eda LEE, Yu-Ling HUANG, Johnson LAU
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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: 20130165483Abstract: This invention provides compounds of formula IB: wherein HY, R1, R2, R3, R15, G5, G6, G7, G8, and G9 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: December 20, 2012Publication date: June 27, 2013Applicant: MILLENNIUM PHARMACEUTICALS, INC.Inventor: Millennium Pharmaceuticals, Inc.
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Publication number: 20130158078Abstract: Heterocyclic sulfone compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: May 12, 2011Publication date: June 20, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Publication number: 20130143927Abstract: 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: June 8, 2012Publication date: June 6, 2013Applicant: CalciMedica, Inc.Inventors: Jeffrey P. WHITTEN, Jonathan GREY, Jianguo CAO, Zhijun WANG, Evan ROGERS
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Patent number: 8445690Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: February 16, 2011Date of Patent: May 21, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130116228Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: ApplicationFiled: August 2, 2012Publication date: May 9, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Michael Mortimore, Julian Golec, Christopher Davis, Daniel Robinson, John Studley
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Patent number: 8435976Abstract: The invention relates to compounds of formula (I) which are useful as kinase inhibitors, more specifically useful as PIM kinase inhibitors, thus useful as cancer therapeutics. The invention also relates to compositions, more specifically pharmaceutical compositions comprising these compounds and methods of using the same, either alone or in combination, to treat various forms of cancer and hyperproliferative disorders, as well as methods of using the compounds for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, or associated pathological conditions.Type: GrantFiled: September 8, 2010Date of Patent: May 7, 2013Assignee: F. Hoffmann-La RocheInventors: Xiaojing Wang, Allen J. Ebens, Jr.
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Publication number: 20130109667Abstract: The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: June 28, 2011Publication date: May 2, 2013Applicants: Pfizer Limited, Icagen ,Inc.Inventors: Christopher John Markworth, Brian Edward Marron, David James Rawson, Robert Ian Storer, Nigel Alan Swain, Christopher William West, Shulan Zhou
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Publication number: 20130102637Abstract: Provided is a novel pest control agent using at least one imino derivative represented by the following chemical formula (I):Type: ApplicationFiled: July 4, 2011Publication date: April 25, 2013Applicants: GIFU UNIVERSITY, MEIJI SEIKA PHARMA CO., LTD.Inventors: Shinzo Kagabu, Masaaki Mitomi, Shigeki Kitsuda, Masahiro Nomura, Satoshi Nakamura, Kazumi Yamamoto
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Patent number: 8426604Abstract: The present invention relates to compounds of Formula (I), methods for preparing these compounds, compositions, intermediates and derivatives thereof and for treating a condition including but not limited to ankylosing spondylitis, artherosclerosis, arthritis (such as rheumatoid arthritis, infectious arthritis, childhood arthritis, psoriatic arthritis, reactive arthritis), bone-related diseases (including those related to bone formation), breast cancer (including those unresponsive to anti-estrogen therapy), cardiovascular disorders, cartilage-related disease (such as cartilage injury/loss, cartilage degeneration, and those related to cartilage formation), chondrodysplasia, chondrosarcoma, chronic back injury, chronic bronchitis, chronic inflammatory airway disease, chronic obstructive pulmonary disease, diabetes, disorders of energy homeostasis, gout, pseudogout, lipid disorders, metabolic syndrome, multiple myeloma, obesity, osteoarthritis, osteogenesis imperfecta, osteolytic bone metastasis, osteomalacType: GrantFiled: February 16, 2011Date of Patent: April 23, 2013Assignee: Janssen Pharmaceutica NVInventors: Gilles Bignan, Micheal Gaul, Guozhang Xu, Bao-Ping Zhao
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Publication number: 20130096056Abstract: Methods of treating an SCD-mediated disease or condition in a mammal, preferably a human, are disclosed, wherein the methods comprise administering to a mammal in need thereof a compound of formula (I): where V, W, R1, R2, R3 and R4 are defined herein. Pharmaceutical compositions comprising the compounds of formula (I) are also disclosed.Type: ApplicationFiled: September 14, 2012Publication date: April 18, 2013Applicant: XENON PHARMACEUTICALS INC.Inventors: Jianmin Fu, Duanjie Hou, Rajender Kamboj, Vishnumurthy Kodumuru, Natalia Pokrovskaia, Vandna Raina, Shaoyi Sun, Serguei Sviridov, Zaihui Zhang
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Patent number: 8420827Abstract: Wherein n is an integer of from 0 to 3; R1A is a 5-membered aromatic heterocyclic group containing at least one oxygen atom; R2A is —COR8 (wherein R8 is aryl); R3A is hydrogen or lower alkyl; and R12 represents cycloalkyl, aryl, aralkyl, alicyclic heterocyclic group, aromatic heterocyclic group, alicyclic hetocyclic-alkyl, or aromatic heterocyclic-alkyl, and R1A, R2A, R3A and R12 are individually optionally substituted.Type: GrantFiled: December 6, 2010Date of Patent: April 16, 2013Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takao Nakajima, Masamori Sugawara, Shin-ichi Uchida, Tetsuji Ohno, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Patent number: 8420642Abstract: Novel heterocyclic compounds of the formula I in which R1, R2, R3, R4 and D have the meanings indicated in Claim 1, are activators of glucokinase and can be used for the prevention and/or treatment of Diabetes Typ 1 and 2, obesity, neuropathy and/or nephropathy.Type: GrantFiled: August 13, 2008Date of Patent: April 16, 2013Assignee: Merck Patent GmbHInventors: Lars Thore Burgdorf, Norbert Beier, Johannes Gleitz, Christine Charon, Daniel Cravo
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.