The -c(=x)- Group Is Bonded Directly To The Nitrogen Patents (Class 548/195)
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Publication number: 20120053210Abstract: 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: August 26, 2011Publication date: March 1, 2012Applicant: CalciMedica, Inc.Inventors: Jeffrey P. Whitten, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
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Publication number: 20120046250Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.Type: ApplicationFiled: March 2, 2010Publication date: February 23, 2012Applicant: STEMSYNERGY THERAPEUTICS, INCInventor: Darren Orton
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Patent number: 8119646Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituents, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a carbocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 12, 2007Date of Patent: February 21, 2012Assignee: Bayer CropScience AGInventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
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Patent number: 8119645Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I) wherein T represent a tetrazolyl substituent, A represents a carbo- or heterocycle, L1 and L2 represent various linking groups and Q represents a 5-membered heterocycle, their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 12, 2007Date of Patent: February 21, 2012Assignee: Bayer Cropscience AGInventors: Isabelle Christian, Marie-Claire Grosjean-Cournoyer, Pierre Hutin, Philippe Rinolfi, Arounarith Tuch, Jacky Vidal
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Publication number: 20120015929Abstract: Disclosed herein are compounds of formula (I) wherein R1, R2, R3, R25a, R26a, X, and n are as defined in the specification. Pharmaceutical compositions comprising such compounds, and methods of treating conditions and disorders using such compounds and pharmaceutical compositions are also described.Type: ApplicationFiled: September 26, 2011Publication date: January 19, 2012Applicant: ABBOTT LABORATORIESInventors: Teodozyj Kolasa, Jennifer M. Frost, Meena V. Patel, Steven P. Latshaw, Arturo Perez Medrano, Xueqing Wang, Karin Rose Marie Tietje, Sridhar Peddi, William A. Carroll
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Publication number: 20120015946Abstract: A compound of formula (I): wherein A1, A2, A3, A4, G1, R1, R2, R3, R4, R5a, R5b and R6 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 18, 2010Publication date: January 19, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Peter Renold, Thomas Pitterna, Jerome Yves Cassayre, Myriem El Qacemi
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Publication number: 20120010184Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: September 21, 2011Publication date: January 12, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Alessandra BARTOLOZZI, Angela BERRY, Eugene Richard HICKEY, Markus OSTERMEIER, Doris RIETHER, Achim SAUER, David Smith THOMSON, Lifen WU, Renee M. ZINDELL, Patricia AMOUZEGH, Nigel James BLUMIRE, Stephen Peter EAST, Monika ERMANN, Someina KHOR, Innocent MUSHI
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Publication number: 20110313152Abstract: The present invention provide a tetrazolyl oxime derivative represented by formula (1) (in formula (1), X represents a halogen atom or the like, n1 represents an integer of 0 to 5, A represents a tetrazolyl group, Het represents a group represented by formula (4) or the like, in formula (4), R represents a halogen atom or the like, n2 represents an integer of 0 to 3, Z represents a group represented by formula (a), in formula (a), R50-R53 represents a hydrogen atom or the like, n3 represents an integer of 0 to 2, n4 represents 1 or 2, n5 represents 0 or 1) or salt thereof, and a plant disease control agent containing the same as an active ingredient.Type: ApplicationFiled: February 26, 2010Publication date: December 22, 2011Applicant: Nippon Soda Co., Ltd.Inventors: Syuichi Ito, Kazushige Fujii, Hiroyasu Hosokawa, Ichirou Urihara, Atsunori Isshiki
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Publication number: 20110313002Abstract: The present invention provides novel compounds of formula I, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of metabolic diseases and disorders such as, for example, type II diabetes mellitus.Type: ApplicationFiled: June 9, 2011Publication date: December 22, 2011Inventor: Ramakanth Sarabu
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Publication number: 20110306637Abstract: 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: ApplicationFiled: May 20, 2011Publication date: December 15, 2011Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Sabina Hadida-Ruah, Peter Diederik Jan Grootenhuis, Mark Thomas Miller, Matthew Hamilton
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Publication number: 20110281922Abstract: The present invention relates to the field of drugs associated with treating diabetes. Particularly, the present invention relates to a dipeptidyl peptidase-IV inhibitor having the structure shown by formula (I), which contains amide thiazole structure and has an effect on treating diabetes, and a preparation method and a pharmaceutical composition containing it, as well as use thereof in manufacture of the drugs for treating the diabetes, wherein, R1 is methyl; R2 is phenyl; phenyl, 2-thienyl substituted in a mono-substituted, bi-substituted manner by fluorine and methyl.Type: ApplicationFiled: June 16, 2011Publication date: November 17, 2011Applicant: TIANJIN INSTITUTE OF PHARMACEUTICAL RESEARCHInventors: Guilong ZHAO, Weiren Xu, Yuli Wang, Lida Tang, Yiliang Li, Meixiang Zou, Wei Liu, Hua Shao, Chubing Tan, Peng Liu
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Patent number: 8053581Abstract: The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.Type: GrantFiled: August 15, 2006Date of Patent: November 8, 2011Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.C. ChinaInventors: Song Li, Changbin Guo, Xiancheng Jiang, Junhai Xiao, Zhong Wu
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Publication number: 20110257211Abstract: Small molecule choline kinase inhibitors having the following formula: are provided herein. Also provided herein are pharmaceutical compositions containing Formula I compounds, together with methods of treating cancer, methods of inhibiting choline kinase enzymatic activity, and methods of treating tumors by administering an effective amount of a Formula I compound.Type: ApplicationFiled: December 22, 2010Publication date: October 20, 2011Applicants: ADVANCED CANCER THERAPEUTICS, LLC, UNIVERSITY OF LOUISVILLE RESEARCH FOUNDATION, INC.Inventors: Pooran Chand, Jason A. Chesney, Brian F. Clem, Gilles H. Tapolsky, Sucheta Telang, John O. Trent
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Publication number: 20110251176Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: April 6, 2011Publication date: October 13, 2011Inventor: Xiaojing Wang
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Patent number: 8034819Abstract: A compound, or a pharmaceutically acceptable salt thereof, represented by the formula (1), (wherein, the carbon atom marked with an * is in the R-configuration, R1 represents a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1-C6 alkyl group, or a C1-C6 alkoxy group, R2 represents a C3-C6 cycloalkylsulfanyl group, a C3-C6 cycloalkylsulfinyl group, or a C3-C6 cycloalkylsulfonyl group, and A represents a substituted or unsubstituted heteroaryl group).Type: GrantFiled: March 6, 2008Date of Patent: October 11, 2011Assignees: Kyorin Pharmaceutical Co., Ltd., Teijin Pharma LimitedInventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Kohei Ohata, Tomohiro Ide, Fumiyoshi Kobayashi, Shinji Kobayashi, Kanji Komatsu, Masanori Yamamoto
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Publication number: 20110245239Abstract: Novel isoxazoline compounds and compositions containing the compounds are disclosed. The compounds have pesticidal properties and are suitable for use on non-human animals.Type: ApplicationFiled: December 17, 2009Publication date: October 6, 2011Inventors: Steve Nanchen, Noëlle Gauvry, Thomas Goebel
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Publication number: 20110230477Abstract: The present invention is directed to novel compounds of formula (I) and their use in treating metabolic diseases.Type: ApplicationFiled: December 7, 2009Publication date: September 22, 2011Applicant: Euroscreen S.A.Inventors: Hamid Hoveyda, Cyrille Evangelos Brantis, Guillaume Dutheuil, Ludivine Zoute, Didier Schils, Jerome Bernard
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Publication number: 20110230486Abstract: Compounds, compositions, and methods for modulation of Hec1/Nek2 interaction are provided. Especially preferred compounds disrupt Nek2/Hec1 binding and are therefore useful as chemotherapeutic agent for neoplastic diseases.Type: ApplicationFiled: March 15, 2011Publication date: September 22, 2011Inventors: Johnson Lau, Jiann-Jyh Huang
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Patent number: 8022096Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: GrantFiled: February 25, 2009Date of Patent: September 20, 2011Assignee: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu
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Patent number: 8013241Abstract: Disclosed is a novel ionic liquid gel electrolyte having high photoelectric conversion efficiency. Also disclosed are a novel dye-sensitized photoelectric conversion device using such an ionic liquid gel electrolyte, and a solar cell composed of such a dye-sensitized photoelectric conversion device. Specifically disclosed is an ionic liquid gel electrolyte obtained by gelling a liquid electrolyte by using an ionic organic oligomer gelling agent represented by the general formulae (1) and (2) below. Also specifically disclosed are a dye-sensitized photoelectric conversion device, wherein the ionic liquid gel electrolyte is arranged between a counter electrode and a dye-absorbed semiconductor substrate which is arranged in contact with a transparent conductive substrate, and a solar cell.Type: GrantFiled: October 16, 2006Date of Patent: September 6, 2011Assignee: National Institute of Advanced Industrial Science and TechnologyInventors: Nagatoshi Koumura, Koujirou Hara, Zhong-Sheng Wang, Masaru Yoshida, Nobuyuki Tamaoki
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Publication number: 20110212994Abstract: Small molecule choline kinase inhibitors, pharmaceutical compositions thereof, and screening methods for identifying and evaluating choline kinase inhibitors are provided. Safe and effective methods for treating subjects suffering from a disorder or disease characterized by neoplastic cell proliferation employing the choline kinase inhibitors are also provided.Type: ApplicationFiled: June 28, 2010Publication date: September 1, 2011Inventors: BRIAN CLEM, SUCHETA TELANG, JOHN TRENT, JASON CHESNEY, POORAN CHAND, GILLES TAPOLSKY
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Publication number: 20110201613Abstract: The present invention relates to hydroximoyl-tetrazole derivatives of formula (I), their process of preparation, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions. wherein A represents a tetrazoyl group, Het represents a pyridyl group or a thiazolyl group and X represents various substituents.Type: ApplicationFiled: July 3, 2009Publication date: August 18, 2011Inventors: Christian Beier, Jürgen Benting, David Bernier, Isabelle Christian, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Patent number: 7999113Abstract: The present invention relates to modulators of cystic fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating CFTR mediated diseases using such modulators.Type: GrantFiled: August 11, 2006Date of Patent: August 16, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sarah Hadida-Ruah, Frederick Van Goor, Mark Miller, Jason McCartney, Jinglan Zhou, Vijayalaksmi Arumugam
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Publication number: 20110190351Abstract: Benzoimidazole Derivatives are provided. The compounds of the present invention are useful for Glycogen Synthase Kinase-3 Beta Inhibitors.Type: ApplicationFiled: July 30, 2009Publication date: August 4, 2011Applicant: Oncotherapy Science, Inc.Inventors: Mitsuaki Ohtani, Yo Matsuo, Yingfu Li, Joel R. Walker, David M. Jenkins, Feryan Ahmed, Ryuji Ohsawa, Shoji Hisada
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Patent number: 7973169Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including CF Transmembrane 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: September 7, 2004Date of Patent: July 5, 2011Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Mark T. Miller, Ashvani K. Singh, Thomas Cleveland, Lewis R. Makings, Matthew Hamilton, Peter D. J. Grootenhuis
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Patent number: 7973061Abstract: The present invention relates to compounds of the Formula I, wherein L, X, Y, Z, R1, R2, R3 and R4 are defined herein. The invention also provides methods of using the compounds for inhibition of kinases, more specifically ALK kinases. The invention provides compounds for modulating protein kinase enzymatic activity for modulating cellular activities such as proliferation, differentiation, programmed cell death, migration and chemoinvasion. Compounds of the invention inhibit, regulate and/or modulate kinase receptor signal transduction pathways related to the changes in cellular activities as mentioned above, and the invention includes compositions which contain these compounds, and methods of using them to treat kinase-dependent diseases and conditions; (Formula I).Type: GrantFiled: March 31, 2005Date of Patent: July 5, 2011Assignee: Exelixis, Inc.Inventors: James William Leahy, Gary Lee Lewis, John M. Nuss, Brain Hugh Ridgway, Joan C. Sangalang
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Publication number: 20110160211Abstract: A compound having a hypoglycemic effect is provided. The compound and a pharmaceutically acceptable salt thereof are useful for the treatment or prevention of diabetes, obesity, and the like. The compound is represented by the general formula (1): (wherein R1 and R2 are each independently a hydrogen atom, a halogen atom, an amino group, a hydroxyl group, a hydroxyamino group, a nitro group, a cyano group, a sulfamoyl group, a C1 to C6 alkyl group, a C1 to C6 alkoxy group, a C1 to C6 alkylsulfanyl group, a C1 to C6 alkylsulfinyl group, a C1 to C6 alkylsulfonyl group, or a C1 to C6 alkoxy-C1 to C6 alkylsulfonyl group, and A is a substituted or unsubstituted heteroaryl group).Type: ApplicationFiled: April 27, 2009Publication date: June 30, 2011Inventors: Yasumichi Fukuda, Yoshikazu Asahina, Masanori Takadoi, Masanori Yamamoto
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Patent number: 7968577Abstract: Novel non-steroidal compounds are provided which are useful in treating diseases associated with modulation of the glucocorticoid receptor, AP-1, and/or NF-?B activity including inflammatory and immune diseases, obesity and diabetes having the structure of formula (I) an enantiomer, diastereomer, tautomer, solvate (e.g.Type: GrantFiled: October 31, 2007Date of Patent: June 28, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Bingwei Vera Yang, Lidia M. Doweyko, Wayne Vaccaro, Tram N. Huynh, David R. Tortolani, T. G. Murali Dhar
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Publication number: 20110152236Abstract: The invention relates to compounds of the formula (I) where: R is a (C1-C6)alkyl group, a halo(C1-C6)alkyl group; R1 is a hydrogen atom; R2 is a heteroaromatic group or a heteroaromatic(C1-C4)alkyl group, said groups being optionally substituted; R3 and R4 represent independently from each other an optionally substituted phenyl group; Y is a hydrogen atom, a halogen, a cyano, a (C1-C6)alkyl group, a halo(C1-C6)alkyl group, a (C1-C6)alkoxy group, a halo(C1-C6)alkoxy group or a (C1-C6)alkylS(O)p group; and p is 0 to 2. Said compounds can be in the form— of a base or a salt for addition to an acid. The invention also relates to a method for preparing same and to the therapeutic application thereof.Type: ApplicationFiled: August 13, 2009Publication date: June 23, 2011Applicant: SANOFI-AVENTISInventors: Patrick Bernardelli, Jean-Francois Sabuco, Corinne Terrier
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Publication number: 20110152533Abstract: The present invention provides prodrugs of compounds that inhibit the activity of plasma kallikrein (PK) and methods of preventing and treating plasma kallikrein dependent diseases or conditions, for example, diabetic macular edema, with the prodrugs having the formula:Type: ApplicationFiled: December 17, 2010Publication date: June 23, 2011Applicant: Activesite Pharmaceuticals, Inc.Inventors: Sukanto Sinha, Tamie Jo Chilcote
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Patent number: 7956076Abstract: Provided herein are novel compounds that inhibit ribonucleotide reductase (RR) by binding to RRM2 and interfering with the activity of the RRM1/RRM2 holoenzyme. These inhibitors may be used to inhibit RR activity and to treat various conditions associated with RRM2 expression, such as for example certain cancer types, mitochondrial diseases, or degenerative diseases.Type: GrantFiled: April 8, 2009Date of Patent: June 7, 2011Assignee: City of HopeInventors: Yun Yen, David Horne, Yate-Ching Yuan, Bing-Sen Zhou, Angela L Perkins Harki, Leila Su
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Publication number: 20110130397Abstract: Provided herein are compounds that modulate the activity of a bacterial peptidyl tRNA hydrolase, including compositions and dosage forms comprising the compounds. Further provided herein are methods for preventing or inhibiting bacterial proliferation as well as methods for preventing, treating, and/or managing a bacterial infection using such compounds and compositions.Type: ApplicationFiled: September 21, 2007Publication date: June 2, 2011Inventors: Soongyu Choi, Arthur Branstrom, Scott A. Gothe, Richard Lipman, Tamil Arasu, Richard G. Wilde
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Publication number: 20110130402Abstract: The present invention describes 2,3-di-substituted N-heteroaromatic propionamides, wherein the substitution at the 3-position is an optionally substituted phenyl ring and the substitution at the 2-position is an alkyl or cycloalkyl group; pharmaceutical compositions comprising the same; and, methods of using the same. The propionamides are glucokinase activators which increase insulin secretion for the treatment of type II diabetes.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: Novo Nordisk A/SInventors: Lone Jeppesen, Marit Kristiansen
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Publication number: 20110130431Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 8, 2011Publication date: June 2, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Angela BERRY, Pier Francesco CIRILLO, Eugene Richard HICKEY, Doris RIETHER, David THOMSON, Renee M. ZINDELL, Nigel BLUMIRE, Chandana CHOWDHURY, Monika ERMANN, James Edward JENKINS, Innocent MUSHI, Christopher Francis PALMER, Malcolm TAYLOR
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Publication number: 20110118236Abstract: An object of the present invention is to provide a novel AMPA receptor potentiator. A compound represented by the following formula (I) or a salt thereof: wherein in formula (I) R1 represents (1) a halogen atom, or (2) cyano group, or the like; Ra and Rb each independently represent a hydrogen atom or C1-4 alkyl; L represents a bond, or a spacer in which the number of atoms in the main chain is 1 to 8; Ring A represents (1) a non-aromatic carbon ring of 4-8 carbon atoms, or (2) a 4- to 8-membered non-aromatic heterocycle either of which is optionally substituted with 1 or more substituents selected from (a) halogen atoms, and (b) cyano group; and Ar represents a substituted phenyl group, or optionally substituted 5- or 6-membered aromatic heterocyclic group.Type: ApplicationFiled: March 25, 2009Publication date: May 19, 2011Inventors: Michiyo Mochizuki, Shotaro Miura
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Publication number: 20110112080Abstract: The invention relates to compounds of formula I wherein the definitions of X, R and R1 are as defined herein. The compounds of formula I have a good affinity to the trace amine associated receptors (TAARs), especially for TAAR1. The compounds can be used for the treatment of depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder (ADHD), stress-related disorders, psychotic disorders such as schizophrenia, neurological diseases such as Parkinson's disease, neurodegenerative disorders such as Alzheimer's disease, epilepsy, migraine, hypertension, substance abuse and metabolic disorders such as eating disorders, diabetes, diabetic complications, obesity, dyslipidemia, disorders of energy consumption and assimilation, disorders and malfunction of body temperature homeostasis, disorders of sleep and circadian rhythm, and cardiovascular disorders.Type: ApplicationFiled: November 3, 2010Publication date: May 12, 2011Inventors: Guido Galley, Roger Norcross, Alessandra Polara
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Publication number: 20110112073Abstract: The present invention relates to HSF activating compounds, methods for their discovery, and their research and therapeutic uses, as well as pharmaceutically acceptable salts, solvates, chelates, non-covalent complexes, prodrugs, mixtures (including both R and S enantiomeric forms and racemic mixtures thereof), and pharmaceutical Formulations thereof. In particular, the present invention provides compounds capable of facilitating HSF1 homotrimerization, and methods of using such compounds as therapeutic agents to treat a number of conditions associated with irregular HSF1 activity.Type: ApplicationFiled: November 12, 2010Publication date: May 12, 2011Applicant: DUKE UNIVERSITYInventors: Dennis J. Thiele, Daniel W. Neef, Jose S. Mendoza
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Patent number: 7928123Abstract: Compounds of formula (I) are disclosed. Compounds according to the invention bind to and are agonists, antagonists or inverse agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: GrantFiled: September 13, 2007Date of Patent: April 19, 2011Assignee: Boehringer Ingelheim International GmbHInventors: Angela Berry, Pier Francesco Cirillo, Doris Riether, David Thomson, Renee M. Zindell, Nigel Blumire, Chandana Chowdhury, Monika Ermann, James Edward Jenkins, Innocent Mushi, Christopher Francis Palmer, Malcolm Taylor
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Publication number: 20110082144Abstract: This invention relates to compounds that are activators of glucokinase and thus may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial. The compounds are of the general formula (I) wherein A and B are further defined in the application.Type: ApplicationFiled: September 30, 2010Publication date: April 7, 2011Applicant: TransTech Pharma, Inc.Inventors: Jesper F. Lau, Per Vedsø, János Tibor Kodra, Anthony Murray, Lone Jeppesen, Michael Ankersen, Govindan Subramanian, Adnan M. M. Mjalli, Robert Carl Andrews, Dharma Rao Polisetti, Daniel Peter Christen
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Publication number: 20110077265Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds having the general formula U1-M-U2 wherein M is a linking group covalently joining R2, R3, R4 or R5 of U1 to an R2, R3, R4 or R5 group of U2; U1 and U2 have the general formula (I) and G, X1, X2, R2, R3, R3?, R4, R4? and R5, are as described herein.Type: ApplicationFiled: April 29, 2008Publication date: March 31, 2011Applicant: Genentech, Inc.Inventors: John A. Flygare, Frederick Cohen, Kurt Deshayes, Michael F. T. Koehler, Lewis J. Gazzard, Lan Wang, Chudi Ndubaku
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Publication number: 20110071113Abstract: The present invention is related to thiazole derivatives of Formula (I) in particular for the treatment and/or prophylaxis of autoimmune disorders and/or inflammatory diseases, cardiovascular diseases, neurodegenerative diseases, bacterial or viral infections, kidney diseases, platelet aggregation, cancer, transplantation, graft rejection or lung injuries.Type: ApplicationFiled: November 23, 2010Publication date: March 24, 2011Applicant: MERCK SERONO SAInventors: Anna Quattropani, David Covini, Vincent Pomel, Jérôme Dorbais, Thomas Rueckle
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Patent number: 7910613Abstract: The Invention relates to compounds of the formula I, wherein the variables are as defined in the claims, for use as a medicament. The compounds are A2A-receptor legends and are useful in the treatment of neurological and psychiatric disorders where an A2A-receptor is implicated.Type: GrantFiled: September 20, 2005Date of Patent: March 22, 2011Assignee: H. Lundbeck A/SInventors: Mogens Larsen, Annette Graven Sams, Gitte Mikkelsen, Benny Bang-Andersen
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MODULATORS OF THE PROSTACYCLIN (PGI2) RECEPTOR USEFUL FOR THE TREATMENT OF DISORDERS RELATED THERETO
Publication number: 20110053958Abstract: The present invention relates to amide derivatives of Formula (XIIIa) and pharmaceutical compositions thereof that modulate the activity of the PGI2 receptor.Type: ApplicationFiled: March 17, 2009Publication date: March 3, 2011Applicant: ARENA PHARMACEUTICALS, INC.Inventors: Thuy-Anh Tran, Weichao Chen, Bryan A. Kramer, Abu J.M. Sadeque, Anna Shifrina, Young-Jun Shin, Pureza Vallar, Ning Zou -
Publication number: 20110053955Abstract: Heterocyclic compounds which are inhibitors of Mitrogen-Activated Protein Kinase-Activated Protein Kinase-2 (MAPKAP-K2) as described, in addition to their use in the treatment of cytokine mediated diseases.Type: ApplicationFiled: February 7, 2008Publication date: March 3, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Denise Andersen, Tina Marie Morwick, Roger John Snow, Yancey David Ward
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Patent number: 7897628Abstract: This invention relates to aryl carbonyl derivatives which are activators of glucokinase which may be useful for the management, treatment, control, or adjunct treatment of diseases, where increasing glucokinase activity is beneficial.Type: GrantFiled: October 31, 2007Date of Patent: March 1, 2011Assignee: Novo Nordisk A/SInventors: Dharma Rao Polisetti, Janos Tibor Kodra, Jesper Lau, Paw Bloch, Maria Carmen Valcarce Lopez, Niels Blume, Mustafa Guzel, Kalpathy Chidambareswaran Santhosh, Adnan M.M. Mjalli, Robert Carl Andrews, Govindan Subramanian, Michael Ankersen, Per Vedso, Anthony Murray, Lone Jeppesen
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Publication number: 20110034432Abstract: Compounds of Formula (I): wherein: R1 is methoxymethyl; R2 is selected from —C(O)NR4R5, —SO2NR4R5, —S(O)pR4 and HET-2; HET-1 is a 5- or 6-membered, optionally substituted C-linked heteroaryl ring; HET-2 is a 4-, 5- or 6-membered, C- or N-linked optionally substituted heterocyclyl ring; R3 is selected from halo, fluoromethyl, difluoromethyl, trifluoromethyl, methyl, methoxy and cyano; R4 is selected from for example hydrogen, optionally substituted (1-4C)alkyl and HET-2; R5 is hydrogen or (1-4C)alkyl; or R4 and R5 together with the nitrogen atom to which they are attached may form a heterocyclyl ring system as defined by HET-3; HET-3 is for example an optionally substituted N-linked, 4, 5 or 6 membered, saturated or partially unsaturated heterocyclyl ring; p is (independently at each occurrence) 0, 1 or 2; m is 0 or 1; n is 0, 1 or 2; provided that when m is 0, then n is 1 or 2; or a salt, pro-drug or solvate thereof, are described.Type: ApplicationFiled: March 12, 2010Publication date: February 10, 2011Applicant: AstraZeneca ABInventors: Craig JOHNSTONE, Darren MCKERRECHER, Kurt Gordon PIKE
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Patent number: 7880013Abstract: (Wherein n is an integer of from 0 to 3; R1 is substituted or unsubstituted cycloalkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, or a substituted or unsubstituted aromatic heterocyclic group; R2 is halogen, substituted or unsubstituted lower alkyl, substituted or unsubstituted aryl, a substituted or unsubstituted alicyclic heterocyclic group, a substituted or unsubstituted aromatic heterocyclic group, —COR8, or the like; R3 and R4 may be the same or different, and each represents a hydrogen atom, substituted or unsubstituted lower alkyl, substituted or unsubstituted aralkyl, —COR12, or the like) For example, provided are adenosine A2A receptor antagonists comprising, as the active ingredient, a thiazole derivative represented by a general formula (I), or a pharmaceutically acceptable salt thereof, and the like.Type: GrantFiled: April 26, 2010Date of Patent: February 1, 2011Assignee: Kyowa Hakko Kirin Co., Ltd.Inventors: Takao Nakajima, Masamori Sugawara, Yuji Nomoto, Noriaki Uesaka, Yoshisuke Nakasato
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Publication number: 20110021480Abstract: Substituted steroid compounds which represent selective inhibitors of 17?-hydroxysteroid dehydrogenase type I (17?-HSD1) and, in addition, which may represent inhibitors of the steroid sulfatase, salts thereof, pharmaceutical preparations containing these compounds, and a process for the preparation of these compounds. Also disclosed is a therapeutic method of using such substituted steroid compounds, particularly in the treatment, inhibition, prophylaxis or prevention of steroid hormone dependent diseases or disorders, such as steroid hormone dependent diseases or disorders requiring the inhibition of 17?-hydroxysteroid dehydrogenase type I and/or steroid sulfatase enzymes and/or requiring lowering of the endogenous 17?-estradiol concentration.Type: ApplicationFiled: September 28, 2010Publication date: January 27, 2011Applicant: Solvay Pharmaceuticals GmbHInventors: Josef Messinger, Heinrich-Hubert Thole, Bettina Husen, Michael Weske, Pasi Koskimies, Lila Pirkkala
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Publication number: 20110021582Abstract: Disclosed are a novel thiazole-containing benzophenone derivative represented by formula 1, and an isomer thereof, a pharmaceutically acceptable salt thereof, a hydrate thereof and a solvate thereof, a pharmaceutical composition comprising the derivative, a use of the derivative as therapeutic agent and a method for preparing the derivative. The benzophenone thiazole derivatives inhibit formation of microtubules and eliminate actively proliferating cells of malignant tumors to control general cell proliferation. In formula 1, R, R1 and R2 are defined as above.Type: ApplicationFiled: March 5, 2009Publication date: January 27, 2011Applicant: CHONG KUN DANG PHARMACEUTICAL CORP.Inventors: Nam-Song Choi, Young-Hoon Kim, Jae-Kwang Lee, Hee-Ryong Kang, Ho-Jin Choi, Seung-Kee Moon, Soo-Jin Kim, Gyu-Tae Park, Byeong-Hoon Han, Dal-Hyun Kim, Jae-Hoon Choi, Sung-Sook Lee, Soon-Kil Ahn, Kyung-Joo Lee, Su-Yeal Bae