C=x Bonded Directly To The Nitrogen Which Is Bonded Directly To The Thiazole Ring (x Is Chalcogen) Patents (Class 514/371)
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Patent number: 8404859Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: GrantFiled: February 17, 2012Date of Patent: March 26, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Patent number: 8399484Abstract: The present invention relates to therapeutic combinations comprising (a) Compound (1), or a pharmaceutically acceptable salt thereof, as herein described, (b) an interferon alfa and (c) ribavirin. Compound (1) is a selective and potent inhibitor of the HCV NS3 serine protease. The present invention also relates to methods of using such therapeutic combinations for treating HCV infection or alleviating one or more symptoms thereof in a patient.Type: GrantFiled: September 16, 2009Date of Patent: March 19, 2013Assignee: Boehringer Ingelheim International GmbHInventors: David Huang, Gerhard Gustav Steinmann, Jerry Oscar Stern
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Patent number: 8394843Abstract: Compounds are provided which have the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture which contain such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to activate glucokinase.Type: GrantFiled: July 18, 2011Date of Patent: March 12, 2013Assignee: Takeda California, Inc.Inventors: Jun Feng, Stephen L. Gwaltney, Robert J. Skene, Mingnam Tang, Sheldon X. Cao, David J. Hossfield, Jeffrey A. Stafford
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Publication number: 20130059896Abstract: Inhibitors of LIM kinase 2 are disclosed, along with pharmaceutical compositions comprising them and methods of their use.Type: ApplicationFiled: January 21, 2011Publication date: March 7, 2013Inventors: Nicole Cathleen Goodwin, David Brent Rawlins
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Publication number: 20130045982Abstract: Disclosed are benzamide derivatives useful in slowing the expansion of cancer cells including the killing of cancer cells and in the treatment of cancer.Type: ApplicationFiled: December 17, 2010Publication date: February 21, 2013Applicant: THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTEInventors: Tong Wang, Stephen Gately
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Publication number: 20130045967Abstract: The application describes an assay for the identification of small molecule modulators of integrin CD11b/CD18 and small molecules capable of modulating activity of this receptor. Such compounds may be used in certain embodiments for treating a disease or condition selected from inflammation, immune-related disorders, cancer, ischemia-reperfusion injury, stroke, neointimal thickening associated with vascular injury, bullous pemphigoid, neonatal obstructive nephropathy, and cardiovascular disease, or in other embodiments for the treatment of a disease or condition selected from immune deficiency, acquired immune deficiency syndrome (AIDS), myeloperoxidase deficiency, Wiskott-Aldrich syndrome, chronic granulomatous disease, hyper-IgM syndromes, leukocyte adhesion deficiency, Chediak-Higashi syndrome, and severe combined immunodeficiency.Type: ApplicationFiled: September 13, 2012Publication date: February 21, 2013Inventors: Vineet Gupta, M. Amin Arnaout
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Publication number: 20130040994Abstract: The present invention includes a crystal comprising a complex of the pro form of a matrix metalloprotease (proMMP) and a small-molecule allosteric processing inhibitor that inhibits that activation of the proMMP, methods for identifying small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP, and methods of treatment using small-molecule allosteric processing inhibitors that inhibit the activation of a proMMP. The present invention relates to the crystal structure of a complex of proMMP9 bound to a small-molecule allosteric processing inhibitor that inhibits activation of proMMP9. The invention further relates to the use of the methods and the crystal and related structural information for designing, selecting and/or optimizing small-molecule allosteric processing inhibitors that inhibit activation of proMMP9 and proMMP9 homologues.Type: ApplicationFiled: June 26, 2012Publication date: February 14, 2013Inventors: Kristi A. Leonard, Richard Scott Alexander, Joseph Kent Barbay, Roger F. Bone, Carl Crysler, Ingrid Christa Deckman, Paul F. Jackson, Lawrence C. Kuo, Frank A. Lewandowski, Diane M. Maguire, Carl Manthey, Cynthia M. Milligan, Beverley Moore, Kenneth J. Rhodes, Robert H. Scannevin, Celine Schalk-Hihi, Barry Springer, John C. Spurlino, Matthew J. Todd, Brett Andrew Tongue, Aihua Wang
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Patent number: 8362267Abstract: 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: GrantFiled: March 5, 2009Date of Patent: January 29, 2013Assignee: 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
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Publication number: 20130023463Abstract: A compound of the formula is disclosed as an HIV protease inhibitor. Methods and compositions for inhibiting an HIV infection are also disclosed.Type: ApplicationFiled: April 19, 2012Publication date: January 24, 2013Applicant: ABBOTT LABORATORIESInventors: Charles A. Flentge, Hui-Ju Chen, David A. DeGoey, William J. Flosi, David J. Grampovnik, Peggy P. Huang, Dale J. Kempf, Larry L. Klein, Allan C. Krueger, Darold L. Madigan, John T. Randolph, Minghua Sun, Ming C. Yeung, Chen Zhao
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Publication number: 20130019348Abstract: This document discloses molecules having the following formula (“Formula One”) The molecules disclosed in this document are related to the field of processes to produce molecules that are useful as pesticides (e.g., acaricides, insecticides, molluscicides, and nematicides), such molecules, and processes of using such molecules to control pests.Type: ApplicationFiled: July 11, 2012Publication date: January 17, 2013Applicant: DOW AGROSCIENCES LLCInventors: Gary D. Crouse, David A. Demeter, Thomas C. Sparks, Nick X. Wang, William H. Dent, III, Carl Deamicis, Noormohamed M. Niyaz, Erich W. Baum, Lindsey G. Fischer, Natalie C. Giampietro
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Publication number: 20130012546Abstract: 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: December 28, 2010Publication date: January 10, 2013Inventors: Christian Beier, Jurgen Benting, David Bernier, Pierre-Yves Coqueron, Philippe Desbordes, Christophe Dubost, Stephanie Gary, Pierre Genix, Daniela Portz, Ulrike Wachendorff-Neumann
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Patent number: 8349880Abstract: The present disclosure provides a series of compounds of the formula (I) which reduce ?-amyloid peptide (?-AP) production and are useful in the treatment of Alzheimer's Disease and other conditions affected by ?-amyloid peptide (?-AP) production.Type: GrantFiled: January 7, 2010Date of Patent: January 8, 2013Assignee: Bristol-Myers Squibb CompanyInventors: Lawrence R. Marcin, Lorin A. Thompson, III, Kenneth M. Boy, Jason M. Guernon, Mendi A. Higgins, Jianliang Shi, Yong-Jin Wu, Yunhui Zhang, John E. Macor
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Patent number: 8349871Abstract: 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 21, 2011Date of Patent: January 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Alessandra Bartolozzi, Angela Berry, Eugene Richard Hickey, 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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Patent number: 8344153Abstract: 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: GrantFiled: June 9, 2010Date of Patent: January 1, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin Michael Cottrell, Alex Aronov, Robert J. Davies, Jon H. Come, David Messersmith, Jinwang Xu, Upul Keerthi Bandarage, Jingrong Cao
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Patent number: 8338467Abstract: 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: GrantFiled: September 26, 2011Date of Patent: December 25, 2012Assignee: AbbVie Inc.Inventors: 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: 20120322761Abstract: Compounds of formula Ia and Ib wherein A, B, C and R1 are described herein.Type: ApplicationFiled: August 29, 2012Publication date: December 20, 2012Inventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20120322786Abstract: A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Thomas H. Jozafiak, Frederic Vinick, Yibin Xiang, John Kane, Junkai Liao
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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: 20120309794Abstract: The present invention concerns compounds, some of which are novel, and their pharmaceutical applications. The compounds of the invention inhibit the enzyme lactate dehydrogenase (LDH) involved both in the metabolic process of hypoxic tumour cells, and in the process used by parasitic protozoa that cause malaria to obtain most of the energy they need.Type: ApplicationFiled: November 5, 2010Publication date: December 6, 2012Applicant: UNIVERSITÀ DI PISAInventors: Filippo Minutolo, Marco Macchia, Carlotta Granchi, Sarabindu Roy, Gino Giannaccini, Antonio Lucacchini
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Patent number: 8324396Abstract: The present invention relates generally to compounds represented in Formula I, pharmaceutical compositions comprising them and methods of treating of diseases or disorders related to the function of the calcium sensing receptor. The invention also relates to processes for making such compounds and to intermediates useful in these processes.Type: GrantFiled: July 10, 2008Date of Patent: December 4, 2012Assignee: Amgen Inc.Inventors: Pierre Deprez, Christopher Fotsch, Paul Harrington, Sarah Lively, Kanaka Pattabiraman, David St. Jean, Taoues Temal-Laib
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Publication number: 20120302573Abstract: This invention relates to methods for preventing, treating or ameliorating an MMP9 and/or MMP13 mediated syndrome, disorder or disease comprising administering to a subject in need thereof an effective amount of a compound listed in the examples section of this specification, or a form, composition or medicament thereof. Disorders treated and/or prevented include rheumatoid arthritis.Type: ApplicationFiled: May 24, 2012Publication date: November 29, 2012Inventors: Paul Francis JACKSON, Carl Manthey, Kenneth Rhodes, Robert Scannevin, Kristi Anne Leonard, Joseph Kent Barbay, Matthew Todd, Barry A. Springer
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Patent number: 8318728Abstract: Compounds and compositions for treating injuries caused by exposure to chemical warfare agents are described herein.Type: GrantFiled: May 14, 2009Date of Patent: November 27, 2012Assignee: Hydra Biosciences, Inc.Inventor: Jayhong A. Chong
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120283255Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 27, 2012Publication date: November 8, 2012Inventors: Pierre DEPREZ, Hélène Jary, Taoues Temal
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Publication number: 20120283268Abstract: Thiazole and thiophene compounds are disclosed having utility in treating inflammatory conditions, immunoinflammatory conditions, autoimmune diseases, and cancers. Methods for the synthesis of these compounds are also disclosed.Type: ApplicationFiled: June 15, 2012Publication date: November 8, 2012Inventors: Anthony Giordano, Kamala K. Vasu, Hardik M. Thakar, Rajan S. Giri, Vasudevan Sudarsanam, Swapnil G. Yerande, Gajanan S. Inamdar
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Patent number: 8304403Abstract: Compounds of formula Ia and Ib and wherein A, B, C and R1 are described herein.Type: GrantFiled: June 10, 2010Date of Patent: November 6, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Mark E. Salvati, Heather Finlay, Bang-Chi Chen, Lalgudi S. Harikrishnan, Ji Jiang, James A. Johnson, Muthoni G. Kamau, R. Michael Lawrence, Jianqing Li, John Lloyd, Michael M. Miller, Zulan Pi, Jennifer X. Qiao, Richard A. Rampulla, Jacques Y. Roberge, Tammy C. Wang, Yufeng Wang, Wu Yang
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Publication number: 20120276111Abstract: The invention relates generally to methods and compositions for treating conditions associated with angiogenesis, and, more specifically, the invention relates to methods and compositions for treating conditions associated with angiogenesis using vascular adhesion protein-1 (VAP-1) inhibitors. The invention also relates to methods and compositions for treating conditions associated with lymphangiogenesis using VAP-1 inhibitors.Type: ApplicationFiled: November 30, 2011Publication date: November 1, 2012Inventor: Ali Hafezi-Moghadam
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Publication number: 20120270914Abstract: A split luciferase-based sensor system was developed to noninvasively monitor and image phosphorylation-mediated c-Myc activation, in which the complementation of the split FL is induced by phosphorylation-mediated interaction between GSK3? and c-Myc. The complemented luciferase activity resulting from this interaction is specific to c-Myc phosphorylation and correlated with the steady-state and temporal regulation of c-Myc phosphorylation in cell culture. The sensor system also allows monitoring of c-Myc—targeted drug efficacy in intact cells and living animals. This new imaging sensor can provide insight into the role of functional c-Myc in cancer biology and is useful for the discovery and development of specific anti-c-Myc drugs.Type: ApplicationFiled: April 25, 2012Publication date: October 25, 2012Applicant: THE BOARD OF TRUSTEES OF THE LELAND STANFORD JUNIOR UNIVERSITYInventors: Hua Fan-Minogue, Sanjiv S. Gambhir
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Patent number: 8293753Abstract: The present invention relates to compounds of formula I and salts thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameliorated by inhibition of phosphatidylinositol 3-kinase.Type: GrantFiled: June 28, 2010Date of Patent: October 23, 2012Assignee: Novartis AGInventors: Robin Alec Fairhurst, Pascal Furet, Marc Gerspacher, Robert Mah
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Patent number: 8293919Abstract: The present invention provides novel sulfone and sulfoxide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and methods of production are provided.Type: GrantFiled: July 23, 2008Date of Patent: October 23, 2012Assignee: Crestone, Inc.Inventors: Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
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Publication number: 20120263712Abstract: The present invention relates to a compound of formula (I) or a salt thereof, wherein the substituents are as defined in the description, to compositions and use of the compounds in the treatment of diseases ameloriated by inhibition of phosphatidylinositol 3-kinase.Type: ApplicationFiled: June 5, 2012Publication date: October 18, 2012Applicant: NOVARTIS AGInventors: Robin Alec FAIRHURST, Vito GUAGNANO, Patricia IMBACH, Giorgio CARAVATTI, Pascal FURET
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Publication number: 20120263659Abstract: The invention relates to a TRPM8 modulator for achieving a cooling effect on the skin or a mucous membrane.Type: ApplicationFiled: November 22, 2010Publication date: October 18, 2012Applicants: BASF SE, SYMRISE AGInventors: Thomas Subkowski, Michael Backes, Heiko Oertling, Arnold Machinek, Hubert Loges, Ulrike Simchen, Horst Surburg, Claus Bollschweiler, Jens Wittenberg, Wolfgang Siegel
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Publication number: 20120252759Abstract: Compounds of the formula Ia and Ib, in which R1, R1?, R2, R3, R5, R6 and R7 have the meanings indicated in claim 1, are kinase inhibitors and can be employed, inter alia, for the treatment of tumours.Type: ApplicationFiled: November 9, 2010Publication date: October 4, 2012Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKER HAFTINGInventors: Timo Heinrich, Hannes Koolman
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Publication number: 20120238569Abstract: Provided herein are compounds of the formula (I): as well as pharmaceutically acceptable salts thereof, wherein the substituents are as those disclosed in the specification. These compounds, and the pharmaceutical compositions containing them, are useful for the treatment of inflammatory diseases and disorders such as, for example, asthma and COPD.Type: ApplicationFiled: February 17, 2012Publication date: September 20, 2012Inventors: Paul Gillespie, Christophe Michoud, Kenneth Carey Rupert, Kshitij Chhabilbhai Thakkar
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Patent number: 8268818Abstract: 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: GrantFiled: September 4, 2007Date of Patent: September 18, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Tiansheng Wang, Jeremy Green, Brian Ledford, François Maltais, Andreas P. Termin, Mark Cornebise, Jonathan Parsons, Adam Tanner, James Westcott
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Publication number: 20120225887Abstract: Compounds are provided for use with glucokinase that comprise the formula: wherein the variables are as defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.Type: ApplicationFiled: April 10, 2012Publication date: September 6, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Zacharia Cheruvallath, Stephen L. Gwaltney, Andrew John Jennings, Mark Sabat, Jeffrey A. Stafford, Mingnam Tang, Haxia Wang
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Publication number: 20120214786Abstract: 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. A, M, W, R1, R2, R6, R7, R8 have meanings given in the description.Type: ApplicationFiled: August 17, 2011Publication date: August 23, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Benjamin PELCMAN, Robert ROENN
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Publication number: 20120214808Abstract: A method of treating a condition associated with the CB-1 receptor, in particular obesity, by administering an effective amount of an aryl urea CB-1 receptor modulating compound to a subject in need of such treatment.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Prosidion LimitedInventors: Jason Bloxham, Matthew Colin Thor Fyfe, James Horswill, Revathy Perpetua Jeevaratnam, John Keily, Martin James Procter, Karen Lesley Schofield, Salam Shaaban, Simon Andrew Swain, Philippe Wong-Kai-In
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Publication number: 20120214735Abstract: Acetamide derivatives, their stereoisomers, tautomers, prodrugs, pharmaceutically acceptable salts, polymorphs, solvates and formulations thereof for the prophylaxis, management, treatment, control of progression, or adjunct treatment of diseases and/or medical conditions where the activation of glucokinase would be beneficial, are disclosed. The disclosure also provides process of preparation of these acetamide derivatives.Type: ApplicationFiled: February 17, 2012Publication date: August 23, 2012Applicant: Advinus Therapeutics LimitedInventors: Debnath Bhuniya, Anil Deshpande, Sachin Kandalkar, Balasaheb Kobal, Santosh Kurhade, Vinod Vyavahare, Rahul Kaduskar
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Publication number: 20120207826Abstract: There is disclosed herein a composition for treating extracellular parasitic infections, the composition comprising one or more of the following combinations: at least one quinolone or fluoroquinolone together with at least one tetracycline, iodoquinol, an azole or imidazole; or at least two agents selected from the group consisting of iodoquinol, thiazolidones, tetracycline, nitroimidazoles, cotrimoxazole and diloxanide furoate.Type: ApplicationFiled: October 22, 2010Publication date: August 16, 2012Inventors: Thomas Julius Borody, Soledad Carsula
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Patent number: 8236835Abstract: The present invention provides heterocyclic derivatives that modulate the activity of stearoyl-CoA desaturase. Methods of using such derivatives to modulate the activity of stearoyl-CoA desaturase and pharmaceutical compositions comprising such derivatives are also encompassed.Type: GrantFiled: September 19, 2007Date of Patent: August 7, 2012Assignees: Novartis AG, Xenon Pharmaceuticals Inc.Inventors: Natalie Dales, Zaihui Zhang, Rajender Kamboj, Jianmin Fu, Shaoyi Sun, Natalia Pokrovskaia, Serguei Sviridov
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Publication number: 20120184554Abstract: Provided are an agent for the treatment and/or prophylaxis of a mood disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: September 2, 2010Publication date: July 19, 2012Applicant: Kyowa Hakko Kirin Co., Ltd.Inventors: Koji Yamada, Tomoyuki Kanda
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Patent number: 8222285Abstract: Compounds are provided which are glucokinase activators and thus are useful in treating diabetes and related diseases and have the structure wherein in the ring represents one or two double bonds; R1 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R2 is alkyl, aryl, arylalkyl, heteroaryl, or heteroarylalkyl; R5 is as defined herein; Z is O, S, S(O), S(O)2, or NR5a; X is S, O, N, NR3, or CR3; Y is NCR4 or NR4; R3, R4, and R5 are as defined herein; R8 is aryl, heteroaryl, —PO(OR9)(OR10), —PO(OR9)R10 or —P(O)(R9)R10 (wherein R9 and R10 are as defined herein)/R6 and R7 are independently H, halogen, or alkyl; m is 0 or 1; and n is 0 to 3, or a pharmaceutically acceptable salt thereof. A method for treating diabetes and related diseases employing the above compounds is also provided.Type: GrantFiled: June 11, 2008Date of Patent: July 17, 2012Assignee: Bristol-Myers Squibb CompanyInventors: Sean Chen, Peter T. W. Cheng, Rebecca A. Smirk
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Publication number: 20120178765Abstract: The present invention provides an amide derivative having a stilbene or 1,2-diphenylethane moiety within the molecule thereof, a process for the preparation thereof, and a pharmaceutical composition comprising the same. The amide derivative of the present invention activates glucokinase remarkably, and therefore they can be usefully applied for treating glucokinase-mediated diseases, such as hyperglycemia and diabetes.Type: ApplicationFiled: September 17, 2010Publication date: July 12, 2012Applicant: YUHAN CORPORATIONInventors: Won-Hui Yi, Tae-Dong Han, Koo-Yeon Lee, Young-Hwan Kim, Eun-Hye Jung, Dong-Hoon Lee, Yoo-Hoi Park, Kyung-Nan Min, Jae-Gyu Kim, Byung-Kyu Lee
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Publication number: 20120172374Abstract: Compounds represented by the formula (I) or pharmaceutically acceptable salts thereof: R2—Y—Z-Q-A-R1??Formula (I) wherein R1, R2, Y, Z, Q, and A are as defined. These compounds are inhibitors of tubulin polymerization by binding at colchicines binding site and are useful in the treatment of tumors or mitotic diseases such as cancers, gout, and other conditions associated with abnormal cell proliferation.Type: ApplicationFiled: December 29, 2011Publication date: July 5, 2012Applicant: DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Meng-Hsin Chen, Shih-Hsien Chuang, Yi-Jen Chen, Lien-Hsiang Chang, Tsung-Hui Li, Ching-Hui Chen, Win-Yin Wei
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Publication number: 20120172362Abstract: Provided are an agent for the treatment and/or prophylaxis of an anxiety disorder comprising, as an active ingredient, a thiazole derivative represented by the formula (I) wherein R1 represents aryl or the like, and R2 represents pyridyl or the like, or a pharmaceutically acceptable salt thereof, and the like.Type: ApplicationFiled: September 2, 2010Publication date: July 5, 2012Applicant: KYOWA HAKKO KIRIN CO., LTD.Inventors: Junya Kase, Tomoyuki Kanda
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Patent number: 8211926Abstract: The present invention provides substituted pyrazolo-heterocycles having the general structure of formula I Also provided are pharmaceutically acceptable salts, acid salts, hydrates, solvates and stereoisomers of the compounds of formula I. The compounds are useful as modulators of cannabinoid receptors and for the prophylaxis and treatment of cannabinoid receptor-associated diseases and conditions, such as pain, inflammation and pruritis.Type: GrantFiled: June 16, 2010Date of Patent: July 3, 2012Assignee: Cara Therapeutics, Inc.Inventor: Robert Zhiyong Luo
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Patent number: 8211882Abstract: The present invention discloses methods of modulating the activity of Group I mGluRs using a defined class of benzamide compounds. In one embodiment, methods of modulating the activity of mGluR1 are provided. In another embodiment, methods of modulating the activity of mGluR5 are provided. In still another embodiment, methods of simultaneously modulating the activities of both mGluR1 and mGluR5 are provided. The present invention also provides methods of treating diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of benzamide compounds. The present invention further provides methods of preventing diseases or disorders which are mediated in full or in part by Group I mGluRs using one or more compounds belonging to the defined class of compounds.Type: GrantFiled: March 6, 2009Date of Patent: July 3, 2012Inventors: Richard Delarey Wood, William J Welsh, Sean Ekins, Ni Ai
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Patent number: 8211925Abstract: The present invention relates to N-heteroaryl-benzamides, pharmaceutical compositions comprising the same, and methods of using the same. The N-heteroaryl-benzamides are useful in diseases or medical conditions mediated by glucokinase.Type: GrantFiled: April 27, 2007Date of Patent: July 3, 2012Assignee: TransTech Pharma, Inc.Inventors: Anthony Murray, Jesper Lau, Lone Jeppsen, Per Vedsø, Dharma Rao Polisetti, Bapu Reddy Gaddam, Daniel P. Christen, Kalpathy Chidambareswaran Santhosh, Jeremy T. Cooper, Robert Carl Andrews
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Publication number: 20120165339Abstract: A cyclopropane derivative represented by the following formula (I) or a pharmaceutically acceptable salt thereof has orexin receptor inhibitory action, and thus, is extremely useful as an agent for preventing or treating sleep disorder or dyssomnia caused by orexin, including insomnia as a typical example: wherein A1, A2 and A3 each independently represent an aryl group, a heterocyclyl group or the like, R1, R2 and R3 each independently represent a hydrogen atom, a C1-6 alkyl group or the like, X represents an oxygen atom or the like, and L represents a bond or the like.Type: ApplicationFiled: December 20, 2011Publication date: June 28, 2012Applicant: EISAI R&D MANAGEMENT CO., LTD.Inventors: Taro Terauchi, Ayumi Takemura, Yuji Kazuta, Fumihiro Ozaki, Takashi Doko, Yu Yoshida, Toshiaki Tanaka, Keiichi Sorimachi, Yoshimitsu Naoe, Carsten Beuckmann