Having -c(=x)-, Wherein X Is Chalcogen, Bonded Directly To The Thiazine Ring Patents (Class 544/58.4)
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Patent number: 8227473Abstract: This invention provides compounds having the structure which may be used for the treatment of tumors.Type: GrantFiled: July 17, 2009Date of Patent: July 24, 2012Assignee: Lixte Biotechnology, Inc.Inventors: John S. Kovach, Francis Johnson
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Publication number: 20120184538Abstract: The present invention is concerned with isoxazole-pyridine derivatives of formula I wherein X, R1 to R6 are as described herein. The compounds are active on the GABA A ?5 receptor binding site and useful for the treatment of cognitive disorders, such as Alzheimer's disease.Type: ApplicationFiled: February 10, 2012Publication date: July 19, 2012Inventors: Bernd Buettelmann, Roland Jakob-Roetne, Henner Knust, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120122842Abstract: Disclosed are compounds which inhibit the activity of NAMPT, compositions containing the compounds and methods of treating diseases during which NAMPT is expressed. Disclosed are compounds which inhibit the activity of ROCK, compositions containing the compounds and methods of treating diseases during which ROCK is expressed.Type: ApplicationFiled: November 11, 2011Publication date: May 17, 2012Applicant: Abbott LaboratoriesInventors: Michael L. Curtin, Bryan K. Sorensen, Howard R. Heyman, Richard F. Clark, Kevin R. Woller, Omar J. Shah, Michael Michaelides, Chris Tse, Anil Vasudevan, Helmut Mack, Todd M. Hansen, Ramzi Sweis, Marina A. Pliushchev
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Patent number: 8178522Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: GrantFiled: April 28, 2010Date of Patent: May 15, 2012Assignee: Hoffmann-La Roche Inc.Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20120115855Abstract: Provided herein are compounds, pharmaceutical compositions and combination therapies for inhibition of hepatitis C.Type: ApplicationFiled: December 2, 2009Publication date: May 10, 2012Applicant: PRESIDIO PHARMACEUTICALS, INC.Inventors: Leping Li, Min Zhong
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Publication number: 20120077787Abstract: New compounds of the Formula (I): for the treatment of non-insulin-dependent diabetes mellitus.Type: ApplicationFiled: December 6, 2011Publication date: March 29, 2012Applicant: NOVARTIS AGInventors: Daniel Kaspar Baeschlin, Nils OSTERMANN, Francois GESSIER, Finton SIROCKIN, Kenji NAMOTO
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Patent number: 8129358Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: GrantFiled: November 8, 2007Date of Patent: March 6, 2012Assignee: Novartis AGInventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Publication number: 20120046268Abstract: The invention relates to novel substituted piperidines, 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, in particular of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: March 12, 2010Publication date: February 23, 2012Applicant: BAYER PHARMA AKTIENGESELLSCHAFTInventors: Mario Jeske, Dirk Heimbach, Susanne Röhrig, Yolanda Cancho Grande, Dirk Schneider, Ulrich Rester, Eckhard Bender, Mark Meininghaus, Katja Zimmermann, Dmitry Zubov, Anja Buchmüller, Georges Von Degenfeld, Christoph Gerdes, Michael Gerisch, Mark Jean Gnoth, Kersten Matthias Gericke
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Publication number: 20120035149Abstract: Contemplated compounds, compositions, and methods of prokineticin antagonists are presented where a prokineticin antagonist is used in the treatment and prevention of various conditions and disorders, and especially type II diabetes.Type: ApplicationFiled: December 16, 2009Publication date: February 9, 2012Applicant: THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: Qun-Yong Zhou, Jia-Da Li, Qi Huang
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Patent number: 8088763Abstract: Novel cyclohexyl-1,4-diamine compounds corresponding to formula I, processes for the production thereof, pharmaceutical compositions containing these compounds, methods of producing pharmaceutical compositions including these compounds and related methods of treating or inhibiting certain diseases or conditions.Type: GrantFiled: November 9, 2006Date of Patent: January 3, 2012Assignee: Gruenenthal GmbHInventors: Corinna Sundermann, Bernd Sundermann
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Publication number: 20110312944Abstract: Compounds which modulate the CB2 receptor are disclosed. Compounds according to the invention bind to and are agonists of the CB2 receptor, and are useful for treating inflammation. Those compounds which are agonists are additionally useful for treating pain.Type: ApplicationFiled: February 16, 2010Publication date: December 22, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Alessandra Bartolozzi, Angela Berry, Pier Francesco Cirillo, Eugene Richard Hickey, Doris Riether, Lifen Wu, Renee M. Zindell
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Patent number: 8080551Abstract: HIV replication inhibitors having formula (I) defined herein are disclosed. Pharmaceutical compositions containing the HIV replication inhibitors; the use of the HIV replication inhibitors in the treatment of HIV; and processes for preparing the HIV replication inhibitors are also disclosed.Type: GrantFiled: June 26, 2006Date of Patent: December 20, 2011Assignee: Janssen Pharmaceutica N.V.Inventors: Jérôme Emile Georges Guillemont, Patrice Palandijian, Marc René De Jonge, Lucien Maria Henricus Koymans, Hendrik Maarten Vinkers, Frederik Frans Desiré Daeyaert, Jan Heeres, Koen Jeanne Alfons Van Aken, Paulus Joannes Lewi, Paul Adriaan Jan Janssen, Frank Xavier Jozef Herwig Arts, legal representative
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Publication number: 20110251187Abstract: The present invention relates to a compound represented by wherein each symbol is as defined in the specification, a salt thereof and the like.Type: ApplicationFiled: May 29, 2009Publication date: October 13, 2011Inventors: Shizuo Kasai, Masahiro Kamaura, Nobuo Cho
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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: 20110236395Abstract: Inhibitors of matrix metalloproteinase 2 are used to treat or prevent a fibrotic disorder of the posterior capsule of the eye, for example posterior capsule opacification (PCO), or of a tissue or structure of the eye other than the lens or capsular bag.Type: ApplicationFiled: September 9, 2009Publication date: September 29, 2011Applicant: UNIVERSITY OF EAST ANGLIAInventors: Ian Michael Wormstone, Lucy Dawes, Julie Ann Eldred, Dylan Edwards, Lisa Hodgkinson
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Publication number: 20110201604Abstract: Substituted fused imidazole derivatives, methods of their preparation, pharmaceutical compositions comprising a substituted fused imidazole derivative, and methods of use in treating inflammation are provided. The substituted fused imidazole derivatives may control the activity or the amount or both the activity and the amount of heme-oxygenase.Type: ApplicationFiled: February 16, 2011Publication date: August 18, 2011Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Adnan M. M. Mjalli, Dharma Rao Polisetti, Jareer Nabeel Kassis, Matthew J. Kostura, Mustafa Guzel, Otis Clinton Attucks, Robert Carl Andrews, Samuel Victory, Suparna Gupta
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Publication number: 20110178062Abstract: Certain substituted indole and benzothiophene compounds are histamine H3 receptor modulators useful in the treatment of histamine H3 receptor-mediated diseases.Type: ApplicationFiled: February 28, 2008Publication date: July 21, 2011Inventors: Brett D. Allison, Cheryl A. Grice, Kelly J. McClure, Alejandro Santillan, JR.
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Publication number: 20110172207Abstract: The present invention relates to novel substituted pyrazolamides, methods for their preparation, their use for the treatment and/or prophylaxis of diseases, as well as their use for the manufacture of medicaments for the treatment and/or prophylaxis of diseases, especially of retroviral diseases, in humans and/or animals.Type: ApplicationFiled: September 16, 2010Publication date: July 14, 2011Applicant: AiCuris Gmbh & Co. KGInventors: Rudolf SCHOHE-LOOP, Reinhold Welker, Arnold Paessens, Marcus Bauser, Friederike Stoll, Frank Dittmer, Kerstin Henninger, Daniela Paulsen, Dieter Lang
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Publication number: 20110136735Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: ApplicationFiled: November 30, 2010Publication date: June 9, 2011Inventors: David BARNES, Gregory Raymond BEBERNITZ, Scott Louis COHEN, Robert Edson DAMON, Robert Francis DAY, Monish JAIN, Rajeshri Ganesh KARKI, Louise Clare KIRMAN, Tajesh Jayprakash PATEL, Brian Kenneth RAYMER, Herbert Franz SCHUSTER, Wei ZHANG
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Publication number: 20110111959Abstract: This disclosure relates, inter alia, to stimulants of pollen tube germination and growth of pollen tubes, and methods of their use to stimulate in vitro and in vivo pollen germination and pollen tube growth.Type: ApplicationFiled: March 26, 2010Publication date: May 12, 2011Inventors: Yuan Qin, Ravishankar Palanivelu, Ronald J. Wysocki, JR., Arpad Somogyi, Yelena Feinstein
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Patent number: 7939525Abstract: Novel chemical conjugates of psychotropic drugs and organic acids, uses thereof in the treatment of psychotic and/or proliferative disorders and diseases and as chemosensitizing agents, and their syntheses are disclosed. The organic acids are selected to reduce side effects induced by the psychotropic drugs and/or to exert an anti-proliferative activity.Type: GrantFiled: September 1, 2009Date of Patent: May 10, 2011Assignees: Bar-Ilan University, Ramot at Tel Aviv University Ltd.Inventors: Abraham Nudelman, Ada Rephaeli, Irit Gil-Ad, Abraham Weizman
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Publication number: 20110046109Abstract: Novel substituted 2,4,8-trisubstituted-8H-pyrido[2,3-d]pyrimidin-7-one compounds and compositions for use in therapy as CSBP/p38 kinase inhibitors.Type: ApplicationFiled: August 19, 2010Publication date: February 24, 2011Applicant: GLAXOSMITHKLINE LLCInventors: Jerry L. Adams, Jeffrey C. Boehm, Ralph Hall, Qi Jin, Jiri Kasparec, Domingos J. Silva, John J. Taggart
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Publication number: 20110034433Abstract: The present invention relates to novel 4-(4-cyano-2-thioaryl)dihydropyrimidin-2-one derivatives, to processes for their preparation, to their use alone or in combination for the treatment and/or prevention of diseases and also to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of disorders of the lung and the cardiovascular system.Type: ApplicationFiled: December 9, 2008Publication date: February 10, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Franz Von Nussbaum, Dagmar Karthaus, Sonja Anlauf, Martina Delbeck, Volkhart Min-Jian Li, Daniel Meibom, Klemens Lustig, Jens Schamberger
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Patent number: 7884098Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1? R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.Type: GrantFiled: January 25, 2008Date of Patent: February 8, 2011Assignee: GlaxoSmithKline LLCInventors: Jeffrey Michael Axten, Deborah L. Bryan, David Harold Drewry, Thomas H Faitg, Timothy Francis Gallagher, Neil W Johnson, Jiri Kasparec, Jeffrey M Ralph, Domingos J. Silva
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Publication number: 20110021489Abstract: The invention relates to novel substituted piperidines, to processes for preparation thereof, to the use thereof for treatment and/or prophylaxis of diseases and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially of cardiovascular disorders and tumour disorders.Type: ApplicationFiled: May 27, 2010Publication date: January 27, 2011Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Dirk HEIMBACH, Susanne Röhrig, Yolanda Cancho Grande, Eckhard Bender, Katja Zimmermann, Anja Buchmüller, Christoph Gerdes, Mark Jean Gnoth, Kersten Matthias Gericke, Mario Jeske
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Publication number: 20110015178Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain amido-thiophene compounds that, inter alia, inhibit 11?-hydroxysteroid dehydrogenase type 1 (11?-HSD1). The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit 11?-hydroxysteroid dehydrogenase type 1; to treat disorders that are ameliorated by the inhibition of 11?-hydroxysteroid dehydrogenase type 1; to treat the metabolic syndrome, which includes disorders such as type 2 diabetes and obesity, and associated disorders including insulin resistance, hypertension, lipid disorders and cardiovascular disorders such as ischaemic (coronary) heart disease; to treat CNS disorders such as mild cognitive impairment and early dementia, including Alzheimer's disease; etc.Type: ApplicationFiled: March 13, 2009Publication date: January 20, 2011Applicant: THE UNIVERSITY OF EDINBURGHInventors: Scott Peter Webster, Jonathan Robert Seckl, Brian Robert Walker, Peter Ward, Thomas David Pallin, Hazel Joan Dyke, Trevor Robert Perrior
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Publication number: 20110009620Abstract: The present invention provides 4-amino-5-cyanopyrimidine derivatives of the formula: wherein R1, R2 and R3 are defined herein, or pharmaceutically acceptable salts thereof, having a safe and potent adenosine A2a receptor agonistic activity; and also provides an adenosine A2a receptor agonist, an intraocular pressure reducing agent, or a medicine for treating glaucoma, etc., which comprises the compound as an active ingredient.Type: ApplicationFiled: September 22, 2010Publication date: January 13, 2011Inventors: Masaya Kato, Norifumi Sato, Minoru Okada, Tetsuyuki Uno, Nobuaki Ito, Yasuhiro Takeji, Hisashi Shinohara, Masahiro Fuwa
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Publication number: 20110003788Abstract: The present invention provides a compound having a superior Smo inhibitory activity and lower toxicity, which is sufficiently satisfactory as a pharmaceutical product. The present invention provides a compound represented by the formula (I) wherein ring A is 5- to 7-membered ring optionally having substituent(s), where substituents are optionally bonded to each other to form a ring; X is O, S or NR1 (R1 is a hydrogen atom or a hydrocarbon group optionally having substituent(s)); R2 is carbamoyl optionally having substituent(s); and R3 is hydroxy optionally having substituent(s), or a salt thereof.Type: ApplicationFiled: February 25, 2009Publication date: January 6, 2011Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Nobuhiro Fujii, Yuya Oguro, Satoshi Sasaki, Shigeru Kondo
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Publication number: 20110003799Abstract: The invention provides compounds of the formula (0) or salts or tautomers or N-oxides or solvates thereof for use in the prophylaxis or treatment of disease states and conditions such as cancers mediated by cyclin-dependent kinase and glycogen synthase kinase-3. In formula (0): X is a group R1-A-NR4— or a 5- or 6-membered carbocyclic or heterocyclic ring; A is a bond, SO2, C?O, NRg(C?O) or O(C?O) wherein Rg is hydrogen or C1-4 hydrocarbyl optionally substituted by hydroxy or C1-4 alkoxy; Y is a bond or an alkylene chain of 1, 2 or 3 carbon atoms in length; R1 is hydrogen; a carbocyclic or heterocyclic group having from 3 to 12 ring members; or a C1-8 hydrocarbyl group optionally substituted by one or more substituents selected from halogen (e.g.Type: ApplicationFiled: September 8, 2010Publication date: January 6, 2011Applicant: ASTEX THERAPEUTICS, LTD.Inventors: Valerio BERDINI, Michael Alistair O'BRIEN, Maria Grazia CARR, Theresa Rachel EARLY, Adrian Liam GILL, Gary TREWARTHA, Alison Jo-Anne WOOLFORD, Andrew James WOODHEAD, Paul Graham WYATT
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Publication number: 20100324010Abstract: A renin inhibitor comprising a compound represented by the formula: wherein each symbol is as defined in the description, or a salt thereof or a prodrug thereof. The compound of the present invention has a superior renin inhibitory activity, and thus is useful as an agent for the prophylaxis or treatment of hypertension, various organ damages attributable to hypertension and the like.Type: ApplicationFiled: October 14, 2008Publication date: December 23, 2010Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Yasuhiro Imaeda, Takanobu Kuroita, Yoshiyuki Fukase, Shinkichi Suzuki, Michiko Amano
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Publication number: 20100317656Abstract: Compounds of Formula (I): wherein X, Y, R1, R2, R3, and R4 are as defined in the disclosure, or a acid addition salt thereof; and therapeutic use thereof.Type: ApplicationFiled: July 1, 2010Publication date: December 16, 2010Applicant: SANOFI-AVENTISInventor: Jean-Francois PEYRONEL
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Publication number: 20100291003Abstract: Novel compounds of the general formula (I), having histone deacetylase (HDAC) inhibiting enzymatic activity, their derivatives, analogs, tautomeric forms, stereoisomers, polymorphs, hydrates, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. The present invention more particularly provides novel compounds of the general formula (I). Also included is a method for treatment of cancer, psoriasis, proliferative conditions and conditions mediated by HDAC, in a mammal comprising administering an effective amount of a novel compound of formula (I).Type: ApplicationFiled: October 21, 2008Publication date: November 18, 2010Applicant: ORCHID RESEARCH LABORATORIES LIMITEDInventors: Sridharan Rajagopal, Virendra Kachhadia, Thanasekaran Ponpandian, Abdul Raheem Keeri, Karnambaram Anandhan, Sriram Rajagopal, Rajendran Praveen, Prabhu Daivasigamani
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Publication number: 20100286116Abstract: The present invention is concerned with isoxazole-thiazole derivatives of formula I, having affinity and selectivity for GABA A ?5 receptor, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful as cognitive enhancer or for the therapeutic and/or prophylactic treatment of cognitive disorders like Alzheimer's disease.Type: ApplicationFiled: April 28, 2010Publication date: November 11, 2010Inventors: Roland Jakob-Roetne, Matthew C. Lucas, Andrew Thomas
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Publication number: 20100280018Abstract: A compound of formula (I), or an enantiomer or diastereoisomer thereof, or a salt, hydrate or solvate thereof: for the treatment or prophylaxis of arthritis in mammals.Type: ApplicationFiled: July 20, 2010Publication date: November 4, 2010Applicants: Laboratoires Serono S.A., Vernalis (Oxford) LimitedInventors: Gilles Pain, Stephen John Davies, Agnes Bombrun
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Publication number: 20100256359Abstract: This invention is directed to vanilloid receptor VR1 ligands. More particularly, this invention relates to hetero isonipecotic amides that are potent modulators of VR1 which are useful for the treatment and prevention of disease conditions in mammals.Type: ApplicationFiled: October 6, 2009Publication date: October 7, 2010Inventors: Micheal D. Gaul, Bao-Ping Zhao, Daniel A. Hutta
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Publication number: 20100210629Abstract: The present invention provides for tricyclic compounds having the formula (I), wherein R1, R2, R5, R6, R7, and R8 are as described herein. The present invention further provides pharmaceutical compositions comprising such compounds, as well as the use of such compounds for treating inflammatory and immune diseases.Type: ApplicationFiled: April 23, 2010Publication date: August 19, 2010Inventors: William J. Pitts, James Kempson, Junqing Guo, Jagabandhu Das, Charles M. Langevine, Steven H. Spergel, Scott Hunter Watterson
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Publication number: 20100204200Abstract: The present invention provides compounds, compositions and methods for the selective inhibition of cathepsin S. In a preferred aspect, cathepsin S is selectively inhibited in the presence of at least one other cathepsin isozyme. The present invention also provides methods for treating a disease state in a subject by selectively inhibiting cathepsin S. More particularly, the present invention provides compounds having Formula 1: wherein Q is an optionally substituted azetidinyl, pyrrolidinyl, piperidyl, and indolinyl; or Q is NR25R26; and A, R5, R6, R7, R8, R9, R25, R26 and Ar are substituents.Type: ApplicationFiled: April 21, 2010Publication date: August 12, 2010Applicant: IRM LLCInventors: Hong Liu, Arnab Chatterjee, David C. Tully, Phillip Alper, Badry Bursulaya, Jianhua Guo, David H. Woodmansee, Daniel Mutnick, Donald S. Karanewsky, Yun He
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Publication number: 20100144721Abstract: 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: September 4, 2007Publication date: June 10, 2010Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Tiansheng Wang, Jeremy Green, Brain Ledford, Francois Maltais, Andreas Termin
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Publication number: 20100144588Abstract: Novel iminium-type coupling agents containing proton acceptors in their iminium moiety, which can be used beneficially as coupling agents in various chemical polypeptide and/or polynucleotide syntheses, and are particularly useful as yield enhancing and racemization suppressing coupling agents for use in peptide syntheses, are disclosed. Further disclosed are a process of preparing such iminium-type coupling agents and their use in the preparation of polypeptides and/or polynucleotides.Type: ApplicationFiled: May 15, 2008Publication date: June 10, 2010Applicant: LUXEMBOURG BIO TECHNOLOGIES LTD.Inventors: Fernando Albericio, Ayman El-Faham, Yoav Luxembourg, Ariel Ewenson
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Publication number: 20100130485Abstract: Certain cyclopropyl amines are histamine H3 modulators useful in the treatment of histamine H3 receptor mediated diseases.Type: ApplicationFiled: January 28, 2010Publication date: May 27, 2010Inventors: Brett D. Allison, Nicholas I. Carruthers, Cheryl A. Grice, Michael A. Letavic
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Publication number: 20100113433Abstract: The present invention relates to N-Substituted thiomorpholine compounds of formula I, the possible isomers, the pharmaceutically acceptable salts, the solvates, the hydrates or the prodrugs thereof as inhibitors of dipeptidyl peptidase IV (DPP-IV); and to a method for preparing the compounds of formula I, pharmaceutical compositions comprising the compounds of formula I and use of the compounds of formula II in medical field, particularly in the preparation of medicaments for treating and preventing diabetes (in particular type II diabetes), hyperglycemia, X syndrome, hyperinsulinemia, obesity, atherosclerosis and all kinds of diseases modulated by immune system.Type: ApplicationFiled: June 1, 2007Publication date: May 6, 2010Inventors: Song Li, Wu Zhong, Junhai Xiao, Xinghai Ma, Lili Wang, Hongying Liu, Zhibing Zheng
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Publication number: 20100099662Abstract: 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: ApplicationFiled: January 9, 2008Publication date: April 22, 2010Inventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20100075931Abstract: Certain oxazole ketone compounds are described, which are useful as FAAH inhibitors. Such compounds may be used in pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by fatty acid amide hydrolase (FAAH) activity. Thus, the compounds may be administered to treat, e.g., anxiety, pain, inflammation, sleep disorders, eating disorders, or movement disorders (such as multiple sclerosis).Type: ApplicationFiled: September 7, 2007Publication date: March 25, 2010Applicant: THE SCRIPPS RESEARCH INSTITUTEInventor: Dale L. Boger
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Patent number: 7683055Abstract: The present invention provides compositions comprising lanthionine ketimine derivatives and thiomorpholine dicarboxylic acid derivatives, as well as processes for the preparation of such compounds. The invention also concerns the use of lanthionine, lanthionine ketimine (LK), LK derivatives, thiomorpholine dicarboxylic acid (TMDCA), and TMDCA derivatives. It concerns the use of these compounds for the treatment and/or prevention diseases, including diseases affecting the central nervous system. The invention provides for compounds and methods having anti-oxidant, anti-neuroinflammatory and neuroprotective activities. It also provides for compounds having the ability to pass through and/or be transported through cellular membranes, such the blood-brain barrier.Type: GrantFiled: January 9, 2007Date of Patent: March 23, 2010Assignee: Oklahoma Medical Research FoundationInventor: Kenneth Hensley
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Publication number: 20100063036Abstract: The present invention relates to morpholine and thiomorpholine derivatives of the general formula I or pharmaceutically acceptable salts thereof and their use.Type: ApplicationFiled: November 3, 2009Publication date: March 11, 2010Applicant: H. Lundbeck A/SInventors: Christian Wenzel Tornøe, Mario Rottländer, Nikolay Khanzhin, Andreas Ritzén, William Patrick Watson
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Publication number: 20100034813Abstract: Disclosed are new substituted pyrazole and triazole compounds of Formula (I) and pharmaceutically acceptable salts, esters or prodrugs thereof, compositions of the derivatives together with pharmaceutically acceptable carriers, and uses thereof:Type: ApplicationFiled: November 8, 2007Publication date: February 11, 2010Inventors: Yi Xia, Kris G. Mendenhall, Paul A. Barsanti, Annette O. Walter, David Duhl, Paul A. Renhowe
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Publication number: 20100016318Abstract: The present invention relates to a compound represented by the following formula: or a pharmaceutically acceptable salt thereof; wherein R1, R1? R2, R3, R4, R5, r and s are as defined herein. Compounds of the present invention are useful in the treatment of diseases associated with Aurora kinase activity such as cancer.Type: ApplicationFiled: January 25, 2008Publication date: January 21, 2010Applicant: SMITHKLINE BEECHAM CORPORATIONInventors: Jeffrey Michael Axten, Deborah L. Bryan, David Harold Drewry, Thomas H. Faitg, Timothy Francis Gallagher, Neil W. Johnson, Jiri Kasparec, Jeffrey M. Ralph, Domingos J. Silva
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Publication number: 20090275569Abstract: The invention provides benzotriazine compounds having formula (I). The benzotriazine compounds of the invention are capable of inhibiting kinases, such members of the Src kinase family, and various other specific receptor and non-receptor kinases.Type: ApplicationFiled: September 9, 2008Publication date: November 5, 2009Inventors: Xianchang Gong, Kathy Barrett, Jianguo Cao, Colleen Gritzen, Glenn Noronha, John D. Hood, Chi Ching Mak, Andrew McPherson, Ved Prakash Pathak, Joel Renick, Richard M. Soll, Ute Splittgerber, Wolfgang Wrasidlo, Ningning Zhao, Elena Dneprovskaia, Binqi Zeng, Glenn Noronha
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Publication number: 20090275538Abstract: The present invention relates to Arylmethylidene heterocycles, compositions comprising an Arylmethylidene heterocycle, and methods useful for treating or preventing pain comprising administering an effective amount of an Arylmethylidene heterocycle. The compounds, compositions, and methods of the invention are also useful for treating or preventing inflammation.Type: ApplicationFiled: February 9, 2009Publication date: November 5, 2009Inventors: Giorgio Attardo, Sasmita Tripathy, Martin Gagnon
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Publication number: 20090227569Abstract: Pyrrolidine compounds described herein and methods for using them to inhibit dipeptidyl peptidase IV and treat Type II diabetes.Type: ApplicationFiled: February 25, 2009Publication date: September 10, 2009Applicant: National Health Research InstitutesInventors: Weir-Torn Jiaang, Yu-Sheng Chao, Ting-Yueh Tsai, Tsu Hsu