1,3-oxazoles (including Hydrogenated) Patents (Class 514/374)
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Patent number: 8362003Abstract: The present invention relates to 3-aminopyrrolidine derivatives of the formula I: (wherein R1, R2, R3, R4, R5, R6, R7, R8, X, Y and X are as defined herein) which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of chemokine receptors and more specifically as a modulator of the CCR2 and/or CCR5 receptor. The compounds and compositions of the invention may bind to chemokine receptors, e.g., the CCR2 and/or CCR5 chemokine receptors, and are useful for treating diseases associated with chemokine, e.g., CCR2 and/or CCR5, activity, such as atherosclerosis, restenosis, lupus, organ transplant rejection and rheumatoid arthritis.Type: GrantFiled: June 16, 2011Date of Patent: January 29, 2013Assignee: Incyte CorporationInventors: Chu-Biao Xue, Brian W. Metcalf, Hao Feng, Ganfeng Cao, Taisheng Huang, Changsheng Zheng, Darius J. Robinson, Amy Qi Han
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Patent number: 8357712Abstract: The invention relates to compounds of formula I wherein R1, R2, X, Y, and n are defined in the specification and to pharmaceutically acceptable acid addition salts thereof. The invention also provides pharmaceutical compositions and methods of manufacture of such compounds. The compounds are useful for the treatment of diseases related to the biological function of the trace amine associated receptors, which diseases are depression, anxiety disorders, bipolar disorder, attention deficit hyperactivity disorder, stress-related disorders, psychotic disorders, schizophrenia, neurological diseases, Parkinson's disease, neurodegenerative disorders, Alzheimer's disease, epilepsy, migraine, substance abuse and metabolic disorders, 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: GrantFiled: February 24, 2011Date of Patent: January 22, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Guido Galley, Annick Goergler, Katrin Groebke Zbinden, Roger Norcross
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Patent number: 8354410Abstract: The disclosure provides compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and may be useful in treating those infected with HCV.Type: GrantFiled: March 9, 2011Date of Patent: January 15, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Kap-Sun Yeung, Katharine A. Grant-Young, John F. Kadow
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Patent number: 8354436Abstract: The present invention relates to compounds of the general formula (I), and the pharmaceutically acceptable salt or solvate thereof, as anti-inflammatory and immunomodulatory agents.Type: GrantFiled: January 27, 2012Date of Patent: January 15, 2013Assignee: 4SC Discovery GmbHInventors: Johann Leban, Stefan Tasler, Wael Saeb, Carine Chevrier
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Publication number: 20130012552Abstract: The present invention provides a composition having an excellent controlling activity on plant disease. The composition comprising the compound represented by the formula (1) and one or more azole fungicidal compound selected from the group (A) shows an excellent controlling activity on a plant disease.Type: ApplicationFiled: March 2, 2011Publication date: January 10, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventors: So Kiguchi, Soichi Tanaka, Mayuko Ozawa, Atsushi Iwata
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Publication number: 20130012540Abstract: This disclosure concerns novel compounds of Formula (I) or as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: September 12, 2012Publication date: January 10, 2013Inventors: Rico Lavoie, John A. Bender, Jeffrey Lee Romine, Edward H. Ruediger, Carol Bachand, Omar D. Lopez, Qi Chen, Makonen Belema, John F. Kadow, Lawrence G. Hamann
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Publication number: 20130011361Abstract: The present invention provides heterocyclic derivatives of formula (I) 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: ApplicationFiled: October 1, 2010Publication date: January 10, 2013Applicants: XENON PHARMACEUTICALS INC., NOVARTIS AGInventors: Natalie Dales, Jianmin Fu, Qi Jia, Natalia Pokrovskaia, Shaoyi Sun, Zaihui Zhang
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Publication number: 20130012513Abstract: Described herein are compounds, pharmaceutical compositions and methods for the inhibition of Hedgehog signaling. Said compounds, pharmaceutical compositions and methods have utility in the treatment of human and veterinary disease and disorders.Type: ApplicationFiled: January 6, 2011Publication date: January 10, 2013Inventors: Jean-Michel Vernier, John May, Patrick O'Connor, William Ripka, Anthony Pinkerton, Pierre-Yves Bounaud, Stephanie Hopkins
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Publication number: 20130012514Abstract: Aminoalkyloxazole and aminoalkylthiazolecarboxylic acid amides of formulae (1) and (2) where X represents O or S, Y represents C or N, where the two atoms must be different from one another, R2 represents hydrogen or acyl and R1 and R3, which may be identical or different, represent a substituent selected from the group consisting of branched or straight-chain, substituted or unsubstituted alkyl groups, alkylcycloalkyl groups, alkylaryl groups, cycloalkyl groups, cycloalkylaryl groups, aryl groups and arylcycloalkyl groups which optionally contain heteroatoms, a pharmaceutically acceptable salt, a stereoisomer, a stereoisomer mixture, a tautomer or a prodrug compound, preferably a prodrug ester and a prodrug peptide, thereof.Type: ApplicationFiled: February 4, 2011Publication date: January 10, 2013Applicant: EMC microcollections GmbHInventors: Holger Eickhoff, Hubert Löwenheim
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Patent number: 8349881Abstract: Methods for preserving technical products such as fuels and lubricants with a microbicidal composition. The composition is made up of at least one formaldehyde donor compound and at least one antioxidant. The antioxidant is either a gallic ester, a phenol derivative, a L-ascorbic acid, including salts and derivatives thereof, a tocopherol or one of its associated derivatives.Type: GrantFiled: May 7, 2010Date of Patent: January 8, 2013Assignee: Air Liquide Sante (International)Inventors: Ralf Gradtke, Wolfgang Beilfuss, Klaus Weber, Wolfgang Siegert
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Patent number: 8349874Abstract: A method relieves both nociceptive pain and neuropathic pain and has fewer side effects. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof.Type: GrantFiled: June 27, 2012Date of Patent: January 8, 2013Assignee: Toray Industries, Inc.Inventors: Yasuhiro Morita, Katsuhiko Iseki, Yuji Sugawara, Hideyuki Tsutsiu, Shunsuke Iwano, Naoki Izumimoto, Tadamasa Arai, Hidetoshi Noda, Chihiro Yoshida
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Publication number: 20130005730Abstract: The present invention relates to certain novel 1,3-oxazolidine compounds of formula (I), to processes for making such compounds and to their utility as renin inhibitors or prodrugs of renin inhibitors.Type: ApplicationFiled: October 29, 2010Publication date: January 3, 2013Inventors: Piaoyang Sun, Mikhajlovich Antonov Dmitry, Xiao Xiong Zhou
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Patent number: 8344002Abstract: A novel compound represented by the formula (1) below which has ?-secretase inhibitory activity, its pharmaceutically acceptable salt or a prodrug thereof. wherein Ar is a substituted or unsubstituted 5 to 6 membered mono cyclic aromatic group; R1, R2 and R3 are hydrogen atom, substituted or unsubstituted alkyl group or the like, or R2 and R3 may be taken together with the adjacent nitrogen atom and carbon atom respectively to form a 3 to 6 membered ring; R4 is C1-6 alkyl group, C1-6 alkyl group substituted by phenyl, phenylthio, or a hetero ring, or the like; A is represented by the formula below: wherein X and Y are oxygen atom, NH or sulfur atom, Z is hydrogen atom, hydroxy group which may be substituted, amino group, thiol group, or the like; and B is hydroxy group, substituted or unsubstituted amino group, substituted or unsubstituted aliphatic or aromatic amino group, or the like.Type: GrantFiled: June 18, 2008Date of Patent: January 1, 2013Inventor: Yoshiaki Kiso
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Patent number: 8343511Abstract: The present disclosure provides improved compositions comprising rifabutin, clarithromycin, and clofazimine for use in the treatment of Inflammatory Bowel Diseases. In one instance, the compositions may comprise a formulation of rifabutin, clarithromycin, and clofazimine in a single dosage form, such as a capsule, tablet, etc., with one or more specific excipients.Type: GrantFiled: February 5, 2009Date of Patent: January 1, 2013Assignee: Red Hill Biopharma Ltd.Inventors: Thomas Julius Borody, Patrick Gosselin
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Patent number: 8343970Abstract: Compounds that inhibit PDE10 are disclosed that have utility in the treatment of a variety of conditions, including (but not limited to) psychotic, anxiety, movement disorders and/or neurological disorders such as Parkinson's disease, Huntington's disease, Alzheimer's disease, encephalitis, phobias, epilepsy, aphasia, Bell's palsy, cerebral palsy, sleep disorders, pain, Tourette's syndrome, schizophrenia, delusional disorders, drug-induced psychosis and panic and obsessive-compulsive disorders. Pharmaceutically acceptable salts, stereoisomers, solvates and prodrugs of the compounds are also provided. Also disclosed are compositions containing a compound in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for inhibiting PDE10 in a warm-blooded animal in need of the same.Type: GrantFiled: March 10, 2011Date of Patent: January 1, 2013Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20120329843Abstract: The present invention provides a method of treating a patient suffering from pain or other FAAH mediated conditions by administering a fatty acid amide inhibiting amount of a compound represented by the formula: wherein R1 is H; R2 is a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; R3 is a radical selected from the group consisting of H, hydrocarbyl and substituted hydrocarbyl; X is CHCH, (CH2)n or O(CH2)n, wherein n is 0 or an integer of from 1 to 4; and W is O, S, or NR6, wherein R6 is selected from the group consisting of H and alkyl.Type: ApplicationFiled: May 23, 2012Publication date: December 27, 2012Inventors: David F. Woodward, Jose L. Martos, William R. Carling, Andrew D. Jones, Jenny W. Wang
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Patent number: 8338469Abstract: The invention provides compounds and pharmaceutical compositions thereof, which are useful for modulating channel activating proteases, and methods for, using such compounds to treat, ameliorate or prevent a condition associated with a channel activating protease, including but not limited to prostasin, PRSS22, TMPRSS11 (e.g., TMPRSS11B, TMPRSS11E), TMPRSS2, TMPRSS3, TMPRSS4 (MTSP-2), matriptase (MTSP-1), CAP2, CAP3, trypsin, cathepsin A, or neutrophil elastase.Type: GrantFiled: April 19, 2011Date of Patent: December 25, 2012Assignee: IRM LLCInventors: David C. Tully, Amab K. Chatterjee, Agnes Vidal, Hank Michael James Petrassi, Zhiwei Wang, Badry Bursulaya, Glen Spraggon
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Patent number: 8338440Abstract: Novel compounds that inhibit the binding of the Smac protein to Inhibitor of Apoptosis Proteins (IAPs) of the formula (I).Type: GrantFiled: April 26, 2012Date of Patent: December 25, 2012Inventors: Mark G. Palermo, Sushil Kumar Sharma, Christopher Sean Straub, Run-Ming Wang, Leigh Zawel, Yanlin Zhang, Zhuoliang Chen, Yaping Wang, Fan Yang, Wojciech Wrona, Gang Liu, Mark G. Charest, Feng He
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Publication number: 20120322827Abstract: Disclosed are compounds having the formula: wherein X1, X2, X3, R1, R2, R3, R4, Y, A, n and L are as defined herein, and methods of making and using the same.Type: ApplicationFiled: January 13, 2011Publication date: December 20, 2012Inventors: Erkan Baloglu, Shomir Ghosh, Mercedes Lobera, Darby Schmidt
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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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Patent number: 8334316Abstract: The present invention provides substituted di-, tri-, tetra- and penta-sulfide compounds and compositions, and methods of using the same for the treatment and/or prevention of a cell proliferative disorder. The present invention also provides methods for preparing trisulfide compounds and compositions.Type: GrantFiled: February 9, 2009Date of Patent: December 18, 2012Assignee: ACEA Biosciences, Inc.Inventors: Xiao Xu, Haoyun An, Xiaobo Wang
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Publication number: 20120315303Abstract: Methods and intravascular treatment devices for treating atherosclerosis are provided.Type: ApplicationFiled: May 4, 2012Publication date: December 13, 2012Applicant: Medtronic Vascular, Inc.Inventors: AYALA HEZI-YAMIT, SUSAN EDWARDS, CAROL SULLIVAN, OLUWASHOLA SHAKIRAT SULAIMON, LORI GARCIA, STEFAN TUNEV
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Patent number: 8329685Abstract: The invention provides a method of enhancing the action of a pharmaceutical agent selected from the group consisting of the anti-infective agents, the group comprising of the antimicrobial agents, the anthelmintic agents and the anti-ectoparasitic agents, but excluding coal tar solution and H1-antagonist antihistamines, and from the group consisting of the CPNS agents selected from the group of compounds acting on the central or peripheral nervous system, but excluding coal tar solution and H1-antagonist antihistamines and also excluding anti-inflammatory, analgesic and antipyretic agents and also provides an enhanced method for the administration of a nucleic acid substance to the cells of an animal, a plant or a micro-organism.Type: GrantFiled: January 16, 2003Date of Patent: December 11, 2012Assignee: North West UniversityInventor: Petrus Johannes Meyer
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Patent number: 8329913Abstract: An object of the present invention is to provide novel carbazole derivatives, solvates thereof, or pharmaceutically acceptable salts thereof having an excellent adipose tissue weight reducing effect, hypoglycemic effect, and hypolipidemic effect, which are useful as a preventive and/or therapeutic agent for fatty liver, obesity, lipid metabolism abnormality, visceral adiposity, diabetes, hyperlipemia, impaired glucose tolerance, hypertension, non-alcoholic fatty liver disease, non-alcoholic steatohepatitis, and the like.Type: GrantFiled: October 28, 2005Date of Patent: December 11, 2012Assignee: Zeria Pharmaceutical Co., Ltd.Inventors: Masakazu Murata, Yoshihiko Itokazu, Ryu Nakao
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Publication number: 20120309724Abstract: In one aspect, the invention relates to compounds having the formula: where R1, R2, R3, X, R4, R5, and R6 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.Type: ApplicationFiled: May 18, 2012Publication date: December 6, 2012Applicant: THERAVANCE, INC.Inventors: Melissa Fleury, Roland Gendron, Adam D. Hughes, Jane Schmidt
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Publication number: 20120309738Abstract: This invention relates to compounds of formula I their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), to 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, R3, R4, R6, R2, R7, R8, R9, Ra, Rb have meanings given in the description.Type: ApplicationFiled: December 8, 2011Publication date: December 6, 2012Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning Priepke, Raimund Kuelzer, Juergen Mack, Roland Pfau, Dirk Stenkamp, Benjamin Pelcman, Robert Roenn, Dimitrijs Lubriks, Edgars Suna
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Publication number: 20120302562Abstract: Compounds that may be used to inhibit Notum Pectinacetylesterase are described, as well as compositions comprising them, and methods of their use to treat diseases and disorders affecting bone.Type: ApplicationFiled: May 23, 2012Publication date: November 29, 2012Inventors: Joseph BARBOSA, Kenneth Gordon CARSON, Michael Walter GARDYAN, Jason Patrick HEALY, Qiang HAN, Ross MABON, Praveen PABBA, James TARVER, JR., Kristen M. TERRANOVA, Ashok TUNOORI, Xiaolian XU
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Publication number: 20120302607Abstract: The invention provides a series of C4-substituted oxazole compounds having an alpha keto side chain at the 2 position, for example, compounds of formula I. The compounds can inhibit fatty acid amide hydrolase and can be useful for treatment of malconditions modulated by fatty acid amide hydrolase. The invention further provides methods of making compounds of formula I, useful intermediates in the preparation of compounds of formula I, and methods of using compounds of formula 1 and compositions thereof.Type: ApplicationFiled: August 2, 2012Publication date: November 29, 2012Applicant: The Scripps Research InstituteInventor: Dale L. Boger
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Publication number: 20120295923Abstract: Compounds and pharmaceutically acceptable salts of the compounds are disclosed, wherein the compounds have the structure of Formula I as defined in the specification. Corresponding pharmaceutical compositions, methods of treatment, methods of synthesis, and intermediates are also disclosed.Type: ApplicationFiled: January 19, 2011Publication date: November 22, 2012Inventors: Christopher William Am Ende, Benjamin Adam Fish, Douglas Scott Johnson, Ricardo Lira, Christopher John O'Donnell, Martin Youngjin Pettersson, Corey Michael Stiff
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Publication number: 20120295897Abstract: This invention is directed to spiro-oxindole compounds, as stereoisomers, enantiomers, tautomers thereof or mixtures thereof; or pharmaceutically acceptable salts, solvates or prodrugs thereof, for the treatment and/or prevention of sodium channel-mediated diseases or conditions, such as pain.Type: ApplicationFiled: July 25, 2012Publication date: November 22, 2012Applicant: Xenon Pharmaceuticals Inc.Inventors: Mikhail Chafeev, Sultan Chowdhury, Lauren Fraser, Jianmin Fu, Jonathan Langille, Shifeng Liu, Jianyu Sun, Shaoyi Sun, Serguei Sviridov, Mark Wood, Alla Yurevna Zenova, Qi Jia, Jean-Jacques Cadieux, Simon J. Gauthier, Amy Frances Douglas, Tom Hsieh, Nagasree Chakka, Zoran Cikojevic
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Publication number: 20120295894Abstract: Described herein are novel beta-secretase inhibitors and methods for their use, including methods of treating Alzheimer's disease.Type: ApplicationFiled: December 1, 2011Publication date: November 22, 2012Inventors: Geoffrey M. BILCER, Thippeswamy Devasamudram, Sudha V. Ankala, John C. Lilly, Chunfeng Liu, Hui Lei, Arun K. Ghosh, Makoto Inoue
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Publication number: 20120289505Abstract: The present invention relates to heterocyclic compounds in all their stereoisomeric and tautomeric forms; and their pharmaceutically acceptable salts, pharmaceutically acceptable solvates and pharmaceutically acceptable polymorphs. The invention also relates to processes for the manufacture of the heterocyclic compounds and to pharmaceutical compositions containing them. The said compounds and their pharmaceutical compositions are useful in the prevention and treatment of diseases or disorders mediated by diacylglycerol acyltransferase (DGAT), particularly DGAT1. The present invention further provides a method of treatment of such diseases or disorders by administering a therapeutically effective amount of said compounds or their pharmaceutical compositions, to a mammal in need thereof.Type: ApplicationFiled: December 30, 2010Publication date: November 15, 2012Inventors: Ravindra Dnyandev Jadhav, Rajiv Sharma
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Patent number: 8309608Abstract: The present invention relates to the use of compounds which enhance the transcription of endothelial nitric oxide synthase (eNOS) for treating stem and progenitor cells in the cell therapy of patients with ischemic heart diseases such as coronary heart disease or ischemic cardiomyopathy. Treatment of such cells which are isolated from bone marrow, for example, with an eNOS transcription enhancer prior to their administration improves their functional activity and ameliorates neovascularization of the heart and cardiac regeneration.Type: GrantFiled: November 2, 2004Date of Patent: November 13, 2012Assignee: Sanofi-Aventis Deutschland GmbHInventors: Andreas Zeiher, Stefanie Dimmeler, Christopher Heeschen, Hartmut Ruetten
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Patent number: 8304409Abstract: The invention describes novel nitrosated nonsteroidal antiinflammatory drugs (NSAIDs) and pharmaceutically acceptable salts thereof, and novel compositions comprising at least one nitrosated NSAID, and, optionally, at least one compound that donates, transfers or releases nitric oxide, stimulates endogenous synthesis of nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor or is a substrate for nitric oxide synthase, and/or at least one therapeutic agent. The invention also provides novel compositions comprising at least one nitrosated NSAID, and at least one compound that donates, transfers or releases nitric oxide, elevates endogenous levels of endothelium-derived relaxing factor, stimulates endogenous synthesis of nitric oxide or is a substrate for nitric oxide synthase and/or at least one therapeutic agent. The invention also provides novel kits comprising at least one nitrosated NSAID, and, optionally, at least one nitric oxide donor and/or at least one therapeutic agent.Type: GrantFiled: December 11, 2009Date of Patent: November 6, 2012Assignee: Nicox S.A.Inventors: Richard A. Earl, Maiko Ezawa, Xinqin Fang, David S. Garvey, Ricky D. Gaston, Subhash P. Khanapure, L. Gordon Letts, Chia-En Lin, Ramani R. Ranatunge, Stewart K. Richardson, Joseph D. Schroeder, Cheri A. Stevenson, Shiow-Jyi Wey
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Publication number: 20120277222Abstract: Novel compounds and methods for activating the TrkB receptor are provided. The methods include administering in vivo or in vitro a therapeutically effective amount of a compound containing four six-membered rings and a substituted or unsubstituted C5 or C6 heteroaryl or heterocycloalkyl ring and pharmaceutically acceptable salts, prodrugs, and derivatives thereof. Specifically, methods and compounds for the treatment of disorders including neurologic, neuropsychiatric, and metabolic disorders are provided. For example, a method is provided of treating or reducing the risk of depression, anxiety, or obesity in a subject, which includes selecting a subject with or at risk of developing depression, anxiety, or obesity, and administering to the subject a therapeutically effective amount of the described compounds.Type: ApplicationFiled: May 24, 2012Publication date: November 1, 2012Applicant: EMORY UNIVERSITYInventor: Keqiang Ye
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Publication number: 20120277266Abstract: This disclosure concerns novel compounds of Formula (I) as defined in the specification and compositions comprising such novel compounds. These compounds are useful antiviral agents, especially in inhibiting the function of the NS5A protein encoded by Hepatitis C virus (HCV). Thus, the disclosure also concerns a method of treating HCV related diseases or conditions by use of these novel compounds or a composition comprising such novel compounds.Type: ApplicationFiled: July 13, 2012Publication date: November 1, 2012Inventors: Omar D. Lopez, Qi Chen, Makonen Belema, Lawrence G. Hamann
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Publication number: 20120277275Abstract: Compounds of formula (I) are useful in the treatment of diseases where enhanced M3 receptor activation is implicated, such as respiratory tract diseases:Type: ApplicationFiled: April 24, 2012Publication date: November 1, 2012Applicant: PULMAGEN THERAPEUTICS (SYNERGY) LIMITEDInventors: Nicholas Charles Ray, Richard James Bull, Harry Finch, Marco van den Heuvel, Jose Antonio Bravo
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Patent number: 8299102Abstract: The present invention relates to heteroarylcyclopropanecarboxamides of the formula I, in which Het, X, Ra, Rb, Rc, Rd, R1, R2 and R3 have the meanings indicated in the claims, which modulate the transcription of endothelial nitric oxide (NO) synthase and are valuable pharmacologically active compounds. Specifically, the compounds of the formula I upregulate the expression of the enzyme endothelial NO synthase and can be applied in conditions in which an increased expression of said enzyme or an increased NO level or the normalization of a decreased NO level is desired.Type: GrantFiled: June 17, 2009Date of Patent: October 30, 2012Assignee: SanofiInventors: Hartmut Strobel, Paulus Wohlfart, Gerhard Zoller, David William Will
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Patent number: 8299066Abstract: This invention provides a compound of the formula (I): a pharmaceutically acceptable salt or solvate thereof, wherein R1 is substituted or unsubstituted alkyl or the like, R2 is hydrogen or substituted or unsubstituted alkyl, Ring A is monocyclic or bicyclic aromatic heterocycle, R3 is substituted or unsubstituted aryl, substituted or unsubstituted heteroaryl or substituted or unsubstituted heterocycle, R4 is halogen, cyano, substituted or unsubstituted alkyl, substituted or unsubstituted cycloalkyl or the like, m is an integer between 0 and 2, n is an integer between 0 and 5, R is halogen, oxo, cyano, nitro, substituted or unsubstituted alkyl or the like, and p is an integer between 0 and 2 as novel compounds having NPY Y5 antagonistic activity.Type: GrantFiled: January 20, 2012Date of Patent: October 30, 2012Assignee: Shionogi & Co., Ltd.Inventors: Masahiro Sakagami, Hiroshi Hashizume, Satoru Tanaka
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Publication number: 20120270915Abstract: Compounds of Formula 1 are described herein. These compounds may be administered to a patient for treatment of suffering from pain or other FAAH mediated conditions.Type: ApplicationFiled: April 23, 2012Publication date: October 25, 2012Inventors: David F. Woodward, Jose L. Martos, William R. Carling, Neil J. Poloso, Jenny W. Wang
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Publication number: 20120270906Abstract: A method relieves both nociceptive pain and neuropathic pain and has fewer side effects. The compound includes cyclohexane derivatives represented by the following compound, or pharmaceutically acceptable salts thereof or prodrugs thereof.Type: ApplicationFiled: June 27, 2012Publication date: October 25, 2012Applicant: Toray Industries, Inc.Inventors: Yasuhiro Morita, Katsuhiko Iseki, Yuji Sugawara, Hideyuki Tsutsui, Shunsuke Iwano, Naoki Izumimoto, Tadamasa Arai, Hidetoshi Noda, Chihiro Yoshida
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Publication number: 20120264744Abstract: A series of oxazole and thiazole compounds are shown herein to be small molecule inhibitors of the Wnt pathway that specifically target the activity of the stabilized pool of ?-catenin. Oxazole and thiazole compounds are disclosed that have a formula represented by the following: The compounds may be prepared as pharmaceutical compositions, and may be used for the prevention and treatment of a variety of conditions in mammals including humans, including by way of non-limiting example, cancer, and others.Type: ApplicationFiled: April 17, 2012Publication date: October 18, 2012Inventors: Ramanuj DASGUPTA, Foster GONSALVES, Susan Katherine LOGAN, Eugine LEE
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Patent number: 8288423Abstract: The present invention relates to novel oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof, and processes for preparing the same, and pharmaceutical compositions comprising the same. The oxazolidinone derivatives with cyclic amidines, and prodrugs, hydrates, solvates, isomers and pharmaceutically acceptable salts thereof can be usefully employed as an anticoagulant for treating thromboembolism and tumors via inhibition of coagulation factor Xa.Type: GrantFiled: May 9, 2008Date of Patent: October 16, 2012Assignee: Legochem Bioscience Ltd.Inventors: Young Lag Cho, Ho Young Song, Dae Yon Lee, Sung Yoon Baek, Sang Eun Chae, Sang Hui Jo, Yeon Ok Kim, Hyang Sook Lee, Ju Hyun Park, Tae Kyo Park, Sung Ho Woo, Yong Zu Kim
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Patent number: 8288419Abstract: The invention relates to aminopyrazole derivatives of formula (I), wherein A, E, R1 and R2 are as defined in the description, their preparation and their use as pharmaceutically active compounds.Type: GrantFiled: December 12, 2008Date of Patent: October 16, 2012Assignee: Actelion Pharmaceuticals, LtdInventors: Daniel Bur, Oliver Corminboeuf, Sylvaine Cren, Heinz Fretz, Corinna Grisostomi, Xavier Leroy, Julien Pothier, Sylvia Richard-Bildstein
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Publication number: 20120258990Abstract: The present invention relates to heterocyclic compounds of formula (I) which have microbiocidal activity, in particular fungicidal activity: formula (I) wherein G1 and G2 are independently O or S; T is —C(R9R10)—, —C(R11)?C(R12)—, —C?C—, NR13 or O; Y1 and Y2 are independently CR14 or N; Q is —C(?O)—N(R15)-z, —C(?S)—N(R16)-z, —C(?O)—O-z, —N(R17)—C(?O)-z, —N(R18)—C(?S)-z, —N(R19)—C(?O)—O-z or —N(R20)—C(?O)—N(R21)-z, in each case z indicates the bond that is connected to R8; n is 1, 2, 3 or 4 when T is —C(R9R10)—, NR13 or O; n is 1, 2, 3 when T is —C(R11)?C(R12)— or —C?C—; R1, R2, R3, R4, R11, R12 and R14 each independently are hydrogen, halogen, cyano, C1-C4alkyl, or C1-C4haloalkyl; R5, R13, R15, R16, R17, R18, R19, R20 and R21 each independently are hydrogen, C1-C4alkyl or C1-C4alkoxy; R6 and R7 each independently are hydrogen, halogen, cyano, hydroxy, C1-C4alkyl, C1-C4alkoxy, C1-C4alkylthio, C1-C4haloalkyl, C1-C4haloalkoxy, C1-C4haloalkylthio or together from a carbonyl group (?O); R9 and R10 each independentType: ApplicationFiled: November 25, 2010Publication date: October 11, 2012Applicant: SYNGENTA CROP PROTECTION, LLCInventors: Sarah Sulzer, Clemens Lamberth
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Publication number: 20120252798Abstract: The present invention relates to new indole compounds, pharmaceutically acceptable salts or isomers thereof which are useful for the prevention or treatment of cellular necrosis and necrosis-associated diseases. The present invention also relates to a method and a composition for the prevention or treatment of cellular necrosis and necrosis-associated diseases, comprising said indole compounds as an active ingredient.Type: ApplicationFiled: June 11, 2012Publication date: October 4, 2012Inventors: Soon Ha KIM, Hyoung Jin Kim, Sun Young Koo, Sung Bae Lee, Heui Sul Park, Seung Hyun Yoon, Seung Yup Paek, Hyo Shin Kwak, Dong Ook Seo, Eok Park
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Publication number: 20120252796Abstract: The present invention relates to compounds of the general formula (I), their tautomeric forms, their stereoisomers, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, methods for their preparation, use of these compounds in medicine and the intermediates involved in their preparation.Type: ApplicationFiled: September 29, 2010Publication date: October 4, 2012Inventors: Harikishore Pingali, V.V.M. Sairam Kalapatapu, Pankaj Makadia, Mukul R. Jain
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Patent number: 8278268Abstract: Combination therapy comprising PPAR modulators and glucose reabsorption inhibitors useful for the treatment of diabetes and Syndrome X are disclosed.Type: GrantFiled: October 24, 2007Date of Patent: October 2, 2012Assignee: Ortho-McNeil Pharmaceutical, Inc.Inventors: Jacqueline C. Bussolari, Xiaoli Chen, Bruce R. Conway, Keith T. Demarest, Hamish N. M. Ross, Rafael Severino
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Publication number: 20120238601Abstract: The present invention provides compositions of matter, kits and methods for their use in the treatment of cancer. In particular, the invention provides compositions and methods for treating cancer in a subject by inhibiting a poly-ADP-ribose polymerase, as well as providing formulations and modes of administering such compositions.Type: ApplicationFiled: December 12, 2011Publication date: September 20, 2012Applicant: BiPar Sciences, Inc.Inventors: Jerome MOORE, Bruce KEYT, John BURNIER, Barry SHERMAN, Max TOTROV, Valeria S. OSSOVSKAYA
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Publication number: 20120238559Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of PI3-kinase activity.Type: ApplicationFiled: December 3, 2010Publication date: September 20, 2012Applicant: GLAXO GROUP LIMITEDInventors: Ian Robert Baldwin, Kenneth David Down, Paul Faulder, Simon Gaines, Julie Nicole Hamblin, Joelle Le, Christopher James Lunniss, Nigel James Parr, Timothy John Ritchie, John Edward Robinson, Juliet Kay Simpson, Christian Alan Paul Smethurst