Nitrogen Bonded Directly To Ring Carbon Of The Thiazole Ring Patents (Class 514/370)
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Patent number: 8124632Abstract: A new class of alkylsulfonyl-substituted thiazolide compounds is described. These compounds show strong activity against hepatitis virus.Type: GrantFiled: August 1, 2008Date of Patent: February 28, 2012Assignee: Romark Laboratories, L.C.Inventors: Jean-Francois Rossignol, J. Edward Semple
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Patent number: 8124610Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides substituted sulfonamides, compositions comprising these compounds, as well as methods of using these compounds or compositions in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: GrantFiled: July 14, 2008Date of Patent: February 28, 2012Assignee: Icagen Inc.Inventors: Alan Bradley Fulp, Matthew Scott Johnson, Christopher John Markworth, Brian Edward Marron, Darrick Conway Seconi, Christopher William West, Xiaodong Wang, Shulan Zhou
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Patent number: 8119626Abstract: The problem of the present invention is to provide a useful compound as a glucokinase activating agent, which is the oxime derivative of the formula [I]: wherein Ring A is aryl or heteroaryl; Q is cycloalkyl, heterocycle, alkyl or alkenyl; Ring T is heteroaryl or heterocycle; R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl or the like; R3 and R4 are independently hydrogen atom, hydroxy, oxo, halogen atom or the like; R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl or the like; or a pharmaceutically acceptable salt thereof.Type: GrantFiled: November 20, 2008Date of Patent: February 21, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Kazutoshi Sugawara, Tetsuji Matsudaira, Hiroshi Sugama, Masao Nawano, Rikiya Ohashi
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Publication number: 20120028981Abstract: Provided herein are electrophilically enhanced kinase inhibitors. Also provided herein are methods of making and utilizing the same.Type: ApplicationFiled: November 5, 2009Publication date: February 2, 2012Applicant: PRINCIPIA BIOPHARMA INC.Inventor: Richard Miller
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Publication number: 20120029029Abstract: The present invention is directed to substituted thiazol-2-ylamine derivatives and pharmaceutically acceptable salts thereof that inhibit 11?HSD1 and that may be useful in the treatment of diseases in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the treatment of such diseases, disorders, or conditions in which modulation or inhibition of 11?HSD1 is beneficial or where a reduction in intracellular glucorticoid levels is desirable.Type: ApplicationFiled: July 25, 2011Publication date: February 2, 2012Applicant: HIGH POINT PHARMACEUTICALS, LLCInventors: Dharma Rao Polisetti, Suparna Gupta
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Publication number: 20120027879Abstract: Buccal aerosol sprays or capsules using polar and non-polar solvent have now been developed which provide biologically active compounds for rapid absorption through the oral mucosa, resulting in fast onset of effect. The buccal polar compositions of the invention comprise formulation I: aqueous polar solvent, active compound, and optional flavoring agent; formulation II: aqueous polar solvent, active compound, optionally flavoring agent, and propellant; formulation III: non-polar solvent, active compound, and optional flavoring agent; and formulation IV: non-polar solvent, active compound, optional flavoring agent, and propellant.Type: ApplicationFiled: August 3, 2011Publication date: February 2, 2012Inventor: Harry A. DUGGER, III
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Patent number: 8105581Abstract: The present invention provides compositions and methods for inducing neuronal cell differentiation.Type: GrantFiled: December 1, 2006Date of Patent: January 31, 2012Assignees: The Scripps Research Institute, Salk Institute for Biological StudiesInventors: Masaki Warashina, Kyung Hoon Min, Fred Gage, Peter G. Schultz, Sheng Ding, Tomoko Kuwabara
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Publication number: 20120022122Abstract: The present invention provides to methods and compositions that treat or prevent deleterious effects associated with alcohol consumption including alcohol-induced flush reaction and hangover. The methods and compositions include famotidine and optionally succinic acid. The present invention further demonstrates compositions that include famotidine are effective at treating symptoms associated with a flush reaction in subjects that are not significantly responsive to treatments with the H1 antagonist loratidine or the H2 antagonist cimetidine.Type: ApplicationFiled: September 29, 2011Publication date: January 26, 2012Inventor: Richard Tokunaga
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Publication number: 20120022052Abstract: The present invention relates to compounds of formula Ia or Ib below and their tautomers and/or pharmaceutically acceptable salts and compositions and methods of uses thereof.Type: ApplicationFiled: June 29, 2011Publication date: January 26, 2012Inventors: Paul J. Muchowski, Joseph M. Muchowski, Robert Schwarcz, Paolo Guidetti
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Publication number: 20120015926Abstract: This invention relates to compounds of the Formula (I): (Chemical formula should be inserted here as it appears on abstract in paper form) (I) or a pharmaceutically acceptable salt thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF- or combinations thereof.Type: ApplicationFiled: November 9, 2009Publication date: January 19, 2012Inventors: Ling Tong, Brian J. Lavey, Bandarpalle B. Shankar, Seong Heon Kim, Wensheng Yu, Joseph A. Kozlowski, Michael K.C. Wong, Lei Chen, Guowei Zhou, Razia K. Rizvi, Robert Feltz, Aneta Maria Kosinski, De-Yi Yang, Chaoyang Dai, Luke Fire, Vinay Girijavallabhan, Dansu Li, Janeta Popovici-Muller, Judson E. Richard, Kristen E. Rosner, M. Arshad Siddiqui, Liping Yang
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Publication number: 20120010182Abstract: The invention relates to sulfonamide derivatives, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. More particularly the invention relates to new sulfonamide Nav1.7 inhibitors of formula (I): or pharmaceutically acceptable salts thereof, wherein Z1, Ra, Rb, R1, R2, R3, R4 and R5 are as defined in the description. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.Type: ApplicationFiled: July 8, 2011Publication date: January 12, 2012Applicants: ICAGEN INC., PFIZER LIMITEDInventors: Alan Daniel Brown, Marcel John De Groot, Brian Edward Marron, David James Rawson, Thomas Ryckmans, Robert Ian Storer, Paul Anthony Stupple, Nigel Alan Swain, Christopher William West
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Publication number: 20120010186Abstract: Heterocyclic compounds of structural formula I are inhibitors of stearoyl-coenzyme A delta-9 desaturase (SCD). The compounds of the present invention are useful for the prevention and treatment of conditions related to abnormal lipid synthesis and metabolism, including cardiovascular disease; atherosclerosis; obesity; diabetes; neurological disease; Metabolic Syndrome; insulin resistance; cancer, liver steatosis; and non-alcoholic steatohepatitis.Type: ApplicationFiled: March 18, 2010Publication date: January 12, 2012Applicant: MERCK FROSST CANADA LTD.Inventors: Nicolas Lachance, Serge Leger, Renata M. Oballa, David Powell, Geoffrey K. Tranmer, Evelyn Martins, Yves Gareau
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Publication number: 20120004099Abstract: Disclosed is a composition for controlling plant diseases, which contains ethaboxam and metconazole as active ingredients. Also disclosed is a method for controlling plant diseases, which is characterized in that effective amounts of ethaboxam and metconazole are applied to a plant or the soil where the plant grows.Type: ApplicationFiled: November 20, 2009Publication date: January 5, 2012Inventors: Makoto Kurahashi, Yuichi Matsuzaki
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Patent number: 8088806Abstract: The present invention provides compounds, salts and hydrates of Formula I, wherein the variables Ar1, R2, R3, R4, r, q, and t are defined herein. Certain compounds of Formula I described herein possess potent antiviral activity. The invention also provides compounds of Formula I that are potent and/or selective inhibitors of Hepatitis C virus replication. Certain compounds described herein inhibit assembly of the HCV replication complex. The invention also provides pharmaceutical compositions containing one or more compounds of Formula I, or a salt, solvate, or acylated prodrug of such compounds, and one or more pharmaceutically acceptable carriers, excipients, or diluents. The invention further comprises methods of treating patients suffering from certain infectious diseases by administering to such patients an amount of a compound of Formula I effective to reduce signs or symptoms of the disease. These infectious diseases include viral infections, particularly HCV infections.Type: GrantFiled: May 9, 2006Date of Patent: January 3, 2012Assignee: Achillion Pharmaceuticals, Inc.Inventors: Suoming Zhang, Avinash Phadke, Cuixian Liu, Xiangzhu Wang, Jesse Quinn, Dawei Chen, Venkat Gadhachanda, Shouming Li, Milind Deshpande
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Patent number: 8084479Abstract: The invention relates to methods of using thiazole compounds of Formula I and Formula II and compositions thereof for treating diseases mediated by protein kinase B (PKB) such as cancer and other proliferative disorders where the variables have the definitions provided herein.Type: GrantFiled: February 11, 2009Date of Patent: December 27, 2011Assignee: Amgen Inc.Inventors: Qingping Zeng, John G. Allen, Matthew P. Bourbeau, Celia Dominguez, Christopher H. Fotsch, Nianhe Han, Fang-Tsao Hong, Xin Huang, Matthew R. Lee, Aiwen Li, Qingyian Liu, James T. Rider, Seifu Tadesse, Andrew S. Tasker, Vellarkad N. Viswanadhan, Xianghong Wang, Kurt E. Weiler, George E. Wohlhieter, Guomin Yao, Chester Chenguang Yuan
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Publication number: 20110311636Abstract: A method for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine is administered three times per day.Type: ApplicationFiled: August 25, 2011Publication date: December 22, 2011Inventors: George Tidmarsh, Barry L. Golombik, Puneet Sharma
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Publication number: 20110311637Abstract: A method for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine is administered three times per day.Type: ApplicationFiled: August 25, 2011Publication date: December 22, 2011Inventors: George Tidmarsh, Barry L. Golombik, Puneet Sharma
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Publication number: 20110313009Abstract: The present invention generally relates to unit dosage forms of naproxen and H2-receptor antagonists, comprising an immediate-release formulation of naproxen; an immediate-release formulation of an H2-receptor antagonist, and a delayed-burst release formulation of an H2-receptor antagonist.Type: ApplicationFiled: July 17, 2009Publication date: December 22, 2011Inventors: George Tidmarsh, Leah Appel
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Patent number: 8080668Abstract: The present application provides novel thiazole derivatives that are useful as activators of Adenosine 5?-Monophosphate-Activated Protein Kinase and pharmaceutical compositions containing such compounds.Type: GrantFiled: June 30, 2006Date of Patent: December 20, 2011Assignees: Dr. Reddy's Laboratories Limited, Dr. Reddy's Laboratories, Inc.Inventors: Vijay Kumar Potluri, Saibal Kumar Das, Pradip Kumar Sasmal, Javed Iqbal, Parimal Misra, Ranjan Chakrabarti, Rashmi Talwar
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Publication number: 20110301180Abstract: It has been discovered that inhibiting mitochondrial respiration in platelets reduces platelet activation or platelet aggregation. Certain heterocyclic compounds significantly reduced one or more platelet functions including clumping, sticking or platelet-stimulated clotting. Thus diseases or disorders mediated by inappropriately high levels of platelet activation or platelet aggregation can be treated by administering a therapeutically effective amount of a heterocyclic compound or nonheterocyclic mitochondrial inhibitor that significantly reduces one or more platelet functions including clumping, sticking or platelet-stimulated clotting, preferably in a reversible manner.Type: ApplicationFiled: April 25, 2011Publication date: December 8, 2011Applicant: Stanford UniversityInventors: James P. Collman, Paul Clifford Herrmann, David Alvin Tyvoll, Richard Decreau, Brian Stanley Bull, Christopher Jeffrey Barile
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Publication number: 20110301155Abstract: The present invention aims to provide a glucokinase activator useful as a pharmaceutical agent such as an agent for the prophylaxis or treatment of diabetes, obesity and the like, and the like.Type: ApplicationFiled: June 18, 2008Publication date: December 8, 2011Inventors: Tsuneo Yasuma, Shigekazu Sasaki, Osamu Ujikawa, Yasufumi Miyamoto, Stephen L. Gwaltney, Sheldon Cao, Andy Jennings
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Patent number: 8071605Abstract: Compounds of formula (I) and their pharmaceutically acceptable salts are described. Processes for their preparation, pharmaceutical compositions containing them, their use as medicaments and their use in the treatment of bacterial infections are also described.Type: GrantFiled: December 10, 2009Date of Patent: December 6, 2011Assignee: AstraZeneca ABInventors: Gregory Basarab, Pamela Hill, Brian Sherer, Fei Zhou
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Publication number: 20110294829Abstract: The present invention relates to hydroximoyl-heterocycle derivatives of formula (I) wherein T represents a substituted or non-substituted heterocyclyl group, Q represents a carbo or heterocyclic group, A represent a carbo or heterocyclic group or a carbo or hetero-polycylic group, and L1 represents various linking groups, their process of preparation, intermediate compounds for their preparation, their use as fungicide active agents, particularly in the form of fungicide compositions, and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: ApplicationFiled: December 8, 2009Publication date: December 1, 2011Inventors: 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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Publication number: 20110293673Abstract: The present invention provides a film-form base having one or more sugars or sugar alcohols dispersed as fine particles therein, and also provides a film-form preparation containing the base and a drug. The base is produced by dispersing, in an organic solvent having a solubility parameter of 9.7 or higher, an edible polymer soluble in water and the organic solvent, and particles of one or two or more compounds selected from the group consisting of mono- to hexasaccharide sugars and sugar alcohols thereof which have an average particle size of 0.1 ?m to 60 ?m and are insoluble in an organic solvent. The present invention can therefore provide oral film-form base and preparation which have a rapid dissolution profile in the mouth and sufficient film strength, and provide a reduced sticky sensation attributed to the water-soluble polymer in the mouth and an improved feel when handled with the fingers.Type: ApplicationFiled: March 6, 2009Publication date: December 1, 2011Applicant: NITTO DENKO CORPORATIONInventors: Daisuke Asari, Mitsuhiko Hori, Keiko Ogawa
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Patent number: 8067451Abstract: A method for administration of ibuprofen to a subject in need of ibuprofen treatment is provided, in which an oral dosage form comprising a therapeutically effective amount of ibuprofen and a therapeutically effective amount of famotidine is administered three times per day.Type: GrantFiled: July 17, 2007Date of Patent: November 29, 2011Assignee: Horizon Pharma USA, Inc.Inventors: George Tidmarsh, Barry L. Golombik, Puneet Sharma
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Patent number: 8067033Abstract: Stable pharmaceutical compositions of famotidine and ibuprofen in a single unit dosage form are disclosed herein. The compositions comprise a famotidine core having a reduced or minimal surface area surrounded by a layer of ibuprofen. In some embodiments, the ibuprofen is in direct physical contact with the famotidine.Type: GrantFiled: November 26, 2008Date of Patent: November 29, 2011Assignee: Horizon Pharma USA, Inc.Inventors: Jerry Xu, George Tidmarsh
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Patent number: 8063080Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the inhibition of sodium ion flux through voltage-gated sodium channels. More particularly, the invention provides heterocyclic aryl sulfonamides, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders, particularly pain and chronic pain by blocking sodium channels associated with the onset or recurrence of the indicated conditions. The compounds, compositions and methods of the present invention are of particular use for treating neuropathic or inflammatory pain by the inhibition of ion flux through a voltage-gated sodium channel.Type: GrantFiled: September 16, 2009Date of Patent: November 22, 2011Assignee: Icagen, Inc.Inventors: Alan Fulp, Brian Marron, Mark J. Suto, Xiaodong Wang
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Patent number: 8058296Abstract: The present invention provides to methods and compositions that treat or prevent deleterious effects associated with alcohol consumption including alcohol-induced flush reaction and hangover. The methods and compositions include famotidine and optionally succinic acid. The present invention further demonstrates compositions that include famotidine are effective at treating symptoms associated with a flush reaction in subjects that are not significantly responsive to treatments with the H1 antagonist loratidine or the H2 antagonist cimetidine.Type: GrantFiled: November 25, 2008Date of Patent: November 15, 2011Inventor: Richard Tokunaga
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Patent number: 8053581Abstract: The present invention relates to 2,4,5-trisubstituted thiazole compounds of formula (I) or all possible isomers, prodrugs, pharmaceutically acceptable salts, solvates or hydrates thereof for the inhibition of plasma PLTP activity and/or plasma CETP activity, wherein the substituents are as defined in the specification; a process for the preparation of the compounds of formula (I); a pharmaceutical composition comprising the compound of formula (I) and its use for the preparation of a medicament for treatment and/or prevention of diseases associated with the increased plasma PLTP activity and/or the increased plasma CETP activity in a mammal, such as atherosclerosis, cardiovascular diseases and peripheral vascular diseases, etc.Type: GrantFiled: August 15, 2006Date of Patent: November 8, 2011Assignee: Institute of Pharmacology and Toxicology Academy of Military Medical Sciences P.L.C. ChinaInventors: Song Li, Changbin Guo, Xiancheng Jiang, Junhai Xiao, Zhong Wu
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Publication number: 20110269748Abstract: This invention concerns the use of a compound of formula (I) a N-oxide, a pharmaceutically acceptable addition salt, a quaternary amine and a stereochemically isomeric form thereof, wherein Z is hydrogen, halo, C1-6alkyl, Het1, HO—C1-6alkyl-, cyano-C1-6alkyl-, amino-C(?O)—C1-6alkyl-, formylamino-C1-6alkyl-, C1-6alkyl-C(?O)—NH—C1-6alkyl-, mono- or di(C1-6alkyl)amino-C(?O)—C1-6alkyl-, phenyl-C1-6alkyl-, or Het4-C1-6alkyl-; Q is phenyl, pyridyl, benzofuranyl, 2,3-dihydro-benzofuranyl, pyrazolyl, isoxazolyl or indazolyl wherein each of said ring systems is optionally being substituted with up to three substituents each independently selected from halo, cyano, C1-6alkyl, C1-6alkyl-O—, C1-6alkylthio, Ar or polyhaloC1-6alkyl; L is phenyl, pyridyl, pyrimidazolyl, 8-Azapyrimidazolyl, pyridazinyl, imidazothiazolyl or furanyl wherein each of said ring systems may optionally be substituted with one or two or more substituents, each substituent independently being selected from halo, hydroxy, amino, cyano, C1-6alkylType: ApplicationFiled: February 13, 2008Publication date: November 3, 2011Inventors: Johannes Wilhelmus John F. Thuring, Gregor James MacDonald, Christopher James Grantham, Theodorus Dinklo, Anne Simone Josephine Lesage
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Publication number: 20110263421Abstract: The present invention provides a composition for controlling pests comprising, as active ingredients, ethaboxam and a neonicotinoid compound represented by formula (1).Type: ApplicationFiled: November 20, 2009Publication date: October 27, 2011Inventors: Makoto Kurahashi, Yuichi Matsuzaki
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Publication number: 20110263556Abstract: This invention relates to compounds of formula I, their use as inhibitors of the microsomal prostaglandin E2 synthase-1 (mPGES-1), pharmaceutical compositions containing them, and their use as medicaments for the treatment and/or prevention of inflammatory diseases and associated conditions such as inflammatory/nociceptive pain. A, M, R1, R2, R7, Ra, Rb, Q3, Q4, Q6, Z2, Z4, Z5, Z6 and W have meanings given in the description.Type: ApplicationFiled: October 20, 2010Publication date: October 27, 2011Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Henning PRIEPKE, Henri DOODS, Raimund KUELZER, Roland PFAU, Dirk STENKAMP, Robert ROENN, Benjamin PELCMAN
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Patent number: 8044213Abstract: The invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.Type: GrantFiled: December 10, 2009Date of Patent: October 25, 2011Assignee: Hoffmann-La Roche Inc.Inventors: Jianping Cai, Shaoqing Chen, Yi Chen, Xin-Jie Chu, Robert Alan Goodnow, Jr., Kang Le, Kin-Chun Luk, Steven Gregory Mischke, Peter Michael Wovkulich
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Publication number: 20110257179Abstract: The present invention relates to novel compounds of Formula (I), wherein M, P, A and (B)n are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.Type: ApplicationFiled: January 12, 2010Publication date: October 20, 2011Inventor: Christelle Bolea
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Publication number: 20110245263Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: ApplicationFiled: June 15, 2011Publication date: October 6, 2011Applicant: SANOFI-AVENTISInventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
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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: 20110236436Abstract: A pharmaceutical composition for modified release comprising (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or a pharmaceutically acceptable salt thereof, and a carrier for a sustained release pharmaceutical composition, wherein a dissolution rate of the drug from the composition is less than 85% after 30 minutes from the beginning of a dissolution test, is disclosed.Type: ApplicationFiled: March 28, 2011Publication date: September 29, 2011Applicant: Astellas Pharma Inc.Inventors: Yuuki Takaishi, Soichiro Nakamura
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Publication number: 20110237589Abstract: The present invention relates to guanidine compounds of the general formula I corresponding enantiomeric, diastereomeric and/or tautomeric forms thereof as well as pharmaceutically acceptable salts thereof. The present compound further relates to the use of guanidine compounds as binding partners for 5-HT5 receptors for the treatment of diseases which are modulated by a 5-HT5 receptor activity, in particular for the treatment of neurodegenerative and neuropsychiatric disorders as well as the associated signs, symptoms and dysfunctions.Type: ApplicationFiled: February 4, 2011Publication date: September 29, 2011Inventors: Astrid Netz, Wilhelm Amberg, Udo Lange, Michael Ochse, Charles W. Hutchins, Francisco-Xavier Garcia-Ladona, Wolfgang Wernet, Andreas Kling, Andrea Hager-Wernet
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Patent number: 8026266Abstract: Compositions, and methods of use thereof, are provided for the treatment of painful neuropathy by local or topical delivery of compounds that interact with ?-adrenergic receptors, especially an alpha2 adrenergic agonist such as clonidine, to the entire painful area such that the need for systemic dosing is minimized. The compounds are delivered to or adjacent to painful areas in patients with painful length dependent neuropathy, and other neuropathies that affect the pain signaling fibers in the skin. A preferred compound for the treatment of patients with length dependent neuropathy is clonidine applied in a transdermal patch, gel, ointment, lotion, liposomal formulation, cream, or emulsion, wherein the concentration is sufficient to provide an effective dose in the painful area or immediately adjacent areas.Type: GrantFiled: November 7, 2006Date of Patent: September 27, 2011Assignee: Arcion Therapeutics, Inc.Inventor: James N. Campbell
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Publication number: 20110230530Abstract: (R)-2-(2-aminothiazol-4-yl)-4?-[2-[(2-hydroxy-2-phenylethyl)amino]ethyl]acetic acid anilide or its salt shows a potent bladder relaxation effect in “isolated rat bladder smooth muscle relaxation test”, dose-dependently lowers the contraction frequency of rhythmic bladder contractions in “rat rhythmic bladder contraction measurement test” and, moreover, prolongs the urination intervals in “urination functions measurement test on cyclophosphamide-induced overactive bladder model rat”. Owing to these effects, the above compound is useful as a remedy for overactive bladder.Type: ApplicationFiled: May 27, 2011Publication date: September 22, 2011Applicant: ASTELLAS PHARMA INC.Inventors: Toshiyuki TAKASU, Shuichi SATO, Masashi UKAI, Tatsuya MARUYAMA
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Patent number: 8022079Abstract: Novel compounds having the general formula (I) below: are useful in a wide variety of applications in human or veterinary medicine (in dermatology, and also in the fields of cardiovascular diseases, immune diseases and/or diseases associated with lipid metabolism), or, alternatively are formulated into cosmetic compositions.Type: GrantFiled: September 18, 2009Date of Patent: September 20, 2011Assignee: Galderma Research & DevelopmentInventors: Laurence Clary, Etienne Thoreau, Michel Rivier, Jerome Aubert, Laurent Chantalat, Johannes Voegel
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Publication number: 20110224269Abstract: The invention relates to compounds, compositions, and methods for diminishing pain in a subject in need thereof comprising administering the compounds and compositions herein described.Type: ApplicationFiled: March 8, 2011Publication date: September 15, 2011Inventors: James C. Mannion, Scott L. Dax
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Publication number: 20110224075Abstract: The present invention relates to pesticidal mixtures comprising as active compounds 1) at least one aminothiazoline compound I of formula I: wherein R1 is selected from hydrogen, COCH3, COCH2CH3 or COCH2C(CH3)3; R2 and R3 together with the carbon atoms of the phenyl ring to which they are attached form a ring which, depending on the tautomeric formula I a) or b) is depicted as: a benzene ring, a saturated 5-, 6-, or 7-membered carbocycle, a partially unsaturated 5-, 6-, or 7-membered carbocycle, a 5-, 6-, or 7-membered saturated heterocycle, a partially unsaturated 5-, 6-, or 7-membered heterocycle, which heterocycles contain 1, 2, or 3 heteroatoms selected from O, S and N as ring members, and a 5- or 6-membered heteroaromatic ring which contains 1, 2, or 3 heteroatoms selected from O, S and N as ring members, and wherein the ring is unsubstituted or may carry any combination of 1, 2, 3, or 4 radicals selected from the group consisting of halogen, CH3, CH2CH3, CF3, CH3O, cyano and (?O) (oxo); R4 is seType: ApplicationFiled: March 24, 2009Publication date: September 15, 2011Applicant: BASF SEInventors: Markus Kordes, Ronan Le Vezouet, Jurgen Langewald, Ralph Paulini, Deborah L. Culbertson, Douglas D. Anspaugh, Luiz Antonio Jose, Hassan Oloumi-Sadeghi
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Publication number: 20110224230Abstract: Compounds of formula (I): wherein variables B, G1, G2, G3, G4, Ea, Eb, Ec, A1, A2, A3, A4, R6 and RPG and Y are as described herein, which are antagonists of CGRP receptors and which are useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.Type: ApplicationFiled: September 10, 2009Publication date: September 15, 2011Inventor: Craig A. Stump
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Publication number: 20110218160Abstract: The present invention relates to an arylalkylamine compound represented by the following formula [I] or a pharmaceutically acceptable salt thereof, a process for preparing the same, and use of the above-mentioned compound as an activating compound (CaSR agonist) of a Ca sensing receptor, a pharmaceutical composition containing the above-mentioned compound as an effective ingredient, etc.Type: ApplicationFiled: May 12, 2011Publication date: September 8, 2011Inventors: Hiroshi Miyazaki, Junko Tsubakimoto, Kosuke Yasuda, Iwao Takamuro, Osamu Sakurai, Tetsuya Yanagida, Yutaka Hisada
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Patent number: 8012971Abstract: Disclosed is a method for the prevention and/or treatment of a chronic obstructive pulmonary disease by administrating a 5-membered cyclic compound represented by the formula below: or a pharmaceutically acceptable salt of the compound or a prodrug of the compound or salt: wherein X represents an oxygen or sulfur atom; R1 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; R2 represents a hydrogen atom, a substituted or unsubstituted alkyl or the like; Y1 represents single bond, a substituted or unsubstituted alkylene or the like; the wavy line means an (E) or (Z) coordination; R3 represents a hydrogen atom, a substituted or unsubstituted aryl or the like; Y2 represents a substituted or unsubstituted alkylene or an alkenylene; R4 represents a hydrogen atom, a substituted or unsubstituted alkanoyl or the like; and R5 represents a hydrogen atom or a substituted or unsubstituted alkyl.Type: GrantFiled: April 28, 2006Date of Patent: September 6, 2011Assignee: Dainippon Sumitomo Pharma Co., Ltd.Inventors: Toshinari Sugasawa, Takashi Nakajima, Hitoshi Fujita, Toshio Kanai
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Publication number: 20110212951Abstract: The present disclosure relates to compounds effective as human protein tyrosine phosphatase beta (HPTP-?) inhibitors thereby regulating angiogenesis. The present disclosure further relates to compositions comprising said human protein tyrosine phosphatase beta (HPTP-?) inhibitors, and to methods for regulating angiogenesis.Type: ApplicationFiled: August 4, 2010Publication date: September 1, 2011Inventors: Jeffery Lyle Gray, Kande K.D. Amarasinghe, Cynthia Monesa Clark, Ryan Matthew Nichols, Matthew B. Maier
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Publication number: 20110207785Abstract: The present invention relates to (R,S) 2-aryl-propionic acids and derivatives, their single enantiomer (S) and to pharmaceutical compositions containing them, which are used in the prevention and treatment of tissue damage due to the exacerbated recruitment of polymorphonucleated neutrophils (PIvTN leukocytes) at inflammation sites. The present invention provides compounds for use in the treatment of transient cerebral ischemia, bullous pemphigo, rheumatoid arthritis, idiopathic fibrosis, glomerulonephritis and damages caused by ischemia and reperfusion.Type: ApplicationFiled: September 18, 2009Publication date: August 25, 2011Applicant: Dompe S.p.A.Inventors: Marcello Allegretti, Andrea Aramini, Gianluca Bianchini, Maria Candida Cesta
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Patent number: 8003677Abstract: The invention relates to heterocyclic derivatives of formula I wherein R, R1, A, B, D, M, L and n are as defined herein, or their physiologically compatible salts, their pharmaceutical compositions and their uses as SCD1 inhibitors.Type: GrantFiled: October 26, 2009Date of Patent: August 23, 2011Assignee: Sanofi-AventisInventors: Gerhard Zoller, Marc Dietrich Voss, Stefanie Keil, Andreas Herling, Hans Matter
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Publication number: 20110201660Abstract: The combination of ethaboxam and transgenic plants provides enhanced plant protection in controlling plant disease. According to the present invention, an application of an effective amount of ethaboxam to transgenic plants applied to plant foliage parts; soil-applied in drench or soil incorporation; or applied to seed using seed slurry application, seed film coating and seed pelleting technologies for seed, gives a good controlling effect on plant diseases. Application of ethaboxam to transgenic plants encompasses all monocotyledonous and dicotyledonous crop types.Type: ApplicationFiled: September 11, 2009Publication date: August 18, 2011Inventors: Christopher B. Meador, Karen S. Arthur