1,3-thiazoles (including Hydrogenated) Patents (Class 514/365)
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Publication number: 20140135332Abstract: The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: April 20, 2012Publication date: May 15, 2014Applicant: BIOTA SCIENTIFIC MANAGEMENT PTY LTDInventors: David John Haydon, Lloyd George Czaplewski, Neil Robert Stokes, David Davies, Ian Collins, James T Palmer, Jeffrey Peter Mitchell, Gary Robert William Pitt, Daniel Offermann
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Patent number: 8722678Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G, W2 and Z are as defined in the disclosure. Also disclosed are compositions containing the compounds of Formula 1 and methods for controlling plant disease caused by a fungal pathogen comprising applying an effective amount of a compound or a composition of the invention. Also disclosed are compounds of Formula 1A including all stereoisomers, N-oxides, and salts thereof, wherein E, X, G and Z1 are as defined in the disclosure. Also disclosed is the use of the compounds of Formula 1A as intermediates for preparing compounds of Formula 1.Type: GrantFiled: April 15, 2011Date of Patent: May 13, 2014Assignee: E I du Pont de Nemours and CompanyInventors: Mary Ann Hanagan, Eric Allen Marshall
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Patent number: 8722899Abstract: Compounds represented by structural formulas described herein, such as Structural Formula (I): or a pharmaceutically acceptable salt thereof are useful in treating conditions such as metal overload, oxidative stress, and neoplastic and preneoplastic conditions.Type: GrantFiled: September 28, 2012Date of Patent: May 13, 2014Assignee: University of Florida Research Foundation, Inc.Inventor: Raymond J. Bergeron, Jr.
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Patent number: 8722901Abstract: Heteroaryl compounds, processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of diseases or disorders mediated by Diacylglycerol acyltransferase (DGAT) enzyme, particularly DGAT-1 is described.Type: GrantFiled: November 1, 2010Date of Patent: May 13, 2014Assignee: Piramal Enterprises LimitedInventors: Ravindra Dnyandev Jadhav, Rajiv Sharma, Kishorkumar Shivajirao Kadam, Shivaji Sadashiv Kandre
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Publication number: 20140128376Abstract: Pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein X is a thiazolyl, picolinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: January 13, 2014Publication date: May 8, 2014Applicant: Genentech, Inc.Inventor: Xiaojing Wang
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Publication number: 20140128384Abstract: The present invention relates to imidazole, oxazole and thiazole derivatives of tumor-targeted drug combretastatin A4, and phosphate esters, sulfonate esters or pharmaceutically acceptable salts, glycoside derivatives, solvates thereof, wherein the A-ring comprises a 3,5-dimethoxyphenyl group having a substituent at the 4-position. The pharmacological activity assays have demonstrated that the compounds of the present invention have good in vitro anti-tumor activity and excellent tubulin inhibitory effect.Type: ApplicationFiled: July 4, 2012Publication date: May 8, 2014Applicant: NANJING SANHOME PHARMACEUTICAL CO., LTD.Inventors: Yong Wang, Cang Zhang, Xiaorong Liu, Yan Zhang, Yunyun Wang, Wenping Zhang
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Publication number: 20140128439Abstract: Methods of treating gout flares comprising administering a composition comprising a first urate-lowering agent are disclosed. In some aspects, the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salt thereof. Other aspects provide for methods of reducing the number, duration, frequency or intensity of gout flares experienced by a subject.Type: ApplicationFiled: August 7, 2013Publication date: May 8, 2014Applicant: Metabolex, Inc.Inventors: Brian Edward Lavan, Gopal Chandra Saha, Brian K. Roberts, Charles A. McWerther
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Publication number: 20140127158Abstract: A method of treating hepatitis C virus infection, comprising administering to a subject in need thereof (a) an effective amount of at least one HCV inhibitor selected from the group consisting of an HCV NS3 inhibitor, an HCV NS5B inhibitor, ribavirin, and an IFN-?; and (b) an effective amount of an anti-HCV compound of formula (I).Type: ApplicationFiled: November 6, 2013Publication date: May 8, 2014Applicant: National Health Research InstituteInventors: Andrew Yueh, Yu-Sheng Chao
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Publication number: 20140128383Abstract: The present invention relates to compounds, their use in the treatment or the prevention of viral disorders, including HIV.Type: ApplicationFiled: April 6, 2012Publication date: May 8, 2014Applicant: LABORATOIRE BIODIMInventors: Sophie Chasset, Francis Chevreuil, Benoit Ledoussal, Frédéric Le Strat, Richard Benarous
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Publication number: 20140128437Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.Type: ApplicationFiled: January 10, 2014Publication date: May 8, 2014Applicants: President and Fellows of Harvard College, TRUSTEES OF BOSTON UNIVERSITY, THE BRIGHAM AND WOMEN'S HOSPITAL, INC., Tufts UniversityInventors: Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterrev, John A. Proco, JR.
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Publication number: 20140128438Abstract: Methods of treating gout flares comprising administering a composition comprising a first urate-lowering agent are disclosed. In some aspects, the first urate-lowering agent is (?)-halofenate, (?)-halofenic acid, or a pharmaceutically acceptable salt thereof. Other aspects provide for methods of reducing the number, duration, frequency or intensity of gout flares experienced by a subject.Type: ApplicationFiled: November 2, 2012Publication date: May 8, 2014Inventors: Brian Edward Lavan, Gopal Chandra Saha, Charles A. McWherter, Brian K. Roberts
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Publication number: 20140128427Abstract: Provided are a novel derivative of 5-carbamoyl adamantan-2-yl amide or a pharmaceutically acceptable salt thereof, and a pharmaceutical use thereof for inhibiting the activity of 11?-hydroxystreroid dehydrogenase type 1 (11b-HSD1) or for preventing and/or treating various diseases mediated by 11?-hydroxystreroid dehydrogenase type 1.Type: ApplicationFiled: June 11, 2012Publication date: May 8, 2014Applicant: SK BIOPHARMACEUTICALS CO., LTD.Inventors: Coo-Min Chung, Choon-Ho Ryu, Yoon-Kyeong Lee, Jin-Sook Moon, Hye-Sung Lee, Seon-Jeong Lee, Kyung-Seok Oh
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Patent number: 8716322Abstract: Peptide-based compounds including heteroatom-containing, three-membered rings efficiently and selectively inhibit specific activities of N-terminal nucleophile (Ntn) hydrolases associated with the proteasome. The peptide-based compounds include an epoxide or aziridine, and functionalization at the N-terminus. Among other therapeutic utilities, the peptide-based compounds are expected to display anti-inflammatory properties and inhibition of cell proliferation. Oral administration of these peptide-based proteasome inhibitors is possible due to their bioavailability profiles.Type: GrantFiled: November 9, 2006Date of Patent: May 6, 2014Assignee: Onyx Therapeutics, Inc.Inventors: Han-Jie Zhou, Congcong M. Sun, Kevin D. Shenk, Guy J. Laidig
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Publication number: 20140121249Abstract: Disclosed are compositions having activity against MRSA and/or VRSA, and methods of using the compositions to treat microbial infections.Type: ApplicationFiled: October 31, 2013Publication date: May 1, 2014Inventors: Mark Stanley Cushman, Mohamed Seleem, Abdelrahman S. Mayhoub
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Publication number: 20140121236Abstract: Disclosed is a compound for treatment of Myotonic Dystrophy type 1 having the formula: Wherein X is selected from the group consisting of O, N, C, or S, Y is a homo- or heteroatomic 5-membered ring comprising one or more atoms selected from the group consisting of N, O, S, and C, Z is an optionally substituted aryl group or optionally substituted heteroaryl, including but not limited to halogenated benzenes, pyridines, substituted benzene, substituted pyridine, R2=hydroxy, acyl, alkoxyl, esters, ethers, cyclic ethers, and lactones, R3=H, alkyl, an optionally substituted alkyl, aliphatic ether, ester, cyclic unsaturated and aromatic ring groups, and R1, R4 and R5 are independently selected from the group consisting of hydrogen, halogen, alkyl, and alkoxyl or a pharmaceutically or cosmetically acceptable salt, solvate, or hydrate thereof.Type: ApplicationFiled: November 19, 2013Publication date: May 1, 2014Applicant: UNIVERSITY OF SOUTHERN CALIFORNIAInventors: Sita REDDY, Lucio COMAI, Nouri NEAMATI
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Publication number: 20140121206Abstract: The present invention relates to spirocarbamate compounds of Formula (I) in which R1, (R2)Y, R3, R4, X and A have the meanings given in the specification. The invention further provides pharmaceutical compositions containing the compounds or pharmaceutically acceptable salts thereof and relates to their use of these compounds as TRPV4 antagonists in treating or preventing conditions associated with TRPV4 imbalance.Type: ApplicationFiled: June 15, 2012Publication date: May 1, 2014Applicant: GlaxoSmithKliine, LLCInventors: Carl Brooks, Mui Cheung, Hilary Schenck Eidam, Krista B. Goodman, Marlys Hammond, Mark A. Hilfiker, Tram H. Hoang, Jaclyn R. Patterson, Patrick Stoy, Guosen Ye
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Patent number: 8710087Abstract: Disclosed herein are new salts and polymorphs of desazadesferrithiocin polyether (DADFT-PE) analogues, as well as pharmaceutical compositions comprising them and their application as metal chelation agents for the treatment of disease. Methods of chelation of iron and other metals in a human or animal subject are also provided for the treatment of metal overload and toxicity.Type: GrantFiled: August 4, 2011Date of Patent: April 29, 2014Assignee: Ferrokin Biosciences, Inc.Inventors: Amy E. Tapper, Hugh Y. Rienhoff, Jr., Stephan D. Parent, Patricia Andres, Jason A. Hanko, Huamin Zhang
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Publication number: 20140112992Abstract: The present invention provides a process for the preparation of 2-(4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention also provides a process for the preparation of 2-(3-formyl-4-hydroxyphenyl)-4-methylthiazole-5-carboxylic acid ethyl ester. The present invention further provides novel crystalline Forms of febuxostat, processes for their preparation and pharmaceutical compositions comprising them. The present invention further provides febuxostat crystalline particles having a mean particle size of less than about 25 ?m, the methods for the manufacture of said crystalline particles, and pharmaceutical compositions comprising said crystalline particles.Type: ApplicationFiled: May 21, 2012Publication date: April 24, 2014Applicant: HETERO RESEARCH FOUNDATIONInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Matta Ramakrishna Reddy, Bandi Vamsi Krishna
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Patent number: 8703962Abstract: The invention relates to compounds of formula I and pharmaceutically acceptable derivatives thereof, compositions comprising an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof, and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a compound of formula I or a pharmaceutically acceptable derivative thereof.Type: GrantFiled: October 22, 2009Date of Patent: April 22, 2014Assignee: Purdue Pharma L.P.Inventors: Donald J. Kyle, Laykea Tafesse
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Publication number: 20140107169Abstract: A process for formulating certain epothilone analogs for parenteral administration is disclosed wherein the analog is dissolved in a mixture of at least 50% by volume tertiary-butanol in water, the mixture is lyophilized, the resulting lyophilized product is packaged in one vial with a sufficient amount of solvent comprising anhydrous ethanol and a suitable nonionic surfactant in a second vial. All steps are carried out with protection from light. In use, the contents of the second or diluent vial are added to the lyophilized product and mixed to constitute the epothilone analog and the resulting solution is diluted with a suitable diluent to produce a solution for intravenous injection containing the epothilone analog in a concentration of from about 0.1 mg/mL to about 0.9 mg/mL. A preferred surfactant is polyethoxylated castor oil and a preferred diluent is Lactated Ringer's Injection.Type: ApplicationFiled: December 19, 2013Publication date: April 17, 2014Inventors: Rebanta Bandyopadhyay, Timothy M. Malloy, Andrea Panaggio, Krishnaswamy Srinivas Raghavan, Sailesh Amilal Varia
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Publication number: 20140107134Abstract: The invention relates to compounds of formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, or prodrug thereof wherein X, Y, A, Z, L and n are defined herein. These compounds are useful as immunosuppressive agents and for treating and preventing inflammatory conditions and immune disorders.Type: ApplicationFiled: September 27, 2013Publication date: April 17, 2014Applicant: Synta Pharmaceuticals Corp.Inventors: Yu Xie, Mats Holmqvist, Jerome Mahiou, Mitsunori Ono, Lijun Sun, Shoujun Chen, Shijie Zhang, Jun Jiang, Dinesh Chimmanamada, Chih-Yi Yu
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Publication number: 20140107112Abstract: The present invention relates to compositions for controlling plant pests, which contain the compound of the formula (I) in a mixture with fungicidally active compounds, except for cyclopropylcarboxamide derivatives and azolylmethylcycloalkanes.Type: ApplicationFiled: December 13, 2013Publication date: April 17, 2014Applicant: Bayer Intellectual Property GmbHInventors: Christoph ERDELEN, Wolfram Andersch, Klaus Stenzel, Astrid Mauler-Machnik, Wolfgang Krämer
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Publication number: 20140107136Abstract: Disclosed herein are methods of delaying the onset or treating diabetes that comprises administering a uric acid lowering agent. The inventors have made the remarkable discovery that elevated uric acid levels are not a corollary to insulin resistance, but rather a primary mediator of insulin resistance. Specifically exemplified are methods that involve administering to a patient susceptible to development of diabetes a composition comprising a uric acid lowering agent in a regimen that maintains serum uric acid levels below at least 5.2 to 5.5 mg/dl.Type: ApplicationFiled: October 14, 2013Publication date: April 17, 2014Inventors: Richard Johnson, Takahiko Nakagawa
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Patent number: 8697696Abstract: The present invention is concerned with novel triazole compounds of formula (I) wherein A, X, Y, u, v, R1, R2, and R3 are as described herein, as well as pharmaceutically acceptable salts thereof. The compounds of present invention have affinity and selectivity for the GABA A ?5 receptor. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions comprising them and their use as pharmaceuticals.Type: GrantFiled: November 2, 2011Date of Patent: April 15, 2014Assignee: Roche Palo Alto LLCInventors: Stephen Deems Gabriel, Andrew Thomas
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Patent number: 8697883Abstract: The invention relates to cyclopenta[c]pyrrole-2-carboxylate derivatives, to their preparation and to their therapeutic use.Type: GrantFiled: May 11, 2010Date of Patent: April 15, 2014Assignee: SanofiInventors: Ahmed Abouabdellah, Luc Even, Aude Fayol, Julien Vache, Philippe Yaiche
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Patent number: 8697734Abstract: This invention pertains to a method for controlling lepidopteran, homopteran, hemipteran, thysanopteran and coleopteran insect pests comprising contacting the insects or their environment with an arthropodicidally effective amount of a compound of Formula I, its N-oxide or an agriculturally suitable salt thereof wherein A and B and R1 through R8 are as defined in the disclosure. This invention further relates to a benzoxazinone compound of Formula 10 wherein R4 through R8 are as defined in the disclosure, useful for preparation of a compound of Formula I.Type: GrantFiled: August 10, 2012Date of Patent: April 15, 2014Assignee: E I du Pont de Nemours and CompanyInventors: George Philip Lahm, Stephen Frederick McCann, Thomas Paul Selby, Thomas Martin Stevenson
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Publication number: 20140100108Abstract: 3-Phenylisoxazoline-5-carboxamides and 3-phenylisoxazoline-5-thioamides of the formula (I) and their use as herbicides and fungicides are described. In this formula (I), X, X2 to X6, R1 to R4 are radicals such as hydrogen, halogen and organic radicals such as substituted alkyl. A is a bond or a divalent unit. Y is a chalcogen.Type: ApplicationFiled: March 26, 2012Publication date: April 10, 2014Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Jan Dittgen, Dieter Feucht, Jeffrey Martin Hills, Philippe Rinolfi, Heinz KEHNE
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Publication number: 20140100252Abstract: The present invention relates to amorphous ritonavir co-precipitated on copovidone, process for its preparation and pharmaceutical compositions comprising it.Type: ApplicationFiled: May 21, 2012Publication date: April 10, 2014Inventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Dasari Muralidhara Reddy, Bandi Vamsi Krishna
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Publication number: 20140100193Abstract: Diazonamide analogs having anti-mitotic activity, useful for the treatment of cancer and other proliferative disorders, and related pharmaceutical compositions are provided.Type: ApplicationFiled: November 25, 2013Publication date: April 10, 2014Applicant: Joyant Pharmaceuticals, Inc.Inventors: Qi Wei, Ming Zhou, Xiaoming Xu, Charles Caldwell, Susan Harran, Lai Wang
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Patent number: 8691812Abstract: A composition comprising a carboxamide compound represented by following formula (I), wherein R1 represents a hydrogen atom or a methyl group, and R2 represents a methyl group, a difluoromethyl group or a trifiuoromethyl group, and one or more neonicotinoid compound selected from group (A) consisting of acetamiprid, clothianidin, dinotefuran, imidacloprid, nitenpyram thiacloprid and thiamethoxam possesses an excellent pesticidal effect.Type: GrantFiled: April 25, 2011Date of Patent: April 8, 2014Assignee: Sumitomo Chemical Company, LimitedInventor: Yuichi Matsuzaki
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Patent number: 8691855Abstract: This present invention relates to novel compounds, isomer thereof or pharmaceutically acceptable salts thereof as vanilloid receptor (Vanilloid Receptor 1; VR1; TRPV1) antagonist; and a pharmaceutical composition containing the same. The present invention provides a pharmaceutical composition for preventing or treating a disease such as pain, migraine, arthralgia, neuralgia, neuropathies, nerve injury, skin disorder, urinary bladder hypersensitiveness, irritable bowel syndrome, fecal urgency, a respiratory disorder, irritation of skin, eye or mucous membrane, stomach-duodenal ulcer, inflammatory diseases, ear disease, heart disease and so on.Type: GrantFiled: July 2, 2009Date of Patent: April 8, 2014Assignee: Amorepacific CorporationInventors: Byoung Young Woo, Sun-Young Kim, Yeonjoon Kim, Song Seok Shin, Jin Kwan Kim, Ki-Wha Lee, Dong Hyun Kim, Kyung Min Lim, Joo-Hyun Moh, Yeon Su Jeong, Jin Kyu Choi, Hyun Ju Koh, Jeongho Lee, Hyuk Kim, Jeong Hoon Yoon, Funan Li, Jee-Suk Kim, Young-Ger Suh
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Publication number: 20140094450Abstract: The present invention relates to benzoimidazole-carboxylic acid amide compounds of the formula I, in which R?, R?, R??, R1, R2, R3, R4, R5, R6 and Z are defined as indicated below. The compounds of the formula I are APJ receptor modulators, and are useful for the treatment of diseases associated with increased blood pressure for example. The invention furthermore relates to the use of compounds of the formula I, in particular as active ingredients in pharmaceuticals, and pharmaceutical compositions comprising them.Type: ApplicationFiled: September 19, 2013Publication date: April 3, 2014Applicant: SANOFIInventors: Stephanie HACHTEL, Paulus WOHLFART, John WESTON, Marco MUELLER, Elisabeth DEFOSSA, Katharina MERTSCH, Jian-Hui WENG, Robert Alan BINNIE, Farid ABDUL-LATIF, William Jerome BOCK, Armin WALSER
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Publication number: 20140094490Abstract: The present invention has an object to provide a novel agent for anti-neurodegenerative diseases and solves the object by providing an agent for anti-neurodegenerative diseases containing, as an effective ingredient, the compound(s) represented by the following General formula 1: wherein in General formula 1, R1 through R3 independently represent a hydrogen atom or an appropriate substituent; Z1 represents a heterocyclic ring and Z2 represents the same or different heterocyclic or aromatic ring as in Z1, wherein the heterocyclic and aromatic rings optionally have a substituent; o represents an integer of 0, 1 or 2; p represents an integer of 0 or 1, with the proviso that p is 1 when o is 0 or 2, and p is 0 when o is 1; R1 and R2 do not exist when o is 0, while, when p is 0, R3 does not exist and the binding between the carbon atom to which R2 binds and Z2 is a single bond; X1? represents an appropriate counter anion and q represents an integer of 1 or 2.Type: ApplicationFiled: December 5, 2013Publication date: April 3, 2014Applicant: KABUSHIKI KAISHA HAYASHIBARA SEIBUTSU KAGAKU KENKYUJOInventors: Hitomi OHTA, Kenji AKITA, Tsunetaka OHTA, Toshio KAWATA, Shigeharu FUKUDA
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Publication number: 20140093563Abstract: The present invention relates to an oral pharmaceutical composition of febuxostat which comprises an intragranular component and an extragranular component. Further, it relates to processes for the preparation of said composition and a method of using said composition.Type: ApplicationFiled: December 5, 2013Publication date: April 3, 2014Applicant: RANBAXY LABORATORIES LIMITEDInventors: Abhishek SRIVASTAVA, Surajit N. DAS, Mukesh Kumar GARG, Ajay Kumar SINGLA, Amit GUPTA, Prakash A. JADHAV
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Publication number: 20140094489Abstract: The present invention provides a blood glucose elevation inhibitor having a serine protease inhibitory action, which is a novel therapeutic or prophylactic agent for obesity. A compound represented by the following formula (I) wherein each symbol is as described in the specification, or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: December 6, 2013Publication date: April 3, 2014Applicant: AJINOMOTO CO., INC.Inventors: Tamotsu SUZUKI, Takahiro KOSHIBA, Munetaka TOKUMASU, Koji OHSUMI
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Publication number: 20140093570Abstract: The present disclosure relates to crystalline form of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluorobenzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, salts and hydrates thereof. This disclosure also relates to solid oral formulation of (S)—N—((S)-1-cyclohexyl-2-{(S)-2-[4-(4-fluoro-benzoyl)-thiazol-2-yl]-pyrrolidin-1-yl}-2-oxo-ethyl)-2-methylamino-propionamide, pharmaceutically acceptable salts, solvates (including hydrates) thereof, as well as methods of treatment using the same.Type: ApplicationFiled: December 3, 2013Publication date: April 3, 2014Applicant: Novartis AGInventors: Jeewan Thakur, Dong Yang, Lili Feng
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Patent number: 8685975Abstract: 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: November 16, 2012Date of Patent: April 1, 2014Assignee: Omeros CorporationInventors: Neil S. Cutshall, Jennifer Lynn Gage, Thomas Neil Wheeler, Thomas L. Little
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Publication number: 20140088092Abstract: The present invention relates to the use of active substance combinations for controlling animal pests, for example, from the chinch bug family (Lygaeidae), as well as animal pests that has shown resistance to pyrethroids.Type: ApplicationFiled: March 8, 2013Publication date: March 27, 2014Applicant: Bayer CropScience LPInventors: Jeffrey A. MICHEL, Kenneth A. KUKOROWSKI
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Publication number: 20140088094Abstract: The invention provides tetrahydroquinoline and related compounds, pharmaceutical compositions, methods of inhibiting ROR? activity, reducing the amount of IL-17 in a subject, and treating immune disorders and inflammatory disorders using such tetrahydroquinoline and related compounds are provided.Type: ApplicationFiled: November 8, 2011Publication date: March 27, 2014Applicants: Merck Sharp & Dohme Corp., Lycera CorporationInventors: Gary D. Glick, Peter L. Toogood, Arthur Glenn Romero, Chad A. Van Huis, Thomas Daniel Aicher, Carl Kaub, Matthew N. Mattson, William David Thomas, Karin Ann Sttein, Erik Krogh-Jespersen, Zhan Wang
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Publication number: 20140088074Abstract: Fluorinated arylalkylaminocarboxamide derivatives of formula (I) are described wherein W, J, n, R1, R2, R3, R4, R5 and R6 have the meanings as defined in the specification and pharmaceutically salts thereof, pharmaceutical compositions containing them as active ingredients and their use as sodium and/or calcium channel modulators useful in preventing, alleviating and curing a wide range of pathologies, including neurological, psychiatric, cardiovascular, inflammatory, ophthalmic, urological, and gastrointestinal diseases, where the above mechanisms have been described as playing a pathological role.Type: ApplicationFiled: May 29, 2012Publication date: March 27, 2014Applicant: NEWRON PHARMACEUTICALS S.P.A.Inventor: Paolo Pevarello
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Publication number: 20140088071Abstract: Compounds of Formula (IA) and Formula (IB) are described. They are useful as stimulators of sGC, particularly NO-independent, heme-dependent stimulators. These compounds may be useful for treating, preventing or managing various disorders that are herein disclosed.Type: ApplicationFiled: November 2, 2011Publication date: March 27, 2014Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, Thomas Wai-Ho Lee, Charles Kim, Joel Moore, Nicholas Robert Perl, Jason Rohde
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Publication number: 20140088046Abstract: The present invention provides novel phenicol derivatives, their use for the treatment of infections in mammals, pharmaceutical composition containing these novel compounds, and methods for the preparation of these compounds.Type: ApplicationFiled: September 5, 2013Publication date: March 27, 2014Applicant: ZOETIS LLCInventors: Denis Billen, Michael Curtis, Richard Andrew Ewin, Richard M. Goodwin, Paul D. Johnson, Timothy Allan Johnson, Graham M. Kyne, Todd M. Maddux, Susan Mary Kult Sheehan, Rajendran Vairagoundar
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Publication number: 20140088117Abstract: Cyclic ether pyrazol-4-yl-heterocyclyl-carboxamide compounds of Formula I, including stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof, wherein R2 is a cyclic ether and X is thiazolyl, pyrazinyl, pyridinyl, or pyrimidinyl, are useful for inhibiting Pim kinase, and for treating disorders such as cancer mediated by Pim kinase. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.Type: ApplicationFiled: September 25, 2013Publication date: March 27, 2014Applicant: Genentech, Inc.Inventors: Jason Burch, Minghua Sun, Xiaojing Wang, Wesley Blackaby, Alastair James Hodges, Andrew Sharpe
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Patent number: 8680126Abstract: Compounds of formula (I) or their pharmaceutically acceptable salts, or their stereoisomers or mixtures of stereoisomers, where: R1 is selected from the group consisting of: phenyl, and phenyl mono-, di-, or tri-substituted by a radical independently selected from the group consisting of F, Cl, Br, I, (C1-C6)-alkyl, COO—(C1-C6)-alkyl, and (C1-C6)-alkoxy; and R2 is a radical selected from the same group as R1, further including a phenyl substituted in 4-position by a radical independently selected from the group consisting of —O(CH2)CONH(CH2)3CH3 and OCH2COOC(CH3)3, a biphenyl-4-yl, thiazol-2-yl, and a thiazol-2-yl mono- or di-substituted by a radical selected from F and phenyl; inhibit cell proliferation of tumor cells independently of p53 protein and may also induce apoptosis in several tumor cells independently of p53 protein, being useful for the treatment of several types of cancer.Type: GrantFiled: August 29, 2011Date of Patent: March 25, 2014Assignees: Universitat de Barcelona, Fundacio Privada Institut d'Inbestigacio Biomedica de Bell Vitge, Fundacio Privada Institute de Recerca Biomedica de Barcelona, Fundacio Privada Parc Cientific de BarcelonaInventors: Joan Gil Santano, Rodolfo Lavilla Grifols, Fernando Albericio Palomera, Alba Pérez Perarnau, Sara Preciado Gallego, Diana Ma González Gironès, Daniel Iglesias Serret, Rosario Ramón Albalate
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Patent number: 8680100Abstract: The present invention is directed to compounds represented by structural formula (I), or a pharmaceutically acceptable salt or a transition metal chelate, coordinate or complex thereof or a transition metal chelate, coordinate or complex of a deprotonated form of the compound. Pharmaceutical composition and method of use for these compounds are also included.Type: GrantFiled: December 1, 2009Date of Patent: March 25, 2014Assignee: Synta Pharmaceuticals Corp.Inventors: Jun Jiang, Teresa Kowalczyk-Przewloka, Stefan M. Schweizer, Zhi-Qiang Xia, Shoujun Chen, Christopher Borella, Lijun Sun
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Patent number: 8680157Abstract: The invention relates to the use of at least one amine oxidase inhibitor for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal and to pharmaceutical compositions for controlling the androgen receptor-dependent gene expression, comprising an effective dose of at least one amine oxidase inhibitor suitable for modulating the activity of the lysine-specific demethylase (LSD1) in a mammal. The invention also relates to assay systems allowing to test LSD1 inhibitors for their ability to inhibit LSD1 function.Type: GrantFiled: February 16, 2006Date of Patent: March 25, 2014Assignee: Universitaetsklinikum FreiburgInventors: Roland Schuele, Eric Metzger
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Patent number: 8680127Abstract: The present invention relates to N-cycloalkyl-N-biphenylmethyl-carboxamide derivatives of formula (I) wherein A, Z1, Z2, Z3, X, n, Y and m represent various substituents, their process of preparation, preparation intermediate compounds, their use as fungicide active agents, particularly in the form of fungicide compositions and methods for the control of phytopathogenic fungi, notably of plants, using these compounds or compositions.Type: GrantFiled: July 30, 2009Date of Patent: March 25, 2014Assignee: Bayer Intellectual Property GmbHInventors: Philippe Desbordes, Ralf Dunkel, Stephanie Gary, Marie-Claire Grosjean-Cournoyer, Benoit Hartmann, Philippe Rinolfi, Jean-Pierre Vors, Rachel Rama
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Publication number: 20140080787Abstract: The present invention relates to compositions and methods for the treatment, prevention, and diagnosis of neuropathies due to PMP22 mis-expression in a subject having Charcot-Marie-Tooth disease, especially Charcot-Marie-Tooth 1A disease. The present invention incorporates the use of small molecule proteasome inhibitors such as, but not limited to, Bortezomib to inhibit or reduce the overexpression of the PMP2 gene.Type: ApplicationFiled: September 13, 2013Publication date: March 20, 2014Inventors: James Inglese, John Peter Svaren, Sung-Wook Jang, Mark Albert Scheideler, Lars Jacob Stray Knutsen
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Publication number: 20140080805Abstract: The invention provides novel inhibitors of IAP that are useful as therapeutic agents for treating malignancies where the compounds have the general formula I: wherein A, Q, X1, X2, Y, R1, R2, R3, R4, R4?, R5, R6 and R6? are as described herein.Type: ApplicationFiled: November 22, 2013Publication date: March 20, 2014Applicant: Genentech, Inc.Inventors: Frederick COHEN, Vickie Hsiao-Wei TSUI, Cuong LY, John A. FLYGARE
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Publication number: 20140079806Abstract: The invention relates to the use of penflufen for protecting wood and wood-comprising materials against wood-destroying basidiomycetes.Type: ApplicationFiled: September 30, 2011Publication date: March 20, 2014Applicant: LANXESS Deutschland GmbHInventors: Bernd Koop, Martin Kugler, Thomas Jaetsch, Johannes Kaulen, Tanja Gerharz