Nitrogen Attached Indirectly To The Six-membered Hetero Ring By Nonionic Bonding Patents (Class 514/357)
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Publication number: 20130273034Abstract: The present invention relates to compounds and compositions for the inhibition of NAMPT, their synthesis, applications and antidotes.Type: ApplicationFiled: September 2, 2011Publication date: October 17, 2013Inventors: Kenneth W. Bair, Timm R. Baumeister, Alexandre J. Buckmelter, Karl H. Clodfelter, Bingsong Han, Jian Lin, Dominic J. Reynolds, Chase C. Smith, Zhongguo Wang, Xiaozhang Zheng, Po-Wai Yuen
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Patent number: 8557853Abstract: The invention provides well-defined aryl fluoroethyl ureas that are useful as selective alpha2 adrenergic agonists. As such, the compounds described herein are useful in treating a wide variety of disorders associated with modulation of alpha2 adrenergic receptors.Type: GrantFiled: December 5, 2007Date of Patent: October 15, 2013Assignee: Allergan, Inc.Inventors: Ken Chow, Wenkui K. Fang, Evelyn G. Corpuz, Daniel W. Gil, Michael E. Garst
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Publication number: 20130266651Abstract: Provided are oral dosage forms that contain carbinoxamine in an immediate release format, and pseudoephedrine in a prolonged release format. The biphasic oral dosage forms may also contain other active ingredients in combination with carbinoxamine, including other decongestants, antitussives, analgesics and expectorants.Type: ApplicationFiled: March 15, 2013Publication date: October 10, 2013Inventors: Robert J. Edwards, Jr., Chih-Ting Huang, Nam-Mew Pul
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Publication number: 20130267536Abstract: The present invention relates to novel substituted methyl-amines, serotonin 5-HT6 receptor antagonists, to active components, pharmaceutical compositions, method for prophylaxis and treatment of CNS diseases and “molecular tools”, in which novel substituted methyl-amines represent compounds of the general formula 1 and their crystalline forms and pharmaceutically acceptable salts, wherein: W represents benzene, naphthalene, indolizine, quinoline or oxazole cycle; R1=H, F, Cl; R2 represents hydrogen, fluoro, methyl, phenyl, thienyl, furan-2-yl, pyridyl, piperazin-1-yl or 4-methylpiperazin-1-yl; R3 represents cyclopropyl or optionally substituted methyl; with the exception of the compounds in which W simultaneously represents oxazole cycle and R2=phenyl or pyridyl.Type: ApplicationFiled: December 13, 2011Publication date: October 10, 2013Applicant: ALLA CHEM, LLCInventors: Alexandre Vasilievich Ivachtchenko, Oleg Dmitrievich Mitkin, Madina Georgievna Kadieva
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Publication number: 20130267415Abstract: The present invention relates to pesticidal mixtures comprising a component A and a component B, wherein component A is a compound of formula I wherein one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl, 3,5-dichloro-4-fluoro-phenyl, or 3,5-bis-trifluoromethylphenyl; R4 is methyl or chlorine; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; and wherein component B is an insecticide. The invention also relates to methods of controlling insects, acarines, nematodes or molluscs which comprises applying to a pest, to a locus of a pest, or to a plant susceptible to attack by a pest a combination of components A and B.Type: ApplicationFiled: December 15, 2011Publication date: October 10, 2013Applicant: SYNGENTA PARTICIPATIONS AGInventors: Peter Renold, Jerome Yves Cassayre, Myriem El Qacemi, Jagadish Pabba, Thomas Pitterna
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Patent number: 8552036Abstract: The present invention provides a novel crystalline form of atazanavir sulfate, process for its preparation and to pharmaceutical composition containing it. In accordance with the present invention atazanavir sulfate was dissolved in methanol, to the solution was added ethyl acetate, the solid obtained was collected by filtration and dried to give atazanavir sulfate crystalline form H1.Type: GrantFiled: January 12, 2009Date of Patent: October 8, 2013Assignee: Hetero Research FoundationInventors: Bandi Parthasaradhi Reddy, Kura Rathnakar Reddy, Rapolu Raji Reddy, Dasari Muralidhara Reddy, Kesireddy Subash Chander Reddy
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Patent number: 8552056Abstract: The present invention relates to a novel chemical compound of formula S-(1): for use in the treatment of cancer, to compositions containing said compound, methods of manufacture and combinations with other therapeutic agents.Type: GrantFiled: September 15, 2012Date of Patent: October 8, 2013Assignee: Tapestry Pharmaceuticals, Inc.Inventors: James D. McChesney, Gilles Tapolsky, David E. Emerson, John Marshall, Tauseef Ahmed, Allen Cohn, Michael Kurman, Manuel Modiano
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Publication number: 20130261069Abstract: The present invention provides pesticidal mixtures comprising a component A, a component B and a component C, wherein component A is a compound of formula (I) wherein one of Y1 and Y2 is S, SO or SO2 and the other is CH2; L is a direct bond or methylene; A1 and A2 are C—H, or one of A1 and A2 is C—H and the other is N; R1 is hydrogen or methyl; R2 is chlorodifluoromethyl or trifluoromethyl; R3 is 3,5-dibromo-phenyl, 3,5-dichloro-phenyl, 3,4-dichloro-phenyl, or 3,4,5-trichloro-phenyl; R4 is methyl; R5 is hydrogen; or R4 and R5 together form a bridging 1,3-butadiene group; component B is a compound selected from Sedaxane, Fludioxonil, Metalaxyl, Mefenoxam, Cyprodinil, Azoxystrobin, Tebuconazole, Difenoconazole, Thiabendazole, Fluopyram, Penflufen, N-[9-(dichloromethylene)-1,2,3,4-tetrahydro-1,4-methanonaphthalen-5-yl]-3-(difluoromethyl)-1-methyl-1H-pyrazole-4-carboxamide and Fuxapyroxad; or component B is a compound selected from Tefluthrin, Lambda-cyhalothrin, Abamectin, Spinosad, Spinetoram, Chlorpyrifos, ThiType: ApplicationFiled: June 9, 2011Publication date: October 3, 2013Applicant: SYNGENTA CROP PROTECTION LLCInventors: Ana Dutton, Jerome Yves Cassayre, Ulrich Johannes Haas
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Patent number: 8546304Abstract: The present invention relates to plant-protecting active ingredient mixtures comprising, as active components, a neonicotinoid and one or two fungicides selected from pyraclostrobin and boscalid, in synergistically effective amounts and to a method of improving the health of plants by to the plants or the locus thereof by applying said mixtures.Type: GrantFiled: August 15, 2011Date of Patent: October 1, 2013Assignee: BASF SEInventors: Dirk Voeste, Martin P. Mascianica, Hendrik Ypema, Henry Van Tuyl Cotter
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Patent number: 8546382Abstract: Described herein are methods for improving engraftment of hematopoietic cells in an individual following hematopoietic progenitor cell transplantation (e.g., via bone marrow or cord blood transplantation). Methods for increasing hematopoietic progenitor cell proliferation in individuals with bone marrow aplasia are also described. The methods involve administering an agent that inhibits adipogenesis, adipocyte growth, adipocyte differentiation and/or adipocyte proliferation.Type: GrantFiled: April 15, 2010Date of Patent: October 1, 2013Assignee: Children's Medical Center CorporationInventors: Olaia Naveiras, George Daley, Pamela L. Wenzel
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Publication number: 20130253018Abstract: The present invention relates generally to the use of pyridylethylbenzamide derivatives for controlling nematodes and to methods particularly useful for controlling nematodes and/or increasing crop yield.Type: ApplicationFiled: November 30, 2011Publication date: September 26, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Heike Hungenberg, Helmut Fuersch, Heiko Rieck, Elke Hellwege
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Publication number: 20130252947Abstract: The present disclosure relates to a method to stimulate endogenous BMP-2 up-regulation in a subject which method comprises administering to a subject an effective amount of an H1 receptor antagonist, whereby endogenous BMP-2 up-regulation is stimulated in said subject. Also provided is a pharmaceutical formulation including an H1 receptor antagonist present in an effective amount to stimulate BMP-2 up-regulation in a subject and a kit.Type: ApplicationFiled: May 17, 2013Publication date: September 26, 2013Applicant: Southwest Research InstituteInventor: Jorge Gianny ROSSINI
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Publication number: 20130252916Abstract: This invention relates to an oramucosal pharmaceutical dosage form in the form of a wafer. The wafer comprises a porous, hydroscopic, muco-adhesive polymeric matrix with at least one desired pharmaceutically active compound added thereto. The polymer is selected from a number of polymers having different dissolution rates and, in use when taken orally, the matrix adheres to an oramucosal surface to dissolve over a predetermined period of time to release the pharmaceutically active compound. The invention also extends to a method of manufacturing an oramucosal pharmaceutical dosage form in the form of a wafer which involves freeze drying or lyophilisation.Type: ApplicationFiled: January 8, 2013Publication date: September 26, 2013Applicant: UNIVERSITY OF THE WITWATERSRAND, JOHANNESBURGInventor: UNIVERSITY OF THE WITWATERSRAND, JOHANNESBURG
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Publication number: 20130253017Abstract: A method of delivering a health care active having the steps of administering to a mammal in need of a health benefit or a treatment for a health condition a personal health care article and consuming the article. The article contains one or more filaments that contain a backbone material, a health care active and optionally aesthetic agents, extensional aids, plasticizers, and crosslinking agents.Type: ApplicationFiled: May 14, 2013Publication date: September 26, 2013Applicant: The Procter & Gamble CompanyInventors: Trevor John Darcy, Steven Ray Gilbert, Gregory Charles Gordon, Rajeev Chhabra, William Maxwell Allen, JR.
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Publication number: 20130244986Abstract: Embodiments of the invention generally relate to pharmaceutical compositions containing at least one caffeic acid compound and methods for the topical treatment of proliferative and inflammatory skin disorders such as plaque psoriasis, atopic dermatitis, and other disorders. In some embodiments, the topical treatment includes applications of the pharmaceutical composition containing at least one caffeic acid compound or a mixture of caffeic acid compounds such as caffeic acid ester compounds, caffeic acid amide compounds, analogues thereof, derivatives thereof, salts thereof, or mixtures thereof. The pharmaceutical composition or topical dosage may contain the caffeic acid compound at a concentration by weight within a range from about 0.01% to about 20%, preferably, from about 0.1% to about 15%, preferably, from about 1% to about 10%, more preferably, from about 3% to about 7%, and more preferably, from about 4% to about 6%.Type: ApplicationFiled: April 26, 2013Publication date: September 19, 2013Applicant: Moleculin LLCInventors: Waldemar Priebe, Charles Conrad, Timothy Madden
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Publication number: 20130245062Abstract: Disclosed are nitrile derivatives and pharmaceutical compositions comprising nitrile derivatives. The pharmaceutical compositions comprise compounds of the formula I and the pharmaceutically acceptable salts of such compounds. Also disclosed are processes for the preparation of such compounds, intermediates used in the preparation of such compounds, and the uses of such compounds in treating hyperproliferative diseases, inflammatory diseases and viral and bacterial infections and inducing apoptosis in cancer cells.Type: ApplicationFiled: November 27, 2012Publication date: September 19, 2013Applicant: CELLCEUTIX CORPORATIONInventor: KRISHNA MENON
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Publication number: 20130245018Abstract: The present invention pertains generally to the field of therapeutic compounds, and more specifically to certain aryl-phenyl-sulfonamido-cycloalkyl compounds of the following formula (collectively referred to herein as “APSAC compounds”).Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Applicant: PIMCO 2664 LIMITEDInventors: Iain Robert Greig, Rose Mary Sheridan, Raymond Fisher, Matthew John Tozer, Juha Andrew Clase, Andrew Smith, Andrew Robert Tuffnell, Robert Jurgen Van 't Hof
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Publication number: 20130244962Abstract: Several parasites responsible for mammalian diseases are dependent on cysteine protease for various life-cycle functions. Inhibition or decreasing function of these proteases can be useful in the treatment and/or prevention of these parasitic diseases including; toxoplasmosis, malaria, African trypanosomiasis, Chagas disease, leishmaniasis, schistosomiasis, amebiasis, giardiasis, clonorchiasis, opisthorchiasis, paragonimiasis, fasciolopsiasis, lymphatic filariasis, onchocerciasis, dracunculiasis, ascariasis, trichuriasis, stronglyoidiasis, trichostrongyliasis, trichomoniasis or cestodiasis.Type: ApplicationFiled: April 11, 2013Publication date: September 19, 2013Applicant: Merck Frosst Canada Ltd.Inventors: Elise ISABEL, Christopher MELLON, Christian BEAULIEU
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Publication number: 20130245019Abstract: Acrylamido derivatives useful as therapeutic agents, particularly for the prevention and/or treatment of diseases and conditions associated with the activity of the mitochondrial permeability transition pore (MPTP), such as the diseases characterized by ischemia/reperfusion, oxidative or degenerative tissue damage, are herein described. These compounds belong to the structural formula (I) wherein R, R?, R?, W and a are as defined in the specification. The invention also relates to the preparation of these compounds, as well as to pharmaceutical compositions comprising them.Type: ApplicationFiled: April 30, 2013Publication date: September 19, 2013Applicant: CONGENIA SRLInventors: Daniele Fancelli, Mario Varasi, Simon Plyte, Marco Ballarini, Anna Cappa, Giacomo Carenzi, Saverio Minucci, Gilles Pain, Manuela Villa
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Patent number: 8536182Abstract: The present invention relates to novel benzylpiperazine derivatives such as compounds of formula (I), which have activity as agonists of the GPR38 receptor and the use of such compounds or pharmaceutical compositions thereof in the treatment of gastrointestinal disorders.Type: GrantFiled: July 24, 2006Date of Patent: September 17, 2013Assignee: Glaxo Group LimitedInventors: Christopher Norbert Johnson, David Timothy Macpherson, Steven James Stanway, Geoffrey Stemp, Mervyn Thompson, Susan Marie Westaway
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Publication number: 20130237502Abstract: 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: March 5, 2013Publication date: September 12, 2013Inventors: Michael Curtis, Brian A. Duclos, Richard A. Ewin, Paul D. Johnson, Timothy Allen Johnson, Rajendran Vairagoundar, Denis Billen, Richard M. Goodwin, Andrea K. Haber-Stuk, Graham M. Kyne, Susan M. K. Sheehan
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Publication number: 20130232645Abstract: The present invention relates generally to the use of fluopyram and compositions comprising fluopyram for controlling nematodes in nematode resistant crops and/or increasing crop yield and to methods particularly useful for controlling nematodes and/or increasing crop yield in those crops.Type: ApplicationFiled: September 21, 2011Publication date: September 5, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Wolfram Andersch, Bill Striegel, Kevin Bugg, Steven Riniker, Nalini Desai, Candace Poutre
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Publication number: 20130225621Abstract: In one aspect, the invention relates to substituted 2-hydroxy-4-(2-(phenylsulfonamido)acetamido)benzoic acid analogs, derivatives thereof, and related compounds, which are useful as inhibitors of STAT protein activity; synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of treating disorders of uncontrolled cellular proliferation associated with a STAT protein activity dysfunction using the compounds and compositions. This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.Type: ApplicationFiled: August 2, 2011Publication date: August 29, 2013Applicants: University of Toronto Mississauga, University of Central Florida Research Foundation, Inc.Inventors: James Turkson, Patrick Gunning
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ACYLAMINO-SUBSTITUTED FUSED CYCLOPENTANECARBOXYLIC ACID DERIVATIVES AND THEIR USE AS PHARMACEUTICALS
Publication number: 20130225605Abstract: The present invention relates to compounds of the formula I, wherein A, Y, Z, R3 to R6, R20 to R22 and R50 have the meanings indicated in the claims, which are valuable pharmaceutical active compounds. Specifically, they are inhibitors of the endothelial differentiation gene receptor 2 (Edg-2, EDG2), which is activated by lysophosphatidic acid (LPA) and is also termed as LPA1 receptor, and are useful for the treatment of diseases such as atherosclerosis, myocardial infarction and heart failure, for example. The invention furthermore relates to processes for the preparation of the compounds of the formula I, their use and pharmaceutical compositions comprising them.Type: ApplicationFiled: April 22, 2013Publication date: August 29, 2013Applicant: SANOFIInventor: SANOFI -
Publication number: 20130225619Abstract: The present invention relates generally to compositions and methods for treating neurodegenerative diseases and disorders, particularly ophthalmic diseases and disorders. Provided herein are substituted heterocyclic amine derivative compound and pharmaceutical compositions comprising these compounds. The subject compositions are useful for treating and preventing ophthalmic diseases and disorders, including age-related macular degeneration (AMD) and Stargardt's Disease.Type: ApplicationFiled: January 18, 2013Publication date: August 29, 2013Applicant: Acucela Inc.Inventors: Vladimir A. Kuksa, Mark W. Orme, Feng Hong, Ryo Kubota
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Patent number: 8518940Abstract: The present invention embraces compounds selected for interacting with the Fingers-Palm pocket of telomerase and use thereof for modulating the activity of telomerase and preventing or treating diseases or conditions associated with telomerase.Type: GrantFiled: February 8, 2010Date of Patent: August 27, 2013Assignee: The Wistar InstituteInventor: Emmanuel Skordalakes
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Patent number: 8519142Abstract: The present invention provides a compound of formula I; a method for manufacturing the compounds of the invention, and its therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.Type: GrantFiled: September 14, 2012Date of Patent: August 27, 2013Assignee: Novartis AGInventors: Sylvie Chamoin, Qi-Ying Hu, Julien Papillon
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Patent number: 8519137Abstract: The present invention relates to compounds useful as inhibitors of voltage-gated sodium channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.Type: GrantFiled: October 10, 2008Date of Patent: August 27, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Pramod Joshi, Paul Krenitsky, Andreas Termin, Dean Wilson
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Patent number: 8519188Abstract: The present invention relates to a compound of general formula (I): and also to the pharmaceutically acceptable salts thereof, to the isomers or isomer mixtures thereof in all proportions, in particular to an enantiomer mixture, and especially to a racemic mixture. The present invention also relates to the use of these compounds as a medicament, and in particular for the treatment of cancer, and also to the compositions containing them.Type: GrantFiled: June 15, 2009Date of Patent: August 27, 2013Assignee: Marc-Henry PittyInventors: Denis Carniato, Karine Jaillardon, Olivier Busnel, Mathieu Gutmann, Jean-Francois Briand, Benoit Deprez, Dominique Thomas, Cécile Bougeret
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Patent number: 8513428Abstract: A process is provided for preparing the HIV protease inhibitor atazanavir bisulfate wherein a solution of atazanavir free base is reacted with concentrated sulfuric acid in an amount to react with less than about 15% by weight of the free base, seeds of Form A crystals of atazanavir bisulfate are added to the reaction mixture, and as crystals of the bisulfate form, additional concentrated sulfuric acid is added in multiple stages at increasing rates according to a cubic equation, to effect formation of Form A crystals of atazanavir bisulfate. A process is also provided for preparing atazanavir bisulfate as Pattern C material. A novel form of atazanavir bisulfate is also provided which is Form E3 which is a highly crystalline triethanolate solvate of the bisulfate salt from ethanol.Type: GrantFiled: October 8, 2010Date of Patent: August 20, 2013Assignee: Bristol-Meyers Squibb CompanyInventors: Soojin Kim, Bruce T. Lotz, Mary F. Malley, Jack Z. Gougoutas, Martha Davidovich, Sushil K. Srivastava
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Publication number: 20130210835Abstract: A composition of an antitussive, a decongestant, or an antihistamine to treat respiratory and oral pharyngeal congestion and related symptoms in a patient.Type: ApplicationFiled: June 13, 2011Publication date: August 15, 2013Applicant: GM PHARMACEUTICAL, INCInventor: Odes W. Mitchell
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Patent number: 8507532Abstract: Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed.Type: GrantFiled: December 22, 2009Date of Patent: August 13, 2013Assignee: Dow AgroSciences, LLC.Inventors: Kuide Qin, Raymond E. Boucher, Jr.
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Patent number: 8507536Abstract: GnRH receptor antagonists are disclosed which have utility in the treatment of a variety of sex-hormone related conditions in both men and women. The compounds of this invention have the structure: wherein R1a, R1b, R1c, R1d, R2, R2a, and A are as defined herein, including stereoisomers, esters, solvates, and pharmaceutically acceptable salts thereof. Also disclosed are compositions containing a compound of this invention in combination with a pharmaceutically acceptable carrier, as well as methods relating to the use thereof for antagonizing gonadotropin-releasing hormone in a subject in need thereof.Type: GrantFiled: August 10, 2012Date of Patent: August 13, 2013Assignee: Neurocrine Biosciences, Inc.Inventors: Graham Beaton, Mi Chen, Timothy Richard Coon, Todd Ewing, Wanlong Jiang, Jinghua Yu, Willy Moree, Warren Wade, Liren Zhao, Yun-fei Zhu, Martin Rowbottom, Neil Ashweek
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Publication number: 20130203747Abstract: Compounds of formula I: wherein a, R1, R2, R3, R4, R5 and R6 are defined herein, are useful as inhibitors of HIV replication.Type: ApplicationFiled: November 21, 2012Publication date: August 8, 2013Applicant: Gilead Sciences, Inc.Inventor: Gilead Sciences, Inc.
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Publication number: 20130203751Abstract: The present application relates to novel substituted 8-alkoxy-2-aminotetraline derivatives, to processes for their preparation, to their use for the treatment and/or prevention of diseases and to their use for preparing medicaments for the treatment and/or prevention of diseases, in particular for the treatment and/or prevention of cardiovascular disorders.Type: ApplicationFiled: May 9, 2011Publication date: August 8, 2013Applicant: BAYER INTELLECTUAL PROPERTY GMBHInventors: Walter Hübsch, Michael Hahn, Alexandros Vakalopoulos, Volkhart Min-Jian Li, Frank Wunder, Johannes-Peter Stasch, Karl-Heinz Schlemmer, Friederike Stoll, Niels Lindner
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Publication number: 20130203759Abstract: Disclosed are compressed tablets containing atazanavir sulfate and an acidifying agent, optionally with another active agent, e.g., anti-HIV agents, and optionally with precipitation retardant agents. Also disclosed are processes for making the tablets, and methods of treating HIV.Type: ApplicationFiled: April 7, 2011Publication date: August 8, 2013Inventors: Faranak Nikfar, Munir Alwan Hussain, Feng Qian
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Publication number: 20130203691Abstract: Insect controlling compositions including an N-substituted (6-haloalkylpyridin-3-yl)alkyl sulfoximine compound exhibiting increased stability, along with methods for preparing same, are disclosed.Type: ApplicationFiled: March 15, 2013Publication date: August 8, 2013Applicant: Dow AgroSciences, LLCInventor: Dow AgroSciences, LLC
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Publication number: 20130203793Abstract: Method and composition for protection and treatment against influenza viral infection by modulating the activity of at least one essential host signaling pathways, including the Hedgehog (Hh), the Bone Morphogenetic Protein (BMP), the Notch (N) signaling pathways or combinations thereof, which activity is altered by the viral protein NS1. The method and composition comprise use of a compound that modulates at least one of these essential host signaling pathways for preventing or controlling symptoms associated with influenza viral infection. The method or composition can also be used either alone or in combination with other therapeutic agents for treating or protecting against influenza infection, and associated syndromes.Type: ApplicationFiled: February 7, 2013Publication date: August 8, 2013Applicants: THE SCRIPPS RESEARCH INSTITUTE, THE REGENTS OF THE UNIVERSITY OF CALIFORNIAInventors: THE REGENTS OF THE UNIVERSITY OF CALIFORNIA, THE SCRIPPS RESEARCH INSTITUTE
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Publication number: 20130197042Abstract: Compounds of formula (I) inhibit HDAC activity: wherein A, B and D independently represent ?C— or ?N—; W is a divalent radical —CH?CH— or CH2CH2—; R1 is a carboxylic acid group (—COOH), or an ester group which is hydrolysable by one or more intracellular carboxyesterase enzymes to a carboxylic acid group; R2 is the side chain of a natural or non-natural alpha amino acid; z is 0 or 1; and Y, L1, and X1 are as defined in the claims.Type: ApplicationFiled: March 14, 2013Publication date: August 1, 2013Inventors: Alan Hornsby DAVIDSON, David Charles Festus MOFFAT, Francesca Ann DAY, Alastair David Grahm DONALD
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Publication number: 20130197041Abstract: The present invention provides a method of selection of a patient, who is a candidate for treatment with an NMDA antagonist drug, such as (S)-1-phenyl-2-(pyridin-2-yl)ethanamine or ketamine, whereby to predict an increased or decreased likelihood of response to the NMDA antagonist. The invention provides a method for determining the sequence of GABR-A2 at any of four single nucleotide polymorphism (SNP) sites known as rs3756007, rs11503016, rs17537359 or rs1372472. The method also provides ARMS primers optimised for determining the sequence at these GABR-A2 SNPs and diagnostic kits comprising suitable primers or probes for determining the particular SNPs.Type: ApplicationFiled: December 14, 2012Publication date: August 1, 2013Applicant: ASTRAZENECA ABInventor: AstraZeneca AB
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Publication number: 20130197013Abstract: The invention relates to cyclopropylamine compounds, in particular the compounds of Formula (I), and their use in therapy, including e.g. in the treatment or prevention of cancer, a neurological disease or condition, or viral infection.Type: ApplicationFiled: July 27, 2011Publication date: August 1, 2013Inventors: Mathew Colin Thor Fyfe, Alberto Ortega Muñoz, Julio Castro-Palomino Laria, Marc Martinell Pedemonte, Maria de los Ángeles Estiarte-Martínez, Nuria Valls Vidal
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Patent number: 8497379Abstract: The present invention is directed to a method for the preparation of 2,2,2-trifluoro-n-(4-fluoro-3-pyridin-4-yl-benzyl)-acetamide hydrochloride of the formula: and reaction intermediates used in the method.Type: GrantFiled: June 27, 2012Date of Patent: July 30, 2013Assignee: SanofiInventors: Yong Mi Choi-Sledeski, Nakyen Choy, Gregory B. Poli, John J. Shay, Jr., Patrick Wai-Kwok Shum, Adam W. Sledeski
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Patent number: 8497380Abstract: The present invention relates to a compound according to formula: (1); wherein X1, X2, X3, X4 and X5 independently of each other represent —CH— or N; or X3, X4 and X5 independently of each other represent —CH— or N, and X1 and X2 independently of each other represent C and form part of an additional 6-membered aromatic ring; R1 represents hydrogen, alkyl, alkenyl, alkynyl, haloalkyl, hydroxyalkyl, or alkylcarbonyl, all of which are optionally substituted; R2 and R3 independently represent hydrogen, —CH2, —C(O)NR—R?, alkyl, cycloalkyl, alkenyl, cycloalkenyl, alkynyl, haloalkyl, hydroxyalkyl, heterocycloalkenyl, alkylaryl, alkylalkoxycarbonyl, aikylcarbonyloxy, or alkoxyalkyl, all of which are optionally substituted; R11 represents hydrogen, halogen, cyano, amino, alkoxy or alkylamino, X1-X5 represent —CH— or N, including N-oxides, enantiomers and diastereomers; and pharmaceutically acceptable salts, hydrates, or solvates thereof. The invention relates further to methods of treating dermal disease.Type: GrantFiled: July 11, 2012Date of Patent: July 30, 2013Assignee: Leo Pharma A/SInventors: Jakob Felding, Simon Feldbæk Nielsen
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Publication number: 20130190356Abstract: Compounds of the formula I: or pharmaceutically acceptable salts thereof, wherein m, A, B, C, R1, R2, R3, R4 and R5 are as defined herein. Also disclosed are methods of making the compounds and using the compounds for treatment of inflammatory diseases such as arthritis.Type: ApplicationFiled: December 18, 2012Publication date: July 25, 2013Applicant: GENENTECH, INC.Inventor: Genetech, Inc.
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Publication number: 20130189333Abstract: An oral product includes a body that is wholly receivable in an oral cavity. The body includes a mouth-stable polymer matrix, cellulosic fibers embedded in the mouth-stable polymer matrix, and an additive dispersed in the mouth-stable polymer matrix. The oral product is adapted to release the additive from the body when the body is received within the oral cavity and exposed to saliva.Type: ApplicationFiled: January 18, 2013Publication date: July 25, 2013Applicant: ALTRIA CLIENT SERVICES INC.Inventor: Altria Client Services Inc.
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Patent number: 8492365Abstract: The present invention pertains, at least in part, to novel 7-substituted tetracycline compounds. These tetracycline compounds can be used to treat numerous tetracycline compound-responsive states, such as bacterial infections and neoplasms, as well as other known applications for minocycline and tetracycline compounds in general, such as blocking tetracycline efflux and modulation of gene expression.Type: GrantFiled: June 9, 2009Date of Patent: July 23, 2013Assignees: Trustees of Tufts College, Paratek Pharmaceuticals, Inc.Inventors: Mark L. Nelson, Roger Frechette, Peter Viski, Mohamed Ismail, Todd Bowser, Beena Bhatia, David Messersmith, Laura McIntyre, Darrell Koza, Glen Rennie, Paul Sheahan, Paul Hawkins, Atul Verma, Tadeusz Warchol, Upul Bandarage
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Publication number: 20130184279Abstract: Compounds of formula Ia and Ib wherein A, B, C, R1 and R14 are described herein.Type: ApplicationFiled: December 18, 2012Publication date: July 18, 2013Applicant: Bristol-Myers Squibb CompanyInventor: Bristol-Myers Squibb Company
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Patent number: 8486381Abstract: The present invention relates to methods for treating intestinal fluid balance disorders and modulating intestinal fluid secretion and absorption using calcimimetics and calcilytics.Type: GrantFiled: August 28, 2006Date of Patent: July 16, 2013Assignee: Amgen Inc.Inventors: John Peter Geibel, Steven Charles Hebert, David Martin, Deborah A. Russell
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Publication number: 20130178457Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of cannabinoid (CB) receptors of Formula (I).Type: ApplicationFiled: July 5, 2012Publication date: July 11, 2013Applicant: LUPIN LIMITEDInventors: Sanjeev Anant KULKARNI, Sachin MADAN, Nirmal Kumar JANA, Prashant Vitthalrao TALE, Narasimha Murthy CHEEMALA, Sachin Jaysing MAHANGARE, Prashant Popatrao VIDHATE, Chaitanya Prabhakar KULKARNI, Sapana Suresh PATEL, Amolsing Dattu PATIL, Seema Prabhakar ZADE, Rohan Mahadev SHINDE, Venkata P. PALLE, Rajender Kumar KAMBOJ
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Patent number: 8481571Abstract: A method of treating coronavirus infection. The method includes administering to a subject suffering from or being at risk of suffering from such infection an effective amount of a compound of formula (I). Each variable in this formula is defined in the specification.Type: GrantFiled: May 3, 2005Date of Patent: July 9, 2013Assignee: Academia SinicaInventors: Chi-Huey Wong, Chung-Yi Wu, Jia-Tsrong Jan