Chalcogen Bonded Directly To Pyrimidine At 2-position Patents (Class 514/274)
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Patent number: 8420658Abstract: Method and composition of Carboxyamidotriazole orotate for treating age-related macular degeneration and other angiogenesis-dependent diseases.Type: GrantFiled: May 24, 2010Date of Patent: April 16, 2013Assignee: Tactical Therapeutics IncInventor: Rashida A Karmali
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Publication number: 20130090339Abstract: Novel 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives that are effective for use in treating viral infections are described. Also described are pharmaceutical compositions comprising the 3-N-cycloalkyl-5-substituted-2-thioxothiazolidin-4-one derivatives and methods for using the compounds or compositions.Type: ApplicationFiled: June 17, 2011Publication date: April 11, 2013Applicants: THE UAB RESEARCH FOUNDATION, FUZIANS BIOMEDICALS, INC.Inventors: Guoxin Wang, Ming Luo, Zhen Yang
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Publication number: 20130090297Abstract: Compositions for the promotion of muscle protein synthesis and control of tumor-induced weight loss in patients that are, for example, suffering from cancer cachexia, and methods of administering such compositions.Type: ApplicationFiled: November 28, 2012Publication date: April 11, 2013Applicant: NESTEC S.A.Inventor: NESTEC S.A.
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Patent number: 8415351Abstract: This invention relates to: (a) compounds and salts thereof that, inter alia, inhibit HCV; (b) intermediates useful for the preparation of such compounds and salts; (c) compositions comprising such compounds and salts; (d) methods for preparing such intermediates, compounds, salts, and compositions; (e) methods of use of such compounds, salts, and compositions; and (f) kits comprising such compounds, salts, and compositions.Type: GrantFiled: March 17, 2010Date of Patent: April 9, 2013Assignee: Abbott LaboratoriesInventors: Rolf Wagner, Warren M. Kati, Dachun Liu, Yaya Liu, Kenton L. Longenecker, Clarence J. Maring, John K. Pratt, Todd W. Rockway, Kent D. Stewart, Michael D. Tufano
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Publication number: 20130085132Abstract: The present invention provides a pyrazole compound of the following general Formula [Ib] having SGLT1 inhibitory activity, or a pharmaceutically acceptable salt thereof, a pharmaceutical composition comprising the same, and its pharmaceutical use: wherein each symbol is the same as defined in the description.Type: ApplicationFiled: August 30, 2012Publication date: April 4, 2013Applicant: JAPAN TOBACCO INC.Inventors: Tomoya MIURA, Yosuke OGOSHI, Kazuhito UEYAMA, Dai MOTODA, Toshihiko IWAYAMA, Koichi SUZAWA, Hironobu NAGAMORI, Hiroshi UENO, Akihiko TAKAHASHI, Kazuyuki SUGIMOTO
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Publication number: 20130084345Abstract: The invention provides combination therapy, wherein one or more other therapeutic agents are administered with indibulin or a pharmaceutically acceptable salt thereof and the combination is synergistic. Another aspect of the invention relates to the treatment of cancer with indibulin as a single agent. Another aspect of the invention relates to dosing regimen for administration of oral dosage forms of indibulin.Type: ApplicationFiled: November 20, 2012Publication date: April 4, 2013Applicant: ZIOPHARM ONCOLOGY, INC.Inventor: Ziopharm Oncology, Inc.
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Patent number: 8410125Abstract: This invention relates to pharmaceutical compositions comprising a sulfonated biological precursor of thymidine, such as a precursor of 4-thiothymidine (4-TT), and their use in the photodynamic treatment of skin hyperplasias, including cancer, psoriasis, actinic keratosis and keloids, by topical or systemic administration.Type: GrantFiled: November 5, 2008Date of Patent: April 2, 2013Assignee: Yagna LimitedInventor: Giuseppe Trigiante
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Patent number: 8410116Abstract: Disclosed are bis(styryl)pyrimidine or bis(styryl)benzene compounds, represented by Chemical Formula 1, pharmaceutically acceptable salts, a method for preparing the same, and a pharmaceutical composition for the prevention and treatment of amyloidosis-associated diseases, comprising the same as an active ingredient. Having the ability to inhibit the deposition of beta amyloid and to reduce the toxicity of beta amyloid, the derivatives can improve learning and memory and can be useful in the prevention and treatment of amyloidosis-associated diseases. (wherein R1, R2, R3 and X are as defined in the specification).Type: GrantFiled: April 24, 2009Date of Patent: April 2, 2013Assignee: Korea Institute of Science and TechnologyInventors: Kye Jung Shin, Eun Joo Roh, Yun Suk Lee
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Patent number: 8410096Abstract: Disclosed are an antitumor preparation comprising a combination of (1) a combination drug of tegafur/gimeracil/oteracil potassium, (2) at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof, and (3) cis-oxalate(1R,2R-diaminocyclohexane)platinum(II); a kit comprising a combination of pharmaceutical compositions for treating cancer in a mammal, comprising: (a) a combination drug of tegafur/gimeracil/oteracil potassium in a therapeutically effective amount; (b) a composition containing at least one ingredient selected from the group consisting of folinic acid and pharmacologically acceptable salts thereof in an amount effective for enhancing antitumor effects, and (c) a composition containing cis-oxalate(1R,2R-diaminocyclohexane)platinum(II) in an amount effective for enhancing antitumor effects; and a method for treating cancer.Type: GrantFiled: November 12, 2010Date of Patent: April 2, 2013Assignees: Shizuoka Prefecture, Taiho Pharmaceutical Co., Ltd.Inventor: Sung Hwa Park
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Publication number: 20130078256Abstract: The invention is related to compounds of Formula (I): or a pharmaceutically acceptable salt, solvate, ester, and/or phosphonate thereof, compositions containing such compounds, and therapeutic methods that include the administration of such compounds.Type: ApplicationFiled: November 20, 2012Publication date: March 28, 2013Applicant: Korea Research Institute of Chemical TechnologyInventor: Korea Research Institute of Chemical Technology
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Publication number: 20130079362Abstract: Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including, but not limited to, malignant melanomas, solid tumors, glioblastomas, ovarian cancer, pancreatic cancer, prostate cancer, lung cancers, breast cancers, kidney cancers, hepatic cancers, cervical carcinomas, metastasis of primary tumor sites, myeloproliferative diseases, chronic myelogenous leukemia, leukemias, papillary thyroid carcinoma, non-small cell lung cancer, mesothelioma, hypereosinophilia syndrome, gastrointestinal stromal tumors, colonic cancers, ocular diseases characterized by hyperproliferation leading to blindness including various retinopathies, diabetic retinopathy, rheumatoid arthritis, asthma, chronic obstructive pulmonary disease, mastocytosis, mast cell leukemia, and diseases caused by PDGFR-? kinase, PDGFR-? kinase, c-KIT kinase, cFMS kinase, c-MET kinase, and oncogenic forms, aberrant fusion proteins and polymorphs of any of the foregoing kinases.Type: ApplicationFiled: August 21, 2012Publication date: March 28, 2013Applicant: DECIPHERA PHARMACEUTICALS, LLCInventors: Daniel L. Flynn, Peter A. Petillo, Michael D. Kaufman
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Publication number: 20130079361Abstract: Compounds useful for the inhibition of macrophage migration inhibitory factor (MIF) are provided herein, having the Formula (I): wherein A is selected from the group consisting of aromatic or non-aromatic rings, bicyclic rings, polycyclic rings, alkenes or alkynes; B is H, OH, OR, SR, NH2, NHR, or alkyl; R is H or alkyl, and X and Y are independently N or CH, but one of X and Y must be N. Also provided are pharmaceutical compositions comprising a Formula I compound and methods for the treatment of MIF-implicated diseases or conditions, comprising administering a safe and effective amount of a Formula I compound.Type: ApplicationFiled: September 24, 2010Publication date: March 28, 2013Inventors: Robert A. Mitchell, John O. Trent, Pooran Chand, Gilles Hugues Tapolsky
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Publication number: 20130079343Abstract: Disclosed are a 1,3,6-substituted indole compound having inhibitory activity for protein kinases, a pharmaceutically acceptable thereof, and a pharmaceutical composition for prevention and treatment of diseases caused by abnormal cell growth including the compound as an active ingredient. Since the novel indole compound exhibits superior inhibitory activity for various protein kinases involved in growth factor signal transduction, it is useful as an agent for preventing or treating cancers caused by abnormal cell growth.Type: ApplicationFiled: November 24, 2012Publication date: March 28, 2013Applicant: Korea Institute of Science and TechnologyInventor: Korea Institute of Science and Technology
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Publication number: 20130072486Abstract: The present invention provides a class of pyrimidinedione cyclohexyl compounds and methods of using these compounds as glucocorticoid receptor modulators.Type: ApplicationFiled: March 16, 2012Publication date: March 21, 2013Applicant: Corcept Therapeutics, Inc.Inventors: Robin Clark, George Hynd, Nicholas Ray, Mohammad Sajad
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Publication number: 20130072487Abstract: The invention described herein relates to certain pyrimidinetrione N-substituted glycine derivatives of formula (I) which are antagonists of HIF prolyl hydroxylases and are useful for treating diseases benefiting from the inhibition of this enzyme, anemia being one example.Type: ApplicationFiled: November 2, 2012Publication date: March 21, 2013Applicant: GLAXOSMITHKLINE LLCInventor: GLAXOSMITHKLINE LLC
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Publication number: 20130072508Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.Type: ApplicationFiled: November 12, 2012Publication date: March 21, 2013Applicant: AbbVie Inc.Inventor: AbbVie Inc.
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Patent number: 8399015Abstract: A solid pharmaceutical dosage form providing improved oral bioavailability is disclosed for inhibitors of HIV protease. In particular, the dosage form comprises a solid dispersion of at least one HIV protease inhibitor and at least one pharmaceutically acceptable water-soluble polymer and at least one pharmaceutically acceptable surfactant, said pharmaceutically acceptable water-soluble polymer having a Tg of at least about 50° C. Preferably, the pharmaceutically acceptable surfactant has an HLB value of from about 4 to about 10.Type: GrantFiled: September 22, 2011Date of Patent: March 19, 2013Assignee: AbbVie Inc.Inventors: Joerg Rosenberg, Ulrich Reinhold, Bernd Liepold, Gunther Berndl, Joerg Breitenbach, Laman Alani, Soumojeet Ghosh
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Patent number: 8399436Abstract: The present invention relates to amide compounds, processes for their preparation, pharmaceutical compositions containing these compounds and to their use in the treatment of disorders, conditions or disorders such as allergic disorders, inflammatory disorders and disorders of the immune system.Type: GrantFiled: April 22, 2010Date of Patent: March 19, 2013Assignee: Glaxo Group LimitedInventors: David George Allen, Diane Mary Coe, Anthony William James Cooper, Paul Martin Gore, David House, Stefan Senger, Steven Leslie Sollis, Sadie Vile, Caroline Wilson
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Publication number: 20130065901Abstract: Provided are compounds that are useful in the treatment and/or prevention of diseases mediated by deficient levels of glucokinase activity, such as diabetes mellitus. Also provided are methods of treating or preventing diseases and disorders characterized by underactivity of glucokinase or which can be treated by activating glucokinase.Type: ApplicationFiled: November 5, 2012Publication date: March 14, 2013Applicant: ARRAY BIOPHARMA INC.Inventor: Array BioPharma Inc.
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Publication number: 20130065895Abstract: Pyrazolopyridine, pyrazolopyrazine, pyrazolopyrimidine, pyrazolothiophene and pyrazolothiazole compounds which are useful as allosteric potentiators/positive allosteric modulators of the metabotropic glutamate receptor subtype 4 (mGluR4); synthetic methods for making the compounds; pharmaceutical compositions comprising the compounds; and methods of using the compounds, for example, in treating neurological and psychiatric disorders or other disease state associated with glutamate dysfunction.Type: ApplicationFiled: August 13, 2012Publication date: March 14, 2013Applicant: VANDERBILT UNIVERSITYInventors: P. Jeffrey Conn, Craig W. Lindsley, Corey R. Hopkins, Colleen M. Niswender, Rocco D. Gogliotti, James M. Salovich, Darren W. Engers, Yiu-Yin Cheung
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Publication number: 20130065890Abstract: A compound of the following formula: wherein R1, R2, R3, R4, R5, T, U, V, X, Y, Z, G, and Z are defined herein. It also discloses a method of treating an angiogenesis-related disorder, e.g., cancer or age-related macular degeneration, with such a compound.Type: ApplicationFiled: November 8, 2012Publication date: March 14, 2013Inventor: Hutchison Medipharma Enterprises Limited
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Publication number: 20130064901Abstract: The invention relates to methods for diagnosis and prognosis of gastric cancer. The approach described herein can distinguish intestinal-type gastric cancer (G-INT) from diffuse-type gastric cancer (G-DIF). The genomic expression signatures of G-INT and G-DIF define two major sets of genes. A diagnosis of gastric cancer G-INT and G-DIF can be made on the basis of the expression levels of these genes. This can lead to a better prognosis and treatment of gastric cancer.Type: ApplicationFiled: April 18, 2012Publication date: March 14, 2013Applicant: Agency for Science, Technology and ResearchInventors: Patrick Tan, Iain Tan
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Patent number: 8394809Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, Y, R2, R3, and Ra are defined herein.Type: GrantFiled: October 28, 2010Date of Patent: March 12, 2013Assignee: Janssen Pharmaceutica, NVInventors: Steven J. Coats, Yue-Mei Zhang, Shu-Chen Lin, Li Liu, Tamara A. Miskowski, Scott L. Dax, Henry Breslin, Bart L. De Corte, Wei He
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Publication number: 20130059858Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, where-in A, L, m, n, o, p, R2, R3, R3, R4 and R5 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: March 7, 2013Applicant: Bristol-Myers Squibb CompanyInventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl
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Publication number: 20130059850Abstract: The present invention is directed to certain Aza-Indole derivatives which are useful as modulators of Fatty Acid Amide Hydrolase (FAAH) and as FAAH imaging agents. The invention is also concerned with pharmaceutical formulations comprising these compounds as active ingredients and the use of the compounds and their formulations in the treatment of certain disorders, including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer Disease, and Parkinson's Disease.Type: ApplicationFiled: May 4, 2011Publication date: March 7, 2013Applicant: MERCK SHARP & DOHME CORP.Inventors: Abbas M Walji, Philippe G. Nantermet, Keith P. Moore, Rachel Anne Storr, Laura Vassallo, Constantine Kreatsoulas
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Publication number: 20130059872Abstract: The present invention provides new amorphous forms of alogliptin benzoate, pharmaceutical compositions comprising same, methods for their preparation and use thereof in treating conditions mediated by DPP-IV, in particular, type 2 diabetes.Type: ApplicationFiled: November 22, 2010Publication date: March 7, 2013Applicant: MAPI PHARMA LIMITEDInventors: Ehud Marom, Shai Rubnov
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Publication number: 20130059849Abstract: Herein are disclosed azaindazoles of formula (I) where the various groups are defined herein, and which are useful for treating cancer.Type: ApplicationFiled: May 5, 2011Publication date: March 7, 2013Inventors: Joelle Lorraine Burgess, Neil Johnson, Steven D. Knight, Louis Lafrance, William H. Miller, Kenneth Newlander, Stuart Romeril, Meagan B. Rouse, Xinrong Tian, Sharad Kumar Verma, Dominic Suarez
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Patent number: 8389516Abstract: Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(?O)NR6—, —S(O)NR6—, —C(?O)O— or —S(?O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.Type: GrantFiled: June 7, 2011Date of Patent: March 5, 2013Assignee: Biota Europe LimitedInventors: David John Haydon, Lloyd George Czaplewski, Nicholas John Palmer, Dale Robert Mitchell, John Frederick Atherall, Christopher Richard Steele, Tamara Ladduwahetty
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Publication number: 20130053362Abstract: Compounds and pharmaceutical compositions that modulate kinase activity, including PI3 kinase activity, and compounds, pharmaceutical compositions, and methods of treatment of diseases and conditions associated with kinase activity, including P13 kinase activity, are described herein.Type: ApplicationFiled: July 18, 2012Publication date: February 28, 2013Applicants: INTELLKINE, LLC, INFINITY PHARMACEUTICALS, INC.Inventors: Alfredo C. CASTRO, Catherine A. EVANS, Somarajannair JANARDANANNAIR, Andre LESCARBEAU, Tao LIU, Daniel A. SNYDER, Martin R. TREMBLAY, Pingda REN, Yi LIU, Liansheng LI, Katrina CHAN
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Publication number: 20130053403Abstract: The present invention provides compounds of Formula (I), pharmaceutical compositions thereof, and methods of using the same in the treatment or prevention of diseases mediated by the activation of b3-adrenoceptor.Type: ApplicationFiled: April 25, 2011Publication date: February 28, 2013Inventors: Richard Berger, Scott D. Edmondson, Bart H. Harper
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Publication number: 20130052173Abstract: A method for limiting the growth of microorganisms in a biomass that can he used for, or is the result of, the production of biofuels by treating said biomass with a compound selected from the group constituted by menadione, menadione derivatives and mixtures thereof.Type: ApplicationFiled: July 2, 2010Publication date: February 28, 2013Inventor: Paolo Alberto Manzotti
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Publication number: 20130053386Abstract: The invention encompasses a novel class of diaryl ether derivatives which inhibit the processing of APP by the putative ?-secretase while sparing Notch signaling pathway, and thus are useful in the treatment or prevention of Alzheimer's disease without the development of Notch inhibition mediated gastrointestinal issues. Pharmaceutical compositions and methods of use are also included.Type: ApplicationFiled: October 5, 2010Publication date: February 28, 2013Inventors: William Colby Brown, Richard W. Heidebrecht, Jason Brubaker, Christian Fischer, John T. Hendrix, Elizabeth H. Kelley, Rachel N. MacCoss, Joey L. Methot, Thomas Miller, Karin M. Otte, Phieng Siliphaivanh, Thomas Reger, Peter D. Williams, Catherine M. Wiscount
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Publication number: 20130053375Abstract: Disclosed are quinoline compounds having the formula: wherein R1, R2 and A are as defined herein, and methods of making and using the same.Type: ApplicationFiled: May 6, 2011Publication date: February 28, 2013Inventors: Michael Jonathan Bury, Linda N. Casillas, Adam Kenneth Charnley, Michael P. DeMartino, Xiaoyang Dong, Patrick Eidam, Pamela A. Haile, Philip Anthony Harris, Ami Lakdawala Shah, Bryan W. King, Robert W. Marquis, JR., John F. Mehlmann, Joseph J. Romano, Clark A. Sehon
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Publication number: 20130053345Abstract: Novel compounds of structure Formula I: or an enantiomer, diastereomer, tautomer, prodrug or salt thereof, wherein A, D, Di, E, J, L, n, Q, R2 and R4 are defined herein, are provided which are GPR119 G protein-coupled receptor modulators. GPR119 G protein-coupled receptor modulators are useful in treating, preventing, or slowing the progression of diseases requiring GPR119 G protein-coupled receptor modulator therapy. Thus, the disclosure also concerns compositions comprising these novel compounds and methods of treating diseases or conditions related to the activity of the GPR119 G protein-coupled receptor by using any of these novel compounds or a composition comprising any of such novel compounds.Type: ApplicationFiled: May 4, 2011Publication date: February 28, 2013Inventors: Xiang-Yang Ye, Dean A. Wacker, Jeffrey A. Robl, Ying Wang
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Patent number: 8383633Abstract: The present invention relates to compounds useful as inhibitors of Aurora protein kinases. The invention also provides pharmaceutically acceptable compositions comprising those compounds and methods of using the compounds and compositions in the treatment of various disease, conditions, and disorders. The invention also provides processes for preparing compounds of the invention.Type: GrantFiled: October 30, 2009Date of Patent: February 26, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Michael Mortimore, Julian Golec, Daniel Robinson, John Studley
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Patent number: 8383641Abstract: The present invention relates to aryloxyethylamine compounds of the formula I and the physiologically tolerated acid addition salts thereof. The variables have the meanings given in the claims and the description. The invention also relates to the use of a compound of the formula I or a pharmaceutically acceptable salt thereof for preparing a pharmaceutical composition for the treatment of a medical disorder susceptible to treatment with a dopamine D3 receptor ligand.Type: GrantFiled: April 13, 2007Date of Patent: February 26, 2013Assignee: Abbott GmbH & Co. KGInventors: Roland Grandel, Wilfried Martin Braje, Andreas Haupt, Sean Colm Turner, Udo Lange, Karla Drescher, Liliane Unger
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Publication number: 20130045985Abstract: This present disclosure is related to the field of N-(5-fluoro-2-((4-methylbenzyl)oxy)pyrimidin-4-yl)benzamides and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 15, 2012Publication date: February 21, 2013Applicant: Dow AgroSciences LLCInventors: Kristy Bryan, Beth Lorsbach, Kevin G. Meyer, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20130045203Abstract: This disclosure relates to methods of treating or preventing cancer comprising administering a pharmaceutical composition comprising noscapine or noscapine derivatives to a subject diagnosed with a mutated adenomatous polyposis coli (APC) gene.Type: ApplicationFiled: February 25, 2011Publication date: February 21, 2013Applicant: EMORY UNIVERSITYInventors: Harish C. Joshi, Vincent Yang
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Publication number: 20130045286Abstract: Compounds of Formula I are useful for inhibition of CHK1 and/or CHK2. Methods of using compounds of Formula I and stereoisomers and pharmaceutically acceptable salts thereof, 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: March 20, 2012Publication date: February 21, 2013Applicant: ARRAY BIOPHARMA INC.Inventors: Yvan Le Huerou, James F. Blake, Indrani W. Gunwardana, Pete Mohr, Eli M. Wallace, Bin Wang, Mark Joseph Chicarelli, Michael Lyon
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Publication number: 20130045948Abstract: Disclosed are compounds of Formula 1, including all stereoisomers, N-oxides, and salts thereof, wherein A, W, X, G, R1, R2, R3, R4, m and n are as defined in the disclosure. Also disclosed are pharmaceutical compositions containing the compounds of Formula 1 and methods for treating a disease or condition mediated by fatty acid amide hydrolase activity comprising applying a therapeutically effective amount of a compound or a composition of the invention.Type: ApplicationFiled: December 10, 2010Publication date: February 21, 2013Applicant: E I DU PONT DE NEMOURS AND COMPANYInventors: Mei H. Dung, Robert James Pasteris
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Publication number: 20130045962Abstract: The present invention is directed to certain {2-(alkyl)-3-[2-(5-fluoro-4-pyrimidinyl)hydrazino]-3-oxopropyl}hydroxyformamide derivatives. Specifically, the invention is directed to compounds of formula (I): wherein R1, R2 and R3 are defined below and to pharmaceutically acceptable salts thereof. The compounds of this invention are bacterial peptide deformylase inhibitors and can be useful in the treatment of bacterial infections.Type: ApplicationFiled: November 6, 2008Publication date: February 21, 2013Inventors: Donghui Qin, Beth Norton, Xiangmin Liao, Andrew Nicholson Knox, Jinhwa Lee, Yuhong Fang, Jason Christopher Dreabit, Siegfried Benjamin Christensen, IV, Andrew B. Benowitz, Kelly M. Aubart
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Publication number: 20130045984Abstract: This present disclosure is related to the field of 5-fluoro-4-imino-3-(substituted)-3,4-dihydropyrimidin-2(1H)ones and their derivatives and to the use of these compounds as fungicides.Type: ApplicationFiled: August 15, 2012Publication date: February 21, 2013Applicant: Dow AgroSciences LLCInventors: Timothy A. Boebel, Beth Lorsbach, W. John Owen, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao
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Publication number: 20130045974Abstract: Compounds of the formula Ia***** in which the substituents have the definitions provided in the specification, are novel, effective PDE4 inhibitors, useful in the treatment of psoriasis.Type: ApplicationFiled: October 26, 2012Publication date: February 21, 2013Applicant: NYCOMED GMBHInventor: NYCOMED GMBH
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Patent number: 8377933Abstract: A method for treating a pulmonary hypertension condition such as pulmonary arterial hypertension (PAH) in a subject comprises administering to the subject a therapeutically effective amount of ambrisentan, wherein, at baseline, time from first diagnosis of the condition in the subject is not greater than about 2 years.Type: GrantFiled: June 16, 2011Date of Patent: February 19, 2013Assignee: Gilead Colorado, Inc.Inventors: Michael J. Gerber, Christopher Dufton
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Publication number: 20130039998Abstract: The present invention is directed to a composition comprising a modulator of the Wnt/?-catenin pathway, such as a GSK-3 inhibitor, or a pharmaceutically acceptable salt thereof either with a benzamide derivative or a pharmaceutically acceptable salt thereof or with a hydroxamic acid or a pharmaceutically acceptable salt thereof. The present invention is also directed to a method of treating bipolar disorder in a subject by administering either a benzamide derivative or a hydroxamic acid to the subject under conditions effective to treat a bipolar disorder. A modulator of the Wnt/?-catenin pathway, such as a GSK-3 inhibitor, or a pharmaceutically acceptable salt thereof may also be administered to a subject.Type: ApplicationFiled: December 23, 2009Publication date: February 14, 2013Applicants: UNIVERSITY OF WASHINGTON, MASSACHUSETTS INSTITUTE OF TECHNOLOGYInventors: Daniel Fass, Stephen Haggarty, Edward Scolnick, Randall T. Moon, Travis L. Biechele, Nathan D. Camp
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Patent number: 8372873Abstract: The present invention relates to compounds of formula (I): or a pharmaceutically acceptable salt thereof. These compounds inhibit serine protease, particularly the hepatitis C virus NS3-NS4A protease.Type: GrantFiled: March 29, 2011Date of Patent: February 12, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Kevin M. Cottrell, John Maxwell, Qing Tang, Anne-Laure Grillot, Arnaud Le Tiran, Emanuele Perola
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Publication number: 20130035351Abstract: The present invention relates to non-charged oxime compounds which are acetyl cholinesterase (AChE) reactivators of inhibited AChE and which protect against organophosphate poisoning both peripherally and in the central nervous system. Also disclosed are pharmaceutical compositions and methods for preparing the reactivator compounds and associated intermediates.Type: ApplicationFiled: August 3, 2011Publication date: February 7, 2013Applicant: SOUTHWEST RESEARCH INSTITUTEInventors: Stanton F. MCHARDY, Richard M. CORBETT, Donald M. MAXWELL, Michael W. TIDWELL, Bismarck CAMPOS, Christopher J. BEMBEN
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Patent number: 8367683Abstract: Provided is a composition comprising 5-FU and salicylic acid. This composition is useful as a treatment for warts. As opposed to conventional compositions and methods, this composition need only be applied once a day. Also provided are methods for the preparation and use of the composition for treatment of warts.Type: GrantFiled: January 19, 2010Date of Patent: February 5, 2013Assignee: Medcara, L.L.C.Inventor: Craig Herman
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Publication number: 20130030000Abstract: The present invention is directed to a composition useful for the treatment of a FAAH mediated disease, disorder or conditions comprising a FAAH inhibitor and a second activation, comprising a selected imidazole or oxazole FAAH inhibitor and a second active agent. The compositions will be useful in the treatment of a wide range of disease, disorder, or conditions including osteoarthritis, rheumatoid arthritis, diabetic neuropathy, postherpetic neuralgia, skeletomuscular pain, and fibromyalgia, as well as acute pain, migraine, sleep disorder, Alzheimer disease, and Parkinson's disease. In another aspect the invention discloses herein is directed to compositions useful in the treatment of neuropathic and nociceptive pain, said compositions comprising etoricoxib.Type: ApplicationFiled: January 25, 2011Publication date: January 31, 2013Inventors: Harry R. Chobanian, Linus S. Lin, Ping Liu, Marc D. Chioda, Robert J. DeVita, Ravi P. Nargund, Yan Guo, Terence G. Hamill, Wenping Li, Darrell Arthur Henze
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Publication number: 20130028946Abstract: The present invention provides a composition and an antiviral drug preparation, each comprising at least one water-insoluble antiviral drug and at least one water-soluble carrier material, wherein the water-insoluble antiviral drug is dispersed through the water-soluble carrier material in nano-disperse form. The present invention further provides processes for preparing the compositions and drug preparations, and also aqueous nano-dispersions obtained by combining water and the compositions.Type: ApplicationFiled: October 12, 2011Publication date: January 31, 2013Applicant: IOTA NANOSOLUTIONS LIMITEDInventors: Alison J. Foster, James Long, Steven P. Rannard, Dong Wang, David J. Duncalf