Ring Nitrogen Shared By Two Of The Cyclos Patents (Class 514/230.2)
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Publication number: 20120295898Abstract: The present invention relates to combinations of compounds comprising HIV integrase inhibitors and other therapeutic agents. Such combinations are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: January 24, 2011Publication date: November 22, 2012Inventor: Mark Richard Underwood
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Publication number: 20120276153Abstract: Methods for treating cystic fibrosis. The method includes administering to a human in need thereof an aerosol solution comprising levofloxacin or ofloxacin and a divalent or trivalent cation. More particularly, the method includes administering the aerosol solution to a human having a pulmonary infection comprising P. aeruginosa.Type: ApplicationFiled: March 5, 2012Publication date: November 1, 2012Applicant: MPEX PHARMACEUTICALS, INC.Inventors: Jeffery S. Loutit, Elizabeth E. Morgan, Michael N. Dudley, David C. Griffith, Olga Lomovskaya
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Patent number: 8288376Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: January 24, 2012Date of Patent: October 16, 2012Assignee: SanofiInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Patent number: 8288375Abstract: Disclosed are compounds of Formulae 1 and 1a, N-oxides, and salts thereof, wherein R1, R1a, Y, and J 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. Further disclosed is a method for preparing compounds of Formula 1 from compounds of Formula 1a.Type: GrantFiled: December 10, 2008Date of Patent: October 16, 2012Assignee: E.I. du Pont de Nemours and CompanyInventors: Andrew Edmund Taggi, Thomas Martin Stevenson
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Publication number: 20120252720Abstract: The present invention relates to compositions and methods useful for the treatment of ear disorders, administered to a treated ear in the form of a foam or a mousse. Administering a medicament in such forms will increase the residence time of the medicament in the ear canal, provide relatively uniform distribution of the composition, and can increase the penetration of the active pharmaceutical ingredient in the affected area, may release active substances slowly, enhance treatment effectiveness, increase compliance and is more convenient to use than currently available ear medications. The administration in the form of a foam or a mousse may preferably be provided as a metered dose, of a volume suitable to fill the ear canal.Type: ApplicationFiled: April 2, 2012Publication date: October 4, 2012Applicant: Otic Pharma Ltd.Inventor: Eran Eilat
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Publication number: 20120245161Abstract: The present invention discloses and claims a series of substituted indolyl-piperidinyl benzylamines of the formula wherein R1, R2, R4 and R5 are as described herein. More specifically, the compounds of this invention are inhibitors of ?-tryptase and are, therefore, useful as pharmaceutical agents. Additionally, this invention also discloses methods of preparation of substituted indolyl-piperidinyl benzylamines.Type: ApplicationFiled: June 5, 2012Publication date: September 27, 2012Applicant: SANOFIInventors: Yong Mi CHOI-SLEDESKI, Guyan LIANG, Thaddeus R. NIEDUZAK, Gregory B. POLI, Patrick Wai-Kwok SHUM, Gregory T. STOKLOSA, Zhicheng ZHAO
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Publication number: 20120245107Abstract: The invention relates to formulations of an antimicrobial agent, a lipid, and optionally a surfactant, and uses thereof for reducing the proliferation and viability of microbial agents.Type: ApplicationFiled: June 7, 2012Publication date: September 27, 2012Inventors: William Henry, Henk-Andre Kroon, Linda Summerton
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Publication number: 20120237564Abstract: The present invention relates to methods and compositions for treating obstructive pulmonary disorders. In particular, compositions and methods described herein relate to the use of an aerosolized antibiotic for treating obstructive pulmonary disorders including chronic obstructive pulmonary disorder (COPD) and chronic bronchitis (CB).Type: ApplicationFiled: February 16, 2012Publication date: September 20, 2012Applicant: MPEX Pharmaceuticals, Inc.Inventors: Michael N. Dudley, Neil Berkley, David C. Griffith, Jeffery S. Loutit, Elizabeth E. Morgan, Keith A. Bostian, Sanjay Sethi
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Patent number: 8268819Abstract: The present invention relates to intermediates of the formula wherein G1 is N; G2 is selected from the group consisting of C?O and CH2; X is a halogen; and the other groups are defined herein.Type: GrantFiled: March 26, 2012Date of Patent: September 18, 2012Assignee: Takeda Pharmaceutical Company LimitedInventors: Bohan Jin, Nicholas Scorah, Qing Dong
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Publication number: 20120231995Abstract: There is provided the use of compounds of formula I wherein R1, R2, R3 and X have meanings given in the description, for the preparation of a medicament for killing clinically latent microorganisms. There is also provided the use of compounds of formula I for treating microbial infections, as well as certain compounds of formula I per se.Type: ApplicationFiled: May 17, 2012Publication date: September 13, 2012Applicant: HELPERBY THERAPEUTICS LIMITEDInventors: Petra Helga Beck, Marc Barry Brown, David Edward Clark, Anthony Coates, Hazel Joan Dyke, Yanmin Hu, Derek John Londesbrough, Keith Mills, Thomas David Pallin, Gary Patrick Reid, Gerlinda Stoddart
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Publication number: 20120232057Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: ApplicationFiled: May 25, 2012Publication date: September 13, 2012Inventors: George W. GRIESGRABER, Tushar A. KSHIRSAGAR, Azim A. CELEBI, Sarah J. SLANIA, Michael E. DANIELSON, Michael J. RICE, Joshua R. WURST
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Publication number: 20120220575Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein Ar, R1, R2, R3, G1, G2, and m are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating inflammatory disorders, cardiovascular disease, cancer, and other conditions associated with PI3K?.Type: ApplicationFiled: February 24, 2012Publication date: August 30, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Edcon Chang, Tony Gibson, Bohan Jin, Nicholas Scorah, Qing Dong
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Publication number: 20120214781Abstract: The present invention relates to an antibacterial food composition comprising a Propolis extract and a Vaccinium macrocarpon cranberry extract.Type: ApplicationFiled: April 1, 2010Publication date: August 23, 2012Inventor: Loïc Renard
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Publication number: 20120190654Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.Type: ApplicationFiled: July 28, 2010Publication date: July 26, 2012Applicant: MERCK PATENT GMBHInventors: Xiaoling Chen, Srinivasa R. Karra, Bayard R. Huck, Ruoxi Lan, Amanda E. Sutton, Andreas Goutopoulos, Brian L. Hodous, Reinaldo Jones
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Publication number: 20120178748Abstract: Provided herein are heteroaryl compounds, methods of their synthesis, pharmaceutical compositions comprising the compounds, and methods of their use. In one embodiment, the compounds provided herein are useful for the treatment, prevention, and/or management of various disorders, such as CNS disorders and metabolic disorders, including, but not limited to, e.g., neurological disorders, psychosis, schizophrenia, obesity, and diabetes.Type: ApplicationFiled: January 10, 2012Publication date: July 12, 2012Applicant: Sunovion Pharmaceuticals Inc.Inventors: John Emmerson CAMPBELL, Philip JONES, Michael Charles HEWITT
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Patent number: 8217034Abstract: The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: GrantFiled: July 23, 2009Date of Patent: July 10, 2012Assignees: Shionogi & Co., Ltd., GlaxoSmithKline LLCInventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama
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Publication number: 20120172352Abstract: The present invention is related to pyrazoline dione derivatives of Formula (I), pharmaceutical composition thereof and to their use for the treatment and/or prophylaxis of disorders or conditions related to Nicotinamide adenine dinucleotide phosphate oxidase (NADPH Oxidase).Type: ApplicationFiled: September 27, 2010Publication date: July 5, 2012Applicant: GENKYOTEX SAInventors: Patrick Page, Francesca Gaggini, Benoît Laleu
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Publication number: 20120171199Abstract: Tricyclic PI3k inhibitor compounds of Formula I with anti-cancer activity, anti-inflammatory activity, or immunoregulatory properties, and more specifically with PI3 kinase modulating or inhibitory activity are described. Methods are described for using the tricyclic PI3K inhibitor compounds of Formula I for in vitro, in situ, and in vivo diagnosis or treatment of mammalian cells, organisms, or associated pathological conditions. Formula I compounds include stereoisomers, geometric isomers, tautomers, and pharmaceutically acceptable salts thereof. The dashed lines indicate an optional double bond, and at least one dashed line is a double bond. The substituents are as described.Type: ApplicationFiled: December 15, 2011Publication date: July 5, 2012Inventors: Jennafer Dotson, Robert Andrew Heald, Timothy Heffron, Graham Elgin Jones, Sussie Lerche Krintel, Neville James McLean, Chudi Ndubaku, Alan G. Olivero, Laurent Salphati, Lan Wang, BinQing Wei
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Patent number: 8207162Abstract: Fused [1,2]imidazo[4,5-c] ring compounds (e.g., imidazo[4,5-c]quinolines, 6,7,8,9-tetrahydroimidazo[4,5-c]quinolines, imidazo[4,5-c]naphthyridines, and 6,7,8,9-tetrahydroimidazo[4,5-c]naphthyridines) with a —CH(—X1—R1)— group in the fused ring at the 1-position of the imidazo ring, pharmaceutical compositions containing the compounds, intermediates, methods of making the compounds, and methods of use of these compounds as immunomodulators, for inducing cytokine biosynthesis in animals and in the treatment of diseases including viral and neoplastic diseases, are disclosed.Type: GrantFiled: April 20, 2011Date of Patent: June 26, 2012Assignee: 3M Innovative Properties CompanyInventors: George W. Griesgraber, Sarah J. Slania
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Publication number: 20120142635Abstract: The present invention relates to compounds of the Formula (I) that are useful antimicrobial agents and effective against a variety of multi-drug resistant bacteria:Type: ApplicationFiled: February 8, 2012Publication date: June 7, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Christine Schmitt, Stefan Müller, Michael W. Cappi
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Publication number: 20120135961Abstract: The present invention relates to the use of compounds, in which the pharmacophores of quinolone and oxazolidinone are chemically linked together through a linker that is stable under physiological conditions, for the treatment of anthrax and other infections.Type: ApplicationFiled: January 10, 2011Publication date: May 31, 2012Applicant: Morphochem Aktiengesellschaft Fur Kombinatorische ChemieInventors: Christian Hubschwerlen, Jean-Luc Specklin, Daniel Baeschlin, Hans Locher, Christine Schmitt
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Publication number: 20120129846Abstract: In its many embodiments, the present invention provides a novel class of heterocyclic compounds of the formula: as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: May 24, 2012Inventors: Zhaoning Zhu, William J. Greenlee, Mihir Baran Mandal, Duane A. Burnett, Chad E. Bennett, Troy McCracken
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Publication number: 20120122852Abstract: The invention concerns tricyclic N-heteroaryl-carboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: ApplicationFiled: January 24, 2012Publication date: May 17, 2012Applicant: SANOFI-AVENTISInventors: Laurent DUBOIS, Yannick EVANNO, Luc EVEN, Catherine GILLE, Andre MALANDA, David MACHNIK, Nathalie RAKOTOARISOA
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Publication number: 20120122835Abstract: Disclosed are compounds of the following formula: in which R1, R2, R3, R4, R5, R6, R7, X, and t are defined in the specification. Also disclosed are pharmaceutical compositions, kits, and articles of manufacture, which contain the compounds, methods and intermediates useful for making the compounds, and methods of using the compounds to treat diseases, disorders, and conditions related to PARP activity.Type: ApplicationFiled: January 18, 2012Publication date: May 17, 2012Applicant: TAKEDA PHARMACEUTICAL COMPANY LIMITEDInventors: Anthony R. Gangloff, Andrew John Jennings, Benjamin Jones, Andre A. Kiryanov
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Publication number: 20120108582Abstract: A quinolone synthetic antibacterial agent having excellent properties as a medicine is provided, which has strong antibacterial activity not only to Gram-negative bacteria but also to Gram-positive cocci that have low sensitivity to quinolone antibacterial agents, and which exhibits high safety and excellent pharmacokinetics. A compound represented by the formula (I) or a salt thereof, or a hydrate thereof. Specifically, a quinolone derivative of the formula (I) wherein substituents R6 and R7 taken together with the carbon atoms to which they are bonded form a cyclic structure which may contain an oxygen atom as a ring constituent atom, the cyclic structure forming a 5-4, 5-5, or 5-6 fused bicyclic pyrrolidinyl substituent, the substituent being bonded to a quinolone mother skeleton Q containing a pyridobenzoxazine structure.Type: ApplicationFiled: July 2, 2009Publication date: May 3, 2012Inventors: Hisashi Takahashi, Satoshi Komoriya, Takahiro Kitamura, Takashi Odagiri, Hiroaki Inagaki, Toshifumi Tsuda, Kiyoshi Nakayama, Makoto Takemura, Kenichi Yoshida, Rie Miyauchi, Masatoshi Nagamochi
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Publication number: 20120094989Abstract: The present invention relates to compounds having 5-hydroxytryptamine receptor modulating activity, in particular compounds having an acidic moiety held distant from the 5-HT pharmacophore by a rigid linker group, to compositions containing such compounds and methods of treatment using them. Such compounds have an increased affinity for the 5-HT receptor and a reduced hERG effect. Certain compounds of the invention further exhibit an angiotensin II receptor modulating activity. Claimed are compounds of formula (I): HT-L-A. HT is a 5-HT receptor modulating moiety containing a basic nitrogen atom; A is an acid moiety; L is a linker moiety.Type: ApplicationFiled: April 1, 2010Publication date: April 19, 2012Applicant: SERODUS ASInventors: Jo Klaveness, Bjame Brudeli, Finn Olav Levy, Lise Roman Moltzau, Trygve Gulbrandsen
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Patent number: 8143248Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.Type: GrantFiled: August 1, 2008Date of Patent: March 27, 2012Assignee: Sanofi-AventisInventors: Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa
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Publication number: 20120058201Abstract: The present invention describes an association between genetic polymorphisms in the FAM13A1 (family with sequence similarity 13, member A1) gene and a predisposition to prolongation of the QT interval, and provides related methods for the prediction of such a predisposition, the administration of QT interval- prolonging compounds to individuals having such a predisposition, and determining whether a compound is capable of inducing QT prolongation.Type: ApplicationFiled: April 5, 2010Publication date: March 8, 2012Applicant: VANDA PHARMACEUTICALS, INC.Inventors: Christian Lavedan, Simona Volpi, Louis Licamele
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Publication number: 20120035166Abstract: Disclosed herein are methods of treating a pulmonary bacterial infection comprising bacteria growing under anaerobic conditions using a fluoroquinolone antibiotic. The fluoroquinolone antibiotic may, for example, be levofloxacin or ofloxacin. Also disclosed are methods of inhibiting bacteria growing under anaerobic conditions by exposing the bacteria to an amount of fluoroquinolone antibiotic effective to inhibit growth of said bacteria.Type: ApplicationFiled: October 21, 2011Publication date: February 9, 2012Inventors: Mike Dudley, David Griffith, Olga Rodny
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Publication number: 20120035409Abstract: This invention relates to novel bi- and tricyclic indazole-substituted 1,4-dihydropyridine derivatives having protein tyrosine kinase inhibitory activity, to a process for the manufacture thereof and to the use thereof for the treatment of c-Met-mediated diseases or c-Met-mediated conditions, particularly cancer and other proliferative disorders.Type: ApplicationFiled: February 5, 2010Publication date: February 9, 2012Applicant: BAYER SCHERING PHARMA AKTIENGESELLSCHAFTInventors: Martin Michels, Markus Follmann, Alexandros Vakalopoulos, Katja Zimmermann, Mario Lobell, Nicole Teusch, Shendong Yuan
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Publication number: 20120028972Abstract: Provided herein are methods for detecting and/or measuring the inhibition of TOR kinase activity in a subject and uses associated therewith.Type: ApplicationFiled: July 28, 2011Publication date: February 2, 2012Inventors: Lilly Wong, Shuichan Xu, Jian-Hua Ding
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Publication number: 20120022056Abstract: Compounds of formula (I) wherein R1, R2, X, A, Y, B, Z1, Q, p, r and s are defined in the specification for treating inter alia psychotic disorders, depressive disorders, anxiety disorders and sexual dysfunctions.Type: ApplicationFiled: August 29, 2005Publication date: January 26, 2012Inventors: Jonathan Bentley, Markus Bergauer, Babara Bertani, Matteo Biagetti, Manuela Borriello, Steven Mark Bromidge, Massimo Gianotti, Enrica Granci, Colin Philip Leslie, Alessandra Pasquarello, Valeria Zucchelli
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Publication number: 20110306601Abstract: Antagonists of group 1 metabotropic glutamate receptors (mGluR) potentiate the effect of positive AMPA receptor modulators on neurotrophin expression, such as brain-derived neurotrophic factor (BDNF). The findings described herein suggest a combinatorial approach for drug therapies, using both positive AMPA receptor modulators and mGluR antagonists, to enhance brain neurotrophism.Type: ApplicationFiled: August 19, 2011Publication date: December 15, 2011Applicant: The Regents of the University of CaliforniaInventors: Julie C. Lauterborn, Christine M. Gall, Gary Lynch
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Publication number: 20110301127Abstract: The instant methods and compositions represent an advance in controlling drug resistance in microbes. AcrAB-like efflux pumps have been found to control resistance to drugs, even in highly resistant microbes. Accordingly, methods of treating infection, methods of screening for inhibitors of AcrAB-like efflux pumps, and methods of enhancing antimicrobial activity of drugs are provided. Pharmaceutical composition comprising an inhibitor of an AcrAB-like efflux pump and an antimicrobial agent are also provided.Type: ApplicationFiled: August 16, 2011Publication date: December 8, 2011Applicant: TRUSTEES OF TUFTS COLLEGEInventors: Margret OETHINGER, Stuart B. LEVY
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Patent number: 8071591Abstract: Provided herein are aminoquinolones of formula I and compositions containing the compounds, wherein formula I is The compounds and compositions provided herein are useful in the amelioration or treatment of GSK-3 inhibitors mediated diseases.Type: GrantFiled: March 10, 2010Date of Patent: December 6, 2011Assignee: Kyorin Pharmaceutical Co., Ltd.Inventors: Masahiro Nomura, Kyoko Okada, Taro Sato, Yasushi Kohno
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Publication number: 20110280807Abstract: The invention disclosed relates to methods and models for enhancing stress-induced analgesia through non-opioid mechanisms.Type: ApplicationFiled: April 27, 2006Publication date: November 17, 2011Applicant: UNIVERSITY OF GEORGIA RESEARCH FOUNDATION, INC.Inventor: Andrea G. Hohmann
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Publication number: 20110275621Abstract: Tricyclic compounds of Formula I are inhibitors of HIV integrase and inhibitors of HIV replication: wherein bond a, ring A, R1, R2 and R3 are defined herein. The compounds are useful for the prophylaxis or treatment of infection by HIV and the prophylaxis, treatment, or delay in the onset of AIDS. The compounds are employed against HIV infection and AIDS as compounds per se or in the form of pharmaceutically acceptable salts. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.Type: ApplicationFiled: May 13, 2011Publication date: November 10, 2011Inventors: Joseph P. Vacca, John S. Wai, Linda S. Payne
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Publication number: 20110269751Abstract: The heterocyclic nitrogenous or oxygenous compounds of formula (A), (B), (C) or (D) formed from dialdehydes, their optical isomers, cis- and trans- isomers, or agrochemically acceptable salts, their preparation methods, agrochemical compositions comprising the compounds and the uses thereof are provided. The compounds and their derivatives have high insecticidal activities to several farming and forestry pests including homoptera and lepidoptera pests, such as aphis, fulgorid, whitefly, leafhopper, common thrips, cotton bollworm, cabbage caterpillar, cabbage moth, cotton leafworm, armyworm and so on.Type: ApplicationFiled: December 18, 2009Publication date: November 3, 2011Applicants: SHANGHAI SHENGNONG PESTICIDE CO., LTD., EAST CHINA UNIVERSITY OF SCIENCE AND TECHNOLOGYInventors: Zhong Li, Xuhong Qian, Xusheng Shao, Xiaoyong Xu, Liming Tao, Gonghua Song
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Publication number: 20110263587Abstract: The present invention relates to a reversibly heat-gelable aqueous composition comprising a reversibly heat-gelable aqueous composition according to conventional technique, to which a thixotropic property-increasing substance is added. The thixotropic property-increasing substance is preferably at least one member selected from the group consisting of sugar alcohol, lactose, carmellose or pharmaceutically acceptable salts thereof and cyclodextrin. This composition can be stored at room temperature and accordingly, it is quite convenient for users to carry about the same.Type: ApplicationFiled: July 1, 2011Publication date: October 27, 2011Applicant: WAKAMOTO PHARMACEUTICAL CO., LTD.Inventor: Hidekazu SUZUKI
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Publication number: 20110262543Abstract: Carrier particles for dry powder formulations for inhalation having reduced electrostatic charges are prepared.Type: ApplicationFiled: April 21, 2011Publication date: October 27, 2011Applicant: Chiesi Farmaceutici S.p.A.Inventors: Daniela Cocconi, Rossella Musa
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Publication number: 20110263567Abstract: The present invention relates to compounds of general formula (i) having an oxime moiety or a pharmaceutically acceptable salt, hydrate or solvate thereof and its use for inhibiting semicarbazide-sensitive amine oxidase (SSAO), also known as vascular adhesion protein-1 (VAP-1), a pharmaceutical composition comprising the compound or a salt, hydrate or solvate thereof as an active ingredient, a method for the prevention or the treatment of a SSAO/VAP-1 related disease, said diseases including acute or chronic inflammatory diseases, diseases related to carbohydrate metabolism, diabetes-associated complications, diabetic retinopathy and macular oedema, diseases related to adipocyte or smooth muscle dysfunctions, neurodegenerative diseases and vascular diseases.Type: ApplicationFiled: September 11, 2009Publication date: October 27, 2011Applicant: Semmelweis EgyetemInventors: Péter Mátyus, Kálmán Magyar, Marjo Pihlavisto, Klára Gyires, Norbert Haider, Yinghua Wang, Patrick Woda, Petra Dunkel, Éva Tóth-Sarudy, Gÿorgy Túrós
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Publication number: 20110257156Abstract: In its many embodiments, the present invention provides novel heterocyclic compounds as modulators of gamma secretase, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the central nervous system using such compounds or pharmaceutical compositions.Type: ApplicationFiled: November 5, 2009Publication date: October 20, 2011Inventors: Zhaoning Zhu, William J. Greenlee, David James Cole, Dmitri A. Pissarnitski, Gioconda V. Gallo, Hongmei Li, Hubert B. Josien, Jun Qin, Chad E. Knutson, Mihirbaran Mandal, Monica L. Vicarel, Murali Rajagopalan, Pawan Kumar Dhondi, Ruo Xu, Zhong-Yue Sun, Thomas A. Bara, Xianhai Huang, Xiaohong Zhu, Zhiqiang Zhao, John W. Clader, Anandan Palani, Theodros Asberom, Troy McCracken, Chad E. Bennett
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Publication number: 20110257167Abstract: Provided herein are methods for treating and/or preventing a cancer or a tumor syndrome in a patient, comprising administering an effective amount of a TOR kinase inhibitor to a patient having cancer or a tumor syndrome, characterized by a LKB1 and/or AMPK gene or protein loss or mutation.Type: ApplicationFiled: February 3, 2011Publication date: October 20, 2011Inventors: Rajesh Chopra, Yuhong Ning, Sabita Sankar, Shuichan Xu, Weiming Xu
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Publication number: 20110251177Abstract: The present disclosure provides biologically active 2,4-pyrimidinediamine compounds of formulae (I) and (II): and salts thereof, compositions comprising these compounds, and methods of using these compounds in a variety of applications.Type: ApplicationFiled: April 13, 2011Publication date: October 13, 2011Applicant: RIGEL PHARMACEUTICALS, INC.Inventors: Jiaxin Yu, Jeffrey Clough, Rajinder Singh
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Publication number: 20110223131Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: ApplicationFiled: February 22, 2011Publication date: September 15, 2011Applicant: Gilead Sciences, Inc.Inventors: Haolun JIN, Choung U. Kim, Barton W. Phillips
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Publication number: 20110212942Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, X, R1, R2, R3, R4, R5 and R6 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: September 1, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Publication number: 20110207716Abstract: The present invention provides compounds having a structure according to Formula (I): or a salt or solvate thereof, wherein ring A, E1, E2, R1, R2, R3 and R4 are defined herein. The invention further provides pharmaceutical compositions including the compounds of the invention and methods of making and using the compounds and compositions of the invention, e.g., in the treatment and prevention of various disorders, such as Parkinson's disease.Type: ApplicationFiled: December 21, 2010Publication date: August 25, 2011Inventors: Robert A. Galemmo, Dean R. Artis, Xiaocong Michael Ye, Danielle Aubele, Anh Truong, Simeon Bowers, Roy K. Hom, Yong-Liang Zhu, R. Jeffrey Neitz, Jennifer Sealy, Marc Adler, Paul Beroza, John P. Anderson
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Patent number: 7998950Abstract: The invention is related to anti-viral compounds, compositions containing such compounds, and therapeutic methods that include the administration of such compounds, as well as to processes and intermediates useful for preparing such compounds.Type: GrantFiled: July 24, 2009Date of Patent: August 16, 2011Assignee: Gilead Sciences, Inc.Inventors: Evangelos Aktoudianakis, Azim Alan Celebi, Zhimin Du, Salman Y. Jabri, Haolun Jin, Choung U. Kim, Jiayao Li, Samuel E. Metobo, Michael R. Mish, Barton W. Phillips, Joseph H. Saugier, Zheng-Yu Yang, Catalin Sebastian Zonte
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Patent number: 7998951Abstract: The invention encompasses compounds of Formula I as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.Type: GrantFiled: March 3, 2008Date of Patent: August 16, 2011Assignee: Bristol-Myers Squibb CompanyInventors: Kap-Sun Yeung, John F. Kadow
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Publication number: 20110190236Abstract: The present invention features compounds that are prodrugs of HIIV integrase inhibitors and therefore are useful in the inhibition of HIV replication, the prevention and/or treatment of infection by HIV, and in the treatment of AIDS and/or ARC.Type: ApplicationFiled: July 23, 2009Publication date: August 4, 2011Inventors: Brian Alvin Johns, Jason Gordon Weatherhead, Toshikazu Hakogi, Yasunori Aoyama