Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/233.8)
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Patent number: 8481532Abstract: Vicinal substituted cyclopropyl compounds which are inhibitors of phosphodiesterase 10 are described as are processes, pharmaceutical compositions, pharmaceutical preparations and pharmaceutical use of the compounds in the treatment of mammals, including human(s) for central nervous system (CNS) disorders and other disorders which may affect CNS function, for example neurological, neurodegenerative and psychiatric disorders including, but not limited to, those comprising cognitive deficits or schizophrenic symptoms.Type: GrantFiled: July 9, 2009Date of Patent: July 9, 2013Assignee: EnVivo Pharmaceuticals, Inc.Inventors: Amy Ripka, Gideon Shapiro, Richard Chesworth
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Publication number: 20130165432Abstract: The present invention relates to compounds of the formula (I) wherein R1, R2, X and n are as defined in the specification as dual modulators of the serotonin 5-HT2a and dopamine D3 receptors, their manufacture, pharmaceutical compositions containing them and their use for the treatment of psychotic disorders, as well as other diseases such as depression and anxiety, drug dependence, dementias and memory impairment.Type: ApplicationFiled: February 21, 2013Publication date: June 27, 2013Applicant: Hoffmann-La Roche Inc.Inventor: Hoffmann-La Roche Inc.
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Publication number: 20130165438Abstract: The present invention provides a piperidine compound represented by Formula (I) (wherein X1, X2, X2, A, B and N are as defined in the Description); or a salt thereof.Type: ApplicationFiled: September 6, 2011Publication date: June 27, 2013Applicant: TAIHO PHARMACEUTICAL CO., LTD.Inventors: Yoshihiro Urade, Makoto Kitade, Keiko Yamane, Shinichi Aoki, Hiroyoshi Yamanaka
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Patent number: 8470817Abstract: Compounds for treating, preventing or managing cancer are disclosed. Also provided are methods for using the compounds in treatment of various cancers. Also provided are methods of treatment using the compounds together with another chemotherapy, radiation therapy, hormonal therapy, biological therapy, or immunotherapy. Pharmaceutical compositions suitable for use in the methods are also disclosed.Type: GrantFiled: October 26, 2010Date of Patent: June 25, 2013Assignee: Sunesis Pharmaceuticals, Inc.Inventor: Anantha Sudhakar
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Patent number: 8470850Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds and methods for inhibiting VEGF receptor signaling and HGF receptor signaling.Type: GrantFiled: May 6, 2010Date of Patent: June 25, 2013Assignee: MethylGene Inc.Inventors: Arkadii Vaisburg, Stephen William Claridge, Franck Raeppel, Oscar Mario Saavedra, Noemy Berstein, Marie-Claude Granger, Lijie Zhan, Amal Wahhab, David Liewellyn
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Patent number: 8461156Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: August 27, 2012Date of Patent: June 11, 2013Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D. J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Patent number: 8455484Abstract: The invention provides new compounds and compositions thereof. The invention also provides methods for treating ophthalmic diseases, disorders and conditions.Type: GrantFiled: April 8, 2011Date of Patent: June 4, 2013Assignee: MethylGene Inc.Inventors: Stéphane Raeppel, Lijie Zhan, Stephen William Claridge, Franck Raeppel, Frédéric Gaudette, Arkadii Vaisburg
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Publication number: 20130129677Abstract: Methods and pharmaceutical compositions for treating viral infections, by administering certain thienopyridine derivative compounds in therapeutically effective amounts are disclosed. Methods of using the compounds and pharmaceutical compositions thereof are also disclosed. In particular, the treatment of viral infections such as caused by flavivirus is disclosed, i.e., including but not limited to, Dengue virus, West Nile virus, yellow fever virus, Japanese encephalitis virus, and tick-borne encephalitis virus.Type: ApplicationFiled: December 7, 2012Publication date: May 23, 2013Applicant: Siga Technologies, Inc.Inventor: Siga Technologies, Inc.
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Patent number: 8445480Abstract: Compounds having the structure of Formula I1 including pharmaceutically acceptable salts of the compounds, are potent CETP (cholesterol ester transfer protein) inhibitors, and are useful for raising HDL-cholesterol, reducing LDL-cholesterol, and for treating or preventing atherosclerosis Atherosclerosis and its clinical consequences, coronary heart disease (CHD), stroke and penpheral vascular disease, represent a truly enormous burden to the health care systems of the industrialized world In formula I, A-B is an arylamide moiety.Type: GrantFiled: June 16, 2008Date of Patent: May 21, 2013Assignee: Merck Sharp & Dohme Corp.Inventors: Julianne A. Hunt, Ramzi F. Sweis, Dooseop Kim, Florida Kallashi, Peter J. Sinclair
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Pyrrolo[2,3-b]pyridin-4-yl-amines and pyrrolo[2,3-b]pyrimidin-5-yl-amines as Janus kinase inhibitors
Patent number: 8445488Abstract: The present invention provides pyrrolo[2,3-b]pyridine-4-yl amines pyrrolo[2,3-b]pyrimidin-4-yl amines that modulate the activity of Janus kinases and are useful in the treatment of diseases related to activity of Janus kinases including, for example, immune-related diseases and cancer.Type: GrantFiled: September 26, 2011Date of Patent: May 21, 2013Assignee: Incyte CorporationInventors: James D. Rodgers, Haisheng Wang, Andrew P. Combs, Richard B. Sparks -
Publication number: 20130102595Abstract: The present invention provides a method of treating a cancer associated with a K-ras mutation in a subject in need thereof. The method comprises the steps of: (1) identifying a subject with a cancer associated with a K-ras mutation; and (2) administering to the subject (i) an inhibitor of PI3 kinase and (ii) an HDAC inhibitor, wherein the PI3 kinase inhibitor and the HDAC inhibitor are administered in amounts which together are therapeutically effective.Type: ApplicationFiled: October 15, 2012Publication date: April 25, 2013Inventor: Curis, Inc.
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Patent number: 8410109Abstract: The present invention relates to polyphenol-like compounds that are useful for inhibiting VCAM-1 expression, MCP-1 expression and/or SMC proliferation in a mammal. The disclosed compounds are useful for regulating markers of inflammatory conditions, including vascular inflammation, and for treatment and prevention of inflammatory and cardiovascular diseases and related disease states.Type: GrantFiled: July 28, 2006Date of Patent: April 2, 2013Assignee: Resverlogix Corp.Inventors: Norman C. W. Wong, Henrik C. Hansen, Fabrizio S. Chiacchia, Jan O. Johansson
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Publication number: 20130079340Abstract: Certain novel benzothiazoles and benzoxazoles, e.g., 2-(piperazin-1-yl)benzothiazoles and 2-(piperazin-1-yl)benzoxazoles, optionally substituted in the 3 and/or 4 positions of the piperazine rings, having histamine H3 antagonistic activity can be used in pharmaceutical compositions.Type: ApplicationFiled: October 25, 2012Publication date: March 28, 2013Inventors: Florencio Zaragoza Dorwald, Rolf Hohlweg, Inge Thoger Christensen, Jane Marie Lundbeck, Knud Erik Andersen
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Publication number: 20130079339Abstract: The invention discloses compounds of formula I wherein Y is a group of formula A, B, C, D, or E: and W, Q, n, R1, R2, R3, U1-U5, J and K have the meanings given in the description. The compounds of formula I are TRPV1 antagonists and are useful as active ingredients of pharmaceutical compositions for the treatment of pain and other conditions ameliorated by the inhibition of the vanilloid receptor TRPV1.Type: ApplicationFiled: December 22, 2010Publication date: March 28, 2013Applicant: PHARMESTE S.R.L.Inventors: Mauro Napoletano, Marcello Trevisani, Maria Giovanna Pavani, Francesca Fruttarolo
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Publication number: 20130072482Abstract: The present invention is for the anti-inflammatory compounds that have an inhibitory activity against protein tyrosine kinases and their pharmaceutical composition(s) containing the compound as the active ingredient. Since the compounds of the present invention can inhibit multiple protein kinases associated with inflammatory diseases and immune disorders, they are useful for their prevention or treatment.Type: ApplicationFiled: May 26, 2011Publication date: March 21, 2013Inventors: Beom-Seok Yang, Yong-Zu Kim, Tae-Kyo Park, Sung-Ho Woo, Hyang-Sook Lee, Sun-Young Kim, Jong-Un Cho, Hong-Bum Lee
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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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Patent number: 8389517Abstract: A method of treating a glomerular disease selected from the group consisting of mesangial proliferative glomerulonephritis, collapsing glomerulopathy, proliferative lupus nephritis, crescentic glomerulonephritis and membranous nephropathy in a subject comprises administering to the subject an effective amount of a glucosylceramide synthase inhibitor.Type: GrantFiled: July 27, 2009Date of Patent: March 5, 2013Assignee: Genzyme CorporationInventors: Oxana Ibraghimov-Beskrovnaya, Thomas A. Natoli
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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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Publication number: 20130053380Abstract: The invention provides modulators for the orphan nuclear receptor ROR? and methods for treating ROR? mediated diseases by administrating these novel ROR? modulators to a human or a mammal in need thereof. Specifically, the present invention provides compounds of Formula (1) and the enantiomers, diastereomers, tautomers, solvates and pharmaceutically acceptable salts thereof.Type: ApplicationFiled: February 28, 2011Publication date: February 28, 2013Applicant: PHENEX PHARMACEUTICALS AGInventors: Olaf Kinzel, Christoph Steeneck, Gerald Klaymann, Michael Albers, Thomas Hoffman, Claus Kremoser, Sanja Perovic-Ottstadt, Thomas Schlüter
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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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Patent number: 8377921Abstract: The invention provides novel pyrimidine and pyridine derivatives and pharmaceutical compositions thereof, and methods for using such compounds. For example, the pyrimidine and pyridine derivatives of the invention may be used to treat, ameliorate or prevent a condition which responds to inhibition of anaplastic lymphoma kinase (ALK) activity, focal adhesion kinase (FAK), zeta-chain-associated protein kinase 70 (ZAP-70), insulin-like growth factor (IGF-1R), or a combination thereof.Type: GrantFiled: June 29, 2011Date of Patent: February 19, 2013Assignee: IRM LLCInventors: Pierre-Yves Michellys, Wei Pei, Thomas H. Marsilje, Bei Chen, Tetsuo Uno
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Publication number: 20130040948Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein n, Y, R1, R2, R3, and R4 are as described herein, as well as pharmaceutically acceptable salts and esters thereof. Further the present invention is concerned with the manufacture of the compounds of formula (I), pharmaceutical compositions containing them and their use as pharmaceutical agents.Type: ApplicationFiled: February 10, 2012Publication date: February 14, 2013Inventors: Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
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Publication number: 20130035332Abstract: The present invention is directed to benzothiazol-one and thiazolo pyridine-one derivatives which are potentiators of metabotropic glutamate receptors, particularly the mGluR2 receptor, and which are useful in the treatment or prevention of neurological and psychiatric disorders associated with glutamate dysfunction and diseases in which metabotropic glutamate receptors are involved. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which metabotropic glutamate receptors are involved.Type: ApplicationFiled: April 25, 2011Publication date: February 7, 2013Inventors: Mark E. Layton, Michael J. Kelly
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Publication number: 20130029970Abstract: The present disclosure relates to compounds of formula I useful as agonists of cannabinoid receptors. The disclosure also provides pharmaceutically acceptable compositions comprising the compounds of the disclosure and methods of using the compositions in the treatment of various disorders.Type: ApplicationFiled: July 9, 2010Publication date: January 31, 2013Applicant: IRONWOOD PHARMACEUTICALS, INCInventors: Kevin Sprott, Jason Rohde, Takashi Nakai, Bo Peng, John Jeffrey Talley
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Publication number: 20130018037Abstract: Spirocyclic amide derivatives of formula I wherein ArCH2CH2NH— represents a ?-adrenoceptor binding group, processes for their preparation, pharmaceutical compositions containing them, a process for preparing such pharmaceutical compositions, their use in therapy, and intermediates for use in their preparation.Type: ApplicationFiled: September 14, 2012Publication date: January 17, 2013Inventors: Lilian Alcaraz, Andrew Bailey, Nicholas Kindon
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Publication number: 20130005723Abstract: Compounds of formula I wherein: R1 is and R2, R4, and R6-9 are defined herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit PI3 kinase and mTOR, and may be used to treat diseases mediated by PI3 kinase and mTOR, such as a variety of cancers. Methods for making and using the compounds of this invention are disclosed. Various compositions containing the compounds of this invention are also disclosed.Type: ApplicationFiled: June 6, 2012Publication date: January 3, 2013Inventors: Aranapakam Mudumbai Venkatesan, Zecheng Chen, Christoph Martin Dehnhardt, Osvaldo Dos Santos, Efren Guillermo Delos Santos, Arie Zask, Jeroen Cunera Verheijen, Joshua Aaron Kaplan, David James Richard, Semiramis Ayral-Kaloustian, Tarek Suhayl Mansour, Ariamala Gopalsamy, Kevin Joseph Curran, Mengxiao Shi
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Patent number: 8343954Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful. Also disclosed are methods of making the compounds.Type: GrantFiled: July 27, 2011Date of Patent: January 1, 2013Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
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Publication number: 20120329774Abstract: A series of thieno[2,3-b]pyridine derivatives which are substituted in the 2-position by a substituted anilino moiety, being selective inhibitors of human MEK (MAPKK) enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, proliferative (including oncological) and nociceptive conditions.Type: ApplicationFiled: September 5, 2012Publication date: December 27, 2012Applicant: UCB Pharma S.A.Inventors: Clive Martin Hutchings, Sarah Catherine Archibald, Daniel Christopher Brookings, Jeremy Martin Davis, James Andrew Johnson, Barry John Langham, Judi Charlotte Neuss
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Publication number: 20120322788Abstract: The present invention relates to spirocyclic amide derivatives of the formula I, pharmaceutically acceptable salts thereof, a process for their preparation, pharmaceutical compositions containing them, and their use in therapy.Type: ApplicationFiled: April 2, 2012Publication date: December 20, 2012Inventors: Lilian Alcaraz, Andrew Bailey, Richard James Bull, Timothy Johnson, Nicholas David Kindon, Andrew Stuart Lister, Andrew James Robbins, Michael John Stocks, Barry John Teobald
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Publication number: 20120322787Abstract: A compound is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. The subject has type 2 diabetes; renal hypertrophy or hyperplasia associated with diabetic nephropathy; Tay-Sachs; Gaucher's; or Fabry's disease. Methods of decreasing plasma TNF-?, lowering blood glucose levels, decreasing glycated hemoglobin levels, inhibiting glucosylceramide synthase, and lowering glycosphingolipid concentrations in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Frederic Vinick, Thomas H. Jozefiak, Yibin Xiang, John Kane, Junkai Liao
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Publication number: 20120322786Abstract: A compound for use in treating polycystic kidney disease is represented by Structural Formula (I): or a pharmaceutically acceptable salt thereof. A pharmaceutical composition comprises a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. A method of treating polycystic kidney disease in a subject in need thereof comprises administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof. Methods of treating in polycystic kidney disease in a subject in need thereof respectively comprise administering to the subject a therapeutically effective amount of a compound represented by Structural Formula (I) or a pharmaceutically acceptable salt thereof.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: Genzyme CorporationInventors: Craig Siegel, Cecilia M. Bastos, David J. Harris, Angeles Dios, Edward Lee, Richard Silva, Lisa M. Cuff, Mikaela Levine, Cassandra A. Celatka, Thomas H. Jozafiak, Frederic Vinick, Yibin Xiang, John Kane, Junkai Liao
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Publication number: 20120321637Abstract: Embodiments are directed to compositions and methods related combination therapy with HERV inhibition.Type: ApplicationFiled: June 18, 2012Publication date: December 20, 2012Applicant: The Board of Regents of the University of Texas SystemInventors: Jianli Dong, Gengming Huang
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Publication number: 20120322798Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTC”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: ApplicationFiled: August 27, 2012Publication date: December 20, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
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Publication number: 20120316162Abstract: Compounds of the formula (I), in which R1, R2, R3, D, G, Q and W have the meanings indicated in claim (1), can and be employed for the treatment of tumours.Type: ApplicationFiled: August 22, 2012Publication date: December 13, 2012Applicant: Merck Patent Gesellschaft Mit Beschrankter HaftungInventors: Kai SCHIEMANN, Melanie SCHULTZ, Andree BLAUKAT, Ingo KOBER
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Patent number: 8329726Abstract: The invention relates to the inhibition of VEGF receptor signaling and HGF receptor signaling. The invention provides compounds of general formula (A) wherein A1 is sulfur, A3 is CH, A2 is CH, D is heterocycle, Z is oxygen, SO0-2 or NR, Ar is phenyl and G is not a ring, and methods for inhibiting VEGF receptor signaling and HGF receptor signaling. The invention also provides compositions and methods for treating cell proliferative diseases and conditions.Type: GrantFiled: December 8, 2011Date of Patent: December 11, 2012Assignee: MethylGene Inc.Inventors: Oscar Mario Saavedra, Stephen William Claridge, Lijie Zhan, Franck Raeppel, Arkadii Vaisburg, Stephane Raeppel, Michael Mannion, Frederic Gaudette, Ljubomir Isakovic, Marie-Claude Granger, Naomy Bernstein
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Publication number: 20120309739Abstract: The invention relates to a series of compounds with particular activity as inhibitors of the serine-threonine kinase AKT. Also provided are pharmaceutical compositions comprising same as well as methods for treating cancer.Type: ApplicationFiled: November 3, 2010Publication date: December 6, 2012Applicant: ALMAC DISCOVERY LIMITEDInventors: Mark Peter Bell, Colin Roderick O'Dowd, James Samuel Shane Rountree, Graham Peter Trevitt, Timothy Harrison, Mary Melissa McFarland
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Patent number: 8324200Abstract: Disclosed are compounds of formula I, compositions containing them, and methods of use for the compounds and compositions in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK 2 and JAK3, are therapeutically useful.Type: GrantFiled: January 22, 2010Date of Patent: December 4, 2012Assignee: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo J. Heckrodt, Yan Chen, Darren John McMurtrie, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Sambaiah Thota, Rose Yen
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Patent number: 8324204Abstract: A series of 5,6-dihydro-1-benzothiophen-7(4H)-one derivatives, and analogues thereof, which are substituted in the 2-position by an optionally substituted morpholin-4-yl moiety, being selective inhibitors of PI3 kinase enzymes, are accordingly of benefit in medicine, for example in the treatment of inflammatory, autoimmune, cardiovascular, neurodegenerative, metabolic, oncological, nociceptive or ophthalmic conditions.Type: GrantFiled: June 4, 2007Date of Patent: December 4, 2012Assignee: UCB Pharma SAInventors: Rikki Peter Alexander, Stuart Bailey, Stephen Brand, Daniel Christopher Brookings, Julien Alistair Brown, Alan Findlay Haughan, Natasha Kinsella, Christopher Lowe, Stephen Robert Mack, William Ross Pitt, Marianna Dilani Richard, Andrew Sharpe, Laura Jane Tait
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Publication number: 20120302547Abstract: The present invention relates to a melanin concentrating hormone antagonist compound of formula (I) wherein R1, Ra, Rb, R2, L1, R3, R4 and R5 are as defined, or a pharmaceutically acceptable salt, enantiomer, diastereomer or mixture of diasteromers thereof useful in the treatment, obesity and related diseases.Type: ApplicationFiled: August 8, 2012Publication date: November 29, 2012Applicant: ELI LILLY AND COMPANYInventors: Macklin Brian Arnold, Yen Dao, Kevin Matthew Gardinier, David Joseph Garmene, Steven James Green, Erik James Hembre, Jianliang Lu
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Patent number: 8318733Abstract: Compounds of the present invention, and pharmaceutically acceptable compositions thereof, are useful as modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”). The present invention also relates to methods of treating ABC transporter mediated diseases using compounds of the present invention.Type: GrantFiled: May 16, 2011Date of Patent: November 27, 2012Assignee: Vertex Pharmaceuticals IncorporatedInventors: Sara Sabina Hadida-Ruah, Matthew Hamilton, Mark Thomas Miller, Peter Diederik Jan Grootenhuis, Jinglan Zhou, Brian Richard Bear, Jason McCartney
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Patent number: 8314121Abstract: The present invention relates to imidazolone derivatives of formula (I) to methods of preparing such derivatives, intermediates thereto, pharmaceutical compositions comprising such derivatives, and methods of inhibiting protein kinase, and methods of treatment comprising administration of such derivatives.Type: GrantFiled: March 31, 2009Date of Patent: November 20, 2012Assignee: SanofiInventors: Vincent Leroy, Eric Bacque, Emmanuel Conseiller, Anke Steinmetz, Baptiste Ronan, Jean-Philippe Letallec
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Patent number: 8314247Abstract: A hydrazone derivative of formula [I]: wherein Ring A is aryl or heteroaryl, Ring T is heteroaryl or heterocycle, R1 and R2 are independently hydrogen atom, halogen atom, cycloalkylsulfonyl, etc., R3 and R4 combine each other together with the adjacent nitrogen atom to form substituted or unsubstituted heterocycle, R5 is hydrogen atom, halogen atom, cyano, nitro, tetrazolyl, etc., and R6 is hydrogen atom, etc.; or a pharmaceutically acceptable salt thereof is useful as a glucokinase activation agent.Type: GrantFiled: January 9, 2008Date of Patent: November 20, 2012Assignee: Mitsubishi Tanabe Pharma CorporationInventors: Iwao Takamuro, Kazutoshi Sugawara, Hiroshi Sugama
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Publication number: 20120288501Abstract: New substituted benz-azole compounds, compositions and methods of inhibition of Raf kinase activity in a human or animal subject are provided. The new compounds compositions may be used either alone or in combination with at least one additional agent for the treatment of a Raf kinase mediated disorder, such as cancer.Type: ApplicationFiled: July 24, 2012Publication date: November 15, 2012Applicant: Novartis Vaccines and Diagnostics, Inc. formerly known as Chiron CorporationInventors: Payman Amiri, Wendy Fantl, Barry Haskell Levine, Daniel J. Poon, Savithri Ramurthy, Paul A. Renhowe, Sharadha Subramanian, Leonard Sung
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Publication number: 20120288492Abstract: The present invention relates to pyrimidine compounds of formula (I): which are useful in treating mTOR kinase- or PI3K kinase-related diseases.Type: ApplicationFiled: December 27, 2010Publication date: November 15, 2012Applicants: DCB-USA LLC, DEVELOPMENT CENTER FOR BIOTECHNOLOGYInventors: Mann-Yan Kuo, Ying-Shuan Lee, Paonien Chen, Li Jung Chen, Yann Yu Lu, Yi-Ting Huang, Hung-Yi Hsu, Ping-Kuei Tsai
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Publication number: 20120283255Abstract: The present invention provides compounds of formula (I): in which R1, R?1, R2, R?2, R3, and Y have the meanings given in the description, to a process for their preparation, their application by way of medicaments, and to pharmaceutical compositions containing them.Type: ApplicationFiled: June 27, 2012Publication date: November 8, 2012Inventors: Pierre DEPREZ, Hélène Jary, Taoues Temal
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Publication number: 20120277212Abstract: The present invention provides new oxime derivatives of the general formula (I), pharmaceutical compositions containing them and their use for the treatment and/or prophylaxis of conditions associated with altered glutamatergic signalling and/or functions, and/or conditions which can be affected by alteration of glutamate level or signalling in mammals. This invention further provides new oxime derivatives of the general formula (I) consisting of modulators of nervous system receptors sensitive to glutamate, which makes them particularly suitable for the treatment and/or prophylaxis of acute and chronic neurological and/or psychiatric disorders. In particular embodiments, the new oxime derivatives of the invention are modulators of metabotropic glutamate receptors (mGluRs). The invention further provides positive allosteric modulators of mGluRs and more specifically positive alSosteric modulators of mGluR4.Type: ApplicationFiled: October 29, 2010Publication date: November 1, 2012Applicants: PRESTWICK CHEMICAL, INC., DOMAIN THERAPEUTICSInventors: Stephan Schann, Stanislas Mayer, Christophe Morice, Bruno Giethlen
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Publication number: 20120277209Abstract: Pyrazine compounds of formula (I): or a pharmaceutically acceptable salt thereof, wherein m, n, p, R1, R2, R3, R4, X1, X2, X3, X4, X5, X6, X7, X8, X9, X10, X11, Y and Z are defined in the specification, and compositions containing them, and processes for preparing such compounds. Provided herein also are methods of treating disorders or diseases treatable by inhibition of PDE10, such as obesity, non-insulin dependent diabetes, schizophrenia, bipolar disorder, obsessive-compulsive disorder, and the like.Type: ApplicationFiled: June 22, 2012Publication date: November 1, 2012Applicant: Amgen Inc.Inventors: Jennifer R. Allen, Matthew P. Bourbeau, Ning Chen, Essa Hu, Roxanne Kunz, Shannon Rumfelt
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Publication number: 20120270869Abstract: The present invention relates to modulators of ATP-Binding Cassette (“ABC”) transporters or fragments thereof, including Cystic Fibrosis Transmembrane Conductance Regulator (“CFTR”), compositions thereof, and methods therewith. The present invention also relates to methods of treating ABC transporter mediated diseases using such modulators.Type: ApplicationFiled: June 26, 2012Publication date: October 25, 2012Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
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Publication number: 20120270868Abstract: The present invention relates to compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein R1, R2, R3 and X are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.Type: ApplicationFiled: October 17, 2011Publication date: October 25, 2012Applicant: Boehringer Ingelheim International GmbHInventors: Thomas Martin KIRRANE, Daniel Richard MARSHALL, Robert SIBLEY, Roger John SNOW, Fariba SOLEYMANZADEH, Ronald John SORCEK
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Publication number: 20120270867Abstract: The invention relates to the novel materials of formula (I), where: R1 is an optionally substituted aryl or heteroaryl; R is an H or, when formed with R1, a 5- or 6-member ring fused with an aryl or heretoaryl group optionally containing one or more of O, S, N, NH, and Nalk, being optionally substituted; R2 and R3 are, independently, an H, Hal, or alkyl optionally substituted by one or more Hal; R4 is H; and R5 is an H or alkyl optionally substituted by one or more halogen atoms. Said materials being in any isomeric form and the salts thereof, and are intended for drugs, particularly AKT(PKB) phosphorylation inhibitors.Type: ApplicationFiled: December 27, 2011Publication date: October 25, 2012Applicant: SANOFIInventors: Jean-Christophe CARRY, Victor CERTAL, Frank HALLEY, Karl Andreas KARLSSON, Laurent SCHIO, Fabienne THOMPSON