Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/233.8)
-
Publication number: 20140057906Abstract: 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: ApplicationFiled: October 21, 2013Publication date: February 27, 2014Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S. Hadida Ruah, Peter D.J. Grootenhuis, Fredrick Van Goor, Jinglan Zhou, Brian Bear, Mark T. Miller, Jason McCartney, Mehdi Michel Jamel Numa, Xiaoqing Yang
-
Publication number: 20140045811Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 18, 2013Publication date: February 13, 2014Inventors: Heather Finlay, Ji Jiang, Soong-Hoon Kim, Brandon Parkhurst, Jennifer X. Qiao, Tammy C. Wang, Zulan Pi, George O. Tora, John Lloyd, James A. Johnson
-
Publication number: 20140045829Abstract: 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: October 8, 2013Publication date: February 13, 2014Applicant: Merck Sharp & Dohme Corp.Inventors: MARK E. LAYTON, Michael J. Kelly
-
Patent number: 8637508Abstract: The invention relates to novel heterocyclic compounds of the formula in which all of the variables are as defined in the specification, pharmaceutical compositions thereof, combinations thereof, and their use as medicaments, particularly for the treatment of Alzheimer's Disease or diabetes via inhibition of BACE-1 or BACE-2.Type: GrantFiled: January 11, 2012Date of Patent: January 28, 2014Assignee: Novartis AGInventors: Sangamesh Badiger, Murali Chebrolu, Konstanze Hurth, Sébastien Jacquier, Rainer Martin Lueoend, Rainer Machauer, Heinrich Rueeger, Marina Tintelnot-Blomley, Siem Jacob Veenstra, Markus Voegtle
-
Publication number: 20140011799Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are endothelial lipase inhibitors which may be used as medicaments.Type: ApplicationFiled: July 8, 2013Publication date: January 9, 2014Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
-
Publication number: 20140005190Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: ApplicationFiled: June 27, 2013Publication date: January 2, 2014Applicants: Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research, AbbVie Inc.Inventors: JONATHAN BAYLDON BAELL, CHINH THIEN BUI, PETER COLMAN, DANETTE A. DUDLEY, WAYNE J. FAIRBROTHER, JOHN A. FLYGARE, GUILLAUME LAURENT LESSENE, CHUDI NDUBAKU, GEORGE NIKOLAKOPOULOS, CARL STEVEN RYE, BRAD EDMUND SLEEBS, BRIAN JOHN SMITH, KEITH GEOFFREY WATSON, STEVEN W. ELMORE, ANDREW M. PETROS, ANDREW J. SOUERS, PETER CZABOTAR
-
Publication number: 20130345195Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Michael J. BURKE, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Anil Kumar PADYANA, Lana Louise SMITH KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, QIANG ZHANG, Qing ZHANG
-
Publication number: 20130345213Abstract: Compounds of Formula (I) along with processes for their preparation that are useful for treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors. Methods of treating, managing and/or lessening the diseases, disorders, syndromes or conditions associated with the modulation of calcium sensing (CaSR) receptors of Formula (I).Type: ApplicationFiled: March 9, 2012Publication date: December 26, 2013Applicant: LUPIN LIMITEDInventors: Manojkumar Ramprasad Shukla, Vinod Dinkar Chaudhari, Majid Bashir Sayyed, Ramesh Dattatraya Phadtare, Navnath Bajirao Walke, Sanjeev Anant Kulkarni, Venkata P. Palle, Rajender Kumar Kamboj
-
Publication number: 20130345193Abstract: Described herein are compounds and pharmaceutical compositions containing such compounds, which modulate the activity of store-operated calcium (SOC) channels. Also described herein are methods of using such SOC channel modulators, alone and in combination with other compounds, for treating diseases or conditions that would benefit from inhibition of SOC channel activity.Type: ApplicationFiled: August 23, 2013Publication date: December 26, 2013Applicant: CALCIMEDICA, INC.Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
-
Patent number: 8609655Abstract: This invention relates generally to the field of medicine and, more specifically, to methods for treating epithelial injury, in particular, due to ischemia, hypoxia, trauma, chemolytics or radiation exposure.Type: GrantFiled: March 27, 2009Date of Patent: December 17, 2013Assignee: Amgen Inc.Inventors: John Peter Geibel, David Martin, Gordon Ng, William G. Richards, Joanne L. Viney, Patricia R. Hebert
-
Publication number: 20130331390Abstract: Nitrogen-containing biphenyl compounds as represented by formula (I), pharmaceutically acceptable salts or derivatives thereof, pharmaceutical compositions, and preparation methods therefore, and anti-HIV-1 use of the compound. Each substituent group in formula (I) is as defined in the description.Type: ApplicationFiled: October 13, 2011Publication date: December 12, 2013Applicants: Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming Institute of Zoology, The Chinese Academy of Sciences, Yunnan UniversityInventors: Jingping Liu, Handong Sun, Hongbin Zhang, Yongtong Zheng, Weilie Xiao, Jianxin Pu, Ruirui Wang, Liumeng Yang
-
Publication number: 20130324524Abstract: The present invention provides 2,4-pyrimidinediamine compounds that inhibit the IgE and/or IgG receptor signaling cascades that lead to the release of chemical mediators, intermediates and methods of synthesizing the compounds and methods of using the compounds in a variety of contexts, including in the treatment and prevention of diseases characterized by, caused by or associated with the release of chemical mediators via degranulation and other processes effected by activation of the IgE and/or IgG receptor signaling cascades.Type: ApplicationFiled: August 7, 2013Publication date: December 5, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Rajinder Singh, Ankush Argade, Donald G. Payan, Susan Molineaux, Sacha J. Holland, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Catherine Sylvain, Hui Li, Alexander B. Rossi
-
Publication number: 20130317019Abstract: Methods are described for inducing cognition and motor function enhancement in patients suffering from Parkinson's disease by administering an effective amount of an Adenosine 2a antagonist.Type: ApplicationFiled: November 4, 2011Publication date: November 28, 2013Applicant: BIOTIE THERAPIES, INC.Inventors: Stephen I. Bandak, Kevin J. Black, Meghan C. Campbell
-
Publication number: 20130317025Abstract: 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: ApplicationFiled: June 17, 2013Publication date: November 28, 2013Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
-
Publication number: 20130317020Abstract: 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: August 2, 2013Publication date: November 28, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
-
Publication number: 20130310364Abstract: 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: ApplicationFiled: July 16, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
-
Publication number: 20130310340Abstract: A method for treating muscular deterioration is disclosed. Also disclosed are embodiments of a compound, and compositions comprising the compound, for inhibiting muscular deterioriation, including atrophy, dystrophy, and cachexia, such as may result from ventilation.Type: ApplicationFiled: May 15, 2013Publication date: November 21, 2013Applicant: Rigel Pharmaceuticals, Inc.Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
-
Publication number: 20130310375Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.Type: ApplicationFiled: July 22, 2013Publication date: November 21, 2013Applicant: IRM LLCInventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
-
Patent number: 8586579Abstract: The present invention is concerned with novel dual modulators of the 5-HT2A and D3 receptors of formula (I) wherein X, Y, A, R1, R2, and R3 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 comprising them and their use as therapeutics.Type: GrantFiled: June 16, 2011Date of Patent: November 19, 2013Assignee: Hoffmann-La Roche Inc.Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
-
Patent number: 8580968Abstract: Compounds of formula (I) are useful in treating conditions or disorders prevented by or ameliorated by histamine-3 receptor ligands. Also disclosed are pharmaceutical compositions of compounds of formula (I), methods for using such compounds and compositions, and a process for preparing the compounds.Type: GrantFiled: March 1, 2012Date of Patent: November 12, 2013Assignee: AbbVie Inc.Inventors: Lawrence A. Black, Marlon D. Cowart, Gregory A. Gfesser, Brian D. Wakefield, Robert J. Altenbach, Huaqing Liu, Chen Zhao, Gin C. Hsieh
-
Publication number: 20130296317Abstract: Disclosed are compounds of Formula (I): and the pharmaceutically acceptable salts thereof, wherein “A” is S—; —SO—, —SO2—, —O— or NRac—, wherein Rac is H, or C1-20 alkyl and R1 through R5 are defined herein. Also disclosed are pharmaceutical formulations comprising a compound of Formula I and methods of treating, managing, or ameliorating diseases amenable to treatment, management, or amelioration by inhibition of LRRK2 kinase activity, for example, Parkinson's disease.Type: ApplicationFiled: October 25, 2011Publication date: November 7, 2013Inventors: John A. McCauley, Hemaka A. Rajapakse, Thomas J. Greshock, John Sanders, Boyoung Kim, Vanessa L. Rada, Jonathan T. Kern, Heather H. Stevenson, Mark T. Bilodeau
-
Publication number: 20130296306Abstract: 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: ApplicationFiled: June 27, 2013Publication date: November 7, 2013Applicant: VERTEX PHARMACEUTICALS INCORPORATEDInventors: Sara S Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
-
Publication number: 20130281434Abstract: Compounds of formula I?: or salts thereof are provided. Pharmaceutical compositions comprising a compound of formula I?, processes for preparing compounds of formula I?, intermediates useful for preparing compounds of formula I? and therapeutic methods for treating the proliferation of the HIV virus, treating AIDS or delaying the onset of AIDS or ARC symptoms in a mammal are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Applicant: Gilead Sciences, Inc.Inventors: Kerim Babaoglu, Gediminas Brizgys, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
-
Publication number: 20130281447Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis.Type: ApplicationFiled: June 18, 2013Publication date: October 24, 2013Inventors: Stephen S. Palmer, Selvaraj Nataraja
-
Publication number: 20130281433Abstract: Compounds disclosed herein including compounds of formula I?: and salts thereof are provided. Pharmaceutical compositions comprising compounds disclosed herein, processes for preparing compounds disclosed herein, intermediates useful for preparing compounds disclosed herein and therapeutic methods for treating an HIV infection using compounds disclosed herein are also provided.Type: ApplicationFiled: April 19, 2013Publication date: October 24, 2013Inventors: Kerim Babaoglu, Gediminas Brizgys, Jake Cha, Xiaowu Chen, Hongyan Guo, Randall L. Halcomb, Xiaochun Han, Richard Huang, Hongtao Liu, Ryan McFadden, Michael L. Mitchell, Yingmei Qi, Paul A. Roethle, Lianhong Xu, Hong Yang
-
Patent number: 8557811Abstract: Provided are a method for dual-color imaging of sodium/calcium activities using a two-photon fluorescent probe and a method for preparing the two-photon fluorescent probe. The disclosed two-photon fluorescent probe for detecting calcium ions near the cell membrane reacts with calcium cations to exhibit strong two-photon fluorescence and may be selectively and easily loaded into the cell membrane by forming a complex with a calcium ion. Further, it allows imaging of the distribution of calcium cations in a living cell or tissue since it can selectively detect calcium ions in the living cell or tissue at a depth of 100 to 200 ?m for more than 60 minutes. In addition, by staining the living cell or tissue with two probes of different fluorescent colors, the calcium and sodium activities can be imaged simultaneously at different channels.Type: GrantFiled: October 27, 2010Date of Patent: October 15, 2013Assignee: Ajou University Industry—Academic Cooperation FoundationInventors: Hwan Myung Kim, Bong Rae Cho
-
Publication number: 20130267512Abstract: This invention relates to a method of treating and/or preventing endometriosis comprising administering a JNK inhibitor. The JNK inhibitor can also be administered combined with a hormonal suppressor. The invention further relates to the treatment of endometriosis.Type: ApplicationFiled: May 21, 2013Publication date: October 10, 2013Inventors: Stephen S. Palmer, Selvaraj Nataraja
-
Patent number: 8551982Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: GrantFiled: March 13, 2012Date of Patent: October 8, 2013Assignee: Boehringer Ingelheim International GmbHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
-
Publication number: 20130252938Abstract: The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.Type: ApplicationFiled: March 21, 2013Publication date: September 26, 2013Applicant: Biota Europe Ltd.Inventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
-
Publication number: 20130245015Abstract: Compounds having the formula are useful for inhibiting protein tyrosine kinases. The present invention also discloses methods of making the compounds, compositions containing the compounds, and methods of treatment using the compounds.Type: ApplicationFiled: May 3, 2013Publication date: September 19, 2013Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
-
Publication number: 20130244996Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 5, 2013Publication date: September 19, 2013Applicant: Boehringer Ingelheim International GmbHInventors: Asitha ABEYWARDANE, Steven Richard BRUNETTE, Michael J. BURKE, Suresh R. KAPADIA, Thomas Martin KIRRANE, Matthew Russell NETHERTON, Hossein RAZAVI, Sonia RODRIGUEZ, Anjan SAHA, Robert SIBLEY, Lana Louise SMITH-KEENAN, Hidenori TAKAHASHI, Michael Robert TURNER, Jiang-Ping WU, Erick Richard Roush YOUNG, Qiang ZHANG, Qing ZHANG, Renee M. ZINDELL
-
Publication number: 20130245008Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.Type: ApplicationFiled: November 18, 2011Publication date: September 19, 2013Applicant: SANOFIInventor: Alain Pellet
-
Publication number: 20130245010Abstract: 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: April 26, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
-
Publication number: 20130245005Abstract: Compounds of Formula (I): able to inhibit kinase activity, in particular Phosphatidylinositol 3-Kinases activity. The disclosure also relates to the use of compounds of Formula (I) for treatment of pathological conditions associated to alterations in Phosphatidylinositol 3-Kinases activity.Type: ApplicationFiled: November 28, 2011Publication date: September 19, 2013Applicants: UNIVERSITA DEGLI STUDI DEL PIEMONTE ORIENTALE "AMEDEO AVOGADRO", UNIVERSITA DEGLI STUDI DI TORINOInventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
-
Publication number: 20130245011Abstract: 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: May 6, 2013Publication date: September 19, 2013Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
-
Patent number: 8536166Abstract: This application discloses 5-phenyl-1H-pyrazin-2-one derivatives according to generic Formulae I-V: wherein, variables Q, R, Y1, Y2, Y2?, Y3, Y4, n and m are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation such as rheumatoid arthritis. Also disclosed are compositions comprising compounds of Formulae I-V and at least one carrier, diluent or excipient.Type: GrantFiled: July 1, 2009Date of Patent: September 17, 2013Assignee: Roche Palo Alto LLCInventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
-
Publication number: 20130236468Abstract: The present invention relates to a combination comprising compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein, and an additional active agent. The present invention also relates to pharmaceutical compositions comprising these combinations, and methods of using these combinations to treat various diseases and disorders.Type: ApplicationFiled: March 5, 2013Publication date: September 12, 2013Applicant: Boehringer Ingelheim International GmbHInventor: Lars Anders BYLOCK
-
Publication number: 20130225573Abstract: 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: ApplicationFiled: February 7, 2013Publication date: August 29, 2013Applicant: GENZYME CORPORATIONInventor: Genzyme Corporation
-
Publication number: 20130225569Abstract: Compounds of the formula I in which R1 and R2 have the meanings indicated in Claim 1, are inhibitors of Syk, and can be employed, inter alia, for the treatment of rheumatoid arthritis and/or systemic lupusType: ApplicationFiled: July 29, 2011Publication date: August 29, 2013Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNGInventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
-
Publication number: 20130225574Abstract: The present invention relates to oxazolidin-2-one substituted pyrimidine compounds that act as PI3K (phosphatidylinositol-3-kinase) inhibitors, as well as pharmaceutical compositions thereof, methods for their manufacture and uses for the treatment of conditions, diseases and disorders dependent on PI3K.Type: ApplicationFiled: February 22, 2013Publication date: August 29, 2013Applicant: NOVARTIS AGInventor: Novartis AG
-
Patent number: 8518970Abstract: In one aspect, the present invention provides for a compound of Formula I in which in Formula I, the variables X1, X2a, X2b, X2c, R1, B, L, E, A and the subscript n are as defined herein. In another aspect, the present invention provides for pharmaceutical compositions comprising compounds of Formula I as well as methods for using compounds of Formula I for the treatment of diseases and conditions (e.g., cancer, thrombocythemia, etc) characterized by the expression or over-expression of Bcl-2 anti-apoptotic proteins, e.g., of anti-apoptotic Bcl-xL proteins.Type: GrantFiled: January 10, 2012Date of Patent: August 27, 2013Assignees: AbbVie Inc., Genentech, Inc., The Walter and Eliza Hall Institute of Medical ResearchInventors: Jonathan Bayldon Baell, Chinh Thien Bui, Peter Colman, Danette A. Dudley, Wayne J. Fairbrother, John A. Flygare, Guillaume Laurent Lessene, Chudi Ndubaku, George Nikolakopoulos, Carl Steven Rye, Brad Edmund Sleebs, Brian John Smith, Keith Geoffrey Watson, Steven W. Elmore, Andrew M. Petros, Andrew J. Souers, Peter Czabotar
-
Publication number: 20130216552Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein.Type: ApplicationFiled: June 24, 2011Publication date: August 22, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Takashi Nakai, James Jia, Jason Rohde, Regina Graul, Ara Mermerian
-
Publication number: 20130210810Abstract: This disclosure concerns compounds which are useful as inhibitors of protein kinase C (PKC) and are thus useful for treating a variety of diseases and disorders that are mediated or sustained through the activity of PKC. This disclosure 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: December 18, 2012Publication date: August 15, 2013Applicant: RIGEL PHARMACEUTICALS, INC.Inventor: Rigel Pharmaceuticals, Inc.
-
Patent number: 8507483Abstract: The invention relates to the novel products of formula (I): in which Z represents —O—, —NH or Nalk; n represents 0 to 4; R1 represents Hal, hydroxyl, alkyl or alkoxy; the alkyl and alkoxy radicals being optionally substituted; R2 and R3 represent H, Hal or alkyl optionally substituted with one or more halogen atoms; R4 represents H; these products being in all the isomer forms and the salts, as medicaments, in particular as inhibitors of AKT(PKB) phosphorylation.Type: GrantFiled: December 20, 2011Date of Patent: August 13, 2013Assignee: SanofiInventors: Victor Certal, Bruno Filoche-Rommé, Frank Halley, Karl Andreas Karlsson, Fabienne Thompson
-
Publication number: 20130203730Abstract: A compound of formula I or a pharmaceutically acceptable salt thereof in which R1, R2, R3, R4 and m are as described in the specification for use in the treatment of obesity and/or diabetes.Type: ApplicationFiled: March 13, 2013Publication date: August 8, 2013Applicant: AstraZeneca ABInventor: AstraZeneca AB
-
Publication number: 20130196960Abstract: The present disclosure relates to compounds 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 either alone or in combination therapy.Type: ApplicationFiled: February 9, 2011Publication date: August 1, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
-
Publication number: 20130196973Abstract: The present invention relates to compounds of formula (I): wherein R1 to R3, A, X and n are as defined herein. The compounds of formula (I) are useful as inhibitors of leukotriene A4 hydrolase (LTA4H) and treating LTA4H related disorder. The present invention also relates to pharmaceutical compositions comprising the compounds of formula (I), methods of using these compounds in the treatment of various diseases and disorders, and processes for preparing these compounds.Type: ApplicationFiled: March 13, 2012Publication date: August 1, 2013Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBHInventors: Asitha Abeywardane, Michael J. Burke, Thomas Martin Kirrane, Matthew Russell Netherton, Anil Kumar Padyana, Lana Louise Smith Keenan, Hidenori Takahashi, Michael Robert Turner, Qiang Zhang, Qing Zhang
-
Publication number: 20130190271Abstract: Disclosed is a harmful arthropod control composition comprising, as an active ingredient, a fused heterocyclic compound represented by formula (1) [wherein A1 and A2 independently represent a nitrogen atom or the like; R1 and R4 independently represent a halogen atom or the like; R2 and R3 independently represent a halogen atom or the like; R5 and R6 independently represent a linear C1-C6 hydrocarbon group which may be substituted, or the like (provided that both R5 and R6 cannot represent a hydrogen atom simultaneously); and n represents 0 or 1]. The harmful arthropod control composition has an excellent efficacy to control harmful arthropods.Type: ApplicationFiled: March 8, 2013Publication date: July 25, 2013Applicant: SUMITOMO CHEMICAL COMPANY, LIMITEDInventor: Sumitomo Chemical Company, Limited
-
Publication number: 20130178453Abstract: The present disclosure relates to compounds useful as agonists of the 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, either alone or in combination therapy. The compounds of the invention have Formula (I).Type: ApplicationFiled: February 9, 2011Publication date: July 11, 2013Applicant: Ironwood Pharmaceuticals, Inc.Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
-
Publication number: 20130178471Abstract: 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: ApplicationFiled: February 28, 2013Publication date: July 11, 2013Applicant: Vextex Pharmaceuticals IncorporatedInventor: Vertex Pharmaceuticals Incorporated