Plural Ring Hetero Atoms In The Bicyclo Ring System Patents (Class 514/233.8)
  • Publication number: 20140057906
    Abstract: 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: Application
    Filed: October 21, 2013
    Publication date: February 27, 2014
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: 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: 20140045811
    Abstract: 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: Application
    Filed: July 18, 2013
    Publication date: February 13, 2014
    Inventors: 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: 20140045829
    Abstract: 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: Application
    Filed: October 8, 2013
    Publication date: February 13, 2014
    Applicant: Merck Sharp & Dohme Corp.
    Inventors: MARK E. LAYTON, Michael J. Kelly
  • Patent number: 8637508
    Abstract: 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: Grant
    Filed: January 11, 2012
    Date of Patent: January 28, 2014
    Assignee: Novartis AG
    Inventors: 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: 20140011799
    Abstract: 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: Application
    Filed: July 8, 2013
    Publication date: January 9, 2014
    Inventors: James A. Johnson, Ji Jiang, Soong-Hoon Kim, Zulan Pi, Jennifer X. Qiao, George O. Tora, Tammy C. Wang, Heather Finlay
  • Publication number: 20140005190
    Abstract: 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: Application
    Filed: June 27, 2013
    Publication date: January 2, 2014
    Applicants: 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: 20130345195
    Abstract: 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: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: 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: 20130345213
    Abstract: 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: Application
    Filed: March 9, 2012
    Publication date: December 26, 2013
    Applicant: LUPIN LIMITED
    Inventors: 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: 20130345193
    Abstract: 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: Application
    Filed: August 23, 2013
    Publication date: December 26, 2013
    Applicant: CALCIMEDICA, INC.
    Inventors: Jeffrey P. WHITTEN, Yazhong Pei, Jianguo Cao, Zhijun Wang, Evan Rogers, Brian Dyck, Jonathan Grey
  • Patent number: 8609655
    Abstract: 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: Grant
    Filed: March 27, 2009
    Date of Patent: December 17, 2013
    Assignee: Amgen Inc.
    Inventors: John Peter Geibel, David Martin, Gordon Ng, William G. Richards, Joanne L. Viney, Patricia R. Hebert
  • Publication number: 20130331390
    Abstract: 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: Application
    Filed: October 13, 2011
    Publication date: December 12, 2013
    Applicants: Kunming Institute of Botany, The Chinese Academy of Sciences, Kunming Institute of Zoology, The Chinese Academy of Sciences, Yunnan University
    Inventors: Jingping Liu, Handong Sun, Hongbin Zhang, Yongtong Zheng, Weilie Xiao, Jianxin Pu, Ruirui Wang, Liumeng Yang
  • Publication number: 20130324524
    Abstract: 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: Application
    Filed: August 7, 2013
    Publication date: December 5, 2013
    Applicant: 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: 20130317019
    Abstract: 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: Application
    Filed: November 4, 2011
    Publication date: November 28, 2013
    Applicant: BIOTIE THERAPIES, INC.
    Inventors: Stephen I. Bandak, Kevin J. Black, Meghan C. Campbell
  • Publication number: 20130317025
    Abstract: 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: Application
    Filed: June 17, 2013
    Publication date: November 28, 2013
    Inventors: Amy RIPKA, Gideon SHAPIRO, Richard CHESWORTH
  • Publication number: 20130317020
    Abstract: 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: Application
    Filed: August 2, 2013
    Publication date: November 28, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara Hadida Ruah, Mark Miller, Jinglan Zhou, Brian Bear, Peter Grootenhuis
  • Publication number: 20130310364
    Abstract: 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: Application
    Filed: July 16, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Hui Li, Thilo Heckrodt, Yan Chen, Vanessa Taylor, Rajinder Singh, Pingyu Ding, Rose Yen
  • Publication number: 20130310340
    Abstract: 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: Application
    Filed: May 15, 2013
    Publication date: November 21, 2013
    Applicant: Rigel Pharmaceuticals, Inc.
    Inventors: Donald G. Payan, Esteban Masuda, Todd Kinsella
  • Publication number: 20130310375
    Abstract: The present invention relates to compositions and methods for modulating the Wnt signaling pathway.
    Type: Application
    Filed: July 22, 2013
    Publication date: November 21, 2013
    Applicant: IRM LLC
    Inventors: Dai Cheng, Guobao Zhang, Dong Han, Wenqi Gao, Shifeng Pan
  • Patent number: 8586579
    Abstract: 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: Grant
    Filed: June 16, 2011
    Date of Patent: November 19, 2013
    Assignee: Hoffmann-La Roche Inc.
    Inventors: Luca Gobbi, Rosa Maria Rodriguez Sarmiento, Juergen Wichmann
  • Patent number: 8580968
    Abstract: 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: Grant
    Filed: March 1, 2012
    Date of Patent: November 12, 2013
    Assignee: 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: 20130296317
    Abstract: 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: Application
    Filed: October 25, 2011
    Publication date: November 7, 2013
    Inventors: 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: 20130296306
    Abstract: 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: Application
    Filed: June 27, 2013
    Publication date: November 7, 2013
    Applicant: VERTEX PHARMACEUTICALS INCORPORATED
    Inventors: Sara S Hadida Ruah, Mark T. Miller, Brian Bear, Jason McCartney, Peter D.J. Grootenhuis
  • Publication number: 20130281434
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Applicant: 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: 20130281447
    Abstract: 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: Application
    Filed: June 18, 2013
    Publication date: October 24, 2013
    Inventors: Stephen S. Palmer, Selvaraj Nataraja
  • Publication number: 20130281433
    Abstract: 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: Application
    Filed: April 19, 2013
    Publication date: October 24, 2013
    Inventors: 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: 8557811
    Abstract: 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: Grant
    Filed: October 27, 2010
    Date of Patent: October 15, 2013
    Assignee: Ajou University Industry—Academic Cooperation Foundation
    Inventors: Hwan Myung Kim, Bong Rae Cho
  • Publication number: 20130267512
    Abstract: 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: Application
    Filed: May 21, 2013
    Publication date: October 10, 2013
    Inventors: Stephen S. Palmer, Selvaraj Nataraja
  • Patent number: 8551982
    Abstract: 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: Grant
    Filed: March 13, 2012
    Date of Patent: October 8, 2013
    Assignee: Boehringer Ingelheim International GmbH
    Inventors: 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: 20130252938
    Abstract: 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: Application
    Filed: March 21, 2013
    Publication date: September 26, 2013
    Applicant: Biota Europe Ltd.
    Inventors: Christopher James Lunniss, James T. Palmer, Gary Robert William Pitt, David Davies, Lorraine Claire Axford
  • Publication number: 20130245015
    Abstract: 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: Application
    Filed: May 3, 2013
    Publication date: September 19, 2013
    Inventors: YUJIA DAI, STEVEN K. DAVIDSEN, ANNA M. ERICSSON, KRESNA HARTANDI, ZHIQIN JI, MICHAEL R. MICHAELIDES
  • Publication number: 20130244996
    Abstract: 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: Application
    Filed: March 5, 2013
    Publication date: September 19, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventors: 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: 20130245008
    Abstract: The invention relates to the nitrobenzothiazole derivatives of general formula (I): and to the use thereof for treating tuberculosis.
    Type: Application
    Filed: November 18, 2011
    Publication date: September 19, 2013
    Applicant: SANOFI
    Inventor: Alain Pellet
  • Publication number: 20130245010
    Abstract: 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: Application
    Filed: April 26, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Publication number: 20130245005
    Abstract: 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: Application
    Filed: November 28, 2011
    Publication date: September 19, 2013
    Applicants: UNIVERSITA DEGLI STUDI DEL PIEMONTE ORIENTALE "AMEDEO AVOGADRO", UNIVERSITA DEGLI STUDI DI TORINO
    Inventors: Giovanni Sorba, Gian Cesare Tron, Ubaldina Galli, Alberto Massarotti, Emilio Hirsch, Elisa Ciraolo, Tracey Pirali
  • Publication number: 20130245011
    Abstract: 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: Application
    Filed: May 6, 2013
    Publication date: September 19, 2013
    Inventors: Sara S. Hadida Ruah, Matthew Hamilton, Mark Miller, Peter D.J. Grootenhuis, Brian Bear, Jason McCartney, Jinglan Zhou
  • Patent number: 8536166
    Abstract: 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: Grant
    Filed: July 1, 2009
    Date of Patent: September 17, 2013
    Assignee: Roche Palo Alto LLC
    Inventors: Nolan James Dewdney, Yan Lou, Eric Brian Sjogren, Michael Soth, Zachary Kevin Sweeney
  • Publication number: 20130236468
    Abstract: 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: Application
    Filed: March 5, 2013
    Publication date: September 12, 2013
    Applicant: Boehringer Ingelheim International GmbH
    Inventor: Lars Anders BYLOCK
  • Publication number: 20130225573
    Abstract: 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: Application
    Filed: February 7, 2013
    Publication date: August 29, 2013
    Applicant: GENZYME CORPORATION
    Inventor: Genzyme Corporation
  • Publication number: 20130225569
    Abstract: 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 lupus
    Type: Application
    Filed: July 29, 2011
    Publication date: August 29, 2013
    Applicant: MERCK PATENT GESELLSCHAFT MIT BESCHRANKTER HAFTUNG
    Inventors: Lars Burgdorf, Melanie Schultz, Tatjana Ross, Brian Hodous, Justin Potnick, Amanda E. Sutton, Bayard R. Huck
  • Publication number: 20130225574
    Abstract: 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: Application
    Filed: February 22, 2013
    Publication date: August 29, 2013
    Applicant: NOVARTIS AG
    Inventor: Novartis AG
  • Patent number: 8518970
    Abstract: 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: Grant
    Filed: January 10, 2012
    Date of Patent: August 27, 2013
    Assignees: AbbVie Inc., Genentech, Inc., The Walter and Eliza Hall Institute of Medical Research
    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: 20130216552
    Abstract: Modulators of CRTH2, particularly antagonists of CRTH2, that are useful for treating various disorders, including asthma and respiratory disorders are disclosed herein.
    Type: Application
    Filed: June 24, 2011
    Publication date: August 22, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Takashi Nakai, James Jia, Jason Rohde, Regina Graul, Ara Mermerian
  • Publication number: 20130210810
    Abstract: 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: Application
    Filed: December 18, 2012
    Publication date: August 15, 2013
    Applicant: RIGEL PHARMACEUTICALS, INC.
    Inventor: Rigel Pharmaceuticals, Inc.
  • Patent number: 8507483
    Abstract: 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: Grant
    Filed: December 20, 2011
    Date of Patent: August 13, 2013
    Assignee: Sanofi
    Inventors: Victor Certal, Bruno Filoche-Rommé, Frank Halley, Karl Andreas Karlsson, Fabienne Thompson
  • Publication number: 20130203730
    Abstract: 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: Application
    Filed: March 13, 2013
    Publication date: August 8, 2013
    Applicant: AstraZeneca AB
    Inventor: AstraZeneca AB
  • Publication number: 20130196960
    Abstract: 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: Application
    Filed: February 9, 2011
    Publication date: August 1, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Jason Rohde, Charles Kim, Takashi Nakai, Galen John Carey
  • Publication number: 20130196973
    Abstract: 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: Application
    Filed: March 13, 2012
    Publication date: August 1, 2013
    Applicant: BOEHRINGER INGELHEIM INTERNATIONAL GMBH
    Inventors: 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: 20130190271
    Abstract: 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: Application
    Filed: March 8, 2013
    Publication date: July 25, 2013
    Applicant: SUMITOMO CHEMICAL COMPANY, LIMITED
    Inventor: Sumitomo Chemical Company, Limited
  • Publication number: 20130178453
    Abstract: 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: Application
    Filed: February 9, 2011
    Publication date: July 11, 2013
    Applicant: Ironwood Pharmaceuticals, Inc.
    Inventors: Jason Rohde, Bo Peng, Takashi Nakai, Kevin Sprott, Ara Mermerían, Wayne C. Schairer, Galen John Carey
  • Publication number: 20130178471
    Abstract: 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: Application
    Filed: February 28, 2013
    Publication date: July 11, 2013
    Applicant: Vextex Pharmaceuticals Incorporated
    Inventor: Vertex Pharmaceuticals Incorporated