Inventors:
Marion Hitchcock, Anne Mengel, Anja Richter, Hans Briem, Knut Eis, Vera Pütter, Gerhard Siemeister, Stefan Prechtl, Amaury Ernesto Fernández-Montalván, Christian Stegmann, Simon Holton, Mark Jean Gnoth, Cornelia Preuβe
Abstract: Compounds are provided that modulate the glucagon-like peptide 1 (GLP-1) receptor, as well as methods of their synthesis, and methods of their therapeutic and/or prophylactic use. Such compounds can act as modulators or potentiators of GLP-1 receptor on their own, or with incretin peptides such as GLP-1(7-36) and GLP-1(9-36), or with peptide-based therapies, such as exenatide and liraglutide, and have the following general structure (where “” represents either or both the R and S form of the compound): where A, B, C, Y1, Y2, Z, R1, R2, R3, R4, R5, W1, n, p and q are as defined herein.
Type:
Grant
Filed:
June 11, 2014
Date of Patent:
February 16, 2016
Assignee:
Receptos, Inc.
Inventors:
Marcus F. Boehm, Esther Martinborough, Manisha Moorjani, Junko Tamiya, Liming Huang, Adam R. Yeager, Enugurthi Brahmachary, Thomas Fowler, Andrew Novak, Premji Meghani, Michael Knaggs
Abstract: The present invention is related to a substantially pure compound of structural formula (VIII), a process for the purification of a compound of structural formula (VIII) and an improved process of preparing an alcaftadine compound of structural formula (I).
Abstract: The present invention relates generally to compositions and methods for treating cancer and neoplastic disease. Provided herein are substituted heterocyclic derivative compounds and pharmaceutical compositions comprising said compounds. The subject compounds and compositions are useful for inhibition of lysine specific demethylase-1. Furthermore, the subject compounds and compositions are useful for the treatment of cancer.
Type:
Grant
Filed:
April 30, 2015
Date of Patent:
February 9, 2016
Assignee:
QUANTICEL PHARMACEUTICALS, INC.
Inventors:
Young K. Chen, Toufike Kanouni, Stephen W. Kaldor, Jeffrey Alan Stafford, James Marvin Veal
Abstract: Novel compound having the following formula: Also disclosed are a pharmaceutical compositions comprising the same, methods for treating cancer using the same, and methods for the synthesis of the same. The novel compounds of the present invention are found to inhibit protein kinases, especially Checkpoint kinase Chk1/Chk2.
Abstract: The invention encompasses compounds having formula I-V and the compositions and methods using these compounds in the treatment of conditions in which modulation of the JAK pathway or inhibition of JAK kinases, particularly JAK3, may be therapeutically useful.
Type:
Grant
Filed:
June 25, 2014
Date of Patent:
February 2, 2016
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Hui Li, Sambaiah Thota, David Carroll, Ankush Argade, Kin Tso, Arvinder Sran, Jeffrey Clough, Holger Keim, Somasekhar Bhamidipati, Vanessa Taylor, Robin Cooper, Rajinder Singh, Brian Wong
Abstract: A process for making the compound of Formula I utilizes the starting compound, together with sulfilimine and sulfoxide process steps later on.
Type:
Grant
Filed:
May 22, 2013
Date of Patent:
February 2, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Adrian Ortiz, Tamas Benkovics, Zhongping Shi, Prashant P. Deshpande, Zhiwei Guo, David R. Kronenthal, Chris Sfouggatakis
Abstract: A stable amorphous form of dasatinib of Formula (I) wherein amorphous dasatinib after exposure to a relative humidity of 75% at 40 ° C. or 60% at 25 ° C. for a period of at least three months doesn't change to crystalline form and a process for the preparation of the amorphous form of dasatinib of Formula (I).
Abstract: An object of the present invention is to provide a drug containing a compound having Trk-inhibiting activity as an active ingredient in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease. A compound represented by the general formula (I): (wherein all symbols represent the same meanings as described in the specification), a salt thereof, an N-oxide thereof, a solvate thereof or a prodrug thereof is useful as a drug component having Trk-inhibiting activity in prophylaxis and/or therapy of diseases such as pain, pruritus, lower urinary tract dysfunction, asthma, allergic rhinitis, inflammatory bowel disease or Chagas disease.
Abstract: The present invention provides compounds of Formula (I) as described herein, and salts thereof, and therapeutic uses of these compounds for treatment of disorders associated with Raf kinase activity. The invention further provides pharmaceutical compositions comprising these compounds, and compositions comprising these compounds and a therapeutic co-agent.
Type:
Grant
Filed:
March 11, 2014
Date of Patent:
January 26, 2016
Assignee:
Novartis AG
Inventors:
Paul A. Barsanti, Matthew Burger, Yan Lou, Gisele Nishiguchi, Valery Polyakov, Savithri Ramurthy, Alice Rico, Lina Setti, Aaron Smith, Benjamin Taft, Huw Tanner, Alan DiPesa, Naeem Yusuff
Abstract: The present disclosure is directed to methods of using fibroblast growth factor-inducible 14 (Fn14) antagonists to modulate activity at a TNF-like weak inducer of apoptosis (TWEAK) binding site on a cysteine-rich domain (CRD) of Fn14. The present disclosure also provides pharmaceutical compositions comprising synergistic combinations Fn14 antagonists and chemotherapeutic agents.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
January 19, 2016
Assignee:
THE TRANSLATIONAL GENOMICS RESEARCH INSTITUTE
Abstract: This invention relates to a compound of the formula (I): The invention also relates to processes for the preparation of the compound of the formula (I), pharmaceutical agents or compositions containing the compound or a method of using the compound for the treatment of proliferative diseases, such as cancer, as well as the treatment of diseases ameliorated by the control and/or inhibition of lymphangiogenesis.
Type:
Grant
Filed:
August 16, 2013
Date of Patent:
January 19, 2016
Assignee:
CANCER THERAPEUTICS CRC PTY LIMITED
Inventors:
Richard Charles Foitzik, Benjamin Joseph Morrow, Catherine Fae Hemley, Gillian Elizabeth Lunniss, Michelle Ang Camerino, Danny Ganame, Paul Anthony Stupple, Romina Lessene, Wilhelmus Johannes Antonius Kersten, Andrew John Harvey, Ian Peter Holmes
Abstract: The present invention provides thiazole sulfonamide and oxazole sulfonamide compounds, compositions containing the same, as well as processes for the preparation and methods for their use as pharmaceutical agents.
Abstract: Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
Type:
Grant
Filed:
September 5, 2011
Date of Patent:
December 29, 2015
Assignee:
Zhejian Hisun Pharmaceutical Co., Ltd.
Inventors:
Yili Ding, Xuan Yang, Qingyan Yan, Hua Bai, Lifeng Cai, Kenneth Smith, Jian Chai
Abstract: The present invention relates to compounds and methods useful as inhibitors of phosphodiesterase 4 (PDE4) for the treatment or prevention of disease.
Type:
Grant
Filed:
October 24, 2013
Date of Patent:
December 29, 2015
Assignee:
Tetra Discovery Partners, LLC
Inventors:
Mark E. Gurney, Timothy J. Hagen, Xuesheng Mo, A. Samuel Vellekoop, Donna L. Romero, Robert F. Campbell, Joel R. Walker, Lei Zhu
Abstract: This present disclosure is related to the field of 5-fluoro pyrimidines and their derivatives and to the use of these compounds as fungicides.
Type:
Grant
Filed:
September 19, 2013
Date of Patent:
December 8, 2015
Assignee:
Dow AgroSciences LLC
Inventors:
Timothy Boebel, Kristy Bryan, Carla J. R. Klittich, Beth Lorsbach, Timothy P. Martin, Mark A. Pobanz, Michael T. Sullenberger, Jeffery D. Webster, Chenglin Yao, W. John Owen
Abstract: The present invention related to compounds of formula (I) wherein n represents 0, 1, 2, 3, 4 or 5, R represents independent from each other hydroxyl, cyano, nitro, halogen, alkyl, alkoxy alkylcarbonyl, alkoxycarbonyl, alkylamine, dialkylamine, alkylcarbonylamine, alkylcarbamate Y represents one of the following groups: (Ia) in free base or acid addition salt form, to processes for their production, to pharmaceutical compositions comprising them and their use in the manufacture of a medicament for the treatment and/or delay of progression of psychotic and neurodegenerative disorders.
Type:
Grant
Filed:
May 23, 2014
Date of Patent:
December 8, 2015
Assignee:
Novartis AG
Inventors:
Mathias Frederiksen, Dominik Feuerbach, Konstanze Hurth, Manuel Koller, Bernard Lucien Roy
Abstract: The present invention relates to ethynyl derivatives of formula I wherein R1 is hydrogen or halogen; R2 is C1-3-alkyl or —(CH2)n—O—CH3; n is 2 or 3; m is 1 or 2; or to a pharmaceutically acceptable acid addition salt, to a racemic mixture, or to its corresponding enantiomer and/or optical isomer and/or stereoisomer thereof. It has been found that the compounds of general formula I are allosteric modulators of the metabotropic glutamate receptor subtype 5 (mGluR5) with improved properties for the treatment of schizophrenia, cognitive diseases, fragile X syndrome or autism.
Type:
Grant
Filed:
February 13, 2015
Date of Patent:
December 1, 2015
Assignee:
Hoffman-La Roche Inc.
Inventors:
Georg Jaeschke, Lothar Lindemann, Heinz Stadler, Eric Vieira
Abstract: The present invention is directed to substituted triazolyl compounds which are useful as therapeutic agents for the treatment of central nervous system disorders associated with phosphodiesterase 10 (PDE10). The present invention also relates to the use of such compounds for treating neurological and psychiatric disorders, such as schizophrenia, psychosis or Huntington's disease, and those associated with striatal hypofunction or basal ganglia dysfunction.
Type:
Grant
Filed:
October 3, 2012
Date of Patent:
December 1, 2015
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Christopher D. Cox, Vadim Y. Dudkin, June J. Kim, Scott D. Kuduk, Carol A. McVean, Thomas Reger, Justin T. Sheen, Thomas Steele
Abstract: The invention provides novel substituted azaheterocyclic compounds according to Formula (I), their manufacture and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
June 11, 2012
Date of Patent:
December 1, 2015
Assignee:
Merck Patent GmbH
Inventors:
Timo Heinrich, Nadia Brugger, Kristopher Josephson