Abstract: Compounds and compositions comprising compounds that modulate pyruvate kinase M2 (PKM2) are described herein. Also described herein are methods of using the compounds that modulate PKM2 in the treatment of cancer.
Type:
Grant
Filed:
June 29, 2010
Date of Patent:
July 22, 2014
Assignee:
Agios Pharmaceuticals, Inc.
Inventors:
Francesco G. Salituro, Jeffrey O. Saunders, Shunqi Yan
Abstract: A dye, having a structure represented by formula (1A): wherein A represents a group of atoms necessary for forming a ring together with the carbon-nitrogen bond; at least one of Y1A and Y2A represents an acidic group, in which when they each represent an acidic group, they may be the same as or different from each other, or when only one of them represents an acidic group, the other represents an electron-withdrawing group; D represents a group to give a dye; n represents an integer of 1 or greater; L represents a single bond or a divalent linking group; and Y3A represents an acidic group.
Abstract: Compounds of formula (I): wherein: R1 represents a hydrogen atom or an alkyl group; R2 represents an alkyl group; R3 represents an aryl or heteroaryl group. Medicinal products containing the same which are useful in the treatment or prevention of psychiatric and neurological disorders characterized by cognitive deficits.
Type:
Grant
Filed:
March 7, 2012
Date of Patent:
July 15, 2014
Assignees:
Les Laboratoires Servier, Egis Gyogyszergyar Nyrt
Inventors:
István Ling, József Barkóczy, Ferenc Antoni, István Gascályi, György Lévay, Michael Spedding, László Hársing
Abstract: The present invention relates to new compounds of general formula (I), wherein the groups R1 to R3, X1, X2, X3 and L1 are defined as in claim 1, which are suitable for the treatment of diseases characterised by excessive or abnormal cell proliferation, and the use thereof in such a treatment.
Type:
Grant
Filed:
September 28, 2009
Date of Patent:
July 15, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Steffen Steurer, Peter Ettmayer, Andreas Mantoulidis
Abstract: Provided herein are compounds and methods of synthesis thereof. The compounds set forth herein are useful for the treatment, prevention, and/or management of various disorders, such as neurological disorders, neurodegenerative disorders, neuropsychiatric disorders, disorders of cognition, learning or memory, gastrointestinal disorders, lower urinary tract disorder, and cancer. Compounds set forth herein modulate the activity of metabotropic glutamate receptor 5 (mGluR5) in the central nervous system or the periphery. Pharmaceutical formulations containing the compounds and their methods of use are also provided herein.
Type:
Grant
Filed:
December 17, 2010
Date of Patent:
July 8, 2014
Assignee:
Sunovion Pharmaceuticals, Inc.
Inventors:
Larry Wendell Hardy, Michele L. R. Heffernan, Frank Xinhe Wu, Kerry L. Spear, Lakshmi D. Saraswat
Abstract: Compounds of the general structural formula (I) and (II) and use of the compounds and salts and hydrates thereof, as therapeutic agents are disclosed. Treatable diseases and conditions include cancers, inflammatory diseases and conditions, and immunodeficiency diseases.
Type:
Grant
Filed:
October 5, 2009
Date of Patent:
July 1, 2014
Assignee:
Incuron, LLC
Inventors:
John Tucker, Sergey Sviridov, Leonid Brodsky, Catherine Burkhart, Andrei Purmal, Katerina Gurova, Andrei Gudkov
Abstract: This invention provides novel compounds that are modulators of gamma secretase. The compounds have the formula (Chemical formula should be inserted here as it appears on abstract in paper form). Also disclosed are methods of modulating gamma secretase activity and methods of treating Alzheimer's Disease using the compounds of formula (I).
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
June 24, 2014
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Theodros Asberom, Xianhai Huang, Zhaoning Zhu, John W. Clader, Dmitri A. Pissarnitski, Hubert B. Josien, Hongmei Li
Abstract: The present invention relates to pyrroloquinolinyl-pyrrolidine-2,5-dione compounds in combination with chemotherapeutic agents. The present invention provides methods of treating a cell proliferative disorder, such as a cancer, by administering to a subject in need thereof a therapeutically effective amount of a pyrroloquinolinyl-pyrrole-2,5-dione compound or pyrroloquinolinyl-pyrrolidine-2,5-dione compound of the present invention and also administering a effective amount of a chemotherapeutic agent.
Type:
Grant
Filed:
February 7, 2013
Date of Patent:
June 17, 2014
Assignee:
ArQule, Inc.
Inventors:
Chiang J. Li, Mark A. Ashwell, Jason Hill, Magdi M. Moussa, Neru Munshi
Abstract: The present invention relates to 1,4-Oxazepines of formula I having BACE1 and/or BACE2 inhibitory activity, their manufacture, pharmaceutical compositions containing them and their use as therapeutically active substances. The active compounds of the present invention are useful in the therapeutic and/or prophylactic treatment of e.g. Alzheimer's disease and type 2 diabetes.
Type:
Grant
Filed:
March 9, 2012
Date of Patent:
June 10, 2014
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Emanuele Gabellieri, Wolfgang Guba, Hans Hilpert, Harald Mauser, Alexander V. Mayweg, Mark Rogers-Evans, Didier Rombach, Andrew Thomas, Thomas Woltering, Wolfgang Wostl
Abstract: The present invention is directed to novel processes for the preparation of histamine H3 receptor modulators, in the treatment of for example, cognitive disorders, sleep disorders and/or psychiatric disorders.
Type:
Grant
Filed:
March 17, 2010
Date of Patent:
June 10, 2014
Assignee:
Janssen Pharmaceutica NV
Inventors:
Diego Broggini, Vit Lellek, Susanne Lochner, Neelakandha S. Mani, Adrian Maurer, Daniel J. Pippel, Lana K. Young
Abstract: This invention relates generally to prodrugs of noribogaine. This invention also relates to pharmaceutical compositions comprising the prodrugs of noribogaine as well as method of treating pain, addiction and/or stress using such compounds and/or pharmaceutical compositions.
Abstract: The present invention provides a new cyclic compound having a CCR antagonist activity, especially a CCR5 antagonist activity, and the use thereof. The compound of the present invention is represented by the formula: wherein, R1 is a 5- to 6-membered ring group which may be substituted; X1 is a bond or the like; ring A is a 5- to 6-membered ring group which may be substituted; ring B is a 8- to 10-membered ring group which may be substituted; X2 is a bivalent group of 1 to 4 atoms; Z1 is a bivalent cyclic ring group or the like; Z2 is a bond or the like; and R2 is an amino group, a nitrogen-containing heterocyclic group which may be substituted or the like, or a salt thereof.
Abstract: The present invention relates to new substituted prolinamides of general formula (I) wherein D, Y, A, B, R3, R4 and R5 are defined as in the specification, the tautomers, the enantiomers, the diastereomers, the mixtures thereof and the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids or bases, which have valuable properties.
Type:
Grant
Filed:
November 14, 2008
Date of Patent:
June 3, 2014
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Kai Gerlach, Herbert Nar, Henning Priepke, Annette Schuler-Metz, Wolfgang Wienen
Abstract: Described are crystalline forms of the pharmaceutical compound “[9S-(9?,10?,12?)]-5,16-Bis[(ethylthio)methyl]-2,3,9,10,11,12-hexahydro-10-hydroxy-9-methyl-1-oxo-9,12-epoxy-1H-diindolo[1,2,3-fg:3?,2?,1?-kl]pyrrolo[3,4-i][1,6]benzodiazocine-10-carboxylic acid methyl ester”, as well as methods for their use and preparation.
Type:
Grant
Filed:
January 3, 2011
Date of Patent:
May 20, 2014
Assignee:
Cephalon, Inc.
Inventors:
Michael Harold Rock, Heidi Lopez De Diego, Kim Lasse Christensen, Ole Nielsen, Anders Buur, Mark Howells
Abstract: Provided is a compound having a monoamine reuptake inhibitory activity, which is represented by the formula (I) wherein ring A is an optionally substituted 6-membered aromatic ring, ring B is the substituents on ring A are optionally bonded to form, together with ring A, an optionally substituted 9- or 10-membered aromatic fused ring, and other symbols are as defined in the specification, or a salt thereof.
Abstract: The present invention relates to novel heterocyclic compounds as diacylglycerol acyltransferase (“DGAT”) inhibitors, pharmaceutical compositions comprising the heterocyclic compounds and the use of the compounds for treating or preventing a cardiovascular disease, a metabolic disorder, obesity or an obesity-related disorder, diabetes, dyslipidemia, a diabetic complication, impaired glucose tolerance or impaired fasting glucose.
Type:
Grant
Filed:
November 17, 2009
Date of Patent:
May 6, 2014
Assignee:
Merck Sharp & Dohme Corporation
Inventors:
Pauline C. Ting, Robert Aslanian, Mary Ann Caplen, Jianhua Cao, Tin-Yau Chan, David Kim, Hyunjin Kim, Jae-Hun Kim, Rongze Kuang, Joe F. Lee, John Schwerdt, Heping Wu, Nicolas Zorn
Abstract: The present invention generally relates to a series of compounds, to pharmaceutical compositions containing the compounds, and to use of the compounds and compositions as therapeutic agents. More specifically, compounds of the present invention are thiophenyl and pyrrolyl azepine compounds. These compounds are serotonin receptor (5-HT2c) ligands and are useful for treating diseases, disorders, and conditions wherein modulation of the activity of serotonin receptors (5-HT2c) is desired (e.g. addiction, anxiety, depression, obesity, and others).
Type:
Grant
Filed:
January 12, 2011
Date of Patent:
May 6, 2014
Assignee:
Athersys, Inc.
Inventors:
L. Nathan Tumey, David C. Bom, Youssef L. Bennani, Michael J. Robarge
Abstract: The present invention provides compounds of Formula I and salts, hydrates, solvates, complexes, and prodrugs thereof. The present invention further provides methods for synthesizing compounds of Formula I. The invention additionally provides pharmaceutical compositions comprising the compounds of Formula I and methods of using the pharmaceutical compositions of Formula I to treat and prevent disorders and diseases associated with the RyR receptors that regulate calcium channel functioning in cells.
Type:
Grant
Filed:
November 2, 2010
Date of Patent:
April 29, 2014
Assignee:
The Trustees of Columbia University in the City of New York
Inventors:
Andrew Robert Marks, Donald W. Landry, Shixian Deng
Abstract: The invention relates to a new crystalline form II of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of crystalline form II of of N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans. The invention relates to the amorphous forms of N-benzoyl-staurosporine; compositions containing the same; processes for the preparation thereof; and the use of amorphous N-benzoyl-staurosporine in diagnostic methods or therapeutic treatment of warm-blooded animals, especially humans.
Type:
Grant
Filed:
May 15, 2012
Date of Patent:
April 29, 2014
Assignee:
Novartis AG
Inventors:
Pascale Hoehn, Bernd Koch, Michael Mutz