Abstract: The present invention relates to crystal modifications of N-{(2R)-2-[({[3,3-dibutyl-7-(methyl-thio)-1,1-dioxido-5-phenyl-2,3,4,5-tetrahydro-1,5-benzothiazepin-8-yl]oxy}acetyl)amino]-2-phenylethanolyl}glycine (elobixibat), more specifically crystal modifications I, IV, MeOH-1, EtOH-1, 1-PrOH-1 and 2-PrOH-1. The invention also relates to a process for the preparation of these crystal modifications and to a pharmaceutical composition comprising crystal modification IV.
Type:
Grant
Filed:
October 22, 2015
Date of Patent:
August 9, 2016
Assignee:
Elobix AB
Inventors:
Martin Bohlin, Erica Tjerneld, Andreas Vestermark, Ingvar Ymen
Abstract: Myeloperoxidase inhibitors, pharmaceutical compositions containing such inhibitors and the use of such inhibitors to treat, for example, cardiovascular conditions.
Type:
Grant
Filed:
June 9, 2014
Date of Patent:
July 26, 2016
Assignee:
Pfizer Inc.
Inventors:
Philip A. Carpino, Edward L. Conn, Robert L. Dow, Matthew S. Dowling, David Hepworth, Daniel Wei-Shung Kung, Suvi Orr, Benjamin N. Rocke, Roger B. Ruggeri, Matthew F. Sammons, Joseph S. Warmus, Yan Zhang
Abstract: The present invention provides compounds of Formula (I): (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:
Grant
Filed:
April 1, 2013
Date of Patent:
July 19, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Carol Hui Hu, Jennifer X. Qiao, Tammy C. Wang
Abstract: Provided herein are novel compounds and pharmaceutically acceptable salts thereof that are liver X receptor modulators. Also provided are compositions comprising compounds of the invention and a carrier. Additionally, use of the compounds herein and methods for treating a disease or disorder associated with the liver X receptor are further described.
Type:
Grant
Filed:
March 13, 2015
Date of Patent:
July 12, 2016
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
Chengguo Dong, Yi Fan, Katerina Leftheris, Stephen D. Lotesta, Suresh B. Singh, Colin M. Tice, Wei Zhao, Yajun Zheng, Linghang Zhuang
Abstract: The present invention relates to novel acylaminocycloalkyl compounds, in particular to the compounds of the formula I as described herein and to their salts and N-oxides. The compounds possess valuable therapeutic properties and are suitable, in particular, for treating diseases that respond to modulation of the dopamine D3 receptor.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
July 12, 2016
Assignees:
AbbVie Inc., AbbVie Deutschland GmbH & Co. KG
Inventors:
Andreas Haupt, Jürgen Dinges, Liliane Unger, Karsten Wicke, Robert Van Waterschoot, Karla Drescher, Ana Relo
Abstract: Disclosed herein are, inter alia, compositions for modulating Ire1, Src, or Abl, methods for identifying modulating activity in test compounds, and methods for treating diseases caused by the activity or inactivity of Ire1, Src, or Abl.
Type:
Grant
Filed:
July 2, 2014
Date of Patent:
July 5, 2016
Assignee:
The Regents of the University of California
Inventors:
Peter Walter, Alexei Korennykh, Kevan M. Shokat, Chao Zhang, Janet Finer-Moore, Robert Stroud, Pascal Egea, Andrei Korostelev, Arvin Dar, Sebastian Bernales
Abstract: Compounds of Formula I and Formula IA are inhibitors of dihydrofolate reductase and are suitable for use in compositions and methods for dihydrofolate reductase inhibition or, more specifically, treatment of a fungal infection, a bacterial infection or a protozoal infection, and, in specific embodiments, treatment of a fungal infection caused by C. albicans or C. glabrata: wherein R, R1, R2, R3, R4, A, B, E, V, W, X, Y and Z are as defined herein.
Type:
Grant
Filed:
February 12, 2015
Date of Patent:
July 5, 2016
Assignees:
PROMILIAD BIOPHARMA INC., UNIVERSITY OF CONNECTICUT
Inventors:
Dennis L Wright, Amy C Anderson, Grant Sormunen
Abstract: Compounds of formula (I) i.e. monocyclic or bicyclic diamine-substituted thieno[2,3-d]pyrimidine and isothiazolo[5,4-d]pyrimidine derivatives substituted by an optionally substituted oxazolin-2-yl moiety, are beneficial in the treatment and/or prevention of various human ailments, including inflammatory, autoimmune and oncological disorders; viral diseases; and organ and cell transplant rejection.
Type:
Grant
Filed:
October 2, 2013
Date of Patent:
July 5, 2016
Assignee:
UCB Biopharma SPRL
Inventors:
Claire Louise Kulisa, Daniel Christopher Brookings, Daniel James Ford, Richard Jeremy Franklin, James Thomas Reuberson, Anant Ramrao Ghawalkar
Abstract: The invention relates to spiro derivatives, to the use of said derivatives intreating diseases and conditions mediated by modulation of voltage-gated sodium channels, to compositions containing said derivatives and processes for their preparation.
Type:
Grant
Filed:
May 22, 2013
Date of Patent:
June 28, 2016
Assignee:
Convergence Pharmaceuticals Limited
Inventors:
Gerard M. P. Giblin, David T. MacPherson, David R. Witty, Steven J. Stanway
Abstract: The invention provides certain substituted pyridines of the Formula (I) or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, Rcy, Cy, and t are as defined herein. The invention also provides pharmaceutical compositions comprising such compounds, and methods of using the compounds for treating diseases or conditions mediated by Spleen Tyrosine Kinase (Syk) kinase.
Type:
Grant
Filed:
June 17, 2013
Date of Patent:
June 28, 2016
Assignees:
Merck Sharp & Dohme Corp., Merck Canada Inc.
Inventors:
Andrew M. Haidle, Sandra Lee Knowles, Solomon D. Kattar, Denis Deschenes, Jason Burch, Joel Robichaud, Matthew Christopher, Michael D. Altman, James P. Jewell, Alan B. Northrup, Marc Blouin, John Michael Ellis, Hua Zhou, Christian Fischer, Adam J. Schell, Michael H. Reutershan, Brandon M. Taoka, Anthony Donofrio
Abstract: The present invention relates to compounds of formula (I) having a bicyclic aza-amides scaffold, pharmaceutically acceptable salts of these compounds and pharmaceutical compositions containing at least one of these compounds together with pharmaceutically acceptable carrier, excipient and/or diluents. Said bicyclic aza-amides compounds can be used for prophylaxis and/or treatment of psychiatric disorders and neurodegenerative diseases, disorders and conditions.
Type:
Grant
Filed:
July 24, 2013
Date of Patent:
June 21, 2016
Assignee:
Max-Planck-Gesellschaft zur Förderung der Wissenschaften e.V.
Abstract: A process for the manufacture of the calcium salt of (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl](3R,5S)-3,5-dihydroxyhept-6-enoic acid, useful as an HMGCoA reductase inhibitor, from a compound of the formula (7) wherein A is an acetal or ketal protecting group and R is alkyl, via isolated crystalline compounds of the formula (8) or of formula (10) is described. Crystalline intermediates of formulae 7, 8 and 10 are also described.
Type:
Grant
Filed:
July 19, 2011
Date of Patent:
June 21, 2016
Assignees:
AstraZeneca UK Limited, Shionogi & Company Limited
Inventors:
Tetsuo Okada, John Horbury, David Dermot Patrick Laffan
Abstract: Disclosed are compounds of Formula 1, and pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, and R10 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating immunological disorders, cardiovascular disease, cancer, and other diseases, disorders or conditions associated with PI3K?.
Type:
Grant
Filed:
January 8, 2015
Date of Patent:
June 21, 2016
Assignee:
AstraZeneca AB
Inventors:
Edcon Chang, Christopher Smith, Xiaolun Wang, Michael B. Wallace
Abstract: Benzoimidazol-2-yl pyrimidines and pyrazines, pharmaceutical compositions and methods for the treatment of disease states, disorders, and conditions mediated by H4 receptor activity, including allergy, asthma, autoimmune diseases, and pruritis.
Type:
Grant
Filed:
January 28, 2015
Date of Patent:
June 14, 2016
Assignee:
Janssen Pharmaceutica NV
Inventors:
James P. Edwards, David E. Kindrachuk, Christopher M. Mapes, Daniel J. Pippel, Jennifer D. Venable
Abstract: The present disclosure provides pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3, R4, R5, X and Y are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
Type:
Grant
Filed:
January 7, 2014
Date of Patent:
June 14, 2016
Assignee:
CONFLUENCE LIFE SCIENCES INC.
Inventors:
Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas
Abstract: Disclosed are bicyclic group substituted pyrimidine compounds, pharmaceutical acceptable salts thereof or stereoisomers thereof. Also disclosed are preparation methods, pharmaceutical formulations, and pharmaceutical compositions of the compounds, and use of the compounds, pharmaceutical formulations, and pharmaceutical compositions for preparing a medicament for treating and/or preventing sexual dysfunction diseases and diseases with lower urinary tract symptoms.
Abstract: The invention relates to compounds of the general formula (I), wherein the variable have the meanings as indicated in the claims, or a physiologically acceptable salt thereof. The active ingredients have advantageous pesticidal properties. They are especially suitable for controlling endoparasites in warm-blooded animals.
Abstract: Provided are cyclopropanecarboxamido-substituted aromatic compounds that inhibit protein kinases and their use in anti-tumor area. In particular, tyrosine-kinase inhibitors and Raf-kinase inhibitors as anti-tumor agents, their preparation, pharmaceutical composition, and their use in the treatment of cancer are also provided.
Type:
Grant
Filed:
June 24, 2013
Date of Patent:
June 7, 2016
Assignee:
CROWN BIOSCIENCE INC. (Taiwan)
Inventors:
Deyi Zhang, Ruihao Zhang, Boyu Zhong, Chuan Shih
Abstract: The present disclosure provides methyl/difluorophenyl-methoxy substituted pyridinone-pyridinyl compounds, methyl-pyridinyl-methoxy substituted pyridinone-pyridinyl compounds, and methyl-pyrimidinyl-methoxy substituted pyridinone-pyridinyl compounds useful in the treatment of p38 kinase mediated diseases, such as lymphoma and auto-inflammatory disease, having the structure of Formula (I): wherein R1, R2, R3 and X are as defined in the detailed description; pharmaceutical compositions comprising at least one of the compounds; and methods for treating p38 kinase mediated diseases using the compound.
Type:
Grant
Filed:
June 7, 2013
Date of Patent:
June 7, 2016
Assignee:
CONFLUENCE LIFE SCIENCES, INC.
Inventors:
Shaun R. Selness, Joseph B. Monahan, John F. Schindler, Balekudru Devadas, Susan L. Hockerman
Abstract: The present invention is directed to substituted cyclopropyl imidazopyridine 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:
November 11, 2013
Date of Patent:
June 7, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Scott D. Kuduk, Douglas C. Beshore, Thomas S. Reger