Abstract: Disclosed are substituted tricyclic benzimidazoles compounds as defined herein in formula (I) or pharmaceutically acceptable salts thereof. The compounds of the invention selectively inhibit CDK8 and are therefore useful for treating diseases related to this kinase, especially colorectal and melanoma cancers and other solid and hemathological malignancies, autoimmune diseases and inflammatory diseases. Also disclosed are processes for preparing these compounds.
Type:
Grant
Filed:
November 7, 2013
Date of Patent:
August 29, 2017
Assignee:
SELVITA SA
Inventors:
Tomasz Rzymski, Adrian Zarebski, Agnieszka Dreas, Karolina Osowska, Katarzyna Kucwaj, Joanna Fogt, Marek Cholody, Michal Galezowski, Wojciech Czardybon, Raymond Horvath, Katarzyna Wiklik, Mariusz Milik, Krzysztof Brzózka
Abstract: Provided herein are curcumin analogues that are able to interact with amyloid ? (A?) and to attenuate the copper-induced crosslinking of A?. Also provided herein are methods of using the compounds in the treatment of Alzheimer's Disease or a related disorder.
Abstract: The problem of the present invention is to provide a production method for safely synthesizing a nitrogen-containing heterocyclic N-oxide compound in high yield. Another problem of the present invention is to provide a novel N-oxide compound. There is provided a method for producing a nitrogen-containing heterocyclic N-oxide compound of Formula (2), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline N-oxide, by oxidizing a nitrogen-containing heterocyclic compound of Formula (1), such as 2,2,7,9-tetramethyl-2H-pyrano[2,3-g]quinoline with a persulfate.
Abstract: The present invention comprises a new class of compounds useful for the modulation of Beta-secretase enzyme activity and for the treatment of Beta-secretase mediated diseases, including Alzheimer's disease (AD) and related conditions. In one embodiment, the compounds have a general Formula I wherein A1, A2, A3, A4, A5, A6, L, R2, R7, X, Y and Z of Formula I are defined herein. The invention also includes use of these compounds in pharmaceutical compositions for treatment, prophylactic or therapeutic, of disorders and conditions related to the activity of beta-secretase protein. Such disorders include, for example, Alzheimer's Disease, cognitive deficits, cognitive impairment, schizophrenia and other central nervous system conditions related to and/or caused by the formation and/or deposition of plaque on the brain. The invention also comprises further embodiments of Formula I, intermediates and processes useful for the preparation of compounds of Formula I.
Type:
Grant
Filed:
November 12, 2013
Date of Patent:
August 8, 2017
Assignee:
Amgen, Inc.
Inventors:
Ryan White, Oleg Epstein, Jason B. Human, Xiao Mei Zheng, Yuan Cheng, Kelvin Sham, Qingyian Liu, Ning Chen
Abstract: The present disclosure provides cyclic sulfonamides of Formula (I), and the pharmaceutically acceptable salts and solvates thereof, wherein R1, R2, R3a, R3b, and n are defined as set forth in the specification. The present disclosure is also directed to the use of compounds of Formula (I) to treat a disorder responsive to the blockade of sodium channels. For example, compounds of the present disclosure are useful for treating pain.
Abstract: The invention relates to a new class of compounds, their pharmaceutically acceptable salts and pharmaceutically acceptable compositions that are effective as selective inhibitors of factor Xa, both in the isolated state and in a complex with other proteins. The compounds of the invention can be used for treating and preventing diseases, such as acute coronary syndrome, myocardial infarction, unstable angina, refractory angina, thromboses caused by post-thrombolytic therapy or coronary angioplasty, acute ischemia mediated cerebrovascular syndrome, embolic stroke, thrombotic stroke, and other diseases in humans and other mammals associated with blood coagulation problems.
Abstract: The present invention relates to a compound represented by formula (I): and pharmaceutically acceptable salts thereof are disclosed as useful for treating or preventing diabetes, hyperlipidemia, obesity, inflammation related disorders, and related diseases and conditions. The compounds are useful as agonists of the G-protein coupled receptor GPR120. Pharmaceutical compositions and methods of treatment are also included.
Type:
Grant
Filed:
October 11, 2013
Date of Patent:
July 18, 2017
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Mariappan Chelliah, Hong Dong Chu, Jason M. Cox, John S. Debenham, Keith Eagen, Ping Lan, Clare London, Michael A. Plotkin, Unmesh Shah, Christopher Joseph Sinz, Zhongxiang Sun, Henry M. Vaccaro, Srikanth Venkatraman
Abstract: The present disclosure is generally directed to compounds which can inhibit AAK1 (adaptor associated kinase 1), compositions comprising such compounds, and methods for inhibiting AAK1.
Type:
Grant
Filed:
February 6, 2014
Date of Patent:
July 18, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Vivekananda M. Vrudhula, Carolyn Diane Dzierba, Joanne J. Bronson, John E. Macor, Susheel Jethanand Nara, Ramkumar Rajamani, Maheswaran Sivasamban Karatholuvhu
Abstract: A compound according to Formula (Ia), wherein Cy, L1, G, and R1 are as described herein. The present invention relates to novel compounds according to Formula (I) that antagonize GPR84, a G-protein-coupled receptor that is involved in inflammatory conditions, and methods for the production of these novel compounds, pharmaceutical compositions comprising these compounds, and methods for the prevention and/or treatment of inflammatory conditions (for example inflammatory bowel diseases (IBD), rheumatoid arthritis, vasculitis), lung diseases (e.g. chronic obstructive pulmonary disease (COPD) and lung interstitial diseases (e.g. idiopathic pulmonary fibrosis (IPF))), neuroinflammatory conditions, infectious diseases, autoimmune diseases, endocrine and/or metabolic diseases, and/or diseases involving impairment of immune cell functions by administering a compound of the invention.
Type:
Grant
Filed:
December 17, 2013
Date of Patent:
July 18, 2017
Assignee:
GALAPAGOS NV
Inventors:
Frédéric Gilbert Labéguère, Gregory John Robert Newsome, Luke Jonathan Alvey, Laurent Raymond Maurice Sanière, Stephen Robert Fletcher
Abstract: The present invention relates to crystalline forms of pyrroloquinoline quinone disodium salt. The present invention provides crystalline Form A and crystalline Form B of pyrroloquinoline quinone disodium salt, and the methods and uses for the preparation thereof. The X-ray powder diffraction patterns of crystalline Form A and crystalline Form B are as shown by FIG. 1 and FIG. 5, respectively. The crystalline forms of the present invention have low moisture absorption and high stability, as well as excellent use and storage performances.
Abstract: The present invention relates to the pharmaceutical field, in particular to a phenanthridine derivative as shown in general formula (1) a pharmaceutical composition comprising the derivative, its preparation method, and its uses in manufacture of a medicament for the prevention or treatment of a disease related to the activity of Wnt signaling pathway, hepatitis C and hepatitis B.
Type:
Grant
Filed:
February 28, 2014
Date of Patent:
June 20, 2017
Assignees:
Kunming Institute of Botany, The Chinese Academy of Sciences, Shanghai Institutes for Biological Sciences, CAS, Institute of Medicinal Biotechnology, Chinese Academy of Medical Sciences
Inventors:
Xiaojiang Hao, Duozhi Chen, Lin Li, Zonggen Peng, Jiandong Jiang, Yingtong Di, Junlin Yin, Sheng Wang, Jieyun Cai
Abstract: The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds modulate the mGluR2 receptor and may be useful for the treatment of various disorders of the central nervous system.
Type:
Grant
Filed:
June 19, 2013
Date of Patent:
June 20, 2017
Assignee:
Bristol-Myers Squibb Company
Inventors:
Ronald J. Mattson, Zhaoxing Meng, Leatte R. Guernon
Abstract: Compounds of Formula (I), including pharmaceutically acceptable salts thereof: wherein A is selected from the group consisting of: and wherein Z is: are useful as HIV attachment inhibitors.
Type:
Grant
Filed:
August 7, 2013
Date of Patent:
May 23, 2017
Assignee:
ViiV Healthcare UK (No.5) Limited
Inventors:
Tao Wang, John F. Kadow, Nicholas A. Meanwell, Zhongxing Zhang, Zhiwei Yin, Edward H. Ruediger, Clint A. James, Daniel H. Deon
Abstract: A 1,9-diazaphenalene derivative is represented by where R, R1, R2, R3, Y1, and Y2 are as defined in the specification and claims. The 1,9-diazaphenalene derivative may emit fluorescence after being excited, and is thus suitable for use as a fluorescent material for an organic light emitting diode. A method for preparing the 1,9-diazaphenalene derivative is also disclosed.
Abstract: The present invention relates to compounds of formula I: in which n, R1, R2, R3a, R4 and R5 are defined in the Summary of the Invention; capable of inhibiting the activity of MEK. The invention further provides a process for the preparation of compounds of the invention, pharmaceutical preparations comprising such compounds and methods of using such compounds and compositions in the management of hyperproliferative diseases like cancer.
Type:
Grant
Filed:
November 13, 2015
Date of Patent:
April 25, 2017
Assignee:
NOVARTIS AG
Inventors:
Mark Gary Bock, Henrik Moebitz, Sunil Kumar Panigrahi, Ramulu Poddutoori, Susanta Samajdar
Abstract: A method for treating a neoplasm in a subject, comprising co-administering to the subject a therapeutically effective amount of an anticancer agent and a substituted 6,7-methylenedioxy-4-amino-quinoline, or a pharmaceutically acceptable salt or ester thereof.
Type:
Grant
Filed:
January 29, 2013
Date of Patent:
April 18, 2017
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Barry I. Gold, Xiangqun Xie, Ajay Srinivasan, LiRong Wang
Abstract: The invention concerns compounds of Formula (I) or pharmaceutically-acceptable salts thereof, wherein R1 to R5 have any of the meanings defined hereinbefore in the description; processes for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
April 11, 2017
Assignee:
AstraZeneca AB
Inventors:
Robert Hugh Bradbury, David Buttar, Christopher De Savi, Craig Samuel Donald, Richard Albert Norman, Alfred Arthur Rabow, Gordon Stuart Currie, Heather Redfearn, Nadim Akhtar, Helen Elizabeth Williams, Matthew Osborne, Neda Yavari
Abstract: The invention provides tricyclic compounds and their use in treating medical disorders, such as obesity. Pharmaceutical compositions and methods of making various tricyclic compounds are provided. The compounds are contemplated to have activity against methionyl aminopeptidase 2.
Type:
Grant
Filed:
February 3, 2016
Date of Patent:
April 11, 2017
Assignee:
Zafgen, Inc.
Inventors:
Susan M. Cramp, Hazel J. Dyke, Thomas D. Pallin, Robert Zahler