Abstract: The present invention is directed to compounds of formula I and pharmaceutically acceptable salts, esters, and prodrugs thereof which are inhibitors of Syk kinase. The present invention is also directed to intermediates used in making such compounds, the preparation of such a compound, pharmaceutical compositions containing such a compound, methods of inhibition Syk kinase activity, methods of inhibition the platelet aggregation, and methods to prevent or treat a number of conditions mediated at least in part by Syk kinase activity, such as Non Hodgkin's Lymphoma.
Type:
Grant
Filed:
May 10, 2016
Date of Patent:
February 27, 2018
Assignee:
PORTOLA PHARMACEUTICALS, INC.
Inventors:
Zhaozhong J. Jia, Yonghong Song, Qing Xu, Brian Kane, Shawn M. Bauer, Anjali Pandey
Abstract: Described herein are compounds that are somatostatin modulators, methods of making such compounds, pharmaceutical compositions and medicaments comprising such compounds, and methods of using such compounds in the treatment of conditions, diseases, or disorders that would benefit from modulation of somatostatin activity.
Type:
Grant
Filed:
July 12, 2017
Date of Patent:
February 20, 2018
Assignee:
CRINETICS PHARMACEUTICALS, INC.
Inventors:
Jian Zhao, Sangdon Han, Sun Hee Kim, Shimiao Wang, Yunfei Zhu
Abstract: The present disclosure describes bicyclic aromatic carboxamide derivatives, as well as their compositions and methods of use. The compounds inhibit the activity of the Pim kinases, and are useful in the treatment of diseases related to the activity of Pim kinases including, e.g., cancer and other diseases.
Type:
Grant
Filed:
January 13, 2017
Date of Patent:
February 13, 2018
Assignee:
Incyte Corporation
Inventors:
Yaping Sun, Hao Feng, Yun-Long Li, Song Mei, Jun Pan, Anlai Wang, Hai-Fen Ye, Ke Zhang
Abstract: The present invention relates to a compound represented by formula I: and pharmaceutically acceptable salts thereof. The compounds of formula I are inhibitors of diacylglyceride O-acyltransferase 2 (“DGAT2”) and may be useful in the treatment, prevention and suppression of diseases mediated by DGAT2. The compounds of the present invention may be useful in the treatment of hepatic steatosis, diabetes mellitus, obesity, hyperlipidemia, hypercholesterolemia, atherosclerosis, cardio renal diseases such as chronic kidney diseases and heart failure and related diseases and conditions.
Type:
Grant
Filed:
August 31, 2015
Date of Patent:
January 30, 2018
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Jason Imbriglio, Clare London, Zhijian Lu, James Tata, Yusheng Xiong, Ming You, Hyewon Youm
Abstract: A crystalline form of a drug, ways to make it, compositions containing it and methods of treatment of diseases and inhibition of adverse physiological events using it are disclosed.
Type:
Grant
Filed:
November 23, 2016
Date of Patent:
January 23, 2018
Assignee:
ABBVIE INC.
Inventors:
Geoff G. Z. Zhang, Michael F. Bradley, David M. Barnes, Rodger Henry
Abstract: Provided herein are novel compounds, pharmaceutical compositions for use, inter alia, in methods of reducing Wnt-mediated effects and treating cancer.
Abstract: Provided are a novel metal catalyst for preparing cyclic carbonate, and a method for preparing cyclic carbonate using the same, and more particularly, a method for selectively preparing cyclic carbonate in a high yield and at a higher conversion rate as compared to the existing catalysts, using the metal complex including a ligand represented by Chemical Formula 1 below and a trivalent metal in Group 8 or Group 13 as a catalyst and using various structures of epoxide compounds and carbon dioxide as raw materials. In addition, provided are the prepared cyclic carbonate, and an electrolyte including the same: in Chemical Formula 1, R1 is hydrogen, (C1-C20)alkyl or halogen; R2 is hydrogen, (C1-C20)alkyl, (C1-C20)alkoxy, halogen or nitro.
Type:
Grant
Filed:
July 12, 2016
Date of Patent:
December 26, 2017
Assignee:
KOREA ADVANCED INSTITUTE OF SCIENCE AND TECHNOLOGY
Abstract: A compound expressed by any one of Structural Formulas (1) to (13), a method for producing the same, and a compound-containing composition, an anti-cancer agent, and an anti-Helicobacter pylori agent each containing the above compound.
Abstract: An effective process of making adamantanamide, which process is fast, does not the use of organic solvents or labor-intensive isolation or purification of the product, by removal of organic solvent or by-products, and has improved yield and purity.
Abstract: The invention relates to inhibitors of mutant isocitrate dehydrogenase (mt-IDH) proteins with neomorphic activity useful in the treatment of cell-proliferation disorders and cancers, having the Formula: where A, U, W1, W2, W3, R1-R6, and R9 are described herein.
Type:
Grant
Filed:
September 18, 2015
Date of Patent:
December 5, 2017
Assignee:
FORMA Therapeutics, Inc.
Inventors:
Jian Lin, Anna Ericsson, Ann-Marie Campbell, Gary Gustafson, Zhongguo Wang, R. Bruce Diebold, Susan Ashwell, David R. Lancia, Jr., Justin Andrew Caravella, Wei Lu
Abstract: The present invention provides compounds of formula (I): compositions comprising such compounds; the use of such compounds in therapy (for example in the treatment or prevention of a disease or condition in which plasma kallikrein activity is implicated); and methods of treating patients with such compounds; wherein R1 to R3, R5 to R9, A, P, V, W, X, Y and Z are as defined herein.
Type:
Grant
Filed:
May 23, 2017
Date of Patent:
December 5, 2017
Assignee:
Kalvista Pharmceuticals Limited
Inventors:
Christine Elizabeth Allan, Andrzej Roman Batt, Rebecca Louise Davie, Hannah Joy Edwards, David Michael Evans, Stephen John Pethen
Abstract: The present invention relates to compounds of general formula I wherein R100 and R200 are each independently hydrogen, C1-C10-alkyl which in case of C2-alkyl may be interrupted by one and in case of C3-C10-alkyl by one or two nonadjacent oxygen atoms, C5-C7-cycloalkyl, aryl, aryl-C1-C10-alkyl or aryloxy-C1-C10-alkyl, D is an m-valent (m=1, 2 or 3) donor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, A is an acceptor moiety which comprises at least one carbon-carbon or carbon-heteroatom double bond and/or at least one unfused or fused carbo- or heterocyclic ring, and the donor moiety D and the acceptor moiety A are ?-conjugated to one another. Furthermore, the present invention relates to the use of compounds of formula I for producing dye-sensitized solar cells and to dye-sensitized solar cells comprising compounds of formula I.
Type:
Grant
Filed:
January 11, 2016
Date of Patent:
November 28, 2017
Assignee:
BASF SE
Inventors:
Ingmar Bruder, Robert Send, Simona Urnikaite, Tadas Malinauskas, Maryte Daskeviciene, Vytautas Getautis
Abstract: The present invention relates to novel biologically active glutarimide derivatives of general formula I or pharmaceutically acceptable salts thereof, their use as an agent for the treatment of upper respiratory tract diseases, pharmaceutical compositions comprising the glutarimide derivatives of general formula I, methods for preparing the glutarimide derivatives of general formula I by heating a dicarboxylic acid monoamide of general formula II with a dehydrating agent.
Type:
Grant
Filed:
April 10, 2014
Date of Patent:
November 14, 2017
Assignee:
OBSCHESTVO S OGRANICHENNOI OTVETSTVENNOSTIYU “PHARMENTERPRISES”
Inventors:
Vladimir Evgenievich Nebolsin, Tatyana Alexandrovna Kromova
Abstract: This invention provides, among other things, novel compounds useful for treating protozoal infections, pharmaceutical compositions containing such compounds, as well as combinations of these compounds with at least one additional therapeutically effective agent.
Type:
Grant
Filed:
February 22, 2017
Date of Patent:
November 14, 2017
Assignee:
Anacor Pharmaceuticals, Inc.
Inventors:
Tsutomu Akama, Eric Easom, Yvonne Freund, Jacob J. Plattner, Jessica Sligar, Daitao Chen, Jennifer Freeman, Joe Perales
Abstract: The present disclosure provides novel crystalline forms of cabozantinib (S)-malate, designated as form-M1, M2, M3 and M4 and novel crystalline forms of cabozantinib free base, form-M1, M2 and M3 and methods of their production. The present disclosure also provides processes for the preparation of crystalline cabozantinib (S)-malate form N-1.
Abstract: Novel CFTR corrector compounds that are effective in rescuing halide efflux, delF508-CFTR protein processing, and apical functional chloride ion transport in a cell are provided. Also provided are methods for treating protein folding disorders (e.g., cystic fibrosis and chronic obstructive pulmonary diseases). The methods include administering a CFTR corrector compound or pharmaceutically acceptable salt or prodrug thereof. Methods of rescuing halide efflux in a cell, correcting a processing defect of a delF508-CFTR protein in a cell, and correcting functional delF508-CFTR chloride channels in a cell are also provided.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
November 14, 2017
Assignee:
DiscoveryBiomed, Inc.
Inventors:
Erik Schwiebert, John Streiff, John Dixon, Hongwu Gao
Abstract: This invention provides novel indole, indazole, benzimidazole, indoline, quinolone, isoquinoline, and carbazole selective androgen receptor degrader (SARD) compounds, pharmaceutical compositions and uses thereof in treating prostate cancer, advanced prostate cancer, castration resistant prostate cancer, androgenic alopecia or other hyper androgenic dermal diseases, Kennedy's disease, amyotrophic lateral sclerosis (ALS), and uterine fibroids, and to methods for reducing the levels of androgen receptor-full length (AR-FL) including pathogenic and/or resistance mutations, AR-splice variants (AR-SV), and pathogenic polyglutamine (polyQ) polymorphisms of AR in a subject.
Type:
Grant
Filed:
April 21, 2016
Date of Patent:
November 14, 2017
Assignees:
UNIVERSITY OF TENNESSEE RESEARCH FOUNDATION, GTX, INC.
Inventors:
Ramesh Narayanan, Duane D. Miller, Thamarai Ponnusamy, Dong-Jin Hwang, Jayaprakash Pagadala, Charles B. Duke, Christopher C. Coss, James T. Dalton, Yali He
Abstract: (E)-2-(2-Quinolin-2-yl-propenyl)-phenol, 2-Quinolin-2-yl-ylethynyl-phenol and salts thereof are useful as medicaments, especially for treatment of an angiogenesis-related disease or disorder.
Type:
Grant
Filed:
June 28, 2016
Date of Patent:
November 14, 2017
Assignees:
THE PROVOST, FELLOWS, FOUNDATION SCHOLARS, AND THE OTHER MEMBERS OF BOARD, OF THE COLLEGE OF THE HOLY AND UNDIVIDED TRINITY OF QUEEN ELIZABETH NEAR DUBLIN, UNIVERSITY COLLEGE DUBLIN NATIONAL UNIVERSITY OF IRELAND, DUBLIN
Inventors:
Breandan Noel Kennedy, Alison Reynolds, Claire Kilty, Jacintha O'Sullivan, Andrew Douglas Baxter
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R11, R12, R13, R14, R15, R16, R17, m and n are as described herein, compositions including the compounds and methods of using the compounds.
Type:
Grant
Filed:
April 27, 2017
Date of Patent:
October 24, 2017
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan, Lisha Wang, Dongbo Li, Jun Wu