Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R10, R11, R12, R13, R14, R15, R16, R17 and m 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, Dongbo Li, Yongfu Liu, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan, Lisha Wang, Jun Wu
Abstract: The present invention provides a method for manufacturing an optically active compound of formula (2), which contains bringing hydrogen into contact with a compound of formula (1) in the presence of a transition metal catalyst having an optically active ligand. In the formula, R1 represents a hydrogen atom or an acetyl group, R2, R3, R4, and R5 each independently represents a hydrogen atom, a halogen atom, an alkyl group, an alkoxy group, a hydroxy group, a nitro group, an amino group, or an acyl group, R6 represents an alkyl group, R7 and R8 each independently represents a hydrogen atom or an alkyl group, and a carbon atom marked with an asterisk (*) represents an asymmetric carbon atom.
Abstract: The invention provides novel compounds having the general formula (I) wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R15, R16, R17 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 17, 2017
Assignee:
Hoffmann-La Roche Inc.
Inventors:
Johannes Aebi, Kurt Amrein, Benoit Hornsperger, Bernd Kuhn, Hans P. Maerki, Rainer E. Martin, Alexander V. Mayweg, Xuefei Tan
Abstract: 3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid amide derivatives which are agonists of somatostatin receptor subtype 4 (SSTR4), useful for preventing or treating medical disorders related to SSTR4.
Type:
Grant
Filed:
May 18, 2016
Date of Patent:
October 17, 2017
Assignee:
Centrexion Therapeutics Corporation
Inventors:
Riccardo Giovannini, Yunhai Cui, Henri Doods, Marco Ferrara, Stefan Just, Raimund Kuelzer, Iain Lingard, Rocco Mazzaferro, Klaus Rudolf
Abstract: The present application relates to a series of substituted imidazo[1,2-a]pyridine compounds of formula (I), pharmaceutically acceptable salts, pharmaceutically acceptable solvates or stereoisomers thereof, their use as tropomyosin receptor kinase (Trk) family protein kinase inhibitors, method of making and pharmaceutical compositions comprising such compounds.
Abstract: The present invention relates to novel isoxazoline carboxamide derivatives, to processes for preparing these compounds, to compositions comprising these compounds, and to the use thereof as biologically active compounds, especially for control of harmful microorganisms in crop protection and in the protection of materials.
Type:
Grant
Filed:
October 27, 2016
Date of Patent:
October 3, 2017
Assignee:
BAYER CROPSCIENCE AG
Inventors:
Lothar Willms, Monika H. Schmitt, Thomas Frenzel, Klaus Bernhard Haaf, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Heinz Kehne, Jan Dittgen, Dieter Feucht, Martin Hills, Jan Peter Schmidt, Mazen Es-Sayed, Philipe Rinolfi, Stephane Brunet, Marie-Claire Grosjean-Cournoyer, Helene Lachaise, Jacky Vidal, Pierre-Yves Coqueron, Arounarith Tuch
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, B, U, V, Z, W1, W2, W3, and R1-R6 are described herein.
Type:
Grant
Filed:
September 18, 2015
Date of Patent:
September 26, 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 invention provides a compound having a selective inhibitory activity against highly-expressed LAT-1 in tumor cell. The compound is represented by the formula (I): wherein each symbol is as defined in the specification, or a salt thereof, and a LAT-1 inhibitor comprising the same.
Abstract: Described herein are compounds and compositions that modulate the activity of beta-lactamases. In some embodiments, the compounds described herein inhibit beta-lactamase. In certain embodiments, the compounds described herein are useful in the treatment of bacterial infections.
Type:
Grant
Filed:
June 27, 2016
Date of Patent:
September 26, 2017
Assignee:
VENATORX PHARMACEUTICALS, INC.
Inventors:
Christopher J. Burns, Denis Daigle, Bin Liu, Daniel McGarry, Daniel C. Pevear, Robert E. Lee Trout, Randy W. Jackson
Abstract: Compounds of formula (I) can modulate the activity of one or more S 1P receptors. Sphingosine 1-phosphate (S IP) is a lysophospholipid mediator that evokes a variety of cellular responses by stimulation of five members of the endothelial cell differentiation gene (EDG) receptor family, namely S1P1, S1P2, S1P3, S1P4, and S1P5 (formerly EDG1, EDG5, EDG3, EDG6 and EDG8). The EDG receptors are G-protein coupled receptors (GPCRs) and on stimulation propagate second messenger signals via activation of heterotrimeric G-protein alpha (Ga.) subunits and beta-gamma (G( )y) dimers.
Type:
Grant
Filed:
January 29, 2014
Date of Patent:
September 19, 2017
Assignee:
BIOGEN MA INC.
Inventors:
Kevin Guckian, Gnanasambandam Kumaravel, Xiaogao Liu, Bin Ma, Hairuo Peng
Abstract: The present invention relates to a method for producing silymarin. The method comprises: pressing silybum marianum seeds to obtain silymarin powder, and soaking the silymarin powder by using alkaline water; extracting, by using acetone, the silymarin powder soaked by using alkaline water, and performing filtering and concentration on the extracted liquid to obtain a concentrated solution; and performing extraction on the concentrated solution by using a non-polar solvent, performing separation to obtain a non-polar solvent layer and an acetone layer, and concentrating and drying the acetone layer to obtain silymarin. The method can greatly improve the extraction efficiency and the yield, shorten the extraction time, needs simple processes and low cost and thoroughly remove residual oil, so that the product has a low impurity, high product quality and a high purity; and the method is applicable to industrial production and has a great application prospect and economic value.
Abstract: The invention relates to pyridone amide compounds of formula I and I? or pharmaceutically acceptable salts thereof, useful as inhibitors of sodium channels: The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders, including pain.
Type:
Grant
Filed:
June 6, 2016
Date of Patent:
September 12, 2017
Assignee:
VERTEX PHARMACEUTICALS INCORPORATED
Inventors:
Sara Sabina Hadida-Ruah, Corey Anderson, Vijayalaksmi Arumugam, Iuliana Luci Asgian, Brian Richard Bear, Andreas P. Termin, James Philip Johnson
Abstract: Novel base addition salts of nitroxoline with improved solubility and increased urine secretion under physiological conditions are described. Pharmaceutical compositions and methods of treatment using the pharmaceutical compositions are also described.
Abstract: Provided is a method of preparing a silylative-reduced N-heterocyclic compound by reducing an N-heteraromatic compound including a sp2 hybridized nitrogen atom while simultaneously introducing a silyl group into a beta-position with respect to a nitrogen atom of the N-heteroaromatic compound, using a silane compound, in the presence of an organoboron catalyst.
Type:
Grant
Filed:
January 29, 2015
Date of Patent:
August 29, 2017
Assignees:
Institute for Basic Science, Korea Advanced Institute of Science and Technology
Inventors:
Sukbok Chang, Sehoon Park, Narasimhulu Gandhamsetty, Seewon Joung, Sung-Woo Park
Abstract: Provided herein are antagonists of prostaglandin EP3 receptor, processes to make said antagonists, and methods comprising administering said antagonists to a mammal in need thereof.
Type:
Grant
Filed:
December 16, 2015
Date of Patent:
August 22, 2017
Assignee:
Pfizer Inc.
Inventors:
Kevin Bahnck, Daniel Canterbury, David James Edmonds, Kentaro Futatsugi, Esther Cheng Yin Lee, Elnaz Menhaji-Klotz, Jana Polivkova, Robert Vernon Stanton
Abstract: The present invention relates to a process for preparing alkaline earth metal-complexed metal bisamides of the formula (I) from metal monoamides of the formula (II). The present invention further relates to a process for preparing alkaline earth metal monoamides of the formula (II-AE), to novel LiCl-free alkaline earth metal monoamides of the formula (II-AE-L), and to the use of these alkaline earth metal monoamides for metallation of aromatics, heteroaromatics, alkenes, alkynes and other organic compounds having activated C—H bonds.
Abstract: This invention relates to triazolones and triazolones for the modulation, notably the inhibition of the activity or function of fatty acid synthase (FAS). Suitably, the present invention relates to the use of triazolones in the treatment of cancer.
Abstract: One class of blue thiophene electrochromic compounds include 3,4-(2,2-bis(2-oxo-3-phenylpropyl))propylenedioxythiophene, 3,4-(2,2-bis(2-oxo-3-phenylbutyl))propylenedioxythiophene, and 3,4-(2,2-bis(2-oxo-3-phenylamyl))propylenedioxythiophene. The thiophene electrochromic compounds can change color between blue and transparency. The thiophene compounds can be electropolymerized on the surface of the ITO glass to form a film. The film has characteristics of low driving voltage (within ±1V), fast response time, and large transmittance difference between colored-state and bleached-state (up to 77.5%). The thiophene electrochromic compounds can be used in the electrochromic window, rearview mirror, electrochomeric display, and the like.
Type:
Grant
Filed:
November 7, 2014
Date of Patent:
July 25, 2017
Assignees:
BOE TECHNOLOGY GROUP CO., LTD., UNIVERSITY OF SCIENCE AND TECHNOLOGY OF CHINA
Abstract: The invention relates to ROR modulators; compositions comprising an effective amount of a ROR modulator; and methods for treating or preventing diseases associated with ROR.
Type:
Grant
Filed:
April 30, 2013
Date of Patent:
July 18, 2017
Assignee:
INNOV17 LLC
Inventors:
Anderson Gaweco, Jefferson W. Tilley, John Walker, Samantha Palmer, James Blinn