Abstract: The present application relates to novel 3-aryl-substituted imidazo[1,2-a]pyridines, to processes for preparation thereof, to the use thereof, alone or in combinations, for treatment and/or prophylaxis of diseases, and to the use thereof for production of medicaments for treatment and/or prophylaxis of diseases, especially for treatment and/or prophylaxis of cardiovascular disorders.
Type:
Grant
Filed:
June 4, 2014
Date of Patent:
October 3, 2017
Assignee:
BAYER PHARMA AKTIENGESELLSCHAFT
Inventors:
Alexandros Vakalopoulos, Markus Follmann, Ingo Hartung, Philipp Buchgraber, Alexey Gromov, Niels Lindner, Frank Wunder, Johannes-Peter Stasch, Gorden Redlich, Volkhart Min-Jian Li
Abstract: Provided herein are processes and intermediate compounds useful for the preparation of 2-carboxamide cycloamino urea derivatives, and useful intermediates therefore.
Type:
Grant
Filed:
April 6, 2017
Date of Patent:
October 3, 2017
Assignee:
Novartis AG
Inventors:
Bernhard Erb, Isabelle Sylvie Gallou, Florian Karl Kleinbeck
Abstract: The invention provides peptides that bind Tissue Factor Pathway Inhibitor (TFPI), including TFPI-inhibitory peptides, and compositions thereof. The peptides may be used to inhibit a TFPI, enhance thrombin formation in a clotting factor-deficient subject, increase blood clot formation in a subject, and/or treat a blood coagulation disorder in a subject.
Type:
Grant
Filed:
March 14, 2013
Date of Patent:
October 3, 2017
Assignees:
Baxalta GmbH, Baxalta Incorporated
Inventors:
Michael Dockal, Hartmut Ehrlich, Friedrich Scheiflinger, Ulf Reimer, Ulrich Reineke, Thomas Polakowski, Eberhard Schneider
Abstract: The present invention provides novel analogs of FR901464, as well as an improved methodology for preparing FR901464 and its analogs. These compounds display an anti-cancer activity and are candidates for therapies against a number of disease states associated with dysfunctional RNA splicing.
Type:
Grant
Filed:
December 19, 2013
Date of Patent:
September 26, 2017
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Inventors:
Kazunori Koide, Sami Saif Eldin Ali Osman
Abstract: The invention features therapeutic compositions comprising agents useful for the treatment or prevention of pruritis, and methods useful for identifying such agents.
Type:
Grant
Filed:
January 24, 2014
Date of Patent:
September 26, 2017
Assignees:
The Johns Hopkins University, California Institute of Technology
Inventors:
Xinzhong Dong, Qin Liu, David J. Anderson
Abstract: The invention provides novel compounds having the general formula: and pharmaceutically acceptable salts thereof, wherein the variables RA, subscript n, ring A, X2, L, subscript m, X1, B, R1, R2, R3, R4, R5 and RN have the meaning as described herein, and compositions containing such compounds and methods for using such compounds and compositions.
Type:
Grant
Filed:
April 19, 2016
Date of Patent:
September 26, 2017
Assignees:
GENENTECH, INC., XENON PHARMACEUTICALS INC.
Inventors:
Sultan Chowdhury, Christoph Martin Dehnhardt, Thilo Focken, Michael Edward Grimwood, Ivan William Hemeon, Qi Jia, Daniel F. Ortwine, Brian Safina, Shaoyi Sun, Daniel P. Sutherlin, Alla Yurevna Zenova
Abstract: This invention is directed to photoluminescent compounds based on rhodamine dyes with red-shifted absorption and emission maxima and uses thereof for photoluminescence based devices.
Type:
Grant
Filed:
August 31, 2016
Date of Patent:
September 26, 2017
Assignee:
StoreDot Ltd.
Inventors:
Evgenia Liel (Jeny) Kuks, Rony Schwarz, Eran Sella, Mor Shmuel Armon, Daniel Szwarcman
Abstract: Compounds of Formula I or II: are described, along with pharmaceutical compositions containing the same and methods of using such compounds for the treatment of cancer.
Type:
Grant
Filed:
November 22, 2013
Date of Patent:
September 26, 2017
Assignee:
The University of North Carolina at Chapel Hill
Inventors:
Xiaodong Wang, Weihe Zhang, Stephen V. Frye, Dmitri Kireev, Andrew Louis McIver, Jing Liu
Abstract: The present invention relates to compounds and methods for the treatment of cancer. In particular, the invention provides potent inhibitors of Aurora A kinase, pharmaceutical compositions comprising the compounds, and methods of using the compounds for the treatment of cancer.
Type:
Grant
Filed:
October 15, 2014
Date of Patent:
September 19, 2017
Assignee:
Millenium Pharmaceuticals, Inc.
Inventors:
Christopher F. Claiborne, Todd B. Sells, Stephen G. Stroud
Abstract: The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain pyridyl-amino-pyrazine carbonitrile compounds that, inter alia, inhibit Checkpoint Kinase 1 (CHK1) kinase function. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, both in vitro and in vivo, to inhibit CHK1 kinase function, and in the treatment of diseases and conditions that are mediated by CHK1, that are ameliorated by the inhibition of CHK1 kinase function, etc., including proliferative conditions such as cancer, etc., optionally in combination with another agent, for example, (a) a DNA topoisomerase I or II inhibitor; (b) a DNA damaging agent; (c) an antimetabolite or thymidylate synthase (TS) inhibitor; (d) a microtubule targeted agent; and (e) ionizing radiation.
Type:
Grant
Filed:
June 24, 2016
Date of Patent:
September 19, 2017
Assignee:
Cancer Research Technology Limited
Inventors:
Ian Collins, Michael Lainchbury, Thomas Peter Matthews, John Charles Reader
Abstract: Compounds of formula (I) wherein R1, R2, R3, R4, R5, R6a and R6b are as defined in the description; or a stereoisomer, salt, tautomer or N-oxide, or a polymorphic crystalline form, a co-crystal or a solvate of a compound or a stereoisomer, salt, tautomer or N-oxide thereof, and to mixtures, methods and uses thereof.
Type:
Grant
Filed:
February 20, 2014
Date of Patent:
September 19, 2017
Assignee:
BASF SE
Inventors:
Florian Kaiser, Karsten Koerber, Prashant Deshmukh, Matthias Pohlman, Jean-Yves Wach, Juergen Langewald, Egon Haden, Deborah L. Culbertson, W. David Rogers, Koshi Gunjima, Michael David, Franz Josef Braun
Abstract: The present invention is directed to 3-ester-4-substituted compounds which are antagonists of orexin receptors. The present invention is also directed to uses of the 3-ester-4-substituted compounds described herein in the potential treatment or prevention of neurological and psychiatric disorders and diseases in which orexin receptors are involved. The present invention is also directed to pharmaceutical compositions comprising these compounds. The present invention is also directed to uses of these pharmaceutical compositions in the prevention or treatment of such diseases in which orexin receptors are involved.
Abstract: The present invention relates to certain tetramic acid derivatives that are suitable for use in the preparation and development of antimicrobial (e.g. antibacterial or antifungal) compositions. The present invention also relates to the use of such compounds as antimicrobial (e.g. antibacterial or antifungal agents) and, in particular, as topical antibacterial or antifungal agents.
Abstract: The present invention includes a method of inhibiting, suppressing or preventing HBV infection in an individual in need thereof, comprising administering to the individual a therapeutically effective amount of at least one compound of the invention.
Type:
Grant
Filed:
December 2, 2015
Date of Patent:
September 19, 2017
Assignee:
NOVIRA THERAPEUTICS, INC.
Inventors:
Ryan C. Clark, Yen Truong, Nicholas Stock, Jason Jacintho
Abstract: The present invention relates to a method for the synthesis of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. iriniotecan), comprising: (a) preparing 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptotecin; and (b) selectively ethylating the compound of step (a) at the 7-position, thus resulting in the preparation of 7-ethyl-10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin. The present invention is further directed to the use of 10-[4-(1-piperidino)-1-piperidino]carbonyloxycamptothecin (i.e. 7-des-ethyl-irinotecan) as intermediate in a method for the synthesis of irinotecan as described.
Abstract: A method of making a furan dicarboxylate by means of reacting 2,5-furan dicarboxylic acid (FDCA) with an alcohol or mixture of alcohols in a CO2-predominant atmosphere without the presence of any other acid catalyst is described. The reaction is conducted under conditions that correspond to either supercritical, critical or near-critical temperatures and pressures for the alcohol species and/or CO2 gas.
Abstract: Compounds of formula (I), defined herein, are both phosphodiesterase 4 (PDE4) enzyme inhibitors and muscarinic M3 receptor antagonists and are useful for the prevention and/or treatment of a disease of the respiratory tract.
Type:
Grant
Filed:
May 28, 2015
Date of Patent:
September 19, 2017
Assignee:
Chiesi Farmaceutici S.p.A.
Inventors:
Elisabetta Armani, Gabriele Amari, Carmelida Capaldi, Wesley Blackaby, Ian Linney, Hervé Van De Poël, Charles Baker-Glenn, Naimisha Trivedi
Abstract: The present invention is directed to [1,2,4]triazolo[4,3-a]pyridine and [1,2,4]triazolo[4,3-a]pyrazine derivatives which are LSD1 inhibitors useful in the treatment of diseases such as cancer.
Type:
Grant
Filed:
July 9, 2015
Date of Patent:
September 12, 2017
Assignee:
Incyte Corporation
Inventors:
Liangxing Wu, Xiaozhao Wang, Wenqing Yao, Colin Zhang
Abstract: A catalyst system includes a transition metal salt containing a halo group, an acetate group, or a combination thereof, and an organic phosphine ligand. The molar ratio of the organic phosphine ligand to the transition metal salt is greater than 0 and less than or equal to 50.
Type:
Grant
Filed:
December 16, 2015
Date of Patent:
September 12, 2017
Assignee:
Industrial Technology Research Institute