Abstract: The invention relates to compounds of formula (I) wherein m, o, Ra, Rb, R1 and T1 have the meaning as cited in the description and the claims. The compounds are useful as inhibitors of mTOR for the treatment or prophylaxis of mTOR related diseases and disorders. The invention also relates to pharmaceutical compositions including the compounds, the preparation of the compounds as well as their use as medicaments.
Type:
Grant
Filed:
October 5, 2012
Date of Patent:
January 26, 2016
Assignee:
CELLZOME LIMITED
Inventors:
Rosemary Lynch, Andrew David Cansfield, Daniel Paul Hardy, John Thomas Feutrill, Rita Adrego, Katie Ellard, Tammy Ladduwahetty
Abstract: The present invention relates to methods for the preparation of a compound having the formula (X). Individual reaction steps as well as intermediates are additionally claimed.
Abstract: This invention relates to inhibitors of mitotic kinesins, particularly KSP, and methods for producing these inhibitors. The invention also provides pharmaceutical compositions comprising the inhibitors of the invention and methods of utilizing the inhibitors and pharmaceutical compositions in the treatment and prevention of various disorders.
Type:
Grant
Filed:
March 19, 2015
Date of Patent:
December 29, 2015
Assignee:
Array BioPharma Inc.
Inventors:
Jeremy Hans, Eli M. Wallace, Qian Zhao, Shelley Allen, Ellen Laird, Joseph P. Lyssikatos, John E. Robinson, Christopher P. Corrette, Robert Kirk DeLisle, Walter C. Voegtli
Abstract: The present invention relates to a process for the preparation of N-hydroxy-1-(1-alkyl-1H-tetrazol-5-yl)-1-phenylmethanimine derivatives of the general formula (I)
Type:
Grant
Filed:
February 6, 2013
Date of Patent:
December 15, 2015
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Pierre-Yves Coqueron, Christophe Dubost, Mark Ford, Anne-Sophie Rebstock
Abstract: Disclosed are 6-(morpholinoalkyl)-substituted pyridines, and pharmaceutically acceptable salts and prodrugs thereof, that are active against a range of mammalian therapeutic indications.
Type:
Grant
Filed:
May 1, 2013
Date of Patent:
December 15, 2015
Assignees:
Trustees of Tufts College, Arisaph Pharmaceuticals, Inc.
Inventors:
William W. Bachovchin, Hung-sen Lai, Daniel P. O'Connell, Wengen Wu, Christopher P. Kiritsy
Abstract: Novel compounds which are inhibitors of receptor tyrosine kinases of the AXL receptor family are described herein. These compounds are suitable for the treatment or prevention of disorders associated with, accompanied by or caused by hyperfunction of a receptor of the AXL family. The compounds are suitable for the treatment of hyperproliferative disorders, such as cancer, particularly cancer metastases.
Type:
Grant
Filed:
April 16, 2009
Date of Patent:
December 8, 2015
Assignee:
Max-Planck-Gesellschaft zur Förderung der Wissenschaften E.V.
Inventors:
Axel Ullrich, Pjotr Knyazev, Yixiang Zhang, Kéri György, László Örfi, István Szabadkai
Abstract: Arylpyrrolidines of formula (I): wherein each substituent is as defined in the specification, and use thereof as pesticides and animal parasite-controlling agents.
Abstract: The invention relates to novel compounds of the formula (I) in which X, Y and CKE have the meanings given herein, to a plurality of processes and intermediates for their preparation, and to their use as pesticides and/or herbicides. The invention also relates to selective herbicidal compositions comprising the 1,2,4-triazolyl-substituted ketoenols and a crop plant compatibility-improving compound. The present invention further relates to boosting the action of said crop protection compositions through the addition of ammonium salts or phosphonium salts and optional penetrants to the corresponding compositions, to processes for producing said compositions, and to their application in crop protection as insecticides and/or acaricides and/or for preventing unwanted plant growth.
Type:
Grant
Filed:
August 10, 2012
Date of Patent:
December 1, 2015
Assignee:
BAYER INTELLECTUAL PROPERTY GMBH
Inventors:
Wolfgang Giencke, Stefan Lehr, Reiner Fischer, David Stephen Lindell, Isolde Haeuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger, Angela Becker, Arnd Voerste, Ulrich D.I. Goergens
Abstract: Compounds of formula (I) or a pharmaceutically acceptable salt thereof, wherein: W is O, N—H, N-(C1-C10 alkyl) or S; each X is independently CH or N; R1 is a 5 to 7-membered saturated or unsaturated, optionally substituted heterocycle containing at least 1 heteroatom selected from N or O; R2 is (LQ)mY; and each R3 is independently H, C1-C10 alkyl, aryl or heteroaryl, are surprisingly found to be inhibitors of PI3K-p110?, and therefore have utility in therapy.
Type:
Grant
Filed:
August 19, 2010
Date of Patent:
December 1, 2015
Assignee:
Karus Therapeutics Limited
Inventors:
Stephen Joseph Shuttleworth, Alexander Richard Liam Cecil, Thomas James Hill, Franck Alexandre Silva
Abstract: Benzoxazepin compounds of Formula I, including stereoisomers, geometric isomers, tautomers, solvates, metabolites and pharmaceutically acceptable salts thereof, wherein: Z1 is CR1 or N; Z2 is CR2 or N; Z3 is CR3 or N; Z4 is CR4 or N; and B is a pyrazolyl, imidazolyl, or triazolyl ring fused to the benzoxepin ring, are useful for inhibiting lipid kinases including p110 alpha and other isoforms of PI3K, and for treating disorders such as cancer mediated by lipid kinases. Methods of using compounds of Formula I for in vitro, in situ, and in vivo diagnosis, prevention or treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.
Type:
Grant
Filed:
June 5, 2014
Date of Patent:
December 1, 2015
Assignee:
GENENTECH, INC.
Inventors:
Nicole Blaquiere, Steven Do, Danette Dudley, Adrian Folkes, Robert Heald, Timothy Heffron, Mark Jones, Aleksandr Kolesnikov, Chudi Ndubaku, Alan G. Olivero, Stephen Price, Steven Staben, Lan Wang
Abstract: The present invention relates to a compound of Formula I, or an isomer, pharmaceutically acceptable salt and solvate of the compound, and to a composition comprising the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof, and a pharmaceutically acceptable carrier, excipient or diluents. The present invention also relates to use of the compound of Formula I, or the isomer, pharmaceutically acceptable salt and solvate thereof for combating apoptosis, preventing or treating a disease or disorder associated with apoptosis; and especially use for protecting cardiomyocyte, and for preventing or treating a disease or disorder associated with cardiomyocyte apoptosis.
Type:
Grant
Filed:
May 14, 2010
Date of Patent:
December 1, 2015
Assignee:
CHINESE PLA GENERAL HOSPITAL
Inventors:
Kunluu He, Song Li, Wu Zhong, Juan Liu, Lili Wang, Xin Li, Guoliang Hu, Jie Wang, Long Long, Junhai Xiao, Zhibing Zheng, Wei Li, Ruijun Li, Chunlei Liu, Jie Tang
Abstract: The present invention relates to compounds useful as inhibitors of protein kinase. The invention also provides pharmaceutically acceptable compositions comprising said compounds and methods of using the compositions in the treatment of various disease, conditions, or disorders. The invention also provides processes for preparing compounds of the inventions. The compounds of the present invention are represented by the structure of formula I: or a pharmaceutically acceptable salt thereof, wherein the variables are defined herein.
Type:
Grant
Filed:
April 30, 2013
Date of Patent:
November 24, 2015
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Juan-Miguel Jimenez, John Studley, Ronald Knegtel, Luca Settimo, Christopher John Davis, Damien Fraysse, Philip N. Collier, Guy Brenchley, Dean Boyall, Andrew Miller, Heather Twin, Stephen Young
Abstract: The invention described herein pertains to compounds and compositions for treating Ape1 mediated diseases. In particular, the invention described herein pertains to quinone compounds and pharmaceutical compositions containing them for treating Ape1 mediated diseases.
Type:
Grant
Filed:
May 25, 2012
Date of Patent:
November 24, 2015
Assignees:
Indiana University Research and Technology Corporation, Apex Therapeutics, Inc.
Abstract: The present disclosure relates to new DNA-directed alkylating agents and water-soluble N-mustard agents with improved chemical stability and anti-tumor therapeutic efficacy.
Type:
Grant
Filed:
June 29, 2012
Date of Patent:
November 24, 2015
Assignee:
Academia Sinica
Inventors:
Tsann-Long Su, Ting-Chao Chou, Te-Chuang Lee
Abstract: Novel p53-Mdm2 antogonists that conform to Formula I or to Formula II: where the prescribed substituent groups are defined, are useful in treating or preventing cancer. In particular, the compounds and their pharmaceutical compositions are useful for treating relapsed/refractory acute myeloid and lymphoid leukemia and refractory chronic lymphocytic leukemia/small cell lymphocytic lymphomas.
Type:
Grant
Filed:
September 8, 2011
Date of Patent:
November 17, 2015
Assignee:
University of Pittsburgh—Of the Commonwealth System of Higher Education
Abstract: The invention relates to compounds of the formula (I) in which R1, L and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I) by reaction of compounds of the formulae (II) and (III) and optionally conversion of a base or acid of the compounds of the formula (I) into a salt thereof.
Type:
Grant
Filed:
October 30, 2012
Date of Patent:
November 17, 2015
Assignee:
Merck Patent GmbH
Inventors:
Werner Mederski, Thomas Fuchss, Ulrich Emde, Hans-Peter Buchstaller
Abstract: Disclosed are methods of identifying, generating and synthesizing compounds that inhibit MAPK13 activity. In various embodiments, compounds, salts thereof and prodrugs thereof of the present teachings can be useful for the treatment of diseases and disorders that involve excess mucus production.
Type:
Grant
Filed:
January 16, 2015
Date of Patent:
November 17, 2015
Assignee:
Washington University
Inventors:
Michael Holtzman, Arthur Romero, Yael Alevy, Anand Patel, Thomas Brett, Dhara Patel
Abstract: The invention relates to new crystalline forms of processes for manufacturing a compound of formula 5, or a stereoisomer, tautomer or a salt thereof, wherein the substituents are as defined in the specification. The invention further relates to new manufacturing processes for specific solid forms of Compound A and its salts, to such solid forms and to use of said solid forms for the therapeutic treatment of warm-blooded animals.
Type:
Grant
Filed:
September 29, 2011
Date of Patent:
November 10, 2015
Assignee:
Novartis AG
Inventors:
Marilyn De La Cruz, Piotr H. Karpinski, Liladhar Murlidhar Waykole
Abstract: The present invention relates to the use of alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds of formula I as defined in the description, and the N-oxides, and salts thereof for combating harmful fungi and seed coated with at least one such compound. The invention also relates to novel alkyl-substituted 2-[2-chloro-4-(4-chloro-phenoxy)-phenyl]-1-[1,2,4]triazol-1-yl-ethanol compounds, processes and intermediates for preparing these compounds and also to compositions comprising at least one such compound.
Type:
Grant
Filed:
July 11, 2012
Date of Patent:
November 3, 2015
Assignee:
BASF SE
Inventors:
Jochen Dietz, Richard Riggs, Nadege Boudet, Jan Klaas Lohmann, Ian Robert Craig, Egon Haden, Erica May Wilson Lauterwasser, Bernd Müller, Wassilios Grammenos, Thomas Grote