Abstract: A method of treating a disorder such as epilepsy, multiple sclerosis, glaucoma and uveitis, cerebral traumas and cerebral ischaemias, stroke, head injury, spinal cord injury, surgical trauma, neurodegenerative disorders, motorneurone disease, Alzheimer's disease, Parkinson's disease, chronic inflammatory pain, neuropathic pain, migraine, bipolar disorder, mood, anxiety and cognitive disorders, schizophrenia, or trigeminal autonomic cephalalgias. The method includes administering to a subject in need thereof substituted 1,2,4-triazine compounds of formula (I): Each of A, N*, X, Y, Z, R1, and R2 is defined herein. Also disclosed are compounds of the formula and a pharmaceutical composition containing such a compound.
Type:
Grant
Filed:
February 6, 2014
Date of Patent:
August 23, 2016
Assignee:
UNIVERSITY OF GREENWICH
Inventors:
Michael Leach, Laurence Harbige, Dieter Riddall, Karl Franzmann
Abstract: This invention relates to pyrimidine derivatives, processes for their preparation, pharmaceutical compositions, and their use in treating viral infections such as HCV or HBV.
Type:
Grant
Filed:
April 10, 2012
Date of Patent:
August 23, 2016
Assignee:
Janssen Sciences Ireland UC
Inventors:
David Mc Gowan, Pierre Jean-Marie Bernard Raboisson, Werner Embrechts, Tim Hugo Maria Jonckers, Stefaan Julien Last, Serge Maria Aloysius Pieters, Jaromir Vlach
Abstract: The present invention provides a compound of Formula I or Formula II: enantiomer, diastereomer, prodrug, solvate, metabolite, or pharmaceutically acceptable salt thereof, wherein constituent variables are provided herein. The compounds of Formula I and II are modulators of metalloproteases and are useful in treating diseases associated with metalloprotease activity such as arthritis, cancer, cardiovascular disorders, skin disorders, inflammation and allergic conditions.
Abstract: Compounds selected from the group according to claim 1 are inhibitors of tyrosine kinases, in particular of Met kinase, and can be employed, inter alia, for the treatment of tumors.
Type:
Grant
Filed:
January 22, 2015
Date of Patent:
August 2, 2016
Assignee:
MERCK PATENT GMBH
Inventors:
Oliver Schadt, Dieter Dorsch, Frank Stieber, Andree Blaukat
Abstract: The present invention relates to processes and intermediates for preparing Gonadotropin-Releasing Hormone (GnRH) receptor antagonists of structure (VI); and stereoisomers and pharmaceutically acceptable salts thereof.
Type:
Grant
Filed:
June 19, 2014
Date of Patent:
July 5, 2016
Assignee:
Neurocine Biosciences, Inc.
Inventors:
Donald J. Gallagher, Laszlo R. Treiber, Robert Michael Hughes, Onorato Campopiano, Peng Wang, Yuxin Zhao, Shine K. Chou, Michael Allen Ouellette, Donald Nicholas Hettinger
Abstract: The present invention provides 2,4-disubstituted pyrimidine compounds useful as kinase inhibitors, pharmaceutically acceptable compositions thereof, and methods of using the same.
Type:
Grant
Filed:
March 3, 2015
Date of Patent:
June 28, 2016
Assignee:
Celgene Avilomics Research, Inc.
Inventors:
Kwangho Lee, Deqiang Niu, Russell C. Petter, Matthew F. Baevsky, Juswinder Singh
Abstract: The present invention relates to compounds useful as inhibitors of DNA-PK. 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.
Type:
Grant
Filed:
October 17, 2013
Date of Patent:
June 28, 2016
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Paul S. Charifson, Kevin Michael Cottrell, Hongbo Deng, John P. Duffy, Huai Gao, Simon Giroux, Jeremy Green, Katrina Lee Jackson, Joseph M. Kennedy, David J. Lauffer, Mark Willem Ledeboer, Pan Li, John Patrick Maxwell, Mark A. Morris, Albert Charles Pierce, Nathan D. Waal, Jinwang Xu
Abstract: The invention relates to a process for preparing polyisocyanates containing isocyanurate groups by trimerising cycloaliphatic diisocyanates using a catalyst solution comprising at least one quaternary ammonium hydroxide, characterized in that the catalyst solution is metered in such that the reaction temperature is >90° C. and ?140° C.
Type:
Grant
Filed:
August 20, 2013
Date of Patent:
June 28, 2016
Assignee:
Covestro Deutschland AG
Inventors:
Reinhard Halpaap, Mario Schneider, Oswald Wilmes, Uwe Werner
Abstract: The present invention is directed to benzoimidazol-2-yl pyrimidine derivatives useful as histamine H4 receptor modulators and processes for the preparation of such compounds.
Type:
Grant
Filed:
August 14, 2014
Date of Patent:
June 21, 2016
Assignee:
Janssen Pharmaceutica NV
Inventors:
Neelakandha S. Mani, Christopher L. Mapes, Daniel J. Pippel, Diego F. Broggini
Abstract: The present invention provides spirolactam derivatives of formula (I): wherein R1-R7 are as defined herein; or a pharmaceutically acceptable salt thereof; and pharmaceutical compositions and uses of the same.
Type:
Grant
Filed:
December 12, 2013
Date of Patent:
June 7, 2016
Assignee:
H. Lundbeck A/S
Inventors:
Hao Zhou, Guiying Li, Dario Doller, Gil Ma
Abstract: The present invention provides low hygroscopic forms of aripiprazole and processes for the preparation thereof which will not convert to a hydrate or lose their original solubility even when a medicinal preparation containing the anhydrous aripiprazole crystals is stored for an extended period.
Abstract: Compounds having the structure of Formula I, including pharmaceutically acceptable salts of the compounds, are CETP inhibitors and may be useful for raising HDL-cholesterol and reducing LDL-cholesterol in human patients and for treating or preventing atherosclerosis.
Type:
Grant
Filed:
April 26, 2013
Date of Patent:
May 31, 2016
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
John J. Acton, III, Feng Ye, Petr Vachal, Deyou Sha, James F. Dropinski, Lin Chu, Debra Ondeyka, Alexander J. Kim, Vincent J. Colandrea, Yi Zang, Fengqi Zhang, Guizhen Dong
Abstract: Provided is a method for the synthesis of N-protected bis-3,6-[4-aminobutyl]-2,5-diketopiperazine including the step of heating a solution of ?-amino protected lysine in the presence of a catalyst selected from the group consisting of sulfuric acid, phosphoric acid, and phosphorus pentoxide.
Type:
Grant
Filed:
April 30, 2014
Date of Patent:
May 24, 2016
Assignee:
MannKind Corporation
Inventors:
John J. Stevenson, Destardi Moye-Sherman
Abstract: The present disclosure relates to salts and compositions of isophosphoramide mustard and isophosphoramide mustard analogs. In one embodiment the salts can be represented by the formula I: (I) wherein A+ represents an ammonium species selected from the protonated (conjugate acid) or quaternary forms of aliphatic amines and aromatic amines, including basic amino acids, heterocyclic amines, substituted and unsubstituted pyridines, guanidines and amidines; and X and Y independently represent leaving groups. Also disclosed herein are methods for making such compounds and formulating pharmaceutical compositions thereof. Methods for administering the disclosed compounds to subjects, particularly to treat hyper-proliferative disorders, also are disclosed.
Abstract: Disclosed are compounds of Formula (I), or a pharmaceutically acceptable salt thereof, wherein: W and Q and G are defined herein. Also disclosed are methods of using such compounds as inhibitors of Bcl-2 family antiapoptotic proteins for the treatment of cancer; and pharmaceutical compositions comprising such compounds.
Type:
Grant
Filed:
May 23, 2012
Date of Patent:
May 24, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Robert M. Borzilleri, Zhen-Wei Cai, Andrew J. Tebben, Heidi L. Perez, Liping Zhang, Gretchen M. Schroeder, Donna D. Wei
Abstract: The invention relates to a compound of formula (I): or a pharmaceutically acceptable salt thereof, thereof, wherein: G is a group of formula (II): and pharmaceutically acceptable salts, prodrugs, hydrates, or solvates, thereof, wherein A, B, L1-L4, A, B, R1-R4, and m are as defined herein. The invention also relates to pharmaceutical compositions comprising the compounds of formula (I) and their use in treating a bacterial infection.
Type:
Grant
Filed:
March 24, 2014
Date of Patent:
May 17, 2016
Assignee:
Pfizer Inc.
Inventors:
Matthew Frank Brown, Charles Francis Donovan, Edmund Lee Ellsworth, Denton Wade Hoyer, Timothy Allan Johnson, Manjinder Singh Lall, Chris Limberakis, Sean Timothy Murphy, Debra Ann Sherry, Clarke Bentley Taylor, Joseph Scott Warmus
Abstract: The present application relates to novel amides and thioamides, to processes for preparation thereof and to the use thereof for controlling animal pests, in particular arthropods and especially insects.
Type:
Grant
Filed:
January 16, 2014
Date of Patent:
May 17, 2016
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Thomas Bretschneider, Adeline Köhler, Reiner Fischer, Martin Fublein, Peter Jeschke, Joachim Kluth, Friedrich August Mühlthau, Arnd Voerste, Olga Malsam, Ulrich Görgens, Yoshitaka Sato