Abstract: The present invention relates to compounds of general formula (I), wherein R1, LP, LQ, (Het)Ar, m and n are as defined in the application, which have valuable pharmacological properties, and in particular bind to the GPR1 19 receptor and modulate its activity.
Type:
Grant
Filed:
September 3, 2013
Date of Patent:
October 18, 2016
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Bernd Nosse, Andreas Blum, Armin Heckel, Frank Himmelsbach, Neil J. Ashweek, Nicole Harriott
Abstract: Agents for modulating methyl modifying enzymes, compositions and uses thereof are provided herein.
Type:
Grant
Filed:
August 28, 2015
Date of Patent:
October 18, 2016
Assignee:
Constellation Pharmaceuticals, Inc.
Inventors:
Brian K. Albrecht, James Edmund Audia, Les A. Dakin, Victor S. Gehling, Jean-Christophe Harmange, Christopher G. Nasveschuk, Rishi G. Vaswani
Abstract: Described are novel salts of the compound (3R,4R,5S)-5-(difluoromethyl) piperidine-3,4-diol, as well as methods of using the same for preventing and/or treating lysosomal storage disorders and/or degenerative disorders of the central nervous system. In particular, the present invention provides methods for preventing and/or treating Gaucher's disease and/or Parkinson's disease.
Type:
Grant
Filed:
March 7, 2013
Date of Patent:
October 11, 2016
Assignee:
Amicus Therapeutics, Inc.
Inventors:
Robert Boyd, Philip J. Rybczynski, Kamlesh Sheth
Abstract: This disclosure is directed to pyrido[4,3-b]indoles having rigid moieties. The compounds in one embodiment are pyrido[4,3-b]indoles having an unsaturated hydrocarbon moiety. The compounds in another embodiment are pyrido[4,3-b]indoles having a cycloalkyl, cycloalkenyl or heterocyclyl moiety. Pharmaceutical compositions comprising the compounds are also provided, as are methods of using the compounds in a variety of therapeutic applications, including the treatment of a cognitive disorder, psychotic disorder, neurotransmitter-mediated disorder and/or a neuronal disorder.
Type:
Grant
Filed:
November 3, 2014
Date of Patent:
October 4, 2016
Assignee:
MEDIVATION TECHNOLOGIES, INC
Inventors:
David T. Hung, Andrew A. Protter, Rajendra Parasmal Jain, Sarvajit Chakravarty
Abstract: This invention relates to 5-substituted isoindoline compounds, and pharmaceutically acceptable salts, solvates, stereoisomers, and prodrugs thereof. Methods of use, and pharmaceutical compositions of these compounds are disclosed.
Type:
Grant
Filed:
September 18, 2014
Date of Patent:
September 20, 2016
Assignee:
Celgene Corporation
Inventors:
George W. Muller, Roger Shen-Chu Chen, Alexander L. Ruchelman
Abstract: Compounds and salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof and uses thereof are described. In certain aspects and embodiments, the described compounds or salts thereof, formulations thereof, conjugates thereof, derivatives thereof, forms thereof are active on each of B-Raf, B-Raf V600E and c-Raf-1 protein kinase. In certain aspects and embodiments, the described compounds are active in inhibiting proliferation of a Ras mutant cell line.
Type:
Grant
Filed:
October 14, 2014
Date of Patent:
September 13, 2016
Assignee:
Plexxikon Inc.
Inventors:
Prabha N. Ibrahim, Guoxian Wu, Jack Lin, Wayne Spevak, Hanna Cho, Todd Ewing, Chao Zhang
Abstract: The invention relates to benzimidazole-carboxamide 5-HT4 receptor agonist compounds of formula (I) wherein R1 and X are as defined in the specification, or a pharmaceutically acceptable salt or solvate or stereoisomer thereof. The invention also relates to pharmaceutical compositions comprising such compounds, methods of using such compounds to treat diseases associated with 5-HT4 receptor activity, and processes and intermediates useful for preparing such compounds.
Type:
Grant
Filed:
September 17, 2014
Date of Patent:
August 30, 2016
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Robert Murray McKinnell, Lan Jiang, Daniel D. Long
Abstract: The present invention relates to novel antiviral active 5-{4-[1H-imidazol-5-ylaryl(or hetaryl)]-buta-1,3-diynyl}-1H-imidazoles of the general formula 1 and pharmaceutically acceptable salt thereof, pharmaceutical composition, antiviral medicament, therapeutic kit for prophylaxis and treatment of hepatisis C virus diseases, and method for prophylaxis and treatment of hepatisis C. wherein: R1 and R2—represent optionally identical radicals selected from 2.1 and 2.2, where an asterisk (*) denotes the position of attachment to the imidazole fragment, (S) and (R) are types of chiral centers; R3 is isopropyl or phenyl radicals; Ar an aromatic or heteroaromatic diradical.
Abstract: This invention relates to organic chemistry, in particular to processes for the preparation of pyrazoline carboxamidine derivatives of formula (I), known as potent 5-HT6 antagonists. The invention also relates to novel intermediates of these compounds. wherein the symbols have the meanings given in the description.
Type:
Grant
Filed:
January 27, 2011
Date of Patent:
August 23, 2016
Assignee:
Abbvie Bahamas Ltd.
Inventors:
Arnold van Loevezijn, Josephus H. M. Lange, Gerrit A. Barf, Arnold P. den Hartog
Abstract: The disclosure relates particularly to certain carboxamide, sulfonamide and amine compounds and pharmaceutical compositions thereof, and to methods of treating and ameliorating disorders and conditions related to the adiponectin pathway, sphingolipid metabolism, oxidative stress, mitochondrial dysfunction, free radical damage and metabolic inefficiency, among others. In certain embodiments, the compounds have the structures (I-1), (2-I) and (3-I) in which the variables are as described herein.
Type:
Grant
Filed:
January 31, 2013
Date of Patent:
August 9, 2016
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Dane Goff, Donald Payan, David Carroll, Simon Shaw, Hitoshi Yasumichi
Abstract: The present application relates to a process for preparing chloroamines which can be used as precursors for syntheses of fine chemicals and active ingredients from pharmaceuticals and/or agriculture, by reaction of secondary amines of the formula (II) with chlorine gas in the presence of an aqueous alkali metal or alkaline earth metal oxide base.
Abstract: The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.
Abstract: A process for preparing fexofenadine is described, which provides for the hydrolysis of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid-alkyl ester, in a mixture of water and optionally an organic solvent, in the presence of a base; the carboxylate salt of 4-[4-[4-(hydroxydiphenylmethyl)-1-piperidyl]-1-oxobutyl]-?,?-dimethylbenzeneacetic acid is thus obtained, which is then directly reduced as carboxylate in a basic environment with hydrogen in the presence of a suitable hydrogenation catalyst to give the carboxylate of fexofenadine, which is precipitated by neutralization of the solution.
Type:
Grant
Filed:
July 25, 2007
Date of Patent:
August 2, 2016
Assignee:
Euticals SPA
Inventors:
Giorgio Bertolini, Maurizio Gallina, Giuseppe Motta, Domenico Vergani
Abstract: The present invention relates to particulate forms of anamorelin monohydrochloride or a composition comprising anamorelin monohydrochloride having controlled chloride content, preferably isolated in an amorphous and/or fine particulate state, processes for making the particulate forms, and pharmaceutical compositions comprising the particulate forms.
Type:
Grant
Filed:
November 12, 2014
Date of Patent:
August 2, 2016
Assignees:
Ono Pharmaceuticals Co., Ltd., Helsinn Healthcare SA
Inventors:
Shin-Itsu Kuwabe, Takehiko Yanagimachi, Hideyuki Yoshiyama, Seemon Pines, Eleanor De Groot, Silvina Garcia Rubio, Peter Manini
Abstract: The invention provides a crystalline hydrochloride salt of 1-isopropyl-2-oxo-1,2-dihydroquinoline-3-carboxylic acid {(1S,3R,5R)-8-[(R)-2-hydroxy-3-(methanesulfonyl-methyl-amino)propyl]-8-azabicyclo[3.2.1]oct-3-yl}amide or a solvate thereof. The invention also provides pharmaceutical compositions comprising such crystalline salt forms, methods of using such crystalline salt forms to treat diseases associated with 5-HT4 receptor activity, and processes useful for preparing such crystalline salt forms.
Type:
Grant
Filed:
August 3, 2015
Date of Patent:
August 2, 2016
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Paul R. Fatheree, S. Derek Turner, Adam A. Goldblum, Robert S. Chao, Daniel Genov
Abstract: The present invention provides a compound of the Formula II: wherein X is: R1 is H, —CN, or F; R2 is H or methyl; R3 is H; and R4 is H, methyl, or ethyl; or R3 and R4 joined together form a cyclopropyl ring; or a pharmaceutically acceptable salt thereof.
Type:
Grant
Filed:
January 13, 2015
Date of Patent:
August 2, 2016
Assignee:
Eli Lilly and Company
Inventors:
Matthew Allen Schiffler, Jeremy Schulenburg York
Abstract: The present invention relates to synthetic green tea derived polyphenolic compounds, their modes of syntheses, and their use in inhibiting proteasomal activity and in treating cancers. The present invention is also directed to pharmaceutical compositions useful in methods of inhibiting proteasomes and of treating cancers.
Type:
Grant
Filed:
October 18, 2013
Date of Patent:
July 26, 2016
Assignees:
UNIVERSITY OF SOUTH FLORIDA, MCGILL UNIVERSITY, THE HONG KONG POLYTECHNIC UNIVERSITY
Inventors:
Q. Ping Dou, Tak-Hang Chan, David M. Smith
Abstract: Heterocyclic compounds which modulate cannabinoid receptors are presented. Pharmaceutical compositions containing these compounds, methods of using these compounds as modulators of cannabinoid receptors and processes for synthesizing these compounds are also described herein.
Abstract: The present invention provides new processes for the preparation of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds which are useful, for example, for preventing or treating diseases or conditions related to an abnormally high level or activity of TNF-?. The invention can provide improved and/or efficient processes for the commercial production of unsubstituted and substituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione compounds, including, but not limited to, unsubstituted 4-amino-2-(2,6-dioxopiperidin-3-yl)isoindoline-1,3-dione.
Type:
Grant
Filed:
April 29, 2014
Date of Patent:
July 19, 2016
Assignee:
Celgene Corporation
Inventors:
Chuansheng Ge, George W. Muller, Roger Chen, Manohar Tukaram Saindane
Abstract: Heteroarylpiperidine and -piperazine derivatives of the formula (I) in which the symbols RA1, RA2, X, Y, L1, L2, RB1, RB2, G, Q, p, R1, R2 and R10 are each as defined in the description, and salts, metal complexes and N-oxides of the compounds of the formula (I), and the use thereof for controlling phytopathogenic harmful fungi and processes for preparing compounds of the formula (I).
Type:
Grant
Filed:
December 21, 2012
Date of Patent:
June 28, 2016
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Tomoki Tsuchiya, Pierre Wasnaire, Sebastian Hoffmann, Thomas Seitz, Stefan Hillebrand, Juergen Benting, Jan Peter Schmidt, Pierre Cristau