Abstract: 5-(Difluoromethyl)pyrazine-2-carboxylic acid, which is a raw material for the construction of 5-(difluoromethyl)pyrazine-2-carboxamide, which is a common partial structural motif of the compound having an A? production inhibitory action or a BACE1 inhibitory action, can be industrially advantageously produced by decarboxylating 5-[carboxy(difluoro)methyl]pyrazine-2-carboxylic acid, which is obtainable from 5-chloropyrazine-2-carboxylate.
Type:
Grant
Filed:
April 25, 2013
Date of Patent:
January 5, 2016
Assignee:
Eisai R&D Management Co., Ltd.
Inventors:
Kazuhiro Yoshizawa, Masayuki Omori, Yuzo Watanabe, Mitsuo Nagai, Masabumi Takahashi, Francis G. Fang
Abstract: The present invention relates to disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof, the use of these derivatives as pharmaceutically active agents, especially for the prophylaxis and/or treatment of infectious diseases, including opportunistic diseases, immunological diseases, autoimmune diseases, cardiovascular diseases, cell proliferative diseases, inflammation, erectile dysfunction and stroke, and pharmaceutical compositions containing at least one of said disubstituted triazine derivatives and/or pharmaceutically acceptable salts thereof. Furthermore, the present invention relates to the use of said disubstituted triazine derivatives as inhibitors for a protein kinase.
Type:
Grant
Filed:
March 1, 2012
Date of Patent:
January 5, 2016
Assignee:
Bayer Intellectual Property GMBH
Inventors:
Gerd Rühter, Uwe Koch, Peter Nussbaumer, Carsten Schulz-Fademrecht, Jan Eickhoff
Abstract: In one aspect, the invention relates to compounds having the formula: wherein: Ar, Z, R3, R4 and R5 are as defined in the specification, or a pharmaceutically acceptable salt thereof. These compounds have AT1 receptor antagonist activity and neprilysin inhibition activity. In another aspect, the invention relates to pharmaceutical compositions comprising such compounds; methods of using such compounds; and process and intermediates for preparing such compounds.
Type:
Grant
Filed:
December 18, 2014
Date of Patent:
December 22, 2015
Assignee:
Theravance Biopharma R&D IP, LLC
Inventors:
Paul R. Fatheree, Robert Murray McKinnell
Abstract: Described herein are novel platinum-based compounds having the formula: and methods of using platinum-based compounds in the treatment of diseases, such as cancer, that are associated with cells expressing solute transporter proteins.
Type:
Grant
Filed:
February 7, 2014
Date of Patent:
December 22, 2015
Assignee:
The Regents of the University of California
Abstract: There is provided a metalloporphyrin complex represented by general formula (1): wherein M is a metal; A1 to A4 are independently of each other a substituent represented by general formula (2): -D-E+X???(2) wherein D is a divalent organic group having 1 to 20 carbon atoms; E+ is a quaternary ammonium group or quaternary phosphonium group having 3 to 60 carbon atoms; and X is a halogen atom. There is thus provided a metalloporphyrin complex which, when used as a carbon dioxide fixation catalyst, exhibits high catalytic activity, has a small environmental burden and can be easily synthesized.
Type:
Grant
Filed:
September 19, 2012
Date of Patent:
December 15, 2015
Assignee:
NATIONAL UNIVERSITY CORPORATION OKAYAMA UNIVERSITY
Inventors:
Tadashi Ema, Takashi Sakai, Yuki Miyazaki
Abstract: Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
Abstract: Embodiments describe methods of synthesizing metal mesoporphyrin compounds. In embodiments, a metal mesoporphyrin compound may be formed by hemin transmetallation and subsequent hydrogenation of the tin protoporphyrin IX to form a metal mesoporphyrin. In other embodiments, a method of synthesizing a metal mesoporphyrin compound comprises forming a protoporphyrin methyl ester from hemin and converting the protoporphyrin methyl ester intermediate to a metal mesoporphyrin compound through metal insertion and hydrogenation. In other embodiments, a metal mesoporphyrin compound may be formed from hemin by a hydrogen-free hydrogenation method to form a mesoporphyrin IX intermediate followed by metal insertion and hydrogenation. In embodiments, a method of synthesizing a metal mesoporphyrin compound comprises forming a mesoporphyrin IX dihydrochloride intermediate compound and converting the mesoporphyrin IX intermediate to a metal mesoporphyrin compound through metal insertion.
Abstract: The present invention relates generally to the field of treatment and prophylaxis of retinal degenerative diseases. More particularly, the present invention contemplates a method for preventing, reducing the risk of development of, or otherwise treating or ameliorating the symptoms of, age-related macular degeneration (AMD) or related retinal conditions in mammals and in particular humans. The present invention further provides therapeutic compositions enabling dose-dependent or dose-specific administration of agents useful in the treatment and prophylaxis of age-related macular degeneration or related retinal degenerative conditions.
Abstract: The present invention provides biologically active compounds that can be used as photosensitizers for diagnostic and therapeutic applications, particularly for PDT of cancer, infections and other hyperproliferative diseases, fluorescence diagnosis and PdT treatment of a non-tumorous indication such as arthritis, inflammatory diseases, viral or bacterial infections, dermatological, ophthalmological or urological disorders.
Type:
Grant
Filed:
August 12, 2011
Date of Patent:
October 13, 2015
Assignee:
Biolitec Pharma Marketing LTD
Inventors:
Daniel Aicher, Arno Wiehe, Christian B. W. Stark, Volker Albrecht, Susanna Gräfe
Abstract: The present application relates to novel substituted imidazopyridazines having the following formula (I): to processes for their preparation, to their use, alone or in combinations, for the treatment and/or prophylaxis of diseases and to their use for production of medicaments for the treatment and/or prophylaxis of diseases, especially for the treatment and/or prophylaxis of cardiovascular disorders.
Inventors:
Markus Follmann, Johannes-Peter Stasch, Gorden Redlich, Alexander Straub, Jens Ackerstaff, Nils Griebenow, Andreas Knorr, Frank Wunder, Volkhart Min-Jian Li
Abstract: The invention relates to new sulfonamide Nav1.7 inhibitors and pharmaceutically acceptable salts thereof, to their use in medicine, to compositions containing them, to processes for their preparation and to intermediates used in such processes. Nav 1.7 inhibitors are potentially useful in the treatment of a wide range of disorders, particularly pain.
Type:
Grant
Filed:
June 28, 2011
Date of Patent:
September 29, 2015
Assignees:
Pfizer Limited, Icagen, Inc.
Inventors:
Christopher John Markworth, Brian Edward Marron, David James Rawson, Robert Ian Storer, Nigel Alan Swain, Christopher William West, Shulan Zhou
Abstract: The invention relates to a new solvate, Vilazodone hydrochloride monoethanol monohydrate solvate, and to a process for the preparation of polymorphic form III of Vilazodone hydrochloride via the Vilazodone hydrochloride monoethanol monohydrate solvate.
Type:
Grant
Filed:
July 9, 2014
Date of Patent:
September 29, 2015
Assignee:
Sandoz AG
Inventors:
Marijan Stefinovic, Clemens Haefele, Ulrich J. Griesser
Abstract: The invention provides novel heterocyclic carboxamide compounds according to Formula (I), their manufacture, and use for the treatment of hyperproliferative diseases, such as cancer.
Type:
Grant
Filed:
December 17, 2012
Date of Patent:
September 22, 2015
Assignee:
Merck Patent GmbH
Inventors:
Bayard R. Huck, Xiaoling Chen, Yufang Xiao, Ruoxi Lan, Lizbeth Celeste De Selm, Constantin Neagu, Justin Potnick, Srinivasa R. Karra, Theresa L. Johnson
Abstract: Provided herein are compounds, such as compounds of Formula I, that bind to androgen receptors and/or modulate activity of androgen receptors. Also provided are methods for making and using such compounds. Also provided are compositions including such compounds and methods for making and using such compositions.
Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, and the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
Abstract: The present invention relates to compounds of general formula (I) and the tautomers and the salts thereof, particularly the pharmaceutically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on epithelial sodium channels, the use thereof for the treatment of diseases, particularly diseases of the lungs and airways.
Type:
Grant
Filed:
July 14, 2014
Date of Patent:
September 8, 2015
Assignee:
Boehringer Ingelheim International GmbH
Inventors:
Joerg Kley, Sara Frattini, Dieter Hamprecht
Abstract: The present invention relates to certain substituted 1,2,3,4-tetrahydrocyclopenta[b]indol-3-yl)acetic acid derivatives of Formula (Ia) and pharmaceutically acceptable salts thereof, which exhibit useful pharmacological properties, for example, as agonists of the S1P1 receptor. Also provided by the present invention are pharmaceutical compositions containing compounds of the invention, and methods of using the compounds and compositions of the invention in the treatment of S1P1 receptor-associated disorders, for example, psoriasis, rheumatoid arthritis, Crohn's disease, transplant rejection, multiple sclerosis, systemic lupus erythematosus, ulcerative colitis, type I diabetes, acne, microbial infections or diseases and viral infections or diseases.
Type:
Grant
Filed:
October 8, 2013
Date of Patent:
September 8, 2015
Assignee:
Arena Pharmaceuticals, Inc.
Inventors:
Robert M. Jones, Daniel J. Buzard, Sangdon Han, Sun Hee Kim, Juerg Lehmann, Brett Ullman, Jeanne V. Moody, Xiuwen Zhu, Scott Stim
Abstract: A compound of the formula (I): where R1 or R2 is a cyclc amine group and R5 is an aromatic group with a carbonyl containing substituent for use as a FAK inhibitor.
Type:
Grant
Filed:
July 6, 2012
Date of Patent:
September 1, 2015
Assignee:
Cancer Therapeutics CRC PTY LTD
Inventors:
Ian Peter Holmes, Ylva Bergman, Gillian Elizabeth Lunniss, Marica Nikac, Neil Chol, Catherine Fae Hemley, Scott Raymond Walker, Richard Charles Foitzik, Danny Ganame, Romina Lessene
Abstract: The present invention provides compounds of formula (I) and compounds of formula (VII-a) as well as pharmaceutical compositions comprising said compounds and their use as PARP inhibitors wherein n, R1, R2, R3, R4, R5, R6, R7, Re, Rd and X have defined meanings.
Type:
Grant
Filed:
April 25, 2013
Date of Patent:
August 25, 2015
Assignee:
Janssen Pharmaceutica, NV
Inventors:
Dominique Jean-Pierre Mabire, Jerome Emile Georges Guillemont, Jacobus Alphonsus Josephus van Dun, Maria Victorina Francisca Somers, Walter Boudewijn Leopold Wouters
Abstract: A core of a cyclic structure represented by (—N—(CH2)n—)k is bonded to a dendrimer-type side chain with a specific branched structure at all nitrogen atoms in the core to produce a compound with a specific structure for producing a metal complex that exhibits a T1-reducing effect, and the resulting compound is coordinated to a metal ion that has a T1-reducing effect to obtain a metal complex that exhibits an excellent T1-reducing effect which is useful as an effective component of an MRI contrast agent and an MRI contrast agent using the same.