Abstract: The present invention relates to novel 5,6-disubstituted oxindole derivatives and pharmaceutically acceptable salts thereof, and pharmaceutical compositions comprising such derivatives, and to the use of such derivatives for the manufacture of a medicament, and methods of treating disorders in a subject in need thereof, such as vasopressin-dependent disorders, using 5,6-disubstituted oxindole derivatives.
Type:
Grant
Filed:
September 27, 2013
Date of Patent:
September 6, 2016
Assignee:
ABBVIE DEUTSCHLAND GMBH & CO. KG
Inventors:
Wilfried Braje, Thorsten Oost, Astrid Netz, Wolfgang Wernet, Liliane Unger, Wilfried Hornberger, Wilfried Lubisch
Abstract: Disclosed are compounds, compositions and methods for treating various diseases, syndromes, conditions and disorders, including pain. Such compounds are represented by Formula I as follows: wherein R1, R2, ring A, and G are defined herein.
Type:
Grant
Filed:
August 16, 2013
Date of Patent:
September 6, 2016
Assignee:
Janssen Pharmaceutica NV
Inventors:
Mark Wall, Nalin Subasinghe, Zhihua Sui, Christopher Flores
Abstract: The present invention provides compounds represented by formula (1) below and pharmacologically acceptable salts thereof: wherein R1, R2, R3, and R4 are as defined in the claims.
Abstract: The present invention relates to inhibitors of the oncogenic protein kinase ALK of formula (I) as herein described and pharmaceutical compositions thereof, as well as to key intermediates towards their synthesis. The compounds of formula (I) are useful in the preparation of a medicament, in particular for the treatment of cancer.
Type:
Grant
Filed:
May 10, 2013
Date of Patent:
August 30, 2016
Assignees:
UNIVERSITA DEGLI STUDI DI MILANO—BICOCCA, UNIVERSITE DE GENEVE, UNIVERSITE CLAUDE BERNARD—LYON
Inventors:
Carlo Gambacorti-Passerini, Luca Mologni, Leonardo Scapozza, William Bisson, Shaheen Ahmed, Peter Goekjian, Sébastien Tardy, Alexandre Orsato, David Gueyrard, Joseph Benoit
Abstract: The specification generally relates to compounds of Formula (I): and pharmaceutically acceptable salts thereof, where Q, R1, R2, R3, R4 and R5 have any of the meanings defined herein. The specification also relates to the use of such compounds and salts thereof to treat or prevent ATM kinase mediated disease, including cancer. The specification further relates to crystalline forms of compounds of imidazo[4,5-c]quinolin-2-one compounds and pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds and salts; kits comprising such compounds and salts; methods of manufacture of such compounds and salts; intermediates useful in the manufacture of such compounds and salts; and to methods of treating ATM kinase mediated disease, including cancer, using such compounds and salts.
Type:
Grant
Filed:
May 5, 2015
Date of Patent:
August 30, 2016
Assignee:
AstraZeneca AB
Inventors:
Bernard Christophe Barlaam, Kurt Gordon Pike
Abstract: The present invention provides compounds of Formula (I): as defined in the specification and compositions comprising any of such novel compounds. These compounds are antagonists of P2Y1 receptor and may be used as medicaments in the treatment and/or prophylaxis of thromboembolic disorders.
Type:
Grant
Filed:
July 30, 2013
Date of Patent:
August 30, 2016
Assignee:
Bristol-Myers Squibb Company
Inventors:
Carl Thibeault, Charles G. Clark, Indawati DeLucca, Carol Hui Hu, Yoon Jeon, Patrick Y. S. Lam, Jennifer X. Qiao, Wu Yang, Yufeng Wang, Tammy C. Wang
Abstract: The present disclosure relates to compounds that are sodium channel inhibitors and to their use in the treatment of various disease states, including cardiovascular diseases and diabetes. In particular embodiments, the structure of the compounds is given by Formula I: wherein X, Y, Z, R2, R3, R4, p and q are as described herein, to methods for the preparation and use of the compounds and to pharmaceutical compositions containing the same.
Type:
Grant
Filed:
December 3, 2014
Date of Patent:
August 16, 2016
Assignee:
Gilead Scineces, Inc.
Inventors:
Michael Graupe, Yafan Lu, Jeff A. Zablocki
Abstract: A new class of ligands derived from benzo[h]quinoline are described and these ligands are used to prepare several novel transition metal complexes. The complexes are preferably of the group VIII transition metals iron, ruthenium or osmium, with the benzo[h]quinoline ligands acting as tridentate ligands. The complexes described are proved to be very active catalysts for the reduction of ketones and aldehydes to alcohols, via hydrogen transfer and hydrogenation reactions. These compounds hence can be usefully employed as catalysts in said reduction reactions.
Type:
Grant
Filed:
November 19, 2013
Date of Patent:
August 9, 2016
Assignee:
Universita' Degli Studi Di Udine
Inventors:
Pierluigi Rigo, Walter Baratta, Katia Siega, Giorgio Adolfo Chelucci, Maurizio Ballico, Santo Magnolia
Abstract: The present invention relates to apoptosis signal-regulating kinase 1 (“ASK1”) inhibiting compounds of the formula wherein the variables are as defined herein. The invention also relates to pharmaceutical compositions, kits and articles of manufacture comprising such compounds; methods and intermediates useful for making the compounds; and methods of using said compounds.
Abstract: The invention relates to pyran spirocyclic piperidine amide compounds useful as inhibitors of ion channels. The invention also provides pharmaceutically acceptable compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various disorders.
Type:
Grant
Filed:
January 15, 2013
Date of Patent:
August 2, 2016
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Sara Sabina Hadida-Ruah, Vijayalaksmi Arumugam, Michael Paul Deninno, Bryan A. Frieman, Edward Adam Kallel, Mark Thomas Miller, Johnny Uy, Jinglan Zhou
Abstract: Disclosed are compounds of Formula 1, or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, and R4 are defined in the specification. This disclosure also relates to materials and methods for preparing compounds of Formula 1, to pharmaceutical compositions which contain them, and to their use for treating Type I hypersensitivity reactions, autoimmune diseases, inflammatory disorders, cancer, non-malignant proliferative disorders, and other conditions associated with BTK.
Type:
Grant
Filed:
March 10, 2014
Date of Patent:
August 2, 2016
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
John David Lawson, Mark Sabat, Nicholas Scorah, Christopher Smith, Phong H. Vu, Haixia Wang
Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.
Type:
Grant
Filed:
September 14, 2011
Date of Patent:
July 19, 2016
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Daniel G. Genov, Brian C. Austad, Brian H. White
Abstract: An object of the present invention is to provide a pyrroloquinoline quinone tetraalkali salt needing no special reagent, having a high solubility in a solvent, being capable of providing a high-concentration pyrroloquinoline quinone aqueous solution, being hardly changed in color even if being concurrently used with ascorbic acid, and being of a high quality and a high purity; a crystal of a pyrroloquinoline quinone tetrasodium salt; a composition; and a simple method for producing the pyrroloquinoline quinone tetraalkali salt. The pyrroloquinoline quinone tetraalkali salt is represented by the formula (1): wherein M is each independently one selected from the group consisting of Li, K, Na, Rb and Cs.
Abstract: The disclosure relates to Compounds of Formula (I): and pharmaceutically acceptable derivatives thereof wherein Ar1, Ar2, L1, L2, X, R3, R22, and m are as defined herein, compositions comprising an effective amount of a Compound of Formula (I), and methods for treating or preventing a condition such as pain, UI, an ulcer, IBD and IBS, comprising administering to an animal in need thereof an effective amount of a Compound of Formula (I).
Abstract: A transition metal-containing compound having a tridentate chiral ligand bound to iron, cobalt, or nickel. The tridentate ligands are bound to the metal via nitrogen, phosphorus, and/or arsenic atoms. The tridentate ligand has a chiral group bound at least one of the nitrogen, phosphorus, and arsenic atoms, and a blocking group may be bound to another one of the nitrogen, phosphorus, and arsenic atoms. The transition metal-containing compound is useful for the catalyzing the asymmetric hydrogenation of olefins.
Type:
Grant
Filed:
August 20, 2012
Date of Patent:
July 19, 2016
Assignee:
The Trustees of Princeton University
Inventors:
Paul J. Chirik, Sebastien Monfette, Jordan M. Hoyt, Max R. Friedfeld
Abstract: Described herein are compounds of Formula (I), pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof. Compounds of the present invention are useful for inhibiting arginine methyltransferase activity. Methods of using the compounds for treating arginine methyltransferase-mediated disorders are also described.
Type:
Grant
Filed:
March 14, 2014
Date of Patent:
July 19, 2016
Assignee:
Epizyme, Inc.
Inventors:
Richard Chesworth, Lorna Helen Mitchell, Gideon Shapiro, Kevin Wayne Kuntz
Abstract: The present invention relates to a novel nickel complex and its derivatives, which mimic the active site of Ni-containing superoxide dismutase (NiSOD). The five-coordinate Ni(II) and Ni(III) complexes or their derivatives, and six-coordinate derivatives have the following structures of formula (I) and (II): The nickel complexes and their derivatives of the invention act as anti-oxidants or free radical scavengers. The invented nickel complexes can be used in the preparation of medicines, health foods or cosmetics for human, animals and plants, or can be used in environmental or soil protection.
Type:
Grant
Filed:
October 30, 2013
Date of Patent:
July 12, 2016
Assignee:
NATIONAL TAIWAN NORMAL UNIVERSITY
Inventors:
Way-Zen Lee, Chien-Wei Chiang, Tsung-Han Lin, Ting-Shen Kuo
Abstract: Provided herein is a process for the transfer-hydrogenation of ketone analogs of members of the jervine type of Veratrum alkaloids, such as cyclopamine. Also provided herein are novel ruthenium transfer-hydrogenation catalysts.
Type:
Grant
Filed:
September 14, 2011
Date of Patent:
June 28, 2016
Assignee:
Infinity Pharmaceuticals, Inc.
Inventors:
Daniel G. Genov, Brian C. Austad, Brian H. White