Abstract: The present application relates to novel substituted 1-[3-(heterocyclyl)benzyl]-1H-pyrazole derivatives, to processes for preparation thereof, to use thereof for treatment and/or prevention of diseases and to use thereof for production of medicaments for treatment and/or prevention of diseases, more particularly for treatment and/or prevention of hyperproliferative and angiogenic diseases and those diseases which arise from metabolic adaptation to hypoxic states. Such treatments can be effected in the form of monotherapy or else in combination with other medicaments or further therapeutic measures.
Type:
Grant
Filed:
May 9, 2011
Date of Patent:
June 25, 2013
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Michael Härter, Hartmut Beck, Susanne Greschat, Peter Ellinghaus, Kerstin Berhörster, Joachim Schuhmacher
Abstract: The invention relates to a series of thiazoline and oxazoline derivatives, compositions thereof, and methods of treating conditions and disorders using such compounds.
Type:
Grant
Filed:
January 28, 2010
Date of Patent:
June 25, 2013
Assignee:
AbbVie Inc.
Inventors:
Ramin Faghih, Gregory A. Gfesser, Christopher L. Lynch, Murali Gopalakrishnan, Sujatha Gopalakrishnan, John Malysz, Earl J. Gubbins, Rachid El Kouhen, Jinhe Li, Kathy A. Sarris, Melissa J. Michmerhuizen, Ying Wang
Abstract: Described are novel compounds of the Formula (I), their derivatives, analogs, tautomeric forms, regioisomers, stereoisomers, polymorphs, solvates, intermediates, pharmaceutically acceptable salts, pharmaceutical compositions, metabolites and prodrugs thereof. These compounds are effective in lowering blood glucose, serum insulin, free fatty acids, cholesterol, triglyceride levels; treatment of obesity, inflammation, autoimmune diseases such as multiple sclerosis, rheumatoid arthritis; treatment and/or prophylaxis of type II diabetes. These compounds are more particularly dipeptidyl peptidase (DPP IV) inhibitors.
Abstract: The present invention provides an improved method of chromatographically separating the isomers of (1R,rR)-atracurium salts by high-performance liquid chromatography (HPLC), in the absence of a strong acid. The separation is preferably performed on a silica gel HPLC column using an eluent containing an organic solvent, a polar aprotic co-solvent and a weak organic acid.
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, to methods and intermediates useful for making the compounds, and to methods of using the compounds.
Type:
Grant
Filed:
March 30, 2009
Date of Patent:
June 11, 2013
Assignee:
Takeda Pharmaceutical Company Limited
Inventors:
Edcon Chang, Tracy Duong, Takehiro Hirano, Matthew H. McNiell, Yoshito Terao, Angie Vassar
Abstract: The present invention relates to compounds of Formula (I) and/or Formula (Ia): and to their salts, pharmaceutical compositions, methods of use, and methods for their preparation. These compounds inhibit ALK kinase activity, and thus may be used for the treatment of cancer.
Type:
Grant
Filed:
August 2, 2011
Date of Patent:
June 11, 2013
Assignee:
Astrazeneca AB
Inventors:
Brian Aquila, Victor Kamhi, Bo Peng, Timothy Pontz, Jamal Carlos Saeh, Kumar Thakur, Bin Yang
Abstract: The present invention relates to processes for the preparation of compounds useful as inhibitors of p38 kinase. The processes of the present invention are amenable for large scale preparation and produce stable phenyl-6-(1-(phenyl)ureido)nicotinamides in high purity and yields.
Type:
Grant
Filed:
August 22, 2012
Date of Patent:
June 11, 2013
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Stefanie Roeper, Adam R. Looker, Theodore A. Martinot, Bobbianna Neubert-Langille, Michael P. Ryan, John R. Snoonian
Abstract: The present invention relates generally to the field of therapy. The invention particularly relates to insulin sensitizers and methods of regulating glucose homeostasis and to the therapeutic or prophylactic treatment of diseases and associated conditions, in which impaired glucose uptake due to insulin resistance is involved or implicated, such as diabetes, syndrome X, hyperglycaemia, vascular disease and kidney disease. The present invention further relates to compounds and agents and compositions thereof for use in the treatment methods.
Type:
Grant
Filed:
January 25, 2008
Date of Patent:
June 4, 2013
Assignee:
Verva Pharmaceuticals Ltd.
Inventors:
Gregory Royce Collier, Kenneth Russell Walder, James Alexander Campbell, Juan-Carlos Molero-Navajas, Nicky Konstantopoulos, Guy Yeoman Krippner
Abstract: The present invention is directed to a compound represented by the following structural formula: or a pharmaceutically acceptable salt thereof. Pharmaceutical composition comprising a compound represented by Structural Formula (I) and method of use of these compound for inhibiting BACE activity in a subject in need of such treatment are also described.
Type:
Grant
Filed:
August 14, 2009
Date of Patent:
May 28, 2013
Assignee:
Vitae Pharmaceuticals, Inc.
Inventors:
Lawrence W. Dillard, Jing Yuan, Lanqi Jia, Yajun Zheng
Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as pharmaceutical compositions thereof and methods of use thereof relating to the treatment of cancer and other diseases.
Type:
Grant
Filed:
December 19, 2006
Date of Patent:
May 28, 2013
Assignee:
Incyte Corporation
Inventors:
Andrew P. Combs, Amy Takvorian, Wenyu Zhu, Richard B. Sparks
Abstract: Described herein are compounds that are antagonists of lysophosphatidic receptor(s). Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists, alone and in combination with other compounds, for treating LPA-dependent or LPA-mediated conditions or diseases.
Type:
Grant
Filed:
April 22, 2011
Date of Patent:
May 14, 2013
Assignee:
Amira Pharmaceuticals, Inc.
Inventors:
John Howard Hutchinson, Thomas Jon Seiders, Bowei Wang, Jeannie M. Arruda, Jeffrey Roger Roppe, Timothy Parr
Abstract: Substituted 3-(4-((1H-imidazol-1-yl)methyl)phenyl)-5-phenyl-1,2,4-oxadiazole derivatives which are useful as sphingosine-1-phosphate modulators and useful for treating a wide variety of disorders associated with modulation of sphingosine-1-phosphate receptors.
Abstract: The present invention relates to novel carboxamide compounds and their use for the manufacture of a medicament. The carboxamide compounds are inhibitors of calpain (calcium dependant cysteine proteases). The invention therefore also relates to the use of these carboxamide compounds for treating a disorder associated with an elevated calpain activity. The carboxamide compounds are compounds of the general formula I in which R1, R2, R3a, R3b, W, Y and X have the meanings mentioned in the claims and the description, the tautomers thereof and the pharmaceutically suitable salts thereof. In particular, the compounds have the general formula I-A.a? and I-A.a? in which m, E, R1, R3a, R3b, R2, Ry, Rw and Rw6* have the meanings mentioned in the claims, n is 0, 1 or 2, the tautomers thereof and the pharmaceutically suitable salts thereof.
Type:
Grant
Filed:
December 28, 2007
Date of Patent:
May 7, 2013
Assignee:
Abbott GmbH & Co. KG
Inventors:
Andreas Kling, Wilfried Hornberger, Helmut Mack, Achim Moeller, Volker Nimmrich, Dietmar Seeman, Wilfried Lubisch
Abstract: Substituted sulfonamide derivatives, a process for their preparation, pharmaceutical compositions containing these compounds, and to the use of substituted sulfonamide derivatives in the treatment or inhibition of pain and/or various disorders or disease states.
Type:
Grant
Filed:
August 24, 2010
Date of Patent:
May 7, 2013
Assignee:
Gruenenthal GmbH
Inventors:
Stefan Oberboersch, Melanie Reich, Stefan Schunk, Sabine Hees, Ruth Jostock, Michael Franz-Martin Engels, Achim Kless, Thomas Christoph, Klaus Schiene, Tieno Germann, Edward Bijsterveld
Abstract: An olefin metathesis process for converting a reactant olefin or a mixture of reactant olefins into one or more product olefins that are different from the reactant olefin(s). The process employs a catalyst system containing a carbene-generating agent and a bimetallic ruthenium complex comprising one or more ?-hydrido bridging ligands, and optionally containing di(t-butyl)phosphine. The catalyst system is advantageously active at process temperatures greater than 90° C. Cyclization metathesis and ring-opening polymerization metathesis are preferred olefin metathesis processes.
Abstract: Compounds, compositions and methods are provided which are useful in the treatment of diseases through the modulation of potassium ion flux through voltage-dependent potassium channels. More particularly, the invention provides heterocycles, compositions and methods that are useful in the treatment of central or peripheral nervous system disorders (e.g., migraine, ataxia, Parkinson's disease, bipolar disorders, trigeminal neuralgia, spasticity, mood disorders, brain tumors, psychotic disorders, myokymia, seizures, epilepsy, seizure, retinal degeneration, hearing and vision loss, Alzheimer's disease, age-related memory loss, learning deficiencies, anxiety, neuronal degeneration and motor neuron diseases, maintaining bladder control or treating urinary incontinence) and as neuroprotective agents (e.g., to prevent stroke and the like) by modulating potassium channels associated with the onset or recurrence of the indicated conditions.
Type:
Grant
Filed:
February 16, 2010
Date of Patent:
April 30, 2013
Assignee:
Icagen Inc.
Inventors:
Thomas Eugene Christos, George S. Amato, Robert N. Atkinson, Maria Graciela Barolli, Lilli Ann Wolf-Gouveia, Mark J. Suto
Abstract: A process is provided to produce 2,3,5,6-tetraaminotoluene. Highly pure salts of 2,3,5,6-tetraaminotoluene are produced via reduction of 2,6-diamino-3,5-dinitrotoluene. The 2,3,5,6-tetraaminotoluene salt is precipitated as a clean (>99% purity) product. The salt is a precursor for monomers to make a polybenzimidazole for high performance fibers.
Abstract: Disclosed is a separated fraction of a reaction product of an enzymatically catalyzed polymerization of a flavonoid. The separated fraction is highly resistant to oxidation and is useful in numerous applications such as an antioxidant in food products and medical applications.
Type:
Grant
Filed:
March 8, 2010
Date of Patent:
April 30, 2013
Assignee:
The United States of America as Represented by the Secretary of the Army
Inventors:
Kenneth Racicot, Nicole Favreau, Ferdinando Bruno
Abstract: A multi-step method for the continuous synthesis of ibuprofen or a synthetic precursor of ibuprofen is provided that does not require any intermediate purification or isolation steps and uses reagents compatible with downstream reactions. According to some embodiments, a method is provided wherein isobutylbenzene and a propionyl compound may be converted into a first product in a first Friedel Crafts acylation reaction. The first product may then be converted into a second product in a 1,2-aryl migration reaction. Finally, the second product may be converted into ibuprofen in a hydrolysis reaction. The present invention also provides a method wherein only the first and second reaction steps or only the second and third reaction steps are performed. An apparatus is also provided having two or more microreactors and two or more junctions in particular arrangements for the synthesis of ibuprofen or a synthetic precursor of ibuprofen.
Type:
Grant
Filed:
August 26, 2010
Date of Patent:
April 23, 2013
Assignee:
Florida State University Research Foundation
Inventors:
D. Tyler McQuade, Andrew Bogdan, Sarah Lihoa Poe
Abstract: Pleckstrin homology domain binding compounds, pharmaceutical compositions including such compounds, and methods for their use are described herein.
Type:
Grant
Filed:
April 14, 2009
Date of Patent:
April 16, 2013
Assignees:
Board of Regents, The University of Texas System, Arizona Board of Regents on Behalf of the University of Arizona
Inventors:
Daruka Mahadevan, Emmanuelle J. Meuillet, Eugene A. Mash, Jr., Vijay M. Gohkale, Garth Powis, Shuxing Zhang