Abstract: This invention relates to compounds of the Formula (I): or a pharmaceutically acceptable salt, solvate or isomer thereof, which can be useful for the treatment of diseases or conditions mediated by MMPs, ADAMs, TACE, aggrecanase, TNF-? or combinations thereof.
Type:
Grant
Filed:
January 20, 2010
Date of Patent:
May 15, 2012
Assignee:
Schering Corporation
Inventors:
Brian J. Lavey, Joseph A. Kozlowski, Guowei Zhou, Ling Tong, Wensheng Yu, Michael K. C. Wong, Shankar B. Bandarpalle, Neng-Yang Shih, M. Arshad Siddiqui, Kristin E. Rosner, Chaoyang Dai, Janeta Popovici-Muller, Vinay M. Girijavallabhan, Dansu Li, Aneta Maria Kosinski, Seong-Heon Kim, De-Yi Yang, Razia K. Rizvi
Abstract: Kinetic stabilization of the native state of transthyretin is an effective mechanism for preventing protein misfolding. Because transthyretin misfolding plays an important role in transthyretin amyloid diseases, inhibiting such misfolding can be used as an effective treatment or prophylaxis for such diseases. Treatment methods are disclosed.
Type:
Grant
Filed:
June 9, 2009
Date of Patent:
May 1, 2012
Assignee:
The Scripps Research Institute
Inventors:
Jeffery W. Kelly, Evan T. Powers, Hossein Razavi
Abstract: The present invention relates to novel 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) in which A, D, G, W, X, Y and Z are as defined above, to a plurality of processes for the preparation and to their use as pesticides and/or herbicides and/or microbicides. Moreover, the invention relates to selective herbicidal compositions comprising both the 4-biphenyl-substituted pyrazolidine-3,5-dione derivatives of the formula (I) and a crop plant compatibility-improving compound.
Type:
Grant
Filed:
January 31, 2011
Date of Patent:
May 1, 2012
Assignee:
Bayer CropScience AG
Inventors:
Reiner Fischer, Thomas Bretschneider, Ernst Rudolf F. Gesing, Dieter Feucht, Karl-Heinz Kuck, Peter Lösel, Olga Malsam, Christian Arnold, Thomas Auler, Martin Jeffrey Hills, Heinz Kehne
Abstract: There is provided a novel LXR? agonist useful as a preventative and/or therapeutic agent for arteriosclerosis; arteriosclerosis such as those resulting from diabetes; hyperlipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases caused by inflammatory cytokines, skin diseases such as allergic skin diseases, diabetes or Alzheimer's disease. The agonist is a carbinol derivative represented by the following general formula (1) or salt thereof, or their solvate.
Abstract: The invention relates to substituted phenoxyacetic acids of formula (I), where the variables are as defined in claim 1, as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
April 24, 2012
Assignee:
AstraZeneca AB
Inventors:
Timothy Jon Luker, Timothy Nicholas Birkinshaw, Rukhsana Tasneem Mohammed
Abstract: The present invention relates to phenyl sulfonamides 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, including for example the treatment of pain.
Type:
Grant
Filed:
July 27, 2010
Date of Patent:
April 24, 2012
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Esther Martinborough, Lev T. D. Fanning, Urvi Sheth, Dean Wilson, Andreas P. Termin, Timothy D. Neubert, Nicole Hilgraf, Tara Leanne Hampton, Tara Whitney, Aarti Sameer Kawatkar, Danielle Lehsten, Dean Stamos, Jinglan Zhou, Vijayalaksmi Arumugam, Corey Anderson
Abstract: The present invention relates also to a process for the preparation of intermediate compounds useful in preparing the compounds of Formula (I) using the process of Scheme (II).
Type:
Grant
Filed:
December 18, 2007
Date of Patent:
April 24, 2012
Assignee:
Schering Corporation
Inventors:
George S. K. Wong, Hong-Chang Lee, Jennifer A. Vance, Weidong Tong, Tetsuo Iwama
Abstract: The invention provides a crystalline hydrochloride salt of (S)-3-[(S)-1-(4-chlorophenoxy)-2-methylpropyl]pyrrolidine. This invention also provides pharmaceutical compositions comprising the crystalline salt, processes and intermediates for preparing the crystalline salt, and methods of using the crystalline salt to treat diseases.
Abstract: Charged and neutral small fluorescent molecules based upon the styryl scaffold are useful as imaging agents for misfolded proteins such as amyloid plaque. Charged molecules are prepared using pyrrolidine catalyzed reactions by solution-phase synthesis. Neutral styryl molecules are prepared using acetic anhydride catalyzed reactions, Horner-Emmons reactions or Wittig reactions.
Type:
Grant
Filed:
February 11, 2008
Date of Patent:
April 17, 2012
Assignee:
New York University
Inventors:
Thomas Wisniewski, Jaeki Min, Qian Li, Young-Tae Chang
Abstract: The present invention relates to a method of treatment and/or prophylaxis of a microbial infection, comprising the step of administering an effective amount of a compound of formula (I), in which X and Y are either the same or different and selected from a heteroatom; is a double or single bond depending on the heteroatoms X and Y; R1 to R5 are either the same or different and selected from hydrogen or a non-deleterious substituent; and R6 and R7 are either the same or different and selected from hydrogen and a non-deleterious substituent or one of R6 and R7 are absent when there is a double bond present, pharmaceutically acceptable salts or derivatives, pro-drugs, tautomers and/or isomers thereof. The present invention also relates to a method for protecting a subject from radiation damage, a method of cancer radiotherapy and use as an antimicrobial or radioprotective agent of the compound of formula (I) defined above.
Type:
Grant
Filed:
May 10, 2010
Date of Patent:
April 17, 2012
Assignee:
Biodiem Ltd.
Inventors:
Peter Prokofievich Denisenko, Nikolay Sergeevich Sapronov, Alexander Alexandrovich Tarasenko
Abstract: The present invention provides for a process for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate, an intermediate useful in the efficient preparation of (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof, processes for preparing (1R,2S,5S)-methyl 6,6-dimethyl-3-azabicyclo[3,1,0]hexane-2-carboxylic acid and esters and salts thereof from the sulfonate intermediate and processes for preparing 6,6-Dimethyl-3-aza-bicyclo[3.1.0]hexane-2-sulfonate.
Abstract: The present invention relates to novel arylpyrrolines having the formula (I) and their use as insecticides, as well as to processes for the preparation of the arylpyrrolines wherein L, A1 to A4, Y1 to Y3, R1 to R3 are as defined in the specification of the patent application.
Abstract: The present invention related to compounds that bind to and modulate the activity of neuronal nicotinic acetylcholine receptors, to novel salts thereof, to processes for preparing these compounds, to pharmaceutical compositions containing these compounds, and to methods of using these compounds for treating a wide variety of conditions and disorders, including those associated with dysfunction of the central nervous system (CNS).
Abstract: [Object] To provide a novel LXR? agonist that is useful as a preventative and/or therapeutic agent for atherosclerosis; arteriosclerosis such as those resulting from diabetes; dyslipidemia; hypercholesterolemia; lipid-related diseases; inflammatory diseases that are caused by inflammatory cytokines; skin diseases such as allergic skin diseases; diabetes; or Alzheimer's disease. [Solving Means] A carbinol compound represented by the following general formula (I) or salt thereof, or their solvate.
Abstract: The invention relates to novel thiophene derivatives (I), their preparation and their use as pharmaceutically active compounds. Said compounds particularly act as immunomodulating agents. Formula (I).
Type:
Grant
Filed:
December 9, 2008
Date of Patent:
April 3, 2012
Assignee:
Actelion Pharmaceuticals Ltd.
Inventors:
Martin Bolli, Cyrille Lescop, Boris Mathys, Claus Mueller, Oliver Nayler, Beat Steiner
Abstract: The present invention provides novel amide and sulfonamide substituted heterocyclic urea compounds having useful antibacterial activity. Use of these compounds as pharmaceutical compositions and method of their production are also provided.
Type:
Grant
Filed:
July 23, 2008
Date of Patent:
April 3, 2012
Assignee:
Crestone, Inc.
Inventors:
Joseph Guiles, Thale Jarvis, Sarah Strong, Xicheng Sun, Jian Qiu, John C. Rohloff
Abstract: Prodrugs of methyl hydrogen fumarate, pharmaceutical compositions comprising prodrugs of methyl hydrogen fumarate, and methods of using prodrugs of methyl hydrogen fumarate and pharmaceutical compositions thereof for treating diseases such as psoriasis, asthma, multiple sclerosis, inflammatory bowel disease, and arthritis are disclosed.
Type:
Grant
Filed:
August 19, 2009
Date of Patent:
April 3, 2012
Assignee:
XenoPort, Inc.
Inventors:
Archana Gangakhedkar, Xuedong Dai, Noa Zerangue, Peter A. Virsik
Abstract: The present invention discloses processes for producing ?-nitrocarbonyl and ?-dicarbonyl compounds, which can be precursors in the synthesis of pyrrole compounds. A process for producing pyrroles such as 2,5-dimethylpyrrole, and structurally similar pyrrole compounds, is also disclosed.
Abstract: The present invention is directed to compounds of Formula I: (where variables A1, A2, B, J, K, m, n, R4, R5a, R5b and R5c are as defined herein) useful as antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as headache, migraine and cluster headache. 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.
Type:
Grant
Filed:
March 7, 2008
Date of Patent:
April 3, 2012
Assignee:
Merck, Sharp & Dohme, Corp.
Inventors:
Craig A. Stump, Ian M. Bell, Harold G. Selnick
Abstract: The invention concerns tricyclic N-heteroarylcarboxamide derivatives containing a benzimidazole unit of general formula (I): Wherein A, P, Y, R1, R2 and R3 are as defined herein. The invention also concerns a method of preparing the compounds and their therapeutic use.
Type:
Grant
Filed:
August 1, 2008
Date of Patent:
March 27, 2012
Assignee:
Sanofi-Aventis
Inventors:
Laurent Dubois, Yannick Evanno, Luc Even, Catherine Gille, Andre Malanda, David Machnik, Nathalie Rakotoarisoa