Abstract: The present invention provides ?-hydroxy-?-aminophosphonates, ?-amino-?-aminophosphonates, and analogs thereof that inhibit carnitine acyltransferases. The invention also provides compositions comprising these ?-hydroxy-?-aminophosphonates, ?-amino-?-aminophosphonates, and analogs, and methods of the use of such compounds and compositions in the treatment, amelioration or prevention of pathological conditions, diseases or disorders that are linked with fatty acid metabolism, such as non-insulin dependent diabetes or obesity. The invention also provides processes for the preparation of such compounds and compositions.
Type:
Grant
Filed:
March 22, 2012
Date of Patent:
September 17, 2013
Assignee:
Nucitec S.A. de C.V.
Inventors:
Ricardo Abraham De La Cruz Cordero, Miguel Ångel Duarte Vázquez, Jorge Luis Rosado Loria
Abstract: The present invention relates to novel indole derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
November 10, 2011
Date of Patent:
September 10, 2013
Assignee:
Allergan, Inc.
Inventors:
Santosh C. Sinha, Smita S. Bhat, Ken Chow, Michael E. Garst, Wha Bin Im
Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
Abstract: This invention relates to deuterated compounds that are useful in electroluminescent applications. It also relates to electronic devices in which the active layer includes such a deuterated compound.
Type:
Grant
Filed:
December 21, 2009
Date of Patent:
September 10, 2013
Assignee:
E I du Pont de Nemours and Company
Inventors:
Norman Herron, Vsevolod Rostovtsev, Jeffrey A. Merlo, Michael Henry Howard, Jr., Adam Fennimore, Weiying Gao, Kalindi Dogra, Nora Sabina Radu, Weishi Wu, Eric Maurice Smith, Daniel David Lecloux
Abstract: The present invention provides novel substituted pyrimidinyl-amines that are useful as inhibitors of protein kinases, especially c-Jun N-terminal kinases (JNK) and pharmaceutical compositions thereof and methods of using the same for treating conditions responsive to the inhibition of the JNK pathway.
Type:
Grant
Filed:
September 3, 2008
Date of Patent:
September 10, 2013
Assignee:
The Scripps Research Institute
Inventors:
Theodore Kamenecka, Rong Jiang, Xinyi Song, Philip LoGrasso, Michael Darin Cameron, Derek R. Duckett
Abstract: The present invention relates to novel compounds of Formula (I), wherein X1, X2, X3, X4, Y1, Y2, Y3, Y4, M1, M2, M3, Am and Bn are defined as in Formula (I); invention compounds are modulators of metabotropic glutamate receptors—subtype 4 (“mGluR4”) which are useful for the treatment or prevention of central nervous system disorders as well as other disorders modulated by mGluR4 receptors. The invention is also directed to pharmaceutical compositions and the use of such compounds in the manufacture of medicaments, as well as to the use of such compounds for the prevention and treatment of such diseases in which mGluR4 is involved.
Abstract: The invention is directed to certain novel compounds. Specifically, the invention is directed to compounds of formula (I): and salts thereof. The compounds of the invention are inhibitors of kinase activity, in particular PI3-kinase activity.
Type:
Grant
Filed:
March 5, 2010
Date of Patent:
September 3, 2013
Assignee:
GlaxoSmithKline Intellecutual Property Development
Inventors:
Julie Nicole Hamblin, Zoe Alicia Harrison, Paul Spencer Jones, Suzanne Elaine Keeling, Joelle Le, Christopher James Lunniss, Nigel James Parr
Abstract: A compound of Formula (I) wherein: either X is N and Y is CR5 or X is C and Y is S; Z is selected from N and CH; R1 is selected from H and Me; R2 is selected from H, OH, OMe and Me; each R3 is independently selected from C1-3alkyl, F, Cl, Br, CF3 and NH2; R4 is selected from Me, CF3, NO2 and CHF2; R5 is selected from H, Me and CHF2; R6 is selected from H and Me; and p is 0-3, compositions containing them, their use in therapy, for example in the treatment of tuberculosis, and methods for the preparation of such compounds, are provided.
Type:
Grant
Filed:
April 13, 2010
Date of Patent:
September 3, 2013
Assignee:
Glaxo Group Limited
Inventors:
Lluis Ballell Pages, Julia Castro Pichel, Raquel Fernandez Menendez, Esther Pilar Fernandez Velando, Silvia Gonzalez Del Valle, Maria Luisa Leon Diaz, Alfonso Mendoza Losana, Matthew James Wolfendale
Abstract: The present invention provides a method for the treatment of inflammatory diseases and/or conditions, e.g. allergic conjunctivitis, uveitis or phacoanaphylactic endophthalmitis in an eye of a mammal, said method comprising administering to said mammal in need of treatment a therapeutically effective amount of a novel cyclosporin A derivative selected from the group consisting of compounds represented by the formula: wherein R1 is S-Alk-R wherein Alk is an alkylene linkage, preferably a methylene or poly methylene linkage, or a polyalkenylene linkage, e.g. a C3 to C6 alkenylenyl linkage and R is a hydrogen or a unsubstituted or substituted hydrocarbyl group.
Abstract: Described herein are antagonists of PGD2 receptors. Also described are pharmaceutical compositions and medicaments that include the compounds described herein, as well as methods of using such antagonists of PGD2 receptors, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2-mediated conditions or diseases.
Type:
Grant
Filed:
October 7, 2009
Date of Patent:
September 3, 2013
Assignee:
Panmira Pharmaceuticals, LLC
Inventors:
John Howard Hutchinson, Thomas Jon Seiders, Jeannie M. Arruda, Jeffrey Roger Roppe
Abstract: A process for producing Fischer-Tropsch hydrocarbon products onboard a marine vessel from carbonaceous feedstock by gasification in a thermal conversion plant connected to an onboard power plant unit includes the steps of forming Fischer-Tropsch hydrocarbons in a Fischer-Tropsch reactor having a recycle line from the Fischer-Tropsch reactor to the thermal conversion plant and recycling at least one of carbon dioxide and tail gas from the Fischer-Tropsch reactor to the thermal conversion plant during gasification.
Abstract: A process for preparing a compound of formula (I) or a salt thereof: (I) wherein R1 is H or optionally substituted aryl or heteroaryl; comprising reacting 2,3-dichloropyrazine with a suitable diaryl imine followed by hydrolysis.
Type:
Grant
Filed:
April 19, 2010
Date of Patent:
August 20, 2013
Assignee:
OSI Pharmaceuticals, LLC
Inventors:
Yunyu Mao, Josef A. Rechka, Paula A. Tavares-Greco
Abstract: Disclosed are compounds of the general formula (I): compositions comprising an effective amount of said compounds either alone or in combination with other chemotherapeutic agents, and methods useful for treating or preventing cancer and for inhibiting tumor tissue growth. These compounds attenuate the oxidative damage associated with increased heme-oxygenase activity and can reduce cell proliferation in transformed cells. In addition, the described compounds and compositions are useful as neuroprotectants and for treating or preventing neurodegenerative disorders and other diseases of the central nervous system.
Type:
Grant
Filed:
January 13, 2011
Date of Patent:
August 20, 2013
Assignees:
Osta Biotechnologies, Queens University at Kingston, The Sir Mortimer B. Davis-Jewish General Hospital
Inventors:
Ajay Gupta, Hyman M. Schipper, Moulay Alaoui-Jamali, Walter A. Szarek, Kanji Nakatsu, Jason Z. Vlahakis
Abstract: An ester compound represented by formula (1): wherein R1 represents C1-C4 alkyl, has an excellent pest control effect and is therefore useful as an active ingredient of a pest control agent.
Abstract: The present invention is directed to N-hydroxyamidino compounds which are modulators of indoleamine 2,3-dioxygenase (IDO), as well as compositions and pharmaceutical methods thereof.
Type:
Grant
Filed:
March 17, 2011
Date of Patent:
August 13, 2013
Assignee:
Incyte Corporation
Inventors:
Andrew P. Combs, Brian M. Glass, Richard B. Sparks, Eddy Wai Tsun Yue
Abstract: The present invention relates to (2S)-2-({3?-Chloro-4?-[(2,2-dimethylpyrrolidin-1-yl) carbonyl]-5-fluorobiphenyl-2-yl}oxy)propanoic acid and (2R)-2-({3?-chloro-4?-[(2,2-dimethylpyrrolidin-1-yl) carbonyl]-5-fluorobiphenyl-2-yl}oxy)propanoic acid of formula (I), and crystalline forms and pharmaceutically acceptable salts thereof useful as pharmaceuticals.
Type:
Grant
Filed:
July 3, 2008
Date of Patent:
August 13, 2013
Assignee:
Astrazeneca AB
Inventors:
Roger Victor Bonnert, Timothy Jon Luker, Anil Patel, Aaron Rigby
Abstract: A monomer of formula (1) is provided wherein R1 is hydrogen or a monovalent C1-C6 hydrocarbon group, and R2 is a group having polymerization functionality. Using the monomer, crosslinking units can be incorporated into a polymer chain. A chemically amplified negative resist composition comprising a base polymer having crosslinking units incorporated therein has a high sensitivity and forms a resist pattern with minimized LER.
Abstract: The invention relates to a bimodal or multimodal polyethylene which comprises ethylene homopolymers and/or copolymers of ethylene with ?-olefins, has a polydispersity index Mw/Mn of the low molecular weight component of less than 10 and can be prepared using a polymerization catalyst based on a Ziegler component and a late transition metal component having a tridentate ligand which bears at least two ortho,ortho-disubstituted aryl radicals and also a catalyst system and a process for preparing the polyethylene and also fibers, moldings, films and polymer blends comprising this material.
Abstract: The present invention relates to novel azetidine derivatives, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals as modulators of sphingosine-1-phosphate receptors.
Type:
Grant
Filed:
November 10, 2011
Date of Patent:
August 6, 2013
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
Abstract: The present invention provides a compound represented by the formula (I): wherein R1, R2, R3, Z1, Z2, Ra, Rb, q, A and n are as defined in the description, a pharmaceutically acceptable salt or solvate thereof. The compound is useful as P2X3 and/or P2X2/3 receptor antagonist.