Abstract: The present invention relates to substituted indolo-pyridinone compounds and methods of synthesizing these compounds. The present invention also relates to pharmaceutical compositions containing substituted indolo-pyridinone compounds and methods of treating cell proliferative disorders, such as cancer, by administering these compounds or pharmaceutical compositions to subjects in need thereof.
Type:
Grant
Filed:
March 31, 2010
Date of Patent:
April 2, 2013
Assignee:
ArQule, Inc.
Inventors:
Nivedita Namdev, Manish Tandon, Jianqiang Wang, Audra Dalton, David Vensel, Rocio Palma, Mark A. Ashwell, Neil Westlund
Abstract: Compounds are disclosed herein having the formula (I). Therapeutic methods, compositions, and medicaments related thereto are also disclosed.
Abstract: The present invention provides imidazole derivatives of Formula (I-IV), methods of their preparation, pharmaceutical compositions comprising the compounds of Formula (I-IV), and their use in treating human or animal disorders. The compounds of the invention inhibit protein tyrosine phosphatase 1B and thus can be useful for the management, treatment, control, or the adjunct treatment of diseases mediated by PTPase activity. Such diseases include Type I diabetes and Type II diabetes.
Type:
Grant
Filed:
January 11, 2010
Date of Patent:
March 26, 2013
Assignee:
TransTech Pharma, Inc.
Inventors:
Adnan M. M. Mjalli, Dharma R. Polisetti, Govindan Subramanian, James C. Quada, Ravindra R. Yarragunta, Robert C. Andrews, Rongyuan Xie
Abstract: This invention relates composition and methods for making and using chemically modified oligonucleotides agents for inhibiting gene expression.
Type:
Grant
Filed:
July 2, 2009
Date of Patent:
March 26, 2013
Assignee:
Alnylam Pharmaceuticals, Inc.
Inventors:
Muthiah Manoharan, Kallanthottathil G. Rajeev, Venkitasamy Kesavan
Abstract: The invention relates to a sulfur-containing compound and the preparation thereof. The invention also relates to the uses of the sulfur-containing compound in inhibiting inducible nitric oxide synthase and/or cyclooxygenase-2 and in treating the diseases associated with inducible nitric oxide synthase and/or cyclooxygenase-2. This invention also describes a series of chemical analogues of the said sulfur-containing compound and the preparation of these compounds.
Abstract: The invention relates to an improved process for preparing alkoxyamines resulting from ?-phosphorated nitroxides corresponding to the formula (I): by reaction with a halogenated derivative in the presence of an organometallic system. This process comprises carrying out the reaction in a water-miscible organic solvent and precipitating the alkoxyamine directly from the organic medium by adding an aqueous solution of a strong acid. These alkoxyamines can be used in particular as radical polymerizations initiators.
Abstract: This invention provides, but is not limited to, novel oleanolic acid derivatives having the formula: wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such compounds, methods and intermediates useful for making the compounds, and methods of using the compounds and compositions.
Type:
Grant
Filed:
February 23, 2011
Date of Patent:
March 12, 2013
Assignee:
Reata Pharmaceuticals, Inc.
Inventors:
Xin Jiang, Xiaofeng Liu, Jack Greiner, Stephen S. Szucs, Melean Visnick
Abstract: The invention relates to substituted phenoxyacetic acids as useful pharmaceutical compounds for treating respiratory disorders, pharmaceutical compositions containing them, and processes for their preparation.
Type:
Grant
Filed:
July 26, 2011
Date of Patent:
March 12, 2013
Assignee:
AstraZeneca AB
Inventors:
Roger Victor Bonnert, Anil Patel, Stephen Thom
Abstract: Compound of formula I are antagonists of the PGD2 receptor, CRTH2, and as such are useful in the treatment and/or prevention of CRTH2-mediated diseases such as asthma.
Type:
Grant
Filed:
February 19, 2010
Date of Patent:
March 12, 2013
Assignee:
Merck Sharp & Dohme Corp.
Inventors:
Carl Berthelette, Michael Boyd, John Colucci, Karine Villeneuve, Joey Methot
Abstract: The invention relates to a method for producing phosphoric acid triesters of formula (I). According to said method, phosphoric acid or a phosphoric acid derivative selected from orthophosphoric acid, tetraphosphoric decaoxide and polyphosphoric acid is reacted with alkoxylated alcohols of formulae (II) R1—(OA1)x-OH, (III) R2—(OA2)y-OH, and (IV) R3—(OA3)Z-OH, in the molar ratio phosphoric acid or phosphoric acid derivative to alkoxylated alcohol of 1:2.5 to 1:3.3, at between 200 and 240° C.
Type:
Grant
Filed:
July 29, 2008
Date of Patent:
March 5, 2013
Assignee:
Clariant Finance (BVI) Limited
Inventors:
Peter Klug, Franz-Xaver Scherl, Waltraud Simsch, Adelgunde Oberhauser
Abstract: Embodiments of methods for making renewable diesel by deoxygenating (decarboxylating/decarbonylating/dehydrating) fatty acids to produce hydrocarbons are disclosed. Fatty acids are exposed to a catalyst selected from a) Pt and MO3 on ZrO2 (M is W, Mo, or a combination thereof), or b) Pt/Ge or Pt/Sn on carbon, and the catalyst decarboxylates at least 10% of the fatty acids. In particular embodiments, the catalyst consists essentially of 0.7 wt % Pt and 12 wt % WO3, relative to a mass of catalyst, or the catalyst consists essentially of a) 5 wt % Pt and b) 0.5 wt % Ge or 0.5 wt % Sn, relative to a mass of catalyst. Deoxygenation is performed without added hydrogen and at less than 100 psi. Disclosed embodiments of the catalysts deoxygenate at least 10% of fatty acids in a fatty acid feed, and remain capable of deoxygenating fatty acids for at least 200 minutes to more than 350 hours.
Type:
Grant
Filed:
September 14, 2012
Date of Patent:
March 5, 2013
Assignee:
Battelle Memorial Institute
Inventors:
Richard T. Hallen, Karl O. Albrecht, Heather M. Brown, James F. White
Abstract: The invention relates to difluoroboradiazaindacene dyes of the formula (1) where R1=fluoro-substituted phenyl residue C6HmFn where n=1 to 5 and m+n=5; or fluoro-substituted naphthyl residue C10HmFn where n=1 to 9 and m+n=9; R2=CH3, C2H5, C3H7, or C4H9; R3=alkyl, aryl, or vinyl aryl; R4, R5=H, F, or an R4 and R5 bridging residue CH?CH—CH?CH; R6, R7=H, F, or an R6 and R7 bridging residue CH?CH—CH?CH; and R8=alkyl or aryl.
Abstract: The use of substituted amides for modulating the activity of 11?-hydroxysteroid dehydrogenase type 1 (11?HSD1) and the use of these compounds as pharmaceutical compositions, are described. Also a novel class of substituted amides, of the general formula I. Their use in therapy, pharmaceutical compositions comprising the compounds, as well as their use in the manufacture of medicaments are described. The present compounds are modulators and more specifically inhibitors of the activity of 11?HSDI and may be useful in the treatment of a range of medical disorders where a decreased intracellular concentration of active glucocorticoid is desirable.
Abstract: The invention relates to novel thiazolylidine urea and amide derivatives that are PAMs of neuronal nicotinic receptors, compositions comprising the same, processes for preparing such compounds, and methods for using such compounds and compositions.
Type:
Grant
Filed:
December 18, 2008
Date of Patent:
February 26, 2013
Assignee:
Abbott Laboratories
Inventors:
Ramin Faghih, Gregory A. Gfesser, Kathleen H. Mortell, Murali Gopalakrishnan
Abstract: The invention provides compounds of formula I: in salt or zwitterionic form or a pharmaceutically acceptable salt thereof, wherein R1-6, a-e and Q are as defined in the specification. These compounds are muscarinic receptor antagonists. The invention also provides pharmaceutical compositions containing such compounds, processes for preparing such compounds and methods of using such compounds to, for example, treat pulmonary disorders such as chronic obstructive pulmonary disease and asthma.
Type:
Grant
Filed:
October 6, 2010
Date of Patent:
February 19, 2013
Assignee:
Theravance, Inc.
Inventors:
YuHua Ji, Craig Husfeld, Christopher Lange, Rick Lee, YongQi Mu
Abstract: This invention is directed to a hexahydro-cycloheptapyrazole cannabinoid modulator compound of formula (I): and a method for use in treating, ameliorating or preventing a cannabinoid receptor mediated syndrome, disorder or disease.
Type:
Grant
Filed:
March 20, 2007
Date of Patent:
February 19, 2013
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Fina Liotta, Mingde Xia, Huajun Lu, Meng Pan, Michael P. Wachter, Mark J. Macielag
Abstract: Embodiments of methods for making renewable diesel by deoxygenating (decarboxylating/decarbonylating/dehydrating) fatty acids to produce hydrocarbons are disclosed. Fatty acids are exposed to a catalyst selected from a) Pt and MO3 on ZrO2 (M is W, Mo, or a combination thereof), or b) Pt/Ge or Pt/Sn on carbon, and the catalyst decarboxylates at least 10% of the fatty acids. In particular embodiments, the catalyst consists essentially of 0.7 wt % Pt and 12 wt % WO3, relative to a mass of catalyst, or the catalyst consists essentially of a) 5 wt % Pt and b) 0.5 wt % Ge or 0.5 wt % Sn, relative to a mass of catalyst. Deoxygenation is performed without added hydrogen and at less than 100 psi. Disclosed embodiments of the catalysts deoxygenate at least 10% of fatty acids in a fatty acid feed, and remain capable of deoxygenating fatty acids for at least 200 minutes to more than 350 hours.
Type:
Grant
Filed:
August 2, 2010
Date of Patent:
February 5, 2013
Assignee:
Battelle Memorial Institute
Inventors:
Richard T. Hallen, Karl O. Albrecht, Heather M. Brown, James F. White
Abstract: Compounds are described that are active on PPARs, including pan-active compounds. Also described are methods for developing or identifying compounds having a desired selectivity profile.
Type:
Grant
Filed:
April 28, 2010
Date of Patent:
February 5, 2013
Assignee:
Plexxikon Inc.
Inventors:
James Arnold, Dean R. Artis, Clarence R. Hurt, Prabha N. Ibrahim, Heike Krupka, Jack Lin, Michael V. Milburn, Weiru Wang, Chao Zhang
Abstract: A quaternary ammonium salt of the formula (1), a composition containing the quaternary ammonium salt and an organic solvent, and an electrochemical device using the salt wherein R1 and R2 are both methyl and X? is BF4? or N(CF3SO2)2?.
Type:
Grant
Filed:
November 9, 2010
Date of Patent:
February 5, 2013
Assignees:
Otsuka Chemical Co., Ltd., Stella Chemifa Corporation
Abstract: An ester compound represented by the formula (1): wherein R represents a C1-C4 alkyl group or a C3-C4 alkenyl group, and A represents a single bond or an oxygen atom, has an excellent pest controlling efficacy, and it is useful as an active ingredient of a pest controlling agent.