Abstract: Compounds of Formulas 1 and 2 where the variables have the meaning disclosed in the specification, have analgesic and in some cases immunostimulant activity.
Type:
Grant
Filed:
January 25, 2006
Date of Patent:
October 16, 2012
Assignees:
Allergan, Inc., Exonhit Therapeutics SA
Inventors:
Bertrand Leblond, Eric Beausoleil, Thierry Taverne, John E. Donello
Abstract: Diaminothiazoles and pharmaceutical compositions containing them are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the diaminothiazoles in treating diseases or conditions associated with Axl activity are also disclosed.
Type:
Grant
Filed:
December 23, 2010
Date of Patent:
October 16, 2012
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Dane Goff, Jing Zhang, Raj Singh, Sacha Holland
Abstract: The present invention provides the compounds of general formula 5 and 9 useful as potential antitumour agents against human cancer cell lines. The present invention further provides the process for preparation of napthalimide-benzimidazole hybrids of general formula 5 and 9, n-1-2, R=n-methylpiperazine or morpholine (Formula 9), wherein: n=2-3, m=2-3 and R=n-methylpiperazine or morpholine.
Type:
Grant
Filed:
March 3, 2009
Date of Patent:
October 16, 2012
Assignee:
Council of Scientific & Industrial Research
Abstract: Embodiments disclosed herein relate to new imidazolidinedione derivatives, methods of making these compounds, and methods of using the same to prevent, treat, or inhibit malaria in a subject.
Type:
Grant
Filed:
October 2, 2009
Date of Patent:
October 9, 2012
Assignee:
The United States of America as Represented by the Secretary of the Army
Inventors:
Ai Jeng Lin, Michael P. Kozar, Michael T. O'Neil, Alan J. Magill, David L. Saunders
Abstract: Gabapentin enacarbil was prepared and purified from intermediates such as 1-haloalkyl carbamate or carbonate and diacid acetal skeleton. For example, a 1-haloalkyl carbonate or carbamate was prepared by combining a C1 to C10 alcohol or C1 to C10 primary amine, a solvent selected from the group consisting of: acetonitrile, C3 to C7 ketone, C5 to C10 ether, C2 to C7 ester, C5 to C10 hydrocarbon and a combination thereof; a 1-haloalkyl haloformate of the following formula: wherein each X is independently selected from Br, I, or Cl; R1 is alkyl or H; and a C6 to C21 tertiary amine.
Type:
Grant
Filed:
November 26, 2009
Date of Patent:
October 9, 2012
Assignee:
Teva Pharmaceutical Industries Ltd.
Inventors:
Elena Ben Moha-Lerman, Tamar Nidam, Meital Cohen, Sharon Avhar-Maydan, Anna Balanov
Abstract: The present invention relates to novel 1-benzyl-3-hydroxymethylindazole derivatives according to formula (I) described in the claims, and to a pharmaceutical composition comprising them, together with a pharmaceutically acceptable vehicle. In addition, the present invention relates to the use of 1-benzyl-3-hydroxymethylindazole derivatives for the preparation of a pharmaceutical composition that is active in the treatment of diseases based on the expression of MCP-1, CX3CR1 and p40, and to their use in a method for treating or preventing diseases based on the expression of MCP-1, CX3CR1 and p40.
Type:
Grant
Filed:
March 7, 2011
Date of Patent:
October 9, 2012
Assignee:
Aziende Chimiche Riunite Angelini Francesco A.C.R.A.F. S.p.A.
Abstract: It is an object of the present invention to provide a photopolymerization initiator composition having high sensitivity and excellent storage properties, a photosensitive composition containing the photopolymerization initiator composition, and a thiourethane compound preferable for the photopolymerization initiator composition. The thiourethane compound of the present invention has 2 to 6 units each of which contains a moiety represented by the following formula (i) and a moiety represented by the following formula (ii). wherein R1 is a hydrogen atom or a methyl group, and R2 is —CO—, —COO— or —COOR3— (wherein R3 is an alkylene group of 2 to 6 carbon atoms).
Abstract: This invention relates to compounds of the general formula: in which the variable groups are as defined herein, and to their preparation and use.
Type:
Grant
Filed:
May 8, 2007
Date of Patent:
October 2, 2012
Assignee:
ARIAD Pharmaceuticals, Inc.
Inventors:
William C. Shakespeare, Wei-Sheng Huang, David C. Dalgarno, Xiaotian Zhu, R. Mathew Thomas, Yihan Wang, Jiwei Qi, Rajeswari Sundaramoorthi, Dong Zou, Chester A. Metcalf, III, Tomi K. Sawyer, Jan Antoinette C. Romero
Abstract: The invention features a series of heterocyclic derivatives that inhibit tumor necrosis factor alpha (TNF-?) induced necroptosis. The heterocyclic compounds of the invention are described by Formulas (I) and (Ia)-(Ie) and are shown to inhibit TNF-? induced necroptosis in FADD-deficient variant of human Jurkat T cells. The invention further features pharmaceutical compositions featuring the compounds of the invention. The compounds and compositions of the invention may also be used to treat disorders where necroptosis is likely to play a substantial role.
Type:
Grant
Filed:
August 20, 2010
Date of Patent:
October 2, 2012
Assignees:
The Brigham and Women's Hospital, Inc., President and Fellows of Harvard College, Tufts University
Inventors:
Gregory D. Cuny, Xin Teng, Junying Yuan, Alexei Degterev
Abstract: The invention provides a reaction system for the production of an alkylene carbonate comprising: an epoxidation zone containing an epoxidation catalyst located within an epoxidation reactor; a carboxylation zone containing an bromide-containing carboxylation catalyst located within an alkylene oxide absorber; and one or more purification zones containing a purification absorbent capable of reducing the quantity of bromide-containing impurities in a feed comprising a recycle gas, which purification zones are located upstream from the epoxidation zone; and a process for the production of an alkylene carbonate and an alkylene glycol.
Type:
Grant
Filed:
May 13, 2009
Date of Patent:
September 25, 2012
Assignee:
Shell Oil Company
Inventors:
Wayne Errol Evans, Martin Lysle Hess, Marek Matusz, Eugene Marie Godfried Andre Van Kruchten
Abstract: The present invention provides phenoxyacetic acid derivatives of Formula (I) for the treatment of CRTH2 related disorders and disease selected from asthma, atopic dermatitis and inflammatory dermatoses.
Abstract: The present application is directed to novel P2X7R antagonists that are N-indol-3-yl-acetamide and N-azaindol-3-yl-acetamide compounds, pharmaceutical compositions comprising the same and their use for the prophylactic or therapeutic treatment of diseases mediated by P2X7R activity.
Abstract: This invention provides compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig or salts thereof, pharmaceutical compositions comprising a compound of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and a pharmaceutically acceptable excipient, methods of modulating the androgen receptor, methods of treating diseases beneficially treated by an androgen receptor modulator (e.g., sarcopenia, prostate cancer, contraception, type 2 diabetes related disorders or diseases, anemia, depression, and renal disease) and processes for making compounds of formulas I, Ia, Ib, Ic, Id, Ie, If or Ig and intermediates useful in the preparation of same.
Abstract: Processes for preparing an amine, which processes comprise: reacting a reactant selected from the group consisting of primary alcohols, secondary alcohols, aldehydes, ketones, and mixtures thereof, with hydrogen and a nitrogen compound selected from the group consisting of ammonia, primary amines, secondary amines and mixtures thereof, in the presence of a zirconium dioxide-, copper- and nickel-containing catalyst; wherein the catalyst comprises a catalytically active composition which comprises, before reduction with hydrogen, oxygen compounds of zirconium, copper, and nickel, and 0.2 to 40% by weight of an oxygen compound of cobalt, calculated as CoO, 0.1 to 5% by weight of an oxygen compound of iron, calculated as Fe2O3, and 0.1 to 5% by weight of at least one oxygen compound of lead, tin, bismuth or antimony, calculated as PbO, SnO, Bi2O3 and Sb2O3 respectively.
Type:
Grant
Filed:
December 10, 2008
Date of Patent:
September 18, 2012
Assignee:
BASF SE
Inventors:
Petr Kubanek, Wolfgang Mägerlein, Ekkehard Schwab, Johann-Peter Melder, Manfred Julius
Abstract: The present invention relates to a process for the sulfinylation of a pyrazole derivative, characterized in that 5-amino-1-[2,6-dichloro-4-(trifluoromethyl)phenyl]-1H-pyrazole-3-carbonitrile (II) is reacted with a sulfinylating agent selected from trifluoromethylsulfinic acid, trifluoromethylsulfinic acid anhydride, and a trifluoromethylsulfinate alkaline or alkaline earth metal salt and mixtures of the acid and/or the salt(s), in the presence of at least one amine acid complex wherein the amine(s) are selected from tertiary amines and the acid(s) are selected from hydrofluoric, hydrochloric, hydrobromic and hydroiodic acid and sulfonic acid derivatives, and with the addition of a halogenating agent.
Type:
Grant
Filed:
November 5, 2007
Date of Patent:
September 11, 2012
Assignee:
BASF SE
Inventors:
Martin Sukopp, Oliver Kuhn, Carsten Gröning, Michael Keil, Jon J. Longlet
Abstract: The invention relates to aryl-substituted heterocycles, to processes for their preparation, to their use for the treatment and/or prophylaxis of diseases and to their use for preparing medicaments for the treatment and/or prophylaxis of diseases, in particular of thromboembolic disorders.
Type:
Grant
Filed:
May 25, 2007
Date of Patent:
September 11, 2012
Assignee:
Bayer Intellectual Property GmbH
Inventors:
Michael Härter, Tobias Wunberg, Swen Allerheiligen, Marcus Bauser, Ulrich Rester, Stefan Heitmeier
Abstract: A crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug and methods of preparing a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug, and methods of using a crystalline form of a (3S)-aminomethyl-5-hexanoic acid prodrug are provided.
Type:
Grant
Filed:
December 7, 2010
Date of Patent:
September 4, 2012
Assignee:
XenoPort, Inc.
Inventors:
Fenmei Yao, Mark A. Gallop, Ronald W. Barrett, Peter A. Virsik
Abstract: Disclosed is a compound represented by general formula (I) or a pharmaceutically acceptable salt thereof, which is useful as a selective antagonist of a 5-HT2B receptor. The compound and salt are useful for treatment or prevention of various diseases and conditions associated with a 5-HT2B receptor.