Abstract: The present invention relates to novel oxadiazole 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 14, 2011
Date of Patent:
July 30, 2013
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
Abstract: Bicyclic aryl substituted triazoles or heteroaryl substituted triazoles and pharmaceutical compositions containing the compounds are disclosed as being useful in inhibiting the activity of the receptor protein tyrosine kinase Axl. Methods of using the compounds in treating diseases or conditions associated with Axl activity are also disclosed.
Type:
Grant
Filed:
December 1, 2010
Date of Patent:
July 23, 2013
Assignee:
Rigel Pharmaceuticals, Inc.
Inventors:
Dane Goff, Jing Zhang, Rajinder Singh, Sacha Holland, Thilo J. Heckrodt, Pingyu Ding, Jiaxin Yu, Joane Litvak
Abstract: An acoustic wave biosensor comprising a surface of a mixed self-assembling monolayer for receiving a probe-biomolecule is described herein. The biosensor surface may comprise a piezoelectric quartz crystal,—for detection purposes with the electromagnetic piezoelectric acoustic sensor (EMPAS)—upon which a mixed self-assembling monolayer is formed, which includes at least one linker, such as 2,2,2-trifluoroethyl-13-trichlorosilyl-tridecanoate (TTTA); its oligoethylene glycol (OEG) analog OEGylated TTTA (OEG-TTTA); S-(2-(2-(2-(3-trichlorosilyl-propyloxy)-ethoxy)-ethoxy)-ethyl)-benzenethiosulfonate (OEG-TUBTS). Linker/diluent systems for attaching a functionalizing entity to the surface of a biosensor are described, as well as methods for preparing a biosensor surface with an oligoethylene glycol linker.
Type:
Grant
Filed:
June 6, 2011
Date of Patent:
July 23, 2013
Assignee:
Econous Systems Inc.
Inventors:
Michael Thompson, Sonia Sheikh, Jack Chih-Chieh Sheng, Christophe Blaszykowski
Abstract: The present invention relates to novel compounds, ester pro-drugs of [3-(1-1H-imidazol-4-yl)ethyl)-2-methylphenyl]methanol, processes for preparing them, pharmaceutical compositions containing them and their use as pharmaceuticals in the treatment of conditions mediated by adrenergic receptors.
Type:
Grant
Filed:
September 15, 2011
Date of Patent:
July 23, 2013
Assignee:
Allergan, Inc.
Inventors:
Ken Chow, Liming Wang, Michael E. Garst, John E. Donello, Daniel W. Gil, Mohammad I. Dibas
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 28, 2011
Date of Patent:
July 23, 2013
Assignee:
Allergan, Inc.
Inventors:
Santosh C. Sinha, Smita S. Bhat, Evelyn G. Corpuz, Ken Chow, Wenkui K. Fang, Wha-Bin Im
Abstract: The invention relates to novel curcumin and tetrahydrocurcumin derivatives, which have been modified at one phenolic group to incorporate more-reactive groups. The curcumin and tetrahydrocurcumin derivatives are in the form of monomers, dimmers, and polymers.
Type:
Grant
Filed:
October 12, 2007
Date of Patent:
July 16, 2013
Assignee:
The Research Foundation of the City University of New York
Inventors:
Krishnaswami Raja, Probal Banerjee, Andrew Auerbach, Wei Shi, William L'Amoreaux
Abstract: The present invention relates to novel phenyl oxadiazole 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 14, 2011
Date of Patent:
July 16, 2013
Assignee:
Allergan, Inc.
Inventors:
Wenkui K. Fang, Liming Wang, Evelyn G. Corpuz, Ken Chow, Wha Bin Im
Abstract: Provided is a tricyclic compound having a PPAR ? agonist activity, which is represented by the general formula (I) wherein Z represents a single bond or the like, Y represents a hydrogen atom, lower alkyl optionally having substituent(s) or the like, X represents a hydrogen atom or the like, A represents aryl or the like, B and C are the same or different and each represents an aromatic carbocycle or the like, R4-R9 are the same or different and each represents hydrogen or the like, V represents a single bond or the like, R10 and R11 are the same or different and each represents hydrogen or the like, or a pharmaceutically acceptable salt thereof or the like:
Abstract: The invention deals with a preparation method of salts of 5-chloro-4-(2-imidazolin-2-yl-amino)-2,1,3-benzothiadiazole (tizanidine) of formula I, especially tizanidine hydrochloride, comprising preparation of a salt of tizanidine of formula I and a carboxylic acid as an intermediate, from which, after acidification with hydrogen chloride, tizanidine hydrochloride is obtained in a high yield and purity.
Type:
Grant
Filed:
December 18, 2009
Date of Patent:
July 16, 2013
Assignee:
Farmak, A.S.
Inventors:
Pavel Hradil, Lubomir Kvapil, Martin Grepl, Jan Novotny
Abstract: N-[4-(3-Amino-1H-indazol-4-yl)phenyl]-N?-(2-fluoro-5-methylphenyl)urea Hydrate Crystalline Form 1, ways to make it, formulations comprising it and made with it and methods of treating patients having disease using it are disclosed.
Abstract: Cycloalkylcarbonylamino acid derivatives, which are raw material intermediates of a novel cycloalkane carboxamide derivative that selectively inhibits cathepsin K, and a production process thereof, are provided. A cycloalkylcarbonylamino acid derivative represented by the following general formula (I), or a pharmaceutically acceptable salt thereof: (wherein, R1 and R2 represent alkyl groups, alkenyl groups, alkynyl groups, aromatic hydrocarbon groups, heterocyclic groups or the like, and ring A represents a cyclic alkylidene group having 5, 6 or 7 carbon atoms).
Abstract: The invention includes methods for isolating crystalline Form I of 5-azacytidine substantially free of other forms, wherein 5-azacytidine is represented by the formula: The invention also includes pharmaceutical compositions comprising Form I of 5-azacytidine.
Type:
Grant
Filed:
June 5, 2012
Date of Patent:
July 9, 2013
Assignee:
Pharmion LLC
Inventors:
Dumitru Ionescu, Peter Blumbergs, Gary L. Silvey
Abstract: N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides of the formula (I) are described as herbicides. In this formula (I), X, Y, Z and R represent radicals such as hydrogen, organic radicals such as alkyl, and other radicals such as halogen. A and B represent N and CY.
Type:
Grant
Filed:
August 31, 2011
Date of Patent:
July 9, 2013
Assignee:
Bayer Cropscience AG
Inventors:
Ralf Braun, Arnim Köhn, Andreas Almsick, Hartmut Ahrens, Simon Dörner-Rieping, Lothar Willms, Isolde Häuser-Hahn, Ines Heinemann, Elmar Gatzweiler, Christopher Hugh Rosinger
Abstract: An apparatus and method using an array of VCSELs operable to emit light at one or more wavelengths, pulse-repetition rates, pulse durations, pulse powers, pulse energies, and/or light-distribution spatial and/or temporal patterns, that are effective to stimulate or photostimulate human or other animal tissue, and in particular, nerve tissue. In some embodiments, the invention provides an implantable device that includes an array having a plurality of VCSELs in a spatial pattern suitable to stimulate or photostimulate a plurality of different areas of tissue (e.g., a plurality of different nerves). In some embodiments, the device is instead partially implantable. In some embodiments, the device is instead external to the body of the animal.
Abstract: The present invention is directed to ?-ketoamide derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by endothelial lipase, for example, cardiovascular disorders.
Type:
Grant
Filed:
September 26, 2011
Date of Patent:
July 2, 2013
Assignee:
Janssen Pharmaceutica N.V.
Inventors:
Michael N. Greco, Margery A. Connelly, Shyamali Ghosh, Dennis J. Hlasta, Edward C. Lawson, Eric Strobel, Michele A. Weidner-Wells, Hong Ye
Abstract: A fluorine-containing polyether carboxylic acid amide represented by the general formula: CnF2n+1O(C3F6O)mRfCONHAr, wherein Rf is a fluorocarbon group having 1 to 2 carbon atoms, Ar is a nitrogen-containing heterocyclic group, n is an integer of 1 to 3, and m is an integer of 10 to 30, is produced by reacting a fluorine-containing polyether carboxylic acid fluoride represented by the general formula: CnF2n+1(C3F6O)mRfCOF, wherein Rf, n, and m are as defined above, with a nitrogen-containing heterocyclic amine compound represented by the general formula: ArNH2, wherein Ar is as defined above; wherein the reaction is carried out while a reaction temperature is first increased to 80 to 100° C., and then increased at a temperature increase rate that produces a temperature difference of 3 to 5° C. after 48 hours.
Abstract: The invention relates to compounds of formula (I) having pharmacological activity towards the sigma receptor, to processes of preparation of such compounds, to pharmaceutical compositions comprising them, and to their use for the treatment and or prophylaxis of a disease in which the sigma receptor is involved.
Type:
Grant
Filed:
February 9, 2010
Date of Patent:
June 25, 2013
Assignee:
Laboratorios Del Dr. Esteve, S.A.
Inventors:
Christian Laggner, María Rosa Cuberes-Altisent, Joerg Holenz, Juana María Berrocal-Romero, Maria Montserrat Contijoch-Llobet
Abstract: There is provided a compound of Formula I wherein X, Y and Z are each independently of each other an optional linker group; R1 is a ring system; R2 is selected from hydrocarbyl groups, oxyhydrocarbyl groups, cyano (—CN), nitro (—NO2) and halogens; R3 and R4 are independently selected from H and hydrocarbyl, ring A and B are independently optionally further substituted.
Type:
Grant
Filed:
July 22, 2010
Date of Patent:
June 25, 2013
Assignee:
Sterix Limited
Inventors:
Lok Wai Lawrence Woo, Toby Jackson, Christian Bubert, Atul Purohit, Michael John Reed, Barry Victor Lloyd Potter
Abstract: Fatty acid inhibitors, pharmaceutical compositions including fatty acid inhibitors, methods for using fatty acid inhibitors to treat a variety of diseases, and methods for preparing fatty acid inhibitors are provided herein.