Abstract: A process for the preparation of 4-[2-(Di-n-propylamino)ethyl]-2,3-dihydro-1H-indol-2-one of formula (I) and its pharmaceutically acceptable salts, solvates Formula I involving new intermediates of compound of formula (A) and (B) wherein R represents (i) a halogen atom selected from fluorine, chlorine atom, bromine atom and iodine atom; (ii) lower alkanesulfonyloxy group selected from methanesulfonyloxy, ethanesulfonyloxy, isopropanesulfonyloxy, propanesulfonyloxy, butanesulfonyloxy, tert-butanesulfonyloxy, pentanesulfonyloxy, hexanesulfonyloxy; (iii) substituted or unsubstantiated arylsulfonyloxy group selected from phenylsulfonyloxy, 4-methylphenylsulfonyloxy, 2-methylphenylsulfonyloxy, 4-nitrophenylsulfonyloxy, 4-methoxyphenylsulfonyloxy, 3-chlorophenylsulfonyloxy; (iv) arylalkylsulfonyloxy group selected from benzylsulfonyloxy, 2-phenylethylsulfonyloxy, 4-phenylbutylsulfonyloxy, 4-methylbenzylsulfonyloxy, 2-methylbenzylsulfonyloxy, 4-nitrobenzylsulfonyloxy, 4-methoxybenzylsulfonyloxy, 3-chlorobenzylsulfon
Abstract: Selected compounds are effective for treatment of pain and diseases, such as inflammation mediated diseases. The invention encompasses novel compounds, analogs, prodrugs and pharmaceutically acceptable derivatives thereof, pharmaceutical compositions and methods for prophylaxis and treatment of diseases and other maladies or conditions involving pain, inflammation, and the like. The subject invention also relates to processes for making such compounds as well as to intermediates useful in such processes.
Type:
Grant
Filed:
October 11, 2005
Date of Patent:
November 3, 2009
Assignee:
Amgen Inc.
Inventors:
Toshihiro Aya, Guolin Cai, Jian J. Chen, Derin D'Amico, Thomas Nguyen, Wenyuan Qian
Abstract: The invention concerns certain crystalline solvates and hydrates of the compound of the Formula (I) which is known inter alia by way of the code number ZD1839. In particular, the invention concerns a first solvate that occurs in the presence of methanol which is designated as Form 2 ZD1839 MeOH solvate, a second solvate that occurs in the presence of dimethyl sulphoxide which is designated as Form 3 ZD1839 DMSO solvate and a trihydrate that occurs in the presence of water which is designated Form 5 ZD1839 trihydrate. The invention further concerns processes for the preparation of these solvates and the trihydrate and for their conversion back to the compound ZD1839, pharmaceutical compositions containing them and their use in the manufacture of medicaments for use the production of an anti-proliferative effect in a warm-blooded animal such as man.
Abstract: This invention relates to an improved process of preparing carvedilol, as well as a new crystalline hydrate and solvate and forms of carvedilol, processes for the manufacture thereof, and pharmaceutical compositions thereof.
Type:
Grant
Filed:
April 15, 2008
Date of Patent:
October 20, 2009
Assignee:
Teva Pharmaceutical Industries Ltd
Inventors:
Jean Hildesheim, Sergei Fine, Judith Aronhime, Ben-Zion Dolitzky, Shoshana Ben-Valid, Ilan Kor-Sade
Abstract: Heterocyclic compounds, compositions comprising them, and methods of their use for the treatment, prevention and management of inflammatory and autoimmune diseases and disorders are disclosed.
Type:
Grant
Filed:
February 28, 2008
Date of Patent:
October 6, 2009
Assignee:
Lexicon Pharmaceuticals, Inc.
Inventors:
David J. Augeri, Jeffrey Bagdanoff, Simon D. P. Baugh, Kenneth G. Carson, Theodore C. Jessop, James E. Tarver
Abstract: Compounds are provided that act as potent antagonists of the CCR9 receptor, and which have been further confirmed in animal testing for inflammation, one of the hallmark disease states for CCR9. The compounds are generally aryl sulfonamide derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR9-mediated diseases, and as controls in assays for the identification of CCR9 antagonists.
Type:
Grant
Filed:
January 27, 2005
Date of Patent:
September 1, 2009
Assignee:
ChemoCentryx, Inc.
Inventors:
Solomon Ugashe, Zheng Wei, John J. Wright, Andrew Pennell
Abstract: The present invention discloses a structure of camphor-derived chiral auxiliary with a general formula (I), wherein R1 and R2 groups are independently hydrogen or C1 to C10 alkyl, X group is oxygen, two hydrogen atoms, or sulfur, and Y group is a functional group with stereo effect. Moreover, this invention also discloses a method for forming the above-mentioned chiral auxiliary.
Abstract: There are presented compounds of the formula or pharmaceutically acceptable salts thereof, wherein Y1, Y2, X1, X2, X3 and R are as described in this application. These compounds are believed to inhibit MDM2-p53 interaction and as such the compounds will have anti-hyperproliferative cellular activity.
Type:
Grant
Filed:
March 13, 2006
Date of Patent:
August 25, 2009
Assignee:
Hoffman-La Roche Inc.
Inventors:
Nader Fotouhi, Gregory Jay Haley, Klaus B. Simonsen, Binh Thanh Vu, Stephen Evan Webber
Abstract: The present invention provides an asymmetric hydrogenation process for the preparation of chiral cycloalkanoindole DP receptor antagonists in high enantiomeric excess.
Abstract: A melanogenesis inhibitor characterized by containing at least one kind of piperonyl alcohol represented by the following general formula (1) wherein R is a straight chain or branched chain alkyl group having 3 to 18 carbon atoms, a straight chain or branched chain alkenyl group having 3 to 18 carbon atoms, or an optionally substituted alicyclic alkyl group. The melanogenesis inhibitor is superior in stability and safety and has a high melanogenesis-inhibiting effect; and a skin preparation containing the melanogenesis inhibitor is very stable, safe, and has a sufficient fair skin effect and a sufficient effect for curing skin dyspigmentation.
Abstract: The invention relates to thiophene carboxamides of formula (I), wherein A, R1, R2, R3, R4, R5 and X are as defined in the specification, processes and intermediates used in their preparation, pharmaceutical compositions containing them and their use in therapy.
Type:
Grant
Filed:
January 13, 2004
Date of Patent:
August 11, 2009
Assignee:
AstraZeneca AB
Inventors:
Alan Wellington Faull, Craig Johnstone, Andrew David Morley, Jeffrey Philip Poyser
Abstract: The invention relates to compounds of structural formula (I): or a pharmaceutically acceptable salt, solvate, clathrate, and prodrug thereof, wherein Ra, Rb, and R2 are defined herein. These compounds inhibit tubulin polymerization and/or target vasculature and are useful for treating proliferative disorders, such as cancer.
Type:
Grant
Filed:
November 17, 2006
Date of Patent:
August 11, 2009
Assignee:
Synta Pharmaceuticals Corp.
Inventors:
Lijun Sun, Jun Jiang, Christopher Borella, Shoujun Chen, Keizo Koya
Abstract: The present invention provides a compound represented by the formula (I): [wherein R is an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, p is 0, 1 or 2, and when p is 2, each R may be the same or different, R1 is a hydrogen atom or an optionally substituted hydrocarbon group, R2 is an optionally substituted aromatic group, Ring A is an optionally substituted monocyclic aromatic ring or optionally substituted bicyclic aromatic fused ring, X1 is an oxygen atom or a sulfur atom, X2 is a bond, an oxygen atom or —S(O)n— (wherein n is 0, 1 or 2), Y is a bond, an oxygen atom, —S(O)m—, —C(?O)—N(R3)— or —N(R3)—C(?O)— (R3 is a hydrogen atom, an optionally substituted hydrocarbon group or an optionally substituted heterocyclic group, and m is 0, 1 or 2), M1, M2 and M3 may be the same or different and are each independently a bond or an optionally substituted divalent aliphatic hydrocarbon group, and M4 is an optionally substituted divalent aliphatic hydrocarbon group] or a
Abstract: Novel salt forms of [R-(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid characterized by their X-ray powder diffraction pattern and solid-state NMR spectra are described, as well as methods for the preparation and pharmaceutical composition of the same, which are useful as agents for treating hyperlipidemia, hypercholesterolemia, osteoporosis, benign prostatic hyperplasia, and Alzheimer's Disease.
Type:
Grant
Filed:
July 9, 2008
Date of Patent:
May 19, 2009
Assignee:
Pfizer Inc.
Inventors:
Anthony Michael Campeta, Joseph F. Krzyzaniak, Jason Albert Leonard
Abstract: The present invention relates to compounds that inhibit TACE, compositions thereof, and methods of using those compounds and compositions for treating diseases.
Type:
Grant
Filed:
December 19, 2003
Date of Patent:
February 3, 2009
Assignee:
Vertex Pharmaceuticals Incorporated
Inventors:
Upul Bandarage, Jon H. Come, Emanuele Perola, Govinda Rao Bhisetti, Jeffrey O. Saunders, Tiansheng Wang, Shi-Kai Tian
Abstract: The present invention relates to triazole derivatives of formula (I) notably for use as pharmaceutically active compounds, as well as pharmaceutical formulations containing such triazole derivatives. Said triazoles are useful in the treatment and/or prevention of preterm labor, premature birth, dysmenorrhea, inappropriate secretion of vasopressin, congestive heart failure, arterial hypertension, liver cirrhosis, nephrotic syndrome and ocular hypertension. In particular, the present invention is related to triazole derivatives displaying a substantial modulatory, in particular antagonistic activity, of the oxytocin and/or vasopressin receptor. More preferably, said compounds are useful in the treatment and/or prevention of disease states mediated by oxytocin and/or vasopressin. The present invention is furthermore related to novel triazole derivatives as well as to methods of their preparation.
Type:
Grant
Filed:
December 19, 2002
Date of Patent:
December 23, 2008
Assignee:
Laboratoires Serono SA
Inventors:
Anna Quattropani, Matthias Schwarz, Russell J. Thomas, Thomas Coulter
Abstract: A regiospecific process for the preparation of 4-[1-(4-cyanophenyl)-1-(1,2,4-triazol-1-yl)methyl]benzonitrile comprising reacting 4-halomethylbenzonitrile with 4-amino-1,2,4-triazole followed by deamination and reaction with 4-fluorobenzonitrile.
Type:
Grant
Filed:
February 5, 2004
Date of Patent:
December 2, 2008
Assignee:
Sun Pharmaceutical Industries Limited
Inventors:
Hetalkumar Virendrabhai Patel, Raja Jyotir Jani, Rajamannar Thennati
Abstract: Heterocycle substituted ketoamide derivatives of Formula (I), wherein the substitutes A, D, A and R are defined as in claim in, which are useful as cathepsin K inhibitors are described herein. The described invention also includes methods of making such heterocycle substituted ketoamide derivatives as well as method of using the same in the manufacture of medicaments for the treatment of disorders, including osteoporosis, associated with an imbalance between bone resorption and formation which can ultimately lead to fracture.
Type:
Grant
Filed:
April 1, 2003
Date of Patent:
July 22, 2008
Assignee:
SmithKline Beecham Corporation
Inventors:
David Gene Barrett, John G. Catalano, David Norman Deaton, Aaron Bayne Miller, John A. Ray, Vicente Samano
Abstract: [R-(R*,R*)]-2-(4-fluorophenyl)-?,?-dihydroxy-5-((1-methylethyl)-3-phenyl-4-[(phenylamino)-carbonyl)]-1H-pyrrole-1-heptanoic acid or (2R-trans)-5-(4-fluoro-phenyl)-2-(1-methylethyl-N,4-diphenyl-1-[2-(tetrahydro-4-hydroxy-6-oxo-2H-pyran-2-yl)ethyl]-1H-pyrrole-3-carboxamide; and pharmaceutically acceptable salts thereof.