Abstract: The invention relates to triamide MTP/ApoB inhibitors of the formula 1 wherein R1-R8 are as defined in the specification, as well as pharmaceutical compositions and uses thereof, and processes for preparing the compounds. The compounds of the invention are useful for the treatment of obesity and lipid disorders.
Type:
Grant
Filed:
February 10, 2006
Date of Patent:
March 25, 2008
Assignee:
Pfizer Inc.
Inventors:
Peter Bertinato, Alan E. Blize, Brian Bronk, Hengmiao Cheng, Jin Li, Hiep Huatan, Clive Mason
Abstract: The present invention is directed to 4-cyclopentyl resorcinol monohydrate, its Form I polymorph, formulations containing at least one of these compounds, and their use to lighten skin.
Type:
Grant
Filed:
January 28, 2004
Date of Patent:
March 4, 2008
Assignee:
Warner-Lambert Company
Inventors:
Martin James Procter, William Thomas Gattrell
Abstract: Compounds of Formula (I) that act as cannabinoid receptor ligands and their uses in the treatment of diseases linked to the mediation of the cannabinoid receptors in animals are described herein.
Abstract: The present invention relates to novel triazolo-pyridines of the formula wherein X is >CH2, >NH, sulfur, >S?O, >SO2 or oxygen; wherein said >CH2 and >NH may optionally be substituted with a suitable substituent; R1 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; R2 is selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; s is an integer from 0-4; R3 is R4, R5—(NR6)—, R5—S—, R5—(S?O)—, R5—(SO2)—, R5—SO2—NR6—, R5—(NR6)—SO2—, R5—O—, R5—(C?O)—, R5—(NR6)—(C?O)—, R5—(C?O)—NR6—, R5—O—(C?O)—, R5—(C?O)—O—, R5—CR7?CR8— or R5—C?C—; such that the molecular weight of R3 is less than 500 AMU, preferably less than 250 AMU; R4, R5 and R6 are each selected from the group consisting of hydrogen, (C1-C6)alkyl and other suitable substituents; or a pharmaceutically acceptable salt thereof; to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use.
Type:
Grant
Filed:
February 11, 2004
Date of Patent:
January 22, 2008
Assignee:
Pfizer Inc.
Inventors:
John Frederick Braganza, Michael Anthony Letavic, Kim F. McClure
Abstract: The present invention provides peptides and peptide analogues that mimic the structural and pharmacological properties of human ApoA-I. The peptides and peptide analogues are useful to treat a variety of disorders associated with dyslipidemia.
Type:
Grant
Filed:
March 15, 2004
Date of Patent:
December 25, 2007
Inventors:
Jean-Louis Dasseux, Renate Sekul, Klaus Büttner, Isabelle Cornut, Günther Metz, Jean Dufourcq
Abstract: Compounds of formula (I), or a pharmaceutically acceptable derivative thereof, wherein R1 and R3 independently represent H, C1-6alkyl, C3-8cycloalkyl, or halogen; R2 represents C1-6alkyl, CF3 or aryl; a represents 1 or 2; R4, R5, R7 and R8 independently represent H, C1-6alkyl, C1-6alkyloxy, CN or halogen, or R4 and R5, or R7 and R8, together with the ring to which they are attached form an aryl or heterocyclic fused ring system; X represents C or N; Y represents CH2 or O; R6 represents H, CN or halo provided that, when X represents N, R6 is absent. The compounds are useful for treating endometriosis, uterine fibroids (leiomyomata), menorrhagia, adenomyosis, primary and secondary dysmenorrhoea (including symptoms of dyspareunia, dyschexia and chronic pelvic pain), or chronic pelvic pain syndrome.
Type:
Grant
Filed:
November 3, 2006
Date of Patent:
December 18, 2007
Assignee:
Pfizer Limited
Inventors:
Paul Anthony Bradley, Kevin Neil Dack, Patrick Stephen Johnson, Sarah Elizabeth Skerratt
Abstract: The present invention provides peptides and peptide analogues that mimic the structural and pharmacological properties of human ApoA-I. The peptides and peptide analogues are useful to treat a variety of disorders associated with dyslipidemia.
Type:
Grant
Filed:
November 17, 2003
Date of Patent:
December 11, 2007
Inventors:
Jean-Louis Dasseux, Renate Sekul, Klaus Büttner, Isabelle Cornut, Günther Metz, Jean Dufourcq
Abstract: A process and intermediates for producing 3-amino nitrites. The process involves resolving an enantiomeric mixture of chiral 3-amino nitrites in the presence of a chiral acid in a solvent system to produce a chiral 3-amino nitrile salt. The process may further comprise a recrystalizing step, wherein an enantiomerically enriched 3-amino nitrile salt is produced. The process may further comprise a salt exchanging step, wherein another acid is added to the chiral 3-amino nitrile salt or the enantiomerically enriched 3-amino nitrile salt to produce another 3-amino nitrile salt.
Type:
Grant
Filed:
September 21, 2004
Date of Patent:
November 27, 2007
Assignee:
Pfizer Inc.
Inventors:
David Robert Allen, Crystal A Achenbach-McCarthy
Abstract: The invention provides compounds of formula (I), prodrugs and stereoisomers thereof, and the pharmaceutically acceptable salts of the compounds, prodrugs, and stereoisomers, wherein R1, R2, R3, HET, n, Q, X, Y, and Z are as described herein; compositions thereof; and uses thereof in treating diabetic complications including diabetic neuropathy, diabetic nephropathy, diabetic microangiopathy, and the like.
Abstract: Novel 3,3-diphenylpropylamines of the formula and stereoisomers and physiologically acceptable acid addition salt thereof; wherein R1, R2, R3, R4, R5, and R6 are as defined herein; methods of use thereof; and pharmaceutical compositions thereof.
Type:
Grant
Filed:
August 24, 2006
Date of Patent:
November 6, 2007
Assignee:
Pfizer Inc.
Inventors:
John Gregory Slatter, Raymond Charles Grabiak, Robert John Kaufman
Abstract: The present invention relates to a class of substituted 1,2,4-triazoles of formula (I) with activity as oxytocin antagonists, uses thereof, processes for the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including sexual dysfunction, particularly premature ejaculation (P.E.
Type:
Grant
Filed:
September 20, 2004
Date of Patent:
November 6, 2007
Assignee:
Pfizer Inc.
Inventors:
Alan Daniel Brown, David Ellis, Christopher Ronald Smith
Abstract: This invention provides the compounds of formula (I): or a pharmaceutically acceptable ester of such compound, or a pharmaceutically acceptable salt thereof, wherein R1 and R2 independently represent a hydrogen atom or the like; R3 represents an aryl group having from 6 to 10 ring atoms or the like; X represents an oxygen atom, or the like; Y represents an oxygen atom or the like; and n represents an integer 0, 1 or 2. These compounds have ORL1-receptor antagonist activity; and therefore, are useful to treat diseases or conditions such as pain, various CNS diseases etc.
Abstract: Novel oxazole and thiazole compounds, including derivatives thereof, to intermediates for their preparation, to pharmaceutical compositions containing them and to their medicinal use are described. The compounds of the present invention are potent inhibitors of transforming growth factor (“TGF”)-? signaling pathway. They are useful in the treatment of various TGF-related disease states including, for example, cancer and fibrotic diseases.
Abstract: The present invention provides peptides and peptide analogues that mimic the structural and pharmacological properties of human ApoA-I. The peptides and peptide analogues are useful to treat a variety of disorders associated with dyslipidemia.
Abstract: The invention relates to compounds of formula (1) and to processes for the preparation of, intermediates used in the preparation of, compositions containing and the uses of, such derivatives. The compounds according to the present invention are useful in numerous diseases, disorders and conditions, in particular inflammatory, allergic and respiratory diseases, disorders and conditions.
Type:
Grant
Filed:
May 6, 2004
Date of Patent:
September 11, 2007
Assignee:
Pfizer Inc
Inventors:
Mark Edward Bunnage, Paul Alan Glossop, Charlotte Alice Louise Lane, Russell Andrew Lewthwaite