Pfizer Corporation

Other

Derek Lawrence Tickner

Marcus D Ewing

Clifford N Meltz

Michel A Couturier

Ernest S Hamanaka

Peter Bertinato

Ralph P Robinson

Zheng Jane Li

Joseph P Lyssikatos

Peter Robert Rose

Frank R Busch

Subramanian Sam Guhan

Kees Pouwer

Bryan Li

Linda S Newton

Susan L Orrill

Harry O Tobiassen

R Mark Guinn

Karl K Ng

Jotham Wadsworth Coe

Stanton F McHardy

Joseph Francis Krzyzaniak

John Anthony Ragan

Douglas J M Allen

Brian C Vanderplas

Morgan Meltz

John Joseph Teixeira, Jr

Gregory J Withbroe

Mark T Barrila

This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R&#x2014;R, X, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

Substituted quinoline compounds

This invention relates to MTP/Apo-B secretion inhibitors of Formula (I) wherein R-R, X, m and n are as defined in the specification, as well as pharmaceutical compositions comprising the compounds, and methods of use of the compounds and compositions. The compounds of the invention are useful in treating obesity and associated diseases, conditions or disorders.

Triamide-substituted heterobicyclic compounds

This invention relates to the enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one, prodrugs thereof, and pharmaceutically acceptable salts and solvates of said compounds and said prodrugs, that are useful in the treatment of hyperproliferative diseases, such as cancers, in mammals. The invention also relates to processes for the production of enantiomerically pure or optically enriched (+)- or (&#x2212;)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one enantiomers from a mixture containing two enantiomers using continuous chromatography. The invention further relates to the L-(+)-tartaric acid or (S)-(&#x2212;)-1,1'-binapthyl-2,2&#x2032;-diyl hydrogenphosphate salts of (+)-6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one.

Enantiomers of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-[3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl]-1-methyl-1H-quinolin-2-one and salts thereof, useful in the treatment of cancer

A process for preparing azabicyclo[3.1.0]hexane compounds having reduced process-related impurities, e.g. 3-azabicyclo[3.1.0]hexane derivatives having reduced levels of etheric impurities, e.g. THF, is disclosed.

Purification process for an azabicyclo[3.1.0]hexane compound

This present invention relates to a new and improved reductive amination process for the preparation of 3-azabicyclo[3.1.0]hexane derivatives and pharmaceutical compositions comprising such derivatives. The invention particularly relates to using such derivatives to treat certain disorders and conditions, including, for example, irritable bowel syndrome, drug addiction or dependency, alcohol addiction or dependency, depression, and eating disorders.

Preparation of 3-azabicyclo [3.1.0] hexane derivatives

This invention relates to the enantiomers of 6-&lsqb;(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl&rsqb;-4-&lsqb;3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl&rsqb;-1-methyl-1H-quinolin-2-one, prodrugs thereof, and pharmaceutically acceptable salts and solvates of said compounds and said prodrugs, that are useful in the treatment of hyperproliferative diseases, such as cancers, in mammals. The invention also relates to processes for the production of enantiomerically pure or optically enriched (&plus;)- or (&minus;)-6-&lsqb;(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl&rsqb;-4-&lsqb;3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl&rsqb;-1-methyl-1H-quinolin-2-one enantiomers from a mixture containing two enantiomers using continuous chromatography. The invention further relates to the L-(&plus;)-tartaric acid or (S)-(&minus;)-1,1&prime;-binapthyl-2,2&prime;-diyl hydrogenphosphate salts of (&plus;)-6-&lsqb;(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl&rsqb;-4-&lsqb;3-(3-hydroxy-3-methyl-but-1-ynyl)-phenyl&rsqb;-1-methyl-1H-quinolin-2-one.

ENANTIOMERS OF 6-&lsqb;(4-CHLORO-PHENYL)-HYDROXY-(3-METHYL-3H-IMIDAZOL-4-YL)-METHYL&rsqb;-4-&lsqb;3-(3-HYDROXY-3-METHYL-BUT-1-YNYL)-PHENYL&rsqb;-1-METHYL-1H-QUINOLIN-2-ONE AND SALTS THEREOF, USEFUL IN THE TREATMENT OF CANCER

Crystal forms of 6-&lsqb;(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl&rsqb;-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3,- dihydroxybutanedioate salts and method of production

The instant invention provides novel processes and intermediates useful in the preparation of certain N-(indole-2-carbonyl)-&bgr;-alaninamide compounds, which compounds are glycogen phosphorylase inhibitors useful in the treatment of diseases such as hypercholesterolemia, hyperglycemia, hyperinsulinemia, hyperlipidemia, hypertension, atherosclerosis, diabetes, diabetic cardiomyopathy, infection, tissue ischemia, myocardial ischemia, and in inhibiting tumor growth.

Processes and intermediates for preparing glycogen phosphorylase inhibitors

N-(indole-2-carbonyl)-b-alaninamide crystal forms

Crystal forms of 6-&lsqb;(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl&rsqb;-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxybutanedioate salts and method of production

Resolution of 1-azabicyclo[2.2.2]octan-3-amine,

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Waterford, CT, United States of America

Derek Lawrence Tickner