Pfizer Corporation

Marcus D Ewing

Derek Lawrence Tickner

Ernest S Hamanaka

Peter Bertinato

Ralph P Robinson

Michel A Couturier

Clifford N Meltz

Subramanian Sam Guhan

Kees Pouwer

R Mark Guinn

Bryan Li

Karl K Ng

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

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

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Colchester, CT, United States of America

Marcus D Ewing