Abstract: 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 (−)-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.
Type:
Grant
Filed:
August 27, 2002
Date of Patent:
May 25, 2004
Assignee:
Pfizer Inc
Inventors:
R. Mark Guinn, Subramanian Sam Guhan, Karl K Ng, Derek L. Tickner, Marcus Douglas Ewing, Clifford N. Meltz, Bryan Li, Kees Pouwer
Abstract: The invention relates to crystal forms of 6-[(4-chloro-phenyl)-hydroxy-(3-methyl-3H-imidazol-4-yl)-methyl]-4-(3-ethynyl-phenyl)-1-methyl-1H-quinolin-2-one, 2,3-dihydroxy butanedioate salts having the formula shown below:
and to pharmaceutical compositions containing the above compound, methods of treating hyperproliferative diseases, such as cancers, in mammals, especially humans by administering the above compound, and to methods of preparing the crystal forms of the above compound and related compounds.
Type:
Grant
Filed:
May 20, 2003
Date of Patent:
May 11, 2004
Assignee:
Pfizer Inc
Inventors:
Joseph P. Lyssikatos, Derek L. Tickner, Linda S. Newton, Zheng J. Li, Clifford N. Meltz