Agouron Pharmaceuticals, Inc.

Cancer Research Technology Limited

Pfizer Corporation

Naresh Nayyar

Steven Lee Bender

Srinivasan Babu

Michael J Melnick

Terence J Moran

Qingping Tian

Travis Paul Remarchuk

Raymond Dagnino, Jr

Junhua Tao

Lennert J Mitchell, Jr

Bennett C Borer

Ming Guo

Jia Liu

Jan-Jon Chu

Chunrong Ma

Zhen-Ping Wu

Yi Li

Mark Bryan Mitchell

Nebojsa Slobodan Stanković

Aparna Nadig Srirangam

Nebojsa Slobodan Stankovic

Bennett Chaplin Borer

This invention relates to a new and convergent route to small molecule inhibitors of poly(ADP-ribose) polymerase, such as 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, via a key Sonogashira coupling reaction and a CuI-promoted indole formation.

Method of preparing poly(ADP-ribose) polymerases inhibitors

The present invention relates to novel polymorphic and amorphous forms of a phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-cd]indol-6-one, and to processes for their preparation. Such polymorphic forms may be a component of a pharmaceutical composition and may be used to treat a mammalian disease condition mediated by poly(ADP-ribose) polymerase activity including the disease condition such as cancer.

Polymorphic and amorphous forms of the phosphate salt of 8-fluoro-2-{4-[(methylamino)methyl]phenyl}-1,3,4,5-tetrahydro-6H-azepino[5,4,3-ce]indol-6-one

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses.

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors and key intermediates

Efficient synthetic routes for the preparation of rhinovirus protease inhibitors of formula I, as well as key intermediates useful in those synthetic routes. These compounds of formula I, as well as pharmaceutical compositions that contain these compounds, are suitable for treating patients or hosts infected with one or more picornaviruses

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San Diego, CA, United States of America

Naresh Nayyar