Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Emily Aijun Liu

Binh Vu

Norman Kong

Nader Fotouhi

Steven Gregory Mischke

Allen John Lovey

Kyungjin Kim

Gregory Jay Haley

John Guilfoyle Mullin, Jr

Yi Heng Chen

Stephen Evan Webber

Kin-Chun Thomas Luk

Jin-Jun Liu

Christophe Michoud

Giuseppe Federico Weber

Andrzej Robert Daniewski

Marek Michal Kabat

Klaus B Simonsen

William Harris

Binh Thanh Vu

The present invention relates to compounds of the formula and the pharmaceutically acceptable salts and esters thereof, a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show antiproliferative activity and may be especially useful for the treatment of cancer.

CIS-imidazolines

The present invention provides compounds according to formula I having the designations provided herein, and pharmaceutically acceptable salts and esters thereof. These compounds inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.

Cis-imidazolines

The present invention provides compounds according to formula I and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity 

CIS-imidazoles

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR an FGFR kinases and are selective against LCK. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, lung and prostate tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Pyrimido compounds having antiproliferative activity

The present invention provides compounds having formula (II): wherein X, n, R&#x2013;Rare defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (II).

Substituted piperidines

The present invention provides compounds having formula (I):and formula (II):wherein X, n, and R-Rare defined herein, or a pharmaceutically acceptable salt thereof. The invention also provides a pharmaceutical composition comprising a therapeutically effective amount of a compound represented by formula (I) or (II) and a pharmaceutically acceptable carrier or excipient. The invention further provides a method for treating cancer comprising administering to a patient in need of such treatment a therapeutically effective amount of a compound represented by formula (I) or (II).

The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity.

The present invention provides compounds according to formula I and formula II and pharmaceutically acceptable salts and esters thereof, having the designations provided herein and which inhibit the interaction of MDM2 protein with a p53-like peptide and have antiproliferative activity

Substituted pyrroles suitable for continuous infusion

Disclosed are novel substituted pyrroles having the formula

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Nutley, NJ, United States of America

Emily Aijun Liu