Hoffmann-la Roche Inc.

Jin-Jun Liu

Kin-Chun Thomas Luk

Zhuming Zhang

Qingjie Ding

Yi Heng Chen

Peter Michael Wovkulich

Giacomo Pizzolato

Apostolos Dermatakis

Xin-Jie Chu

David Joseph Bartkovitz

Li Chen

Tina Morgan Ross

Binh Vu

Chung-Chen Wei

Christophe Michoud

Jing Zhang

Jefferson Wright Tilley

Sung-Sau So

Song Yang

Vincent Stewart Madison

Yi Ren

Steven Gregory Mischke

Paige Erin Mahaney

Allen John Lovey

Norman Kong

Shaoqing Chen

Wendy Lea Corbett

Kshitij Chhabilbhai Thakkar

Bradford Graves

Nan Jiang

Emily Aijun Liu

Pamela Loreen Rossman

Chunlin Zhao

John Lawson Roberts

Andrzej Robert Daniewski

Marek Michal Kabat

George Kenneth Ehrlich

Frederick M Konzelmann

William Harris

Hanspeter Michel

There are provided compounds of the formula wherein X, Y, Z, R, Rand Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

Substituted pyrrolidine-2-carboxamides

There are provided compounds of the formula wherein X, Y, R, R, R, R, R, R, Rand Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

There is provided a compound of the formula 

Substituted spiroindolinones

There are provided compounds of the formula wherein X, Y, R, R, R, R, R, and Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.

N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions

There is provided a compound of formula I and the pharmaceutically acceptable salts and esters thereofwherein X, X, R, R, R, R, Rand Rare herein described. The compounds exhibit activity as anticancer agents.

4,4,5,5, tetrasubstituted imidazolines

There are provided spiroindolinone derivatives of the formula and pharmaceutically acceptable salts and esters thereof wherein R, R, R, Rand R are as herein described. The compounds exhibit anticancer activity.

Spiroindolinone derivatives

There are provided compounds of the general formulas wherein W, X, Y, R, R, R, and Rare as described herein. The compounds exhibit anticancer activity.

There are provided compounds of the general formulas wherein X, Y, R, R, Rand Rare as described herein. The compounds exhibit anticancer activity.

There are provided compounds of the general formulas wherein X, Y, R, R, R, Rand Rare as described herein. The compounds exhibit anticancer activity.

3,3-spiroindolinone derivatives

The present invention provides compounds of formula I wherein R, R, R, R, and Rare described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.

7,8-disubstituted pyrazolobenzodiazepines

Quinazoline thiazolinone derivatives which demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents.

Quinazoline thiazolinones

The present invention relates to spiroindolinone derivatives of the formula and their enantiomers and pharmaceutically acceptable salts and esters thereof wherein R, R, R, R, R, R, Rand R, are as herein described. The compounds have utility as antiproliferative agents, especially, as anticancer agents.

Substituted 1,5-naphthyridine azolinones inhibit Cdk1 and are selective against Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts have antiproliferative activity and are useful as anti-cancer agents.

Substituted 1,5-naphthyridine azolinones

1,5-Naphthyridine azolinone derivatives are disclosed. These compounds are inhibitors of CDK1 and are useful as antiproliferative agents, such as anti-cancer agents.

1,5-Naphthyridine azolinone

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. 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.

Growing community of inventors

Warren Township, NJ, United States of America

Jin-Jun Liu