Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

David Joseph Bartkovitz

Xin-Jie Chu

Binh Vu

Allen John Lovey

Qingjie Ding

Nan Jiang

Peter Michael Wovkulich

Zhuming Zhang

Jin-Jun Liu

Chunlin Zhao

Kin-Chun Thomas Luk

Tina Morgan Ross

Jing Zhang

John Anthony Moliterni

John Guilfoyle Mullin, Jr

Yi Heng Chen

Hongju Li

Bradford Graves

Jianping Cai

Pamela Loreen Rossman

George Kenneth Ehrlich

Daniel Vincent Fishlock

Hanspeter Michel

Bradford James Graves

George Ehrlich

Yi Chen

Binh Thanh Vu

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, Z, R, R, Rand Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

There are provided compounds of the formula or the pharmaceutically acceptable salts thereof, wherein X, Y, Z, V, V, R, R, R, Rand Rare herein described. These compounds are useful as anticancer agents.

Chiral cis-imidazolines

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 are provided compounds of the formula wherein X, Y and Rto Rare described herein along with the enantiomers, pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

Spiroindolinone pyrrolidines

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 are provided compounds of the formula wherein R, R, R, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.

Substituted thieno[3,2-C]pyridine-7-carboxylic acid derivatives

Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.

Pyrazolo[3,4-d]pyrimidine derivatives

Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.

4-aminopyrimidine-5-one derivatives

Novel 2,6-diaminopyridine derivatives of formula wherein Rand Rare as defined below, are disclosed. These compounds inhibit cyclin-dependent kinases. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 2,6-diaminopyridine derivatives.

2,6-diaminopyridine derivatives

Novel 4-aminopyrimidine-5-one derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors. This invention is also directed to pharmaceutical compositions containing such compounds and to methods of treating or controlling cancer, most particularly the treatment or control of breast, lung, colon and prostate tumors. Also disclosed are intermediates useful in the preparation of these novel 4-aminopyrimidine-5-one derivatives.

Growing community of inventors

Nutley, NJ, United States of America

David Joseph Bartkovitz