Hoffmann-la Roche Inc.

John Guilfoyle Mullin, Jr

Allen John Lovey

Qingjie Ding

Peter Michael Wovkulich

Nader Fotouhi

Binh Vu

Xin-Jie Chu

Nan Jiang

David Joseph Bartkovitz

Emily Aijun Liu

John Anthony Moliterni

Li Chen

Paul Gillespie

Norman Kong

Kyungjin Kim

Giuseppe Federico Weber

Warren William McComas

Agostino Perrotta

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 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.

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Hawthorne, NJ, United States of America

John Guilfoyle Mullin, Jr