Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

John Anthony Moliterni

Norman Kong

Nicholas J S Huby

Zhuming Zhang

Xin-Jie Chu

Shaoqing Chen

Peter Michael Wovkulich

Allen John Lovey

Binh Vu

Qingjie Ding

Nan Jiang

David Joseph Bartkovitz

Lee Apostle McDermott

John Guilfoyle Mullin, Jr

Omar Jose Morales

Yan Lou

Stacy W Remiszewski

Steven Gregory Mischke

Robert Alan Goodnow, Jr

Robert Francis Kester

Nader Fotouhi

Kang Le

Weiya Yun

Christophe Michoud

Xiaochun Han

Andrew Forrest Donnell

Kenneth Carey Rupert

Hong Wang

Nicholas John Silvester Huby

There are provided compounds of the formula 

Substituted hetero-azepinones

The present invention relates to compounds of the formula methods for the preparation thereof, and methods for their use. The compounds are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as cancer, cognitive and CNS disorders, and inflammatory/autoimmune diseases.

Substituted hydantoins

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

This invention relates to compounds of formula I: or pharmaceutically acceptable salts thereof,wherein R1, R2, R3, R4, R5, and R6 are described in this application. These compounds inhibit the enzymes MEK 1 and MEK2, protein kinases that are components of the MAP kinase signal transduction pathway and as such the compounds will have anti-hyperproliferative cellular activity.

The present invention relates to compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.

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.

4-Aminopyrimidine-5-one derivatives

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Bloomfield, NJ, United States of America

John Anthony Moliterni