Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Hudson Biopharma Inc.

Qingjie Ding

Nan Jiang

Allen John Lovey

Peter Michael Wovkulich

Jin-Jun Liu

Xin-Jie Chu

Zhuming Zhang

Kyungjin Kim

Jing Zhang

Warren William McComas

Giacomo Pizzolato

David Joseph Bartkovitz

Paul Gillespie

Binh Vu

Robert James Weikert

John Guilfoyle Mullin, Jr

Agostino Perrotta

Li Chen

Song Yang

Shawn David Erickson

Eric Mertz

Chung-Chen Wei

Bradford Graves

John Anthony Moliterni

Zhi Chen

John Lawson Roberts

Joseph Anthony Bilotta

Jefferson Wright Tilley

Sung-Sau So

Jean-Marc Plancher

Vincent Stewart Madison

Elbert Chin

Tina Morgan Ross

Norman Kong

Buelent Kocer

Stephen Deems Gabriel

Qiang Zhang

Feng Chi

Han Ma

John Guifoyle Mullin, Jr

Yang-sheng Sun

Binh Thanh Vu

Bradford James Graves

Yi Chen

Klaus Klumpp

The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection. 

Antiviral compounds

The present invention discloses compounds of Formula I: wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection.

The present invention discloses compounds of Formula (I): wherein the variables in Formula I are defined as described herein. Also disclosed are pharmaceutical compositions containing such compounds and methods for using the compounds of Formula I in the prevention or treatment of HCV infection. 

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.

Substituted pyrrolidine-2-carboxamides

There are provided compounds of the formula wherein X, Y and Rto Rare as described herein and the enantiomers and pharmaceutically acceptable salts and esters thereof which compounds have anticancer activity.

Spiroindolinone pyrrolidines

There are provided compounds of the formula and pharmaceutically acceptable salts and esters thereof The compounds are useful as anticancer agents.

Spiroindolinone derivatives

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.

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

Novel 4-aminopyrimidine-5-thione derivatives are disclosed. These compounds inhibit cyclin-dependent kinases, in particular Cdk1, Cdk2 and Cdk4. These compounds and their pharmaceutically acceptable salts 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.

4-aminopyrimidine-5-thione 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

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.

Novel pyrazolopyrimidines of formula (I): are discussed. These pyrazolopyrimidines are capable of inhibiting the activity of cyclin-dependent kinases, most particularly cyclin-dependent kinase 1 (Cdk1), cyclin-dependent kinase 2 (Cdk2), and cyclin-dependent kinase 4 (Cdk4) and are thus useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also provides 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.

Pyrazolopyrimidines

Novel diaminothiazoles of formula (I): are discussed. These compounds selectively inhibit the activity of Cdk4 and are thus useful in the treatment or control of cancer, in particular, the treatment or control of solid tumors. This invention also provides pharmaceutical compositions containing such compounds and methods of treating or controlling cancer, most particularly, the treatment or control of breast, lung, colon, and prostate tumors.

Diaminothiazoles

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

Disclosed are novel diaminothiazoles that are selective inhibitors of Cdk4. These compounds and their pharmaceutically acceptable salts and esters 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 as well as intermediates useful in the preparation of the compounds.

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Bridgewater, NJ, United States of America

Qingjie Ding