Hoffmann-la Roche Inc.

F. Hoffmann-la Roche Ag

Allen John Lovey

Michael Rosenberger

Qingjie Ding

Peter Michael Wovkulich

Xin-Jie Chu

Nan Jiang

Edward R Aig

John W Coffey

John Guilfoyle Mullin, Jr

Binh Vu

Kyungjin Kim

Hongju Li

David Joseph Bartkovitz

Nader Fotouhi

Norman Kong

Warren William McComas

Li Chen

Peter Mohr

Michael J Klaus

Sung-Sau So

Javier De Vicente Fidalgo

Michael Soth

Shaoqing Chen

Johannes Cornelius Hermann

Emily Aijun Liu

John Anthony Moliterni

Chunlin Zhao

Binh Thanh Vu

Joseph P Lyssikatos

Jefferson Wright Tilley

Yimin Qian

Eric Brian Sjogren

Matthew Michael Hamilton

Ce Wang

Anthony A Estrada

Huifen Chen

Matthew C Lucas

Shawn David Erickson

Paul Gillespie

Achyutharao Sidduri

Kin-Chun Thomas Luk

Ryan Craig Schoenfeld

Jin-Jun Liu

Giacomo Pizzolato

Stephen Matthew Lynch

Christine E Brotherton-Pleiss

Adrian Wai-Hing Cheung

Joshua Jahmil Kennedy-Smith

Bradford Graves

Fernando Padilla

Jianping Cai

Xiaohu Zhang

Giuseppe Federico Weber

Zhi Chen

John Lawson Roberts

Remy Lemoine

Lin Yi

Joshua Kennedy-Smith

Louise H Foley

Agostino Perrotta

Counde O'yang

Stephen B Ferguson

John Guifoyle Mullin, Jr

Bradford James Graves

Stephen M Lynch

The invention is concerned with the compounds of formula (I): and salts thereof, wherein X, Y, Z, R, R, R, R, R, Rand Rare defined in the detailed description and claims. In addition, the present invention relates to methods of manufacturing and using the compounds of Formula (I) as well as pharmaceutical compositions containing such compounds. The compounds may be useful in treating diseases and conditions mediated by TRPA1, such as pain.

Substituted sulfonamide compounds

The present invention relates to the use of novel pyrrolopyrazine derivatives of Formula I, wherein the variables are defined as described herein, which inhibit JAK and SYK and are useful for the treatment of auto-immune and inflammatory diseases.

Pyrrolopyrazine kinase inhibitors

The present invention relates to the use of novel compounds of Formula I, wherein the variables m, n, p, q, Q, r, R, R', X, X&#x2032;, Y, Z, Z, and Zare defined as described herein, which inhibit JAK and are useful for the treatment of auto-immune and inflammatory diseases.

Inhibitors of JAK

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 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

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-aminothiazole derivatives 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 4-aminothiazole derivatives.

4-Aminothiazole derivatives

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.

Growing community of inventors

North Caldwell, NJ, United States of America

Allen John Lovey