Hoffmann-la Roche Inc.

Takeda Pharmaceutical Company Limited

F. Hoffmann-la Roche Ag

Peter Michael Wovkulich

Milan R Uskokovic

Allen John Lovey

Qingjie Ding

Enrico G Baggiolini

Giacomo Pizzolato

Jin-Jun Liu

Xin-Jie Chu

Kin-Chun Thomas Luk

Shaoqing Chen

Christine E Brotherton-Pleiss

Sung-Sau So

Binh Vu

Andrew D Batcho

Hongju Li

Gary A Truitt

David Joseph Bartkovitz

Yan Lou

Yimin Qian

Matthew C Lucas

Shawn David Erickson

Francisco Javier Lopez-Tapia

Fariborz Firooznia

Timothy D Owens

Steven Gregory Mischke

Ryan Craig Schoenfeld

Roland Joseph Billedeau

Johannes Cornelius Hermann

Kyungjin Kim

Chung-Chen Wei

Buelent Kocer

Steven Joseph Berthel

Joshua Jahmil Kennedy-Smith

Nan Jiang

Saul Jaime-Figueroa

Fernando Padilla

Stephen Deems Gabriel

Jenny Tan

John A McLane

John Anthony Moliterni

Jianping Cai

Zhi Chen

Xiaochun Han

Lin Yi

John Guilfoyle Mullin, Jr

Lucja Orzechowski

Ramona Hilgenkamp

Ann Goldstein

Joseph P Lyssikatos

Yi Heng Chen

Matthew Michael Hamilton

Ce Wang

Anthony A Estrada

Huifen Chen

Vincent Stewart Madison

Yi Ren

Javier De Vicente Fidalgo

Achyutharao Sidduri

Michael Soth

Zhuming Zhang

Robert Alan Goodnow, Jr

Kang Le

Norman Kong

Stephen Matthew Lynch

Kshitij Chhabilbhai Thakkar

Bradford Graves

Xiaohu Zhang

John Lawson Roberts

Joshua Kennedy-Smith

Urvashi Hooda Dhingra

Yuki Takehana

Haruyoshi Shirai

Nami Yabuki

Counde O'yang

Hongmao Sun

Binh Thanh Vu

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 invention is concerned with the compounds of formula (I): and pharmaceutically acceptable salts thereof, wherein Y, R1, R2 and R3 are 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 of formula (I) are antagonists of the TRPA1 channel and may be useful in treating inflammatory diseases and disorders associated with that channel.

Substituted phenylcarbamate compounds

The present invention relates to the use of novel pyrrolo[2,3-b]]pyrazines wherein all variable substituents are defined as described herein, which are SYK inhibitors and are useful for the treatment of auto-immune and inflammatory diseases. 

Pyrrolo[2,3-B]pyrazines as SYK inhibitors

This application discloses 6-(2-Hydroxymethyl-phenyl)-2-methyl-2H-pyridazin-3-one derivatives according to generic Formula I: wherein, variables X, R, and Y, are defined as described herein, which inhibit Btk. The compounds disclosed herein are useful to modulate the activity of Btk and treat diseases associated with excessive Btk activity. The compounds are further useful to treat inflammatory and auto immune diseases associated with aberrant B-cell proliferation, such as rheumatoid arthritis. Also disclosed are compositions containing compounds of Formula I and at least one carrier, diluent or excipient.

Inhibitors of bruton's tyrosine kinase

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 invention is directed to compounds of formula (1) and pharmaceutically acceptable salts thereof, methods for the preparation thereof, and methods of use thereof.

Thiazolyl-benzimidazoles

The present invention provides PLK1 inhibitor compounds of formula I: useful in the treatment or control of cell proliferative disorders, particularly oncological disorders. These compounds and formulations containing such compounds may be useful in the treatment or control of solid tumors, such as, for example, breast, colon, lung and prostate tumors and other oncological diseases such as non-Hodgkin's lymphomas. Also provided are intermediate compounds useful in the synthesis of compounds of formula I.

Halo-substituted pyrimidodiazepines

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 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 provides compounds of formula I wherein R, R, R, R, and Rare described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.

7,8-disubstituted pyrazolobenzodiazepines

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.

4-Aminopyrimidine-5-one derivatives

Disclosed is a novel method for synthesizing pyrazolobenzodiazepines of formula Iusing intermediates of formula Pyrazolobenzodiazepines of formula I are useful in the treatment and control of solid tumors.

Method for synthesizing pyrazolobenzodiazepines

Disclosed are novel pyrazolobenzodiazepines having the formula These compounds are useful in the preparation of the pyrazolobenzodiazepines of formula I, which are useful in the treatment and control of solid tumors.

Pyrazolobenzodiazepines

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Nutley, NJ, United States of America

Peter Michael Wovkulich