Hoffmann-la Roche Inc.

Roche Palo Alto LLC

Takeda Pharmaceutical Company Limited

F. Hoffmann-la Roche Ag

Shaoqing Chen

Li Chen

Steven Gregory Mischke

Matthew C Lucas

Peter Michael Wovkulich

Johannes Cornelius Hermann

Yimin Qian

Achyutharao Sidduri

Kin-Chun Thomas Luk

Norman Kong

Christophe Michoud

John Anthony Moliterni

Nicholas J S Huby

Francisco Xavier Talamas

Robert Francis Kester

Sharada Shenvi Labadie

Allen John Lovey

Kang Le

Xin-Jie Chu

Hongju Li

Clara Jeou Jen Lin

Fernando Padilla

Andreas Kuglstatter

Jianping Cai

Nidhi Arora

Amy Geraldine Moore

Jutta Wanner

Yansheng Zhai

Omar Jose Morales

Eva Papp

Joseph P Lyssikatos

Yi Heng Chen

Yan Lou

Matthew Michael Hamilton

Sung-Sau So

Ce Wang

Anthony A Estrada

Huifen Chen

Stacy W Remiszewski

Shawn David Erickson

Javier De Vicente Fidalgo

Michael Soth

Zhuming Zhang

Ramakanth Sarabu

Robert Alan Goodnow, Jr

Nancy-Ellen Haynes

Ryan Craig Schoenfeld

Jin-Jun Liu

David Robert Bolin

Wendy Lea Corbett

Stephen Matthew Lynch

Christine E Brotherton-Pleiss

Kyungjin Kim

Kevin Richard Guertin

Kshitij Chhabilbhai Thakkar

Joshua Jahmil Kennedy-Smith

Kenneth C Rupert

Nathan Robert Scott

Zhi Chen

Xiaohu Zhang

Francis A Mennona

Andrew Forrest Donnell

Lin Yi

Joshua Kennedy-Smith

Kenneth Carey Rupert

Nam T Le

Martin Weisel

Jianping Lou

Hong Wang

Nicholas John Silvester Huby

Counde O'yang

Hongmao Sun

Clara Jeou Lin

Stephen M Lynch

Disclosed are compounds of Formula I, or pharmaceutically acceptable salts thereof, wherein W, X, Y, Z, R, R, R, Rand Rare as described in this application, and methods of using said compounds in the treatment of cancer. 

Tetrahydro-benzodiazepinones

Compounds of the formula I or II: wherein X, m, Ar, Rand Rare as defined herein. The subject compounds are useful for treatment of IRAK-mediated conditions.

Pyrazolo[1,5a]pyrimidine derivatives as IRAK4 modulators

The present invention relates to the use of novel compounds of Formula I: 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.

Thienopyrimidine compounds

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 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

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

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 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.

Substituted pyrimidodiazepines

Quinazoline thiazolinone derivatives which demonstrate CDK1 antiproliferative activity and are useful as anti-cancer agents.

Quinazoline thiazolinones

Thiazolinone quinoline derivatives having no substitution on the quinoline ring active as CDK1 inhibitors which are useful as anti-proliferation agents such as for treating solid tumors.

Thiazolinone unsubstituted quinolines

Thiazolinone monosubstituted quinoline derivatives where the quinoline ring is mono-substituted at the 4 positions which derivatives demonstrates CDK1 antiproliferative activity and are useful as anti-cancer agents.

Thiazolinone 4-monosubstituted quinolines

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Bridgewater, NJ, United States of America

Shaoqing Chen