Hoffmann-la Roche Inc.

Roche Palo Alto LLC

Takeda Pharmaceutical Company Limited

F. Hoffmann-la Roche Ag

Kin-Chun Thomas Luk

Yi Heng Chen

Jin-Jun Liu

Apostolos Dermatakis

Steven Gregory Mischke

Sung-Sau So

Peter Michael Wovkulich

Xin-Jie Chu

Christophe Michoud

Pamela Loreen Rossman

Zhuming Zhang

Paige Erin Mahaney

Shaoqing Chen

Jianping Cai

Xiaohu Zhang

Matthew C Lucas

Stefan Scheiblich

Michael Soth

Wendy Lea Corbett

Johannes Cornelius Hermann

David Joseph Bartkovitz

Fernando Padilla

Marek Michal Kabat

Jian Jeffrey Chen

Matthew Michael Hamilton

Ce Wang

Yi Ren

Dennis D Keith

Javier De Vicente Fidalgo

Achyutharao Sidduri

Robert Alan Goodnow, Jr

Ryan Craig Schoenfeld

Konrad Honold

Allen John Lovey

Giacomo Pizzolato

Kang Le

Georg Tiefenthaler

Stephen Matthew Lynch

Nikolaos Dimoudis

Jing Zhang

Tobias Gabriel

Hongju Li

Kshitij Chhabilbhai Thakkar

Joel McIntosh

Joshua Jahmil Kennedy-Smith

Emily Aijun Liu

Jutta Wanner

Andrzej Robert Daniewski

Joshua Kennedy-Smith

Wenjian Liu

William Harris

Frederick M Konzelmann

Wenwei Xie

Hongmao Sun

Hilke Sudergat

Oliver Tonn

Lee Edwin Lowrie, Jr

Counde O'yang

Yi Chen

Stephen M Lynch

Jr Lee Edwin Lowrie

The present invention relates to the use of novel thiazolopyrimidine derivatives 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.

Thiazolopyrimidine compounds

Compounds of formula and pharmaceutically acceptable salts thereof are described, as well as the pharmaceutical compositions containing said compounds and their pharmaceutically acceptable salts, and the use of said compounds and pharmaceutical compositions for the treatment, control or amelioration of AML.

Imidazo pyrazines

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

Pyrazolo pyrimidines

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 are provided compounds of the formula wherein R, R, R, X, Y, Q, Ring A and Ring B are as described. The compounds exhibit activity as anticancer agents.

Substituted thieno[3,2-C]pyridine-7-carboxylic acid derivatives

Disclosed are novel pyrazolo[3,4-d]pyrimidine derivatives that are inhibitors of Raf kinase. These compounds and their pharmaceutically-acceptable salts and esters are anti-proliferative agents useful in the treatment or control of proliferative disorders such as solid tumors, in particular breast tumor, colon tumor, lung tumor, prostate tumor, and melanoma. Also disclosed are a composition and a unit dose formulation comprising such a compound, or a pharmaceutically-acceptable salt or ester thereof, methods for making such compounds, and methods for using such compounds, or their pharmaceutically-acceptable salts or esters, in the treatment of proliferative disorders.

Pyrazolo[3,4-d]pyrimidine derivatives

There are provided compounds of the formula wherein R, R, R, X, ring A and ring B are as described. The compounds exhibit anticancer properties.

Substituted thieno[3,2-C]pyridine carboxylic acid derivatives

Compounds of formula I: wherein R, R, Rand Rare as defined herein. Also disclosed are methods of making the compounds, pharmaceutical compositions, methods of using the compounds for treatment of p38 MAP kinase-mediated diseases, and methods of using the compounds for treatment of Raf kinase-mediated diseases.

Kinase inhibitors and methods for using the same

The invention describes compounds of the general formula I or the pharmaceutically acceptable salts thereof,wherein R, R, Rand X are herein described,a process for their manufacture, medicaments containing them as well as the use of these compounds as pharmaceutically active agents. The compounds show activity as antiproliferative agents and may be especially useful for the treatment of cancer.

Oxindole 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 1,3,4-triaza-phenalene and 1,3,4,6-tetraazaphenalene derivatives are disclosed. These compounds inhibit epidermal growth factor receptor ('EGFR') tyrosine kinase. These compounds and their pharmaceutically acceptable salts and esters have antiproliferative activity and are useful, inter alia, in the treatment or control of cancer, in particular solid tumors. This invention also relates 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.

Phenalene derivatives

Disclosed are novel pyrimido compounds that are inhibitors of Src family of tyrosine kinases. These compounds and their pharmaceutically acceptable salts are anti-proliferative agents useful in the treatment or control of solid tumors, in particular breast, colon, hepatic and pancreatic tumors. Also disclosed are pharmaceutical compositions containing these compounds and methods of treating cancer.

Pyrimido compounds having antiproliferative activity

Disclosed are novel pyrimido compounds that are selective inhibitors of both KDR and FGFR kinases. These compounds and their pharmaceutically acceptable salts 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 and methods of treating cancer.

Growing community of inventors

North Caldwell, NJ, United States of America

Kin-Chun Thomas Luk