Hoffmann-la Roche Inc.

Merck Sharp + Dohme Corp.

Takeda Pharmaceutical Company Limited

F. Hoffmann-la Roche Ag

Msd R&d (china) Co., Ltd.

Xin-Jie Chu

David Joseph Bartkovitz

Allen John Lovey

Qingjie Ding

Nan Jiang

Peter Michael Wovkulich

Zhuming Zhang

Binh Vu

Kin-Chun Thomas Luk

Chunlin Zhao

Li Chen

Jin-Jun Liu

Jing Zhang

John Anthony Moliterni

Jianping Cai

Yi Heng Chen

Michael P Dwyer

Bin Hu

John A McCauley

Peter D Williams

Sherman Tim Waddell

Steven Gregory Mischke

Gregori J Morriello

Tina Morgan Ross

Waleed Danho

Shaoqing Chen

Kartik M Keertikar

M Katharine Holloway

Christopher James Bungard

Adrian Wai-Hing Cheung

Lehua Chang

David Jonathan Bennett

Tao Ji

Bin Zhong

Catherine M Wiscount

Joseph Swistok

H Marie Loughran

Keith A Yagaloff

John Guilfoyle Mullin, Jr

Jefferson Wright Tilley

Dong-Ming Shen

Robert Alan Goodnow, Jr

Nader Fotouhi

Kang Le

Norman Kong

Kyungjin Kim

Hongju Li

Nicolas Zorn

Bradford Graves

Edward C Sherer

Lee Apostle McDermott

Alejandro Crespo

Nicholas J S Huby

Satyanarayana Tummanapalli

Pamela Loreen Rossman

Warren William McComas

Jesse J Manikowski

George Kenneth Ehrlich

Daniel Vincent Fishlock

Vijayasaradhi Sivalenka

Hongmao Sun

Hanspeter Michel

Jurgen Schultz

John Guifoyle Mullin, Jr

Jessie J Manikowski

Jurgen Schulz

Yao Wang

Bradford James Graves

Yi Chen

Binh Thanh Vu

The present invention is directed to compounds of Formula I pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. 

Piperazine derivatives as HIV protease inhibitors

The present invention is directed to piperazine derivatives, pharmaceutical compositions comprising the same, and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS.

There are provided compounds of the formula wherein X, Y, Z, 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, Z, R, R, Rand Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof. The compounds are useful as anticancer agents.

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 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.

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 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.

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

There are provided compounds of the formula wherein X, Y, R, R, R, R, R, and Rare as described hereinand enantiomers and pharmaceutically acceptable salts and esters thereof which are useful as anticancer agents.

N-substituted-pyrrolidines as inhibitors of MDM2-P-53 interactions

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

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 compounds of the formula which are useful in treating diseases characterized by the hyperactivity of MEK. Accordingly the compounds are useful in the treatment of diseases, such as, cancer, cognative and CNS disorders and inflammatory/autoimmune diseases.

Substituted hydantoins

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Livingston, NJ, United States of America

Xin-Jie Chu