Schering Corporation

Merck Sharp + Dohme Corp.

Pharmacopeia Inc.

Pharmacopeia Drug Discovery, Inc.

Schering-Plough Corporation

Merck Gmbh

Schering Coporation

F. George Njoroge

Ronald J. Doll

John C. Reader

Alan K. Mallams

Dinanath F. Rane

Randall R. Rossman

Ge Li

John J. Baldwin

Ronald J Doll

Viyyoor Moopil Girijavallabhan

Alan K Mallams

F George Njoroge

Timothy J Guzi

Arthur G Taveras

Stacy W Remiszewski

Kamil Paruch

Michael P Dwyer

Carmen S Alvarez

Alan B Cooper

Ray Anthony James

Lawrence Wayne Dillard

Vinh D Tran

Haengsoon Park

John J Piwinski

Dinanath F Rane

Joanne M Petrin

Tarik Lalwani

Ronald L Wolin

Zhen Min He

Joseph Michael Kelly

Adriano Afonso

W Robert Bishop

Anil K Saksena

Vincent Stewart Madison

Yi-Tsung Liu

Kartik M Keertikar

Jagdish A Desai

Bernard R Neustadt

Stephane L Bogen

Elizabeth M Smith

Thierry Olivier Fischmann

Jonathan A Pachter

James J-s Wang

Jocelyn Rivera

John J Baldwin

Matthew Ernst Voss

Randall R Rossman

Charles V Magatti

Jianping Chao

Hugh Y Zhu

Elijah H Gold

Gerald Wayne Shipps, Jr

Michelle R Machacek

Manami Shizuka

B Wesley Trotter

Tin-Yau Chan

Douglas Walsh Hobbs

Christopher Francis Thompson

Michael Hale Reutershan

Latha G Nair

John C Reader

Francesc Xavier Fradera Llinas

Chad E Knutson

Ashit K Ganguly

Brian Alexander McKittrick

Michael D Altman

Corey Strickland

Vidyadhar Madhav Paradkar

Matthew Christopher

Yaolin Wang

Binyuan Sun

Weidong Pan

Yuan Tian

Michelle Martinez

Johan A Ferreira

Yao Ma

Neng-Yang Shih

Christopher J Dinsmore

M Arshad Siddiqui

Sunil Paliwal

Deen Tulshian

Alan W Hruza

Li Xiao

Yongqi Deng

Craig R Gibeau

Hon-Chung Tsui

Robert W Watkins

Robert Sun

Chia-Yu Huang

Bancha Vibulbhan

Liping Yang

Cynthia J Aki

Tong Wang

Yang Nan

Tin Yau Chan

David L Cutler

Youhao Dong

Keith P Minor

Walter Robert Bishop

Ming Liu

Brian Robert Lahue

Zhenmin He

Robert W Bishop

Joseph J Catino

Paul Kirschimeier

Loretta L Nielsen

Malcolm MacCoss

The present invention provides substituted pyrrolopyrimidines of Formula I as described herein or a pharmaceutically acceptable salt or solvate thereof: The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

Substituted pyrrolopyrimidines as HDM2 inhibitors

The present invention provides 2,6,7,8 Substituted Purines as described herein or a pharmaceutically acceptable salt thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

2,6,7,8 substituted purines as HDM2 inhibitors

The present invention provides a compound of Formula (1): as described herein or a pharmaceutically acceptable salt or solvate thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same. 

Macrocycles that increase p53 activity and the uses thereof

The present invention provides substituted imidazopyridines as described herein or a pharmaceutically acceptable salt or solvate thereof. The representative compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and potential methods of treating cancer using the same.

Substituted imidazopyridines as HDM2 inhibitors

The present invention provides a compound of Formula 1 as described herein or a pharmaceutically acceptable salt, solvate or ester thereof. The compounds are useful as inhibitors of the HDM2 protein. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same.

Substituted piperidines that increase p53 activity and the uses thereof

In its many embodiments, the present invention provides a method of inhibiting one or more cyclin dependent kinases in a patient comprising administering to said patient a therapeutically effective amount of at least one pyrazolo[1,5-a]pyrimidine compound or a pharmaceutical composition comprising such compound, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions. An example pyrazolo[1,5-a]pyrimidine compound useful in the present invention is shown below: 

Substituted pyrazolo[1,5-a]pyrimidines as cyclin dependent kinase inhibitors

Disclosed are the ERK inhibitors of formula 1.0: (Formula (A1)), and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine ring that can have a bridge or a fused ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula A1. 

Compounds that are ERK inhibitors

The present invention provide Imidazole Carboxamide Compounds of Formula (I): wherein D, T, R, R, R, and Rare as defined herein, and pharmaceutically acceptable salts of such Imidazole Carboxamide Compounds. The Imidazole Carboxamide Compounds are useful in the treatment of cancer and other aberrant conditions that result from overstimulation of the PDK-1 signaling pathway. 

N-phenyl imidazole carboxamide inhibitors of 3-phosphoinositide-dependent protein kinase-1

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, esters and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

In its many embodiments, the present invention discloses novel compounds, as inhibitors of HDM2 protein methods for preparing such compounds, pharmaceutical compositions including one or more such compounds, methods of treatment, prevention, inhibition, of one or more diseases associated with the HDM2 protein or P53 using such compounds or pharmaceutical compositions.

Substituted piperidines that increase P53 activity and the uses thereof

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts and solvates thereof. Q is a piperidine or piperazine ring that can have a bridge or a fused ring. The piperidine ring can have a double bond in the ring. All other substituents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0.

In its many embodiments, the present invention provides a novel class of pyrazolo[1,5-a]pyrimidine compounds as inhibitors of cyclin dependent kinases, methods of preparing such compounds, pharmaceutical compositions containing one or more such compounds, methods of preparing pharmaceutical formulations comprising one or more such compounds, and methods of treatment, prevention, inhibition, or amelioration of one or more diseases associated with the CDKs using such compounds or pharmaceutical compositions.

N-heteroaryl pyrazolopyrimidines as cyclin dependent kinase inhibitors

The present invention relates to compounds of Formula I or pharmaceutically acceptable salts or solvates thereof: The present invention provides compositions comprising these compounds that are useful for treating cellular proliferative diseases or disorders associated with KSP kinesin activity and for inhibiting KSP kinesin activity.

Compounds for inhibiting KSP kinesin activity

Disclosed are novel tricyclic compounds of the formula: and a pharmaceutically acceptable salts or solvates thereof. The compounds are useful for inhibiting farnesyl protein transferase. Also disclosed are pharmaceutical compositions comprising the compounds of formula (I). Also disclosed are uses of the compounds of formula (I) for the manufacture of a medicament for the treatment of cancer.

Farnesyl protein transferase inhibitors as antitumor agents

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Convent Station, NJ, United States of America

Ronald J Doll