Bantam Pharmaceutical, LLC

Schering Corporation

Neogenesis Drug Discovery, Inc.

Neogenesis, Inc.

Merck Sharp + Dohme Corp.

Gerald W Shipps

Neng-Yang Shih

Alan B Cooper

M Arshad Siddiqui

Ronald J Doll

Malcolm MacCoss

Timothy J Guzi

Michael P Dwyer

Kamil Paruch

Stephane L Bogen

Vincent Stewart Madison

Janeta Popovici-Muller

Joseph Michael Kelly

Kevin J Wilson

Stephane Ciblat

Huw M Nash

Phieng Siliphaivanh

Malcolm Maccoss

Manami Shizuka

Matthew Ernst Voss

Yuan Liu

Sunil Paliwal

Alan W Hruza

Peter Orth

Umar Faruk Mansoor

Tong Wang

Li Xiao

Johannes H Voigt

Abdelghani Achab

Matthew J Kostura

Thierry Olivier Fischmann

Yongqi Deng

Xiaolei Gao

Craig R Gibeau

Kartik M Keertikar

Christian Fischer

Hon-Chung Tsui

Matthew H Daniels

Jayaram R Tagat

Lianyun Zhao

Latha G Nair

Yaolin Wang

Binyuan Sun

Rumin Zhang

Kristin E Rosner

Weidong Pan

Zhaoyang Meng

Jagdish A Desai

Robert Sun

William T Windsor

Jose S Duca

Sobhana Babu Boga

David Benjamin Belanger

Panduranga Adulla P Reddy

Mehul F Patel

Luis E Torres

Lea Constantineau-Forget

Seth N Birnbaum

Hugh Y Zhu

Chantal Grand-Maitre

Patrick J Curran

Hongbo Zeng

Xiaohua Huang

Liang Zhu

Satish Jindal

Martin Dery

Panduranga Adulla Reddy

Abdul-Basit Alhassan

Adam J Schell

Shuyi Tang

Yang Nan

Duan Liu

Cliff C Cheng

Praveen K Tadikonda

Nicolas Bruneau-Latour

Edward A Wintner

Yao Ma

Youhao Dong

Krishna Kalghatgi

Matthew Richards

Todd W Mayhood

Tzu Tshin Wong

Blake Hamann

Emma M Lees

Xiangyu Guo

Vibha Oza

Amin Nomeir

Sie-Mun Lo

Amit K Mandal

Sanjay Srivastava

Vu Linh Ly

Jedd Levine

Giovanna Scapin

Brian Robert Lahue

Xin Yao

Michael Luther

Margarita Kirova-Snover

Danny J Hicklin

Subrahmanyam Gudipati

Disclosed are methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formula (I), in which X, X, Z, Z, the ring system denoted by 'a', R, L, L, Q, L, R, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene.

Methods of using substituted pyrazole and pyrazole compounds and for treatment of hyperproliferative diseases

Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure and pharmaceutically acceptable salts and N-oxides thereof, wherein X, X, Z, Z, the ring system denoted by 'a', R, A, L, A, L, L, Q, L, R, A, L, A, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism.

Substituted pyrazole and pyrrole compounds and methods for using them for inhibition of initiation of translation and treatment of diseases and disorders relating thereto

Disclosed are compounds useful, for example, in methods of treating hyperproliferative disorders such as cancer, methods of arresting the cell cycle in cancer cells, methods of inhibiting glutathione synthesis in cancer cells, and associated compounds for use and uses in medicaments. In certain embodiments, the methods, uses and compounds are provided with reference to compounds of the structural formulae (Ia), (Ib), (Ic), (Id) and (Ie), in which R, L, L, Q, L, R, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein are especially active against cancers having a mutant KRAS gene. 

Substituted pyrazole compounds and methods of using them for treatment of hyperproliferative diseases

Disclosed are pyrazole compounds, as well as pharmaceutical compositions and methods of use thereof. One embodiment is a compound having the structure (I) and pharmaceutically acceptable salts and/V-oxides thereof, wherein X, X, Z, Z, the ring system denoted by 'a', R, A, L, A, L, L, Q, L, R, A, L, A, L, R, L, and Rare as described herein. In certain embodiments, compounds disclosed herein disrupt the eIF4E/eiF4G interaction, and can be used to treat hyperproliferative disorder, a neurological disease or disorder, or autism. 

The present invention provides a method for identifying a member of a mass-coded combinatorial library which is a ligand for biomolecule and assessing the effect of the binding of the ligand to the biomolecule. The mass-coded molecular library comprises compounds of the general formula XY, wherein n is an integer from 2 to about 6, X is a scaffold and each Y is, independently, a peripheral moiety. The mass-coded combinatorial library is produced by reacting a scaffold precursor with a sufficient number of distant peripheral moiety precursors such that there exist at least about 250 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors.

Method for producing and screening mass-coded combinatorial libraries for drug discovery and target validation

The invention relates to the inhibition of hepatitis C virus (HCV) replication. In particular, embodiments of the invention provide compounds and methods for inhibiting HCV RNA-dependent RNA polymerase enzymatic activity. The invention also provides compositions and methods for the prophylaxis and treatment of HCV infection.

Pyrazolo[1,5a]pyrimidine compounds as antiviral agents

The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y) , where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups. Methods of use of the mass-coded combinatorial library produced by this method for identifying a ligand to a particular biomolecule are also disclosed.

The present invention provides a method for producing a mass-coded combinatorial library comprising a set of compounds having the general formula X(Y),, where X is a scaffold, each Y is, independently, a peripheral moiety, and n is an integer greater than 1. The method comprises selecting a peripheral moiety precursor subset from a peripheral moiety precursor set. The subset includes a sufficient number of peripheral moiety precursors that at least about 50 distinct combinations of n peripheral moieties derived from the peripheral moiety precursors in the subset exist. The subset of peripheral moiety precursors is selected so that at least about 90% of all possible combinations of n peripheral moieties derived from the subset have a molecular mass sum which is distinct from the molecular mass sums of all of the other combinations of n peripheral moieties. The method further comprises contacting the peripheral moiety precursor subset with a scaffold precursor which has n reactive groups. Methods of use of the mass-coded combinatorial library produced by this method for identifying a ligand to a particular biomolecule are also disclosed.

Method for producing and screening mass coded combinatorial libraries for drug discovery and target validation

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Boston, MA, United States of America

Gerald W Shipps