Schering Corporation

Merck Sharp + Dohme Corp.

Bantam Pharmaceutical, LLC

Pharmacopeia Inc.

Merck Sharp + Dohme B.v.

Schering Coporation

Alan B Cooper

Viyyoor Moopil Girijavallabhan

Ronald J Doll

Jagdish A Desai

Anil K Saksena

James J-s Wang

Gerald Wayne Shipps, Jr

Hugh Y Zhu

Ashit K Ganguly

Joseph Michael Kelly

Arthur G Taveras

Dinanath F Rane

Yongqi Deng

Liang Zhu

Raymond G Lovey

Xiaolei Gao

Timothy J Guzi

Alan K Mallams

M Arshad Siddiqui

Jianping Chao

Sobhana Babu Boga

Abdul-Basit Alhassan

F George Njoroge

Stephane Ciblat

Tattanahalli L Nagabhushan

Lea Constantineau-Forget

Chantal Grand-Maitre

Gerald W Shipps

Sie-Mun Lo

John J Baldwin

Neng-Yang Shih

James Han Wang

Carmen S Alvarez

Tong Wang

Yang Nan

Johan A Ferreira

Nicolas Bruneau-Latour

Martin Dery

William N Turner

Xiangyu Guo

Ge Li

Vincent Stewart Madison

Corey Strickland

Sunil Paliwal

Alan W Hruza

Li Xiao

Hon-Chung Tsui

Binyuan Sun

Robert Sun

Ahmed Abdi Samatar

Chia-Yu Huang

Tarik Lalwani

Patrick J Curran

Xiaohua Huang

Cynthia J Aki

Youhao Dong

Vu Linh Ly

Hao Wu

Adriano Afonso

Kevin J Wilson

Younong Yu

Huw M Nash

Jian Liu

Phieng Siliphaivanh

Ronald M Kim

Patrick A Pinto

Umar Faruk Mansoor

Tjeerd Barf

Matthew J Kostura

Abdelghani Achab

Rajan Anand

Jay Weinstein

Kartik M Keertikar

Christian Fischer

Matthew H Daniels

Jayaram R Tagat

Chundao Yang

John C Reader

Kristin E Rosner

Ray Anthony James

Adrianus Petrus Antonius De Man

Shilan Liu

John J Wright

Edwin Jao

Allard Kaptein

Bancha Vibulbhan

Corey E Bienstock

Mehul F Patel

Christiaan Gerardus Johannes Maria Jans

Arthur A Oubrie

Henry M Vaccaro

Johannes Bernardus Maria Rewinkel

Adam J Schell

Brendan O'Boyle

Jacobus C H M Wijkmans

Bama Santhanam

Keith P Minor

Hans C A Raaijmakers

Azim Alan Celebi

This disclosure relates generally to crystalline polymorphs of a thiazolylpyrazole derivative, pharmaceutical compositions comprising them, and methods of using the crystalline polymorphs and their compositions.

Crystalline polymorphs of a 1-thiazol-2-yl-pyrazole-5-carboxylic acid derivative

This disclosure relates generally to improved methods of preparing pyrazolylthiazole-containing compounds and their intermediates.

Methods for making thiazolypyrazole carboxylic acids and intermediates therefor

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. 

Provided are 6-5 membered fused pyridine ring compounds according to Formula (I) or pharmaceutically acceptable salts thereof, pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of 6-5 membered fused pyridine ring compounds in the treatment of Bruton's Tyrosine Kinase (Btk) mediated disorders. 

BTK Inhibitors

The present invention provides a compound of the Formula I, or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R, R, R, m and are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions that comprise the above compounds, and methods of treating cancer using the same. 

Indazole derivatives useful as ERK inhibitors

Disclosed are the ERK inhibitors of Formula (I): (Formula (I)) and the pharmaceutically acceptable salts thereof. All substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of Formula (I). 

Fused pyrazole derivatives as novel ERK inhibitors

Disclosed are the ERK inhibitors of formula (1): and the pharmaceutically acceptable salts thereof, wherein: A is a five membered monocyclic heteroaryl ring; and B is a monocyclic heterocycloalkyl ring, or a monocyclic heterocycloalkenyl ring, or a bridged monocyclic heterocycloalkyl ring, or a fused (monocyclic heterocycloalkyl ring) cyclopropyl ring. Also disclosed are methods of treating cancer using the compounds of formula (1). 

Compounds that are ERK inhibitors

The present invention provides a compound of the Formula I: (Formular I should be inserted here) or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2 and R3 are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. 

Heterocyclic compounds as ERK inhibitors

The present invention provides a compound of the Formula I: Formula I or a pharmaceutically acceptable salt, solvate or ester thereof, wherein R, R1, R2, R3, R4, X, m and n are as defined herein. The compounds are ERK inhibitors. Also disclosed are pharmaceutical compositions comprising the above compounds and methods of treating cancer using the same. 

Disclosed are the ERK inhibitors of formula 1.0: and the pharmaceutically acceptable salts, and solvates thereof. Q is a tetrahydropyridinyl ring. All other substitutents are as defined herein. Also disclosed are methods of treating cancer using the compounds of formula 1.0. 

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. 

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.

Growing community of inventors

West Caldwell, NJ, United States of America

Alan B Cooper