Array Biopharma Inc.

Bristol-myers Squibb Compnay

D David Hennings

Qian Zhao

Joseph P Lyssikatos

James P Rizzi

George T Topalov

Mark C Munson

Mark Laurence Boys

Martha E Rodriguez

John J Venit

Weidong Liu

Fredrik Pehr Marmsater

Victor W Rosso

Jingyang Zhu

Robert Kirk DeLisle

April L Kennedy

Robert Kirk Delisle

Gary D Madding

Jason G Chen

Michael E Randazzo

Bryson Rast

Julie Marie Greschuk

Atul S Kotnis

Fredrik P Marmsäter

Robert P Discordia

Matthew David Medina

Michael F Bradley

Francis J Okuniewicz

Susanne Kiau

Compounds of Formula (I): and pharmaceutically acceptable salts thereof in which R, R, R, Rand Rhave the meanings given in the specification, are inhibitors of cFMS and are useful in the treatment of bone-related diseases, cancer, autoimmune disorders, inflammatory diseases, cardiovascular diseases and pain. 

Substituted N-(1H-indazol-4-yl)imidazo[1,2-a]pyridine-3-carboxamide compounds as cFMS inhibitors

This invention provides compounds of Formula I wherein B, G, A, E, R, R, R, m and n are as defined herein, which are useful as type I receptor tyrosine kinase inhibitors, and methods of use thereof in the treatment of hyperproliferative disorders in mammals.

N4-phenyl-quinazoline-4-amine derivatives and related compounds as ErbB type I receptor tyrosine kinase inhibitors for the treatment of hyperproliferative diseases

Provided is a dynamic resolution method of enriching a desired isomer of an alpha-substituted carboxylic acid relative to an undesired isomer, the method comprising: (a) in a solvent, contacting the alpha-substituted carboxylic acid, wherein the alpha substitution is with a leaving group and wherein the alpha carbon is chiral, with a homochiral amine to form a salt that is partially insoluble under selected reaction conditions, wherein the homochiral amine is selected so that the solubility of the amine salt of the undesired alpha-substituted carboxylic acid is greater than that of the amine salt of the desired alpha-substituted carboxylic acid under the selected reaction conditions; (b) reacting under the selected reaction conditions the salt with a nucleophile, wherein the reacting is effective in producing a net increase in the less soluble amine salt of the alpha-substituted carboxylic acid, and wherein the selected conditions are selected to (i) promote nucleophilic substitution of the nucleophile and the leaving group or (ii) to produce the increase in the less soluble amine salt in the absence of a strong base; and (c) maintaining the reaction for a period of time effective to increase the amount of the desired alpha-substituted carboxylic acid isomer.

Dynamic resolution of isomers and resolved isomers

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Loveland, CO, United States of America

D David Hennings