3-Amido-4-anilinoquinolines as CSF-1R kinase inhibitors 2: Optimization of the PK profile

…, CT Campbell, DJ Cook, LA Dakin, DJ Del Valle…

Index: Scott, David A.; Bell, Kirsten J.; Campbell, Cheryl T.; Cook, Donald J.; Dakin, Les A.; Del Valle, David J.; Drew, Lisa; Gero, Thomas W.; Hattersley, Maureen M.; Omer, Charles A.; Tyurin, Boris; Zheng, Xiaolan Bioorganic and Medicinal Chemistry Letters, 2009 , vol. 19, # 3 p. 701 - 705

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Citation Number: 14

Abstract

The optimization of compounds from the 3-amido-4-anilinoquinolines series of CSF-1R kinase inhibitors is described. The series has excellent activity and kinase selectivity. Excellent physical properties and rodent PK profiles were achieved through the introduction of cyclic amines at the quinoline 6-position. Compounds with good activity in a mouse PD model measuring inhibition of pCSF-1R were identified.