422270-30-2Relevant articles and documents
Structure-activity relationships of novel, highly potent, selective, and orally active CCR1 antagonists
Xie, Yun Feng,Lake, Kirk,Ligsay, Kathleen,Komandla, Mallareddy,Sircar, Ila,Nagarajan, Gobi,Li, Jian,Xu, Kui,Parise, Jason,Schneider, Lisa,Huang, Ding,Liu, Juping,Dines, Kevin,Sakurai, Naoki,Barbosa, Miguel,Jack, Rick
, p. 3367 - 3372 (2008/02/07)
Design and synthesis of a series of 3-amino-4-(2-(2-(4-benzylpiperazin-1-yl)-2-oxoethoxy)phenylamino)cyclobutenedione derivatives as novel CCR1 antagonists are described. Structure-activity relationship studies led to the identification of compound 22, which demonstrated potent binding activity, functional antagonism of CCR1 as well as good species cross-reactivity. In addition, compound 22 also showed desirable pharmacokinetic profiles and was selected for in vivo studies in the mouse collagen-induced arthritis model.
Methods of using piperazine derivatives
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, (2008/06/13)
The present invention relates to compounds of the formula I and the pharmaceutically acceptable forms thereof; wherein X, Y, a, b, c, d, R1, R2, R3, R4 and R5 are as defined herein. Moreover, the present invention is also directed at pharmaceutical compositions comprising a compound of the formula I and a pharmaceutically acceptable carrier. Furthermore, the present invention is directed at methods of using the herein described compounds and compositions for treating or preventing a disorder or condition that can be treated or prevented by antagonizing the CCR1 receptor in a mammal.