Azaindazole compounds and methods of use

摘要

Compounds are provided that act as potent antagonists of the CCR1 receptor, and have in vivo anti-inflammatory activity. The compounds are generally aryl piperazine derivatives and are useful in pharmaceutical compositions, methods for the treatment of CCR1-mediated diseases, and as controls in assays for the identification of competitive CCR1 antagonists.

主权项

1. A compound having the formula: or a pharmaceutically acceptable salt, hydrate or N-oxide thereof, wherein the subscript m is 0 or 1;R1 is methyl;R2a is hydrogen or fluoro;R2c is chloro;R2d is selected from the group consisting of methyl, methoxy, ethoxy and 2-fluoroethoxy;ring vertex a is N;ring vertex b is C(R3a);ring vertex c is N or C(R3a);ring vertex d is C(R3a);each R3a is independently selected from the group consisting of hydrogen, halogen, —ORf, —NRfRg, —Rh, —CN, —NO2, —NRgC(O)Rf, —S(O)2Rh, —N3, —Y, and —X3N3, wherein Y is selected from the group consisting of morpholinyl, oxazolyl, thiazolyl, imidazolyl, oxadiazolyl and pyridyl, each of which is optionally substituted with methyl and wherein each X3 is independently C1-4 alkylene, each Rf and Rg is independently selected from the group consisting of hydrogen, C1-8 alkyl and C1-8 haloalkyl, and each Rh is independently selected from the group consisting of C1-8 alkyl and C1-8 halo alkyl.