Pyrimidinecarboxamides as CXCR2 modulators

摘要

There is disclosed pyridine- and pyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include pyridine- and pyrimidinecarboxamides compounds. More specifically, there is disclosed a genus of CXCR2 inhibitor compounds that are useful for treating a variety of inflammatory and neoplastic disorders.

主权项

1. A compound comprising a compound from formula (1): wherein R1 and R2 are independently selected from hydrogen, 2- or 3- or 4-halo-phenyl, heteroalkyl, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, or heterocyclylalkyl; wherein R3 is selected from —B(R4R5), —R6—B(R4R5), alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl, R6, —O—R6, —S(O)y—R6 (wherein y=0, 1, or 2), —P(O)—(R4R5), —N(R7R8), or C(O)—R9; wherein R6 is selected from alkyl, aryl, arylalkyl, cycloalkyl with 5 to 7 ring atoms, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl; wherein R4 and R5 are independently selected from hydrogen, hydroxyl, aryloxy, or alkoxy, or wherein R4 and R5 together form a cyclic ester, or an acid anhydride (either mixed or symmetrical); wherein R7 and R8 are independently selected from hydrogen, alkyl, haloalkyl, aryl, cycloalkyl, arylalkyl, heteroalkyl, heterocyclyl or heterocyclylalkyl; R7 and R8 are both oxygen to form a nitro group; or R7 and R8 together with the nitrogen to which they are attached, form a heterocyclyl; wherein R9 is selected from an alkyl consisting of 1 or 3-18 carbon atoms or a unsaturated alkyl group consisting of 1-18 carbon atoms, aryl, arylalkyl, cycloalkyl, heteroaryl, heteroarylalkyl, heterocyclyl or heterocyclylalkyl; and wherein X1 is nitrogen; X2 is selected from NH or oxygen; and n is an integer between 0 and 8; or pharmaceutical compositions thereof.