Aminopyrimidinecarboxamides as CXCR2 Modulators

摘要

There are disclosed aminopyrimidinecarboxamide compounds useful as pharmaceutical agents, synthesis processes, and pharmaceutical compositions which include aminopyrimidinecarboxamides 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 the group consisting of hydrogen, 2- or 3- or 4-halo-phenyl, heteroalkyl, alkyl, aryl, arylalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, and heterocyclylalkyl; wherein R3 and R4 are independently selected from the group consisting of hydrogen, heteroalkyl, alkyl, aminoalkyl, aryl, arylalkyl, carboxyalkyl, heteroaryl, heteroarylalkyl, cycloalkyl, cycloalkylalkyl, heterocyclyl, and heterocyclylalkyl, or R3 or R4 are independently an ionizing group selected from the group consisting of carboxylates, amines, phosphonates, and phosphates; wherein R3 and R4 are also independently selected from the group consisting of —B(R5R6), —BF3−M+, —R7—B(R5R6), —R7—BF3−M+, R7, —C(O)—R7, —O—R7, —S(O)y—R7 (wherein y=0, 1, or 2), —P(O)—(R5R6) and —N(R8R9); wherein R7 is selected from the group consisting of alkyl, aryl, arylalkyl, cycloalkyl, heteroaryl, heteroarylalkyl, heterocyclyl and heterocyclylalkyl; wherein M+ is a Group I or a Group II metal; wherein R5 and R6 are independently hydrogen, hydroxyl, aryloxy, or alkoxy, or wherein R5 and R6 together form a cyclic ester, or an acid anhydride (either mixed or symmetrical); and wherein R8 and R9 are independently selected from hydrogen, alkyl, haloalkyl, aryl, cycloalkyl, arylalkyl, heteroalkyl, heterocyclyl and heterocyclylalkyl; R8 and R9 are both oxygen to form a nitro group; or R8 and R9 together with the nitrogen to which they are attached, form a heterocyclyl;and pharmaceutical compositions thereof.