SMALL MOLECULE MYRISTATE INHIBITORS OF BCR-ABL AND METHODS OF USE

摘要

The present invention provides novel heteroaryl compounds having a pyrimidine-containing core that is linked to a 4-trifluoromethoxyphenyl group via an amine linker. Such compounds are useful for the treatment of cancers.

主权项

1. A compound of formula I, or pharmaceutically acceptable salt wherein
each of X1, X2, or X3 is independently NR1, CR1, C(O), O, or S;each R1 is independently selected from H, an optionally substituted C1-6alkyl, an optionally substituted C3-12cycloalkyl, an optionally substituted C3-12heterocycloalkyl, an optionally substituted C3-12aryl, an optionally substituted C3-12heteroaryl, an optionally substituted C1-6aralkyl, an optionally substituted C1-6heteroaralkyl, an optionally substituted C1-6haloalkyl, an optionally substituted (CH2)nC3-12heterocycloalkyl, an optionally substituted (CH2)nC3-12aryl, an optionally substituted (CH2)nC3-12heteroaryl, an optionally substituted (CH2)nC3-12cycloalkyl, C1-6haloalkyl, C1-6-aminoalkyl, hal, (CH2)nC(O)Rx, (CH2)nC(O)ORx, (CH2)nC(O)NRxRx, —(CH2)nC(O)NRxRxS(O)2Rx; —C(O)Rx, —C(S)Rx, —C(NR)Rx, —SRx, —S(O)Rx, —S(O)2Rx, —ORx, —NRxRx, nitro, cyano, or absent;each Rx, for each occurrence, is independently H, an optionally substituted C1-6alkyl, an optionally substituted C3-12cycloalkyl, an optionally substituted C3-12heterocycloalkyl, an optionally substituted C3-12aryl, an optionally substituted C3-12heteroaryl, C1-6haloalkyl; NHNHR2, or C(NH)NH2;R2 is H or C1-6 alkyl;Y is H, OH, NH2 or CH3;m is 1 or 2; andeach n is independently 0, 1 or 2.