Cortistatin analogues and synthesis thereof

摘要

The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: I and salts thereof, wherein R1, R2, R3, R4, n, and m are as defined herein; processes for preparing such compounds and intermediates thereto; pharmaceutical compositions comprising such compounds; methods for treating a proliferative disease; methods for treating a disease associated with aberrant angiogenesis; methods for inhibiting angiogenesis; and processes for preparing cortistatin A, J, K, and L, and analogs thereof.;

主权项

1. A compound of formula:or a pharmaceutically acceptable salt thereof,wherein:
each of the dashed lines independently represents the presence or absence of a bond; each instance of m and n is 1; R1 is substituted or unsubstituted heteroaryl; R2 is C1-C6 aliphatic; R3 is hydrogen; R4 is —N(RD)2; —NHC(═O)RD; —NRAC(═O)N(RD)2; or —NRDC(═O)ORD; and RA is hydrogen, a protecting group, an aliphatic moiety, a heteroaliphatic moiety, an acyl moiety, an aryl moiety, a heteroaryl moiety, alkoxy, aryloxy, alkylthio, arylthio, amino, alkylamino, dialkylamino, heteroaryloxy, or heteroarylthio moiety; and each occurrence of RD is independently hydrogen, a protecting group, aliphatic, heteroaliphatic, acyl, aryl, or heteroaryl.