Cortistatin analogues and syntheses thereof
AssigneePresident and Fellows of Harvard College
InventorsAlec Nathanson Flyer, Hong Myung Lee, Andrew G. Myers, Cristina Montserrat Nieto-Oberhuber, Matthew D. Shair, Chong Si Allston
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Abstract
The present invention relates to analogs of cortistatin A, J, K, and L, having the general formula: 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.
Claims22
A method of treating aberrant angiogenesis comprising administering a therapeutically effective amount of a compound or a pharmaceutically acceptable salt thereof, to a subject suffering from aberrant angiogenesis, wherein the compound is of formula:
- wherein:
- each of the dashed lines independently represents the presence or absence of a bond;
- n is 1;
- m 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;
- and
- each occurrence of RD is independently hydrogen, a protecting group, aliphatic;
- heteroaliphatic, acyl, aryl, or heteroaryl.
Dependencies are inferred from the claim text.