BROMODOMAIN BINDING REAGENTS AND USES THEREOF

摘要

The present invention provides compounds of the Formula (I) and (II), and salts thereof, wherein L1, L2, A, B, Z, and RO are as defined herein. The present invention also provides synthetic intermediates, methods of preparation and use, and kits comprising such compounds. Such compounds, when bound to a label or probe (B), may be useful in various assays for identifying bromodomain binding agents, for example, specific for the BET-family of bromodomains.;

主权项

1. A compound of Formula (I):or salt thereof;wherein:
L1 is a bond or a linking group selected from the group consisting of substituted or unsubstituted alkylene; substituted or unsubstituted alkenylene; substituted or unsubstituted alkynylene; substituted or unsubstituted heteroalkylene; substituted or unsubstituted heteroalkenylene; substituted or unsubstituted heteroalkynylene; substituted or unsubstituted heterocyclylene; substituted or unsubstituted carbocyclylene; substituted or unsubstituted arylene; substituted or unsubstituted heteroarylene; and combinations thereof; L2 is a linking group selected from the group consisting of substituted or unsubstituted alkylene; substituted or unsubstituted alkenylene; substituted or unsubstituted alkynylene; substituted or unsubstituted heteroalkylene; substituted or unsubstituted heteroalkenylene; substituted or unsubstituted heteroalkynylene; substituted or unsubstituted heterocyclylene; substituted or unsubstituted carbocyclylene; substituted or unsubstituted arylene; substituted or unsubstituted heteroarylene; and combinations thereof; A is a bond, —NRW1—, —NRW1—NRW1—, —S—, —O—, —S—S—wherein is a single or double bond, W is —O—, —S—, or —NRW1—, RW1 is hydrogen, substituted or unsubstituted alkyl, or an amino protecting group; and Q is —NRW1—, —NRW1—NRW1—, —S—, —O—; and B is a label or probe.