Patent ID: 8552067
Filing Date: 2013-10-08
Classification: A61K,A61P,Y02A

Abstract:
1. A bioactive agent having the formula I(b)[(A2)−(J) n′ )] n −M, wherein A2 is a compound that inhibits activity of the cystic fibrosis transmembrane conductance regulator protein (CFTR); J is a spacer; and M is a macromolecular moiety capable of interacting with a cell that expresses CFTR, or a pharmaceutically acceptable salt or stereoisomer thereof, such that the bioactive agent has the formula I(b): [(A2)−(J) n′ )] n −M as follows: wherein R R R R R each of R R wherein J is a spacer that comprises a first end and a second end, wherein the spacer is attached to the compound of formula A2 at the first end of the spacer through a first linker functional group and wherein the spacer is attached to the macromolecular moiety M at the second end of the spacer through a second linker functional group, and wherein the first end of the spacer is attached to compound A2 at one or more of R n=1 to 500 and n′=0 or 1, and wherein when n′=0, M forms a direct bond with at least one of R