COMPOUNDS WITH TRPV4 ACTIVITY, COMPOSITIONS AND ASSOCIATED METHODS THEREOF

摘要

Compounds, compositions and methods useful for treating ocular diseases are provided. In particular, antagonists of TRPV4, their synthesis, pharmaceutical compositions thereof and methods of treating ocular diseases such as glaucoma, are disclosed.

主权项

1. A compound of Formula I: wherein L is C(═O)NR10, SO2NR10, a C1-C6 alkylene, or a bond;
Y is N or CR10;Z is O, NR10, S, SO2 or C(R10)2;n is 0, 1, 2, 3, 4, 5, or 6;R1, R2, R3, R4, and R5 are independently selected from at least one of hydro, alkyl, haloalkyl, hydroxy, alkoxy, haloalkoxy, cyano, carboxyl, carboxyalkyl or amido;R6 and R7 are independently selected from at least one of hydro, alkyl, haloalkyl, heterocyclic or aryl, or R6 and R7 are connected to via a cyclic ring system;R8 is hydro, alkyl, haloalkyl, heterocyclic or aryl; andR10 is hydro, alkyl, haloalkyl, carboxyalkyl, carboxyl, alkyl methylene carbonate, methylene carbamyl, thiophenyl or —S-carboxyalkyl; or pharmaceutically acceptable salts thereof.