INHIBITORS OF PEPTIDYL ARGININE DEIMINASE (PAD) ENZYMES AND USES THEREOF

摘要

The present application relates to imidazolidinecliones, compositions comprising these compounds and their use, in particular for the treatment of diseases, disorders or conditions characterized by or associated with the hypercitrullination of proteins by peptidyl arginine deiminase (PAD) enzymes. In particular, the present application includes compounds of Formula I, and compositions and uses thereof: (I).;

主权项

1. A compound of Formula I: wherein R1 and R2 are independently selected from C1-6alkyl and C1-4alkyleneR4; wherein R4 is selected from COOR5, Ph, C3-6cycloalkyl and NHR6; wherein R5 is selected from H and C1-6alkyl, and R6 is selected from H, Ac and Bz; R3 is selected from:in which any one of the available hydrogen atoms on R3 is optionally substituted with C1-4alkyl or cyano; and
m, n, p, and q are, independently, 1, 2 or 3; except when R1 and R2 are C1-2alkyl and R3 is piperazinyl, then n does not equal 1 or 2 and when R3 is pyrrolidinyl, n does not equal 1; or a pharmaceutically acceptable salt or solvate thereof.