SUBSTITUTED 3-HALOALLYLAMINE INHIBITORS OF ASSAO AND USES THEREOF

摘要

The preparation and pharmaceutical use of substituted 3-haloallylamine derivatives as SSAO/VAP-1 inhibitors having the structure of Formula I:;;is described. Methods of using compounds of Formula I, or pharmaceutically acceptable salt or derivatives thereof, for the treatment of a variety of indications, e.g., inflammatory diseases, ocular diseases, fibrotic diseases, diabetes-induced diseases and cancer, are also described.

主权项

1. A compound of formula I:or a stereoisomer, pharmaceutically acceptable salt, polymorphic form, solvate or prodrug thereof; wherein:
R1 and R4 are each independently hydrogen or optionally substituted C1-6 alkyl; R2 and R3 are each independently selected from the group consisting of hydrogen, chlorine and fluorine; providing that R2 and R3 are not both hydrogen; R5 is an optionally substituted arylene group; R6 iswhere R7 and R8 are each independently selected from the group consisting of hydrogen, optionally substituted C1-6 alkyl and optionally substituted C3-7 cycloalkyl; and
X is CH2, oxygen, sulfur or SO2.