Patent ID: 6750250
Filing Date: 2004-06-15
Classification: A61K,C07D

Abstract:
A compostion for the treatment of dry eye and other disorders requiring the wetting of the eye comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of one or more compounds of the following formula I: wherein:R1 is CO2R, CONR2R3, CH2OR4, CH2NR5R6, CH2N3, CH2Hal, CH2NO2, CH2SR20, COSR21, or 2,3,4,5-tetrazol-1-yl, wherein: R is H or CO2R forms a pharmaceutically acceptable salt or a pharmaceutically acceptable ester; NR2R3 and NR5R6 are the same or different and comprise a free or functionally modified amino group, with the proviso that at most only one of R2 and R3 is OH or alkoxy and at most only one of R5 and R6 is OH or alkoxy; OR4 comprises a free or functionally modified hydroxy group; Hal is F, Cl, Br, or I; SR20 comprises a free or functionally modified thiol group; and R21 is H or COSR21 forms a pharmaceutically aceptable salt or a pharmaceutcally acceptable thioester; A, B and D are the same or different and are C1-C5 alkyl, C2-C5 alkenyl, C2-C5 alkynyl, or a C3-C5 allenyl group; C is an oxiran; X is (CH2)m or (CH2)mO, wherein m is 1-6; and Y is a phenyl ring optionally substituted with alkyl, halo, trihalomethyl, acyl, or a free or functionally modified hydroxy, amino, or thiol group; or X-Y is (CH2)pY1; wherein p is 0-6; and â€ƒwherein: W is CH2,O, S(O)q, NR8, CH2CHz, CH&boxH;CH, CH2O, CH2S(O)q, CH&boxH;N, or CH2NR8; wherein q is 0-2, and R8 is H, alkyl, or acyl; Z is H, alkyl, acyl, halo, trihalomethyl, or a free or functionally modified amino, thiol, or hydroxy group; and  is a single or double bond; or X-Y is cyclohexyl or n-C8H11.