Patent ID: 6462061
Filing Date: 2002-10-08
Classification: A61P,C07C,Y10S

Abstract:
A composition for the treatment of dry eye and other disorders requiring the wetting of the eye in mammals 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, where: R is H or a pharmaceutically acceptable cation, or CO2R forms a pharmaceutically acceptable ester moiety; NR2R3, NR5R6 are the same or different and comprise a free or functionally modified amino group; 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; R21 is H or a pharmaceutically acceptable cation, or COSR21 forms a pharmaceutically acceptable thioester moiety; A, B, C, D are the same or different and are C1-C5 alkyl, C2-C5 alkenyl, C1-5 cyclopropyl, C2-C5 alkynyl, or a C3-C5 allenyl group; E is where OR7 comprises a free or functionally modified hydroxy group;X=(CH2)m or (CH2)mO, where m=1-6; and Y=a phenyl ring optionally substituted with alkyl, halo, trihalomethyl, acyl, or a free or functionally modified hydroxy, amino, or thiol group; or Xâˆ’Y=(CH2)pY1; where p=0-6; and wherein:W=CH2, O, S(O)q, NR8, CH2CH2, CH&boxH;CH, CH2O, CH2S(O)q, CH&boxH;N, or CH2NR8; where q=0-2, and R8=H, alkyl, or acyl; Z=H, alkyl, acyl, halo, trihalomethyl, or a free or functionally modified amino, thiol, or hydroxy group; and - - - =single or double bond; orXâˆ’Y=cyclohexyl.