Patent ID: 6348496
Filing Date: 2002-02-19
Classification: A61P,C07C

Abstract:
A composition 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 (CH2)nCO2R, (CH2)nCONR2R3, (CH2)nCH2OR4, (CH2)nCH2NR5R6, (CH2)nCH2N3, (CH2)nCH2Hal, (CH2)nCH2NO2, (CH2)nCH2SR20, (CH2)nCOSR21 or (CH2)n-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; 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 COSR21 forms a pharmaceutically acceptable salt or a pharmaceutically acceptable thioester; n is 0 or 2; A, B, C and D is C1-C5 alkyl, alkenyl, or alkynyl or a C3-C5 allenyl group; Y is â€ƒwherein R8 is H or CH3, and X is CH2, CH(CH3) or C(CH3)2; or Y is CH2, CH(CH3) or C(CH3)2, and X is â€ƒwherein R8 is H or CH3, with the proviso that Y cannot be CH2 when X is R7O comprises a free or functionally modified hydroxy group.