Patent ID: 6353012
Filing Date: 2002-03-05
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 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; 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; E-D is CH2CH2CH2 or cis-CH2CH&boxH;CH; or E is trans-CH&boxH;CH and D is CH(OH) in either configuration, wherein the OH is free or functionally modified; or E is CH2CH2 and D is a direct bond; p is 1 or 3 when E-D is CH2CH2CH2 or cis-CH2CH&boxH;CH, or when E is trans-CH&boxH;CH and D is CH(OH) in either configuration, wherein the OH is free or functionally modified; or p is 0 when E is CH2CH2 and D is a direct bond; G-T is CH2CH2, CH(SR7)CH2 or trans-CH&boxH;CH; R7 is H, alkyl, aryl, aralkyl, cycloalkyl or acyl; Y is CH(OH) in either configuration, in which the OH is free of functionally modified, or C&boxH;O; n is 0, 2, or 4; and Z is CH3, CO2R, CONR2R3 or CH2OR4; with the proviso that compounds comprising all of the following substituents are excluded: R1 is CO2R or CONHR2; E-D is cis-CH2CH&boxH;CH; p is 3; G-T is trans-CH&boxH;CH; Y is CH(OH) in either configuration, wherein the OH group is free or is acylated to form OC(O)R, wherein R is H, substituted or unsubstituted alkyl, cycloalkyl, (cycloalkyl)alkyl, aryl, or arylalkyl, wherein the substitutent is made with a moiety selected from the group consisting of: alkyl, halogen, and free or functionally modified hydroxy; and Z is CH3.