abstract |
A composition for the treatment of dry eye and other disorders that require wetting of the eye, comprising a pharmaceutically acceptable excipient and a pharmaceutically effective amount of one or more compounds of the following formula I: n -C5H11 -Y -A -CH2 - R1 I in which: R1 is CO2R, CONR2R3, CH2OR4, CH2NR5R6, CH2N3, CH2Hal, CH2NO2, CH2SR20, COSR21, or 2, 3, 4, 5-tetrazol 1-yl, where: R is H or an acceptable cation pharmaceutically, 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 hydroxyl group; Hal is F, Cl, Br, or I; R20 is H, alkyl, acyl; R21 is H or a pharmaceutically acceptable cation, or COSR21 forms a pharmaceutically acceptable thioester moiety; A is L1-A1-L2; A1 is CH2CH2; L1 is CH2-B-D; B and D are the same or different and are CH2CH2, CH = CH, or C = -C; L2 is CH2-K-CH2CH2; K is CH2CH2, CH = CH, or C = -C; Y is C (O) (ie, a carbonyl group) or Y is ** (Formula) ** where R 9 O constitutes a free or functionally modified hydroxyl group. |