Patent ID: 6437160
Filing Date: 2002-08-20
Classification: A61P,C07C

Abstract:
A method for the treatment of dry eye and other disorders requiring the wetting of the eye which comprises administering to a mammal a composition comprising a pharmaceutically acceptable carrier and a pharmaceutically effective amount of one or more compounds of the following formula I:whereinR1 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; X is O, S(O)p, NR7 or CH2, with the proviso that X cannot be CH2 when n is 0; p is 0, 1 or 2; NR7 comprises a free or functionally modified amino group; Aâ€”B, Dâ€”E, Gâ€”T and Jâ€”K are the same or different and are CH2CH2, CH&boxH;CH or Câ‰¡C, with the proviso that at least one of Aâ€”B, Dâ€”E, Gâ€”T and Jâ€”K must be CH&boxH;CH or Câ‰¡C, and Y is C(O) (i.e., a carbonyl), or Y is wherein R9O constitutes a free or functionally modified hydroxy group.