Patent ID: 6331566
Filing Date: 2001-12-18
Classification: A61K,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: ##STR17##wherein:R.sup.1 is CO.sub.2 R, CONR.sup.2 R.sup.3, CH.sub.2 OR.sup.4, CH.sub.2 NR.sup.5 R.sup.6, CH.sub.2 N.sub.3, CH.sub.2 --Hal, CH.sub.2 NO.sub.2, CH.sub.2 SR.sup.20, COSR.sup.21 or 2,3,4,5-tetrazol-1-yl, wherein:R is H or CO.sub.2 R forms a pharmaceutically acceptable salt or a pharmaceutically acceptable ester;NR.sup.2 R.sup.3 and NR.sup.5 R.sup.6 are the same or different and comprise a free or functionally modified amino group;OR.sup.4 comprises a free or functionally modified hydroxy group;Hal is F, Cl, Br or I;SR.sup.20 comprises a free or functionally modified thiol group;R.sup.21 is H, or COSR.sup.21 forms a pharmaceutically acceptable salt or a pharmaceutically acceptable thioester;K is C.sub.2 -C.sub.8 alkyl, alkenyl, or alkynyl or a C.sub.3 -C.sub.8 allenyl group;A and X are the same or different and are a direct bond, CH.sub.2, NR.sup.7, O or S, with the proviso that at least one of A and X is S;B is H, or BB together comprises a double bonded O, S or NR.sup.8, with the proviso that BB comprises a double bonded O, S or NR.sup.8 when A and X are the same or different and are NR.sup.7, O or S; wherein:NR.sup.7 and NR.sup.8 are the same or different and comprise a functionally modified amino group;p is 0 or 1;D-E and G-H are the same or different and are CH.sub.2 CH.sub.2, CH.dbd.CH or C.ident.C; andY is C(O) or Y is ##STR18##wherein R.sup.9 O constitutes a free or functionally modified hydroxy group.