Patent ID: 6211226
Filing Date: 2001-04-03
Classification: A61K,C07D

Abstract:
A method of treating glaucoma or ocular hypertension in a patient, which comprises administering to the patient a pharmaceutically effective amount of a compound of formula I: ##STR13##wherein:R.sup.1 =CO.sub.2 R, CONR.sup.4 R.sup.5, CH.sub.2 OR.sup.6, or CH.sub.2 NR.sup.7 R.sup.8 ; where:R=H or cationic salt moiety, or CO.sub.2 R forms a pharmaceutically acceptable ester moiety;R.sup.4, R.sup.5 =same or different=H or alkyl;R.sup.6 =H, acyl, or alkyl;R.sup.7, R.sup.8 =same or different=H, acyl, or alkyl; with the proviso that if one ofR.sup.7, R.sup.8 =acyl, then the other=H or alkyl;n=0 or 2;G=CH.sub.2 or O;R.sup.2 =H, OH, acyloxy, or alkoxy;- - -=single or non-cumulated double bond, with the provisos that when G=O, a single bond exists between carbons 4 and 5, and that if a double bond is present between carbons 13 and 14 that it be of the trans configuration;R.sup.3 =H, R.sup.11, COR.sup.11, or CO.sub.2 R.sup.11, where R.sup.11 =alkyl;one of A, B=H, the other=F, OH, acyloxy, or alkoxy;or A-B=O(CH.sub.2).sub.2 O or O as a carbonyl;X=(CH.sub.2).sub.q or (CH.sub.2).sub.q O; where q=1-6; andY=a phenyl ring optionally substituted with alkyl, halo, trihalomethyl, alkoxy, acyl acyloxy, amino, alkylamino, acylamino, or hydroxy; orX-Y=(CH.sub.2).sub.p Y.sup.1 ; where p=0-6; and ##STR14##wherein:W=CH.sub.2, O, S(O).sub.m, NR.sup.9, CH.sub.2 CH.sub.2, CH.dbd.CH, CH.sub.2 O, CH.sub.2 S(O).sub.m, CH.dbd.N, orCH.sub.2 NR.sup.9 ; where m=0-2, and R.sup.9 =H, alkyl, or acyl;Z=H, alkyl, alkoxy, acyl, acyloxy, halo, trihalomethyl, amino, alkylamino, acylamino, or hydroxy; and- - -=single or double bond.