Patent ID: 6160013
Filing Date: 2000-12-12
Classification: A61K,C07C

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 0;R.sup.2A =H, OH, acyloxy, alkoxy;R.sup.2B =H, halogen, OH, acyloxy, alkoxy, with the provisos that if R.sup.2B =halogen, then R.sup.2A =H, and that R.sup.2A and R.sup.2B cannot both be from the group consisting of: OH, acyloxy, and alkoxy;or, R.sup.2A R.sup.2B taken together=O;R.sup.3A =H, OH, acyloxy, alkoxy;R.sup.3B =H, halogen, OH, acyloxy, alkoxy, with the provisos that if R.sup.3B =halogen, then R.sup.3A =H, and that R.sup.3A and R.sup.3B cannot both be from the group consisting of: OH, acyloxy, and alkoxy;or, R.sup.3A R.sup.3B together=O;with the further provisos: that if one of R.sup.2B, R.sup.3B =halogen, then the other=H; that if one of R.sup.2A R.sup.2B taken together or R.sup.3A R.sup.3B taken together=O, then the other.noteq.O; and that R.sup.2A, R.sup.2B, R.sup.3A, R.sup.3B cannot all=H;- - -=single or non-cumulated double bond, with the proviso that when G=O, a single bond exists between carbons 4 and 5;Z.sup.1 =H or CH.sub.3 ;L=O or S;X=O, S, NH, CH.sub.2, or a direct bond;Y=O, S, NH, CH.sub.2, or a direct bond;with the provisos that Y=CH.sub.2 or a direct bond when X=O, S, or NH, and that X CH.sub.2 or a direct bond when Y=O, S, or NH;Z.sup.2 =(CH.sub.2).sub.q CH.sub.3, cycloalkyl, heteroaryl, or phenyl, the heteroaryl or phenyl being optionally substituted with alkyl, halo, trihalomethyl, alkoxy, acyl, acyloxy, amino, alkylamino, acylamino, or hydroxy;q=0-5;or, Z.sup.2 =(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, or CH.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.