Patent ID: 6025392
Filing Date: 2000-02-15
Classification: A61K,A61P,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 (II): ##STR10## wherein: R=ophthalmically acceptable ester moiety, CO.sub.2 R.sup.1, CONR.sup.7 R.sup.8, CH.sub.2 OR.sup.9, or CH.sub.2 NR.sup.10 R.sup.11 where R.sup.1 =H or cationic salt moiety; R.sup.7 and R.sup.8 are the same or different=H or alkyl; R.sup.9 =H, acyl, or alkyl; R.sup.10 and R.sup.11 are the same or different=H, acyl, or alkyl; with the proviso that if one of R.sup.10 and R.sup.11 =acyl, then the other=H or alkyl;n=0, 2; ##STR11## wherein: Y=cis CH.sub.2 CH.dbd.CH, cis CH.dbd.CHCH.sub.2, or CH.sub.2 CH.sub.2 CH.sub.2 ;Z=C.tbd.C trans CH.dbd.CH, or CH.sub.2 CH.sub.2 ;R.sup.25 =H, acyl, or alkyl;one of R.sup.2 and R.sup.3 =H, and the other=F or OH, where the OH may be free or functionally modified; or R.sup.2 and R.sup.3 taken together=OCH.sub.2 CH.sub.2 O or double bonded O (carbonyl); andR.sup.4 =(CH.sub.2).sub.m Xphenyl or (CH.sub.2).sub.p Z.sup.2, where X=O or CH.sub.2 ; m=1-6; p=0-6; ##STR12## wherein: W=O, CH.sub.2, CH.sub.2 CH.sub.2, or CH.dbd.CH; andwherein the phenyl component of (CH.sub.2).sub.m Xphenyl and the six-membered ring component of Z.sup.2 independently may be unsubstituted or substituted with halogen, CH.sub.3, CF.sub.3, CN, OCH.sub.3, or acetyl;with the proviso that when R.sup.25 =H, then R.sup.4 =(CH.sub.2).sub.p Z.sup.2 and the six-membered ring component of Z.sup.2 is unsubstituted.