申请人:Abbott Laboratories
公开号:US04927807A1
公开(公告)日:1990-05-22
A method and a composition for treating or reducing and/or controlling intraocular pressure comprising administering an effective amount of a renin inhibiting compound of the formula: ##STR1## wherein A is a substituent; W is CO or CHOH and U is CH.sub.2 or NR.sub.2 wherein R.sub.2 is hydrogen or loweralkyl; with the proviso that when W is CHOH then U is CH.sub.2 ; R.sub.1 is loweralkyl, cycloalkyl, benzyl, (alpha, alpha)-dimethylbenzyl, 4-hydroxybenzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, phenethyl, 1-benzyloxyethyl, phenoxy, thiophenoxy or anilino; R.sub.3 is loweralkyl, loweralkenyl, ((alkoxy)alkoxy)alkyl, carboxyalkyl, (thioalkoxy)alkyl, benzyl or heterocyclic ring substituted methyl; and R.sub.4 is a substituted amino group; or pharmaceutically acceptable salts or esters thereof. Also disclosed are compositions, methods and kits for treating glaucoma or reducing and/or controlling intraocular pressure wherein the renin inhibiting compound is administered in combination with a beta-adrenergic antagonist, a steroidal antiinflammatory agent or an angiotensin converting enzyme inhibiting compound.
一种用于治疗或减少和/或控制眼内压的方法和组合物,包括给予有效量的一种肾素抑制化合物,该化合物的化学式为:##STR1## 其中A是取代基;W是CO或CHOH,U是CH.sub.2或NR.sub.2,其中R.sub.2是氢或低碳基;但当W是CHOH时,U是CH.sub.2;R.sub.1是低碳基,环烷基,苯甲基,(α,α)-二甲基苯甲基,4-羟基苯甲基,4-甲氧基苯甲基,卤代苯甲基,(1-萘基)甲基,(2-萘基)甲基,(4-咪唑基)甲基,苯乙基,1-苄氧基乙基,苯氧基,噻吩氧基或苯胺基;R.sub.3是低碳基,低烯基,((烷氧基)烷氧基)烷基,羧基烷基,(硫代烷氧基)烷基,苯甲基或杂环环取代甲基;而R.sub.4是取代氨基基团;或其药学上可接受的盐或酯。还公开了用于治疗青光眼或减少和/或控制眼内压的组合物、方法和试剂盒,其中肾素抑制化合物与β-肾上腺素受体拮抗剂、类固醇抗炎药或血管紧张素转换酶抑制剂联合给药。