申请人:American Home Products Corporation
公开号:US05112859A1
公开(公告)日:1992-05-12
The compounds of the formula: ##STR1## in which R.sup.1 is hydrogen or alkyl; R.sup.2 is alkyl, cycloalkyl, cycloalkylalkyl, phenylalkyl or alkylphenylalkyl; or R.sup.1 and R.sup.2 taken together complete a heterocyclic moiety of the formula: ##STR2## in which X is ##STR3## NR.sup.5,--O-- or --S--; where R.sup.3, R.sup.4 and R.sup.5 are, independently hydrogen, alkyl, phenyl or substituted phenyl, in which the substituents are halogeno, alkoxy or trifluoromethyl; R.sup.6 is hydrogen, alkyl of gemdialkyl and n is one of the integers 0, 1 or 2, are cholesterol ester hydrolase inhibitors useful in the treatment of high serum cholesterol levels and associated disease states in the mammal such as coronary heart disease, atherosclerosis, familial hypercholesterolemia, hyperlipemia, and the like.
该公式的化合物:##STR1##其中R.sup.1是氢或烷基;R.sup.2是烷基,环烷基,环烷基烷基,苯基烷基或烷基苯基烷基;或者R.sup.1和R.sup.2一起形成一个异环的基团,其公式为:##STR2##其中X是##STR3##NR.sup.5,-O-或-S-;其中R.sup.3,R.sup.4和R.sup.5独立地是氢,烷基,苯基或取代苯基,其中取代基是卤素,烷氧基或三氟甲基;R.sup.6是氢,gem-二烷基或n为0,1或2之一的整数,是胆固醇酯酶抑制剂,对治疗高血清胆固醇水平和与哺乳动物相关的疾病状态(如冠心病,动脉粥样硬化,家族性高胆固醇血症,高脂血症等)有用。