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Candida acid protease inhibiting compounds

机译:念珠菌酸性蛋白酶抑制化合物

摘要

Compounds which inhibit Candida acid protease are disclosed which have the formula: ##STR1## wherein R.sub.1 is loweralkyl, loweralkenyl, cycloalkyl, cycloalkenyl, cycloalkylalkyl, cycloalkenylalkyl, arylalkyl or (heterocyclic)alkyl;PPR. sub.2 is loweralkyl, cycloalkylalkyl or arylalkyl;PPR.sub. 3 is --OH or --NH. sub.2 ;PPR.sub.4 isPP (a) --CH(OH)--R.sub. 5 wherein R.sub.5 is loweralkyl, cycloalkyl or cycloalkylalkyl orP P(b) --CH.sub.2 CH(R.sub.6)C(O)NHR. sub.7 wherein R.sub.6 is loweralkyl and R.sub.7 is loweralkyl, aminoalkyl, alkylaminoalkyl, dialkylaminoalkyl, hydroxyalkyl, alkoxyalkyl, thioalkoxyalkyl, carboxyalkyl, alkoxycarbonylalkyl, cyanoalkyl or (heterocyclic)alkyl; andPPA is ##STR2## wherein R.sub.8 is arylalkyl, B is -- C(O) or --S(O).sub.2 -- and R.sub.9 is aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl; or ##STR3## wherein R.sub. 10 is arylalkyl and R.sub. 11 is (a) --C(O)R.sub.12 wherein R.sub.12 is alkoxy, arylalkoxy, aryl, arylalkyl, heterocyclic or (heterocyclic)alkyl or (b) --S(O).sub.2 --R. sub.13 wherein R.sub.13 is aryl, arylalkyl, heterocyclic or (heterocyclic) alkyl; or a pharmaceutically acceptable salt, ester or prodrug thereof.
机译:公开了抑制念珠菌酸蛋白酶的化合物,其具有下式:其中R 1是低级烷基,低级烯基,环烷基,环烯基,环烷基烷基,环烯基烷基,芳基烷基或(杂环)烷基;

R. sub.2是低级烷基,环烷基烷基或芳基烷基; 3是-OH或-NH。 sub.2;

R.sub.4是

(a)--CH(OH)-R.sub。 5,其中R 5是低级烷基,环烷基或环烷基烷基或P

(b)-CH 2 CH(R 6)C(O)NHR。 sub.7,其中R.6是低级烷基,R.sub.7是低级烷基,氨基烷基,烷基氨基烷基,二烷基氨基烷基,羟烷基,烷氧基烷基,硫代烷氧基烷基,羧基烷基,烷氧基羰基烷基,氰基烷基或(杂环)烷基;和

A是## STR2 ##,其中R.sub.8是芳基烷基,B是-C(O)或-S(O).2-和R.sub.9是芳基,芳基烷基,杂环或(杂环)烷基;或## STR3 ##,其中R.sub。 10是芳基烷基和R。 11是(a)-C(O)R.sub.12,其中R.sub.12是烷氧基,芳基烷氧基,芳基,芳基烷基,杂环或(杂环)烷基或(b)-S(O)sub。 2 --R sub.13,其中R.sub.13是芳基,芳基烷基,杂环或(杂环)烷基;或其药学上可接受的盐,酯或前药。

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