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4-carbamoyloxy-piperidine-1-carboxylic acid esters: inhibitors of cholesterol absorption

机译:4-氨基甲酰氧基-哌啶-1-羧酸酯:胆固醇吸收抑制剂

摘要

Compounds which inhibit the enzyme cholesterol ester hydrolase (CEH) thus inhibit the formation of esterified cholesterol. Esterified cholesterol is absorbed through the intestine and inhibition of the enzyme therefore results in inhibition of cholesterol absorption. The compounds of this invention inhibit cholesterol ester hydrolase and have the formula: IMAGE I wherein Z is -Ar1, -Ar1-Ar2, -Ar1-O-Ar2, -Ar1-S-Ar2, IMAGE IMAGE -Ar1-(CH2)1-20-Ar2, -Ar1-(CH2)1-20-O-Ar2, -Ar1-O-(CH2)1-20-Ar2, -Ar1-(CR6=CR6)1-3-Ar2 or -Ar1-NR7-Ar2; and A is a hydrocarbon linking group which may be interrupted by a heteroatom or a cycloalkyl, aryl, heterocycloalkyl, or an azacycloalkyl group; and R4 and R5 are independently alkyl, alkenyl, acyl, alkoxycarbonyl or H or R4 and R5 together with the interposed nitrogen form a saturated heterocyclic ring.
机译:抑制酶胆固醇酯水解酶(CEH)的化合物因此抑制了酯化胆固醇的形成。酯化的胆固醇通过肠吸收,因此对该酶的抑制导致胆固醇吸收的抑制。本发明的化合物抑制胆固醇酯水解酶,并具有下式: I,其中Z为-Ar1,-Ar1-Ar2,-Ar1-O-Ar2,-Ar1-S-Ar2, - Ar1-(CH2)1-20-Ar2,-Ar1-(CH2)1-20-O-Ar2,-Ar1-O-(CH2)1-20-Ar2,-Ar1-(CR6 = CR6)1-3 -Ar2或-Ar1-NR7-Ar2; A是可被杂原子或环烷基,芳基,杂环烷基或氮杂环烷基中断的烃连接基; R 4和R 5独立地为烷基,烯基,酰基,烷氧羰基或H,或R 4和R 5与插入的氮一起形成饱和杂环。

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