发明名称 Aminoalkylaminocarbonyl aminodiol amino acid derivatives as anti-hypertensive agents
摘要 Non-peptidyl compounds characterized generally as aminoalkylaminocarbonyl aminodiol derivatives of amino acids are useful as renin inhibitors for the treatment of hypertension. Compounds of particular interest are of the formula <IMAGE> wherein X is selected from oxygen atom and methylene; wherein each of R1 and R9 is independently selected from hydrido, methyl, ethyl, t-butyloxycarbonyl; and methoxymethylcarbonyl; wherein R2 is selected from hydrido, methyl, ethyl and isopropyl; wherein R3 is selected from benzyl, phenethyl, pyridylmethyl and 2-pyridylethyl; wherein each of R4 and R6 is independently selected from hydrido and methyl; wherein R7 is cyclohexylmethyl; wherein R8 is isobutyl; wherein each of R11 and R12 is hydrido; wherein m is zero or one and n is a number selected from zero through five; or a pharmaceutically-acceptable salt thereof; with the proviso that where m is zero, then R5 is selected from imidazolemethyl, thiazolemethyl and isobutyl; and with the further proviso that when m is one, then R5 is methyl or ethyl.
申请公布号 US5229369(A) 申请公布日期 1993.07.20
申请号 US19910746459 申请日期 1991.08.16
申请人 G. D. SEARLE & CO. 发明人 HANSON, GUNNAR J.;BARAN, JOHN S.
分类号 C07C237/22;C07C271/20;C07D233/26 主分类号 C07C237/22
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