发明公开
- 专利标题: Peptidylaminodiols
-
申请号: EP87100424.8申请日: 1987-01-15
-
公开(公告)号: EP0229667A2公开(公告)日: 1987-07-22
- 发明人: Luly, Jay Richard , Kempf, Dale John , Plattner, Jacob John
- 申请人: ABBOTT LABORATORIES
- 申请人地址: One Abbott Park Road Abbott Park, Illinois 60064-3500 US
- 专利权人: ABBOTT LABORATORIES
- 当前专利权人: ABBOTT LABORATORIES
- 当前专利权人地址: One Abbott Park Road Abbott Park, Illinois 60064-3500 US
- 代理机构: Modiano, Guido, Dr.-Ing.
- 优先权: US818734 19860116; US895009 19860807; US943567 19861231
- 主分类号: C07K5/06
- IPC分类号: C07K5/06 ; C07K5/08 ; C07K5/02 ; C07D233/64 ; C07C237/12 ; A61K31/415 ; A61K37/02 ; A61K37/64 ; A61K31/16
摘要:
A renin inhibiting compound of the formula:
wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
wherein A is a substituent; W is C=O or CHOH; U is CH₂ or NR₂, provided that when W is CHOH then U is CH₂; R₁ is loweralkyl, cycloalkylmethyl, benzyl, 4-methoxybenzyl, halobenzyl, (1-naphthyl)methyl, (2-naphthyl)methyl, (4-imidazoyl)methyl, α, α -dimethylbenzyl, 1-benzyloxyethyl, phenethyl, phenoxy, thiophenoxy or anilino; R₂ is hydrogen or loweralkyl; R₃ is loweralkyl, [(alkoxy)alkoxy]alkyl, (thioalkoxy)alkyl, lowerakenyl, benzyl or heterocyclic ring substituted methyl; R₄ is loweralkyl, cycloalkylmethyl or benzyl; R₅ is vinyl, formyl, hydroxymethyl or hydrogen; R₇ is hydrogen or loweralkyl; R₈ and R₉ are independently selected from OH and NH₂; and R₆ is hydrogen, loweralkyl, vinyl or arylalkyl; provided that when R₅ and R₇ are both hydrogen and R₈ and R₉ are OH, the carbon bearing R₅ is of the "R" configuration and the carbon bearing R₆ is of the "S" configuration; or pharmaceutically acceptable salts or esters thereof. Also disclosed are renin inhibiting compositions, a method of treating hypertension, methods of making the renin inhibiting compounds and intermediates useful in making the renin inhibiting compounds.
公开/授权文献
- EP0229667B1 Peptidylaminodiols 公开/授权日:1994-07-13
信息查询