发明名称 N-Heterocyclic alcohol renin inhibitors.
摘要 <p>2-(N-substd. aminoalkanoylamino)-1- (N-heterocyclyl)-alkanols of formula X-(NH-CHR5-CO)p-NH-CHR4- CO-NH-CHR3-CHOH-R1 (I) and their salts are new, where X=R6-(CH2)m-, R6-(CH2)m-C-(-NH-CHR10-CO=-q, R6-(CH2)m-O-CO-, R6-O-(CH2)n-CO-, R6-(CH2)m-NH-CO-, R6-(CH2)m-SO2-, R6-(CH2)m-CH((CH2)m'-R6')-CO- or gp (a) or (b) R3-R5,R10=H, lower alkyl, halo substd. lower alkyl, -(CH2)n-aryl, -(CH2)n-heterocyclo, -(CH2)n-OH, -(CH2)n-O-lower alkyl, -(CH2)n-NH2, -(CH2)n-SH, -(CH2)n-S-lower alkyl, -(CH2)n-O-(CH2)g-OH, -(CH2)n-O-(CH2)g-NH2, -(CH2)n-S-(CH2)g-OH, -(CH2)n-COOH, -(CH2)n-S-(CH2)g-NH2, -(CH2)n-cycloalkyl, -(CH2)n-NH-Cl=NH)-NH2, -(CH2)nCONH2 or gp or (c) or (d) R6 and R'6 =lower alkyl, cycloalkyl, aryl or heterocyclo; p and q=0 or 1; m and m'=0-5; n=1-5; g=2-5; R7=-CH2OCH2Ph or -CH2Ph; R8=2,4-dinitrophenyl, -COOCH2Ph, p-toluenesulphonyl or -CH2OCH2Ph; R1=(i) fully or partially satd or unsatd monocyclic N-hetero-cyclic ring of 5 or 6 atoms contg at least one N atom or (ii) a biscyclic ring in which ring (i) is fused to a benzene ring; ring (i) can also include and O or S atom or up to three additional N-atoms.</p>
申请公布号 EP0231919(A2) 申请公布日期 1987.08.12
申请号 EP19870101373 申请日期 1987.02.02
申请人 E.R. SQUIBB & SONS, INC. 发明人 RYONO, DENIS EVAN;WELLER III, HAROLD NORRIS
分类号 C07K14/81;A61K31/40;A61K31/403;A61K31/404;A61K31/415;A61K31/4184;A61K31/42;A61K31/421;A61K31/423;A61K31/425;A61K31/426;A61K38/00;A61P9/12;A61P43/00;C07D207/333;C07D209/12;C07D231/06;C07D231/08;C07D233/64;C07D231/12;C07D233/24;C07D233/54;C07D235/08;C07D263/32;C07D263/56;C07D277/22;C07D401/06;C07D401/12;C07D403/06;C07D403/12;C07D417/12;C07K5/02;C07K5/06;C07K5/065;C07K5/078;C07K5/08 主分类号 C07K14/81
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