公开(公告)号：US4889869A

公开(公告)日：1989-12-26

申请号：US341239

申请日：1989-04-19

申请人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

发明人： Peter Buhlmayer ,  James L. Stanton ,  Walter Fuhrer ,  Richard Goschke ,  Vittorio Rasetti ,  Heinrich Rueger

IPC分类号： C07D233/54 ,  C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12

CPC分类号： C07D233/64 ,  C07D233/84 ,  C07D401/12 ,  C07D417/12 ,  Y10S530/86

摘要： Compounds of the formula ##STR1## in which R.sub.1 represents acyl substituted by a thio, sulphinyl or sulphonyl group, A represents an optionally N-alkylated .alpha.-amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl-lower alkyl, tricycloalkyl-lower alkyl, aryl or aryl-lower alkyl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents lower alkyl, optionally etherified or esterified hydroxy-lower alkyl, cycloalkyl, cycloalkyl-lower alkyl, bicycloalkyl, bicycloalkyl-lower alkyl, tricycloalkyl, tricycloalkyl-lower alkyl, aryl, aryl-lower alkyl, optionally substituted carbamoyl, optionally substituted amino, optionally substituted hydroxy, optionally substituted mercapto, sulyhinyl or sulphonyl, and R.sub.6 represents substituted amino, and salts of such compounds having salt-forming groups, inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

摘要翻译： 式（I）的化合物，其中R 1表示被硫代，亚磺酰基或磺酰基取代的酰基，A表示任选N-烷基化的α-氨基酸残基，其N-末端与R1和C-末端键合 基团-NR 2 - ，R 2表示氢或低级烷基，R 3表示氢，低级烷基，任选醚化或酯化的羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基 - 低级烷基，三环烷基 - 低级烷基，芳基或芳基 - 低级烷基，R4代表羟基或醚化或酯化的羟基，R5代表低级烷基，任选醚化或酯化羟基 - 低级烷基，环烷基，环烷基 - 低级烷基，双环烷基，双环烷基 - 低级烷基，三环烷基，三环烷基 - 低级烷基，芳基，芳基 - 低级烷基，任选取代的氨基甲酰基，任选取代的氨基，任选取代的羟基，任选取代的巯基，磺酰基或磺酰基，R 6代表取代的氨基， 具有盐形成基团，抑制了肾素素的增压作用，可用作抗高血压药。

公开(公告)号：US4719288A

公开(公告)日：1988-01-12

申请号：US869800

申请日：1986-06-02

申请人： Walter Fuhrer ,  Peter Buhlmayer ,  Vittorio Rasetti ,  Bernhard Riniker

发明人： Walter Fuhrer ,  Peter Buhlmayer ,  Vittorio Rasetti ,  Bernhard Riniker

IPC分类号： C07K14/81 ,  A61K38/00 ,  A61K38/55 ,  A61P9/12 ,  A61P43/00 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/12 ,  C07C237/22 ,  C07C237/42 ,  C07C255/43 ,  C07C255/44 ,  C07D209/16 ,  C07D213/40 ,  C07D233/54 ,  C07D277/46 ,  C07D295/13 ,  C07F7/18 ,  C07K1/113 ,  C07K5/02 ,  C07K9/00 ,  C07K5/08 ,  C07C103/34 ,  C07C103/12 ,  C07C103/20 ,  C07C101/30 ,  C07D277/20 ,  C07D209/18 ,  C07D233/64 ,  C07D207/12 ,  C07D211/70

CPC分类号： C07D213/40 ,  C07C237/06 ,  C07C237/08 ,  C07C237/10 ,  C07C237/12 ,  C07C237/22 ,  C07C237/42 ,  C07C255/43 ,  C07C255/44 ,  C07D209/16 ,  C07D233/64 ,  C07D277/46 ,  C07D295/13 ,  C07F7/1852 ,  C07K5/0207 ,  C07K5/0227 ,  C07K9/001 ,  A61K38/00 ,  Y10S530/80 ,  Y10S530/86

摘要： Compounds of the formula ##STR1## in which R.sub.1 represents hydrogen or acyl, X.sub.1 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to R.sub.1 and C-terminally to X.sub.2, X.sub.2 represents an optionally N-alkylated amino acid residue that is bonded N-terminally to X.sub.1 and C-terminally to the group --NR.sub.2 --, R.sub.2 represents hydrogen or lower alkyl, R.sub.3 represents hydrogen, alkyl, cycloalkyl, aryl-lower alkyl or aryl, R.sub.4 represents hydroxy or etherified or esterified hydroxy, R.sub.5 represents alkyl, cycloalkyl, aryl-lower alkyl or aryl, and R.sub.6 represents free or substituted amino or substituted hydroxy, and salts of such compounds having salt-forming groups inhibit the blood pressure-increasing action of the enzyme renin and can be used as anti-hypertensives.

摘要翻译： 式（I）的化合物，其中R 1表示氢或酰基，X 1表示任选N-烷基化的氨基酸残基，其N-末端与R 1和C-末端键合于X 2，X 2表示任选N-烷基化的 氨基酸残基，其N-末端与X1和C-末端键合在基团-NR2-上，R 2表示氢或低级烷基，R 3表示氢，烷基，环烷基，芳基 - 低级烷基或芳基，R 4表示羟基或醚化或 酯化羟基，R5代表烷基，环烷基，芳基 - 低级烷基或芳基，R6表示游离或取代的氨基或取代的羟基，这些具有成盐基团的化合物的盐抑制酶肾素的增压作用， 用作抗高血压药。