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    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    1.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    公开(公告)号：US4758584A

    公开(公告)日：1988-07-19

    申请号：US011183

    申请日：1987-02-05

    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 ,  C07D401/12 ,  C07D417/12 ,  C07K5/02 ,  A61K37/64 ,  C07K5/08

    CPC分类号： C07D233/64 ,  C07D401/12 ,  C07D417/12 ,  C07K5/0227 ,  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, sulphinyl 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，亚磺酰基或磺酰基，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。

    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups
    3.
    发明授权
    Antihypertensive 5-amino-4-hydroxyvaleryl derivatives substituted by sulphur-containing groups 失效
    由含硫基取代的抗高血压5-氨基-4-羟基戊酰基衍生物

    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。

    DISUBSTITUTED UREAS AS KINASE INHIBITORS
    10.
    发明申请
    DISUBSTITUTED UREAS AS KINASE INHIBITORS 审中-公开
    作为激酶抑制剂的消除性尿路炎

    公开(公告)号：US20090131437A1

    公开(公告)日：2009-05-21

    申请号：US11813067

    申请日：2006-01-03

    申请人： Pascal Furet ,  Georg Martiny-Baron ,  Clive McCarthy ,  Vittorio Rasetti ,  Andrea Vaupel

    发明人： Pascal Furet ,  Georg Martiny-Baron ,  Clive McCarthy ,  Vittorio Rasetti ,  Andrea Vaupel

    IPC分类号： A61K31/5377 ,  C07D413/14

    CPC分类号： C07D403/12 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14

    摘要： The invention relates to compounds of the formula (I), their use as kinase inhibitors, new pharmaceutical formulations comprising said compounds, said compounds for use in the diagnostic or therapeutic treatment of warm-blooded animals, especially humans, their use in the treatment of diseases or for the manufacture of pharmaceutical formulations useful in the treatment of diseases that respond to modulation of kinase activity, methods of treatment comprising administration of said compounds to a warm-blooded animal, especially a human, and processes for the manufacture of said compounds.

    摘要翻译： 本发明涉及式（I）化合物，其作为激酶抑制剂的用途，包含所述化合物的新药物制剂，用于诊断或治疗温血动物，特别是人的所述化合物，其用于治疗 疾病或用于制造可用于治疗对激酶活性调节作出反应的疾病的药物制剂，包括将所述化合物施用于温血动物，特别是人的治疗方法，以及所述化合物的制备方法。