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67 条记录 (耗时 0.036 秒)

    Aminoalkyl and acylaminoalkyl ethers, process for their preparation, and their use as bradykinin receptor antagonists
    5.
    发明授权
    Aminoalkyl and acylaminoalkyl ethers, process for their preparation, and their use as bradykinin receptor antagonists 失效
    氨基烷基和酰氨基烷基醚，其制备方法及其作为缓激肽受体拮抗剂的用途

    公开(公告)号：US6140341A

    公开(公告)日：2000-10-31

    申请号：US820321

    申请日：1997-03-12

    申请人： Holger Heitsch ,  Adalbert Wagner ,  Klaus Wirth ,  Bernward Scholkens ,  Gerhard Nolken

    发明人： Holger Heitsch ,  Adalbert Wagner ,  Klaus Wirth ,  Bernward Scholkens ,  Gerhard Nolken

    IPC分类号： C07D215/48 ,  A61K31/47 ,  A61P43/00 ,  C07D215/26 ,  C07D215/00 ,  C07D215/02

    CPC分类号： C07D215/26

    摘要： Aminoalkyl and acylaminoalkyl ethers which are distinguished by high affinity for the bradykinin B.sub.2 receptor and improved solubility in water are described. These aminoalkyl and acylaminoalkyl ethers can be represented by the formula (I) ##STR1## in which R.sup.1,R.sup.2,R.sup.3 are alkyl, aryl, alkylaryl, halogen, hydrogen, cycloalkyl, CHO, CO--O-alkyl, COOH; R.sup.4, R.sup.5 are hydrogen, halogen, alkoxy, nitro, cyano, S-alkyl; n is a number from 1 to 8; R.sup.6 is hydrogen, alkyl, alkylalkenyl, alkylaryl; R.sup.7 is hydrogen and a substituted or unsubstituted acyl radical. A process for preparing the compounds of the formula (I) is likewise described.

    摘要翻译： 描述了通过对缓激肽B2受体的高亲和力和改善的在水中的溶解度的区别的氨基烷基和酰基氨基烷基醚。 这些氨基烷基和酰基氨基烷基醚可以由其中R 1，R 2，R 3是烷基，芳基，烷基芳基，卤素，氢，环烷基，CHO，CO-O-烷基，COOH的式（I） R4，R5是氢，卤素，烷氧基，硝基，氰基，S-烷基; n是从1到8的数字; R6是氢，烷基，烷基烯基，烷基芳基; R7是氢和取代或未取代的酰基。 同样描述了制备式（I）化合物的方法。

    Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process for their preparation, and their use
    6.
    发明授权
    Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process for their preparation, and their use 失效
    氟烷基和氟烷氧基取代的杂环缓激肽拮抗剂，其制备方法及其应用

    公开(公告)号：US5859025A

    公开(公告)日：1999-01-12

    申请号：US819351

    申请日：1997-03-18

    申请人： Adalbert Wagner ,  Holger Heitsch ,  Gerhard Nolken ,  Klaus Wirth ,  Bernward Scholkens

    发明人： Adalbert Wagner ,  Holger Heitsch ,  Gerhard Nolken ,  Klaus Wirth ,  Bernward Scholkens

    IPC分类号： C07D237/28 ,  A61K31/345 ,  A61K31/47 ,  A61K31/495 ,  A61K31/53 ,  A61P43/00 ,  C07D215/04 ,  C07D215/26 ,  C07D239/72 ,  C07D239/74 ,  C07D241/36 ,  C07D241/44 ,  C07D253/04 ,  C07D253/065 ,  C07D257/10 ,  C07D215/14 ,  C07D215/20 ,  C07D215/38

    CPC分类号： C07D215/26

    摘要： Fluoroalkyl- and fluoroalkoxy-substituted heterocyclic bradykinin antagonists, process or their preparation, and their useHeterocyclic fluoroalkyl derivatives and fluoroalkoxy derivatives of the formula (I) having bradykinin-antagonistic action ##STR1## in which X.sub.1 -X.sub.3 are N or CR.sup.5, R.sup.1 and R.sup.2 are H or halogen, R.sup.3 and R.sup.4 are H, halogen, alkyl or alkenyl, R.sup.5 is H, halogen, (substituted) alkyl, O--R.sup.6, S--R.sup.6, NHR.sup.6, (substituted) aryl, (substituted)aryl-alkyl, --C(O)--OR.sup.6 or --C(O)--H, R.sup.6 and R.sup.8 H, alkyl, alkenyl or aryl-alkyl, R.sup.7 is (substituted) alkyl or (substituted) alkoxy, B is an aminocarboxylic acid, D is alkenediyl, alkanediyl or --(CH.sub.2).sub.n --Y.sub.p --(CH.sub.2).sub.m --, E is oxygen or sulfur, Y is oxygen, sulfur or NR.sup.8, n and m are a number 0-3, o is a number 1-3 and p is 0 or 1, and their physiologically tolerable salts and a process for their preparation are described.

    摘要翻译： 氟烷基和氟烷氧基取代的杂环缓激肽拮抗剂，方法或其制备及其用途具有缓激肽拮抗作用的式（I）的杂环氟烷基衍生物和氟代烷氧基衍生物，其中X1-X3为N或CR5 R 1和R 2为H或卤素，R 3和R 4为H，卤素，烷基或烯基，R 5为H，卤素，（取代的）烷基，O-R 6，S-R 6，NHR 6，（取代的） 芳基 - 烷基，-C（O）-OR 6或-C（O）-H，R 6和R 8 H，烷基，烯基或芳基 - 烷基，R 7是（取代的）烷基或（取代的）烷氧基，B是氨基羧酸 ，D为亚烯基，烷二基或 - （CH2）n-Yp-（CH2）m-，E为氧或硫，Y为氧，硫或NR8，n和m为0-3，o为1 -3和p为0或1，并且描述了它们的生理上可耐受的盐及其制备方法。