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    Angiotensin-II analogues with antagonizing effects, containing an .alpha.-hydroxycarboxylic acid residue in position 8, and a process for the preparation thereof
    3.
    发明授权
    Angiotensin-II analogues with antagonizing effects, containing an .alpha.-hydroxycarboxylic acid residue in position 8, and a process for the preparation thereof 失效
    在8位含有α-羟基羧酸残基的具有拮抗作用的血管紧张素-II类似物及其制备方法

    公开(公告)号：US4330532A

    公开(公告)日：1982-05-18

    申请号：US222765

    申请日：1981-01-06

    申请人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    发明人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07K7/06 ,  A61K38/08 ,  A61K38/55 ,  A61P43/00 ,  C07K7/14 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/14 ,  Y02P20/55

    摘要： New angiotensin-II analogues of the general formula (I),X-Arg-Val-Tyr-Ile-His-Pro-Y-OA (I)whereinX stands for the acyl group of an N-methylamino acid, or the acyl group of an aliphatic .alpha.-aminooxy- or .alpha.-hydroxycarboxylic acid,Y is the residue of an aliphatic .alpha.-hydroxycarboxylic acid, andA is hydrogen or a C.sub.1-5 alkyl group,are prepared by removing the protecting groups of a protected octapeptide derivative of the general formula (II) or (III),B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OF (II)B-X-Arg(C)-Val-Tyr(D)-Ile-His(E)-Pro-Y-OA (III)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andF is a group for the protection of the terminal carboxy group, resistant to the effect of mild acids but removable by catalytic hydrogenolysis or upon treatment with a stronger acid.The new compounds of the invention can be applied to diagnose and differentiate hypertensions of various origin, and in the therapy to suppress hypertensions of renal origin, in the treatment of hypertensive crises, secondary cardiac insufficiency, etc.

    摘要翻译： 通式（I）的新型血管紧张素-II类似物，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X表示N-甲基氨基酸的酰基，或酰基 脂肪族α-氨基氧基或α-羟基羧酸的基团，Y是脂肪族α-羟基羧酸的残基，A是氢或C 1-5烷基，是通过除去保护的八肽衍生物的保护基来制备的 的通式（II）或（III）的BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OF（II）BX-Arg（C）-Val- Tyr（D）-Ile-His（E）-Pro-Y-OA（III）其中B是通过酸解或催化氢化除去的基团，C是用于临时保护Arg部分上胍基的基团，D 是用于临时保护Tyr部分上的芳族羟基的基团，E是His部分上咪唑基的临时保护基团，F是保护末端羧基的基团，耐受 温和酸的作用b 通过催化氢解或用较强酸处理可以除去。 本发明的新化合物可用于诊断和鉴别各种起因的高血压，以及用于抑制肾源性高血压，治疗高血压危象，继发性心脏功能不全等的治疗。

    Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof
    4.
    发明授权
    Angiotensin-II analogues with antagonizing effects, containing an ester group in position 8, and a process for the preparation thereof 失效
    具有拮抗作用的血管紧张素-II类似物，其含有8位的酯基及其制备方法

    公开(公告)号：US4388304A

    公开(公告)日：1983-06-14

    申请号：US225048

    申请日：1981-01-14

    申请人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    发明人： Olga Nyeki ,  Lajos Kisfaludy ,  Egon Karpati ,  Laszlo Szporny

    IPC分类号： C07K7/06 ,  A61K38/00 ,  A61K38/08 ,  A61K38/55 ,  A61P9/12 ,  C07K7/14 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K7/14 ,  A61K38/00 ,  Y02P20/55 ,  Y10S530/80

    摘要： New octapeptides of the general formula (I),X--Arg--Val--Tyr--Ile--His--Pro--Y--OA (I)whereinX stands for the acyl group of an N-methylamino acid or the acyl group of an aliphatic .alpha.-hydroxy- or .alpha.-aminooxycarboxylic acid,Y is the residue of an aliphatic amino acid, andA is a C.sub.1-5 alkyl group, are prepared so that the protecting groups of a protected octapeptide derivative of the general formula (II),B--X--Arg(C)--Val--Tyr(D)--Ile--His(E)--Pro--Y--OA (II)whereinB is a group removable by acidolysis or catalytic hydrogenation,C is a group for the temporary protection of the guanidino group on the Arg moiety,D is a group for the temporary protection of the aromatic hydroxy group on the Tyr moiety,E is a group for the temporary protection of the imidazole group on the His moiety, andA, X and Y are as defined above,are removed either stepwise or in a single step. If desired, a compound of the general formula (I) is converted into its acid addition salt or pharmaceutically acceptable complex.The new compounds according to the invention possess angiotensin-II antagonizing effects, and can be used in the therapy to diagnose or treat hypertensive states.

    摘要翻译： 通式（I）的新八肽，X-Arg-Val-Tyr-Ile-His-Pro-Y-OA（I）其中X代表N-甲基氨基酸的酰基或脂族 α-羟基或α-氨基氧基羧酸，Y是脂族氨基酸的残基，A是C 1-5烷基，使得通式（II）的保护的八肽衍生物的保护基， BX-Arg（C）-Val-Tyr（D）-Ile-His（E）-Pro-Y-OA（II）其中B是通过酸解或催化氢化除去的基团，C是临时保护的基团 Arg部分的胍基，D为Tyr部分上芳香族羟基的临时保护基，E为His部分上咪唑基的临时保护基团，A，X和Y为 如上所定义的，可以逐步地或单步地去除。 如果需要，将通式（I）的化合物转化为其酸加成盐或药学上可接受的络合物。 根据本发明的新化合物具有血管紧张素-II拮抗作用，可用于诊断或治疗高血压状态的治疗。