Peptides having somatostatin activity
    51.
    发明授权
    Peptides having somatostatin activity 失效
    具有生长抑素活性的肽

    公开(公告)号:US4190648A

    公开(公告)日:1980-02-26

    申请号:US20148

    申请日:1979-03-13

    Inventor: Daniel F. Veber

    CPC classification number: C07K14/6555 A61K38/00 Y10S514/806 Y10S930/16

    Abstract: Peptides having the structural formula: ##STR1## wherein A is D-Thr, D-Val;B is D-Phe, D-Tyr;C is D-Phe, D-Tyr, O-Me-D-Tyr;wherein the ring formed by the peptide backbone contains 26 atoms and pharmaceutically acceptable non-toxic acid addition salts thereof are prepared by the solid phase method. These peptides have the property of inhibiting release of insulin, inhibiting growth hormone release and inhibiting glucagon release in humans and animals without materially affecting gastric secretion. They have a longer duration of action than somatostatin.

    Abstract translation: 具有以下结构式的肽:其中A是D-Thr,D-Val;其中A是D-Thr,D-Val;具有以下结构式的肽:< IMAGE> + TR< IMAGE>和< IMAGE> B是D-Phe,D-Tyr; C是D-Phe,D-Tyr,O-Me-D-Tyr; 其中由肽主链形成的环含有26个原子,其药学上可接受的无毒酸加成盐通过固相法制备。 这些肽具有抑制胰岛素释放,抑制生长激素释放并抑制人和动物中胰高血糖素释放而不会对胃分泌有重大影响的性质。 他们的作用时间长于生长抑素。

    (D-Ala.sup.5)-somatostatin and analogues thereof
    52.
    发明授权
    (D-Ala.sup.5)-somatostatin and analogues thereof 失效
    (D-Ala {hu 5 {b) - 抑制素及其类似物

    公开(公告)号:US4159263A

    公开(公告)日:1979-06-26

    申请号:US795685

    申请日:1977-05-11

    Inventor: Victor M. Garsky

    CPC classification number: C07K14/6555 A61K38/00 Y10S514/806 Y10S930/16

    Abstract: Polypeptides of the formula: ##STR1## WHEREIN: R is hydrogen, lower alkanoyl, Ala-Gly-, Gly-Gly-Gly-, Ala-D-Ala- or p-Glu; andX.sub.8 is L-Trp or D-Trp;Or the linear reduced form thereof; or a nontoxic acid addition salt thereof; are described. (D-Ala).sup.5 -Somatostatin and its analogues inhibit the release of growth hormone and insulin without materially affecting the secretion of glucagon, and are useful in the treatment of hyperinsulinemia and acromegaly.

    Abstract translation: 下列公式的多肽: WHEREIN:

    Organic compounds
    55.
    发明授权
    Organic compounds 失效
    有机化合物

    公开(公告)号:US4120852A

    公开(公告)日:1978-10-17

    申请号:US575156

    申请日:1975-05-07

    CPC classification number: C07K14/6555 A61K38/00 Y10S514/806 Y10S930/26

    Abstract: This invention provides new compounds of formula I, ##STR1## wherein X is H-Ala, D-Ala, .beta.-Ala, propionyl or Ac-Ala (wherein Ac is pharmaceutically acceptable acyl),Y is hydrogen or a direct bond between the sulphur atoms in positions 3 and 14, andZ is the radical --COOH, --COOR.sub.1 (wherein R.sub.1 is lower alkyl), ##STR2## (wherein R.sub.2 and R.sub.3 independently are hydrogen or lower alkyl) or --CH.sub.2 OH,with the proviso that X is other than H-Ala, when Z is COOH.useful as agents for the treatment of Diabetes Mellitus, acromegaly and angiopathy.

    Abstract translation: 本发明提供了新的式I化合物,其中X为H-Ala,D-Ala,β-Ala,丙酰或Ac-Ala(其中Ac为药学上可接受的酰基),Y为氢或 位置3和14之间的硫原子之间的直接键,Z是基团-COOH,-COOR1(其中R1是低级烷基),其中R2和R3独立地是氢或低级烷基或-CH2OH,与 条件是X不是H-Ala,当Z是COOH时。

    D-Nle.sup.4 -somatostatin and analogues thereof
    56.
    发明授权
    D-Nle.sup.4 -somatostatin and analogues thereof 失效
    D-Nle {hu 4 {b-促生长素抑制素及其类似物

    公开(公告)号:US4081433A

    公开(公告)日:1978-03-28

    申请号:US759203

    申请日:1977-01-13

    CPC classification number: C07K14/6555 A61K38/00 Y10S514/806 Y10S930/16

    Abstract: Polypeptides of the formula: ##STR1## THE LINEAR PRECURSORS, INTERMEDIATES AND NON-TOXIC ACID ADDITION SALTS THEREOF, WHEREINR is hydrogen or Ala--Gly;X.sub.4 is D--Nle, D--Val, D--Phe, D--Tyr or D--Trp; andX.sub.8 is L--Trp or D--TrpAre described. These polypeptides inhibit the secretion of growth hormone.

    Abstract translation: 下式的多肽:线性前体,中间体和非毒性添加剂,其中R为氢或Ala-Gly; X4是D-Nle,D-Val,D-Phe,D-Tyr或D-Trp; X8是L-Trp或D-Trp描述的。 这些多肽抑制生长激素的分泌。

    Somatostatin analogs and intermediates thereto
    58.
    发明授权
    Somatostatin analogs and intermediates thereto 失效
    生长抑素类似物及其中间体

    公开(公告)号:US4061626A

    公开(公告)日:1977-12-06

    申请号:US681640

    申请日:1976-04-29

    Inventor: James E. Shields

    Abstract: The tetradecapeptides ##STR1## in which Y is Gly or D-Ala are described along with corresponding non-toxic pharmaceutically-acceptable acid addition salts as well as intermediates useful in the synthesis of the tetradecapeptides. The tetradecapeptide in which Y is Gly as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo inhibition of the release of gastric acid. The tetradecapeptide in which Y is D-Ala as well as its pharmaceutically acceptable acid addition salts exhibit as their principal activity the in vivo stimulation of the release of growth hormone.

    Abstract translation: 其中Y是Gly或D-Ala的十四肽“IMAGE”以及相应的无毒的药学上可接受的酸加成盐以及可用于合成十四肽的中间体。 其中Y为Gly的十四肽及其药学上可接受的酸加成盐显示其体内抑制胃酸释放的主要活性。 其中Y是D-Ala的十四肽及其药学上可接受的酸加成盐作为其生物激素释放的体内刺激的主要活性。

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