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6 条记录 (耗时 0.017 秒)

    Gonadoliberin antagonists
    2.
    发明授权
    Gonadoliberin antagonists 失效
    Gonadoliberin拮抗剂

    公开(公告)号：US5434138A

    公开(公告)日：1995-07-18

    申请号：US151056

    申请日：1993-11-12

    申请人： Wolfgang Konig ,  Jurgen Sandow ,  Cenek Kolar

    发明人： Wolfgang Konig ,  Jurgen Sandow ,  Cenek Kolar

    IPC分类号： A61K38/00 ,  A61P5/00 ,  A61P5/24 ,  C07K7/06 ,  C07K7/23 ,  C07K9/00 ,  C07K14/575 ,  C07K7/00

    CPC分类号： C07K7/23 ,  A61K38/00

    摘要： Peptides of the formula ##STR1## in which X is alkanoyl, A is optionally substituted D-Nal(2), D-Phe or D-Trp, B is optionally substituted D-Phe, C is D-Pal(3) or optionally substituted D-Phe or D-Trp, and D is Tyr or His, E is D-Ser (R.sup.1), F is Leu, Trp or Phe, G is L-Ser(R.sup.1), H is Gly-NH.sub.2, D-Ala-NH.sub.2 or Azagly-NH.sub.2 and R.sup.1 is a glycosyl radical. These peptides have an inhibitory effect on the formation of the gonadotropins lutropin and follitropin and thus also on the synthesis of testo-sterone and estrogen. A process for the preparation of these peptides is described.

    摘要翻译： 式中，X为链烷酰基，A为任选取代的D-Nal（2），D-Phe或D-Trp，B为任选取代的D-Phe，C为D-Pal（3）或任选地为 取代的D-Phe或D-Trp，D为Tyr或His，E为D-Ser（R1），F为Leu，Trp或Phe，G为L-Ser（R1），H为Gly-NH2， Ala-NH2或Azagly-NH2，R1是糖基。 这些肽对促性腺激素营养素和叶黄素的形成具有抑制作用，因此也对睾酮和雌激素的合成具有抑制作用。 描述了制备这些肽的方法。

    Cyclopeptides and their use as absorption promoters when applied to the mucosa
    4.
    发明授权
    Cyclopeptides and their use as absorption promoters when applied to the mucosa 失效
    环肽及其作为吸收促进剂用于粘膜时的应用

    公开(公告)号：US5565423A

    公开(公告)日：1996-10-15

    申请号：US418882

    申请日：1995-04-07

    申请人： Jurgen Sandow ,  Walter Durckheimer ,  Gunter Ditzinger ,  Hans-Peter Merkle

    发明人： Jurgen Sandow ,  Walter Durckheimer ,  Gunter Ditzinger ,  Hans-Peter Merkle

    IPC分类号： A61K47/42 ,  A61K38/00 ,  A61K38/04 ,  C07K7/62 ,  A61K38/12

    CPC分类号： C07K7/62 ,  A61K38/00 ,  Y02P20/55

    摘要： Cyclopeptides and their use as absorption promoters when applied to the mucosaThe invention relates to a compound of the formula I ##STR1## or a physiologically tolerated salt thereof, in which X is a basic L- or D-amino acid,Y is a neutral or basic L- or D-amino acid,Z is a neutral or basic L- or D-amino acid, which can be identical to or different from Y,R.sup.1 is an N-bonded acyl radical of the formula II ##STR2## in which Ar is a phenyl radical, which is optionally substituted by 1, 2 or 3 identical or different radicals from the series comprising hydroxyl, (C.sub.1 -C.sub.4)-alkoxy, amino, carboxyl, (C.sub.1 -C.sub.4)-alkylamino and halogen, or is a 2-aminothiazol-4-yl radical,p is an integer from zero to 4 and q, n, m and 1 independently of one another are zero or 1.The invention additionallly relates to the use of compounds of the formula I and physiologically tolerated salts thereof for promoting the absorption of peptides and proteins when applied to the mucosa, and pharmaceutical formulations which contain a pharmacologically active amount of one or more peptides or proteins and a compound of the formula I or physiologically tolerated salts thereof.

    摘要翻译： 环肽及其作为吸收促进剂的用途本发明涉及式I化合物或其生理上耐受的盐，其中X为碱性L-或D-氨基酸，Y 是中性或碱性的L-或D-氨基酸，Z是中性或碱性的L-或D-氨基酸，其可以与Y相同或不同，R1是式II的N-键合的酰基， 其中Ar是苯基，其任选被1,2或3个相同或不同的基团取代，所述基团包含羟基，（C 1 -C 4） - 烷氧基，氨基，羧基，（C 1 -C 4） - 烷基氨基和卤素，或是2-氨基噻唑-4-基，p是0至4的整数，且q，n，m和1彼此独立地为零或1.本发明还涉及使用 式I化合物及其生理学上可耐受的盐，用于在应用于粘膜时促进肽和蛋白质的吸收，以及药物制剂 含有药理活性量的一种或多种肽或蛋白质的离子和式I化合物或其生理学上耐受的盐。