Cyclic peptides as promoters of absorption on administration onto the
mucosa
    1.
    发明授权
    Cyclic peptides as promoters of absorption on administration onto the mucosa 失效
    作为吸收在MUCOSA上的吸收促进剂的循环肽

    公开(公告)号:US5091365A

    公开(公告)日:1992-02-25

    申请号:US228651

    申请日:1988-08-05

    IPC分类号: A61K38/00 A61K47/42 A61P43/00

    CPC分类号: A61K47/42

    摘要: The invention relates to the use of aids of the general formula ##STR1## in which B denotes a basic amino acid, A/B denotes an acidic or basic amino acid, X denotes a neutral and hydrophilic amino acid, L denotes a lipophilic neutral amino acid, and R denotes hydrogen or an acyl radical, or the physiologically tolerated salts thereof, for promoting the absorption of peptides and proteins on administration onto the mocosa, as well as to pharmaceutical compositions which contain a pharmacologically effective amount of one or more peptides or proteins as well as an aid of the abovementioned formula.

    摘要翻译: 本发明涉及使用通式“IMAGE”的助剂,其中B表示碱性氨基酸,A / B表示酸性或碱性氨基酸,X表示中性和亲水性氨基酸,L表示亲脂性中性氨基 酸,R表示氢或酰基,或其生理上耐受的盐,用于促进肽和蛋白质在施用于马卡土上时的吸收,以及含有药理学有效量的一种或多种肽的药物组合物或 蛋白质以及上述配方的辅助。

    Competitive gonadoliberin antagonists
    2.
    发明授权
    Competitive gonadoliberin antagonists 失效
    竞争性GONADOLIBERIN拮抗剂

    公开(公告)号:US5071836A

    公开(公告)日:1991-12-10

    申请号:US448904

    申请日:1989-12-12

    CPC分类号: C07K7/23 A61K38/00

    摘要: Peptides of the formulaAc-D-Nal(2)-D-Phe-D-Phe-Ser-X-D-Ser(Rha)-Leu-Arg-Pro-Yin which X represents Tyr or His and Y represents Gly-NH.sub.2, D-Ala-NH.sub.2, Azgly-NH.sub.2 or NH--C.sub.2 H.sub.5 are competitive antagonists of Gn-RH. They are used for the treatment of gonadotropin- and steroid-dependent diseases and are prepared by known methods of peptide chemistry.

    摘要翻译: 式Ac-D-Nal(2)-D-Phe-D-Phe-Ser-XD-Ser(Rha)-Leu-Arg-Pro-Y的肽,其中X表示Tyr或His,Y表示Gly-NH2 ,D-Ala-NH2,Azgly-NH2或NH-C2H5是Gn-RH的竞争性拮抗剂。 它们用于治疗促性腺激素和类固醇依赖性疾病,并通过已知的肽化学方法制备。

    Analogs of gonadoliberin with improved solubility, methods for their
preparation, agents containing them and their use
    4.
    发明授权
    Analogs of gonadoliberin with improved solubility, methods for their preparation, agents containing them and their use 失效
    具有改善溶解性的甘油二醇的模拟物,其制备方法,包含它们的试剂及其用途

    公开(公告)号:US5091367A

    公开(公告)日:1992-02-25

    申请号:US724477

    申请日:1991-06-28

    CPC分类号: C07K7/23 A61K38/00 Y10S514/80

    摘要: The invention relates to peptides of the formula ##STR1## in which X is absent or is hydrogen or acyl; A is Pgl, de-hydro-Pro, Pro, D-Thi or D-Pgl or represents optionally substituted D-Nal(2), D-Phe or D-Trp; B is His or optionally substituted D-Phe; C is Trp, D-Thi, D-Pal(3) or optionally substituted D-Trp; D is Tyr, Arg of His; E is D-Ser(R.sup.1), .beta.-Asn, .beta.-Asp-OMe, D-Thi or --NH--CH(CH.sub.2 R.sup.2)--CO--; F is Ser(R.sup.1), Leu, Trp or Phe; G is Gly-NH.sub.2, Aza-Gly-NH.sub.2, D-Ala-NH.sub.2 or NH-alkyl; R.sup.1 is glycosyl and R.sup.2 is hydrogen, acyl, aryl or heteroaryl.The invention also relates to methods for the preparation of these peptides, agents containing them and their use.

    摘要翻译: 本发明涉及式“IMAGE”的肽,其中X不存在或为氢或酰基; A是Pgl,de-hydro-Pro,Pro,D-Thi或D-Pgl或代表任选取代的D-Nal(2),D-Phe或D-Trp; B是His或任选被取代的D-Phe; C是Trp,D-Thi,D-Pal(3)或任选取代的D-Trp; D是他的Tyr,Arg; E是D-Ser(R1),β-Asn,β-Asp-OMe,D-Thi或-NH-CH(CH2R2)-CO-; F是Ser(R1),Leu,Trp或Phe; G是Gly-NH 2,Aza-Gly-NH 2,D-Ala-NH 2或NH-烷基; R1是糖基,R2是氢,酰基,芳基或杂芳基。 本发明还涉及制备这些肽,含有它们的试剂及其用途的方法。