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Agonist analogues of luteinizing hormone releasing hormone

机译:黄体生成激素释放激素的激动剂类似物

摘要

Novel peptide compounds of the formula ##EQU1## are provided together with their acid addition salts and their complexes with pharmaceutically acceptable metals. The compounds are LH-RH analogues and together with their salts and complexes exhibit LH-RH agonist activity. In the formulaPPX.sup.3 and X.sup.5 are the same or different and each is phenylalanyl optionally substituted in the benzene ring; PPX.sup.4 and X.sup.6 are the same or different and each is selected from glycyl, alanyl (D- or L-) and asparaginyl;P P X.sup.7 is a radical of a neutral hydrophobic nonsulphur containing non- heterocyclic amino acid;PPX.sup.8 is a radical of a basic amino acid or is glycyl or phenylalanyl optionally substituted in the benzene ring; andPPW is selected from glycine amide and a group --NR.sup.1 R.sup.2.PPAll references are to the L- amino acids and their radicals except in the case of glycine and unless otherwise stated.PPAlso provided are methods for the preparation of the peptides, salts and complexes, pharmaceutical formulations containing them and methods for the preparation of such formulations, and methods for the use of the peptides, salts and complexes in human and in veterinary medicine.
机译:提供了式## EQU1 ##的新型肽化合物,以及它们的酸加成盐以及它们与药学上可接受的金属的配合物。该化合物是LH-RH类似物,并且与它们的盐和配合物一起表现出LH-RH激动剂活性。式中,P X 3和X 5相同或不同,且各自为任选地在苯环中取代的苯丙氨酰基; P 4 X和X。 sup.6是相同或不同的,并且各自选自甘氨酰基,丙氨酰基(D-或L-)和天冬酰胺基;

X.sup.7是含有非杂环氨基的中性疏水性非硫基团酸; P 8 X是碱性氨基酸的基团,或者是苯环中任选取代的甘氨酰基或苯丙氨酰基;并且

W选自甘氨酸酰胺和--NR.sup.1 R.sup.2。

所有参考文献涉及L-氨基酸及其基团,除了除非另有说明,否则为甘氨酸的情况。还提供了肽,盐和复合物的制备方法,包含它们的药物制剂以及此类制剂的制备方法和肽的使用方法,人类和兽医学中的盐,盐和配合物。

著录项

  • 公开/公告号FR2249677B1

    专利类型

  • 公开/公告日1978-07-28

    原文格式PDF

  • 申请/专利权人 WELLCOME FOUNDATION LTD;

    申请/专利号FR19740036431

  • 发明设计人

    申请日1974-10-31

  • 分类号A61K37/38;C07C103/52;

  • 国家 FR

  • 入库时间 2022-08-22 21:49:54

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