Phenylglycine-containing new peptides with gastrine effects and a
process for the preparation thereof
    4.
    发明授权
    Phenylglycine-containing new peptides with gastrine effects and a process for the preparation thereof 失效
    含有苯基甘氨酸的新肽具有胃泌素作用及其制备方法

    公开(公告)号:US4183909A

    公开(公告)日:1980-01-15

    申请号:US859931

    申请日:1977-12-12

    CPC分类号: C07K5/1024 A61K38/00

    摘要: The invention relates to novel peptides of formula (I),A-Try-B-Asp-Phg-NH.sub. 2 (I)whereinA is tert.-butoxycarbonyl-aminooxy-acyl, benzyloxycarbonyl-aminooxy-acyl, (aminooxy)-acyl or E-aminooxy-acyl, wherein E is benzoyl or straight-chained or branched C.sub.1-5 aliphatic acyl, andB represents methionyl, leucyl, norleucyl, norvalyl or 2-amino-decanoyl,or acid addition salts or complexes thereof. The novel compounds according to the invention exert gastrin effects and can be applied to advantage in the diagnostics and therapy. The novel compounds of formula (I) are prepared according to the invention by reacting a tetrapeptideamide of formula (II),H-Try-B-Asp-Phg-NH.sub. 2 (II)wherein B is as defined above, with an (aminooxy)-acyl containing compound of the general formula A.sub.1 -X, whereinA.sub.1 has the same meanings as A with the exception of the (aminooxy)-acyl, andX is hydroxy group, halogen, pivaloyloxy, a group of the formula R--O--CO.sub.2 -- (wherein R is lower alkyl, phenoxy which can have a nitro substituent or one or more halogen or N-succinimidoxy.

    摘要翻译: 本发明涉及式(I)的新型肽A-Try-B-Asp-Phg-NH 2(I),其中A为叔丁氧基羰基 - 氨基氧基 - 酰基,苄氧基羰基 - 氨氧基 - 酰基,(氨氧基) - 酰基 或E-氨基氧基 - 酰基,其中E是苯甲酰基或直链或支链C 1-5脂肪族酰基,B代表甲硫氨酰基,亮氨酰基,正亮氨酰基,缬氨酰基或2-氨基 - 癸酰基,或其酸加成盐或配合物。 根据本发明的新型化合物发挥促胃泌素作用,并且可以在诊断和治疗中有利地应用。 通过使式(II)的四肽酰胺,其中B如上所定义的H-Try-B-Asp-Phg-NH 2(II)与(氨基氧基) ) - 酰基的通式为Al-X的化合物,其中除了(氨基氧基) - 酰基以外,与A相同,A为氧基,X为羟基,卤素,新戊酰氧基,式RO-CO2 - (其中R是低级烷基,可具有硝基取代基的苯氧基或一个或多个卤素或N-琥珀酰亚胺氧基)。

    Pharmaceutical compositions comprising novel oligopeptides exhibiting
selective inhibiting effect upon the proliferation of hemopoietic cells
    7.
    发明授权
    Pharmaceutical compositions comprising novel oligopeptides exhibiting selective inhibiting effect upon the proliferation of hemopoietic cells 失效
    包含对造血细胞增殖具有选择性抑制作用的新型寡肽的药物组合物

    公开(公告)号:US5312812A

    公开(公告)日:1994-05-17

    申请号:US750278

    申请日:1994-05-17

    摘要: The present invention relates to novel peptides of formulaeXaa Glu Asp Cys Lys (SEQ I.D. No: 1),andGlu Asp Cys Lys (SEQ I.D. No: 2)wherein the Cys sulfur is bonded to an acetamidomethyl group, and Xaa is pyro-Glu, the acid addition salts thereof, the pharmaceutical compositions comprising the same and a process for the preparation of the novel peptides and compositions.The novel peptides selectively inhibit the proliferation of hemopoietic cells.The invention also covers the treatment of mammals (including human beings) with the said peptides and compositions for selectively inhibiting the proliferation of hemopoietic cells.The advantage of the novel compounds is that they are almost completely harmless, they do not have any side-effect in therapeutic dose-range, in addition they significantly inhibit the damaging effects of drugs and radiation used for the therapy of tumorous diseases or the dose of drug or radiation can be increased when they are administered.

    摘要翻译: 本发明涉及式Xaa Glu Asp Cys Lys(SEQ ID No:1)和Glu Asp Cys Lys(SEQ ID No:2)的新型肽,其中Cys硫与乙酰氨基甲基结合,Xaa是热解 - Glu,其酸加成盐,包含其的药物组合物和制备新肽和组合物的方法。 新型肽选择性抑制造血细胞的增殖。 本发明还涵盖用所述肽和用于选择性抑制造血细胞增殖的组合物治疗哺乳动物(包括人)。 新化合物的优点是它们几乎完全无害,它们在治疗剂量范围内没有任何副作用,此外它们显着抑制用于治疗肿瘤疾病或剂量的药物和辐射的破坏作用 药物或放射线在施用时可以增加。