Pharmaceutical peptides, preparation, use and intermediates
    3.
    发明授权
    Pharmaceutical peptides, preparation, use and intermediates 失效
    药物肽,制剂,用途和中间体

    公开(公告)号:US4540682A

    公开(公告)日:1985-09-10

    申请号:US613868

    申请日:1984-05-23

    摘要: Novel peptides of formula (I) ##STR1## wherein R.sup.1 is hydrogen, alkyl of 1 or 2 carbon atoms or an amidino group,R.sup.2 is alkyl of 1 or 2 carbon atoms,R.sup.3 is hydrogen or carbamyl,X.sup.2 is a D-radical having the structure: ##STR2## Z.sup.1 and Z.sup.2 are the same or different and each is hydrogen, halo, nitro or trifluoromethyl and at least one is other than hydrogen,m is 2, 3 or 4 andn is 0, 1 or 2,provided that when R.sup.3 is carbamyl then n is always 1;and salts thereof.The compounds have a selectively peripheral analgesic effect when administered to mammals and also exhibit antidiarrhoeal and antitussive activity and may thus be used in human or veterinary medicine for the relief or prevention of pain, for the treatment of diarrhoea or dysentery and for the suppression of cough.

    摘要翻译: 式(I)的新肽其中R1是氢,1或2个碳原子的烷基或脒基,R2是1或2个碳原子的烷基,R3是氢或氨基甲酰基,X2是D 具有以下结构的化合物:< IMAGE> Z1和Z2相同或不同,各自为氢,卤素,硝基或三氟甲基,至少一个不是氢,m为2,3或4,n为0,1或 2,条件是当R 3为氨甲酰基时,则n总是为1; 及其盐。 当给予哺乳动物时,这些化合物具有选择性的外周止痛作用,并且还具有抗腹泻和镇咳作用,因此可用于人或兽医学用于缓解或预防疼痛,用于治疗腹泻或痢疾以及抑制咳嗽 。

    Pharmacologically active compounds and use
    5.
    发明授权
    Pharmacologically active compounds and use 失效
    药理活性化合物及用途

    公开(公告)号:US4837203A

    公开(公告)日:1989-06-06

    申请号:US70407

    申请日:1987-07-07

    摘要: The peptides of the formulaX--Tyr--X.sup.2 --Gly--Phe(4NO.sub.2)--Pro--NH.sub.2wherein X is hydrogen or an amidino group and X.sup.2 is D-S-methylmethionyl or D-arginyl, together with their pharmacologically acceptable salts, which have been described as exhibiting analgesic, antidiarrhoeal and antitussive activity, are effective in reversing neuronally-mediated bronchoconstriction in mammals. The said compounds have application in the palliation of conditions characterized by such a state, in particular asthma in human beings.

    摘要翻译: 式X-Tyr-X2-Gly-Phe(4NO2)-Pro-NH2的肽,其中X是氢或脒基,X 2是DS-甲基甲硫氨酸或D-精氨酰基,以及它们的药理学上可接受的盐, 被描述为显示镇痛,止泻和镇咳活性,有效地逆转哺乳动物中的神经元介导的支气管收缩。 所述化合物可用于缓解特征在于这种状态,特别是人类哮喘的病症。