Peptide, process for preparation thereof and use thereof
    4.
    发明授权
    Peptide, process for preparation thereof and use thereof 失效
    肽,其制备方法及其用途

    公开(公告)号:US4311640A

    公开(公告)日:1982-01-19

    申请号:US93523

    申请日:1979-11-13

    摘要: The invention deals with novel peptides useful for the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. Included is the peptide FR900156 having the structure: ##STR1## as well as the peptides of the structure ##STR2## wherein R.sup.1 is acyl;R.sub.b.sup.1 is hydrogen, methyl, isopropyl, hydroxymethyl, protected hydroxymethyl or benzyl;R.sup.2 is hydrogen, carboxy, protected carboxy, or a group of the formula: ##STR3## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl or ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy,R.sub.b.sup.2 is hydrogen or lower alkyl;R.sup.p and R.sup.q are each hydrogen, carboxy, protected carboxy, with proviso that when one of R.sup.2 and R.sup.q is hydrogen, then the other is carboxy or protected carboxy;R.sup.r is hydrogen or amino protective group; m is an integer 1 to 3; and n is 1 provided that when R.sup.1 is hydrogen, t-butoxycarbonyl or N-acetylmuramyl, R.sub.b.sup.1 is methyl, m is an integer 2 and n is an integer 1, then R.sup.2 is hydrogen, protected carboxy or a group of the formula: ##STR4## wherein R.sub.a.sup.2 is mono- or di-carboxy lower alkyl having 1 and 3 to 6, carbon atoms, .alpha.-carboxyethyl, ar(carboxy) lower alkyl whose aryl moiety may be substituted by hydroxy and R.sub.b.sup.2 is as defined above, or its pharmaceutically acceptable salt.

    摘要翻译: 本发明涉及可用于治疗由病原微生物引起的感染性疾病的新型肽。 包括具有以下结构的肽FR900156:以及结构的肽,其中R 1是酰基; Rb1是氢,甲基,异丙基,羟甲基,保护的羟甲基或苄基; R2是氢,羧基,受保护的羧基或下式的基团:其中R 2a是其芳基部分可以被羟基取代的一或二羧基低级烷基或芳(羧基)低级烷基,R 2b是氢或 低级烷基 Rp和Rq各自为氢,羧基,保护的羧基,条件是当R 2和R q中的一个为氢时,则另一个为羧基或被保护的羧基; Rr为氢或氨基保护基; m为整数1〜3; 并且n为1,条件是当R 1为氢时,叔丁氧基羰基或N-乙酰胞壁酰基,R 1b为甲基,m为整数2,n为整数1,则R 2为氢,被保护的羧基或下式基团: 其中Ra2是具有1和3至6个碳原子的一或二羧基低级烷基,其α-芳基部分可以被羟基取代的α-羧乙基,芳(羧基)低级烷基,如上所定义,或其 药学上可接受的盐。