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    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

    申请人： Yoshio Kuroda ,  Eiko Iguchi ,  Masanobu Kohsaka ,  Hatsuo Aoki ,  Hiroshi Imanaka ,  Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

    发明人： Yoshio Kuroda ,  Eiko Iguchi ,  Masanobu Kohsaka ,  Hatsuo Aoki ,  Hiroshi Imanaka ,  Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

    IPC分类号： A61K38/00 ,  C07K5/02 ,  C07K7/02 ,  C07K9/00 ,  C07C103/52 ,  C07G7/00

    CPC分类号： C07C243/00 ,  C07K5/0215 ,  C07K9/005 ,  C12R1/465 ,  A61K38/00 ,  Y02P20/55

    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。