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。

    Quinolizinone compounds and pharmaceutical composition comprising the
same, useful as anti-ulcerative and anti-allergic agents
    5.
    发明授权
    Quinolizinone compounds and pharmaceutical composition comprising the same, useful as anti-ulcerative and anti-allergic agents 失效
    喹诺酮类化合物和包含其的药物组合物,可用作抗溃疡和抗过敏剂

    公开(公告)号:US4650804A

    公开(公告)日:1987-03-17

    申请号:US712435

    申请日:1985-03-18

    摘要: The invention relates to novel quinolizinone compounds having inhibitory activity on allergies and ulcers, of the formula: ##STR1## wherein R.sup.1 is tetrazolylcarbamoyl;R.sup.7 is hydrogen or aryl selected from phenyl, tolyl, xylyl, cumenyl, naphthyl and biphenylyl;R.sup.2 is hydrogen, hydroxy, lower alkyl or lower alkoxy;R.sup.3 is hydrogen, hydroxy, lower alkyl, lower alkoxy, lower alkenyloxy, phenyl, napthyl, biphenylyl, phenyl having one or more substituent(s) selected from halogen, lower alkyl and lower alkoxy, arylthio selected from phenylthio, tolylthio, xylylthio, cumenylthio, naphthylthio and biphenylthio, aroyl selected from benzoyl, toluoyl and naphthoyl, ar(lower)alkyl selected from phenyl(lower)alkyl, tolyl(lower)alkyl, xylyl(lower)alkyl, cumenyl(lower)alkyl, naphthyl(lower)alkyl and biphenylyl(lower)alkyl, arenesulfonyl selected from benzenesulfonyl and p-toluenesulfonyl, arylamino selected from phenylamino, naphthylamino, biphenylylamino, phenylamino having lower alkyl on the nitrogen atom or aryloxy selected from phenoxy and tolyloxy;or pharmaceutically acceptable salts thereof.

    摘要翻译: 本发明涉及具有下式的过敏和溃疡抑制活性的新型喹嗪酮化合物:其中R1是四唑基氨基甲酰基; R7是氢或选自苯基,甲苯基,二甲苯基,枯烯基,萘基和联苯基的芳基; R2是氢,羟基,低级烷基或低级烷氧基; R3是氢,羟基,低级烷基,低级烷氧基,低级烯氧基,苯基,萘基,联苯基,具有一个或多个选自卤素,低级烷基和低级烷氧基的取代基的苯基,选自苯硫基,甲苯硫基,二甲苯硫基, ,萘基硫基和联苯硫基,选自苯甲酰基,甲苯酰基和萘甲酰基的芳酰基,选自苯基(低级)烷基,甲苯基(低级)烷基,二甲苯基(低级)烷基,枯烯基(低级)烷基,萘基 和选自苯磺酰基和对甲苯磺酰基的联苯基(低级)烷基,芳基磺酰基,选自苯基氨基,萘基氨基,联苯基氨基,在氮原子上具有低级烷基的苯基氨基或选自苯氧基和甲酰基氧基的芳氧基; 或其药学上可接受的盐。