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    Hydroxyaminohydrocarbonphosphonic acid derivatives and use thereof as an antibiotic
    32.
    发明授权
    Hydroxyaminohydrocarbonphosphonic acid derivatives and use thereof as an antibiotic 失效
    羟基氨基烃基膦酸衍生物及其作为抗生素的用途

    公开(公告)号：US4182758A

    公开(公告)日：1980-01-08

    申请号：US819554

    申请日：1977-07-27

    申请人： Takashi Kamiya ,  Masashi Hashimoto ,  Keiji Hemmi ,  Hidekazu Takeno

    发明人： Takashi Kamiya ,  Masashi Hashimoto ,  Keiji Hemmi ,  Hidekazu Takeno

    IPC分类号： C12P13/00 ,  A61K31/66 ,  A61P31/04 ,  C07F9/38 ,  C07F9/40 ,  C12P9/00 ,  C12R1/465 ,  A01N9/36

    CPC分类号： C07F9/4006 ,  C07F9/3808 ,  C07F9/3826

    摘要： Hydroxyaminohydrocarbonphosphonic acid derivatives represented by the formula: ##STR1## wherein R.sup.1 is hydrogen or acyl,R.sup.2 is hydrogen, lower alkyl, ar(lower) alkyl or acyl, andA is lower alkylene, lower alkenylene or hydroxy(lower) alkylene, or the esters at the phosphono group thereof or the pharmaceutically acceptable salts thereof, excepting 3-(N-acetyl-N-hydroxyamino) propylphosphonic acid, 3-(N-acetyl-N-hydroxyamino)-2-hydroxypropylphosphonic acid, and their pharmaceutically acceptable salts, and processes for preparing the same.Included are compounds having antimicrobial activity against various pathogenic organisms.

    摘要翻译： 其中R1是氢或酰基，R2是氢，低级烷基，芳基（低级）烷基或酰基，A是低级亚烷基，低级亚烯基或羟基（低级）亚烷基）的羟基氨基烃基膦酸衍生物，或者 除了3-（N-乙酰基-N-羟基氨基）丙基膦酸，3-（N-乙酰基-N-羟基氨基）-2-羟丙基膦酸及其药学上可接受的盐，其膦酰基酯或其药学上可接受的盐 ，及其制备方法。 包括具有抗各种致病生物的抗微生物活性的化合物。

    Peptides, process for preparation thereof and use thereof
    37.
    发明授权
    Peptides, process for preparation thereof and use thereof 失效
    肽，其制备方法和用途

    公开(公告)号：US4354966A

    公开(公告)日：1982-10-19

    申请号：US193453

    申请日：1980-10-03

    申请人： Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

    发明人： Yoshihiko Kitaura ,  Osamu Nakaguchi ,  Keiji Hemmi ,  Matsuhiko Aratani ,  Hidekazu Takeno ,  Satoshi Okada ,  Hirokazu Tanaka ,  Masashi Hashimoto

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

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

    摘要： The invention relates to novel peptides and their pharmaceutically acceptable salts, particularly useful for pharmaceutical purposes such as in the therapeutic treatment of infectious diseases caused by pathogenic microorganisms. The compounds have the structure ##STR1## wherein R.sup.1 is hydrogen or acyl;R.sup.2 is carboxy or protected carboxy or a group of the formula: --COHN--R.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl;R.sup.3 is carboxy, protected carboxy, lower alkyl, hydroxyphenyl, carbamoyl or a group of the formula: ##STR2## wherein R.sub.a.sup.3 is hydrogen, amino, protected amino or acylamino, R.sub.b.sup.3 is carboxy or protected carboxy;R.sup.p is carboxy, protected carboxy, carbamoyl, carboxy (lower) alkyl or protected carboxy (lower) alkyl;l is an integer 2,m is an integer 0 to 2 andn is an integer 1,provided that,whenR.sup.1 is hydrogen or acyl,R.sup.2 is carboxy, protected carboxy or a group of the formula: --CONHR.sub.a.sup.2 wherein R.sub.a.sup.2 is carboxy (lower) alkyl or protected carboxy (lower) alkyl,R.sup.p is carboxy, or protected carboxy, m is an integer 2, thenR.sup.3 is carbamoyl, lower alkyl or hydroxyphenyl or a group of the formula: ##STR3## wherein R.sub.a.sup.3 is hydrogen or acylamino and R.sub.b.sup.3 is carboxy or protected caboxy, andwhenR.sup.p is carbamoyl, thenR.sup.1 is acyl.

    摘要翻译： 本发明涉及新型肽及其药学上可接受的盐，特别可用于药物目的，例如由病原微生物引起的感染性疾病的治疗性治疗。 这些化合物具有结构，其中R 1是氢或酰基; R2是羧基或保护的羧基或下式基团-COHN-Ra2，其中Ra2是羧基（低级）烷基或被保护的羧基（低级）烷基; R 3是羧基，保护的羧基，低级烷基，羟基苯基，氨基甲酰基或下式的基团：其中R 3a是氢，氨基，被保护的氨基或酰氨基，R 3b是羧基或被保护的羧基; Rp是羧基，保护的羧基，氨基甲酰基，羧基（低级）烷基或被保护的羧基（低级）烷基; l为整数2，m为整数0〜2，n为整数1，条件是当R 1为氢或酰基时，R 2为羧基，被保护的羧基或式-CONHRa 2基团，其中Ra 2为羧基（ 低级）烷基或受保护的羧基（低级）烷基，Rp是羧基或受保护的羧基，m是整数2，则R3是氨基甲酰基，低级烷基或羟基苯基或下式的基团：其中R 3a是氢或酰基氨基 并且R 3b是羧基或被保护的环氧基，当Rp是氨基甲酰基时，则R1是酰基。

    Heterobicyclic derivatives
    39.
    发明授权
    Heterobicyclic derivatives 失效
    异环衍生物

    公开(公告)号：US06727245B2

    公开(公告)日：2004-04-27

    申请号：US10050855

    申请日：2002-01-18

    申请人： Norihiko Shimazaki ,  Shinya Watanabe ,  Akihiko Sawada ,  Keiji Hemmi

    发明人： Norihiko Shimazaki ,  Shinya Watanabe ,  Akihiko Sawada ,  Keiji Hemmi

    IPC分类号： A61P1106

    CPC分类号： C07D471/04

    摘要： Heterobicyclic derivatives of the formula: wherein R1 is aryl which may have suitable substituent(s), ar(lower)alkyl which may have suitable substituent(s), halo(lower)alkyl, protected carboxy(lower)alkyl, acyl(lower)alkyl, heterocyclic group or heterocyclic(lower)alkyl which may have suitable substituent(s), R2 is aryl which may have suitable substituent(s) or heterocyclic group, and R3 is hydrogen, lower alkoxy or arylthio, and a pharmaceutically acceptable salt thereof which are useful as a medicament.

    摘要翻译： 下式的双环衍生物：其中R 1是可以具有合适取代基的芳基，可以具有合适取代基的芳基（低级）烷基，卤代（低级）烷基，保护的羧基（低级）烷基，酰基（ 低级）烷基，杂环基或可具有合适取代基的杂环（低级）烷基，R 2为可具有合适取代基或杂环基的芳基，R 3为氢，低级烷氧基或芳硫基 和其药学上可接受的盐，其可用作药物。