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    • 10. 发明授权
    • Peptides, process for preparation thereof and use thereof
    • 肽,其制备方法和用途
    • US4354966A
    • 1982-10-19
    • US193453
    • 1980-10-03
    • Yoshihiko KitauraOsamu NakaguchiKeiji HemmiMatsuhiko ArataniHidekazu TakenoSatoshi OkadaHirokazu TanakaMasashi Hashimoto
    • Yoshihiko KitauraOsamu NakaguchiKeiji HemmiMatsuhiko ArataniHidekazu TakenoSatoshi OkadaHirokazu TanakaMasashi Hashimoto
    • A61K38/00C07K5/02C07K9/00C07C103/52
    • C07C243/00C07K5/0215C07K9/005C12R1/465A61K38/00
    • 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.
    • 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。