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    New mitomycin derivatives, preparation thereof and pharmaceutical compositions containing them
    2.
    发明授权
    New mitomycin derivatives, preparation thereof and pharmaceutical compositions containing them 失效
    新的丝裂霉素衍生物，其制备方法和含有它们的药物组合物

    公开(公告)号：US4691024A

    公开(公告)日：1987-09-01

    申请号：US915949

    申请日：1986-10-03

    申请人： Kunikatsu Shirahata ,  Motomichi Kono ,  Yutaka Saito ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

    发明人： Kunikatsu Shirahata ,  Motomichi Kono ,  Yutaka Saito ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

    IPC分类号： A61K31/40 ,  A61K38/00 ,  A61P31/04 ,  A61P35/00 ,  C07D487/14 ,  C07K5/02 ,  C07K5/06

    CPC分类号： C07D487/14 ,  C07K5/0215 ,  C07K5/06026 ,  A61K38/00

    摘要： The present invention provides new mitomycin derivatives of general formula (I) ##STR1## [wherein Y and Z, which may be the same or different, each represents a hydrogen atom or a methyl group; represents .alpha. or .beta. bonding and X represents a group of formula (II) ##STR2## (wherein R.sub.1 to R.sub.5 are each selected from hydrogen, halogen, hydroxyl, nitro, amino, lower alkyl, lower alkoxy, lower alkylamino or lower alkanoylamino);or an S-yl group of an amino acid having a thiol group, the carboxyl group optionally being protected e.g. in the form of a lower alkyl ester group and the amino group optionally being protected e.g. in the form of a lower alkanoylamino group;or an S-yl group of a di- or tripeptide containing an amino acid residue with a thiol group, the carboxyl group optionally being protected e.g. in the form of a lower alkyl ester and the amino group optionally being protected e.g. in the form of a lower alkanoylamino group]; and salts thereof.Such mitomycin derivatives have improved anti-bacterial and anti-tumor activities and low toxicity.

    摘要翻译： 本发明提供新的通式（I）的丝裂霉素衍生物：其中Y和Z可以相同或不同，各自表示氢原子或甲基; 表示α或β键，X表示式（II）的基团（II）（其中R 1至R 5各自选自氢，卤素，羟基，硝基，氨基，低级烷基，低级烷氧基，低级烷基氨基或低级 烷酰氨基）; 或具有硫醇基的氨基酸的S-基团，所述羧基任选被保护，例如。 以低级烷基酯基团的形式，并且任选地被保护的氨基，例如。 为低级烷酰氨基的形式; 或含有具有硫醇基的氨基酸残基的二肽或三肽的S-基团，所述羧基任选被保护，例如。 以低级烷基酯的形式，并且任选地被保护的氨基，例如。 以低级烷酰氨基的形式]; 及其盐。 这种丝裂霉素衍生物具有改善的抗细菌和抗肿瘤活性和低毒性。

    7-n-aminomethylenemitomycin derivative
    4.
    发明授权
    7-n-aminomethylenemitomycin derivative 失效
    7-氨基亚甲基霉素衍生物

    公开(公告)号：US4748251A

    公开(公告)日：1988-05-31

    申请号：US824227

    申请日：1986-01-30

    申请人： Kunikatsu Shirahata ,  Motomichi Kono ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

    发明人： Kunikatsu Shirahata ,  Motomichi Kono ,  Masaji Kasai ,  Makoto Morimoto ,  Tadashi Ashizawa

    IPC分类号： A61K31/40 ,  A61P35/00 ,  C07D487/14

    CPC分类号： C07D487/14

    摘要： Mitomycin derivatives represented by the formula (I): ##STR1## wherein R.sub.1 and R.sub.2 may be the same or different, and represent a hydrogen atom or a lower alkyl group; R.sub.3 and R.sub.4 mean that when R.sub.3 is a hydrogen atom, R.sub.4 represents --CH.sub.2 OCONH.sub.2 or ##STR2## (wherein R.sub.1 and R.sub.2 have the same significances as defined above), or R.sub.3 and R.sub.4 are combined to form .dbd.CH.sub.2 ; Y and Z may be the same or different, and represent a hydrogen atom or a methyl group; represents .alpha.- or .beta.-bond, provided that Y represents a hydrogen atom when R.sub.4 takes .beta.-configuration, have an excellent anti-tumor activity.

    摘要翻译： 由式（I）表示的丝裂霉素衍生物：其中R 1和R 2可以相同或不同，表示氢原子或低级烷基; R 3和R 4表示当R 3是氢原子时，R 4表示-CH 2 OCONH 2或者其中R 1和R 2具有与上述相同的含义，或者R 3和R 4组合形成= CH 2; Y和Z可以相同或不同，表示氢原子或甲基; 表示α或β键，条件是当R 4为β-构型时，Y表示氢原子，具有优异的抗肿瘤活性。

    9-Epi-mitomycin B and D compounds
    8.
    发明授权
    9-Epi-mitomycin B and D compounds 失效
    9-丝裂霉素B和D化合物

    公开(公告)号：US4395558A

    公开(公告)日：1983-07-26

    申请号：US323847

    申请日：1981-11-23

    申请人： Masaji Kasai ,  Kunikatsu Shirahata ,  Motomichi Kono

    发明人： Masaji Kasai ,  Kunikatsu Shirahata ,  Motomichi Kono

    IPC分类号： A61K31/40 ,  A61P31/04 ,  C07D487/14 ,  C07D487/04

    CPC分类号： C07D487/14

    摘要： Mitomycin compounds of the general formula (I): ##STR1## wherein X is selected from an alkoxy group having 1 to 4 carbon atoms and amino group; and Z is selected from --OH, --OCONH.sub.2 and --OCO.sub.2 C.sub.6 H.sub.5 groups. The compounds of this formula may be used as starting materials for the preparation of various mitomycin compounds. When X is as hereinbefore defined and Z is --OCONH.sub.2, the compounds exhibit antibacterial activity and are of potential interest as medicaments. Preferred examples of the compounds are 9-Epi-mitomycin B and 9-epi-mitomycin D. The compounds of the formula (I) may be obtained from known mitomycin B or mitomycin D.

    摘要翻译： 通式（I）的丝裂霉素化合物：其中X选自具有1至4个碳原子的烷氧基和氨基; 并且Z选自-OH，-OCONH 2和-OCO 2 C 6 H 5基团。 该配方化合物可用作制备各种丝裂霉素化合物的起始原料。 当X如上所定义且Z为-OCONH 2时，该化合物表现出抗菌活性并且作为药物具有潜在的兴趣。 化合物的优选实例是9-Epi-丝裂霉素B和9-表 - 丝裂霉素D.式（I）化合物可以从已知的丝裂霉素B或丝裂霉素D获得。