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    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use
    1.
    发明公开
    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use 失效
    7-N，8-N-乙酰基丝氨酸8-IMINES，药物组合物和用途

    公开(公告)号：EP0287855A3

    公开(公告)日：1990-04-25

    申请号：EP88105055.3

    申请日：1988-03-29

    申请人： KYOWA HAKKO KOGYO CO., LTD.

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

    IPC分类号： C07D487/22 ,  A61K31/495

    CPC分类号： C07D487/22

    摘要： 7-N,8-N-ethylenemitomycin 8-imines represented by the formula
    wherein one of R₁ and R₂ represents carbamoyloxymethyl and another represents hydrogen or both are combined together to form methylene; R₃, R₄, R₅ and R₆ each independently represent hydrogen or C₁₋₄ alkyl, or R₃ and R₄ may be combined together to represent -(CH₂) n -, wherein n is 3 or 4; and Y and Z represent hydrogen or methyl, provided that when R₁ represents carbamoyloxymethyl and Y represents methyl, R₂, R₃, R₄, R₅, R₆ and Z are not hydrogen simultaneously, has an excellent antitumor activity.

    摘要翻译： 由式表示的7-N，8-N-亚乙基霉素8-亚胺，其中R 1和R 2之一表示氨基甲酰氧基甲基，另一个表示氢或两者结合在一起形成亚甲基; R 3，R 4，R 5和R 6各自独立地表示氢或C 1-4烷基，或者R 3和R 4可以组合在一起表示 - （CH 2）n - ，其中n为3或4; 并且Y和Z表示氢或甲基，条件是当R 1表示氨基甲酰氧基甲基且Y表示甲基时，R 2，R 3，R 4，R 5，R 6和Z不同时为氢，具有优异的抗肿瘤活性。

    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition
    3.
    发明公开
    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition 失效
    7-N-氨基亚甲基螺旋霉素，Verfahren zu ihrer Herstellung und Antitumorzubereitung。

    公开(公告)号：EP0191375A2

    公开(公告)日：1986-08-20

    申请号：EP86101214.4

    申请日：1986-01-30

    申请人： KYOWA HAKKO KOGYO CO., LTD.

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

    IPC分类号： C07D487/14 ,  A61K31/40

    CPC分类号： C07D487/14

    摘要： Mitomycin derivatives represented by the formula (I):

    wherein R 1 and R 2 may be the same or different, and represent a hydrogen atom or a lower alkyl group: R 3 and R 4 mean that when R 3 is a hydrogen atom, R 4 represents -CH 2 0CONH 2 or

    (wherein R 1 and R 2 have the same significances as defined above), or R 3 and R 4 are combined to form =CH 2 ; Y and Z may be the same or different, and represent a hydrogen atom for a methyl group; represents a- or β-bond, provided that
    Y represents a hydrogen atom when R 4 takes β-conflguration, have an excellent antitumor 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R4取β构型时，Y表示氢原子，具有优异的抗肿瘤活性。

    New mitomycins and processes for production thereof
    4.
    发明公开
    New mitomycins and processes for production thereof 失效
    丝裂霉素和Verfahren zu ihrer Herstellung。

    公开(公告)号：EP0008021A1

    公开(公告)日：1980-02-20

    申请号：EP79102497.9

    申请日：1979-07-17

    申请人： KYOWA HAKKO KOGYO CO., LTD

    发明人： Kasai, Masaji ,  Kono, Motomichi ,  Shirahata, Kunikatsu ,  Urakawa, Chikahiro ,  Tsuchiya, Haruko ,  Nakano, Kinichi ,  Takahashi, Itaru ,  Mineura, Kazuyuki

    IPC分类号： C07D487/14 ,  C12P17/18

    CPC分类号： C07D487/14 ,  A01N43/90 ,  C12P17/182 ,  C12R1/465

    摘要： New mitomycins and processes for production thereof.
    Mytomycin represented by general formula:
    Wherein X is amino, substituted amino, hydroxyl or alkoxy; Y is hydrogen, methyl, -COR' wherein R' is hydrogen, alkyl, substituted alkyl, aryl or substituted aryl, or -CH 2 CH 2 Z wherein Z is alkyloxycarbonyl, acyl or cyano; R A is hydrogen and R B is -CH 2 OH or -CH 2 OSO 2 R 2 wherein R 2 is alkyl or aryl, or R A and R B combine to form = CH 2 ; and Rc is hydrogen or alkyl. In spite of the above definition, when R A is hydrogen and R B is -CH 2 OH, Y is -CH 2 CH 2 Z and when R A is hydrogen and R B is -CH 2 OSO 2 R 2 , Y is hydrogen or -CH 2 CH 2 Z, and processes for production thereof.
    The compounds are useful for sterilization of equipment, as washing agent with detergent or as medicament.

    摘要翻译： 新的丝裂霉素及其生产方法。 由通式表示的霉菌素：其中X为氨基，取代氨基，羟基或烷氧基; Y是氢，甲基，-COR 1，其中R 1是氢，烷基，取代的烷基，芳基或取代的芳基或-CH 2 CH 2 Z，其中Z是烷氧基羰基，酰基或氰基; RA是氢，RB是-CH 2 OH或-CH 2 OSO 2 R 2，其中R 2是烷基或芳基，或RA和RB结合形成= CH 2; 和RC是氢或烷基。 尽管上述定义，当RA为氢且RB为-CH2OH时，Y为-CH2CH2Z，当RA为氢，RB为-CH2OSO2R2时，Y为氢或-CH2CH2Z，其制备方法为。 该化合物可用于灭菌设备，作为洗涤剂与洗涤剂或作为药物。

    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use
    5.
    发明公开
    7-n,8-n-ethylenemitomycin 8-imines, pharmaceutical compositions and use 失效
    7-N，8-N-乙基美丝霉素-8-亚胺，药物Zubereitungen和Verwendung。

    公开(公告)号：EP0287855A2

    公开(公告)日：1988-10-26

    申请号：EP88105055.3

    申请日：1988-03-29

    申请人： KYOWA HAKKO KOGYO CO., LTD.

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

    IPC分类号： C07D487/22 ,  A61K31/495

    CPC分类号： C07D487/22

    摘要： 7-N,8-N-ethylenemitomycin 8-imines represented by the formula
    wherein one of R₁ and R₂ represents carbamoyloxymethyl and another represents hydrogen or both are combined together to form methylene; R₃, R₄, R₅ and R₆ each independently represent hydrogen or C₁₋₄ alkyl, or R₃ and R₄ may be combined together to represent -(CH₂) n -, wherein n is 3 or 4; and Y and Z represent hydrogen or methyl, provided that when R₁ represents carbamoyloxymethyl and Y represents methyl, R₂, R₃, R₄, R₅, R₆ and Z are not hydrogen simultaneously, has an excellent antitumor activity.

    摘要翻译： 由式表示的7-N，8-N-亚乙基霉素8-亚胺，其中R 1和R 2之一表示氨基甲酰氧基甲基，另一个表示氢或两者结合在一起形成亚甲基; R 3，R 4，R 5和R 6各自独立地表示氢或C 1-4烷基，或者R 3和R 4可以组合在一起表示 - （CH 2）n - ，其中n为3或4; 并且Y和Z表示氢或甲基，条件是当R 1表示氨基甲酰氧基甲基且Y表示甲基时，R 2，R 3，R 4，R 5，R 6和Z不同时为氢，具有优异的抗肿瘤活性。

    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition
    6.
    发明公开
    7-n-aminomethylenemitomycin derivatives, process for production thereof and anti-tumor composition 失效
    7-N-氨基联苯胺衍生物，其生产方法和抗肿瘤组合物

    公开(公告)号：EP0191375A3

    公开(公告)日：1987-08-19

    申请号：EP86101214

    申请日：1986-01-30

    申请人： KYOWA HAKKO KOGYO CO., LTD.

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

    IPC分类号： C07D487/14 ,  A61K31/40 ,  C07D209/00 ,  C07D203/00

    CPC分类号： C07D487/14

    摘要： Mitomycin derivatives represented by the formula (I):

    wherein R 1 and R 2 may be the same or different, and represent a hydrogen atom or a lower alkyl group: R 3 and R 4 mean that when R 3 is a hydrogen atom, R 4 represents -CH 2 0CONH 2 or

    (wherein R 1 and R 2 have the same significances as defined above), or R 3 and R 4 are combined to form =CH 2 ; Y and Z may be the same or different, and represent a hydrogen atom for a methyl group; represents a- or β-bond, provided that Y represents a hydrogen atom when R 4 takes β-conflguration, have an excellent antitumor 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R4取β构型时，Y表示氢原子，具有优异的抗肿瘤活性。

    Mitomycin analogues
    10.
    发明公开
    Mitomycin analogues 失效
    丝裂霉素类比。

    公开(公告)号：EP0116208A1

    公开(公告)日：1984-08-22

    申请号：EP83307423.0

    申请日：1983-12-06

    申请人： KYOWA HAKKO KOGYO CO., LTD.

    发明人： Kono, Motomichi ,  Saito, Yutaka ,  Goto, Jyoji ,  Shirahata, Kunikatsu ,  Morimoto, Makoto ,  Ashizawa, Tadashi

    IPC分类号： C07D487/14 ,  A61K31/40 ,  A61K31/44

    CPC分类号： C07D487/14

    摘要： Compounds of the general formula:
    {wherein X represents a
    group [in which R 3 represents a cycloalkyl or straight chain or branched alkyl group having up to 7 carbon atoms, said alkyl or cycloalkyl group optionally carrying 1 to 3 amino groups and/or 1 to 3 hydroxyl groups; a -(CH 2 ) n CO 2 R 4 group (in which n is the integer 1, 2 or 3, and R 4 represents a methyl or ethyl group); a pyridyl group; or a group of the formula:
    and R, and R 2 which may be the same or different, each represents a hydrogen atom or a methyl group, and indicates a or β bonding] possess good antibacterial and anti-tumor activity.
    The compounds of formula I may be prepared for example by reaction of mitomycin A, B, F or J with the appropriate amine.

    摘要翻译： 通式的化合物：其中X表示基[其中R 3表示具有至多7个碳原子的环烷基或直链或支链烷基，所述烷基或环烷基任选地含有1-3个氨基 基团和/或1至3个羟基; （CH 2）n CO 2 R 4基团（其中n为整数1,2或3，R 4表示甲基或乙基）; 吡啶基; 或下式的基团：可以相同或不同的R 1和R 2各自表示氢原子或甲基，表示α或β键]具有良好的抗菌和抗肿瘤活性。 式I化合物可以例如通过丝裂霉素A，B，F或J与适当的胺反应来制备。