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    Pyrazoloacridone derivatives
    6.
    发明授权
    Pyrazoloacridone derivatives 失效
    吡咯烷酮衍生物

    公开(公告)号：US5220026A

    公开(公告)日：1993-06-15

    申请号：US793522

    申请日：1991-11-18

    申请人： Yukiteru Mimura ,  Yasushi Shida ,  Masaji Kasai ,  Tadashi Ashizawa ,  Katsushige Gomi

    发明人： Yukiteru Mimura ,  Yasushi Shida ,  Masaji Kasai ,  Tadashi Ashizawa ,  Katsushige Gomi

    IPC分类号： A61K31/47 ,  A61P35/00 ,  C07D471/06

    CPC分类号： C07D471/06

    摘要： Disclosed is pyrazoloacridone derivatives represented by formula (I): ##STR1## wherein: each of R.sup.1a, R.sup.1b, R.sup.1c and R.sup.1d independently represents hydrogen, lower alkyl, --(CH.sub.2).sub.p --Xwherein p represents an integer of 1 to 6, and X represents hydroxy, lower alkoxy or --NR.sup.2a R.sup.2bwherein each of R.sup.2a and R.sup.2b independently represents hydrogen, lower alkyl, or --(CH.sub.2).sub.m --Ywherein m represents an integer of 1 to 6, and Y represents hydroxy, lower alkoxy or --NR.sup.3a R.sup.3bwherein each of R.sup.3a and R.sup.3b independently represents hydrogen or lower alkylor --CH[(CH.sub.2).sub.n OH].sub.2wherein n represents an integer of 1 to 5; or a pharmaceutically acceptable salt thereof.

    DC 107 derivatives and treatment methods
    8.
    发明授权
    DC 107 derivatives and treatment methods 失效
    DC 107衍生物和处理方法

    公开(公告)号：US5733924A

    公开(公告)日：1998-03-31

    申请号：US776938

    申请日：1997-04-17

    申请人： Yutaka Kanda ,  Yutaka Saitoh ,  Hiromitsu Saito ,  Tadashi Ashizawa ,  Kazuyo Sugiyama ,  Katsushige Gomi ,  Shingo Kakita ,  Yuichi Takahashi ,  Chikara Murakata

    发明人： Yutaka Kanda ,  Yutaka Saitoh ,  Hiromitsu Saito ,  Tadashi Ashizawa ,  Kazuyo Sugiyama ,  Katsushige Gomi ,  Shingo Kakita ,  Yuichi Takahashi ,  Chikara Murakata

    IPC分类号： C07D513/08 ,  A61K37/00

    CPC分类号： C07D513/08

    摘要： DC107 derivatives represented by the formula (I): ##STR1## or pharmacologically acceptable slats thereof, �wherein R.sup.1 is hydrogen, lower alkoxyalkyl, aralkyloxyalkyl, lower alkoxyalkoxyalkyl, lower alkoxyalkoxyalkoxyalkyl, aralkyl, tetrahydropyranyl, COR.sup.4 or the like; R.sup.2 represents hydrogen or COR.sup.5 ; R.sup.3 represents lower alkyl, lower alkenyl, aralkyl which may be substituted with substituted or unsubstituted aryl, lower alkoxyalkyl, aralkyloxyalkyl, substituted or unsubstituted aryloxyalkyl, lower alkoxycarbonylalkyl, lower alkanoyloxyalkyl, alicyclic alkanoyloxyalkyl or the like, or bonds to Y to represent a single bond; Y bonds to R.sup.3 to represent a single bond, or bonds to Z to represent a single bond; Z represents hydrogen or bonds to Y to represent a single bond; W represents oxygen or NR.sup.6, with the proviso that the compound wherein R.sup.1, R.sup.2 and Z each represents hydrogen, R.sup.3 bonds to Y to represent a single bond, and W represents oxygen (DC107) is excluded.!

    摘要翻译： PCT No.PCT / JP96 / 01646 Sec。 371日期1997年04月17日 102（e）1997年4月17日PCT PCT 1996年6月14日PCT公布。 出版物WO97 / 00260 PCT 日本1997年3月1日由式（I）代表的DC107衍生物：其中R1为氢，低级烷氧基烷基，芳烷氧基烷基，低级烷氧基烷氧基烷基，低级烷氧基烷氧基烷氧基烷基，芳烷基，四氢吡喃基，COR4或 类似; R2表示氢或COR5; R3代表低级烷基，低级烯基，可被取代或未取代的芳基取代的芳烷基，低级烷氧基烷基，芳烷氧基烷基，取代或未取代的芳氧基烷基，低级烷氧基羰基烷基，低级烷酰氧基烷基，脂环族烷酰氧基烷基等，或与Y键合以表示单键 ; Y键合到R3表示单键，或键合到Z表示单键; Z表示氢或与Y键合以表示单键; W表示氧或NR 6，条件是其中R1，R2和Z各自表示氢，R3与Y键合以表示单键，W表示氧（DC107）的化合物。

    New mitomycin derivatives, preparation thereof and pharmaceutical compositions containing them
    10.
    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。