利索-全球专利检索

  1. 登录
  2. 注册

搜索结果

206 条记录 (耗时 0.03 秒)

    Novel 3-(4'-aminobutylamino) propylaminobleomycin derivatives
    92.
    发明授权
    Novel 3-(4'-aminobutylamino) propylaminobleomycin derivatives 失效
    新型3-（4'-氨基丁基氨基）丙基氨基倍半霉素衍生物

    公开(公告)号：US4808703A

    公开(公告)日：1989-02-28

    申请号：US622884

    申请日：1984-06-21

    申请人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    发明人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    IPC分类号： C07H15/26 ,  A61K31/70 ,  A61K31/7028 ,  A61P31/04 ,  A61P35/00 ,  C07K9/00 ,  C07C103/52

    CPC分类号： C07K9/003

    摘要： Disclosed is a 3-(4'-aminobutylamino) propylaminobleomycin having low pulmonary toxicity, which expressed by the following general formula[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.4 --Bwherein [BX] represents a residue remaining after removing a hydroxyl group from the carboxyl group of bleomycinic acid, A represents a group of the formula ##STR1## in which R.sub.1 represents (i) a hydrogen atom, (ii) an alkyl group having 1 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group having 5 to 13 carbon atoms, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms, and benzyloxy group; and R.sub.2 represents a lower alkyl group having 1 to 4 carbon atoms or a benzyl group, B represents a group of the formula ##STR2## in which R.sub.3 and R.sub.4 each represents (i) a hydrogen atom, (ii) an alkyl group having 5 to 10 carbon atoms, or (iii) a methyl which may be substituted by at least one of a phenyl group and a cycloalkyl group, said substituents being each optionally further substituted more than one position by one or more substituents selected from the class consisting of a halogen atom, a lower alkyl group having 1 to 4 carbon atoms, a lower alkoxy group having 1 to 4 carbon atoms and a benzyloxy group, with the proviso that at least one of R.sub.3 and R.sub.4 is a group other than a hydrogen atom, and salt thereof.

    摘要翻译： 公开了具有低肺毒性的3-（4'-氨基丁基氨基）丙基氨基巴豆霉素，其由以下通式[BX] -NH-（CH 2）3 -A-（CH 2）4 -B表示，其中[BX]表示残基 在从博来霉素酸的羧基中除去羟基后残留，A代表式为“IMAGE”的基团，其中R1表示（i）氢原子，（ii）具有1-10个碳原子的烷基或（ iii）可以被苯基和具有5至13个碳原子的环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个选自下列的取代基中的一个或多个取代基取代： 卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基; 并且R 2表示具有1至4个碳原子的低级烷基或苄基，B表示下式的基团：其中R 3和R 4各自表示（i）氢原子，（ii）具有5个 至少10个碳原子，或（iii）可以被苯基和环烷基中的至少一个取代的甲基，所述取代基各自任选地被一个或多个取代基取代，所述取代基选自： 卤素原子，碳原子数1〜4的低级烷基，碳原子数1〜4的低级烷氧基和苄氧基，条件是R3和R4中的至少一个为氢原子以外的基团， 及其盐。

    Aminopropylaminobleomycin derivatives and process for preparation thereof
    99.
    发明授权
    Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
    氨丙基氨基甜菜碱素衍生物及其制备方法

    公开(公告)号：US4568490A

    公开(公告)日：1986-02-04

    申请号：US743738

    申请日：1985-06-12

    申请人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    发明人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    IPC分类号： C07H15/26 ,  A61K31/70 ,  A61K31/7028 ,  A61P35/00 ,  C07K9/00

    CPC分类号： C07K9/003 ,  Y10S930/19 ,  Y10S930/27

    摘要： An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--)CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.

    摘要翻译： 由下式表示的氨基丙基氨基伯合珠霉素或其盐，其在副作用如肺毒性中最小化：[BX] -NH-（CH2）3-A-）CH2）3-B其中[BX]表示酰基 通过从所述酸的羧基除去羟基，其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团，R 2为低级烷基或苄基，R为低级亚烷基，n为0或1; 并且B代表下式的基团：其中（i）R3是氢，R4是（a）被一个或多个卤素原子取代的苄基，条件是当R 1是低级烷基时，苄基被两个卤原子取代，（ （c）由氰基，两个或多个烷氧基或两个或更多个苄氧基取代的苄基，（c）被环烷基或蒽基取代的低级烷基，（d）被一个或多个卤素原子取代的苯基乙基，或（e）二苯基乙基; 或（ii）R 3和R 4均为可被一个或多个（a）苄氧基取代的苄基，（b）环取代的苄氧基，其中环取代基可以是一个或多个卤素原子，低级烷氧基或苄氧基 ，或（c）环烷基甲氧基; 及其制备方法。

    Aminopropylaminobleomycin derivatives and process for preparation thereof
    100.
    发明授权
    Aminopropylaminobleomycin derivatives and process for preparation thereof 失效
    氨丙基氨基甜菜碱素衍生物及其制备方法

    公开(公告)号：US4537880A

    公开(公告)日：1985-08-27

    申请号：US635096

    申请日：1984-07-27

    申请人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    发明人： Hamao Umezawa ,  Akio Fujii ,  Yasuhiko Muraoka ,  Tokuji Nakatani ,  Takeyo Fukuoka ,  Katsutoshi Takahashi

    IPC分类号： C07H15/26 ,  A61K31/70 ,  A61K31/7028 ,  A61P35/00 ,  C07K9/00 ,  A61K37/00 ,  C07C103/52

    CPC分类号： C07K9/003 ,  Y10S930/19 ,  Y10S930/27

    摘要： An aminopropylaminobleomycin represented by the following formula or a salt thereof, which is minimized in side effects such as pulmonary toxicity:[BX]--NH--(CH.sub.2).sub.3 --A--(CH.sub.2).sub.3 --Bwherein[BX] represents the acyl group of bleomycinic acid whose formula differs from that of bleomycin acid by the removal of the hydroxyl group from the carboxyl group of said acid;A represents a group of the general formula ##STR1## wherein R.sub.1 is a lower alkyl or benzyl,R.sub.2 is a lower alkyl or benzyl,R is a lower alkylene, andn is 0 or 1; andB represents a group of the formula ##STR2## wherein (i) R.sub.3 is hydrogen and R.sub.4 is(a) benzyl substituted by one or more halogen atoms, provided that the benzyl is substituted by two halogen atoms when R.sub.1 is lower alkyl,(b) benzyl substituted by cyano, two or more alkoxy groups or two or more benzyloxy groups,(c) lower alkyl substituted by cycloalkyl or anthranyl,(d) phenylethyl substituted by one or more halogen atoms, or(e) diphenylethyl; or(ii) both R.sub.3 and R.sub.4 are benzyl which may be substituted by one or more(a) benzyloxy groups,(b) ring substituted benzyloxy groups in which the ring substituents may be one or more halogen atoms, lower alkoxy groups or benzyloxy groups, or(c) cycloalkylmethoxy groups;and a process for the preparation thereof.

    摘要翻译： 由下式表示的氨丙基氨基伯基霉素或其盐，其在副作用如肺毒性方面最小化：[BX] -NH-（CH2）3-A-（CH2）3-B其中[BX]表示酰基 通过从所述酸的羧基除去羟基，其公式不同于博来霉素酸的博来霉素酸; A表示通式为其中R 1为低级烷基或苄基的基团，R 2为低级烷基或苄基，R为低级亚烷基，n为0或1; 并且B代表下式的基团：其中（i）R3是氢，R4是（a）被一个或多个卤素原子取代的苄基，条件是当R 1是低级烷基时，苄基被两个卤原子取代，（ （c）由氰基，两个或更多个烷氧基或两个或更多个苄氧基取代的苄基，（c）被环烷基或蒽基取代的低级烷基，（d）被一个或多个卤素原子取代的苯基乙基，或（e）二苯基乙基; 或（ii）R 3和R 4均为可被一个或多个（a）苄氧基取代的苄基，（b）环取代的苄氧基，其中环取代基可以是一个或多个卤素原子，低级烷氧基或苄氧基 ，或（c）环烷基甲氧基; 及其制备方法。