会员体验
专利管家(专利管理)
工作空间(专利管理)
风险监控(情报监控)
数据分析(专利分析)
侵权分析(诉讼无效)
联系我们
交流群
官方交流:
QQ群: 891211   
微信请扫码    >>>
现在联系顾问~
热词
    • 9. 发明授权
    • Aminopropylaminobleomycin derivatives and process for preparation thereof
    • 氨丙基氨基甜菜碱素衍生物及其制备方法
    • US4568490A
    • 1986-02-04
    • US743738
    • 1985-06-12
    • Hamao UmezawaAkio FujiiYasuhiko MuraokaTokuji NakataniTakeyo FukuokaKatsutoshi Takahashi
    • Hamao UmezawaAkio FujiiYasuhiko MuraokaTokuji NakataniTakeyo FukuokaKatsutoshi Takahashi
    • C07H15/26A61K31/70A61K31/7028A61P35/00C07K9/00
    • C07K9/003Y10S930/19Y10S930/27
    • 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.
    • 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。