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    • 2. 发明授权
    • 5,6,-0-Isoalkylidene ascorbic acid derivatives
    • 5,6,-O-异亚烷基抗坏血酸衍生物
    • US4423236A
    • 1983-12-27
    • US314423
    • 1981-10-23
    • Andrew J. Welebir
    • Andrew J. Welebir
    • C07D307/62C07D407/00
    • C07D307/62C07D407/00
    • Novel condensation products between enediol ketolactones such as 5,6-0-isopropylidene ascorbic acid and 2-chloroethyl isocyanates are shown to have potent antitumor activity probably without the release of alkylating agents in vivo. While the structures of the products are not readily elucidated, activity is found to exceed that of BCNU (bis-(2-chloroethyl)-N-nitrosourea) and parallel that of the toxic and highly effective nitrosourea, MeCCNU (1-(4-trans-methylcyclohexyl)-3-(2-chloroethyl)-3-nitrosourea). Preferred compounds are condensation products of ##STR1## wherein R.sub.2 and R.sub.3 are a lower alkyl group containing 1 to 3 carbon atoms or H andhal--CH.sub.2 --CH.sub.2 --N.dbd.C.dbd.O (B)wherein hal is I, Br or Cl.
    • 烯诺酮酮内酯如5,6-0-异亚丙基抗坏血酸和2-氯乙基异氰酸酯之间的新型缩合产物显示具有很强的抗肿瘤活性,可能没有在体内释放烷化剂。 虽然产物的结构不容易阐明,但发现活性超过BCNU(双 - (2-氯乙基)-N-亚硝基脲)的活性,并且与有毒和高效的亚硝基脲MeClNU(1-(4- 反式 - 甲基环己基)-3-(2-氯乙基)-3-亚硝基脲)。 优选的化合物是下式(A)的缩合产物,其中R 2和R 3是含有1至3个碳原子的低级烷基或H和卤素-CH 2 -CH 2 -N = C = O(B),其中hal为I,Br 或Cl。