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    • 10. 发明授权
    • Nitrosourea derivative
    • 亚硝基脲衍生物
    • US4003901A
    • 1977-01-18
    • US527017
    • 1974-11-25
    • Hideo NakaoMasao ArakawaMasami Fukushima
    • Hideo NakaoMasao ArakawaMasami Fukushima
    • C07D211/56C07D235/08C07D239/42
    • C07D239/42C07D211/56C07D235/08Y10S514/908
    • Nitrosourea derivatives represented by the formula ##STR1## wherein A represents a group of the formula B--Y-- in whichB is an unsaturated 5- or 6-membered heterocyclic group which has the as hetero atom at least one nitrogen atom, an unsaturated 9-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring or an unsaturated 10-membered heterocyclic group which has as the hetero atom at least one nitrogen atom and a bicyclic fused ring, the heterocyclic groups optionally having alkyl, alkoxy, hydroxyl, amino, hydroxyalkyl or halogen as ring substituent andY represents a group of the formula --(CH.sub.2).sub.m -- in which m is an integer of 1 or 2, the group optionally having alkyl as a substituent;A group of the formula ##STR2## in which R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.5, R.sup.6, R.sup.7, R.sup.8 and R.sup.9 may be the same or different and each represents a hydrogen atom or an alkyl group; or a group of the formula ##STR3## in which R's may be the same or different and each represents a halogen atom or an alkyl group, n is an integer of 0 to 3 inclusive and Z is an ethylene group which may be substituted with alkyl; andX represents a halogen atom and acid addition salts thereof. The Compounds of the present invention are prepared from the corresponding 2-halogeno-ethylurea derivatives by means of conventional nitrosation procedures and useful as an antileukemic drug for various types of leukemia.
    • 由式(I)表示的亚硝基脲衍生物,其中A表示式BY-的基团,其中B是具有至少一个氮原子的杂原子的不饱和5-或6-元杂环基,不饱和的 具有至少一个氮原子的杂原子的9元杂环基和具有至少一个氮原子和双环稠环的杂原子的双环稠合环或不饱和10元杂环基,任选的杂环基 具有烷基,烷氧基,羟基,氨基,羟烷基或卤素作为环取代基,Y表示式 - (CH 2)m - 的基团,其中m为1或2的整数,该基团任选具有烷基作为取代基; 其中R1,R2,R3,R4,R5,R6,R7,R8和R9可以相同或不同,并且各自表示氢原子或烷基; 或其中R可以相同或不同并且各自表示卤素原子或烷基的式“IMAGE”的基团,n为0〜3的整数,Z为可被烷基取代的亚乙基 ; X表示卤原子及其酸加成盐。 本发明化合物由相应的2-卤代乙基脲衍生物通过常规的亚硝化方法制备,可用作各种白血病的抗白血病药物。