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    • 4. 发明授权
    • 항암성2-아미노카르보닐-1,2-비스(메틸술포닐)-1-(치환)히드라진
    • 항암성2-아미노카르보닐-1,2-비스(메틸술포닐)-1-(치환)히드라진
    • KR100372632B1
    • 2003-05-12
    • KR1019980700031
    • 1996-07-02
    • 예일 유니버시티
    • 사토렐리,알란씨.샤암,크리슈나무르티펜케스,필립지.
    • A61K31/15
    • C07C311/55
    • The present invention relates to novel 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-(2-chloroethyl)hydrazines and 2-aminocarbonyl-1,2-bis(methylsulfonyl)-1-methylhydrazines, and their use to treat malignant tumors. The agents are especially useful in the treatment of animal and human cancers. Two preferred agents in this class, especially for use in the treatment of tumors are 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-(2-chloroethyl)aminocarbonylhydrazine and 1,2-bis(methylsulfonyl)-1-(2-chloroethyl)-2-methylaminocarbonylhydrazine. These agents are characterized by the following: they are incapable of undergoing inactivation by the denitrosation mechanism proposed for the inactivation of the CNUs; they are incapable of generating a hydroxyethylating species by the mechanism proposed for the CNUs; and they are capable of chloroethylation or methylation and carbamoylation.
    • 本发明涉及新的2-氨基羰基-1,2-双(甲基磺酰基)-1-(2-氯乙基)肼和2-氨基羰基-1,2-双(甲基磺酰基)-1-甲基肼,以及它们用于治疗 恶性肿瘤。 这些试剂在动物和人类癌症的治疗中特别有用。 特别用于治疗肿瘤的两类优选药物是1,2-双(甲基磺酰基)-1-(2-氯乙基)-2-(2-氯乙基)氨基羰基肼和1,2-双(甲基磺酰基) -1-(2-氯乙基)-2- methylaminocarbonylhydrazine。 这些药剂的特征如下:它们不能通过用于CNU灭活的脱氮机制而失活; 它们不能通过为CNU提供的机制产生羟乙基化物质; 它们能够氯乙基化或甲基化和氨基甲酰化。