N,n-bis(sulfonyl)hydrazines useful as antineoplastic agents
    1.
    发明授权
    N,n-bis(sulfonyl)hydrazines useful as antineoplastic agents 失效
    N,正 - 双(磺酰基)肼,可用作抗肿瘤剂

    公开(公告)号:US6040338A

    公开(公告)日:2000-03-21

    申请号:US963182

    申请日:1997-11-03

    CPC分类号: C07F9/12 C07C311/61 C07F9/091

    摘要: The present invention relates to a compound of the formula wherein R.sup.1 and R.sup.2 are selected from lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms; R.sup.3 is a substituted or unsubstituted lower alkyl group having 1-6 carbons; and R.sup.4 is selected from substituted or unsubstituted lower alkyl groups having 1-6 carbon atoms, substituted or unsubstituted aryl groups, and unsaturated alkyl groups having 1-6 carbon atoms. The present invention also relates to a pharmaceutical composition comprising the above compound, as well as a method of treating tumor cells with the compound.

    摘要翻译: 本发明涉及下式化合物:其中R1和R2选自具有1-6个碳原子的低级烷基,取代或未取代的芳基和具有1-6个碳原子的不饱和烷基; R3是具有1-6个碳原子的取代或未取代的低级烷基; 并且R 4选自具有1-6个碳原子的取代或未取代的低级烷基,取代或未取代的芳基和具有1-6个碳原子的不饱和烷基。 本发明还涉及包含上述化合物的药物组合物,以及用该化合物治疗肿瘤细胞的方法。

    Antitumor 2-aminocarbonyl-1,
2-bis(methylsulfonyl)-1-(substituted)hydrazines
    3.
    发明授权
    Antitumor 2-aminocarbonyl-1, 2-bis(methylsulfonyl)-1-(substituted)hydrazines 失效
    抗肿瘤剂2-氨基羰基-1,2-双(甲基磺酰基)-1-(取代)肼

    公开(公告)号:US5637619A

    公开(公告)日:1997-06-10

    申请号:US497931

    申请日:1995-07-05

    CPC分类号: C07C311/55

    摘要: 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.

    摘要翻译: 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,及其用于治疗 恶性肿瘤。 这些药剂在治疗动物和人类癌症中尤其有用。 该类中特别用于治疗肿瘤的两种优选的药剂是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-甲基氨基羰基肼。 这些试剂的特征如下:它们不能通过为灭活CNU而提出的脱硝机制灭活; 它们不能通过为CNU提出的机制产生羟乙基化物种; 它们能够进行氯乙基化或甲基化和氨基甲酰化。

    Sulfonylhydrazines and their use as antineoplastic agents and as
antitrypanosomal agents
    5.
    发明授权
    Sulfonylhydrazines and their use as antineoplastic agents and as antitrypanosomal agents 失效
    磺酰肼及其作为抗肿瘤药物和抗抗虫剂的用途

    公开(公告)号:US5214068A

    公开(公告)日:1993-05-25

    申请号:US851384

    申请日:1992-03-12

    IPC分类号: C07C311/49

    CPC分类号: C07C311/49

    摘要: Sulfonylhydrazines of the formula RSO.sub.2 N(CH.sub.2 CH.sub.2 X)N(SO.sub.2 CH.sub.3).sub.2, wherein R is an alkyl or an aryl and X is a halogen or OSO.sub.2 Y, wherein Y is an alkyl or an aryl. Such sulfonylhydrazines are useful in treating cancer.Methylating agents of the formula(a) R'SO.sub.2 N(CH.sub.3)N(SO.sub.2 CH.sub.3).sub.2, wherein R' is an alkyl or an aryl and(b) R"SO.sub.2 N(CH.sub.3)N(CH.sub.3)SO.sub.2 R", wherein R" is an alkyl or an aryl.Such methylating agents are useful as antitrypanosomal and anticancer agents.

    摘要翻译: 式RSO 2 N(CH 2 CH 2 X)N(SO 2 CH 3)2的磺酰肼,其中R是烷基或芳基,X是卤素或OSO 2 Y,其中Y是烷基或芳基。 这样的磺酰肼可用于治疗癌症。 式(a)R'SO2N(CH3)N(SO2CH3)2的甲基化剂,其中R'是烷基或芳基,和(b)R“SO2N(CH3)N(CH3)SO2R”,其中R “是烷基或芳基。 这种甲基化剂可用作抗睾丸激素和抗癌剂。

    N,N'-bis(sulfonyl)hydrazines having antineoplastic activity
    8.
    发明授权
    N,N'-bis(sulfonyl)hydrazines having antineoplastic activity 失效
    N,N'-双(磺酰基)肼具有抗肿瘤活性

    公开(公告)号:US4892887A

    公开(公告)日:1990-01-09

    申请号:US230687

    申请日:1988-08-09

    IPC分类号: A61K31/15 C07C311/49

    CPC分类号: A61K31/15 C07C311/49

    摘要: Compounds of the formula ##STR1## where R is methyl or 2-chloroethyl, and R.sup.1 and R.sup.2 are each an aromatic hydrocarbon, ring substituted aromatic hydrocarbon moiety, or an alkyl moiety. The compounds have been found to be alkylating agents having antineoplastic activity.

    摘要翻译: 其中R是甲基或2-氯乙基,R 1和R 2各自是芳族烃,环取代的芳族烃部分或烷基部分的式“IMAGE”的化合物。 已经发现这些化合物是具有抗肿瘤活性的烷化剂。

    Novel 1-alkyl-1-arenesulfonyl-2-alkoxycarbonylsulfenylhydrazines having
antineoplastic activity
    9.
    发明授权
    Novel 1-alkyl-1-arenesulfonyl-2-alkoxycarbonylsulfenylhydrazines having antineoplastic activity 失效
    具有抗肿瘤活性的新型1-烷基-1-芳烃磺酰基-2-烷氧基羰基亚磺酰肼

    公开(公告)号:US4849563A

    公开(公告)日:1989-07-18

    申请号:US142354

    申请日:1987-12-28

    IPC分类号: C07C329/02

    CPC分类号: C07C329/02

    摘要: Compounds of the formula: ##STR1## wherein R.sub.1 s an alkyl of 1-6 carbon atoms, benzyl, phenyl, or phenyl substituted by halogen, alkoxy of 1 to 4 carbon atoms, alkyl of 1 to 4 carbon atoms, amino, or carbonyl substituents, or --RN(R').sub.2 wherein R and R' are each independently an alkyl of 1 to 4 carbon atoms; R.sub.2 is an aromatic substituent selected from the group consisting of phenyl, benzyl, and naphthyl, and A is an aromatic substitution selected from the group consisting of hydrogen, alkyl of 1-4 carbon atoms, alkoxy of 1-4 carbon atoms, halogen, --NO.sub.2, --NH.sub.2, --COOH, and --NHCOCH.sub.3. The compounds have been found to be alkylating agents having antineoplastic activity for use in inhibiting the growth of tumors.

    摘要翻译: 下式的化合物:其中R 1为1-6个碳原子的烷基,苄基,苯基或被卤素取代的苯基,1至4个碳原子的烷氧基,1至4个碳原子的烷基,氨基或羰基 取代基或-RN(R')2,其中R和R'各自独立地为1至4个碳原子的烷基; R2是选自苯基,苄基和萘基的芳香族取代基,A是选自氢,1-4个碳原子的烷基,1-4个碳原子的烷氧基,卤素, -NO 2,-NH 2,-COOH和-NHCOCH 3。 已经发现这些化合物是具有抗肿瘤活性的烷基化剂,用于抑制肿瘤的生长。