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    Process for producing 1-[2-(2,4-dichlorophenyl)-pentyl]-1H-1,2,4-triazole
    3.
    发明授权
    Process for producing 1-[2-(2,4-dichlorophenyl)-pentyl]-1H-1,2,4-triazole 失效
    1- [2-（2,4-二氯苯基） - 戊基] -1H-1,2,4-三唑的制备方法

    公开(公告)号：US4556717A

    公开(公告)日：1985-12-03

    申请号：US505019

    申请日：1983-06-16

    申请人： Hansjurg Wetter ,  Peter Baumeister ,  Paul Radimerski ,  Pierre Martin

    发明人： Hansjurg Wetter ,  Peter Baumeister ,  Paul Radimerski ,  Pierre Martin

    IPC分类号： C07B61/00 ,  C07C67/00 ,  C07C239/00 ,  C07C241/00 ,  C07C243/18 ,  C07C243/28 ,  C07C243/32 ,  C07C243/38 ,  C07C251/80 ,  C07C275/68 ,  C07C281/04 ,  C07C281/06 ,  C07C281/08 ,  C07D249/08 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07C243/00 ,  C07C251/72 ,  C07D233/56 ,  C07D249/08

    摘要： 1-[2-(2,4-Dichlorophenyl)-pentyl]-1H-1,2,4-triazole can be produced, in a novel, simple, economical and isomer-free form, by reacting 2-(2,4-dichlorophenyl)-valeronitrile, in the presence of hydrogen, an acid and a hydrogenation catalyst, with a compound H.sub.2 N--NH--R to a compound of the formula ##STR1## hydrogenating the compound (III) catalytically to a compound ##STR2## hydrolysing compounds (IV) wherein R is not hydrogen, and converting the compounds (IV) wherein R=H, or salts thereof, with formamide and/or [3-(dimethylamino)-2-azaprop-2-en-1-ylidene]-dimethylammonium chloride, into 1-[2-(2,4-dichlorophenyl)-pentyl]-1H-1,2,4-triazole, or converting compounds (IV) wherein R=--COR', with aqueous formic acid, into the corresponding N,N'-bisformyl derivatives, and reacting these with formamide, optionally in the presence of NH.sub.3, to 1-[2-(2,4-dichlorophenyl)-pentyl]-1H-1,2,4-triazole. R in the formulae is hydrogen, --CHO, --COR', --COOR' or --CONH.sub.2, and R' is C.sub.1 -C.sub.4 -alkyl, benzyl or phenyl.1-[2-(2,4-Dichlorophenyl)-pentyl]-1H-1,2,4-triazole exhibits fungicidal activity, and can be used to control phytopathogenic fungi.

    摘要翻译： 1- [2-（2,4-二氯苯基） - 戊基] -1H-1,2,4-三唑可以以新颖简单，经济和异构体的形式通过2-（2,4 （III）的化合物与化合物H2N-NH-R反应，使化合物（III）催化反应到化合物（III） （IV）水解化合物（Ⅳ），其中R不是氢，并将其中R = H的化合物（Ⅳ）或其盐与甲酰胺和/或[3-（二甲基氨基）-2-氮杂丙-2-酮 烯-1-基] - 二甲基氯化铵转化成1- [2-（2,4-二氯苯基） - 戊基] -1H-1,2,4-三唑或转化其中R = -COR'的化合物（Ⅳ） 与甲酸水溶液加入到相应的N，N'-双甲酰基衍生物中，并将其与甲酰胺（任选在NH 3存在下）与1- [2-（2,4-二氯苯基） - 戊基] -1H-1反应， 2,4-三唑。 式中的R是氢，-CHO，-COR'，-COOR'或-CONH 2，R'是C 1 -C 4烷基，苄基或苯基。 1- [2-（2,4-二氯苯基） - 戊基] -1H-1,2,4-三唑具有杀真菌活性，可用于控制植物病原真菌。

    2-Chloroethyl urea derivatives
    6.
    发明授权
    2-Chloroethyl urea derivatives 失效
    2-氯乙基脲衍生物

    公开(公告)号：US4384140A

    公开(公告)日：1983-05-17

    申请号：US348724

    申请日：1982-02-16

    申请人： Peter Bregnedal ,  Jorn L. M. Buus

    发明人： Peter Bregnedal ,  Jorn L. M. Buus

    IPC分类号： A61K31/17 ,  A61K31/275 ,  A61K31/40 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C275/68 ,  C07C127/17

    CPC分类号： C07C275/68

    摘要： The present invention relates to novel aminoalkyl substituted nitrosourea derivatives as well as their acid addition salts with pharmaceutically acceptable acids showing pronounced antineoplastic effectiveness in animal experiments.The novel compounds of the present invention may be represented by the following formula: ##STR1## wherein X and Y are the same or different, and are selected from the group consisting of a phenyl group and a cyclohexyl group, said phenyl and cyclohexyl groups being optionally substituted with one or two substituents selected from a halogen atom, a lower alkyl group having from one to four carbon atoms inclusive, a trifluore methyl group, a cyano group, a phenyl group, a cyclohexyl group and a lower alkyloxy group having from one to four carbon atoms inclusive."Alkylene" is an alkylene group, branched or unbranched, having from one to four carbon atoms inclusive, and R.sup.1 and R.sup.2 are the same or different, and are each selected from the group consisting of lower alkyl groups having from one to four carbon atoms inclusive, and benzyl groups, or they form together with the nitrogen atom a saturated five- or six-membered heterocyclic ring, such as a pyrrolidine, piperidine, morfoline, thiomorfoline, or N-lower-alkyl-piperazine ring, said heterocyclic ring being optionally substituted with lower alkyl groups having from one to four carbon atoms inclusive, as well as pharmaceutically acceptable acid addition salts thereof.

    摘要翻译： 本发明涉及新的氨基烷基取代的亚硝基脲衍生物及其与药学上可接受的酸的酸加成盐，其在动物实验中显示出明显的抗肿瘤效果。 本发明的新化合物可以由下式表示：其中X和Y相同或不同，并且选自苯基和环己基，所述苯基和环己基 任选被一个或两个选自卤素原子，含有1-4个碳原子的低级烷基，三氟甲基，氰基，苯基，环己基和低级烷氧基的取代基取代， 一至四个碳原子。 “亚烷基”是具有1〜4个碳原子的支链或非支链的亚烷基，R 1和R 2相同或不同，各自选自具有1〜4个碳原子的低级烷基 或者与氮原子一起形成饱和的五元或六元杂环，例如吡咯烷，哌啶，舍弗林，硫代还原或N-低级烷基哌嗪环，所述杂环为 任选被具有1至4个碳原子的低级烷基取代，以及其药学上可接受的酸加成盐。

    Nitrosourea substituted phosphonates and pharmaceutical use
    8.
    发明授权
    Nitrosourea substituted phosphonates and pharmaceutical use 失效
    硝基脲取代膦酸盐和药物用途

    公开(公告)号：US4567169A

    公开(公告)日：1986-01-28

    申请号：US547881

    申请日：1983-11-02

    申请人： Gilbert Lavielle ,  Claude Cudennec

    发明人： Gilbert Lavielle ,  Claude Cudennec

    IPC分类号： A61K31/66 ,  A61K31/67 ,  A61K31/675 ,  A61P31/04 ,  A61P35/00 ,  C07C275/68 ,  C07F9/38 ,  C07F9/40 ,  C07F9/572 ,  C07F9/6553 ,  C07F9/6558 ,  C07F9/58

    CPC分类号： C07F9/3808 ,  C07F9/4006

    摘要： New nitrosourea compounds that can be used as medicaments and correspond to the general formula I ##STR1## in which R.sub.1 is hydrogen, C.sub.1 -C.sub.6 alkyl or phenyl,R.sub.2 is hydrogen, C.sub.1 -C.sub.6 alkyl, thienyl, or phenyl which may carry substituents,R.sub.3 is hydrogen, C.sub.1 -C.sub.6 alkyl, or benzyl which may carry substituents, orR.sub.2 and R.sub.3 together represent --(CH.sub.2).sub.m --, m being 3 or 4.Pharmaceutical compositions; therapeutic administration especially for the treatment of tumours.

    摘要翻译： 可用作药物并且对应于通式I（I）的新的亚硝基脲化合物，其中R 1是氢，C 1 -C 6烷基或苯基，R 2是氢，C 1 -C 6烷基，噻吩基或苯基， 携带取代基，R 3是氢，可以带有取代基的C 1 -C 6烷基或苄基，或者R 2和R 3一起表示 - （CH 2）m - ，m为3或4。 特别是用于治疗肿瘤的治疗性给药。

    Bis(nitrosoureido)-polyol derivatives
    10.
    发明授权
    Bis(nitrosoureido)-polyol derivatives 失效
    双（亚硝基脲基） - 多元醇衍生物

    公开(公告)号：US4237273A

    公开(公告)日：1980-12-02

    申请号：US925822

    申请日：1978-07-17

    申请人： Tibor Horvath ,  Endre Csanyi ,  Sandor Eckhardt ,  Emilia Kiraly nee Vida

    发明人： Tibor Horvath ,  Endre Csanyi ,  Sandor Eckhardt ,  Emilia Kiraly nee Vida

    IPC分类号： A61K31/17 ,  A61P35/00 ,  C07C67/00 ,  C07C239/00 ,  C07C275/68 ,  C07D317/28 ,  A61K31/70 ,  C07H5/06

    CPC分类号： C07C275/68 ,  C07D317/28

    摘要： The invention relates to bis(nitrosoureido)-polyol derivatives of general formula IB.sub.1 --A--B.sub.2 (I)whereinA stands for an open chain polyol comprising 4 to 6 carbon atoms or a six-membered cyclic polyol, andB.sub.1 and B.sub.2 being attached to two different carbon atoms of the chain A, are identical or different, and stand for a group of general formula II ##STR1## wherein X stands for a halogen atom andY and Z stand for a hydrogen atom or a nitroso group, with the restriction, that in B.sub.1 and B.sub.2 Y and Z must be different.The above compounds possess valuable cytostatic activity.

    摘要翻译： 本发明涉及通式ⅠB1-A-B2（Ⅰ）的双（亚硝基脲基）多元醇衍生物，其中A代表含有4-6个碳原子的开链多元醇或六元环状多元醇，而B1和B2是 链A的两个不同碳原子相同或不同，代表通式II（II）的基团，其中X代表卤原子，Y和Z代表氢原子或亚硝基 集团有限，B1和B2中的Y和Z必须不同。 上述化合物具有有价值的细胞生长抑制活性。