Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides
    14.
    发明授权
    Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides 失效
    取代的3-(正 - 杂环)-2,6-二氨基吡啶和 - 氧化物

    公开(公告)号:US4923858A

    公开(公告)日:1990-05-08

    申请号:US352287

    申请日:1989-05-16

    摘要: Compounds of the general formula: ##STR1## wherein the radicals R.sub.1 and R.sub.2 are the same or different and represent hydrogen or C.sub.1 -C.sub.6 -alkyl, the radicals R.sub.3 and R.sub.4 are the same or different and represent hydrogen, C.sub.1 -C.sub.6 -alkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, halogen or C.sub.2 -C.sub.6 -alkanoyl, X is oxygen, sulphur or the group --NR.sub.5 and R.sub.5 is hydrogen, C.sub.1 -C.sub.6 -alkyl, C.sub.2 -C.sub.6 -alkanoyl or benzoyl, m and n in each case may represent the integers 1, 2 or 3 and the phenyl radical A is unsubsituted or is substituted by halogen, nitro, C.sub.1 -C.sub.6 -alkyl, trifluoromethyl, C.sub.3 -C.sub.7 -cycloalkyl, hydroxy, C.sub.1 -C.sub.6 -alkoxy, C.sub.2 -C.sub.6 -alkanoyloxy, amino, C.sub.1 -C.sub.6 -alkylamino, di-C.sub.1 -C.sub.6 -alkylamino, C.sub.2 -C.sub.6 -alkanoylamino, CN, carboxy, C.sub.1 -C.sub.6 -alkoxycarbonyl, phenyl, C.sub.1 -C.sub.6 -alkylphenyl or trifluoromethylphenyl, their pyridine-N-oxides and physiologically acceptable salts thereof, processes for their preparation and medicines containing such compounds as active ingredients.

    摘要翻译: 通式为:其中基团R 1和R 2相同或不同并且表示氢或C 1 -C 6烷基的通式为:其中R 3和R 4相同或不同,表示氢,C 1 -C 6 - 烷基 ,羟基,C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基,卤素或C 2 -C 6 - 烷酰基,X是氧,硫或基团-NR 5和R 5是氢,C 1 -C 6烷基,C 2 -C 6 - 烷酰基或 苯甲酰基,m和n各自可以表示整数1,2或3,苯基A未取代或被卤素,硝基,C 1 -C 6 - 烷基,三氟甲基,C 3 -C 7 - 环烷基,羟基,C 1 -C 6 - C 1 -C 6 - 烷氧基,C 2 -C 6 - 烷酰氧基,氨基,C 1 -C 6 - 烷基氨基,二-C 1 -C 6 - 烷基氨基,C 2 -C 6 - 烷酰基氨基,CN,羧基,C 1 -C 6 - 烷氧基羰基,苯基,C 1 -C 6烷基苯基或 三氟甲基苯基,它们的吡啶-N-氧化物及其生理学上可接受的盐,其制备方法和含有活性成分的化合物的药物。

    Ethylenediamine and guanidine-derivatives
    15.
    发明授权
    Ethylenediamine and guanidine-derivatives 失效
    乙二胺和胍衍生物

    公开(公告)号:US4738983A

    公开(公告)日:1988-04-19

    申请号:US558984

    申请日:1983-12-07

    CPC分类号: C07D307/52 C07D333/20

    摘要: This invention relates to new compounds corresponding to the general formula: ##STR1## R.sub.1 represents a C.sub.3 -C.sub.10 cycloalkyl group substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.3 -C.sub.19 -cycloalkyl-C.sub.1 -C.sub.4 alkyl group which may be substituted by C.sub.1 -C.sub.6 alkyl radicals, a C.sub.6 -C.sub.8 bicycloalkyl group, a C.sub.6 -C.sub.8 bicycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.10 tricycloalkyl group, a C.sub.6 -C.sub.10 tricycloalkyl-C.sub.1 -C.sub.4 alkyl group, a C.sub.6 -C.sub.9 tetracycloalkyl group or a C.sub.6 -C.sub.9 -tetracycloalkyl-C.sub.1 -C.sub.4 alkyl group,R.sub.2 represents hydrogen, a C.sub.1 -C.sub.6 alkyl group, a phenyl-C.sub.1 -C.sub.4 alkyl group or a C.sub.1 -C.sub.6 alkyl group which is substituted by halogen atoms, nitro groups, hydroxy groups, C.sub.2 -C.sub.6 alkanoyloxy groups, C.sub.1 -C.sub.4 alkoxy groups, C.sub.1 -C.sub.4 alkoxy carbonyl groups or carboxy groups,R.sub.3 represented hydrogen, the 2-[5-(dimethylaminomethyl)-2-furyl-methylthio]-ethyl group, a C.sub.1 -C.sub.18 -alkyl group, a C.sub.3 -C.sub.6 -cycloalkyl group, a C.sub.3 -C.sub.6 -alkenyl group, a C.sub.3 -C.sub.6 -alkinyl group, an amino-C.sub.1 -C.sub.4 -alkyl group, a C.sub.2 -C.sub.6 -alkanoylamino-C.sub.1 -C.sub.4 -alkyl group, a mono-C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl group, a di-C.sub.1 -C.sub.6 -alkylamino-C.sub.1 -C.sub.4 -alkyl group or a C.sub.1 -C.sub.18 -alkyl group, which is substituted by halogen atoms, nitro groups, hydroxy groups, C.sub.2 -C.sub.6 alkanoyloxy groups, C.sub.1 -C.sub.4 alkoxy groups, C.sub.1 -C.sub.4 alkoxycarbonyl groups or carboxy groups,A represents a nitrogen atom or a methine group,B represents a cyano radical or a nitro group, andX represents an oxygen atom or a sulphur atom, and salts thereof.The compounds inhibit the secretion of gastric juice. Moreover, they have an ulcer-inhibiting and stomach-spasmolytic effect.

    摘要翻译: 本发明涉及对应于通式的新化合物:其中R1表示被C1-C6烷基取代的C3-C10环烷基,可被C1取代的C3-C19-环烷基-C1-C4烷基 -C 6烷基,C 6 -C 8双环烷基,C 6 -C 8双环烷基-C 1 -C 4烷基,C 6 -C 10三环烷基,C 6 -C 10三环烷基-C 1 -C 4烷基,C 6 -C 9四环烷基或 C 6 -C 9 - 四环烷基-C 1 -C 4烷基,R 2表示氢,C 1 -C 6烷基,苯基-C 1 -C 4烷基或被卤素原子取代的C 1 -C 6烷基,硝基,羟基 基团,C 2 -C 6烷酰氧基,C 1 -C 4烷氧基,C 1 -C 4烷氧基羰基或羧基,R 3表示氢,2- [5-(二甲基氨基甲基)-2-呋喃基 - 甲硫基] - 乙基, -C 18 - 烷基,C 3 -C 6 - 环烷基,C 3 -C 6 - 烯基,C 3 -C 6 - 炔基,氨基-C 1 -C 4 - 烷基,C 2 -C 6 - 烷酰基氨基-C 1 -C 4 - 烷基,单-C 1 -C 6烷基 烯基-C 1 -C 4 - 烷基,被卤素原子取代的二-C 1 -C 6烷基氨基-C 1 -C 4 - 烷基或C 1 -C 18烷基,硝基,羟基,C 2 -C 6烷酰氧基 基团,C 1 -C 4烷氧基,C 1 -C 4烷氧基羰基或羧基,A表示氮原子或次甲基,B表示氰基或硝基,X表示氧原子或硫原子, 其中。 这些化合物抑制胃液的分泌。 此外,它们具有溃疡抑制和胃解痉作用。

    Substituted N-benzylindol-3-ylglyoxylic acid derivatives having antitumor action

    公开(公告)号:US06432987B1

    公开(公告)日:2002-08-13

    申请号:US09736431

    申请日:2000-12-15

    IPC分类号: A01N4340

    摘要: The invention relates to novel, substituted N-benzyl-indol-3-ylglyoxylic acid derivatives of the following formula and their use for the treatment of oncoses The invention further relates to their physiologically tolerable acid addition salts and if possible their N-oxides. In addition, the invention relates to pharmaceutical preparations containing at least one of the compounds of the abovementioned formula or their salts or N-oxides with physiologically tolerable inorganic or organic acids and, if appropriate, pharmaceutically utilizable vehicles and/or diluents or excipients and also administration forms of the compounds of the abovementioned formula containing at least one of the compounds of this formula or their salts in the form of tablets, coated tablets, capsules, solutions for infusion or ampoules, suppositories, patches, powder preparations which can be employed by inhalation, suspensions, creams and ointments