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    • 4. 发明授权
    • Ethylenediamine and guanidine-derivatives
    • 乙二胺和胍衍生物
    • US4738983A
    • 1988-04-19
    • US558984
    • 1983-12-07
    • Peter EmigGerhard SchefflerKlaus ThiemerCarl-Heinrich Weischer
    • Peter EmigGerhard SchefflerKlaus ThiemerCarl-Heinrich Weischer
    • A61K31/34A61K31/341A61K31/38A61K31/381A61P1/04C07D307/52C07D333/20C07D307/02
    • C07D307/52C07D333/20
    • 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.
    • 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。
    • 6. 发明授权
    • Substituted 3-(n-heterocyclic)-2,6-diaminopyridines and -n-oxides
    • 取代的3-(正 - 杂环)-2,6-二氨基吡啶和 - 氧化物
    • US4923858A
    • 1990-05-08
    • US352287
    • 1989-05-16
    • Jurgen EngelPeter EmigBernd NickelIstvan Szelenyi
    • Jurgen EngelPeter EmigBernd NickelIstvan Szelenyi
    • A61K31/44A61K31/535A61P25/04A61P25/08A61P29/00C07D401/04C07D413/04C07D417/04
    • C07D401/04C07D413/04C07D417/04
    • 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.
    • 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。