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    • 12. 发明授权
    • N-Benzoyl-N'-3-indolyl-N'alkyl-1,3-diaminopropanes
    • N-苯甲酰基-N'-3-吲哚基-N'-烷基-1,3-二氨基丙烷
    • US4350634A
    • 1982-09-21
    • US111445
    • 1980-01-11
    • Paul StadlerFranz Troxler
    • Paul StadlerFranz Troxler
    • C07D209/14C07D209/16C07D209/18C07D209/12A61K31/40
    • C07D209/18C07D209/14C07D209/16
    • The invention provides indole compounds useful for the treatment of hypertension, processes for the preparation of said compounds and pharmaceutical compositions containing these compounds.The compounds of the invention have the formula ##STR1## wherein n is 2 or 3, A is 1,4-cyclohexylidene or trimethylene and R.sub.1 is H or alkyl, or A together with NR.sub.1 is 4-piperidyl, R.sub.2 is hydrogen or alkyl, R.sub.3 is alkyl, cycloalkyl, amino, alkylamino, dialkylamino, phenylamino, unsubstituted or substituted phenyl or benzyl, pyridylmethyl or an heterocycle, R.sub.4 is hydrogen, chlorine, bromine or alkyl, R.sub.5 is hydrogen, alkyl, alkoxy or alkylthio, and X is --CO-- or --CS.
    • 本发明提供了可用于治疗高血压的吲哚化合物,所述化合物的制备方法和含有这些化合物的药物组合物。 本发明化合物具有式(Ⅰ)其中n为2或3,A为1,4-亚环己基或三亚甲基,R 1为H或烷基,或A与NR 1一起为4-哌啶基,R 2为氢或烷基, R3是烷基,环烷基,氨基,烷基氨基,二烷基氨基,苯基氨基,未取代或取代的苯基或苄基,吡啶基甲基或杂环,R4是氢,氯,溴或烷基,R5是氢,烷基,烷氧基或烷硫基,X是 - CO-或-CS。
    • 13. 发明授权
    • N-9,10-Dihydrolysergyl-m-aminobenzoic acid amide derivative
    • N-9,10-二氢苯乙烯基 - 间氨基苯甲酰胺衍生物
    • US4248871A
    • 1981-02-03
    • US44916
    • 1979-06-04
    • Paul Stadler
    • Paul Stadler
    • A61K31/48A61K31/495A61P9/00A61P43/00C07D457/06
    • C07D457/06
    • The present invention provides compounds of formula I, ##STR1## wherein X is hydrogen, chlorine or bromine andY is hydrogen or bromine, with the proviso that when X is chlorine Y is hydrogen,Z is carbonyl or sulphonyl,R.sub.1 is alkyl of 1 to 4 carbon atoms, andeither (i)R.sub.2 is hydrogen or alkyl of 1 to 5 carbon atoms, andR.sub.3 is hydrogen, alkyl of 1 to 5 carbon atoms, or phenyl,or (ii)R.sub.2 together with R.sub.3 is a radical of formula ##STR2## wherein R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are, independently, hydrogen or alkyl of 1 to 4 carbon atoms,or (iii)R.sub.2 together with R.sub.4 is a radical of formula--(CH.sub.2).sub.2 --A--(CH.sub.2).sub.2 -- wherein A is a bond, oxygen, sulphur or NR.sub.8 wherein R.sub.8 is hydrogen, alkyl of 1 to 4 carbon atoms, phenyl or alkoxyphenyl,useful as venotonising agents.
    • 本发明提供式I化合物,其中X是氢,氯或溴,Y是氢或溴,条件是当X是氯时,Y是氢,Z是羰基或磺酰基,R 1是 1至4个碳原子,和(i)R 2是氢或1至5个碳原子的烷基,R 3是氢,1至5个碳原子的烷基或苯基,或(ii)R 2与R 3一起是一个基团 其中R 4,R 5,R 6和R 7独立地是氢或1至4个碳原子的烷基,或(iii)R 2与R 4一起是式 - (CH 2)2 -A-(CH 2) )其中A为键,氧,硫或NR8,其中R8为氢,1至4个碳原子的烷基,苯基或烷氧基苯基,可用作静脉诱导剂。
    • 15. 发明授权
    • N-9,10-dihydrolysergyl-m-aminobenzoic acid amide derivative
    • N-9,10-二氢青霉烯基 - 间氨基苯甲酸酰胺衍生物
    • US4180581A
    • 1979-12-25
    • US872639
    • 1978-01-26
    • Paul Stadler
    • Paul Stadler
    • A61K31/48A61K31/495A61P9/00A61P43/00C07D457/06
    • C07D457/06
    • The present invention provides compounds of formula I, ##STR1## wherein X is hydrogen, chlorine or bromine andY is hydrogen or bromine, with the proviso that when X is chlorine Y is hydrogen,Z is carbonyl or sulphonyl,R.sub.1 is alkyl of 1 to 4 carbon atoms, andeither (i)R.sub.2 is hydrogen or alkyl of 1 to 5 carbon atoms, andR.sub.3 is hydrogen, alkyl of 1 to 5 carbon atoms, or phenyl,or (ii)R.sub.2 together with R.sub.3 is a radical of formula ##STR2## wherein R.sub.4, R.sub.5, R.sub.6 and R.sub.7 are, independently, hydrogen or alkyl of 1 to 4 carbon atoms,or (iii)R.sub.2 together with R.sub.4 is a radical of formula--(CH.sub.2).sub.2 --A--(CH.sub.2).sub.2 --wherein A is a bond, oxygen, sulphur or NR.sub.8 wherein R.sub.8 is hydrogen, alkyl of 1 to 4 carbon atoms, phenyl or alkoxyphenyl,useful as venotonising agents.
    • 本发明提供式I化合物,其中X是氢,氯或溴,Y是氢或溴,条件是当X是氯时,Y是氢,Z是羰基或磺酰基,R 1是 1至4个碳原子,和(i)R 2是氢或1至5个碳原子的烷基,R 3是氢,1至5个碳原子的烷基或苯基,或(ii)R 2与R 3一起是一个基团 其中R 4,R 5,R 6和R 7独立地是氢或1至4个碳原子的烷基,或(iii)R 2与R 4一起是式 - (CH 2)2 -A-(CH 2) )其中A为键,氧,硫或NR8,其中R8为氢,1至4个碳原子的烷基,苯基或烷氧基苯基,可用作静脉诱导剂。