Sulfonates of hydroxycoumarins
    1.
    发明授权
    Sulfonates of hydroxycoumarins 失效
    羟基香豆素磺酸盐

    公开(公告)号:US4618622A

    公开(公告)日:1986-10-21

    申请号:US552787

    申请日:1983-11-17

    CPC分类号: C07D311/80 C07D311/16

    摘要: Sulfonates of hydroxycoumarins of the formula I ##STR1## where R.sup.1 and R.sup.2 are identical or different and are each hydrogen, halogen or alkyl of 1 to 5 carbon atoms which can be substituted by --NR.sup.4 R.sup.5, --OR.sup.4 or --OC(O)R.sup.4, where R.sup.4 and R.sup.5 are identical or different and are each hydrogen or alkyl of 1 to 4 carbon atoms, or R.sup.1 and R.sup.2 are each a carboxylic acid group --OC(O)R.sup.4 or a carboxamido radical, with the proviso that R.sup.1 is not methyl when R.sup.2 is hydrogen, or R.sup.1 and R.sup.2 together form a --(CH.sub.2).sub.n -- chain where n is 3-5, and R.sup.3 is a straight-chain or branched alkyl radical of 1 to 8 carbon atoms or cycloalkyl of 3 to 8 carbon atoms, each of which can be substituted by halogen, --OR.sup.4, --NR.sup.4 R.sup.5, --CN or phenyl, or R.sup.3 is a straight-chain or branched alkenyl radical of 3 to 8 carbon atoms, an amino group -- NR.sup.4 R.sup.5, or phenyl or naphthyl, each of which is unsubstituted or monosubstituted or polysubstituted by --OR.sup.4, --NR.sup.4 R.sup.5, --NO.sub.2, halogen, --SR.sup.4, --S(O)R.sup.4, --OS(O)R.sup.4, --SCF.sub.3, --OS(O)CF.sub.3, --CN, --C(O)R.sup.4, --OC(O)R.sup.4, --NHC(O)R.sup.4, --CF.sub.3, C.sub.1 -C.sub.4 -alkyl or a combination of these substituents, a process for their preparation, drugs containing these compounds, and compounds of the formula I, in which R.sup.1 is methyl and R.sup.2 is hydrogen, for use as drugs.

    摘要翻译: 式I的羟基香豆素的磺酸盐其中R 1和R 2相同或不同,各自为氢,卤素或可被-NR 4 R 5,-OR 4或-OC(O)取代的1至5个碳原子的烷基 )R 4,其中R 4和R 5相同或不同并且各自为氢或1至4个碳原子的烷基,或者R 1和R 2各自为羧酸基-OC(O)R 4或甲酰胺基,条件是R 1 当R 2为氢时,R 1和R 2一起形成 - (CH 2)n - 链,其中n为3-5,R 3为1至8个碳原子的直链或支链烷基或3个环烷基 至8个碳原子,每个可以被卤素,-OR4,-NR4R5,-CN或苯基取代,或R3是3-8个碳原子的直链或支链烯基,氨基-NR4R5或 苯基或萘基,它们各自被-OR4,-NR4R5,-NO2,卤素,-SR4,-S(O)R4,-OS(O)R4,-SCF3,-OS(O)未取代或单取代或多取代, CF 3,-CN,-C(O)R 4,-OC(O)R 4, -NHC(O)R 4,-CF 3,C 1 -C 4烷基或这些取代基的组合,其制备方法,含有这些化合物的药物和式I化合物,其中R 1是甲基,R 2是氢, 用作药物。

    Amino derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazoles
    6.
    发明授权
    Amino derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazoles 失效
    3-烷基-5-(2-羟基苯乙烯基) - 异恶唑的氨基衍生物

    公开(公告)号:US4251539A

    公开(公告)日:1981-02-17

    申请号:US30927

    申请日:1979-04-17

    CPC分类号: C07D261/08

    摘要: Alkylamino-propanol derivatives of 3-alkyl-5-(2-hydroxystyryl)-isoxazole, of the general formula ##STR1## where R is hydrogen, alkyl of 1 to 8 carbon atoms, which is unsubstituted or substituted by hydroxyl, alkoxy of 1 to 3 carbon atoms or cycloalkyl with 3 to 8 carbon atoms in the ring, alkenyl or alkynyl of 2 to 8 carbon atoms, or cycloalkyl with 3 to 8 carbon atoms in the ring, the cycloalkyl rings being unsubstituted or mono- or di-substituted by alkyl of 1 to 3 carbon atoms, and R' is alkyl of 1 to 4 carbon atoms, and their addition salts with physiologically acceptable acids, their preparation, and pharmaceutical formulations which contain these compounds and which can be used as valuable drugs in the treatment of hypertonia, coronary diseases of the heart and cardiac arrhythmias.

    摘要翻译: 3-烷基-5-(2-羟基苯乙烯基) - 异恶唑的通式为:其中R为氢的烷基氨基丙醇衍生物,未取代或被羟基取代的碳原子数为1至8的烷基,烷氧基为1 至3个碳原子或环中具有3至8个碳原子的环烷基,2至8个碳原子的链烯基或炔基或环中具有3至8个碳原子的环烷基,环烷基环为未取代的或单或二取代的 具有1至3个碳原子的烷基,R'是1至4个碳原子的烷基,以及它们与生理上可接受的酸的加成盐,它们的制备方法和含有这些化合物的药物制剂,并且可以在 治疗高血压,心脏冠状动脉疾病和心律失常。

    2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole
    10.
    发明授权
    2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole 失效
    2-甲基-5-(2-羟基苯乙烯基)-1,3,4-噻二唑

    公开(公告)号:US4263430A

    公开(公告)日:1981-04-21

    申请号:US30886

    申请日:1979-04-17

    IPC分类号: C07D285/12 C07F9/6539

    CPC分类号: C07D285/12 C07F9/65395

    摘要: 2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole of the formula ##STR1## and processes for its preparation by condensing salicylaldehyde with 2,5-dimethyl-1,3,4-thiadiazole or 2-methyl-5-(triphenylphosphine-methylene)-1,3,4-thiadiazole. 2-Methyl-5-(2-hydroxystyryl)-1,3,4-thiadiazole is a valuable intermediate for the preparation of pharmacologically active compounds; for example the alkylamino-hydroxypropyl ethers can, because of their .beta.-sympatholytic action, be used as drugs for the treatment of coronary diseases of the heart, cardiac arrhythmias and hypertonia.

    摘要翻译: 式(1)的2-甲基-5-(2-羟基苯乙烯基)-1,3,4-噻二唑及其制备方法是将水杨醛与2,5-二甲基-1,3,4-噻二唑 或2-甲基-5-(三苯基膦 - 亚甲基)-1,3,4-噻二唑。 2-甲基-5-(2-羟基苯乙烯基)-1,3,4-噻二唑是制备药理活性化合物的有价值的中间体; 例如,烷基氨基 - 羟丙基醚可以由于其β - 溶血性作用而被用作治疗心脏冠状动脉疾病,心律失常和高渗性的药物。