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    • 8. 发明授权
    • Chromone compounds and preparation thereof
    • 色酮化合物及其制备方法
    • US4105781A
    • 1978-08-08
    • US788735
    • 1977-04-19
    • Suminori UmioShizuo MaenoIkuo UedaYoshinari SatoMasaaki Matsuo
    • Suminori UmioShizuo MaenoIkuo UedaYoshinari SatoMasaaki Matsuo
    • C07D407/12C07D407/14A61K31/34
    • C07D407/12Y02P20/55
    • Chromone compounds having the structure ##STR1## wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy (lower) alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl (lower) alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar (lower) alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##STR2## wherein Y' is hydroxy (lower) alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I'] are prepared by reacting the compound ##STR3## with the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy (lower) alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar (lower) alkyl and Z is as defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.
    • 具有结构(I)或者其中R是芳基,取代的芳基,噻吩基,呋喃基或吡啶基的结构的色酮化合物,Y是羟基(低级)亚烷基,R 1是氢,低级烷基,芳基, 取代的芳基或杂环基,R2是氢或低级烷氧基,Y1是低级亚烷基或羟基(低级)亚烷基,Z是氧或硫,R3是氢,低级烷基,芳基,取代芳基或芳(低级) 抗过敏活性,可用于治疗哮喘。 结构[I]的化合物通过其中Y'是羟基被最佳保护的羟基(低级)亚烷基或其[II]的反应性衍生物与式R-COOH的羧酸反应制备 在碱性催化剂的存在下。 然后将所得化合物与酸反应。 通过使化合物< IMAGE>与化合物X-Y1'-Z-R3'反应其中X是酸残基,Y'是低级亚烷基或羟基(低级)亚烷基 其羟基任选被保护基保护,R 3'是氢,低级烷基,芳基,取代的芳基或芳(低级)烷基,Z如上所定义。 当R3'为氢时,-Z-R3'任选被保护基保护。 当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时,所得化合物进行消除反应。
    • 9. 发明授权
    • Chromone compounds
    • 色酮化合物
    • US4049664A
    • 1977-09-20
    • US679140
    • 1976-04-22
    • Suminori UmioShizuo MaenoIkuo UedaYoshinari SatoMasaaki Matsuo
    • Suminori UmioShizuo MaenoIkuo UedaYoshinari SatoMasaaki Matsuo
    • C07D407/12C07D311/22
    • C07D407/12Y02P20/55Y10S514/826
    • Chromone compounds having the structure ##STR1## wherein R is aryl, substituted aryl, thienyl, furyl or pyridyl, Y is hydroxy (lower) alkylene, R.sub.1 is hydrogen, lower alkyl, aryl, substituted aryl or a heterocyclic group, R.sub.2 is hydrogen or lower alkoxy, Y.sub.1 is lower alkylene or hydroxyl (lower) alkylene, Z is oxygen or sulfur and R.sub.3 is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl have anti-allergic activity and are useful in the treatment of asthma. Compounds of the structure [I] are prepared by reacting ##STR2## wherein Y' is hydroxy (lower) alkylene whose hydroxy group is optimally protected or a reactive derivative of [II] with a carboxylic acid of the formula R--COOH in the presence of a basic catalyst. The resulting compound is then reacted with an acid. Compounds of the structure [I] are prepared by reacting the compound ##STR3## with the compound X--Y.sub.1 '--Z--R.sub.3 ' wherein X is an acid residue, Y' is lower alkylene or hydroxy (lower) alkylene whose hydroxy group is optionally protected by a protective group, R.sub.3 ' is hydrogen, lower alkyl, aryl, substituted aryl, or ar(lower)alkyl and Z is defined above. When R.sub.3 ' is hydrogen, --Z--R.sub.3 ' is optionally protected by a protective group. The resultant compound is subjected to an elimination reaction when Y' is a protected group or when --Z--R.sub.3 ' is protected to split off the protective group.
    • 具有结构(I)的色酮化合物其中R是芳基,取代的芳基,噻吩基,呋喃基或吡啶基,Y是羟基(低级)亚烷基,R1是氢,低级烷基,芳基,取代的 芳基或杂环基,R2是氢或低级烷氧基,Y1是低级亚烷基或羟基(低级)亚烷基,Z是氧或硫,R3是氢,低级烷基,芳基,取代芳基或芳(低级)烷基具有抗 - 过敏活性,可用于治疗哮喘。 结构[I]的化合物通过使(II)其中Y'是羟基被最佳保护的羟基(低级)亚烷基或[II]的反应性衍生物与式R-COOH的羧酸反应制备 在碱性催化剂的存在下。 然后将所得化合物与酸反应。 结构[I]化合物通过使化合物(Ⅳ)与化合物X-Y1'-Z-R3'反应而制备,其中X为酸残基,Y'为低级亚烷基或羟基(低级)亚烷基 羟基任选被保护基保护,R 3'是氢,低级烷基,芳基,取代的芳基或芳(低级)烷基,Z如上所定义。 当R3'为氢时,-Z-R3'任选被保护基保护。 当Y'为受保护基团时或当-Z-R3'被保护以分离保护基团时,所得化合物进行消除反应。