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    Chromone compounds and preparation thereof
    1.
    发明授权
    Chromone compounds and preparation thereof 失效
    色酮化合物及其制备方法

    公开(公告)号：US4105781A

    公开(公告)日：1978-08-08

    申请号：US788735

    申请日：1977-04-19

    申请人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    发明人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    IPC分类号： C07D407/12 ,  C07D407/14 ,  A61K31/34

    CPC分类号： C07D407/12 ,  Y02P20/55

    摘要： 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.

    摘要翻译： 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＆lt; IMAGE＆gt;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。

    Chromone compounds
    2.
    发明授权
    Chromone compounds 失效
    色酮化合物

    公开(公告)号：US4049664A

    公开(公告)日：1977-09-20

    申请号：US679140

    申请日：1976-04-22

    申请人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    发明人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    IPC分类号： C07D407/12 ,  C07D311/22

    CPC分类号： C07D407/12 ,  Y02P20/55 ,  Y10S514/826

    摘要： 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.

    摘要翻译： 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。

    Chromone compounds and preparation thereof
    4.
    发明授权
    Chromone compounds and preparation thereof 失效
    色酮化合物及其制备方法

    公开(公告)号：US3965122A

    公开(公告)日：1976-06-22

    申请号：US213180

    申请日：1971-12-28

    申请人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    发明人： Suminori Umio ,  Shizuo Maeno ,  Ikuo Ueda ,  Yoshinari Sato ,  Masaaki Matsuo

    IPC分类号： C07D311/30 ,  C07D407/12 ,  C07D311/28

    CPC分类号： C07D407/12 ,  C07D311/30 ,  Y02P20/55 ,  Y10S514/826

    摘要： Chromone compounds having the structure ##SPC1##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 ##SPC2##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 ##SPC3##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.

    摘要翻译： 具有下式结构的色酮化合物是芳基，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]的化合物通过在碱存在下使WHEREIN Y'为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的羧酸反应来制备 催化剂。 然后将所得化合物与酸反应。 通过使化合物与化合物X-Y1'-Z-R3'反应制备化合物，其中X是酸残基，Y'是羟基被任选保护的低级亚烷基或羟基（低级）亚烷基 通过保护基团，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。

    Chromone derivatives
    7.
    发明授权
    Chromone derivatives 失效
    色酮衍生物

    公开(公告)号：US4001280A

    公开(公告)日：1977-01-04

    申请号：US371852

    申请日：1973-06-20

    申请人： Suminori Umio ,  Ikuo Ueda ,  Masaaki Matsuo ,  Masakazu Kobayashi ,  Osamu Nakaguti ,  Yoshinari Sato

    发明人： Suminori Umio ,  Ikuo Ueda ,  Masaaki Matsuo ,  Masakazu Kobayashi ,  Osamu Nakaguti ,  Yoshinari Sato

    IPC分类号： C07D311/24

    CPC分类号： C07D311/24

    摘要： Chromone derivatives of the formula: ##STR1## wherein R.sup.1 is alkoxy, an N,S-containing heterocyclic group or aryloxy in which heterocyclic group may be substituted with halogen or acyl, and aryl may be substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy; R.sup.2 is alkylene; R.sup.3 is hydroxy, alkoxy or a group of the formula ##STR2## in which R.sup.4 is hydrogen, R.sup.5 is hydroxy or amino or R.sup.4 and R.sup.5 means taken together with the adjacent nitrogen atom, piperazinyl substituted with alkyl or hydroxyalkyl; provided that when R.sup.3 is hydroxy or alkoxy, R.sup.1 is an N,S-containing heterocyclic group or aryloxy in which heterocyclic group is substituted with halogen or acyl, and aryl is substituted with amino, alkylamino, acylamino, nitro or alkylenedioxy, and nontoxic, pharmaceutically acceptable salt thereof. These compounds are useful as anti-allergic agents.