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    • 4. 发明授权
    • 5-Alkoxy-picolinic acid calcium salts and anti-hypertensive composition
containing 5-alkoxy-picolinic acid calcium salts and anti-hypertensive
composition thereof
    • 含有5-烷氧基 - 吡啶甲酸钙盐及其抗高血压组合物的5-烷氧基 - 吡啶甲酸钙盐和抗高血压组合物
    • US4189489A
    • 1980-02-19
    • US838180
    • 1977-09-30
    • Takemi KoedaTakashi TsuruokaUichi ShibataHiroyasu AsaokaMitsugu HachisuOsamu ItohYasuharu SekizawaShigeharu InouyeTaro Niida
    • Takemi KoedaTakashi TsuruokaUichi ShibataHiroyasu AsaokaMitsugu HachisuOsamu ItohYasuharu SekizawaShigeharu InouyeTaro Niida
    • A61K31/44A61P9/12C07D213/65C07D213/79A61K31/445C07D213/89
    • C07D213/79C07D213/65
    • 5-Alkoxy-picolinic acids and the salts and the esters thereof represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and M represents a hydrogen atom; a calcium atom; a sodium atom; a potassium atom; an aluminum atom; an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom); a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as a chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic acids and the salts and the esters thereof, and anti-hypertensive compositions containing the 5-alkoxy-picolinic acids and the salts and the esters thereof.
    • 5-烷氧基 - 吡啶甲酸及其由式(I)表示的盐及其酯:其中R表示具有1至6个碳原子的烷基,M表示氢原子; 钙原子; 一个钠原子; 钾原子; 铝原子; 未取代的苯基; 被一个或多个具有1至4个碳原子的烷基,具有1至4个碳原子的烷氧基或卤素原子(例如氯,溴,碘等)原子取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 或具有式“IMAGE”的酰氧基烷基,其中R 2表示氢原子或甲基,R 3表示具有1至5个碳原子的烷基(例如甲基,正丙基,异丁基,叔丁基等) ,基团),具有1至4个碳原子的烷氧基,苯基,被一个或多个具有1至4个碳原子的烷基取代的苯基,具有1至4个碳原子的烷氧基或卤素原子 (例如氯,溴,碘等原子)或其中烷基部分具有1至3个碳原子的芳烷基,其可用作抗高血压剂,制备5-烷氧基 - 吡啶甲酸的方法和 其盐和酯,以及含有5-烷氧基 - 吡啶甲酸及其盐及其酯的抗高血压组合物。
    • 6. 发明授权
    • 5-Alkoxy-picolinic esters and anti-hypertensive composition containing
5-alkoxy-picolinic esters
    • 5-烷氧基 - 吡啶甲酸酯和含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物
    • US4198416A
    • 1980-04-15
    • US944683
    • 1978-09-22
    • Takemi KoedaTakashi TsuruokaUichi ShibataHiroyasu AsaokaMitsugu HachisuOsamu ItohYasuharu SekizawaShigeharu InouyeTaro Niida
    • Takemi KoedaTakashi TsuruokaUichi ShibataHiroyasu AsaokaMitsugu HachisuOsamu ItohYasuharu SekizawaShigeharu InouyeTaro Niida
    • C07D213/65C07D213/79A61K31/44
    • C07D213/79C07D213/65
    • 5-Alkoxy-picolinic esters represented by the formula (I): ##STR1## wherein R represents an alkyl group having 1 to 6 carbon atoms and R.sub.1 represents an unsubstituted phenyl group; a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms or an acetyl group; a phthalidyl group; an alkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an alkoxyalkoxyalkyl group wherein the alkyl moiety and the alkoxy moiety each has 1 to 4 carbon atoms; an indanyl group; or an acyloxyalkyl group having the formula ##STR2## wherein R.sub.2 represents a hydrogen atom or a methyl group and R.sub.3 represents an alkyl group having 1 to 5 carbon atoms (such as a methyl, n-propyl, isobutyl, t-butyl, etc., group), an alkoxy group having 1 to 4 carbon atoms, a phenyl group, a phenyl group substituted with one or more of an alkyl group having 1 to 4 carbon atoms, an alkoxy group having 1 to 4 carbon atoms or a halogen atom (such as chlorine, bromine, iodine, etc., atom) or an aralkyl group wherein the alkyl moiety has 1 to 3 carbon atoms, which are useful as anti-hypertensive agents, a process for preparing 5-alkoxy-picolinic esters, and anti-hypertensive compositions containing the 5-alkoxy-picolinic esters.
    • 由式(I)表示的5-烷氧基 - 吡啶甲酸酯:其中R表示具有1至6个碳原子的烷基,R 1表示未取代的苯基; 被一个或多个具有1至4个碳原子的烷基或乙酰基取代的苯基; 苯酞基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷基; 其中烷基部分和烷氧基部分各自具有1至4个碳原子的烷氧基烷氧基烷基; 茚满基; 或具有式“IMAGE”的酰氧基烷基,其中R 2表示氢原子或甲基,R 3表示具有1至5个碳原子的烷基(例如甲基,正丙基,异丁基,叔丁基等) ,基团),具有1至4个碳原子的烷氧基,苯基,被一个或多个具有1至4个碳原子的烷基取代的苯基,具有1至4个碳原子的烷氧基或卤素原子 (例如氯,溴,碘等原子)或其中烷基部分具有1〜3个碳原子的芳烷基,其可用作抗高血压剂,制备5-烷氧基 - 吡啶甲酸酯的方法和 含有5-烷氧基 - 吡啶甲酸酯的抗高血压组合物。
    • 7. 发明授权
    • 5-Substituted picolinic acid derivatives and an anti-hypertensive
composition containing the same
    • 5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物
    • US4229448A
    • 1980-10-21
    • US23504
    • 1979-03-23
    • Yasuharu SekizawaTakashi TsuruokaMitsugu HachisuMasaji SezakiMasashi MiyamotoUichi ShibataKazuko MizutaniShigeharu InouyeTakemi KoedaKeizo ShimomuraTaro Niida
    • Yasuharu SekizawaTakashi TsuruokaMitsugu HachisuMasaji SezakiMasashi MiyamotoUichi ShibataKazuko MizutaniShigeharu InouyeTakemi KoedaKeizo ShimomuraTaro Niida
    • C07D213/65C07D213/79C07D213/81A61K31/455
    • C07D213/79C07D213/65C07D213/81
    • 5-Substituted picolinic acid derivatives represented by the formula (I): ##STR1## wherein R.sub.1 represents a straight or branched chain halogen-substituted alkyl group having 2 to 6 carbon atoms or a substituted phenyl group having the formula ##STR2## wherein R.sub.3 and R.sub.4, which may be the same or different, each represents a hydrogen atom, a halogen atom, a lower alkyl group, a lower alkoxy group, a nitro group, an amino group, an N-alkyl-substituted amino group, an acylamino group, an acetyl group, an acyloxy group, a hydroxy group or a halogen-substituted alkyl group or R.sub.3 and R.sub.4, when taken together, represent a polymethylene chain; and R.sub.2 represents an --OM group wherein M represents a hydrogen, sodium, potassium, calcium, aluminium or magnesium atom, a straight or branched chain or cyclic alkoxy group having 1 to 6 carbon atoms, an aminoalkoxy group, a phenoxy group, a substituted phenoxy group, a 5-indanyloxy group, an acyloxyalkyloxy group having the formula ##STR3## wherein R.sub.5 represents a hydrogen atom or a methyl group and R.sub.6 represents a lower alkyl group having 1 to 6 carbon atoms, a phenyl group or a substituted phenyl group, or an amino group represented by the formula ##STR4## wherein R.sub.7 and R.sub.8, which may be the same or different, each represents a hydrogen atom, a lower alkyl group, or a phenyl group which are useful as anti-hypertensive agents, a process for preparing the above 5-substituted picolinic acid derivatives, and anti-hypertensive compositions containing the same.
    • 由式(I)表示的5-取代的吡啶甲酸衍生物:其中R 1表示具有2至6个碳原子的直链或支链卤素取代的烷基或具有下式的取代苯基: 其中可以相同或不同的R 3和R 4各自表示氢原子,卤素原子,低级烷基,低级烷氧基,硝基,氨基,N-烷基取代的氨基, 酰氨基,乙酰基,酰氧基,羟基或卤素取代的烷基,或者R 3和R 4一起表示聚亚甲基链; R 2表示-OM基,其中M表示氢,钠,钾,钙,铝或镁原子,具有1至6个碳原子的直链或支链或环状烷氧基,氨基烷氧基,苯氧基,取代的 苯氧基,5-茚满氧基,具有式“IMAGE”的酰氧基烷氧基,其中R5表示氢原子或甲基,R6表示碳原子数1〜6的低级烷基,苯基或取代苯基 或由式“IMAGE”表示的氨基,其中R7和R8可以相同或不同,表示可用作抗高血压剂的氢原子,低级烷基或苯基, 制备上述5-取代的吡啶甲酸衍生物的方法和含有它们的抗高血压组合物。