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    5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same
    1.
    发明授权
    5-Substituted picolinic acid derivatives and an anti-hypertensive composition containing the same 失效
    5-取代的吡啶甲酸衍生物和含有它们的抗高血压组合物

    公开(公告)号：US4229448A

    公开(公告)日：1980-10-21

    申请号：US23504

    申请日：1979-03-23

    申请人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

    发明人： Yasuharu Sekizawa ,  Takashi Tsuruoka ,  Mitsugu Hachisu ,  Masaji Sezaki ,  Masashi Miyamoto ,  Uichi Shibata ,  Kazuko Mizutani ,  Shigeharu Inouye ,  Takemi Koeda ,  Keizo Shimomura ,  Taro Niida

    IPC分类号： C07D213/65 ,  C07D213/79 ,  C07D213/81 ,  A61K31/455

    CPC分类号： C07D213/79 ,  C07D213/65 ,  C07D213/81

    摘要： 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.

    摘要翻译： 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。

    5-Alkoxy-picolinic esters and anti-hypertensive composition containing 5-alkoxy-picolinic esters
    2.
    发明授权
    5-Alkoxy-picolinic esters and anti-hypertensive composition containing 5-alkoxy-picolinic esters 失效
    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

    公开(公告)号：US4198416A

    公开(公告)日：1980-04-15

    申请号：US944683

    申请日：1978-09-22

    申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

    发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

    IPC分类号： C07D213/65 ,  C07D213/79 ,  A61K31/44

    CPC分类号： C07D213/79 ,  C07D213/65

    摘要： 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.

    摘要翻译： 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。

    5-Alkoxy-picolinic acid calcium salts and anti-hypertensive composition containing 5-alkoxy-picolinic acid calcium salts and anti-hypertensive composition thereof
    3.
    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 失效
    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

    公开(公告)号：US4189489A

    公开(公告)日：1980-02-19

    申请号：US838180

    申请日：1977-09-30

    申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

    发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Uichi Shibata ,  Hiroyasu Asaoka ,  Mitsugu Hachisu ,  Osamu Itoh ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Taro Niida

    IPC分类号： A61K31/44 ,  A61P9/12 ,  C07D213/65 ,  C07D213/79 ,  A61K31/445 ,  C07D213/89

    CPC分类号： C07D213/79 ,  C07D213/65

    摘要： 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.

    摘要翻译： 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。

    3-Substituted-2(1H)pyridone-6-carboxylic acids
    4.
    发明授权
    3-Substituted-2(1H)pyridone-6-carboxylic acids 失效
    3-取代的2（1H）吡啶酮-6-羧酸

    公开(公告)号：US4156728A

    公开(公告)日：1979-05-29

    申请号：US865213

    申请日：1977-12-28

    申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

    发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

    IPC分类号： C07D213/79 ,  A61K31/44

    CPC分类号： C07D213/79

    摘要： Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a substituted or unsubstituted aralkyl group, that is an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared by reacting D-glucaro-.delta.-lactam or its salt with an aralkyl halide.

    摘要翻译： 提供了用作降压剂的新型化合物，其具有通式I（I），其中R 1表示取代或未取代的芳烷基，即通式为“IMAGE”的芳烷基，其中R 2表示氢，低级烷基 或卤素原子。 此外，还描述了新型的物质治疗组合物，其结合上述新型3-取代-2（1H）吡啶酮-6-羧酸（I）作为活性成分与载体并用作降压剂。 这些新的式I化合物通过D-葡聚糖-δ-内酰胺或其盐与芳烷基卤化物反应来制备。

    3-Substituted-2(1H)pyridon-6-carboxylic acids and process for preparation of same
    5.
    发明授权
    3-Substituted-2(1H)pyridon-6-carboxylic acids and process for preparation of same 失效
    3-取代的2（1H）吡啶酮-6-羧酸及其制备方法

    公开(公告)号：US4083850A

    公开(公告)日：1978-04-11

    申请号：US700340

    申请日：1976-06-28

    申请人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

    发明人： Takemi Koeda ,  Takashi Tsuruoka ,  Hiroyasu Asaoka ,  Uichi Shibata ,  Shigeharu Inoue ,  Taro Niida

    IPC分类号： C07D213/79 ,  C07D213/55

    CPC分类号： C07D213/79

    摘要： Novel compounds useful as hypotensive agents are presented having the general formula I ##STR1## wherein R.sub.1 represents a lower aliphatic acyl group, a straight or branched chain alkyl or alkenyl group or an aralkyl group of the general formula ##STR2## wherein R.sub.2 represents hydrogen, a lower alkyl group or a halogen atom. Furthermore, new therapeutic compositions of matter are also described incorporating the above novel 3-substituted-2(1H)pyridone-6-carboxylic acids (I) as an active ingredient with carriers and showing uses as hypotensive agents. These new compounds of the formula I are prepared either by reacting D-glucaro-.delta.-lactam or its salt with an acid anhydride or by reacting 3-hydroxy-2(1H)pyridone-6-carboxylic acid with an acyl anhydride or alkyl halide, aralkyl halide and an alkenyl halide.

    摘要翻译： 提供了可用作降压剂的新型化合物，其具有通式I（I），其中R 1表示低级脂族酰基，直链或支链烷基或烯基或通式为“IMAGE”的芳烷基，其中R 2 表示氢，低级烷基或卤素原子。 此外，还描述了新型的物质治疗组合物，其结合上述新型3-取代-2（1H）吡啶酮-6-羧酸（I）作为活性成分与载体并用作降压剂。 式I的这些新化合物通过D-葡聚糖-δ-内酰胺或其盐与酸酐反应或通过使3-羟基-2（1H）吡啶酮-6-羧酸与酰基酸酐或烷基卤化物 芳烷基卤化物和烯基卤化物。

    Process for preparing D,L-2-amino-4-methylphosphinobutyric acid
    7.
    发明授权
    Process for preparing D,L-2-amino-4-methylphosphinobutyric acid 失效
    制备D，L-2-氨基-4-甲基膦酰基丁酸的方法

    公开(公告)号：US4264532A

    公开(公告)日：1981-04-28

    申请号：US140198

    申请日：1979-06-15

    申请人： Takashi Tsuruoka ,  Akira Suzuki ,  Kunitaka Tachibana ,  Kazuko Mizutani ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Tetsuo Takematsu

    发明人： Takashi Tsuruoka ,  Akira Suzuki ,  Kunitaka Tachibana ,  Kazuko Mizutani ,  Yasuharu Sekizawa ,  Shigeharu Inouye ,  Tetsuo Takematsu

    IPC分类号： A01N57/20 ,  C07F9/30 ,  C07F9/32

    CPC分类号： C07F9/3211 ,  A01N57/20 ,  C07F9/301

    摘要： PCT No. PCT/JP78/00058 Sec. 371 Date June 15, 1979 Sec. 102(e) Date June 15, 1979 PCT Field Dec. 18, 1978 PCT Pub. No. WO79/00405 PCT Pub. Date July 12, 1979This invention relates to a novel process for preparing D,L-2-amino-4-methylphosphinobutyric acid having herbicidal and antifungicidal activities which comprises subjecting acrolein to reaction with a dialkyl phosphonite to synthesize an acetal of an ester of 3-oxopropylmethylphosphinic acid; treating the thus obtained compound with an acid for deacetalization to obtain an ester of 3-oxopropylmethylphosphinic acid and then applying the Strecker's process used for amino synthesis to the thus obtained ester.

    摘要翻译： PCT No.PCT / JP78 / 00058 Sec。 371日期1979年6月15日 102（e）日期1979年6月15日PCT领域1978年12月18日PCT公布。 公开号WO79 / 00405 日期1979年7月12日本发明涉及一种具有除草和杀真菌活性的D，L-2-氨基-4-甲基膦酰基丁酸的新方法，该方法包括使丙烯醛与二烷基亚膦酸酯反应，合成3 - 氧代丙基甲基次膦酸 用酸脱乙酰化处理得到的化合物，得到3-氧代丙基甲基次膦酸的酯，然后将用于氨基合成的斯特雷克氏法用于得到的酯。