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    Process for the production of nuclear substituted cinnamoylanthranilic acid derivatives
    1.
    发明授权
    Process for the production of nuclear substituted cinnamoylanthranilic acid derivatives 失效
    制备核取代肉桂酰邻氨基苯甲酸衍生物的方法

    公开(公告)号：US4587356A

    公开(公告)日：1986-05-06

    申请号：US654231

    申请日：1984-09-25

    申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    IPC分类号： C07D295/02 ,  C07D295/027 ,  C07C99/00

    CPC分类号： C07D295/027

    摘要： The present invention provides an improved method for producing a nuclear substituted cinnamoylanthranilic acid compound.Illustrative of the process is the reaction of 3-hydroxy-4-methoxybenzaldehyde with 2-carboxymalonanilic acid in an inert solvent medium in the presence of a molar excess of piperidine to provide a high purity intermediate salt precipitate, and the salt is treated with an acidic reagent to yeild N-(3-hydroxy-4-methoxycinnamoyl)anthranilic acid product.

    摘要翻译： 本发明提供了制备核取代肉桂酰邻氨基苯甲酸化合物的改进方法。 该方法的实例是在惰性溶剂介质中，在摩尔过量的哌啶存在下，3-羟基-4-甲氧基苯甲醛与2-羧基丙二酸的反应，得到高纯度的中间盐沉淀物，盐用 酸性试剂洗脱N-（3-羟基-4-甲氧基肉桂酰）邻氨基苯甲酸产物。

    1,3-Disubstituted imidazoles
    3.
    发明授权
    1,3-Disubstituted imidazoles 失效
    1,3-二取代的咪唑

    公开(公告)号：US4469865A

    公开(公告)日：1984-09-04

    申请号：US423332

    申请日：1982-09-24

    申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    IPC分类号： C07D233/60 ,  C07D233/61 ,  C07D521/00

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： 1,3-Disubstituted imidazoles of the general formula (I): ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, Y is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or an dialkoxymethyl group having 3 to 13 carbon atoms, Z is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, n is zero or 1. The said compounds are intermediates for producing the imidazole derivatives of the general formula (V) above which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutical agents for treatment of diseases caused by thromboxane A.sub.2.

    摘要翻译： 通式（I）的1,3-二取代咪唑：其中A和B可以相同或不同，并且各自是具有1至8个碳的直链或支链亚烷基或亚烯基 原子，Y为碳原子数2〜10的酰基，碳原子数2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基，Z为氰基或碳原子数为2〜7的烷氧基羰基， X是卤素原子，n是0或1.所述化合物是用于生产上述通式（V）的咪唑衍生物的中间体，其具有对凝血恶烷合成酶的强和特异性抑制作用，因此可用作治疗药物 血栓素A2引起的疾病。

    Imidazole derivatives
    4.
    发明授权
    Imidazole derivatives 失效
    咪唑衍生物

    公开(公告)号：US4461905A

    公开(公告)日：1984-07-24

    申请号：US413204

    申请日：1982-08-30

    申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Ryoji Yamamoto ,  Hiromu Harada

    IPC分类号： C07D233/54 ,  C07D233/60 ,  C07D521/00

    CPC分类号： C07D233/64 ,  C07D231/12 ,  C07D233/56 ,  C07D249/08

    摘要： The imidazole derivatives of the general formula: ##STR1## wherein A and B may be the same or different, and each is a straight- or branched-chain alkylene or alkenylene group having 1 to 8 carbon atoms, D is an acyl group having 2 to 10 carbon atoms, an alkoxycarbonyl group having 2 to 7 carbon atoms or a dialkoxymethyl group having 3 to 13 carbon atoms, Q is a cyano group or an alkoxycarbonyl group having 2 to 7 carbon atoms, X is a halogen atom, Z is ##STR2## (wherein E is a hydrogen atom, a halogen atom, an alkyl group having 1 to 6 carbon atoms or an alkoxy group having 1 to 6 carbon atoms, Y is an oxygen atom or a sulfur atom and may be connected with either A or B), n is zero or 1, with the proviso that n is 1 when Y connects with B.These compounds are novel compounds and are useful as intermediates in producing 1-substituted imidazole derivatives which possess strong and specific inhibitory effects on thromboxane synthetase and thus are useful as therapeutically active agents for treatment of diseases caused by thromboxane A.sub.2.

    摘要翻译： 具有以下通式的咪唑衍生物：其中A和B可以相同或不同，并且各自是具有1至8个碳原子的直链或支链亚烷基或亚烯基，D是具有2个 碳原子数为2〜7的烷氧基羰基或碳原子数3〜13的二烷氧基甲基，Q为氰基或碳原子数2〜7的烷氧基羰基，X为卤素原子，Z为< IMAGE>（其中E是氢原子，卤素原子，具有1至6个碳原子的烷基或具有1至6个碳原子的烷氧基，Y是氧原子或硫原子，并且可以与A 或B），n为0或1，条件是当Y与B连接时n为1。这些化合物是新化合物，可用作生产1-取代咪唑衍生物的中间体，其具有对凝血恶烷合成酶的强和特异性抑制作用 因此可用作治疗活性剂 治疗由血栓素A2引起的疾病。

    Novel renin inhibitory amino acid derivatives
    10.
    发明授权
    Novel renin inhibitory amino acid derivatives 失效
    新型肾素抑制性氨基酸衍生物

    公开(公告)号：US4857650A

    公开(公告)日：1989-08-15

    申请号：US879741

    申请日：1986-06-27

    申请人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

    发明人： Kinji Iizuka ,  Tetsuhide Kamijo ,  Tetsuhiro Kubota ,  Kenji Akahane ,  Hideaki Umeyama ,  Yoshiaki Kiso

    IPC分类号： C07D233/54 ,  C07D233/61 ,  C07D233/64 ,  C07D403/12

    CPC分类号： C07D233/64 ,  C07D403/12 ,  Y10S530/86

    摘要： New renin inhibitory amino acid derivatives represented by formula (I): ##STR1## wherein A represents an alkoxycarbonyl group having 2 to 7 carbon atoms, ##STR2## wherein R.sup.1 and R.sup.2 are defined as in the specification below or ##STR3## wherein X and Y are defined as in the specification herein below, n represents zero or one, Z represents --O-- or --NH--, and R represents a straight- or branched chain alkyl group having 1 to 7 carbon atoms, and pharmaceutically acceptable salts thereof, useful as a therapeutic agent are disclosed. The amino acid derivatives have a renin inhibitory effect when administered orally and are useful for treatment of hypertension, especially renin-associated hypertension.

    摘要翻译： 由式（I）表示的新的肾素抑制性氨基酸衍生物：其中A表示碳原子数2〜7的烷氧基羰基，其中R1和R2如下面的说明书所定义， 其中X和Y如下面的说明书中所定义，n表示0或1，Z表示-O-或-NH-，R表示具有1至7个碳原子的直链或支链烷基， 公开了可用作治疗剂的盐。 当口服给药时，氨基酸衍生物具有肾素抑制作用，可用于治疗高血压，特别是肾素相关性高血压。