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    Quinazoline-3-alkanoic acid derivatives, their salts and their preparation processes
    1.
    发明授权
    Quinazoline-3-alkanoic acid derivatives, their salts and their preparation processes 失效
    喹诺酮-3-碱性酸衍生物及其制备方法

    公开(公告)号：US5234928A

    公开(公告)日：1993-08-10

    申请号：US721610

    申请日：1991-07-17

    申请人： Shizuyoshi Fujimori ,  Michiro Ohnota ,  Yoshihiro Hirata ,  Koji Murakami

    发明人： Shizuyoshi Fujimori ,  Michiro Ohnota ,  Yoshihiro Hirata ,  Koji Murakami

    IPC分类号： A61K31/505 ,  A61K31/517 ,  A61P3/08 ,  A61P3/10 ,  A61P7/02 ,  A61P43/00 ,  C07D239/80 ,  C07D239/95 ,  C07D239/96 ,  C07D401/06 ,  C07D403/04 ,  C07D403/06 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  C07D417/04 ,  C07D417/06 ,  C07D491/056 ,  C07D521/00 ,  C12N9/99

    CPC分类号： C07D231/12 ,  C07D233/56 ,  C07D239/80 ,  C07D239/95 ,  C07D239/96 ,  C07D249/08 ,  C07D401/06 ,  C07D403/04 ,  C07D405/06 ,  C07D409/06 ,  C07D413/06 ,  Y02P20/55

    摘要： The present invention relates to quinazoline-3-alkanoic acid derivatives having both an inhibitory effect on platelet aggregation and a hindering effect on aldose reductase together, represented by a general formula [I] ##STR1## [wherein R is hydrogen or a protecting group for carboxyl group, R.sup.1 is a lower alkyl group, alkenyl group, alkinyl group, lower alkoxy group, lower alkylthio group, halogen, phenyl group (this phenyl group may be substituted by one to three of lower alkyls, lower alkoxys, halogens, trifluoromethyls, carboxyethylenes or ethoxycarbonylethylenes, naphthyl group, heterocycle (this heterocycle may be substituted by one to three of lower alkyls), cycloalkyl group or benzoyl group (this benzoyl group may be substituted by lower alkyl or halogen), R.sup.2 and R.sup.3 are identically or differently hydrogens, halogens, lower alkyl groups, lower alkoxy groups, aralkyl groups which may be substituted, nitro groups, imidazolyl groups, imidazolylmethyl groups or ##STR2## (R.sup.4 and R.sup.5 indicate identically or differently hydrogens or lower alkyl groups, or connected with each other to make five- or six-membered heterocycles which may contain other hetero atom, X is carbonyl, thiocarbonyl or methylene group (this methylene group may be substituted by lower alkyl group), A is lower alkylene or lower alkenylene, and n indicates an integer of 1 to 3],their salts, their preparation processes and medicinal drugs containing them.

    摘要翻译： PCT No.PCT / JP90 / 01600 Sec。 371日期：1991年7月17日 102（e）日期1991年7月17日PCT 1990年12月10日PCT PCT。 出版物WO91 / 0902400 日本1991年6月27日。本发明涉及具有对血小板聚集的抑制作用和对醛糖还原酶的阻碍作用的喹唑啉-3-链烷酸衍生物，其通式[I]表示[其中R 是氢或羧基的保护基，R1是低级烷基，烯基，炔基，低级烷氧基，低级烷硫基，卤素，苯基（该苯基可被一至三个低级烷基取代， 低级烷氧基，卤素，三氟甲基，羧乙烯或乙氧基羰基乙烯，萘基，杂环（该杂环可被一至三个低级烷基取代），环烷基或苯甲酰基（该苯甲酰基可被低级烷基或卤素取代），R2 和R 3是相同或不同的氢，卤素，低级烷基，低级烷氧基，可被取代的芳烷基，硝基，咪唑基，咪唑基甲基或IM （R 4和R 5表示相同或不同的氢或低级烷基，或彼此连接以形成可含有其它杂原子的五或六元杂环，X为羰基，硫代羰基或亚甲基（该亚甲基可以 被低级烷基取代），A是低级亚烷基或低级亚烯基，n表示1〜3的整数]，它们的盐，它们的制备方法和含有它们的药用药物。

    Cyclic anthranilic acid derivatives and process for their preparation
    3.
    发明授权
    Cyclic anthranilic acid derivatives and process for their preparation 失效
    环丙磺酸衍生物及其制备方法

    公开(公告)号：US5147874A

    公开(公告)日：1992-09-15

    申请号：US560775

    申请日：1990-07-31

    申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06

    CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

    摘要： An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X is oxygen, sulfur, SO or SO.sub.2 ; the acid or alkali salts thereof and an inert, pharmaceutically acceptable carrier.

    Cyclic anthranilic acid derivatives and process for their preparation
    5.
    发明授权
    Cyclic anthranilic acid derivatives and process for their preparation 失效
    环状邻氨基苯甲酸衍生物及其制备方法

    公开(公告)号：US4956372A

    公开(公告)日：1990-09-11

    申请号：US249996

    申请日：1988-09-27

    申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06

    CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

    摘要： An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X indicates a methylene group; their acid or alkali salts and an inert, pharmaceutically acceptable carrier.

    摘要翻译： 含有下式的环状邻氨基苯甲酸衍生物的抗类风湿性药物组合物，其中R1，R2和R3各自独立地表示氢原子，碳原子数1〜3的低级烷基，碳原子数1〜3的低级烷氧基 氨基，硝基，羟基，磺酰胺基，三氟甲基，氰基，羧基，氨基甲酰基，乙酰基，可被取代的苯甲酰甲基，甲硫基，可被取代的苯基乙炔基，可以被取代的乙炔基 取代的碳原子数1〜3的烷酰基氨基，可以被取代的苯甲酰基氨基，碳原子数1〜3的烷基磺酰基氨基或可被取代的苯基磺酰基氨基; R4和R5各自独立地表示氢原子，具有1至3个碳原子的低级烷基，氰基，羧基，羟甲基，可被取代的苯基或苄基; R6表示氢原子，碳原子数1〜3的低级烷基或苄基; X表示亚甲基; 它们的酸或碱盐和惰性的药学上可接受的载体。

    Substituted benzylthiazolidine-2,4-dione derivatives
    7.
    发明授权
    Substituted benzylthiazolidine-2,4-dione derivatives 失效
    取代的苄基噻唑烷-2,4-二酮衍生物

    公开(公告)号：US06545026B1

    公开(公告)日：2003-04-08

    申请号：US10049905

    申请日：2002-02-20

    申请人： Shizuyoshi Fujimori ,  Koji Murakami ,  Masaki Tsunoda

    发明人： Shizuyoshi Fujimori ,  Koji Murakami ,  Masaki Tsunoda

    IPC分类号： C07D27734

    CPC分类号： C07D277/34

    摘要： The invention provides novel substituted benzylthiazolidine-2,4-dione derivatives which increase the transactivation of receptor as a ligand of human peroxisome proliferator-activated receptor (PPAR) and exhibit the blood glucose-decreasing action and lipid-decreasing action, and a process for preparing them. The invention relates to substituted benzylthiazolidine-2,4-dione derivatives represented by the general formula (1) [wherein A denotes a pyridyl group or cyclohexyl group], their medicinally acceptable salts, their hydrates and a process for preparing them.

    摘要翻译： 本发明提供新的取代的苄基噻唑烷-2,4-二酮衍生物，其增加受体作为人类过氧化物酶体增殖物激活受体（PPAR）的配体的反式激活，并显示出血糖降低作用和降脂作用，以及 本发明涉及由通式（1）表示的取代的苄基噻唑烷-2,4-二酮衍生物[其中A表示吡啶基或环己基]，其药学上可接受的盐，它们的水合物及其制备方法。

    Cyclic anthranilic acid derivatives
    8.
    发明授权
    Cyclic anthranilic acid derivatives 失效
    环状邻氨基苯甲酸衍生物

    公开(公告)号：US5281600A

    公开(公告)日：1994-01-25

    申请号：US929526

    申请日：1992-08-14

    申请人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    发明人： Eisuke Kojima ,  Shizuyoshi Fujimori ,  Katsuya Awano

    IPC分类号： C07D215/48 ,  A61K31/47 ,  A61K31/535 ,  A61K31/538 ,  A61K31/54 ,  A61P29/00 ,  A61P37/00 ,  C07D265/36 ,  C07D279/16 ,  C07D471/06 ,  C07D498/06 ,  C07D513/06 ,  C07D215/12 ,  C07D215/14

    CPC分类号： C07D215/48 ,  C07D265/36 ,  C07D279/16

    摘要： An antirheumatoid pharmaceutical composition containing a cyclic anthranilic acid derivative of the following formula, ##STR1## wherein R.sup.1, and R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, halogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, amino group, nitro group, hydroxy group, sulfonamide group, trifluoromethyl group, cyano group, carboxyl group, carbamoyl group, acetyl group, benzoylmethyl group which may be substituted, methylthio group, phenylethynyl group which may be substituted, ethynyl group which may be substituted, alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted; R.sup.4 and R.sup.5 each independently indicate a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, cyano group, carboxyl group, hydroxymethyl group, phenyl group which may be substituted or benzyl group; R.sup.6 indicates a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group; X is a methylene; the acid or alkali salts thereof and an insert, pharamaceutically acceptable carrier.

    摘要翻译： 含有下式的环状邻氨基苯甲酸衍生物的抗风湿病药物组合物（*化学结构*）（I）其中R1，R2和R3各自独立地表示氢原子，卤素原子，碳原子数1〜3的低级烷基 ，具有1至3个碳原子的低级烷氧基，氨基，硝基，羟基，磺酰胺基，三氟甲基，氰基，羧基，氨基甲酰基，乙酰基，可被取代的苯甲酰甲基，甲硫基，苯基乙炔基 可以被取代的，可以被取代的乙炔基，具有1-3个碳原子的烷酰基氨基，可被取代的苯甲酰氨基，可以被取代的苯磺酰氨基; R4和R5各自独立地表示氢原子，具有1至3个碳原子的低级烷基，氰基，羧基，羟甲基，可被取代的苯基或苄基; R6表示氢原子，碳原子数1〜3的低级烷基或苄基; X是亚甲基; 其酸或碱盐和插入物，药物上可接受的载体。