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    Cyclic aminophenylacetic acid derivatives, process for preparing the same and immune response modulator having the same as an effective ingredient
    1.
    发明授权
    Cyclic aminophenylacetic acid derivatives, process for preparing the same and immune response modulator having the same as an effective ingredient 失效
    环状氨基苯乙酸衍生物，其制备方法和具有与有效成分相同的免疫应答调节剂

    公开(公告)号：US5359076A

    公开(公告)日：1994-10-25

    申请号：US956012

    申请日：1992-12-09

    申请人： Yasushi Kohno ,  Katsuya Awano ,  Takayoshi Ishizaki ,  Eisuke Kojima ,  Shinji Kudoh ,  Yasuhiko Sakoe ,  Koji Saito

    发明人： Yasushi Kohno ,  Katsuya Awano ,  Takayoshi Ishizaki ,  Eisuke Kojima ,  Shinji Kudoh ,  Yasuhiko Sakoe ,  Koji Saito

    IPC分类号： A61K31/47 ,  A61P29/00 ,  A61P37/00 ,  A61P37/02 ,  C07C311/21 ,  C07C317/48 ,  C07C323/63 ,  C07C331/14 ,  C07D215/12 ,  C07D215/14 ,  C07D215/18 ,  C07D215/22 ,  C07D215/26 ,  C07D215/36 ,  C07D215/40 ,  C07D215/48 ,  C07D498/04 ,  C07D498/06 ,  C07F7/08 ,  C07D215/24 ,  C07D215/06 ,  C07D215/16

    CPC分类号： C07D215/14 ,  C07C311/21 ,  C07C317/48 ,  C07C323/63 ,  C07C331/14 ,  C07D215/12 ,  C07D215/18 ,  C07D215/36 ,  C07D215/40 ,  C07D215/48 ,  C07F7/0812

    摘要： The present invention provides novel cyclic aminophenylacetic acid derivatives having modulating action on immune response, their optical isomers, their salts and their preparative processes, and therapeutic agents for autoimmune diseases containing them as effective ingredients, the cyclic aminophenylacetic acid derivatives being represented by a general formula (1) ##STR1## wherein R and R.sup.1 each independently denotes hydrogen atom or lower alkyl group having 1 to 3 carbon atoms, R.sup.2 denotes a phenyl group (which may be substituted with 1 to 3 groups of halogen atom, methoxy group or their combinations) or trifluoromethyl group, and X denotes a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms, lower alkoxy group having 1 to 3 carbon atoms, cyano group, thiocyano group, trimethylsilylethinyl group, phenyl group (which may be substituted with halogen atom, methoxy group, methyl group or their combinations), carbamoyl group, carboxyl group, lower alkoxycarbonyl group having 1 to 3 carbon atoms, acetyl group, benzoyl group, nitro group, amino group, lower alkanoylamino group having 1 to 3 carbon atoms, benzoylamino group which may be substituted, phenylsulfonylamino group which may be substituted, lower alkylthio group having 1 to 3 carbon atoms, lower alkylsulfinyl group having 1 to 3 carbon atoms, lower alkylsulfonyl group having 1 to 3 carbon atoms or halogen atom.

    摘要翻译： PCT No.PCT / JP92 / 00476 Sec。 371日期：1992年12月9日 102（e）日期1992年12月9日PCT提交1992年4月15日PCT公布。 公开号WO92 / 18482 本发明提供了具有对免疫应答的调节作用的新型环状氨基苯乙酸衍生物，其旋光异构体，其盐及其制备方法，以及含有它们作为有效成分的自身免疫性疾病的治疗剂，环状氨基苯乙酸 衍生物由通式（1）表示，其中R和R 1各自独立地表示氢原子或具有1至3个碳原子的低级烷基，R 2表示苯基（可被1至3个取代基取代） 卤素原子，甲氧基或它们的组合基团）或三氟甲基，X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，氰基，硫氰基，三甲基甲硅烷基乙炔基 ，苯基（其可以被卤素原子，甲氧基，甲基或它们的组合取代），氨基甲酰基，羧基，低级烷氧基 具有1至3个碳原子的酰基，乙酰基，苯甲酰基，硝基，氨基，具有1至3个碳原子的低级烷酰基氨基，可被取代的苯甲酰基氨基，可被取代的苯基磺酰基氨基，具有1个 3个碳原子，具有1至3个碳原子的低级烷基亚磺酰基，具有1至3个碳原子的低级烷基磺酰基或卤素原子。

    Cyclic anthranilic acid derivatives
    2.
    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。

    Cyclic anthranilic acid derivatives and process for their preparation
    4.
    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.

    Therapeutic agents of metabolic bone disease
    5.
    发明授权
    Therapeutic agents of metabolic bone disease 失效
    代谢性骨髓疾病治疗药物

    公开(公告)号：US5124325A

    公开(公告)日：1992-06-23

    申请号：US536007

    申请日：1990-06-08

    申请人： Eisuke Kojima ,  Koji Saito

    发明人： Eisuke Kojima ,  Koji Saito

    IPC分类号： A61K31/47 ,  A61K31/535 ,  A61K31/54

    CPC分类号： A61K31/535 ,  A61K31/47 ,  A61K31/54

    摘要： New use of cyclic anthranilic acid derivatives of the following formula, ##STR1## wherein R.sup.1, R.sup.2 and R.sup.3 each independently indicate a hydrogen atom, chlorine 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, benzoymethyl group which may be substituted, methylthio group, phenylethnyl 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 benzoyl 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, oxygen atom, sulfur atom, sulfinyl group or sulfonyl group, their acid or alkali salts thereof as therapeutic agents for metabolic bone diseases is described.

    Cyclic anthranililc acid carboxylic acid derivatives and medical therapeutic use thereof
    6.
    发明授权
    Cyclic anthranililc acid carboxylic acid derivatives and medical therapeutic use thereof 失效
    环丙磺酸酸性羧酸衍生物及其医疗治疗用途

    公开(公告)号：US5112836A

    公开(公告)日：1992-05-12

    申请号：US538785

    申请日：1990-06-15

    申请人： Yasushi Kohno ,  Eisuke Kojima

    发明人： Yasushi Kohno ,  Eisuke Kojima

    IPC分类号： A61K31/47 ,  A61P29/00 ,  A61P37/00 ,  C07D215/50 ,  C07D215/52 ,  C07D471/06

    CPC分类号： C07D471/06 ,  C07D215/50 ,  C07D215/52

    摘要： Cyclic anthranilic acid carboxylic acid derivatives of the following formula, ##STR1## wherein R.sup.1 is hydrogen atom, carboxyl group, lower alkoxy carbonyl group having 1 to 3 carbon atoms, or phenyl group which may be substituted, r.sup.2 and R.sup.4 are each independently a hydrogen atom, lower alkyl group having 1 to 3 carbon atoms or benzyl group, R.sup.3 is a hydrogen atom, halogen atom, nitro group, amino group, cyano group, carbamoyl group, carboxyl group, lower alkanoylamino group having 1 to 4 carbon atoms, benzoylamino group, lower alkylsulfonylamino group having 1 to 3 carbon atoms or phenylsulfonylamino group which may be substituted by methyl group; the acid addition or alkali salts thereof, are useful as drugs treat autoimmune diseases, antirheumatic agents and therapeutic or prophylactic agents to treat metabolic bone diseases.

    Cyclic anthranilic acid derivatives and process for their preparation
    7.
    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。