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    Processes for producing 7-isoindoline-quinolonecarboxylic acid derivative and its intermediate, as well as salt of 7-isoindoline-quinolonecarboxylic acid derivative, its hydrate and composition comprising the same as active ingredient
    2.
    发明授权
    Processes for producing 7-isoindoline-quinolonecarboxylic acid derivative and its intermediate, as well as salt of 7-isoindoline-quinolonecarboxylic acid derivative, its hydrate and composition comprising the same as active ingredient 有权
    制备7-异二氢吲哚 - 喹啉酮羧酸衍生物及其中间体的方法，以及7-异二氢吲哚 - 喹诺酮羧酸衍生物的盐，其水合物和包含与活性成分相同的组合物

    公开(公告)号：US07371868B2

    公开(公告)日：2008-05-13

    申请号：US11691740

    申请日：2007-03-27

    Applicant: Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Taro Kiyoto

    Inventor： Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Taro Kiyoto

    IPC: C07D231/00 ,  C07D209/02 ,  C07D209/54

    CPC classification number: C07D401/04 ,  A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07F5/025 ,  Y02P20/55

    Abstract: Process for producing a 7-bromoquinolone-carboxylic acid derivative of the following formula or its salt by reacting a 2,4-dibromo-3-hydroxybenzoic acid ester compound of the formula R7a-x to obtain a 3-alkoxy-2,4-dibromobenzoic acid ester, subjecting the 3-alkoxy-2,4-dibromobenzoic acid ester to elimination reaction of the carboxyl-protecting group to obtain a 3-alkoxy-2,4-dibromobenzoic acid, subjecting the 3-alkoxy-2,4-dibromobenzoic acid to ketoesterification reaction to obtain a 3-alkoxy-2,4-dibromobenyolacetic acid ester, reacting the 3-alkoxy-2,4-dibromobenzoylacetic acid ester with an orthoester or an acetal, then reacting the reaction product with a compound of the formula R2—NH or its salt to obtain a 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester and subjecting the 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester to ring-closing reaction, and products thereof.

    Abstract translation: 制备下式的7-溴喹诺酮 - 羧酸衍生物或其盐的方法，其通过使式<β的在线式描述的2,4-二溴-3-羟基苯甲酸酯化合物=“在线式 “end =”lead“？> R 7a -x <？in-line-formula description =”In-line Formulas“end =”tail“？>以获得3-烷氧基-2， 4-二溴苯甲酸酯，使3-烷氧基-2,4-二溴苯甲酸酯与羧基保护基进行消去反应，得到3-烷氧基-2,4-二溴苯甲酸，将3-烷氧基-2,4-二溴苯甲酸 4-二溴苯甲酸进行酮酯化反应，得到3-烷氧基-2,4-二溴苯乙醇酸乙酯，使3-烷氧基-2,4-二溴苯甲酰基乙酸酯与原酸酯或缩醛反应，然后使反应产物与化合物 的式R 2 -NH或其盐，得到2-（3-烷氧基-2,4-二溴苯甲酰基）-3-取代的氨基丙烯酸酯，并使2-（3-烷氧基 - 3,4-二溴苯甲酰基）-3-取代基 氨基丙烯酸酯进行闭环反应，其产物。

    Processes for producing 7-isoindoline-quinolone carboxylic acid derivative and its intermediate, as well as salt of 7-isoindoline-quinolonecarboxylic acid derivative, its hydrate and composition comprising the same as active ingredient
    4.
    发明申请
    Processes for producing 7-isoindoline-quinolone carboxylic acid derivative and its intermediate, as well as salt of 7-isoindoline-quinolonecarboxylic acid derivative, its hydrate and composition comprising the same as active ingredient 审中-公开
    制备7-异二氢吲哚 - 喹诺酮羧酸衍生物及其中间体的方法，以及7-异二氢吲哚 - 喹诺酮羧酸衍生物的盐，其水合物和包含与活性成分相同的组合物

    公开(公告)号：US20050203301A1

    公开(公告)日：2005-09-15

    申请号：US10209078

    申请日：2002-08-01

    Applicant: Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Taro Kiyoto

    Inventor： Katsuji Ojima ,  Tamotsu Takamatsu ,  Kyoko Taya ,  Taro Kiyoto

    IPC: A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07D401/04 ,  C07D471/02 ,  C07D43/02

    CPC classification number: C07D401/04 ,  A61K31/4709 ,  C07C217/48 ,  C07D209/44 ,  C07D215/56 ,  C07F5/025 ,  Y02P20/55

    Abstract: Process for producing a 7-bromoquinolone-carboxylic acid derivative of the following formula or its salt by reacting a 2,4-dibromo-3-hydroxybenzoic acid ester compound of the formula R7a-x to obtain a 3-alkoxy-2,4-dibromobenzoic acid ester, subjecting the 3-alkoxy-2,4-dibromobenzoic acid ester to elimination reaction of the carboxyl-protecting group to obtain a 3-alkoxy-2,4-dibromobenzoic acid, subjecting the 3-alkoxy-2,4-dibromobenzoic acid to ketoesterification reaction to obtain a 3-alkoxy-2,4-dibromobenyolacetic acid ester, reacting the 3-alkoxy-2,4-dibromobenzoylacetic acid ester with an orthoester or an acetal, then reacting the reaction product with a compound of the formula R2a—NH or its salt to obtain a 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester and subjecting the 2-(3-alkoxy-2,4-dibromobenzoyl)-3-substituted aminoacrylic acid ester to ring-closing reaction, and products thereof.

    Abstract translation: 制备下式的7-溴喹诺酮 - 羧酸衍生物或其盐的方法，其通过使式<β的在线式描述的2,4-二溴-3-羟基苯甲酸酯化合物=“在线式 “end =”lead“？> R 7a -x <？in-line-formula description =”In-line Formulas“end =”tail“？>以获得3-烷氧基-2， 4-二溴苯甲酸酯，使3-烷氧基-2,4-二溴苯甲酸酯与羧基保护基进行消去反应，得到3-烷氧基-2,4-二溴苯甲酸，将3-烷氧基-2,4-二溴苯甲酸 4-二溴苯甲酸进行酮酯化反应，得到3-烷氧基-2,4-二溴苯乙醇酸乙酯，使3-烷氧基-2,4-二溴苯甲酰基乙酸酯与原酸酯或缩醛反应，然后使反应产物与化合物 的式R 2a -NH或其盐，得到2-（3-烷氧基-2,4-二溴苯甲酰基）-3-取代的氨基丙烯酸酯，并使2-（3-烷氧基 - 3,4-二溴苯甲酰基）-3-取代基 叔氨基丙烯酸酯进行闭环反应，及其产物。

    ALKYL ETHER DERIVATIVES OR SALTS THEREOF
    7.
    发明申请
    ALKYL ETHER DERIVATIVES OR SALTS THEREOF 有权
    烷基醚衍生物或其盐

    公开(公告)号：US20090111992A1

    公开(公告)日：2009-04-30

    申请号：US12253379

    申请日：2008-10-17

    Applicant: Akihito Saitoh ,  Noboru Iwakami ,  Tamotsu Takamatsu

    Inventor： Akihito Saitoh ,  Noboru Iwakami ,  Tamotsu Takamatsu

    IPC: C07D409/12

    CPC classification number: C07D207/12 ,  C07D405/12 ,  C07D409/12

    Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.

    Abstract translation: 由以下通式表示的烷基醚衍生物：其中R1和R2各自表示一个或多个选自氢原子，卤素原子，烷基，芳基，芳烷基，烷氧基，芳氧基 ，烷硫基，芳硫基，烯基，烯氧基，氨基，烷基磺酰基，芳基磺酰基，氨基甲酰基，杂环基，羟基，羧基，硝基， 氧代基等; R3是烷基氨基，氨基，羟基等; 环A是5元或6元杂芳环或苯环; m和n各自为1至6的整数; p为1〜3的整数，或其盐具有保护神经元的活性，加速神经再生的活性和加速神经突延伸的活性，因此可用作中枢和外周神经疾病的治疗剂。

    Alkyl ether derivatives or salts thereof
    10.
    发明授权
    Alkyl ether derivatives or salts thereof 有权
    烷基醚衍生物或其盐

    公开(公告)号：US08129535B2

    公开(公告)日：2012-03-06

    申请号：US12253379

    申请日：2008-10-17

    Applicant: Akihito Saitoh ,  Noboru Iwakami ,  Tamotsu Takamatsu

    Inventor： Akihito Saitoh ,  Noboru Iwakami ,  Tamotsu Takamatsu

    IPC: C07D409/12

    CPC classification number: C07D207/12 ,  C07D405/12 ,  C07D409/12

    Abstract: An alkyl ether derivative represented by the general formula: wherein each of R1 and R2 represents one or more groups selected from a hydrogen atom, a halogen atom, an alkyl group, an aryl group, an aralkyl group, an alkoxy group, an aryloxy group, an alkylthio group, an arylthio group, an alkenyl group, an alkenyloxy group, an amino group, an alkylsulfonyl group, an arylsulfonyl group, a carbamoyl group, a heterocyclic group, a hydroxyl group, a carboxyl group, a nitro group, an oxo group and the like; R3 is an alkylamino group, an amino group, a hydroxyl group or the like; the ring A is a 5-membered or 6-membered heteroaromatic ring or a benzene ring; each of m and n is an integer of 1 to 6; and p is an integer of 1 to 3, or its salt has activity to protect neurons, activity to accelerate nerve regeneration and activity to accelerate neurite extension and hence is useful as a therapeutic agent for diseases in central and peripheral nerves.

    Abstract translation: 由以下通式表示的烷基醚衍生物：其中R1和R2各自表示一个或多个选自氢原子，卤素原子，烷基，芳基，芳烷基，烷氧基，芳氧基 ，烷硫基，芳硫基，烯基，烯氧基，氨基，烷基磺酰基，芳基磺酰基，氨基甲酰基，杂环基，羟基，羧基，硝基， 氧代基等; R3是烷基氨基，氨基，羟基等; 环A是5元或6元杂芳环或苯环; m和n各自为1至6的整数; p为1〜3的整数，或其盐具有保护神经元的活性，加速神经再生的活性和加速神经突延伸的活性，因此可用作中枢和外周神经疾病的治疗剂。

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