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    Novel 1-2-Dihydroquinoline Derivative Having Glucocorticoid Receptor Binding Activity
    3.
    发明申请
    Novel 1-2-Dihydroquinoline Derivative Having Glucocorticoid Receptor Binding Activity 有权
    具有糖皮质激素受体结合活性的新型1-2-二氢喹啉衍生物

    公开(公告)号：US20090326009A1

    公开(公告)日：2009-12-31

    申请号：US11992088

    申请日：2006-09-14

    申请人： Mamoru Matsuda ,  Toshiyuki Mori ,  Kenji Kawashima ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Minoru Yamamoto ,  Masatomo Kato ,  Miwa Takai ,  Tomoko Oda

    发明人： Mamoru Matsuda ,  Toshiyuki Mori ,  Kenji Kawashima ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Minoru Yamamoto ,  Masatomo Kato ,  Miwa Takai ,  Tomoko Oda

    IPC分类号： A61K31/4725 ,  C07D215/12 ,  A61K31/47 ,  A61P3/10

    CPC分类号： C07D215/14 ,  C07D215/20 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R4 and R5 represent a hydrogen atom or the like; R6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R7 represents OR8, NR8R9, SR8, S(O)R8 or S(O)2R8, wherein R8 represents an aryl group, a heterocyclic group or the like and R9 represents a hydrogen atom or the like.

    摘要翻译： 本发明的目的是研究新型1,2-二氢喹啉衍生物的合成，并找到衍生物的药理作用。 由通式（1）表示的化合物或其盐在治疗糖皮质激素受体相关疾病方面是有效的。 在该式中，环X表示苯环或吡啶环; R1表示卤素原子，烷基，羟基，烷氧基，氨基等; p表示0〜5的整数， R2表示卤素原子，烷基，羟基等; q表示0〜2的整数， R3表示氢原子，烷基，烯基等; R4和R5表示氢原子等; R6表示氢原子等; A表示亚烷基等; 并且R 7表示OR 8，NR 8 R 9，SR 8，S（O）R 8或S（O）2 R 8，其中R 8表示芳基，杂环基等，R 9表示氢原子等。

    1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity
    4.
    发明授权
    1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity 有权
    具有糖皮质激素受体结合活性的1-2-二氢喹啉衍生物

    公开(公告)号：US08017775B2

    公开(公告)日：2011-09-13

    申请号：US11992088

    申请日：2006-09-14

    申请人： Mamoru Matsuda ,  Toshiyuki Mori ,  Kenji Kawashima ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Minoru Yamamoto ,  Masatomo Kato ,  Miwa Takai ,  Tomoko Oda

    发明人： Mamoru Matsuda ,  Toshiyuki Mori ,  Kenji Kawashima ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Minoru Yamamoto ,  Masatomo Kato ,  Miwa Takai ,  Tomoko Oda

    IPC分类号： C07D215/38

    CPC分类号： C07D215/14 ,  C07D215/20 ,  C07D215/48 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D409/12 ,  C07D417/12

    摘要： An object of the present invention is to study synthesis of a novel 1,2-dihydroquinoline derivative and to find a pharmacological action of the derivative. A compound represented by the general formula (1) or a salt thereof is effective in the treatment of a glucocorticoid receptor-related disease. In the formula, the ring X represents a benzene ring or a pyridine ring; R1 represents a halogen atom, an alkyl group, a hydroxy group, an alkoxy group, an amino group or the like; p represents an integer of 0 to 5; R2 represents a halogen atom, an alkyl group, a hydroxy group or the like; q represents an integer of 0 to 2; R3 represents a hydrogen atom, an alkyl group, an alkenyl group or the like; R4 and R5 represent a hydrogen atom or the like; R6 represents a hydrogen atom or the like; A represents an alkylene group or the like; and R7 represents OR8, NR8R9, SR8, S(O)R8 or S(O)2R8, wherein R8 represents an aryl group, a heterocyclic group or the like and R9 represents a hydrogen atom or the like.

    摘要翻译： 本发明的目的是研究新型1,2-二氢喹啉衍生物的合成，并找到衍生物的药理作用。 由通式（1）表示的化合物或其盐在治疗糖皮质激素受体相关疾病方面是有效的。 在该式中，环X表示苯环或吡啶环; R1表示卤素原子，烷基，羟基，烷氧基，氨基等; p表示0〜5的整数， R2表示卤素原子，烷基，羟基等; q表示0〜2的整数， R3表示氢原子，烷基，烯基等; R4和R5表示氢原子等; R6表示氢原子等; A表示亚烷基等; 并且R 7表示OR 8，NR 8 R 9，SR 8，S（O）R 8或S（O）2 R 8，其中R 8表示芳基，杂环基等，R 9表示氢原子等。

    1,2-dihydroquinoline derivative having substituted phenylchalcogeno lower alkyl group and ester-introduced phenyl group as substituents
    7.
    发明授权
    1,2-dihydroquinoline derivative having substituted phenylchalcogeno lower alkyl group and ester-introduced phenyl group as substituents 有权
    具有取代的苯基硫代低级烷基和酯引入的苯基作为取代基的1,2-二氢喹啉衍生物

    公开(公告)号：US08008496B2

    公开(公告)日：2011-08-30

    申请号：US12312392

    申请日：2007-11-14

    申请人： Mamoru Matsuda ,  Masato Nagatsuka ,  Toshiyuki Mori ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    发明人： Mamoru Matsuda ,  Masato Nagatsuka ,  Toshiyuki Mori ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    IPC分类号： C07D215/38

    CPC分类号： C07D401/12 ,  C07D215/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

    摘要： The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or a nitro group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a chalcogen atom; and P represents 0, 1, 2 or 3.

    摘要翻译： 通式（1）表示的化合物及其盐可用于糖皮质激素受体调节剂。 R1表示氢原子或低级烷基; R2表示氢原子或低级烷基; R 3和R 4可以相同或不同，表示氢原子或低级烷基; R5表示氢原子或低级烷基; R6表示卤素原子，低级烷基，羟基，低级烷氧基或硝基; X表示-C（O） - ， - C（O）NR 8 - ， - S（O）2等） R 7和/或R 8可以相同或不同，表示氢原子，可以具有取代基的低级烷基，可以具有取代基的芳基，可以具有取代基的杂环基，低级烷氧基 可以具有取代基等; Y表示低级亚烷基; Z表示硫属原子; P表示0,1,2或3。

    NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED PHENYLCHALCOGENO LOWER ALKYL GROUP AND ESTER- INTRODUCED PHENYL GROUP AS SUBSTITUENTS
    8.
    发明申请
    NOVEL 1,2-DIHYDROQUINOLINE DERIVATIVE HAVING SUBSTITUTED PHENYLCHALCOGENO LOWER ALKYL GROUP AND ESTER- INTRODUCED PHENYL GROUP AS SUBSTITUENTS 有权
    具有取代的苯乙烯基低级烷基的新的1,2-二氢喹啉衍生物和引入的苯基作为取代基

    公开(公告)号：US20100056504A1

    公开(公告)日：2010-03-04

    申请号：US12312392

    申请日：2007-11-14

    申请人： Mamoru Matsuda ,  Masato Nagatsuka ,  Toshiyuki Mori ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    发明人： Mamoru Matsuda ,  Masato Nagatsuka ,  Toshiyuki Mori ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    IPC分类号： A61K31/541 ,  C07D279/06 ,  C07D413/12 ,  C07D215/38 ,  A61K31/47 ,  A61K31/5377 ,  A61P25/00

    CPC分类号： C07D401/12 ,  C07D215/14 ,  C07D405/12 ,  C07D409/12 ,  C07D409/14 ,  C07D417/12

    摘要： The compounds represented in general formula (1) and a salt thereof are useful for glucocorticoid receptor modulator. The R1 represents a hydrogen atom or a lower alkyl group; R2 represents a hydrogen atom or a lower alkyl group; R3 and R4 may be the same or different and represent a hydrogen atom or a lower alkyl group; R5 represents a hydrogen atom or a lower alkyl group; R6 represents a halogen atom, a lower alkyl group, a hydroxy group, a lower alkoxy group or a nitro group; X represents —C(O)—, —C(O)NR8—, —S(O)2— and the like; R7 and/or R8 may be the same or different and represent a hydrogen atom, a lower alkyl group which may have a substituent, an aryl group which may have a substituent, a heterocyclic group which may have a substituent, a lower alkoxy group which may have a substituent and the like; Y represents a lower alkylene group; Z represents a chalcogen atom; and P represents 0, 1, 2 or 3.

    摘要翻译： 通式（1）表示的化合物及其盐可用于糖皮质激素受体调节剂。 R1表示氢原子或低级烷基; R2表示氢原子或低级烷基; R 3和R 4可以相同或不同，表示氢原子或低级烷基; R5表示氢原子或低级烷基; R6表示卤素原子，低级烷基，羟基，低级烷氧基或硝基; X表示-C（O） - ， - C（O）NR 8 - ， - S（O）2等） R 7和/或R 8可以相同或不同，表示氢原子，可以具有取代基的低级烷基，可以具有取代基的芳基，可以具有取代基的杂环基，低级烷氧基 可以具有取代基等; Y表示低级亚烷基; Z表示硫属原子; P表示0,1,2或3。

    Method for treating a homeostasis-related disease or glaucoma by administering a 1,2,3,4-tetrahyroquinoxaline compound
    10.
    发明授权
    Method for treating a homeostasis-related disease or glaucoma by administering a 1,2,3,4-tetrahyroquinoxaline compound 失效
    通过施用1,2,3,4-四氢喹喔啉化合物治疗体内平衡相关疾病或青光眼的方法

    公开(公告)号：US08569493B2

    公开(公告)日：2013-10-29

    申请号：US13364680

    申请日：2012-02-02

    申请人： Mamoru Matsuda ,  Toshiyuki Mori ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    发明人： Mamoru Matsuda ,  Toshiyuki Mori ,  Masato Nagatsuka ,  Sachiko Kobayashi ,  Masatomo Kato ,  Miwa Takai

    IPC分类号： C07D471/00

    CPC分类号： C07D241/44 ,  C07D405/12 ,  C07D409/12

    摘要： A method for preventing or treating a metabolic disorder, an inflammatory disease, an autoimmune disease, an allergic disease, a central nervous system disease, a cardiovascular disease, a homeostasis-related disease or glaucoma, involving administering a compound or a salt thereof, the compound having the following formula (1): wherein R1 represents alkyl, cycloalkyl, aryl, heterocyclic or aralkyl; R7 represents cycloalkyl, aryl or heterocyclic; W represents oxygen or NR8, Y represents alkylene, Z represents oxygen, sulfur, OCO or NR9; R2, R3, R4, R6, R8 and R9 represent hydrogen or alkyl.

    摘要翻译： 一种预防或治疗代谢紊乱，炎性疾病，自身免疫性疾病，过敏性疾病，中枢神经系统疾病，心血管疾病，体内平衡相关疾病或青光眼的方法，涉及其化合物或其盐的给药， 具有下式（1）的化合物：其中R 1表示烷基，环烷基，芳基，杂环或芳烷基; R 7表示环烷基，芳基或杂环; W表示氧或NR8，Y表示亚烷基，Z表示氧，硫，OCO或NR9; R2，R3，R4，R6，R8和R9表示氢或烷基。