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    1-2-dihydroquinoline derivative having glucocorticoid receptor binding activity
    3.
    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 phenylamino lower alkyl group and ester-introduced phenyl group as substituents
    4.
    发明授权
    1,2-dihydroquinoline derivative having substituted phenylamino lower alkyl group and ester-introduced phenyl group as substituents 失效
    具有取代苯基氨基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：US08008498B2

    公开(公告)日：2011-08-30

    申请号：US12312396

    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 represents 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, a nitro group or a cyano 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; 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; R3和R4可以相同或不同，代表氢原子或低级烷基; 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，硝基或氰基; 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; P表示0,1,2或3。

    1,2-dihydroquinoline derivative having (substituted phenyl or substituted heterocyclic) carbonyloxy lower alkyl group and ester-introduced phenyl group as substituents
    5.
    发明授权
    1,2-dihydroquinoline derivative having (substituted phenyl or substituted heterocyclic) carbonyloxy lower alkyl group and ester-introduced phenyl group as substituents 失效
    具有（取代的苯基或取代的杂环）羰基氧基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：US08008497B2

    公开(公告)日：2011-08-30

    申请号：US12312393

    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, a nitro group or a cyano 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 benzene ring or a heterocyclic ring; 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，硝基或氰基; 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表示苯环或杂环; P表示0,1,2或3。

    1,2,3,4-tetrahydroquinoxaline compound with a phenyl group substituent having a sulfonic acid ester structure or a sulfonic acid amide structure introduced therein and having glucocorticoid receptor-binding activity
    8.
    发明授权
    1,2,3,4-tetrahydroquinoxaline compound with a phenyl group substituent having a sulfonic acid ester structure or a sulfonic acid amide structure introduced therein and having glucocorticoid receptor-binding activity 失效
    具有引入其中具有磺酸酯结构或磺酰胺结构的苯基取代基的1,2,3,4-四氢喹喔啉化合物，并具有糖皮质激素受体结合活性

    公开(公告)号：US08193187B2

    公开(公告)日：2012-06-05

    申请号：US12451653

    申请日：2008-05-29

    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： A61K31/495

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

    摘要： The compounds represented in general formula (1) or a salt thereof are useful for glucocorticoid receptor modulators. In the formula, R1 represents a lower alkyl group, a lower cycloalkyl group, an aryl group and the like; R2 represents a hydrogen atom, a lower alkyl group and the like; R3 represents a hydrogen atom, a lower alkyl group and the like; R4 and R5 represent a hydrogen atom, a lower alkyl group and the like; R6 represents a hydrogen atom, a lower alkyl group and the like; R7 represents a hydrogen atom, a lower alkyl group, a lower alkenyl group and the like; W represents an oxygen atom, a sulfur atom, NR8 and the like; R8 represents a hydrogen atom, a lower alkyl group and the like; X represents an oxygen atom or a sulfur atom; Y represents a lower alkylene group and the like; Z represents an oxygen atom, a sulfur atom, NR9, OCO or OSO2; R9 represents a hydrogen atom, a lower alkyl group and the like respectively.

    摘要翻译： 通式（1）表示的化合物或其盐可用于糖皮质激素受体调节剂。 在该式中，R 1表示低级烷基，低级环烷基，芳基等; R2表示氢原子，低级烷基等; R3表示氢原子，低级烷基等; R4和R5代表氢原子，低级烷基等; R6表示氢原子，低级烷基等; R7表示氢原子，低级烷基，低级烯基等; W表示氧原子，硫原子，NR 8等; R8表示氢原子，低级烷基等; X表示氧原子或硫原子; Y表示低级亚烷基等; Z表示氧原子，硫原子，NR 9，OCO或OSO 2; R 9分别表示氢原子，低级烷基等。