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    HETERODIAZINONE DERIVATIVES
    2.
    发明公开
    HETERODIAZINONE DERIVATIVES 有权
    杂芳二酮衍生物

    公开(公告)号：EP1153922A1

    公开(公告)日：2001-11-14

    申请号：EP00902953.9

    申请日：2000-02-15

    申请人： Eisai Co., Ltd.

    发明人： ITO, Koichi ,  KITAZAWA, Noritaka ,  NAGATO, Satoshi ,  KAJIWARA, Akiharu ,  FUKUSHIMA, Tatsuto ,  HATAKEYAMA, Shinji ,  HANADA, Takahisa ,  UENO, Masataka ,  UENO, Kohshi ,  KAWANO, Koki

    IPC分类号： C07D253/06 ,  C07D273/04 ,  C07D285/18 ,  C07D413/04 ,  A61K31/53 ,  A61K31/5395 ,  A61K31/549 ,  A61P25/00

    CPC分类号： C07D271/113 ,  A61K31/53 ,  A61K31/5395 ,  A61K31/549 ,  C07D249/12 ,  C07D285/16 ,  C07D413/04 ,  C07D413/06 ,  C07D413/12 ,  C07D413/14

    摘要： The present invention provides a novel compound having an excellent 2-amino-3-hydroxy-5-methyl-4-isoxazole propionic acid (AMPA) receptor antagonistic action, particularly a therapeutic, preventing and ameliorating action useful for cerebral ischemia, cerebrospinal injuries, Alzheimer's disease, Parkinson's disease, amyotrophic lateral sclerosis, Huntington's chorea, epilepsy, pain, spastic paralysis, multiple sclerosis etc. That is, the present invention provides a heterodiazinon compound represented by the following formula (I), a pharmacologically acceptable salt thereof or hydrates thereof.
       Wherein A represents an oxygen atom, a sulfur atom or a group represented by the formula >NR 3 (wherein R 3 represents hydrogen atom or a lower alkyl group);

    R 1 and R 2 are the same as or different from each other and each represents an optionally substituted aryl group, an optionally substituted heteroaryl group, an optionally substituted aralkyl group, an optionally substituted heteroaryl alkyl group, an optionally substituted aryl alkenyl group, an optionally substituted heteroaryl alkenyl group, an optionally substituted piperidyl group, an optionally substituted piperazinyl group; a morpholinyl group, an optionally substituted lower cycloalkyl group, a tetrahydrofuranyl group, a tetrahydropyranyl group, an adamantyl group, an optionally substituted amino group or an optionally substituted amide group; and
    R 4 and R 5 are the same as or different from each other and each represents hydrogen atom, hydroxy, a halogen atom, nitrile group, nitro group, a lower alkyl group, an aryl group or a heteroaryl group,
       provided that the compounds represented by the following formula (II):
    (wherein R 11 and R 12 are the same as or different from each other and each represents hydrogen atom, fluorine, chlorine, bromine, iodine, a C1-C2 fluoroalkyl group, a C1-C2 chloroalkyl group, a C1-C2 bromoalkyl group, a C1-C6 alkyl group, a C3-C6 cycloalkyl group, a C7-C9 aralkyl group, phenyl group, a C1-C6 alkoxy group, a C1-C6 alkylthio group, a C1-C6 alkylsulfinyl group, a C7-C9 aralkoxy group, phenoxy group, phenylthio group, phenylsulfonyl group, alkali metal carboxylate C2-C5 alkoxycarbonyl group or a group represented by the formula -N(R 15 )R 16 (wherein R 15 and R 16 are the same as or different from each other and each represents hydrogen atom or a C1-C2 alkyl group); and
    R 13 and R 14 are the same as or different from each other and each represents a C 1-4 alkylsulfonyl group, nitro group, a group represented by the formula -OCH n X 3-n (wherein X represents fluorine, chlorine, bromine or iodine; and n is any of integers 1 to 3) or a group having the same meanings as the definitions of R 11 and R 12 ) are excluded.

    摘要翻译： 本发明提供具有优异的2-氨基-3-羟基-5-甲基-4-异恶唑丙酸（AMPA）受体拮抗作用，特别是对脑缺血，脑脊髓损伤等有用的治疗，预防和改善作用的新型化合物。 阿尔茨海默病，帕金森病，肌萎缩性侧索硬化，亨廷顿舞蹈症，癫痫，疼痛，痉挛性麻痹，多发性硬化症等。即，本发明提供由下式（I）表示的异二嗪酮化合物，其药理学上可接受的盐或水合物 它们。 其中A代表氧原子，硫原子或由式> NR3代表的基团（其中R3代表氢原子或低级烷基）。 R1和R2彼此相同或不同，并且各自表示任选取代的芳基，任选取代的杂芳基，任选取代的芳烷基，任选取代的杂芳基烷基，任选取代的芳基烯基，任选取代的 杂芳基链烯基，任选取代的哌啶基，任选取代的哌嗪基; 吗啉基，任选取代的低级环烷基，四氢呋喃基，四氢吡喃基，金刚烷基，任选取代的氨基或任选取代的酰胺基; R4和R5彼此相同或不同，各自代表氢原子，羟基，卤原子，腈基，硝基，低级烷基，芳基或杂芳基，条件是由 （II）表示：式中，R 11和R 12相同或不同，表示氢原子，氟，氯，溴，碘，碳数1〜2的氟烷基，碳数1〜2的氯烷基， C1-C2溴代烷基，C1-C6烷基，C3-C6环烷基，C7-C9芳烷基，苯基，C1-C6烷氧基，C1-C6烷硫基，C1-C6烷基亚磺酰基 ，C7-C9芳烷氧基，苯氧基，苯硫基，苯基磺酰基，碱金属羧酸盐C2-C5烷氧基羰基或由式-N（R15）R16表示的基团（其中R15和R16相同或不同于 彼此并且各自表示氢原子或C1-C2烷基）;并且R13和R14与上述相同 或者彼此不同，并且各自表示C1-4烷基磺酰基，硝基，由式-OCH n X 3-n表示的基团（其中X表示氟，氯，溴或碘; 并且n是整数1至3中的任一个）或具有与R11和R12的定义相同的含义的基团）被排除。