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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。

    LYMPHOCYTIC ACTIVATION INHIBITOR AND REMEDIAL AGENT FOR AUTOIMMUNE DISEASE
    3.
    发明公开
    LYMPHOCYTIC ACTIVATION INHIBITOR AND REMEDIAL AGENT FOR AUTOIMMUNE DISEASE 审中-公开
    LYMPHOZYTEN-AKTIVIERUNGSHEMMER在MITTEL ZUR BEHANDLUNG VON AUTOIMMUNKRANKHEITEN

    公开(公告)号：EP1430894A1

    公开(公告)日：2004-06-23

    申请号：EP02798032.5

    申请日：2002-09-05

    申请人： Eisai Co. Ltd

    发明人： HANADA, Takahisa ,  YAMAUCHI, Toshihiko ,  CHIBA, Kenichi ,  OWA, Takashi ,  HIDA, Takayuki ,  MIYAMOTO, Norimasa

    IPC分类号： A61K31/404 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K45/00 ,  A61P1/00 ,  A61P1/02 ,  A61P3/10 ,  A61P5/50 ,  A61P19/02 ,  A61P19/04 ,  A61P25/00 ,  A61P27/02

    CPC分类号： A61K31/4439 ,  A61K31/404 ,  A61K31/416 ,  A61K31/4178 ,  A61K31/427 ,  A61K31/437 ,  A61K45/06

    摘要： A lymphocyte activation inhibitor and a therapeutic agent for an autoimmune disease, each comprising, as an active ingredient, a sulfonamide derivative or sulfonic acid ester derivative represented by the following general formula (I):
    wherein the ring A represents a monocyclic or bicyclic aromatic ring which may be substituted,
    the ring B represents a 6-membered unsaturated hydrocarbon ring or a 6-membered unsaturated heterocyclic ring containing one nitrogen atom as a heteroatom, each of which may be substituted,
    the ring C represents a 5-membered heterocyclic ring containing one or two nitrogen atoms, which may be substituted,
    W represents a single bond or -CH=CH-,
    X represents -N(R 1 )- or an oxygen atom,
    Y represents a carbon atom or a nitrogen atom,
    Z represents -N(R 2 )- or a nitrogen atom, and
    R 1 and R 2 may be identical or different and each represents a hydrogen atom or a lower alkyl group, or a pharmacologically acceptable salt thereof, or a hydrate thereof.

    摘要翻译： 淋巴细胞活化抑制剂和自身免疫性疾病的治疗剂，各自包含作为活性成分的由以下通式（I）表示的磺酰胺衍生物或磺酸酯衍生物：，其中环A表示单环或 可以被取代的双环芳环，环B表示含有一个氮原子作为杂原子的6元不饱和烃环或6元不饱和杂环，其各自可以被取代，环C表示5元环 含有一个或两个氮原子的可以被取代的杂环W表示单键或-CH = CH-，X表示-N（R 1） - 或氧原子，Y表示碳原子或氮 原子，Z表示-N（R 2） - 或氮原子，R 1和R 2可以相同或不同，各自表示氢原子或低级烷基，或药理学上可接受的盐 或其水合物。

    PYRIDAZINONES AND TRIAZINONES AND MEDICINAL USE THEREOF
    4.
    发明公开
    PYRIDAZINONES AND TRIAZINONES AND MEDICINAL USE THEREOF 有权
    TRIAZINONE SOWIE DEREN MEDIZINALE ANWENDUNG

    公开(公告)号：EP1319659A1

    公开(公告)日：2003-06-18

    申请号：EP01970120.0

    申请日：2001-09-17

    申请人： Eisai Co., Ltd.

    发明人： NAGATO, Satoshi ,  KAWANO, Koki ,  ITO, Koichi ,  NORIMINE, Yoshihiko ,  UENO, Kohshi ,  HANADA, Takahisa ,  AMINO, Hiroyuki ,  OGO, Makoto ,  HATAKEYAMA, Shinji ,  UENO, Masataka ,  GROOM, Anthony, John ,  RIVERS, Leanne ,  SMITH, Terence

    IPC分类号： C07D237/04 ,  C07D401/04 ,  C07D237/14 ,  C07D401/06 ,  C07D409/04 ,  C07D491/052 ,  C07D491/048 ,  C07D401/14 ,  C07D405/14 ,  C07D403/14 ,  C07D409/14 ,  C07D417/04 ,  C07D253/06 ,  A61K31/501 ,  A61K31/50 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377

    CPC分类号： C07D237/24 ,  C07D237/14 ,  C07D401/04 ,  C07D491/04

    摘要： The present invention provides a novel compound exhibiting an excellent inhibitory action on AMPA receptor and/or kainate receptor. That is, it provides a compound represented by the following formula, a salt thereof or a hydrate of them.
       In the formula, A 1 , A 2 and A 3 are independent of each other and each represents a C 3-8 cycloalkyl group, a C 3-8 cycloalkenyl group, a 5- to 14-membered non-aromatic heterocyclic group, a C 6-14 aromatic hydrocarbon cyclic group or a 5- to 14-membered aromatic heterocyclic group, each of which may be substituted; Q represents O, S or NH; Z represents C or N; X 1 , X 2 and X 3 are independent of each other and each represents a single bond, an optionally substituted C 1-6 alkylene group, an optionally substituted C 2-6 alkenylene group, an optionally substituted C 2-6 alkynylene group, -NH-, -O-, -NHCO-, -CONH-, -SO 0-2 -, etc.; R 1 and R 2 are independent of each other and each represents a hydrogen atom or an optionally substituted C 1-6 alkyl group, or R 1 and R 2 may be bound together such that CR 2 -ZR 1 forms C=C; and R 3 represents a hydrogen atom or an optionally substituted C 1-6 alkyl group etc., or may be bound to any atom in A 1 or A 3 to form, together with the atom, an optionally substituted C 5-8 hydrocarbon ring or an optionally substituted 5- to 8-membered heterocyclic ring.

    摘要翻译： 本发明提供了对AMPA受体和/或红藻氨酸受体具有优异抑制作用的新化合物。 也就是说，它提供由下式表示的化合物，其盐或它们的水合物。 在该式中，A 1，A 2和A 3彼此独立，各自表示C 3-8环烷基，C 3-8环烯基，5-至14元 非芳族杂环基，C 6-14芳族烃环基或5〜14元芳香族杂环基，各自可以被取代; Q表示O，S或NH; Z表示C或N; X 1，X 2和X 3彼此独立，各自表示单键，任选取代的C 1-6亚烷基，任选取代的C 2-6亚烯基，任选取代的C 2-6 亚炔基，-NH-，-O-，-NHCO-，-CONH-，-SOO 2 - 等; R 1和R 2彼此独立并且各自表示氢原子或任选取代的C 1-6烷基，或者R 1和R 2可以结合在一起，使得CR 2 -ZR 1形成C = C; 并且R 3表示氢原子或任选取代的C 1-6烷基等，或者可以与A 1或A 3中的任何原子结合以与原子一起形成任选取代的C 5 -8烃环或任选取代的5至8元杂环。