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    PYRIMIDONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME
    1.
    发明公开
    PYRIMIDONE COMPOUNDS AND PHARMACEUTICAL COMPOSITIONS CONTAINING THE SAME 有权
    PYRIMIDONVERBINDUNGEN UND PHARMAZEUTISCHE ZUSAMMENSETZUNGEN，DIEE ENTHALTEN

    公开(公告)号：EP1439176A1

    公开(公告)日：2004-07-21

    申请号：EP02802051.9

    申请日：2002-10-22

    申请人： Eisai Co., Ltd.

    发明人： HARADA, Hitoshi ,  ASANO, Osamu ,  UEDA, Masato ,  MIYAZAWA, Shuhei ,  KOTAKE, Yoshihiko ,  KABASAWA, Yasuhiro ,  YASUDA, Masahiro ,  YASUDA, Nobuyuki

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/513 ,  A61P1/04 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P7/10 ,  A61P9/12 ,  A61P11/06 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P27/02 ,  A61P43/00

    CPC分类号： C07D239/34 ,  A61K31/513

    摘要： The present invention provides a novel pyrimidone compound having an excellent adenosine receptor (A 1 A 2A , A 2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them.
    In the formula, R 1 and R 2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic cyclic hydrocarbon group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R 3 represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, or an alkynyl group having two to six carbon atoms which may be substituted; R 4 represents an C 6-14 aromatic cyclic hydrocarbon group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one unsaturated bond which may be substituted; and R 5 represents an aromatic cyclic hydrocarbon group having six to fourteen which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

    摘要翻译： 本发明提供具有优异的腺苷受体（A1A2A，A2B受体）拮抗作用的新的嘧啶酮化合物。 更具体地，其提供由下式表示的化合物，其盐或它们的溶剂合物。 式中，R 1和R 2彼此相同或不同，表示氢原子，可被取代的碳原子数1〜6的烷基，具有取代基的碳原子数为1〜 可被取代的2至6个碳原子，可被取代的具有2至6个碳原子的炔基，可被取代的具有3至8个碳原子的环烷基，可具有3至8个碳原子的环烯基 可被取代的5至14元非芳族杂环基，可被取代的具有6至14个碳原子的芳族环状烃基，可被取代的5至14元芳族杂环基，酰基 具有1至6个可被取代的碳原子的基团或可被取代的具有1至6个碳原子的烷基磺酰基; R 3表示氢原子，可以被取代的碳原子数为1〜6的烷基，可以被取代的碳原子数为2〜6的烯基或可以具有2〜6个碳原子的炔基 取代; R 4表示可以被取代的具有6〜14个碳原子的C6-14芳香族环状烃基，可以被取代的5〜14元芳香族杂环基或5〜14元非芳香族杂环基， 至少一个可被取代的不饱和键; R 5表示可被取代的具有6〜14个的芳香族环状烃基或可以被取代的5〜14元芳香族杂环基。

    FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES
    5.
    发明公开
    FUSED POLYCYCLIC HETEROCYCLE DERIVATIVES 失效
    VERKNÜPFTE聚合物杂环化合物VERBINDUNGEN

    公开(公告)号：EP0831094A1

    公开(公告)日：1998-03-25

    申请号：EP96920027.8

    申请日：1996-05-31

    申请人： Eisai Co., Ltd.

    发明人： SUGUMI, Hiroyuki ,  NIIJIMA, Jun ,  KOTAKE, Yoshihiko ,  OKADA, Toshimi ,  KAMATA, Jun-ichi ,  YOSHIMATSU, Kentaro ,  NAGASU, Takeshi ,  NAKAMURA, Katsuji ,  UENAKA, Toshimitsu ,  YAMAGUCHI, Atsumi ,  YOSHINO, Hiroshi ,  KOYANAGI, Nozomu ,  KITO, Kyosuke

    IPC分类号： C07D471/06 ,  C07D471/16 ,  C07D487/06 ,  C07D491/16 ,  C07D495/16 ,  C07D498/06 ,  C07D513/06 ,  A61K31/495 ,  A61K31/535 ,  A61K31/54

    CPC分类号： C07D471/06 ,  C07D487/06 ,  C07D513/06

    摘要： Novel fused polycyclic heterocycle derivatives having excellent antitumor effects and a process for producing the same.
    A compound represented by the following general formula (I) or pharmacologically acceptable salts thereof:
    wherein the ring A represents an optionally substituted monocyclic aromatic ring or a dicyclic fused ring in which at least one of the rings is an aromatic ring; the ring B represents pyrrole, 4H-1,4-oxazine, 4H-1,4-thiazine or 4(1H)-pyridone; the ring C represents an optionally substituted, monocyclic or dicyclic fused aromatic ring; and Y represents a group represented by the formula -e-f (wherein e represents a lower alkylene; and f represents amidino, guanidino or amino optionally substituted by optionally hydroxylated or optionally lower-alkylaminated lower alkyl;
       provided that the cases where the rings A and B are both optionally substituted monocyclic aromatic rings are excluded.
    Which has an excellent antitumor activity.

    摘要翻译： 具有优异抗肿瘤效果的新型稠合多环杂环衍生物及其制备方法。 由以下通式（I）表示的化合物或其药理学上可接受的盐：其中环A表示任选取代的单环芳环或二环稠合环，其中至少一个环为芳环; 环B表示吡咯，4H-1,4-恶嗪，4H-1,4-噻嗪或4（1H） - 吡啶酮; 环C表示任选取代的单环或二环稠合芳环; Y表示由式-ef表示的基团（其中e表示低级亚烷基; f表示任选被羟基化或任选低级烷基化的低级烷基取代的脒基，胍基或氨基）;条件是环A和B 均为任选取代的单环芳环，其具有优异的抗肿瘤活性。

    PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF
    8.
    发明公开
    PYRIMIDINE COMPOUND AND MEDICINAL COMPOSITION THEREOF 有权
    玉米饼干精油

    公开(公告)号：EP1439175A1

    公开(公告)日：2004-07-21

    申请号：EP02802050.1

    申请日：2002-10-22

    申请人： Eisai Co., Ltd.

    发明人： HARADA, Hitoshi ,  ASANO, Osamu ,  UEDA, Masato ,  MIYAZAWA, Shuhei ,  KOTAKE, Yoshihiko ,  KABASAWA, Yasuhiro ,  YASUDA, Masahiro ,  YASUDA, Nobuyuki ,  IIDA, Daisuke ,  NAGAKAWA, Junichi ,  HIROTA, Kazuo ,  NAKAGAWA, Makoto

    IPC分类号： C07D401/04 ,  C07D405/14 ,  C07D409/14 ,  A61K31/506 ,  A61P1/00 ,  A61P1/10 ,  A61P3/04 ,  A61P3/10 ,  A61P9/12 ,  A61P11/06 ,  A61P13/02 ,  A61P19/10 ,  A61P25/16 ,  A61P25/28 ,  A61P43/00

    CPC分类号： C07D405/14 ,  A61K31/506 ,  C07D401/04 ,  C07D409/14

    摘要： The present invention provides a novel pyrimidine compound having an excellent adenosine receptor (A 1 , A 2A , A 2B receptor) antagonistic action. More specifically, it provides a compound represented by the following formula, a salt thereof or a solvate of them.

    In the formula, R 1 and R 2 are the same as or different from each other and each represents a hydrogen atom, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, a cycloalkyl group having three to eight carbon atoms which may be substituted, a cycloalkenyl group having three to eight carbon atoms which may be substituted, a 5 to 14-membered non-aromatic heterocyclic group which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, an acyl group having one to six carbon atoms which may be substituted or an alkylsulfonyl group having one to six carbon atoms which may be substituted; R 3 represents a hydrogen atom, a halogen atom, a cyano group, an alkyl group having one to six carbon atoms which may be substituted, an alkenyl group having two to six carbon atoms which may be substituted, an alkynyl group having two to six carbon atoms which may be substituted, an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted, a nitrogen atom which may be substituted, an oxygen atom which may be substituted or a sulfur atom which may be substituted; R 4 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted, a 5 to 14-membered aromatic heterocyclic group which may be substituted or a 5 to 14-membered non-aromatic heterocyclic group having at least one or more unsaturated bonds which may be substituted; and R 5 represents an aromatic hydrocarbon cyclic group having six to fourteen carbon atoms which may be substituted or a 5 to 14-membered aromatic heterocyclic group which may be substituted.

    摘要翻译： 本发明提供具有优异的腺苷受体（A1，A2A，A2B受体）拮抗作用的新型嘧啶化合物。 更具体地，其提供由下式表示的化合物，其盐或它们的溶剂合物。 式中，R 1和R 2彼此相同或不同，表示氢原子，可以被取代的碳原子数为1〜6的烷基， 具有2-6个可被取代的碳原子的烯基，可被取代的具有2-6个碳原子的炔基，可被取代的具有3-8个碳原子的环烷基，具有3-8个碳原子的环烯基 可被取代的原子，可被取代的5至14元非芳族杂环基，可被取代的具有6至14个碳原子的芳族烃环基，5至14元芳族杂环基，其可以是 取代的，可被取代的具有1至6个碳原子的酰基或可被取代的具有1至6个碳原子的烷基磺酰基; R 3表示氢原子，卤素原子，氰基，可以被取代的碳原子数为1〜6的烷基，可以被取代的碳原子数2〜6的烯基，具有2个 可以被取代的6个碳原子，可以被取代的具有6-14个碳原子的芳族烃环基，可被取代的5至14元芳族杂环基，可被取代的氮原子，氧原子 其可以被取代或可以被取代的硫原子; R 4表示可被取代的碳原子数为6〜14个的芳香族烃基，可以具有取代基的5〜14元芳香族杂环基或具有至少1个的5〜14元非芳香族杂环基 或更多的不饱和键; R 5表示可以被取代的碳原子数为6〜14的芳香族烃基或可以被取代的5〜14元芳香族杂环基。