公开(公告)号：EP1439175B1

公开(公告)日：2011-04-27

申请号：EP02802050.1

申请日：2002-10-22

申请人： Eisai R&D Management 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： A novel pyrimidine compound having an excellent antagonistic activity against adenosine receptors (A1, A2A, and A2B receptors). Specifically, it is a compound represented by the following formula, a salt of the compound, or a solvate of either. (I) In the formula, R1 and R2 are the same or different and each represents hydrogen, optionally substituted C1-6 alkyl, etc.; R3 represents hydrogen, halogeno, etc.; R4 represents an optionally substituted C6-14 aromatic hydrocarbon ring group, optionally substituted 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond, etc.; and R5 represents an optionally substituted C6-14 aromatic hydrocarbon ring group or optionally substituted 5- to 14-membered aromatic heterocyclic group.

公开(公告)号：EP1439176B1

公开(公告)日：2007-03-21

申请号：EP02802051.9

申请日：2002-10-22

申请人： Eisai R&D Management 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 invention provides novel pyrimidone compounds exhibiting excellent antagonism against adenosine receptors (A1, A2A, and A2B receptors), particularly, compounds represented by the general formula (I), salts thereof, or solvates of both: (I) wherein R1 and R2 are each independently hydrogen, C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, C3-8 cycloalkyl, C3-8 cycloalkenyl, a 5- to 14-membered nonaromatic heterocyclic group, a C6-14 aromatic hydrocarbon group, a 5- to 14-membered aromatic heterocyclic group, C1-6 acyl, or C1-6 alkylsulfonyl; R3 is hydrogen, C1-6 alkyl, C2-6 alkenyl, or C2-6 alkynyl; R4 is a C6-14 aromatic hydrocarbon group; a 5- to 14-membered aromatic heterocyclic group, or a 5- to 14-membered nonaromatic heterocyclic group having at least one unsaturated bond; and R5 is a C6-14 aromatic hydrocarbon group or a 5- to 14-membered aromatic heterocyclic group (with the proviso that every group except hydrogen may be substituted).