发明公开
EP3284519A1 POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
审中-公开
具有HIV整合酶抑制活性的多环氨基甲酰基吡啶酮衍生物
- 专利标题： POLYCYCLIC CARBAMOYLPYRIDONE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
- 专利标题（中）： 具有HIV整合酶抑制活性的多环氨基甲酰基吡啶酮衍生物
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申请号： EP17195276.5申请日： 2006-04-28
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公开(公告)号： EP3284519A1公开(公告)日： 2018-02-21
- 发明人: JOHNS, Brian Alvin , Kawasuji, Takashi , Taishi, Teruhiko , Taoda, Yoshiyuki
- 申请人： VIIV Healthcare Company , Shionogi & Co., Ltd
- 申请人地址： 251 Little Falls Drive Wilmington, DE 19808 US
- 专利权人： VIIV Healthcare Company,Shionogi & Co., Ltd
- 当前专利权人： VIIV Healthcare Company,Shionogi & Co., Ltd
- 当前专利权人地址： 251 Little Falls Drive Wilmington, DE 19808 US
- 代理机构： J A Kemp
- 优先权： JP2005131161 20050428; JP2005312076 20051027
- 主分类号： A61P31/18
- IPC分类号： A61P31/18 ; A61K31/4985 ; C07D498/04
摘要：
The present invention is to provide a novel compound (I-1) shown below, having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a drug containing the same, particularly an anti-HIV drug, as well as a process and an intermediate thereof.
wherein
A ring is substituted ring of (a), (b) or (c)
wherein Z is O or NR 19 ,
R 19 is hydrogen, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkylcarbonyl or C 1-10 alkylsulfonyl, and the other substituents on the A ring form a ring;
R 14 and R X are hydrogen;
a broken line represents the presence or absence of a bond, provided that when the broken line represents the presence of a bond, R X is not present;
R 1 is hydrogen or C 1-10 alkyl;
X is C 1-6 alkylene;
R 2 is phenyl or phenyl substituted with at least halogen;
R 3 is hydrogen, halogen, hydroxy, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkoxy, C 2-8 alkenyloxy or amino;
or a pharmaceutically acceptable salt, or solvate thereof.
wherein
A ring is substituted ring of (a), (b) or (c)
wherein Z is O or NR 19 ,
R 19 is hydrogen, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkylcarbonyl or C 1-10 alkylsulfonyl, and the other substituents on the A ring form a ring;
R 14 and R X are hydrogen;
a broken line represents the presence or absence of a bond, provided that when the broken line represents the presence of a bond, R X is not present;
R 1 is hydrogen or C 1-10 alkyl;
X is C 1-6 alkylene;
R 2 is phenyl or phenyl substituted with at least halogen;
R 3 is hydrogen, halogen, hydroxy, C 1-10 alkyl, C 2-8 alkenyl, C 1-10 alkoxy, C 2-8 alkenyloxy or amino;
or a pharmaceutically acceptable salt, or solvate thereof.
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