发明公开
EP1714966A1 NAPHTHYLIDINE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
审中-公开
美国艾滋病毒综合防治艾滋病毒综合征
- 专利标题: NAPHTHYLIDINE DERIVATIVE HAVING HIV INTEGRASE INHIBITORY ACTIVITY
- 专利标题(中): 美国艾滋病毒综合防治艾滋病毒综合征
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申请号: EP05704349.9申请日: 2005-02-02
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公开(公告)号: EP1714966A1公开(公告)日: 2006-10-25
- 发明人: TAISHI, Teruhiko, Shionogi & Co., Ltd. , TADA, Yukio, Shionogi & Co., Ltd.
- 申请人: Shionogi Co., Ltd.
- 申请人地址: 1-8, Doshomachi 3-chome, Chuo-ku Osaka-shi, Osaka 541-0045 JP
- 专利权人: Shionogi Co., Ltd.
- 当前专利权人: Shionogi Co., Ltd.
- 当前专利权人地址: 1-8, Doshomachi 3-chome, Chuo-ku Osaka-shi, Osaka 541-0045 JP
- 代理机构: Vossius & Partner
- 优先权: JP2004027849 20040204
- 国际公布: WO2005075475 20050818
- 主分类号: C07D471/04
- IPC分类号: C07D471/04 ; A61K31/4375 ; A61K31/5377 ; A61K31/541 ; A61P31/12 ; A61P31/18 ; A61P43/00
摘要:
[Problems to be Solved]
To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same.
[Means to Solve the Problem]
A compound of the formula:
(wherein:
R 1 is optionally substituted aralkyl;
R 2 and R 3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for "optionally substituted" is a noncyclic group);
R 4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in "optionally substituted formylamino", "optionally substituted carbamoyl" and "optionally substituted amino" may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
To provide a novel compound having antiviral activity, especially inhibitory activity against HIV integrase, a pharmaceutical composition, especially anti-HIV drug, containing the same.
[Means to Solve the Problem]
A compound of the formula:
(wherein:
R 1 is optionally substituted aralkyl;
R 2 and R 3 are each independently hydrogen, optionally substituted alkyl, optionally substituted amino, optionally substituted alkenyl or optionally substituted alkoxy (provided that each substituent for "optionally substituted" is a noncyclic group);
R 4 is hydrogen, optionally substituted carboxy, optionally substituted formylamino, optionally substituted carbamoyl, optionally substituted amino (provided that a substituent on amino in "optionally substituted formylamino", "optionally substituted carbamoyl" and "optionally substituted amino" may form an optionally-substituted N-atom containing heterocyclic ring together with an adjacent N atom), optionally substituted alkyl, optionally substituted alkenyl, optionally substituted aryl, or optionally substituted heteroaryl) or a salt thereof.
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