公开(公告)号：EP2033954A4

公开(公告)日：2009-08-12

申请号：EP07845259

申请日：2007-06-22

申请人： JAPAN TOBACCO INC

发明人： SATOH MOTOHIDE ,  ARAMAKI HISATERU ,  YAMASHITA MASAKI ,  INOUE MASAFUMI ,  KAWAKAMI HIROSHI ,  SHINKAI HISASHI ,  NAKAMURA HIROSHI ,  MATSUZAKI YUJI ,  WAMAKI SHUICHI

IPC分类号： C07D215/56 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61P31/18 ,  A61P43/00 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

CPC分类号： C07D215/56 ,  C07D401/10 ,  C07D413/10 ,  C07D417/10

摘要： A compound represented by the general formula [I], a pharmaceutically acceptable salt thereof, or a solvate of the compound or the salt; and a pharmaceutical composition, an anti-HIV agent, and an HIV integrase inhibitor, each comprising the compound. [I] wherein each symbol is as defined in the description. The compound has an action of inhibiting the HIV integrase activity, and therefore is useful as an anti-HIV agent or a therapeutic or prophylactic agent for AIDS. By using in combination with other anti-HIV agent such as a protease inhibitor and a reverse transcriptase inhibitor, the compound can act as a more effective anti-HIV agent. Further, because of its high inhibitory activity specifically against an integrase, the compound can act as an agent which is safe for a human body and has few adverse side-effects.

公开(公告)号：EP1564210A4

公开(公告)日：2007-08-22

申请号：EP03811532

申请日：2003-11-20

申请人： JAPAN TOBACCO INC

发明人： SATOH MOTOHIDE ,  KAWAKAMI HIROSHI ,  ITOH YOSHIHARU ,  SHINKAI HISASHI ,  MOTOMURA TAKAHISA ,  ARAMAKI HISATERU ,  MATSUZAKI YUJI ,  WATANABE WATARU ,  WAMAKI SHUICHI

IPC分类号： A61K20060101 ,  A61K31/4375 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  A61P20060101 ,  A61P31/12 ,  A61P31/18 ,  A61P43/00 ,  C07D20060101 ,  C07D215/56 ,  C07D215/58 ,  C07D401/06 ,  C07D409/06 ,  C07D417/06 ,  C07D471/04

CPC分类号： A61K31/47 ,  A61K31/4375 ,  A61K31/4709 ,  A61K31/5377 ,  A61K45/06 ,  C07D215/56 ,  C07D215/58 ,  C07D401/06 ,  C07D409/06 ,  C07D417/06 ,  C07D471/04

摘要： 4-Oxoquinoline compounds represented by the following general formula [I]: [I] wherein each symbol has the meaning as defined in the description; or pharmaceutically acceptable salts thereof and anti-HIV agents containing these compounds. Because of having an activity of inhibiting HIV integrase, the above compounds are useful as anti-HIV agents in remedies or preventives for AIDS. By using together with other anti-HIV agents such as a protease inhibitor and a reverse transcriptase inhibitor, the above compounds can be used as more efficacious anti-HIV agents. Because of having a high inhibitory activity specific to the integrase, furthermore, these compounds are usable as drugs which are safe to the human body with little side effect.