公开(公告)号：EP0533936A4

公开(公告)日：1993-05-19

申请号：EP92901905

申请日：1991-12-27

申请人： JAPAN TOBACCO INC ,  YUKI GOSEI YAKUHIN KOGYO KK

发明人： EBATA TAKASHI ,  MATSUMOTO KATSUYA ,  KOSEKI KOSHI ,  KAWAKAMI HIROSHI ,  MATSUSHITA HAJIME ,  YOSHIKOSHI HAJIME ,  OKANIWA MASAKAZU

IPC分类号： C07D307/33 ,  C07D315/00 ,  C07D307/32 ,  A61K7/46

CPC分类号： C07D307/33 ,  C07D315/00

摘要： A process for producing cis-whiskey-lactone represented by formula (A), which is one of the flavoring components of whiskey or wine, selectively and readily, which comprises hydrolyzing the lactone part of trans-whiskey-lactone with potassium hydroxide, adding an alkyl group to the product by the reaction with isopropyl bromide to form isopropyl (3S, 4S)-4-hydroxy-3-methyloctanoate, reacting the formed ester with diethyl azodicarboxylate in the presence of both triphenylphosphine and an azodicarboxylate in the presence of both triphenylphosphine and an azodicarboxylic ester to form isopropyl (3S, 4S)-4-(3', 5'-dinitrobenzoyloxy)-3-methyloctanoate, and hydrolying the formed ester with a 2 % aqueous sodium hydroxide solution.

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.