发明公开
EP2703399A1 OXAZINE DERIVATIVE AND BACE 1 INHIBITOR CONTAINING SAME
审中-公开
OXAZINDERIVAT UND BACE-1-HEMMER DAMIT
- 专利标题： OXAZINE DERIVATIVE AND BACE 1 INHIBITOR CONTAINING SAME
- 专利标题（中）： OXAZINDERIVAT UND BACE-1-HEMMER DAMIT
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申请号： EP12777494.1申请日： 2012-04-25
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公开(公告)号： EP2703399A1公开(公告)日： 2014-03-05
- 发明人: MASUI, Moriyasu , MITSUOKA, Yasunori , YOSHIDA, Syuhei , KUSAKABE, Ken-ichi , ONODERA, Naohiro , KUROSE, Noriyuki
- 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： JP2011098121 20110426; JP2011127185 20110607; JP2011274039 20111215
- 国际公布： WO2012147763 20121101
- 主分类号： C07D413/12
- IPC分类号： C07D413/12 ; A61K31/5355 ; A61P25/00 ; A61P25/28 ; A61P43/00
摘要：
The present invention provides a compound of formula (I):
wherein
-X= is -CR 7 = or -N=,
ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle,
R 1 is substituted or unsubstituted alkyl or the like,
R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like,
R 3 and R 4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like,
R 5 is hydrogen, substituted or unsubstituted alkyl or the like,
each R 6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R 7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like,
p is an integer of 0 to 3,
or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.
wherein
-X= is -CR 7 = or -N=,
ring B is a substituted or unsubstituted carbocycle or a substituted or unsubstituted heterocycle,
R 1 is substituted or unsubstituted alkyl or the like,
R 2a and R 2b are each independently hydrogen, substituted or unsubstituted alkyl or the like,
R 3 and R 4 are each independently hydrogen, halogen, substituted or unsubstituted alkyl or the like,
R 5 is hydrogen, substituted or unsubstituted alkyl or the like,
each R 6 is independently halogen, hydroxy, substituted or unsubstituted alkyl or the like, R 7 is hydrogen, halogen, hydroxy, substituted or unsubstituted alkyl or the like,
p is an integer of 0 to 3,
or a pharmaceutically acceptable salt thereof which has an effect of inhibiting amyloid β production, especially an effect of inhibiting BACE1, and which is useful as a therapeutic or prophylactic agent for diseases induced by production, secretion and/or deposition of amyloid β proteins.
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