[发明专利]氘化氨基缩水甘油基化合物无效
| 申请号： | 200780028058.5 | 申请日： | 2007-05-25 |
| 公开（公告）号： | CN101528669A | 公开（公告）日： | 2009-09-09 |
| 发明（设计）人： | T·G·甘特;S·萨沙 | 申请（专利权）人： | 奥斯拜客斯制药有限公司 |
| 主分类号： | C07C217/30 | 分类号： | C07C217/30;C07C217/34;C07B59/00;A61K31/138 |
| 代理公司： | 永新专利商标代理有限公司 | 代理人： | 王 磊;过晓东 |
| 地址： | 美国加*** | 国省代码： | 美国;US |
| 权利要求书： | 查看更多 | 说明书： | 查看更多 |
| 摘要： | |||
| 搜索关键词： | 氘化 氨基 缩水 甘油 化合物 | ||
1.下式1的化合物
或其单一对映体、其(+)-对映体和其(-)-对映体的混合物、约90重量％或更多的其(-)-对映体与约10重量％或更少的其(+)-对映体的混合物、约90重量％或更多的其(+)-对映体与约10重量％或更少的其(-)-对映体的混合物、其单一非对映体或其非对映体的混合物；或其药学上可接受的盐、其溶剂化物或其前药：
其中：
R3独立地选自由氢、氘和组成的组；
R4和R5各自独立地为氢或氘，或R4和R5连接在一起以形成从而产生萘环体系；且
R1、R2、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30独立地为氢或氘；
条件为在所述式1的化合物中R1、R2、R3、R4、R5、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个独立地为氘；
条件为，当R4和R5连接在一起以形成时：
1)如果R1和R3为氘，则R2、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
2)如果R3为氘，则R1、R2、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
3)如果R1、R2、R3、R27、R28、R29和R30为氘，则R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25和R26中至少一个为氘；且
4)如果R16为氘，则R1、R2、R3、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
5)如果R13、R14、R15、R17、R18和R19为氘，则R1、R2、R3、R6、R7、R8、R9、R10、R11、R12、R16、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
6)如果R13、R14、R15、R16、R17、R18和R19为氘，则R1、R2、R3、R6、R7、R8、R9、R10、R11、R12、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
7)如果R10和R11为氘，则R1、R2、R3、R6、R7、R8、R9、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
8)如果R6和R7为氘，则R1、R2、R3、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
9)如果R6、R7、R8、R10和R11为氘，则R1、R2、R3、R9、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；
条件为，当R3为时：
1)如果R13、R14、R15、R17、R18和R19为氘，则R1、R2、R4、R5、R6、R7、R8、R9、R10、R11、R12、R16、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
2)如果R6和R7为氘，则R1、R2、R4、R5、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
3)如果R1和R5为氘，则R2、R4、R6、R7、R8、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
条件为，当R3为氢时：
1)如果R8为氘，则R1、R2、R4、R5、R6、R7、R9、R10、R11、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘；且
2)如果R10和R11为氘，则R1、R2、R4、R5、R6、R7、R8、R9、R12、R13、R14、R15、R16、R17、R18、R19、R20、R21、R22、R23、R24、R25、R26、R27、R28、R29和R30中至少一个为氘。
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