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HIV阻害性二環式ピリミジン誘導体
- 专利权人:
- テイボテク・フアーマシユーチカルズ
- 发明人:
- ギルモン,ジエローム・エミーユ・ジヨルジユ,ポーガム,ミカエル,デレスト,ブルノ・フランソワ・マリー,ヘーレス,ジヤン,レウイ,パウルス・ヨアネス,ジヤンセン,パウル・アドリアーン・ジヤン
- 申请号:
- JP2007538423
- 公开号:
- JP5118972B2
- 申请日:
- 2005.10.27
- 申请国别(地区):
- JP
- 年份:
- 2013
- 代理人:
- 摘要:
- HIV replication inhibitors of formula N-oxides, pharmaceutically acceptable addition salts, quaternary amines or stereoisomeric forms thereof, wherein -a1=a2-a3=a4- is &mdashCH&boxHCH&mdashCH&boxHCH&mdash, &mdashN&boxHCH&mdashCH&boxHCH&mdash, &mdashN&boxHCH&mdashN&boxHCH&mdash, &mdashN&boxHCH&mdashCH&boxHN&mdash, &mdashN&boxHN&mdashCH&boxHCH&mdash -b1=b2-b3=b4- is &mdashCH&boxHCH&mdashCH&boxHCH&mdash, &mdashN&boxHCH&mdashCH&boxHCH&mdash, &mdashN&boxHCH&mdashN&boxHCH&mdash, &mdashN&boxHCH&mdashCH&boxHN&mdash, &mdashN&boxHN&mdashCH&boxHCH&mdash n and m is 0, 1, 2, 3 and in certain cases also 4 R1 is hydrogen aryl formyl C1-6alkylcarbonyl optionally substituted C1-6alkyl C1-6alkyloxycarbonyl R2 is OH halo optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl substituted carbonyl carboxyl CN nitro amino substituted amino polyhalomethyl polyhalomethylthio &mdashS(&boxHO)pR6 C(&boxHNH)R6 R2a is CN amino substituted amino optionally substituted C1-6alkyl halo optionally substituted C1-6alkyloxy substituted carbonyl &mdashCH&boxHN&mdashNH&mdashC(&boxHO)&mdashR16 optionally substituted C1-6alkyloxyC1-6alkyl substituted C2-6alkenyl or C2-6alkynyl &mdashC(&boxHN&mdashO&mdashR8)&mdashC1-4alkyl R7 or &mdashX&mdashR7 R3 is CN amino C1-6alkyl halo optionally substituted C1-6alkyloxy substituted carbonyl &mdashCH&boxHN&mdashNH&mdashC(&boxHO)&mdashR16 substituted C1-6alkyl optionally substituted C1-6alkyloxyC1-6alkyl substituted C2-6alkenyl or C2-6alkynyl &mdashC(&boxHN&mdashO&mdashR8)&mdashC1-4alkyl R7 &mdashX&mdashR7 R4 is halo OH optionally substituted C1-6alkyl, C2-6alkenyl or C2-6alkynyl C3-7cycloalkyl C1-6alkyloxy CN nitro polyhaloC1-6alkyl polyhaloC1-6alkyloxy substituted carbonyl formyl amino mono- or di(C1-4alkyl)amino or R7 -A-B&mdash is &mdashCR5&boxHN&mdash, &mdashN&boxHN&mdash, &mdashCH2&mdashCH2&mdash, &mdashCS&mdashNH&mdash, &mdashCO&mdashNH&mdash, &mdashCH&boxHCH&mdash pharmaceutical compositions comprising these methods for the preparation of these compounds
- 来源网站:
- 中国工程科技知识中心
- 来源网址:
- http://www.ckcest.cn/home/