Derivatives of pyrimidine fused with n-containing heterocyclic rings, process for their preparation and pharmaceutical compositions comprising them

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专利权人:

TIBOTEC PHARMACEUTICALS LTD.

发明人:

申请号：

IL18096307

公开号：

IL180963A

申请日:

2007.01.25

申请国别(地区):

IL

年份:

2015

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

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