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HIV-inhibited 5,6-substituted pyrimidines
专利权人:
Janssen Sciences Ireland UC
发明人:
Guillemont, Jerôme,Mordant, Céline,Schmitt, Benoit
申请号:
ES14170114
公开号:
ES2618057T3
申请日:
2007.12.28
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of formula ** Formula ** a pharmaceutically acceptable salt by addition, a pharmaceutically acceptable solvate or a stereochemically isomeric form thereof, wherein: each of R1 is independently hydrogen; aryl; formyl; C1-6 alkylcarbonyl; C1-6 alkyl; C1-6-oxycarbonyl alkyl; R7 and R8 are independently hydrogen; hydroxy; halo; C3-7 cycloalkyl; C1-6-oxy alkyl; carboxyl; C1-6 alkyl oxycarbonyl; cyano; nitro; Not me; mono- or di- (C1-6 alkyl) amino; polyhalo-C 1-6 alkyl; polyhalo-C1-6-oxy alkyl; - C (>; = O) R10; C1-6 alkyl optionally substituted with halo, cyano or -C (>; = O) R10; C2-6 alkenyl optionally substituted with halo, cyano or -C (>; = O) R10; C2-6 alkynyl optionally substituted with halo, cyano or -C (>; = O) R10; R4 is cyano; R9 is C1-6 alkyl; C2-6 alkenyl; C2-6 alkynyl, each substituted with cyano; R5 is -C (>; = O) NR5aR5b; or -CH (OR5c) R5d or R5 is Het; wherein R5a is C1-6-oxy alkyl; C2-6 alkenyl; C3-7 cycloalkyl; or C1-6 alkyl substituted with hydroxy, amino, mono- or di (C1-6 alkyl) amino, C1-6 alkylcarbonylamino, halo, cyano, aryl, pyridyl, thienyl, furanyl, tetrahydrofuranyl, pyrrolidinyl, piperidinyl, morpholinyl, piperazinyl, piperazinyl optionally substituted with C 1-6 alkyl, C 1-6 alkylcarbonyl or with hydroxyC 1-6 alkyl; or R5a is C1-6 alkyl substituted with one or two C1-6-oxy alkyl; R5b is hydrogen or C1-6 alkyl; or R5a and R5b taken together with the nitrogen atom of which they are substituents form pyrrolidinyl; piperidinyl optionally substituted with aminocarbonyl, hydroxy or with C1-6-oxy alkyl; morpholinyl; piperazinyl; piperazinyl optionally substituted with C1-6 alkyl, C1-6 alkylcarbonyl or with hydroxy C1-6 alkyl; R5c is hydrogen, C1-6 alkyl, Het; R5d is C1-6 alkyl, C2-6 alkenyl, C2-6 alkynyl, aryl or Het; R6 is C1-6 alkoxy-C1-6 alkyl; each of R10, independently, is C1-6 alkyl, amino, mono- or di- (C1-6 alkyl) amino or polyhalo-C1-6 alkyl; X is -NR1-; each of r, independently, is 1 or 2; each of Het, independently,
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