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Hepatitis C virus macrocyclic inhibitors
专利权人:
JANSSEN R&D IRELAND;MEDIVIR AB
发明人:
RABOISSON, PIERRE JEAN-MARIE BERNARD,DE KOCK, HERMAN AUGUSTINUS,DORANGE, ISMET,VENDEVILLE, SANDRINE MARIE HELENE,SURLERAUX, DOMINIQUE LOUIS NESTOR GHISLAIN,TAHRI, ABDELLAH,SIMONNET, YVAN,VAN DE VREKEN
申请号:
ES06778068
公开号:
ES2456617T3
申请日:
2006.07.28
申请国别(地区):
ES
年份:
2014
代理人:
摘要:
A compound having the formula ** Formula ** and the N-oxide, salt or stereoisomer thereof, wherein X is N, CH and, in case X carries a double bond, is C; R1 is -NH-SO2R6; R2 is hydrogen, and in the case that X is C or CH, R2 can also be C1-6 alkyl; R3 is hydrogen, C1-6 alkyl, C1-6 alkoxy C1-6 alkyl or C3-7 cycloalkyl; R4 is isoquinolinyl, optionally substituted with one, two or three substituents, each independently selected from C1-6 alkyl, C1-6 alkoxy, hydroxy, halo, polyhalo-C1-6 alkyl, C1-6 polyhaloalkoxy, amino, mono- or dialkyl C1-6amino, monoo di-C1-6alkylcarbonyl, C1-6alkylcarbonylamino, aryl and Het; n is 3, 4, 5 or 6; wherein each of the dashed lines (represented by - - - - -) represents an optional double bond; R6 is aryl; Het; C3-7 cycloalkyl, optionally substituted with C1-6 alkyl; or C1-6 alkyl, optionally substituted with C3-7 cycloalkyl, aryl or with Het; each of the aryls, as a group or part of a group, is phenyl optionally substituted with one, two or three substituents selected from halo, hydroxy, nitro, cyano, carboxyl, C1-6 alkyl, C1-6 alkoxy, C1 alkoxy -6C1-6alkyl, C1-6alkylcarbonyl, amino, mono- or di- C1-6alkyl-amino, azido, mercapto, polyhaloalkylC1-6, polyhaloalkoxyC1-6, cyclopropyl, pyrrolidinyl, piperidinyl, piperazinyl, 4-C1-6piperazinyl , 4-C 1-6 alkylcarbonyl-piperazinyl and morpholinyl; and wherein the morpholinyl and piperidinyl groups may be optionally substituted with one or two C1-6 alkyl radicals; and each of the Het, as a group or part of a group, is a saturated, partially unsaturated or completely unsaturated 5 or 6-membered heterocyclic ring containing 1 to 4 heteroatoms, each independently selected from nitrogen, oxygen and sulfur, said heterocyclic ring being optionally substituted with one, two or three substituents, each independently selected from the group consisting of halo, hydroxy, nitro, cyano, carboxyl, C1-6 alkyl, C1-6 alkoxy, C1- alkoxy 6 C1-6 alkyl, C1-6 alkylcarbonyl, amino, mono- or di- C1-6 alkyl, azido, merca
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