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Macrocyclic inhibitors of hepatitis C virus
专利权人:
Medivir AB;Janssen R&D Ireland
发明人:
Kenneth Alan Simmen,Herman Augustinus De Kock,Pierre Jean-Marie Bernard Raboisson,Lili Hu,Abdellah Tahri,Dominique Louis Nestor Ghislain Surleraux,Karl Magnus Nilsson,Bengt Bertil Samuelsson,Asa Annic
申请号:
US14684649
公开号:
US09353103B2
申请日:
2015.04.13
申请国别(地区):
US
年份:
2016
代理人:
摘要:
Inhibitors of HCV replication of formula (I)and the N-oxides, salts, and stereoisomers, wherein each dashed line represents an optional double bond;X is N, CH and where X bears a double bond it is C;R1 is —OR7, —NH—SO2R8;R2 is hydrogen, and where X is C or CH, R2 may also be C1-6alkyl;R3 is hydrogen, C1-6alkyl, C1-6alkoxyC1-6alkyl, C3-7cycloalkyl;R4 is aryl or Het; n is 3, 4, 5, or 6;R5 is halo, C1-6alkyl, hydroxy, C1-6alkoxy, phenyl, or Het;R6 is C1-6alkoxy, or dimethylamino;R7 is hydrogen; aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;R8 is aryl; Het; C3-7cycloalkyl optionally substituted with C1-6alkyl; or C1-6alkyl optionally substituted with C3-7cycloalkyl, aryl or with Het;aryl is phenyl optionally substituted with one, two or three substituents;Het is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms selected from nitrogen, oxygen and sulfur, and being optionally substituted with one, two or three substituents; pharmaceutical compositions containing compounds (I) and processes for preparing compounds (I). Bioavailable combinations of the inhibitors of HCV of formula (I) with ritonavir are also provided.
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