Kenneth Alan Simmen,Herman Augustinus De Kock,Pierre Jean-Marie Bernard Rabiosson,Abdellah Tahri,Karl Magnus Nilsson,Bengt Bertil Samuelsson,Asa Annica Kristina Rosenquist,Dmitry Antonov
申请号：
US13109395
公开号：
US08754105B2
申请日:
2011.05.17
申请国别(地区):
US
年份:
2014
代理人:
摘要：
Inhibitors of HCV replication of formula (I)the N-oxides, salts, and stereochemically isomeric forms thereof, wherein each dashed line (represented by ) represents an optional double bondX is N, CH and where X bears a double bond it is C R1 is aryl or a saturated, a partially unsaturated or completely unsaturated 5 or 6 membered monocyclic or 9 to 12 membered bicyclic heterocyclic ring system wherein said ring system contains one nitrogen, and optionally one to three additional heteroatoms selected from the group consisting of oxygen, sulfur and nitrogen, and wherein the remaining ring members are carbon atoms wherein said ring system may be optionally substituted on any carbon or nitrogen ring atom with one, two, three, or four substituentsL is a direct bond, —O—, —O—C1-4alkanediyl-, —O—C(═O)—, —O—C(═O)—NR4a— or —O—C(═O)—NR4aC1-4 alkanediyl-R2 is hydrogen, —OR5, —C(═O)OR5, —C(═O)R6, —C(═O)NR4aR4b, —C(═O)NHR4c, —NR4aR4b, —NHR4c, —NR4aSOpNR4aR4b, —NR4aSOpR7, or B(OR5)2R3 is hydrogen, and where X is C or CH, R3 may also be C1-6alkyl n is 3, 4, 5, or 6p is 1 or 2 aryl is phenyl, naphthyl, indanyl, or 1,2,3,4-tetrahydronaphthyl, each of which may be optionally substituted with one, two or three substituentsHet is a 5 or 6 membered saturated, partially unsaturated or completely unsaturated heterocyclic ring containing 1 to 4 heteroatoms each independently selected from nitrogen, oxygen and sulfur, being optionally condensed with a benzene ring, and wherein the group Het as a whole may be optionally substituted with one, two or three substituentspharmaceutical 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.
