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|Title:||Macrocyclic inhibitors of hepatitis C virus|
|Abstract:||Inhibitors of HCV replication of formula (I) ##STR00001## 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; R.sup.1 is --OR.sup.7 or --NH--SO.sub.2R.sup.8; R.sup.2 is hydrogen, and where X is C or CH, R.sup.2 may also be C.sub.1-6alkyl; R.sup.3 is hydrogen, C.sub.1-6alkyl, C.sub.1-6alkoxyC.sub.1-6alkyl, or C.sub.3-7cycloalkyl; R.sup.4 is aryl or Het; n is 3, 4, 5, or 6; R.sup.5 is halo, C.sub.1-6alkyl, hydroxy, C.sub.1-6alkoxy, phenyl, or Het; R.sup.6 is C.sub.1-6alkoxy or dimethylamino; R.sup.7 is hydrogen; aryl; Het; C.sub.3-7cycloalkyl optionally substituted with C.sub.1-6alkyl; or C.sub.1-6alkyl optionally substituted with C.sub.3-7cycloalkyl, aryl or with Het; R.sup.8 is aryl; Het; C.sub.3-7cycloalkyl optionally substituted with C.sub.1-6alkyl; or C.sub.1-6alkyl optionally substituted with C.sub.3-7cycloalkyl, 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.|
|Inventor(s):||Simmen; Kenneth Alan (Tervuren, BE), De Kock; Herman Augustinus (Arendonk, BE), Raboisson; Pierre Jean-Marie Bernard (Sterrebeek, BE), Nilsson; Karl Magnus (Huddinge, SE), Samuelsson; Bengt Bertril (Huddinge, SE), Rosenquist; Asa Annica Kristina (Huddinge, SE)|
|Assignee:||Tibotec Pharmaceuticals Ltd. (Eastgate, County Cork, IE) Medivar AB (Huddinge, SE)|
|Filing Date:||Aug 03, 2011|
|Claims:||1. A process for the preparation of a compound of formula ##STR00196## comprising the ring closure and dehydration of a compound of formula ##STR00197## |
2. The process according to claim 1 wherein the compound of formula (35) is prepared by coupling a compound of formula ##STR00198## with a compound having the formula ##STR00199##
3. The process according to claim 1 wherein the hydroxy function in the compound of formula (36) is converted to a leaving group.
4. The process according to claim 3 wherein the leaving group is a halogen or an arylsulfonyl group.
5. A compound of formula ##STR00200##
6. A compound of formula ##STR00201##
7. A compound of formula ##STR00202##
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