C - Chemistry – Metallurgy – 07 – K
Patent
C - Chemistry, Metallurgy
07
K
C07K 5/12 (2006.01) A61K 38/06 (2006.01) A61K 38/12 (2006.01) A61P 31/12 (2006.01) C07K 5/08 (2006.01) C07K 5/083 (2006.01) C07K 5/087 (2006.01) A61K 38/00 (2006.01)
Patent
CA 2369711
The present invention covers macrocyclic compounds of formula I active in- vitro and in cellular assays against the NS3 protease of the hepatitis C virus. (See formula I) wherein W is CH or N; R21 is H, halo, C1-6 alkyl, cycloalkyl, haloalkyl, C1-6 alkoxy, cycloalkoxy, hydroxy, or N(R23)2, wherein each R23 is independently H, C1-6 alkyl or cycloalkoxy; and R22 is H, halo, C1-6 alkyl, C3-6 cycloalkyl, C1-6 haloalkyl, C1-6 thioalkyl, C1-6 alkoxy, C3-6 cycloalkoxy, C2-7 alkoxyalkyl, C3-6 cycloalkyl, C6 or 10 aryl or Het, wherein Het is a five-, six-, or seven-membered saturated or unsaturated heterocycle containing from one to four heteroatoms selected from nitrogen, oxygen and sulfur; said cycloalkyl; aryl or Het being substituted with R24, wherein R24 is H, C1-6 alkyl, C3-6 cycloalkyl, C1-6 alkoxy, C3-6 cycloalkoxy, NO2, N(R25)2, NH-C(O)-R25; or NH-C(O)-NH-R25, wherein each R25 is independently: H, C1-6 alkyl or C3-6 cycloalkyl; or R24 is NH-C(O)-OR26 wherein R26 is C3-6 alkyl or C3-6 cycloalkyl; R3 is hydroxy, NH2, or a group of formula -NH-R31, wherein R31 is C3-6 to aryl, heteroaryl, -C(O)-R32, -C(O)-OR32 or -C(O)-NHR32, wherein R32 is: C1-6 alkyl or C3-6 cycloalkyl; D is a 5 to 10-atom saturated or unsaturated alkylene chain optionally containing one to three heteroatoms independently selected from: O; S, or N- R41, wherein R41 is H, C1-6 alkyl, cycloalkyl or -C(O)-R42, wherein R42 is C1-6 alkyl, cycloalkyl or C6 or 10 aryl; R4 is H or from one to three substituents at any carbon atom of said chain D, said substituent independently selected from the group consisting of C1-6 alkyl, C1-6 haloalkyl; C1-6 alkoxy, hydroxy, halo, amino, oxo, thio or C1-6 thioalkyl, and A is an amide of formula -C(O)-NH-R5, wherein R5 is selected from the group consisting of: C1-8 alkyl, C3-6 cycloalkyl, C6 or 10 aryl or C7-16 aralkyl; or A is a carboxylic acid or a pharmaceutically acceptable salt or ester thereof.
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Boehringer Ingelheim (canada) Ltd.
Ogilvy Renault Llp/s.e.n.c.r.l.,s.r.l.
Unknown
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