Invention Application
US20140288040A1 SUBSTITUTED BENZYLAMINE COMPOUNDS, THEIR USE IN MEDICINE, AND IN PARTICULAR THE TREATMENT OF HEPATITIS C VIRUS (HCV) INFECTION
审中-公开
替代苄嘧啶化合物,其在医学中的使用,特别是治疗丙型肝炎病毒(HCV)感染的治疗
- Patent Title: SUBSTITUTED BENZYLAMINE COMPOUNDS, THEIR USE IN MEDICINE, AND IN PARTICULAR THE TREATMENT OF HEPATITIS C VIRUS (HCV) INFECTION
- Patent Title (中): 替代苄嘧啶化合物,其在医学中的使用,特别是治疗丙型肝炎病毒(HCV)感染的治疗
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Application No.: US14355780Application Date: 2012-10-31
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Publication No.: US20140288040A1Publication Date: 2014-09-25
- Inventor: Andrew James Woodhead , Gianni Chessari , Gilbert Ebai Besong , Maria Grazia Carr , Steven Douglas Hiscock , Michael Alistair O'Brien , David Charles Rees , Susanne Maria Saalau-Bethell , Hendrika Maria Gerarda Willems , Neil Thomas Thompson
- Applicant: ASTEX THERAPEUTICS LIMITED
- Applicant Address: GB Cambridge
- Assignee: ASTEX THERAPEUTICS LIMITED
- Current Assignee: ASTEX THERAPEUTICS LIMITED
- Current Assignee Address: GB Cambridge
- Priority: GB1118876.0 20111101
- International Application: PCT/EP2012/071560 WO 20121031
- Main IPC: A61K31/505
- IPC: A61K31/505 ; A61K31/137 ; A61K45/06 ; C07C217/74 ; A61K31/135 ; C07D239/42 ; C07C237/20 ; A61K31/165 ; C07D211/70 ; A61K31/4409 ; C07D295/027 ; A61K31/4465 ; A61K31/4462 ; A61K31/397 ; C07C217/58

Abstract:
The invention provides compounds of the formula (6): or a salt, N-oxide or tautomer thereof, wherein A is CH, CF or nitrogen; E is CH, CF or nitrogen; and R0 is hydrogen or C1-2 alkyl; R1a is selected from CONH2; CO2H; an optionally substituted acyclic C1-8 hydrocarbon group; and an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1, 2, 3 or 4 are heteroatom ring members selected from O, N and S; R2 is selected from hydrogen and a group R2a; R2a is selected from an optionally substituted acyclic C1-8 hydrocarbon group; an optionally substituted monocyclic carbocyclic or heterocyclic group of 3 to 7 ring members, of which 0, 1 or 2 ring members are heteroatom ring members selected from O, N and S; and an optionally substituted bicyclic heterocyclic group of 9 or 10 ring members, of which 1 or 2 ring members are nitrogen atoms; wherein at least one of R1 and R2 is other than hydrogen; R3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0, 1, 2 or 3 heteroatom ring members selected from N, O and S; R4a is selected from halogen; cyano; C1-4 alkyl optionally substituted with one or more fluorine atoms; C1-4 alkoxy optionally substituted with one or more fluorine atoms; hydroxy-C1-4 alkyl; and C1-2 alkoxy-C1-4 alkyl; R5 is selected from hydrogen and a substituent R5a; and R5a is selected from C1-2 alkyl optionally substituted with one or more fluorine atoms; C1-3 alkoxy optionally substituted with one or more fluorine atoms; halogen; cyclopropyl; cyano; and amino. The compounds have activity against hepatitis C virus and can be used in the prevention or treatment of hepatitis C viral infections.
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