发明公开
- 专利标题： PHARMACEUTICAL COMPOUNDS
- 专利标题（中）： 药剂师VERBINDUNGEN
-
申请号： EP12798621.4申请日： 2012-10-31
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公开(公告)号： EP2773615A1公开(公告)日： 2014-09-10
- 发明人: WOODHEAD, Andrew James , HAMLETT, Christopher Charles Frederick Hamlett , BESONG, Gilbert Ebai , CHESSARI, Gianni , CARR, Maria Grazia , MILLEMAGGI, Alessia , NORTON, David , SAALAU-BETHELL, Susanne Maria , WILLEMS, Hendrika Maria Gerarda , THOMPSON, Neil Thomas , HISCOCK, Steven Douglas
- 申请人： Astex Therapeutics Limited
- 申请人地址： 436 Cambridge Science Park Milton Park Cambridge Cambridgeshire CB4 0QA GB
- 专利权人： Astex Therapeutics Limited
- 当前专利权人： Astex Therapeutics Limited
- 当前专利权人地址： 436 Cambridge Science Park Milton Park Cambridge Cambridgeshire CB4 0QA GB
- 代理机构： Schlich, George
- 优先权： GB201118874 20111101; GB201118875 20111101; US201161554237P 20111101; US201161554421P 20111101; US201261625925P 20120418
- 国际公布： WO2013064543 20130510
- 主分类号： C07D213/50
- IPC分类号： C07D213/50 ; C07D213/64 ; C07D213/65 ; C07D213/73 ; C07D213/74 ; C07D213/79 ; C07D213/81 ; C07D213/84 ; C07D213/89 ; C07D231/12 ; C07D239/26 ; C07D239/38 ; C07D241/20 ; C07D261/08 ; C07D277/28
摘要：
The invention provides compounds that are useful in the treatment of hepatitis C virus (HCV) infections. The compounds have the formula (1): or a salt, N-oxide, tautomer or stereoisomer thereof, wherein A is CH or N; E is CH or N; R
1 is selected from: an optionally substituted acyclic C
1-8 hydrocarbon group wherein one carbon atom of the acyclic C
1-8 hydrocarbon group may optionally be replaced by O, S, NRC, S(O) or SO
2 , or two adjacent carbon atoms of the acyclic d-β hydrocarbon group may optionally be replaced by CONR
c , NR
c CO, NR
c SO
2 or SO
2 NR
c provided that in each case at least one carbon atom of the acyclic C
1-8 hydrocarbon group remains; 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; R
2 is hydrogen or X-R
8 ; X is a C
1-8 alkanediyl group wherein one carbon atom of the C
1-8 alkanediyl group may optionally be bonded to a -CH
2 -CH
2 - moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C
1-8 alkanediyl group may optionally be bonded to a -(CH
2 )
n moiety, where n is 1 to 5, to form a C
3-7 -cycloalkane-1,2-diyl group; R
3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0-3 heteroatom ring members selected from N, O and S; R
4 is hydrogen or R
43 wherein R
43 is halogen; cyano; C
1-4 alkyl; fluoro-1.4 alkyl; C
1-4 alkoxy; fluoro-C
1-4 alkoxy; hydroxy-C
1-4 alkyl; or C
1-2 alkoxy-C
1-4 alkyl; R
5 is hydrogen or R
53 wherein R
53 is selected from C
1-2 alkyl optionally substituted with fluorine; C
1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R
8 is hydroxy or C(=O)NR
10 R
11 ; provided that when R8 is hydroxy, there are at least two carbon atoms in line between the hydroxy group and the nitrogen atom to which X is attached; R
10 is hydrogen or C
1-4 alkyl; and R
11 is hydrogen; amino-C
2-4 alkyl or hydroxy-C
2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.
1 is selected from: an optionally substituted acyclic C
1-8 hydrocarbon group wherein one carbon atom of the acyclic C
1-8 hydrocarbon group may optionally be replaced by O, S, NRC, S(O) or SO
2 , or two adjacent carbon atoms of the acyclic d-β hydrocarbon group may optionally be replaced by CONR
c , NR
c CO, NR
c SO
2 or SO
2 NR
c provided that in each case at least one carbon atom of the acyclic C
1-8 hydrocarbon group remains; 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; R
2 is hydrogen or X-R
8 ; X is a C
1-8 alkanediyl group wherein one carbon atom of the C
1-8 alkanediyl group may optionally be bonded to a -CH
2 -CH
2 - moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C
1-8 alkanediyl group may optionally be bonded to a -(CH
2 )
n moiety, where n is 1 to 5, to form a C
3-7 -cycloalkane-1,2-diyl group; R
3 is an optionally substituted 3- to 10-membered monocyclic or bicyclic carbocyclic or heterocyclic ring containing 0-3 heteroatom ring members selected from N, O and S; R
4 is hydrogen or R
43 wherein R
43 is halogen; cyano; C
1-4 alkyl; fluoro-1.4 alkyl; C
1-4 alkoxy; fluoro-C
1-4 alkoxy; hydroxy-C
1-4 alkyl; or C
1-2 alkoxy-C
1-4 alkyl; R
5 is hydrogen or R
53 wherein R
53 is selected from C
1-2 alkyl optionally substituted with fluorine; C
1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R
8 is hydroxy or C(=O)NR
10 R
11 ; provided that when R8 is hydroxy, there are at least two carbon atoms in line between the hydroxy group and the nitrogen atom to which X is attached; R
10 is hydrogen or C
1-4 alkyl; and R
11 is hydrogen; amino-C
2-4 alkyl or hydroxy-C
2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.
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