- 专利标题: Pharmaceutical compounds
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申请号: US14355786申请日: 2012-10-31
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公开(公告)号: US09145354B2公开(公告)日: 2015-09-29
- 发明人: Andrew James Woodhead , Christopher Charles Frederick Hamlett , Gilbert Ebai Besong , Gianni Chessari , Maria Grazia Carr , Alessia Millemaggi , David Norton , Susanne Maria Saalau-Bethell , Hendrika Maria Gerarda Willems , Neil Thomas Thompson , Steven Douglas Hiscock
- 申请人: ASTEX THERAPEUTICS LIMITED
- 申请人地址: GB Cambridge
- 专利权人: ASTEX THERAPEUTICS LIMITED
- 当前专利权人: ASTEX THERAPEUTICS LIMITED
- 当前专利权人地址: GB Cambridge
- 代理机构: Heslin Rothenberg Farley & Mesiti P.C.
- 优先权: GB1118874.5 20111101; GB1118875.2 20111101
- 国际申请: PCT/EP2012/071573 WO 20121031
- 国际公布: WO2013/064543 WO 20130510
- 主分类号: C07C225/16
- IPC分类号: C07C225/16 ; C07D213/73 ; C07D213/74 ; C07C255/58 ; C07D213/79 ; C07D213/81 ; C07D213/84 ; C07D213/89 ; C07D231/12 ; C07D401/04 ; C07D239/26 ; C07D239/38 ; C07C225/18 ; C07D241/20 ; C07D261/08 ; C07D277/28 ; C07D498/04 ; C07D213/50 ; C07D213/64 ; C07D213/65 ; C07C225/22 ; C07C229/38 ; C07C237/06 ; C07C237/10 ; C07C237/24 ; C07C237/30 ; A61K9/00 ; A61K9/20 ; A61K9/48 ; C07C313/06 ; A61K31/138 ; A61K31/277 ; A61K31/42 ; A61K31/425 ; A61K31/44 ; A61K31/4965 ; A61K31/505 ; A61K31/5383 ; A61K45/06 ; C07C221/00 ; C07C253/30 ; C07D275/02 ; A61K47/10 ; A61K47/26 ; A61K9/19
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; R1 is selected from: an optionally substituted acyclic C1-8 hydrocarbon group wherein one carbon atom of the acyclic C1-8 hydrocarbon group may optionally be replaced by O, S, NRc, S(O) or SO2, or two adjacent carbon atoms of the acyclic C1-8 hydrocarbon group may optionally be replaced by CONRc, NRcCO, NRcSO2 or SO2NRc provided that in each case at least one carbon atom of the acyclic C1-8 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; R2 is hydrogen or X—R8; X is a C1-8 alkanediyl group wherein one carbon atom of the C1-8 alkanediyl group may optionally be bonded to a —CH2—CH2— moiety to form a cyclopropane-1,1-diyl group or two adjacent carbon atoms of the C1-8 alkanediyl group may optionally be bonded to a —(CH2)n moiety, where n is 1 to 5, to form a C3-7-cycloalkane-1,2-diyl group; R3 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; R4 is hydrogen or R4a wherein R4a is halogen; cyano; C1-4 alkyl; fluoro-1-4 alkyl; C1-4 alkoxy; fluoro-C1-4 alkoxy; hydroxy-C1-4 alkyl; or C1-2 alkoxy-C1-4 alkyl; R5 is hydrogen or R5a wherein R5a is selected from C1-2 alkyl optionally substituted with fluorine; C1-3 alkoxy optionally substituted with fluorine; halogen; cyclopropyl; and cyano; R8 is hydroxy or C(═O)NR10R11; 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; R10 is hydrogen or C1-4 alkyl; and R11 is hydrogen; amino-C2-4 alkyl or hydroxy-C2-4 alkyl; but excluding the compounds 1-(3-benzoylphenyl)-ethylamine and 1-(3-furan-2-oylcarbonylphenyl)-ethylamine.
公开/授权文献
- US20150051199A1 PHARMACEUTICAL COMPOUNDS 公开/授权日:2015-02-19
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