发明名称 Substituted 3-hydroxy-4-pyridone derivative
摘要 This invention provides compounds having antiviral activities especially inhibiting activity for influenza virus, more preferably provides substituted 3-hydroxy-4-pyridone derivatives having cap-dependent endonuclease inhibitory activity.
申请公布号 US8835461(B2) 申请公布日期 2014.09.16
申请号 US201013259956 申请日期 2010.03.23
申请人 Shionogi & Co., Ltd. 发明人 Fujishita Toshio;Mikamiyama Minako;Kawai Makoto;Akiyama Toshiyuki
分类号 A61K31/497;A61K31/44;A61K31/445;C07D413/02;C07D401/02;C07D239/02;C07D403/02;C07D471/02;C07D417/02;C07D413/00;C07D215/00;C07D409/12 主分类号 A61K31/497
代理机构 Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P. 代理人 Finnegan, Henderson, Farabow, Garrett & Dunner, L.L.P.
主权项 1. A compound shown by formula (I), or a pharmaceutically acceptable salt thereof or a solvate thereof: [wherein R1 is chosen from hydrogen and lower alkyl optionally substituted by substituent A, wherein substituent A is at least one group chosen from halogen, amino, and hydroxy; R2 is chosen from a group represented by —(CX1X2)m—Y—(CH2)n—Z, wherein X1 and X2 are each independently hydrogen, hydroxy, hydroxy lower alkyl, lower alkyl, aryl, aryl lower alkyl, or monocyclic heterocycle, Y is a single bond, S, SO2, O, NH, NHCO, or CONH, m and n are each independently an integer of 0 or 1, and each X1 may be the same or different and each X2 may be the same or different, Z is chosen from a) to l) below: A4-Q-C≡C—P—  b)c) A5-Q-C═C—P—,d) A6-Q-(CH2)r1—P—,e) A7-Q-CO—P—,f) A8-Q-(CH2)r2—O—CO—P—,g) A9-Q-CO—(CH2)r3—O—CO—P—,h) A10-Q-CO—NH—P—,i) A11-Q-O—P—,j) A12-Q-S—P—,k) A13-Q-SO2—P—, and wherein P is a single bond or a group chosen from monocyclic hydrocarbon, monocyclic heterocycle, condensed polycyclic hydrocarbon, and condensed polycyclic heterocycle, each may optionally be substituted by at least one substituent chosen from halogen, hydroxy, nitrile, amino, lower alkylamino, aminosulfonyl, aminocarbonyl, lower alkylcarbonyl, lower alkyl, halogeno lower alkyl, lower alkyloxy, oxo and aryl, Q is monocyclic hydrocarbon, condensed polycyclic hydrocarbon, monocyclic heterocycle, or condensed polycyclic heterocycle, T is monocyclic heterocycle, A1, A2, A3, A4, A5, A6, A7, A8, A9, A10, A11, A12, A13, A14 and A15 are each independently chosen from hydrogen, lower alkyl, halogeno lower alkyl, lower alkyloxy lower alkyl, lower alkyloxy, lower alkyloxy lower alkyloxy , halogeno lower alkyloxy , halogeno lower alkylcarbonyl, aryl, aryloxy, lower alkyloxy aryl, aryl lower alkyloxy, lower alkylcarbonyl, aminocarbonyl, lower alkyl aminocarbonyl, cycloalkylaminocarbonyl, amino, lower alkylamino, lower alkylcarbonylamino, cycloalkyl lower alkylamino, aminosulfonyl, arylsulfonyl, lower alkylsulfonyl, lower alkylsulfonylamino, morpholinylcarbonyl, pyrroridinylcarbonyl, hydroxy, hydroxy lower alkyl, nitrile, oxo, arylaminocarbonyl and halogen; r1, r2, and r3 are each independently an integer of 1 or 2] R3 is chosen from: hydroxy, carboxy, phenylaminocarbonyl optionally substituted by substituent C, sulfonylaminocarbonyl optionally substituted by substituent C, and monocyclic heterocycle optionally substituted by substituent C, wherein substituent C is at least one substituent chosen from a) to e) a) lower alkyl optionally substituted with halogen, b) halogen, c) monocyclic hydrocarbon optionally substituted with lower alkyl and/or halogen, d) monocyclic heterocycle, and e) aryl lower alkyl optionally substituted with lower alkyl and/or halogen; R4 is: hydrogen or lower alkyl.
地址 Osaka JP