发明名称 Hydroxyphenyl derivatives and biological applications thereof
摘要 The invention relates to hydroxyphenyl derivatives of formula (I); and uses thereof as anti-bacterial and/or anti-parasitic agents.
申请公布号 US9309179(B2) 申请公布日期 2016.04.12
申请号 US201414228893 申请日期 2014.03.28
申请人 FAB PHARMA 发明人 Denis Alexis;Gerusz Vincent;Bonvin Yannick
分类号 C07C43/295;C07C41/16;C07C41/26;C07C43/23;C07C45/67;C07C45/71;C07C49/84;C07C205/38;C07C209/08;C07C209/14;C07C309/73;C07D213/643;C07D213/73;C07D213/74;C07D213/75;C07D401/12;C07C43/275;C07C217/90;C07C251/54;C07D209/50;C07D213/68;C07D213/69;C07D213/76;C07D295/092;C07D295/16 主分类号 C07C43/295
代理机构 Nixon & Vanderhye P.C. 代理人 Nixon & Vanderhye P.C.
主权项 1. A method of treatment of microbial infection which comprises administering to a patient in need thereof an effective amount of a hydroxyphenyl derivative of formula (I), wherein the microbial infection is an infection by bacteria carrying the FabI enzyme; R1 is phenyl R1 being optionally substituted by 1 to 3 R identical or different, R being selected from the group comprising H, fluoro, C1-C8 alkyl, C1-C4fluoro-alkyl, C2-C8 alkenyl, C2-C8 alkynyl, COORa, CORa, CONRaRb, OCORa, CN, ORa, NRaRb, CRa═NORb, NRaCOORb, OCONRaRb, NRaCONRbRc, SRa, SO2Ra, SO2NRaRb, and NRaC(S)NRbRc, all being possibly substituted by R′, R2 is C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, C1-C4fluoro-alkyl, C2-C4fluoro-alkenyl, ORa, SRa, all being possibly substituted by 1 to 3 identical or different R′, Ra, Rb and Rc, identical or different, are selected from the group consisting of H, C1-C8 alkyl, C2-C8 alkenyl, C2-C8 alkynyl, R′ is selected from the group comprising C1-C8 alkyl, CH2CO2R″, CO2R″, COR″, CONR″R′″, OCOR″, OR″, NR″R′″, NR″COR′″, NR″COOR′″, OCONR″R′″, NR″CONR″R′″, NR″SO2R′″, SO2R″, NR″SO2R′″, halogen and CN, R″ and R′″, identical or different, are H or C1-C8 alkyl, Y represents H, Z1 and Z3, identical or different, are halogen or H, Z2 is fluoro, or a pharmaceutically acceptable organic or mineral salt, as well as the racemic derivatives and each unique not racemic derivatives, in case the derivatives of formula (I) have one or more chiral centers, both the cis (Z) and trans (E) isomers, in cases the derivatives of formula (I) have unsaturated carbon=carbon double bonds, and any N-oxide form of the derivatives.
地址 Paris FR