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    Substituted benzamidines as antibacterial agents
    2.
    发明授权
    Substituted benzamidines as antibacterial agents 有权

    公开(公告)号：US08415383B2

    公开(公告)日：2013-04-09

    申请号：US12679334

    申请日：2008-09-22

    申请人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Ian Collins ,  Lloyd George Czaplewski

    IPC分类号： A01N43/40 ,  A61K31/44

    CPC分类号： C07D277/34 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/429 ,  A61K31/433 ,  C07D271/07 ,  C07D277/64 ,  C07D285/08 ,  C07D417/12

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═C(H)— or ═N—; R3 is a radical of formula -(Alk1)m-(Z1)p-(Alk2)n-Q wherein m, p and n are independently 0 or 1, provided that at least one of m, p and n is 1, Z1 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —0—(C═O)—, —C(═O)—O—, or an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; Alk1 and Alk2 are optionally substituted C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, Or —N(CH2CH3)—; and Q is hydrogen, halogen, nitrile, or hydroxyl, or an optionally substituted monocyclic carbocyclic or heterocyclic radical having 3 to 6 ring atoms; or an optionally substituted bicyclic carbocyclic or heterocyclic radical having 5 to 10 ring atoms; R4 and R5 are optional substituents; and R2, R6 and R7 are independently hydrogen or a radical of formula -(Alk3)x-(Z2)y-(Alk4)z-H wherein x, y and z are independently 0 or 1, Z2 is —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C(—O)—, —0—(C═O)— or —C(═O)—O—; Alk3 and Alk4 are optionally substituted C1-C3 alkylene, C2-C3 alkenylene, or C2-C3 alkynylene radicals, which may optionally terminate with or be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, or —N(CH2CH3)—.

    ANTIBACTERIAL CONDENSED THIAZOLES
    6.
    发明申请
    ANTIBACTERIAL CONDENSED THIAZOLES 有权
    抗菌冷凝型THIAZOLES

    公开(公告)号：US20100305067A1

    公开(公告)日：2010-12-02

    申请号：US12747811

    申请日：2008-12-12

    申请人： David John Haydon ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Lloyd George Czaplewski

    IPC分类号： A61K31/4439 ,  C07D417/10 ,  C07D417/14 ,  A01N43/40 ,  A61K31/437 ,  A01N43/90 ,  A61K31/5383 ,  A61K31/69 ,  A01N55/08 ,  A61P31/04 ,  A01P1/00

    CPC分类号： C07D417/04 ,  C07D277/82 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

    摘要： Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, or —C(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N═ or —CH═Z2 is —N═ or —C(R1)═; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2Jalkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent, or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms.

    摘要翻译： 式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - 或-C（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; Z1是-N =或-CH = Z2是-N =或-C（R1）=; R 1是氢，甲基，乙基，乙烯基，乙炔基，甲氧基，巯基，巯基甲基，卤素，完全或部分氟化的（C1-C2）烷基，（C1-C2烷氧基或（C1-C2）烷硫基，硝基或腈 ）; R2是Q1- [Alk1] q-Q2-，其中q是0或1; Alk1是任选取代的，二价的，直链或支链的C 1 -C 6亚烷基或C 2 -C 6亚烯基或C 2 -C 6亚炔基 可以含有或终止于醚（-O-），硫醚（-S-）或氨基（-NR））连接基团的基团; Q 2是具有5或6个环原子的任选取代的二价单环碳环或杂环基团， 具有9或10个环原子的取代的二价双环碳环或杂环基; Q 1是氢，任选的取代基或具有3-7个环原子的任选取代的碳环或杂环基。

    Antibacterial condensed thiazoles
    8.
    发明授权
    Antibacterial condensed thiazoles 有权
    抗菌缩合噻唑

    公开(公告)号：US08299065B2

    公开(公告)日：2012-10-30

    申请号：US12747811

    申请日：2008-12-12

    申请人： David John Haydon ,  Lloyd George Czaplewski

    发明人： David John Haydon ,  Lloyd George Czaplewski

    IPC分类号： A61K31/5365 ,  A61K31/4427 ,  A61K31/4196 ,  A61K31/497 ,  A61K31/428 ,  A61K31/47 ,  A61K31/5377 ,  A61K31/506 ,  C07D417/14 ,  C07D417/02 ,  C07D265/28 ,  C07D241/10 ,  C07D277/62 ,  C07D401/14 ,  C07D265/30 ,  C07D241/04 ,  C07D239/20

    CPC分类号： C07D417/04 ,  C07D277/82 ,  C07D417/14 ,  C07D471/04 ,  C07D498/04 ,  C07D513/04

    摘要： Compound of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C6 alkylene, alkenylene or alkynylene radical which may contain an ether (—O—), thioether (—S—) or amino (—NR)— link, wherein R is hydrogen, —CN or C1-C3 alkyl; X is —C(═O)NR6—, or —C(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl or C2-C6 alkynyl; Z1 is —N═ or —CH═Z2 is —N═ or —C(R1)═; R1 is hydrogen, methyl, ethyl, ethenyl, ethynyl, methoxy, mercapto, mercaptomethyl, halo, fully or partially fluorinated (C1-C2)alkyl, (C1-C2JaIkoxy or (C1-C2)alkylthio, nitro, or nitrile (—CN); R2 is a group Q1-[Alk1]q-Q2-, wherein q is 0 or 1; AIk1 is an optionally substituted, divalent, straight chain or branched C1-C6 alkylene, or C2-C6 alkenylene or C2-C6 alkynylene radical which may contain or terminate in an ether (—O—), thioether (—S—) or amino (—NR)— link; Q2 is an optionally substituted divalent monocyclic carbocyclic or heterocyclic radical having 5 or 6 ring atoms or an optionally substituted divalent bicyclic carbocyclic or heterocyclic radical having 9 or 10 ring atoms; Q1 is hydrogen, an optional substituent, or an optionally substituted carbocyclic or heterocyclic radical having 3-7 ring atoms.

    摘要翻译： 式（I）化合物具有抗菌活性：其中：m为0或1; Q是氢或环丙基; Alk是可以含有醚（-O-），硫醚（-S-）或氨基（-NR） - 连接的任意取代的二价C 1 -C 6亚烷基，亚烯基或亚炔基，其中R是氢，-CN或 C1-C3烷基; X是-C（= O）NR 6 - 或-C（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基; Z1是-N =或-CH = Z2是-N =或-C（R1）=; R 1是氢，甲基，乙基，乙烯基，乙炔基，甲氧基，巯基，巯基甲基，卤素，完全或部分氟化的（C1-C2）烷基，（C1-C2-烷氧基或（C1-C2）烷硫基，硝基或腈 ）; R2是Q1- [Alk1] q-Q2-，其中q是0或1; Alk1是任选取代的，二价的，直链或支链的C 1 -C 6亚烷基或C 2 -C 6亚烯基或C 2 -C 6亚炔基 可以含有或终止于醚（-O-），硫醚（-S-）或氨基（-NR））连接基团的基团; Q 2是具有5或6个环原子的任选取代的二价单环碳环或杂环基团， 具有9或10个环原子的取代的二价双环碳环或杂环基; Q 1是氢，任选的取代基或具有3-7个环原子的任选取代的碳环或杂环基。