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    Antibacterial condensed thiazoles
    2.
    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。

    ANTIBACTERIAL CONDENSED THIAZOLES
    4.
    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。

    SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS
    6.
    发明申请
    SUBSTITUTED BENAMIDINES AS ANTIBACTERIAL AGENTS 有权

    公开(公告)号：US20100298388A1

    公开(公告)日：2010-11-25

    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： A61K31/4245 ,  A61K31/433 ,  A61K31/428 ,  A61K31/427 ,  C07D285/08 ,  C07D413/12 ,  C07D277/64 ,  C07D413/04 ,  A01N43/78 ,  A01N43/836 ,  A01P1/00 ,  A61P31/04

    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)—, —O—(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)—, —O—(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 Compounds
    8.
    发明申请
    Antibacterial Compounds 有权
    抗菌化合物

    公开(公告)号：US20130252938A1

    公开(公告)日：2013-09-26

    申请号：US13848118

    申请日：2013-03-21

    申请人： BIOTA EUROPE LTD.

    发明人： Christopher James Lunniss ,  James T. Palmer ,  Gary Robert William Pitt ,  David Davies ,  Lorraine Claire Axford

    IPC分类号： C07D417/14 ,  C07D417/04

    CPC分类号： C07D417/04 ,  C07D417/14 ,  C07F9/65583

    摘要： The present invention provides a compound of the following formula, salts, racemates, diastereomers, enantiomers, esters, carbamates, phosphates, sulfates, deuterated forms and prodrugs thereof. Also provided is the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

    摘要翻译： 本发明提供下式的化合物，盐，外消旋体，非对映异构体，对映异构体，酯，氨基甲酸酯，磷酸酯，硫酸酯，氘代形式和前药。 还提供了这些化合物作为抗菌剂的用途，包含它们的组合物及其制备方法。

    ANTIBACTERIAL AGENTS
    9.
    发明申请
    ANTIBACTERIAL AGENTS 有权
    抗菌剂

    公开(公告)号：US20100273837A1

    公开(公告)日：2010-10-28

    申请号：US12678767

    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： A61K31/433 ,  C07D285/08 ,  A61P31/04 ,  A01N43/836 ,  A01P1/00

    CPC分类号： C07D285/08

    摘要： Compounds of formula (IA) or (IB) have antibacterial activity: wherein W is ═CH— or ═N—; Ri and R2 are independently selected from hydrogen, fluoro and chloro, provided that Ri and R2 are not each hydrogen when W is ═CH—; n is 0 or 1; X is —O—, —S—, or —CH2—; and Q is (i) a phenyl radical, a naphthyl radical, a monocyclic carbocyclic or heteroaryl radical having 3 to 6 ring atoms, or a bicyclic heteroaryl radical having 5 to 10 ring atoms, any of which radicals being optionally substituted; or (ii) an optionally substituted C1-C6 alkyl, C2-C6 alkenyl, or C2-C6 alkynyl radical, which may optionally be interrupted by —O—, —S—, —S(O)—, —S(O2)—, —NH—, —N(CH3)—, —N(CH2CH3)—, —C—K═Oh or —C(═O)—O—.

    摘要翻译： 式（IA）或（IB）的化合物具有抗菌活性：其中W是= CH-或= N-; R 1和R 2独立地选自氢，氟和氯，条件是当W是= CH-时，R 1和R 2不是氢。 n为0或1; X是-O - ， - S-或-CH 2 - ; Q为（i）具有3〜6个环原子的苯基，萘基，单环碳环或杂芳基，或环原子数为5〜10的双环杂芳基，其中任意一个为任选被取代的基团; 或（ⅱ）任选被-O - ， - S - ， - S（O） - ， - S（O 2））间隔的任选取代的C 1 -C 6烷基，C 2 -C 6烯基或C 2 -C 6炔基， - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - C-K = Oh或-C（= O）-O-。