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    • 5. 发明授权
      US08415383B2 Substituted benzamidines as antibacterial agents 有权
    • Substituted benzamidines as antibacterial agents
    • US08415383B2
    • 2013-04-09
    • US12679334
    • 2008-09-22
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • A01N43/40 , A61K31/44
    • C07D277/34 , A61K31/4245 , A61K31/427 , A61K31/429 , A61K31/433 , C07D271/07 , C07D277/64 , C07D285/08 , C07D417/12
    • 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)—.
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 7. 发明授权
      US08492414B2 Antibacterial agents 有权
    • Antibacterial agents
    • 抗菌剂
    • US08492414B2
    • 2013-07-23
    • US12678767
    • 2008-09-22
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • A61K31/41
    • C07D285/08
    • 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—.
    • 式（IA）或（IB）的化合物具有抗菌活性：其中W为= CH-或= N-; R 1和R 2独立地选自氢，氟和氯，条件是当W = 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） - ， - K = O或-C（= O）-O-。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Espacenet 法律信息 同族专利 专利引用
    • 9. 发明申请
      US20100273837A1 ANTIBACTERIAL AGENTS 有权
    • ANTIBACTERIAL AGENTS
    • 抗菌剂
    • US20100273837A1
    • 2010-10-28
    • US12678767
    • 2008-09-22
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • David John Haydon , Ian Collins , Lloyd George Czaplewski
    • A61K31/433 , C07D285/08 , A61P31/04 , A01N43/836 , A01P1/00
    • C07D285/08
    • 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—.
    • 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-。
    • 基本信息 添加关注 加入工作空间 PDF全文 PDF下载 全文下载 相似专利 双屏查看 权利要求书 说明书全文 Global Dossier Espacenet 法律信息 同族专利 专利引用
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