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11. 发明申请

US20100305067A1 ANTIBACTERIAL CONDENSED THIAZOLES 有权
标题翻译：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。

12. 发明授权

US08389516B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US08389516B2
公开(公告)日：2013-03-05
申请号：US13154592
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/5377 , A61K31/501 , A61K31/497 , A61K31/496 , A61K31/506 , A61K31/4436 , A61K31/428 , A61K31/429 , C07D239/42
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
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C1-C6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 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

13. 发明授权

US08299065B2 Antibacterial condensed thiazoles 有权
标题翻译：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。

14. 发明授权

US07977340B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US07977340B2
公开(公告)日：2011-07-12
申请号：US12304303
申请日：2007-06-21
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/4412 , A61K31/4436 , A61K31/497 , A61K31/506 , C07D403/14 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
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 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

15. 发明申请

US20120004221A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20120004221A1
公开(公告)日：2012-01-05
申请号：US13154485
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/437 , A01N43/90 , A61K31/497 , A01P1/00 , A61K31/5377 , A61K31/506 , A61K31/5383 , A61P31/04 , C07D513/04 , A61K31/496
CPC分类号： A61K31/437 , A01N47/36 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
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C1-C6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 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N; R2和R3如说明书中所定义。

16. 发明授权

US08481544B2 Antibacterial compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US08481544B2
公开(公告)日：2013-07-09
申请号：US13154485
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/497 , A61K31/4365 , C07D241/12 , C07D513/04
CPC分类号： A61K31/437 , A01N47/36 , A61K31/4375 , A61K31/4439 , A61K31/444 , A61K31/496 , A61K31/497 , A61K31/501 , A61K31/506 , A61K31/5377 , A61K31/5383
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N; R2 and R3 are as defined in the description.
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C1-C6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 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N; R2和R3如说明书中所定义。

17. 发明申请

US20110263590A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20110263590A1
公开(公告)日：2011-10-27
申请号：US13154592
申请日：2011-06-07
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/4439 , A61K31/428 , A61K31/497 , A61K31/496 , A61P31/04 , A61K31/506 , A61K31/501 , A61K31/5383 , A61K31/519 , A61K31/444 , A61K31/5377
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds of formula (I) have antibacterial activity: wherein: m is 0 or 1; Q is hydrogen or cyclopropyl; Alk 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
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C1-C6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 - ， - S（O）NR 6 - ， - C（= O）O-或-S（= O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

18. 发明申请

US20090197877A1 Antibacterial Compositions 有权
标题翻译：抗菌组合物
公开(公告)号：US20090197877A1
公开(公告)日：2009-08-06
申请号：US12304303
申请日：2007-06-21
申请人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
发明人： David John Haydon , Lloyd George Czaplewski , Nicholas John Palmer , Dale Robert Mitchell , John Frederick Atherall , Christopher Richard Steele , Tamara Ladduwahetty
IPC分类号： A61K31/5383 , C07D417/10 , A61K31/4439 , A61K31/496 , C07D417/14 , C07D498/04 , A61P31/04
CPC分类号： C07D417/04 , C07D417/14 , Y02P20/582
摘要： Compounds 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—, —S(O)NR6—, —C(═O)O— or —S(═O)O— wherein R6 is hydrogen, optionally substituted C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, -Cyc, or —(C1-C3 alkyl)-Cyc wherein Cyc is optionally substituted monocyclic carbocyclic or heterocyclic having 3-7 ring atoms; Z is N or CH, or CF; R2 and R3 are as defined in the description.
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 - ， - S（O）NR 6 - ， - C（-O）O-或-S（-O）O-，其中R 6是氢，任选取代的C 1 -C 6烷基， C6链烯基，C2-C6炔基，-Cyc或 - （C1-C3烷基）-Cyc，其中Cyc是具有3-7个环原子的任选取代的单环碳环或杂环; Z是N或CH，或CF; R2和R3如说明书中所定义。

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