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1. 发明申请

US20140135332A1 AROMATIC AMIDES AND USES THEREOF 有权
标题翻译：芳香剂及其用途
公开(公告)号：US20140135332A1
公开(公告)日：2014-05-15
申请号：US14112735
申请日：2012-04-20
申请人： David John Haydon , Lloyd George Czaplewski , Neil Robert Stokes , David Davies , Ian Collins , James T Palmer , Jeffrey Peter Mitchell , Gary Robert William Pitt , Daniel Offermann
发明人： David John Haydon , Lloyd George Czaplewski , Neil Robert Stokes , David Davies , Ian Collins , James T Palmer , Jeffrey Peter Mitchell , Gary Robert William Pitt , Daniel Offermann
IPC分类号： A61K31/5377 , A61K31/506 , A61K31/437 , A61K31/4439 , A61K31/433 , A61K31/427 , A61K31/421 , C07D513/04 , C07D413/12 , C07D285/08 , C07D277/30 , C07D263/32 , A61K31/496 , A61K31/426
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/506 , C07D263/32 , C07D271/06 , C07D277/24 , C07D277/30 , C07D285/08 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.
摘要翻译：本发明提供式（I）的化合物：及其盐，外消旋物，异构体，非对映异构体，对映异构体，水合物，溶剂化物，N-氧化物，其药学上可接受的衍生物或前药。还提供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。

2. 发明授权

US08415383B2 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)—.

3. 发明申请

US20100173933A1 ANTIBACTERIAL AGENTS 有权
标题翻译：抗菌剂
公开(公告)号：US20100173933A1
公开(公告)日：2010-07-08
申请号：US12293608
申请日：2007-03-22
申请人： David Ryall Brown , Ian Collins , Lloyd George Czaplewski , David John Haydon
发明人： David Ryall Brown , Ian Collins , Lloyd George Czaplewski , David John Haydon
IPC分类号： A61K31/437 , C07D277/62 , C07D471/04 , C07D263/34 , C07D271/06 , A61K31/428 , A61K31/421 , A61K31/41 , A61P31/04
CPC分类号： C07C235/46 , A01N37/40 , A01N41/04 , A01N43/08 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/76 , A01N43/78 , A01N43/82 , A01N43/90 , A61K31/166 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4422 , A61K31/4523 , A61K31/4709 , C07C255/16 , C07C309/73 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/81 , C07D215/12 , C07D215/14 , C07D231/12 , C07D233/64 , C07D249/04 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/24 , C07D277/32 , C07D277/64 , C07D307/42 , C07D307/56 , C07D319/20 , C07D333/06 , C07D333/12 , C07D333/16 , C07D333/56 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ═C(R1)— or ═N—; R1 is hydrogen or an optional substituent and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2—, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; R3 is a radical of formula -(Alk1)m-(Z)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, Z 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 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 heterocyclic radical having 5 to 10 ring atoms.
摘要翻译：式（I）化合物具有抗菌活性：其中R表示氢或1,2或3个任选的取代基; W是≡C（R1） - 或=N-; R1是氢或任选的取代基，R 2是氢，甲基或氟; 或R 1和R 2一起为-CH 2 - ， - CH 2 CH 2 - ， - O-，或者在任一取向为-O-CH 2 - 或-OCH 2 CH 2 - ; R3是式 - （Alk1）m-（Z）p-（Alk2）nQ的基团，其中m，p和n独立地为0或1，条件是m，p和n中的至少一个为1，Z为 - （O） - ， - S（O 2） - ， - NH - ， - N（CH 3） - ， - N（CH 2 CH 3） - ， - （C = O） - ， - C（= O）-O-，或具有3至6个环原子的任选取代的二价单环碳环或杂环基; 或具有5至10个环原子的任选取代的二价双环杂环基; Alk1和Alk2是任选取代的C 1 -C 6亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基，其可以任选地被-O - ， - S - ， - S（O） - ， - S（ O，-N（CH 3） - 或-N（CH 2 CH 3） - ; 和Q是氢，卤素，腈或羟基或任选取代的具有3-6个环原子的单环碳环或杂环基; 或具有5〜10个环原子的任意取代的双环杂环基。

4. 发明授权

US08865736B2 Antibacterial agents 有权
标题翻译：抗菌剂
公开(公告)号：US08865736B2
公开(公告)日：2014-10-21
申请号：US13304748
申请日：2011-11-28
申请人： David Ryall Brown , Ian Collins , Lloyd George Czaplewski , David John Haydon
发明人： David Ryall Brown , Ian Collins , Lloyd George Czaplewski , David John Haydon
IPC分类号： A01N43/44 , A61K31/352 , A61K31/381 , A61K31/4192 , A61K31/422 , C07D261/08 , C07D277/24 , A61K31/341 , A61K31/4523 , A61K31/343 , A61K31/428 , C07D413/04 , C07D277/64 , C07D263/56 , A61K31/4178 , C07D231/12 , A61K31/4245 , A61K31/4709 , A61K31/166 , C07D498/04 , C07D471/04 , C07D417/14 , C07D307/42 , C07D213/30 , C07D333/12 , A61K31/4184 , A61K31/433 , C07D417/06 , A61K31/4422 , A61K31/44 , C07D271/10 , C07D215/12 , C07D417/04 , C07D319/20 , A61K31/4155 , C07D513/04 , C07D263/32 , C07D249/04 , C07D233/64 , C07D333/06 , A61K31/4196 , C07D213/81 , C07D333/56 , A61K31/429 , C07D277/32 , C07D271/06 , A61K31/423 , A61K31/4025 , A61K31/427
CPC分类号： C07C235/46 , A01N37/40 , A01N41/04 , A01N43/08 , A01N43/10 , A01N43/40 , A01N43/42 , A01N43/76 , A01N43/78 , A01N43/82 , A01N43/90 , A61K31/166 , A61K31/341 , A61K31/343 , A61K31/352 , A61K31/381 , A61K31/4025 , A61K31/4155 , A61K31/4178 , A61K31/4184 , A61K31/4192 , A61K31/4196 , A61K31/422 , A61K31/423 , A61K31/4245 , A61K31/427 , A61K31/428 , A61K31/429 , A61K31/433 , A61K31/44 , A61K31/4422 , A61K31/4523 , A61K31/4709 , C07C255/16 , C07C309/73 , C07C2601/02 , C07C2601/14 , C07C2601/18 , C07D213/30 , C07D213/81 , C07D215/12 , C07D215/14 , C07D231/12 , C07D233/64 , C07D249/04 , C07D261/08 , C07D263/32 , C07D263/56 , C07D271/06 , C07D271/10 , C07D277/24 , C07D277/32 , C07D277/64 , C07D307/42 , C07D307/56 , C07D319/20 , C07D333/06 , C07D333/12 , C07D333/16 , C07D333/56 , C07D413/04 , C07D417/04 , C07D417/06 , C07D417/14 , C07D471/04 , C07D498/04 , C07D513/04
摘要： Compounds of formula (I) have antibacterial activity: wherein R represents hydrogen or 1, 2 or 3 optional substituents; W is ═C(R1)—; R1 is hydrogen and R2 is hydrogen, methyl, or fluorine; or R1 and R2 taken together are —CH2—, —CH2CH2, —O—, or, in either orientation, —O—CH2— or —OCH2CH2—; and R3 is a radical of formula -(Alk1)m-(Z)p-(Alk2)n-Q.
摘要翻译：式（I）化合物具有抗菌活性：其中R表示氢或1,2或3个任选的取代基; W为═C（R1） - ; R1是氢，R2是氢，甲基或氟; 或R 1和R 2一起为-CH 2 - ， - CH 2 CH 2，-O-，或者在任一取向为-O-CH 2 - 或-OCH 2 CH 2 - ; 并且R3是式 - （Alk1）m-（Z）p-（Alk2）n-Q的基团。

5. 发明申请

US20100311766A1 ANTIBACTERIAL COMPOSITIONS 审中-公开
标题翻译：抗菌成分
公开(公告)号：US20100311766A1
公开(公告)日：2010-12-09
申请号：US12747753
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： A61K31/497 , C07D513/04 , A61K31/444 , A61P31/04 , A01N43/40 , A01N43/60 , A01P1/00
CPC分类号： C07D513/04
摘要： Compounds of formula (I) have antibacterial activity wherein: m is O or 1; Q is hydrogen or cyclopropyl; AIk is an optionally substituted, divalent C1-C3 alkylene, C2-C3 alkenylene or C2-C3 alkynylene radical; X is —C(═O)NH— or —C(═O)O—; R2 and R3 are as defined in the specification.
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是任选取代的二价C 1 -C 3亚烷基，C 2 -C 3亚烯基或C 2 -C 3亚炔基; X是-C（= O）NH-或-C（= O）O-; R2和R3如说明书中所定义。

6. 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。

7. 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。

8. 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。

9. 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。

10. 发明授权

US09511073B2 Aromatic amides and uses thereof 有权
标题翻译：芳族酰胺及其用途
公开(公告)号：US09511073B2
公开(公告)日：2016-12-06
申请号：US14112735
申请日：2012-04-20
申请人： David John Haydon , Lloyd George Czaplewski , Neil Robert Stokes , David Davies , Ian Collins , James T. Palmer , Jeffrey Peter Mitchell , Gary Robert William Pitt , Daniel Offermann
发明人： David John Haydon , Lloyd George Czaplewski , Neil Robert Stokes , David Davies , Ian Collins , James T. Palmer , Jeffrey Peter Mitchell , Gary Robert William Pitt , Daniel Offermann
IPC分类号： C07D263/32 , C07D417/06 , C07D413/06 , C07D277/24 , C07D417/12 , C07D413/12 , C07D285/08 , C07D513/04 , C07D413/10 , C07D271/06 , A61K31/5377 , A61K31/166 , A61K31/4245 , A61K31/421 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/506 , C07D277/30
CPC分类号： A61K31/5377 , A61K31/166 , A61K31/421 , A61K31/4245 , A61K31/426 , A61K31/427 , A61K31/433 , A61K31/437 , A61K31/4439 , A61K31/496 , A61K31/506 , C07D263/32 , C07D271/06 , C07D277/24 , C07D277/30 , C07D285/08 , C07D413/06 , C07D413/10 , C07D413/12 , C07D417/06 , C07D417/12 , C07D513/04
摘要： The present invention provides compounds of Formula (I): and salts, racemates, isomers, diastereoisomers, enantiomers, hydrates, solvates, N-oxides, pharmaceutically acceptable derivatives or prodrugs thereof. Also provided the use of these compounds as antibacterials, compositions comprising them and processes for their manufacture.

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