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1. 发明授权

US07173053B2 N-formyl hydroxylamine derivatives as inhibitors of bacterial polypeptide formylase for treating microbial infections 失效
标题翻译： N-甲酰基羟胺衍生物作为细菌多肽甲酰化酶的抑制剂用于治疗微生物感染
公开(公告)号：US07173053B2
公开(公告)日：2007-02-06
申请号：US10432252
申请日：2001-11-08
申请人： Paul Raymond Beckett , Steven Launchbury , Gilles Pain , Lisa Marie Pratt
发明人： Paul Raymond Beckett , Steven Launchbury , Gilles Pain , Lisa Marie Pratt
IPC分类号： A61K31/4164 , C07D235/04
CPC分类号： C07D233/64 , A61K31/417 , C07D235/14 , Y02A50/411
摘要： Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(═O) or formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluromethyl, or except when Z is a radical of formula —N(OH)(═O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1–C6) alkyl or phenyl(C1–C6)alkyl-; and R5 and R6 are as defined in the specification.
摘要翻译：式（I）化合物是用于治疗人和非人哺乳动物感染的抗细菌剂或抗原虫剂，其中：Z代表式-N（OH）CH（-O）或式C（-O）NH（哦）; 除了当Z是式-N（OH）（ - O），羟基，卤素或氨基的基团时，R 1表示氢，甲基或三氟甲基; R 2表示基团R 10 - （X）n - （ALK）m - 其中R _{10，ALK，X，m和n如说明书中所定义; R 3表示氢，（C 1 -C 6 -C 6）烷基或苯基（C 1 -C 3 - 亚<！ - SIPO < > 6 ）烷基 - ; 和R 5和R 6是如说明书中所定义的。}

2. 发明申请

US20060276409A1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US20060276409A1
公开(公告)日：2006-12-07
申请号：US11497277
申请日：2006-08-02
申请人： Michael Hunter , Raymond Beckett , John Clements , Mark Whittaker , Stephen Davies , Lisa Pratt , Zoe Spavold , Steven Launchbury
发明人： Michael Hunter , Raymond Beckett , John Clements , Mark Whittaker , Stephen Davies , Lisa Pratt , Zoe Spavold , Steven Launchbury
IPC分类号： A61K38/05 , A61K38/04 , A61K31/445 , A61K31/34 , A61K31/198
CPC分类号： C07C259/06 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/198 , A61K31/40 , A61K31/401 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/5375 , C07C239/14 , C07C323/60 , C07C2601/08 , C07C2601/14 , C07D213/75 , C07D217/26 , C07D263/26 , C07D295/185 , C07K5/0202
摘要： Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and m and n are independently 0 or 1; and A represents a group as defined in the specification.
摘要翻译：式（I）的化合物是抗细菌剂：其中：R 1表示氢或C 1 -C 6烷基或C 1 被一个或多个卤素原子取代的C 6 -C 6烷基; R 2表示基团R 10 - （X）n - （ALK）m - 其中R _{10 表示氢或C 1 -C 6烷基，C 2 -C 6亚烷基，C 2 -C 6 烯基，C 2 -C 6炔基，环烷基，芳基或杂环基，其中任何一个可以是未被取代的或被（C 1〜（C 1 -C 6）烷基，（C 1 -C 6 -C 6）烷氧基，羟基，巯基，（C 1 -C 6）烷基，烷基硫基，氨基，卤代（包括氟，氯，溴和碘），三氟甲基，氰基，硝基，-COOH，-CONH 2 - ， - COOR 其中，-NHCOR，A，A，A，A，O，或其中R A和R B各自独立地选自：其中R A，R B，R B， SUP>独立地为（C 1 -C 6 -C 6）烷基，ALK表示直链或支链二价C 1 -C 3 > 6个亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基（C 1 -C 6亚烷基）激进并且可以被一个或多个不相邻的-NH-，-O-或-S-键中断，X表示-NH-，-O-或-S-，m和n独立地为0或1; 并且A表示说明书中定义的组。}

3. 发明申请

US20070129310A1 Antibacterial agents 审中-公开
标题翻译：抗菌剂
公开(公告)号：US20070129310A1
公开(公告)日：2007-06-07
申请号：US10530406
申请日：2002-12-02
申请人： Raymond Beckett , Jac Wijkmans , Thomas Krulle
发明人： Raymond Beckett , Jac Wijkmans , Thomas Krulle
IPC分类号： A61K38/05 , A61K38/04 , A61K31/541 , A61K31/5377 , A61K31/496 , A61K31/551 , A61K31/55 , A61K31/454 , A61K31/427
CPC分类号： C07D295/185 , C07D295/194 , C07D295/205 , C07D295/21 , C07D295/215
摘要： Compounds of formula (II) have antibacterial activity: wherein: Q represents a radical of formula —N(OH)CH(═0) or formula —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Q is a radical of formula —N(OH)CH(═0), a hydroxy, halo or amino group; R2 represents a group R10—(D)n—(ALK)m— wherein R10 represents hydrogen or an optionally substituted C-C6 alkyl, C2-C6 alkynyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group and ALK represents a straight or branched divalent C-C6 alkylene, C2-C6 alkynylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O—or -Slinkages, D represents —NH—, —O—or —S—, and m and n are independently 0 or 1; R4 represents the side chain of a natural or non-natural alpha amino acid; ring A represents an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom shown, the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen; X is oxygen or sulfur; Y is oxygen, sulfur or —NH—; R is 0, 1, 2 or 3; and ring B represents an optionally substituted carbocyclic or heterocyclic ring system.
摘要翻译：式（II）化合物具有抗菌活性：其中：Q表示式-N（OH）CH（-O）或式-C（ - ） - NH（OH）的基团; 除了当Q是式-N（OH）CH（-O），羟基，卤素或氨基的基团时，R 1表示氢，甲基或三氟甲基。 R 2表示基团R 10 - （D）n - （ALK）m - 其中R _{10 表示氢或任选取代的C 1 -C 6烷基，C 2 -C 6亚烷基炔基，C 2 -C 6炔基，环烷基，芳基或杂环基，并且ALK表示直链或支链二价C 1 -C 6烷基，亚烷基，C 2 -C 6亚炔基或C 2 -C 6亚烷基，或C 1 -C 6亚烷基，亚炔基，并且可以被一个或多个不相邻的-NH-，-O-或-S-链接间隔，D表示-NH-，-O-或-S-，m和n独立地为0或1; R 4表示天然或非天然α氨基酸的侧链; 环A表示含有5至7个环原子的任选取代的单环杂环，其中一个是所示的氮原子，剩余的环原子选自碳，氧，硫和氮的相容组合; X是氧或硫; Y是氧，硫或-NH-; R为0,1,2或3; 环B表示任选取代的碳环或杂环系。}

4. 发明申请

US20090069322A1 N-FORMYL HYDROXYLAMINE DERIVATIVES AS INHIBITORS OF BACTERIAL POLYPEPTIDE FORMYLASE FOR TREATING MICROBIAL INFECTIONS 审中-公开
标题翻译：作为细菌多肽甲醛酶抑制剂的N-甲基羟甲苯胺衍生物用于治疗微生物感染
公开(公告)号：US20090069322A1
公开(公告)日：2009-03-12
申请号：US11526591
申请日：2006-09-26
申请人： Paul Raymond Beckett , Steven Launchbury , Gilles Pain , Lisa Marie Pratt
发明人： Paul Raymond Beckett , Steven Launchbury , Gilles Pain , Lisa Marie Pratt
IPC分类号： A61K31/5377 , A61K31/496 , A61K31/454 , A61K31/4439 , A61K31/426 , A61K31/4166 , C07D403/02 , C07D413/02 , C07D417/02
CPC分类号： C07D233/64 , A61K31/417 , C07D235/14 , Y02A50/411
摘要： Compounds of formula (I) are antibacterial or antiprotozoal agents for treatment of infections in humans and non-human mammals, wherein: Z represents a radical of formula —N(OH)CH(═O) or formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or except when Z is a radical of formula —N(OH)CH(═O), a hydroxy, halo or amino group; R2 represents a group R10—(X)n-(ALK)m— wherein R10, ALK, X, m and n are as defined in the specification; R3 represents hydrogen, (C1-C6) alkyl or phenyl(C1-C6)alkyl-; and R5 and R6 are as defined in the specification.
摘要翻译：式（I）化合物是用于治疗人和非人哺乳动物感染的抗细菌剂或抗原虫剂，其中：Z代表式-N（OH）CH（-O）或式C（-O）NH（哦）; 除了当Z是式-N（OH）CH（-O），羟基，卤素或氨基的基团时，R 1表示氢，甲基或三氟甲基。 R2表示R10-（X）n-（ALK）m-基团，其中R10，ALK，X，m和n如说明书中所定义; R3表示氢，（C1-C6）烷基或苯基（C1-C6）烷基 - ; R5和R6如说明书中所定义。

5. 发明授权

US07323563B2 Hydroxamic acid derivatives as antibacterials 失效
标题翻译：羟肟酸衍生物作为抗菌剂
公开(公告)号：US07323563B2
公开(公告)日：2008-01-29
申请号：US11207813
申请日：2005-08-22
申请人： Michael George Hunter , Paul Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
发明人： Michael George Hunter , Paul Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
IPC分类号： C07D279/12 , A61K31/54
CPC分类号： A61K31/4453 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/19 , A61K31/22 , A61K31/40 , A61K31/426 , A61K31/4402 , A61K31/445
摘要： A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:
摘要翻译：一种治疗人和非人哺乳动物细菌感染的方法，其包括通过向受试者施用抗菌有效剂量的式（I）化合物或其药学上或兽医学上可接受的盐来抑制细菌生长：

6. 发明申请

US20060211732A1 Hydroxamic acid derivatives as antibacterials 失效
公开(公告)号：US20060211732A1
公开(公告)日：2006-09-21
申请号：US11207813
申请日：2005-08-22
申请人： Michael George Hunter , Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Spavold
发明人： Michael George Hunter , Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Spavold
IPC分类号： A61K31/445 , A61K31/40 , A61K31/19
CPC分类号： A61K31/4453 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/19 , A61K31/22 , A61K31/40 , A61K31/426 , A61K31/4402 , A61K31/445
摘要： A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:

7. 发明申请

US20050159412A1 Bacterial enzyme inhibitors 失效
标题翻译：细菌酶抑制剂
公开(公告)号：US20050159412A1
公开(公告)日：2005-07-21
申请号：US10497494
申请日：2002-11-27
申请人： Paul Gane , Barry Porter , Henriette Willems , Raymond Beckett , Kenneth Keavey
发明人： Paul Gane , Barry Porter , Henriette Willems , Raymond Beckett , Kenneth Keavey
IPC分类号： A61P31/04 , C07C275/24 , C07D213/40 , C07D295/215 , C07D279/12 , A61K31/18 , A61K31/495 , A61K31/537 , A61K31/54 , C07D265/30
CPC分类号： C07D213/40 , C07C275/24 , C07C2601/08 , C07D295/215
摘要： Compounds of formula (I) are antibacterial agents: wherein: Z is —N(OH)CH(═O) or —C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl or, except when Z is a radical of formula —N(OH)CH(═O), a hydroxy, halo or amino group; R2, R3 and R4 independently represents hydrogen or a group R10-(D)n-(ALK)m- wherein R10, D, n, m and ALK are as defined in the claims; or R3 and R4 taken together with the nitrogen atom to which they are attached form an optionally substituted monocyclic heterocyclic ring containing from 5 to 7 ring atoms, one of which is the nitrogen atom to which R4 and R5 are attached and the remaining ring atoms being selected from compatible combinations of carbon, oxygen, sulfur and nitrogen.
摘要翻译：式（I）化合物是抗菌剂：其中：Z是-N（OH）CH（-O）或-C（-O）NH（OH）; 除了当Z是式-N（OH）CH（-O），羟基，卤素或氨基的基团时，R 1表示氢，甲基或三氟甲基。 R 2，R 3和R 4独立地表示氢或基团R 10 - （D）

8. 发明授权

US07323596B2 Antimicrobial agents 失效
标题翻译：抗微生物剂
公开(公告)号：US07323596B2
公开(公告)日：2008-01-29
申请号：US10433625
申请日：2001-12-21
申请人： Barry Porter , Paul Gane , Raymond Beckett , Kenneth Keavey , Jac Wijkmans , Lydia Saroglou
发明人： Barry Porter , Paul Gane , Raymond Beckett , Kenneth Keavey , Jac Wijkmans , Lydia Saroglou
IPC分类号： C07C239/00 , C07C259/00 , C07C303/00 , C07C307/00 , C07C309/00 , C07C311/00
CPC分类号： C07D285/10 , C07C259/06 , C07C311/19 , C07D209/18 , C07D215/56 , C07D217/22 , C07D263/12 , C07D311/12 , C07D491/04
摘要： Compounds of formula (I) and (IA) have antibacterial or antiprotozoal activity: formula (1) formula (2) wherein: Z represents a radical of formula N(OH)CH(═O) or of formula C(═O)NH(OH); R1 represents hydrogen, methyl or trifluoromethyl, or, except when Z is a radical of formula N(OH)CH(═O), a hydroxy or amino group; R2 represents a radical of formula R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or an optionally substituted c1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 ?alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent NH—, —O— or S— linkages, X represents NH—, —O— or S—, and m and n are independently 0 or 1; R3 represents hydrogen, C1-C6alkyl, or benzyl; and R4 is as defined in the specification.
摘要翻译：式（I）和（IA）的化合物具有抗菌或抗原虫活性：式（1）式（2）其中：Z表示式N（OH）CH（-O）或式C（-O）NH （哦）; R 1表示氢，甲基或三氟甲基，或除Z是式N（OH）CH（-O），羟基或氨基基团时; R 2表示式R 10 - （X）n - （ALK）m - 的基团，其中R C 1 -C 10烷基，C 2 -C 6烷基，C 2 -C 6烷基，C 1 -C 6烷基，C 1 -C 6烷基， 6个烯基，C 2 -C 6炔基，环烷基，芳基或杂环基，ALK表示直链或支链二价C 1 - “C” - “C” - “00”“”=“2.46mm”wi =“1.44mm”file = “US07323596-20080129-P00001.TIF”alt =“自定义字符”img-content =“character”img-format =“tif”/> 6亚链烯基或C 2 -C 6个亚炔基，并且可以被一个或多个不相邻的NH-，-O-或S-键间隔，X表示NH-，-O-或S-，m和n独立地为0或 1; R 3表示氢，C 1 -C 6烷基或苄基; R 4和R 4如本说明书中所定义。

9. 发明授权

US06992190B2 Hydroxamic acid derivatives as antibacterials 失效
公开(公告)号：US06992190B2
公开(公告)日：2006-01-31
申请号：US10179227
申请日：2002-06-26
申请人： Michael George Hunter , Paul Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
发明人： Michael George Hunter , Paul Raymond Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
IPC分类号： C07D211/06 , A61K31/445
CPC分类号： A61K31/4453 , A61K31/16 , A61K31/165 , A61K31/167 , A61K31/19 , A61K31/22 , A61K31/40 , A61K31/426 , A61K31/4402 , A61K31/445
摘要： A method for the treatment of bacterial infections in humans and non-human mammals, which comprises inhibiting bacterial growth by administering to a subject an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof:

10. 发明申请

US20050014702A1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US20050014702A1
公开(公告)日：2005-01-20
申请号：US10901065
申请日：2004-07-29
申请人： Michael Hunter , Raymond Beckett , John Clements , Mark Whittaker , Stephen Davies , Lisa Pratt , Zoe Spavold , Steven Launchbury
发明人： Michael Hunter , Raymond Beckett , John Clements , Mark Whittaker , Stephen Davies , Lisa Pratt , Zoe Spavold , Steven Launchbury
IPC分类号： G01N33/50 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/198 , A61K31/40 , A61K31/401 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/5375 , A61P31/04 , C07C259/06 , C07C323/60 , C07D207/08 , C07D207/16 , C07D211/16 , C07D211/32 , C07D211/62 , C07D213/75 , C07D215/08 , C07D217/26 , C07D233/54 , C07D295/14 , C07D295/18 , G01N33/15 , A61K38/04 , A61K31/455 , C07K5/04
CPC分类号： C07C259/06 , A61K31/00 , A61K31/16 , A61K31/164 , A61K31/165 , A61K31/198 , A61K31/40 , A61K31/401 , A61K31/4402 , A61K31/445 , A61K31/4453 , A61K31/47 , A61K31/472 , A61K31/495 , A61K31/5375 , C07C239/14 , C07C323/60 , C07C2601/08 , C07C2601/14 , C07D213/75 , C07D217/26 , C07D263/26 , C07D295/185 , C07K5/0202
摘要： Compounds of formula (I) are antibacterials: wherein: R1 represents hydrogen, or C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10—(X)n-(ALK)m- wherein R10 represents hydrogen, or a C1-C6 alkyl, C2-C6 alkenyl, C2-C6 alkynyl, cycloalkyl, aryl, or heterocyclyl group, any of which may be unsubstituted or substituted by (C1-C6)alkyl, (C1-C6)alkoxy, hydroxy, mercapto, (C1-C6)alkylthio, amino, halo (including fluoro, chloro, bromo and iodo), trifluoromethyl, cyano, nitro, —COOH, —CONH2, —COORA, —NHCORA, —CONHRA, —NHRA, —NRARB, or —CONRARB wherein RA and RB are independently a (C1-C6)alkyl group, and ALK represents a straight or branched divalent C1-C6 alkylene, C2-C6 alkenylene, or C2-C6 alkynylene radical, and may be interrupted by one or more non-adjacent —NH—, —O— or —S— linkages, X represents —NH—, —O— or —S—, and m and n are independently 0 or 1; and A represents a group as defined in the specification.
摘要翻译：式（I）化合物是抗菌剂：其中：R1代表氢，或C1-C6烷基或被一个或多个卤原子取代的C1-C6烷基; R 2表示R 10 - （X）n-（ALK）m - ，其中R 10表示氢，或C 1 -C 6烷基，C 2 -C 6烯基，C 2 -C 6炔基，环烷基，芳基或杂环基，其中任何一个可以羟基，巯基，（C 1 -C 6）烷硫基，氨基，卤素（包括氟，氯，溴和碘），三氟甲基，氰基，硝基，（C 1 -C 6）烷氧基， -COOH，-CONH 2，-COOR A，-NHCOR A，-CONHR A，-NHR A，-NR A R B或-CONR R B，其中R A和R B独立地为（C 1 -C 6）烷基，并且ALK表示直链或支链二价C 1 -C 6亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基，并且可被中断通过一个或多个不相邻的-NH-，-O-或-S-键，X表示-NH-，-O-或-S-，m和n独立地为0或1; 并且A表示说明书中定义的组。

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