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1. 发明授权

US06423690B1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US06423690B1
公开(公告)日：2002-07-23
申请号：US09355489
申请日：2000-01-07
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
IPC分类号： A61K3116
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： A method for the treatment of bacterial infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterially effective dose of a compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof: 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：一种用于治疗人和非人哺乳动物细菌感染的方法，其包括向患有这种感染的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：其中：R1代表氢或C 1 -C 6烷基或被一个或多个卤素原子取代的C 1 -C 6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，-COORA，-NHCORA，-CONHRA，NHRA，-NRARB或-CONRARB，其中RA和RB独立地为（C 1 -C 6）烷基，ALK表示直链或支链二价C1-C6亚烷基，C 2 -C 6亚烯基或C 2 -C 6亚炔基，并且可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; 并且A表示说明书中定义的组。

2. 发明授权

US07323448B2 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US07323448B2
公开(公告)日：2008-01-29
申请号：US11497277
申请日：2006-08-02
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
IPC分类号： A61K38/05 , C07C259/04 , C07K5/06
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) or a pharmaceutically or veterinarily acceptable salts thereof wherein R1 represents hydrogen, C1-C6 alkyl or C1-C6 alkyl substituted by one or more halogen atoms; R2 represents a group R10-(ALK)m-, and A represents (i) a group of formula (IA): wherein the compounds inhibit the activity of bacterial PDF enzyme.
摘要翻译：式（I）化合物或其药学上或兽医学上可接受的盐，其中R 1表示氢，C 1 -C 6烷基或C 1 -C 6烷基，被一个或多个卤素原子取代的C 1 -C 6烷基; R 2表示基团R 10 - （ALK）m - ，A表示（i）式（IA）的基团：其中该化合物抑制细菌PDF酶的活性。

3. 发明授权

US07148198B2 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US07148198B2
公开(公告)日：2006-12-12
申请号：US10901065
申请日：2004-07-29
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
IPC分类号： A61K38/05 , C07C259/04
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： A compound of formula (I) or a pharmaceutically or veterinarily acceptable salt thereof for the inhibition of activity of bacterial PDF enzyme: wherein A represents a group of formula (IA) or (IB) and wherein R1 is hydrogen, R2 is n-butyl, benzyl or cyclopentylmethyl, R3 is hydrogen, R4 is tert-butyl, iso-butyl, benzyl or methyl, R5 is hydrogen or methyl and R6 is methyl.
摘要翻译：式（I）化合物或其药学上或兽医学上可接受的盐用于抑制细菌性PDF的活性：其中A表示式（IA）或（IB）的基团，其中R 1，是氢，R 2是正丁基，苄基或环戊基甲基，R 3是氢，R 4是叔丁基，异丁基，苄基或甲基，R 5是氢或甲基，R 6是甲基。

4. 发明授权

US06908911B1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US06908911B1
公开(公告)日：2005-06-21
申请号：US10049274
申请日：1999-08-10
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
IPC分类号： A61P31/04 , C07C259/06 , C07C279/14 , C07C321/16 , C07D211/16 , C07D211/48 , C07D211/58 , C07D211/60 , C07D217/06 , C07D295/185 , C07D295/205 , C07D295/32 , A61K31/33 , A61K31/16 , A61K31/19
CPC分类号： C07D295/185 , C07C259/06 , C07C279/14 , C07C321/16 , C07D211/16 , C07D211/48 , C07D211/58 , C07D211/60 , C07D217/06 , C07D295/205 , C07D295/32
摘要： Selected compounds of formula (I) are antibacterial agents: formula (I) wherein R2 represents a substituted or unsubstituted C1-C6 alkyl, cycloalkyl (C1-C6 alkyl)- or aryl (C1-C6 alkyl)-group, and A represents a group of formula (IA), or (IB) wherein R4 represents the side chain of a natural or non-natural alpha amino acid, and R5 and R6 are each independently hydrogen or C1-C6 alkyl, heterocyclic or aryl (C1-C6 alkyl)-, R5 and R6 when taken together with the nitrogen atom to which they are attached from an optionally substituted saturated heterocyclic ring of 3 to 8 atoms which ring is optionally fused to a carbocyclic or second heterocyclic ring
摘要翻译：选择的式（I）化合物是抗细菌剂：式（I）其中R 2代表取代或未取代的C 1 -C 6烷基，环烷基（C 1 -C 6烷基） - 或芳基（C 1 -C 6 -C 6烷基） - 基团，A表示式（IA）或（IB）的基团，其中R 4代表天然或非天然α氨基酸的侧链，R 5， R 3和R 6各自独立地为氢或C 1 -C 6烷基，杂环或芳基（C 1〜 -C 6 -C 6烷基） - ，R 5和R 6与它们所连接的氮原子一起从任选取代的 3至8个原子的饱和杂环，其任选地与碳环或第二个杂环稠合

5. 发明授权

US06787522B2 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US06787522B2
公开(公告)日：2004-09-07
申请号：US10134754
申请日：2002-04-30
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Stephen John Davies , Lisa Marie Pratt , Zoe Marie Spavold , Steven Launchbury
IPC分类号： A61K3116
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。

6. 发明授权

US06441042B1 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：US06441042B1
公开(公告)日：2002-08-27
申请号：US09700424
申请日：2000-11-15
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker , Zoe Marie Spavold
IPC分类号： A61K3119
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： 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表示氢，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） -COOH，-CONH 2，-COORA，-NHCORA，-CONHRA，-NHRA，-NRARB或-CONRARB，其中RA和RB独立地为（C 1 -C 6）烷基，ALK表示直链或支链二价C1-C6 亚烷基，C 2 -C 6亚烯基或C 2 -C 6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; 并且A表示说明书中定义的组。

7. 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:

8. 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：

9. 发明授权

US06545051B1 Antibacterial hydroxamic acid derivatives 失效
标题翻译：抗菌异羟肟酸衍生物
公开(公告)号：US06545051B1
公开(公告)日：2003-04-08
申请号：US09889801
申请日：2001-07-20
申请人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker
发明人： Michael George Hunter , Raymond Paul Beckett , John Martin Clements , Mark Whittaker
IPC分类号： A61K3119
CPC分类号： A61K31/215 , A61K31/22 , A61K31/255
摘要： A method for the treatment of bacterial infections in humans and non-human mammals, which comprises administering to a subject suffering such infection an antibacterial effective dose of a compound of formula (I): wherein R1 represents hydrogen, hydroxy, amino, methyl, or trifluoromethyl; R2 represents a group R10—(X)n—(ALK)— wherein R10 represents hydrogen, a 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, 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 n is 0 or 1; R represents hydrogen or C1-C6 alkyl; R3 represents the characterising group of a natural or non-natural &agr; amino acid in which any functional groups may be protected; and R4 represents an ester or thioester group.
摘要翻译：一种用于治疗人和非人哺乳动物细菌感染的方法，其包括向患有这种感染的受试者施用抗菌有效剂量的式（I）化合物：其中R 1表示氢，羟基，氨基，甲基或三氟甲基 R 2表示R 10 - （X）n-（ALK） - ，其中R 10表示氢，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，ALK表示直链或支链二价C 1 -C 6亚烷基，C 2 -C 6亚烯基，C 2 -C 6亚炔基，并且可被一个或多个不相邻的-NH-，-O-或-S-键间隔; X表示-NH-，-O-或-S-，n表示0或1; R代表氢或C1-C6烷基; R3表示可以保护任何官能团的天然或非天然α氨基酸的表征基团; 并且R 4表示酯或硫酯基。

10. 发明授权

US06503897B1 Antibacterial agents 失效
标题翻译：抗菌剂
公开(公告)号：US06503897B1
公开(公告)日：2003-01-07
申请号：US09914049
申请日：2001-08-22
申请人： Raymond Paul Beckett , Mark Whittaker , Zoe Marie Spavold
发明人： Raymond Paul Beckett , Mark Whittaker , Zoe Marie Spavold
IPC分类号： C07D28106
CPC分类号： C07D513/04 , C07D211/76 , C07D223/12 , C07D225/02 , C07D243/08 , C07D245/02 , C07D281/06 , C07D327/02
摘要： Compounds of formula (I) are antibacterial agents wherein: R3 and R4, taken together with the carbon atoms to which they are respectively attached, form an optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms, which may be benz-fused or fused to a second optionally substituted saturated carbocyclic or heterocyclic ring of 5 to 16 atoms; and R1 and R2 are as defined in the specification.
摘要翻译：式（I）化合物是抗菌剂，其中：R3和R4与它们分别连接的碳原子一起形成任选取代的5至16个原子的饱和碳环或杂环，其可以是苯并稠合的或与5至16个原子的第二任选取代的饱和碳环或杂环稠合; R1和R2如说明书中所定义。

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