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    Antibacterial agents
    1.
    发明授权
    Antibacterial agents 失效
    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。

    Hydroxamic acid derivatives as antibacterials
    6.
    发明授权
    Hydroxamic acid derivatives as antibacterials 失效
    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。

    Antibacterial hydroxamic acid derivatives
    7.
    发明授权
    Antibacterial hydroxamic acid derivatives 失效
    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。

    Antibacterial agents
    8.
    发明授权
    Antibacterial agents 失效
    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。

    Derivatives of succinamide and their use as metalloproteinase inhibitor
    9.
    发明授权
    Derivatives of succinamide and their use as metalloproteinase inhibitor 失效
    琥珀酰胺的衍生物及其作为金属蛋白酶抑制剂的用途

    公开(公告)号：US5908851A

    公开(公告)日：1999-06-01

    申请号：US930620

    申请日：1997-10-07

    申请人： Raymond Paul Beckett ,  Andrew Miller ,  Zoe Marie Spavold ,  Mark Whittaker

    发明人： Raymond Paul Beckett ,  Andrew Miller ,  Zoe Marie Spavold ,  Mark Whittaker

    IPC分类号： A61K31/195 ,  A61P1/00 ,  A61P19/10 ,  A61P25/00 ,  A61P27/02 ,  A61P29/00 ,  A61P35/00 ,  A61P37/00 ,  A61P43/00 ,  C07C237/22 ,  C07C259/06 ,  A61K31/44

    CPC分类号： C07C237/22 ,  C07C259/06

    摘要： Compounds of formula (I), ##STR1## wherein X is a --CO.sub.2 H or --CONHOH group; R.sub.4 is a group --CHR.sup.x R.sup.y wherein R.sup.x and R.sup.y independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C.sub.1 -C.sub.4 alkylene or C.sub.2 -C.sub.4 alkenylene bridge; and R.sub.1, R.sub.2, R.sub.3 and R.sub.5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72 KDa gelatinase.

    摘要翻译： PCT No.PCT / GB96 / 00965 Sec。 371日期1997年10月7日第 102（e）日期1997年10月7日PCT PCT 1996年4月18日PCT公布。 公开号WO96 / 33165 日期：10月24日，式（I）化合物，其中X为-CO 2 H或-CONHOH基; R4是基团-CHRxRy，其中Rx和Ry独立地表示任选取代的苯基或单环杂芳基环，其任选地可以通过键或通过C 1 -C 4亚烷基或C 2 -C 4亚链烯基彼此共价连接; R 1，R 2，R 3和R 5如本说明书中所定义，是相对于人成纤维细胞胶原酶和72KDa明胶酶的基质溶素-1和基质溶素的选择性抑制剂。