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1. 发明授权

US5917090A Matrix metalloproteinase inhibitors 失效
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：US5917090A
公开(公告)日：1999-06-29
申请号：US981221
申请日：1997-12-19
申请人： Philip Huxley , Fionna Mitchell Martin , Andrew Miller , Zoe Marie Spavold
发明人： Philip Huxley , Fionna Mitchell Martin , Andrew Miller , Zoe Marie Spavold
IPC分类号： C07C259/06 , A01N37/28
CPC分类号： C07C259/06
摘要： The invention is directed to therapeutically active hydroxamic acid derivatives of formula (I): ##STR1## wherein the substituents are as defined in the specification. These therapeutically active hydroxamic acid derivatives have high intrinsic activity against a broad spectrum of matrix metalloproteinases (MMPs), good oral bioavailability, and additionally inhibit tissue necrosis factor (TNF) production.
摘要翻译： PCT No.PCT / GB96 / 01578 Sec。 371 1997年12月19日第 102（e）日期1997年12月19日PCT PCT 1996年7月1日PCT公布。第WO97 / 02239号公报日期1997年1月23日本发明涉及式（I）的治疗活性异羟肟酸衍生物：其中取代基如说明书中所定义。这些治疗活性的异羟肟酸衍生物对广泛的基质金属蛋白酶（MMP）具有很高的内在活性，良好的口服生物利用度，另外抑制组织坏死因子（TNF）产生。

2. 发明授权

US5840974A Metalloproteinase inhibitors 失效
标题翻译：金属蛋白酶抑制剂
公开(公告)号：US5840974A
公开(公告)日：1998-11-24
申请号：US925592
申请日：1997-09-08
申请人： Mark Whittaker , Raymond Paul Beckett , Zoe Marie Spavold , Fionna Mitchell Martin
发明人： Mark Whittaker , Raymond Paul Beckett , Zoe Marie Spavold , Fionna Mitchell Martin
IPC分类号： A61K31/197 , A61K31/16 , A61K31/164 , A61K31/417 , A61K31/4402 , A61K31/5375 , A61P29/00 , A61P35/00 , A61P43/00 , C07C237/22 , C07C259/06 , C07D213/75 , C07D233/24 , C07D233/54 , C07D233/64 , C07D295/12 , C07D409/12 , C07C229/00
CPC分类号： C07D213/75 , C07C237/22 , C07C259/06 , C07D233/64 , C07D409/12 , C07C2101/14
摘要： Compound of formula (I) ##STR1## wherein Ar represents an optionally substituted phenyl or heteroaryl group, m is 1 or 2, n is 0, 1, 2, 3 or 4, X represents --COOH or --CONHOH and R.sub.1, R.sub.3 and Y are as defined in the specification,are inhibitors of metalloproteinases involved in tissue degradation.
摘要翻译：式（I）化合物其中Ar表示任意取代的苯基或杂芳基，m为1或2，n为0,1,2,3或4，X为-COOH或-CONHOH，R1为 R3和Y如说明书中所定义，是参与组织降解的金属蛋白酶的抑制剂。

3. 发明授权

US5908851A Derivatives of succinamide and their use as metalloproteinase inhibitor 失效
标题翻译：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。

4. 发明授权

US5840939A Derivatives of succinamide and their use as metalloproteinase inhibitors 失效
标题翻译：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：US5840939A
公开(公告)日：1998-11-24
申请号：US930619
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 , C07C231/00 , A61K31/16 , C07C229/00
CPC分类号： C07C237/22 , C07C259/06
摘要： Compounds of formula (I), wherein X is a --CO.sub.2 H or --CONHOH group; ##STR1## 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 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 / 00930 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 / 33161 日期：10月24日，式（I）化合物，其中X为-CO 2 H或-CONHOH基; （I）R 4是基团-CHR x R y，其中R x和R y独立地表示任选取代的苯基或单环杂芳基环，其任选可以通过键彼此共价连接或通过C 1 -C 4亚烷基或C 2 -C 4亚烯基彼此共价连接桥; 和说明书中定义的R1，R2，R3和R5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。

5. 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:

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

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。

8. 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。

9. 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

10. 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。

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