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1. 发明申请

WO1998024759A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1998024759A1
公开(公告)日：1998-06-11
申请号：PCT/GB1997003316
申请日：1997-12-02
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , WHITTAKER, Mark , BECKETT, Raymond, Paul , SPAVOLD, Zoe, Marie , MARTIN, Fionna, Mitchell
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07D213/75 , C07C237/22 , C07C259/06 , C07C2601/14 , C07D233/64 , C07D409/12
摘要： Compound of formula (I) 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 R1, R3 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表示任选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，R3和Y为在说明书中定义的是参与组织降解的金属蛋白酶的抑制剂。

2. 发明申请

WO1996033997A1 BENZIMIDAZOLE DERIVATIVES BEING DUAL HISTAMINE (H1) AND PLATELET ACTIVATING FACTOR (PAF) ANTAGONISTS 审中-公开
标题翻译：苯并咪唑衍生物是双组胺（H1）和平板激活因子（PAF）拮抗剂
公开(公告)号：WO1996033997A1
公开(公告)日：1996-10-31
申请号：PCT/GB1996000680
申请日：1996-03-22
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , MARTIN, Fionna, Mitchell , FLOYD, Christopher, David , SPAVOLD, Zoe, Marie , AYSCOUGH, Andrew, Paul , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04
摘要： Compounds of formula (I), wherein the variable substituents and groups are as defined in the specification, are dual histamine (H1) and platelet activating factor (PAF) antagonists.
摘要翻译：其中可变取代基和基团如说明书中所定义的式（I）化合物是双组胺（H1）和血小板活化因子（PAF）拮抗剂。

3. 发明申请

WO1996033161A1 DERIVATIVES OF SUCCINAMIDE AND THEIR USE AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：磺胺嘧啶的衍生物及其作为金属蛋白酶抑制剂的用途
公开(公告)号：WO1996033161A1
公开(公告)日：1996-10-24
申请号：PCT/GB1996000930
申请日：1996-04-18
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , MILLER, Andrew , SPAVOLD, Zoe, Marie , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C237/22
CPC分类号： C07C237/22 , C07C259/06
摘要： Compounds of formula (I), wherein X is a -CO2H or -CONHOH group; R4 is a group -CHR R wherein R and R independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C1-C4 alkylene or C2-C4 alkenylene bridge; and R1, R2, R3 and R5 as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72KDa gelatinase.
摘要翻译：式（I）化合物，其中X为-CO 2 H或-CONHOH基团; 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，其任选地可以通过键彼此共价连接或通过C1- C4亚烷基或C2-C4亚烯基桥; 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。

4. 发明申请

WO1996033165A1 DERIVATIVES OF SUCCINAMIDE AND THEIR USE AS METALLOPROTEINASE INHIBITOR 审中-公开
标题翻译：磺胺嘧啶的衍生物及其作为金属蛋白酶抑制剂的用途
公开(公告)号：WO1996033165A1
公开(公告)日：1996-10-24
申请号：PCT/GB1996000965
申请日：1996-04-18
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , MILLER, Andrew , SPAVOLD, Zoe, Marie , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C237/22 , C07C259/06
摘要： Compounds of formula (I), wherein X is a -CO2H or -CONHOH group; R4 is a group -CHR R wherein R and R independently represent optionally substituted phenyl or monocyclic heteroaryl rings, which optionally may be linked covalently to each other by a bond or by a C1-C4 alkylene or C2-C4 alkenylene bridge; and R1, R2, R3 and R5 are as defined in the specification are selective inhibitors of stromelysin-1 and matrilysin relative to human fibroblast collagenase and 72KDa gelatinase.
摘要翻译：式（I）的化合物，其中X是-CO 2 H或-CONHOH基团; 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，其任选地可以通过键彼此共价连接或通过C1- C4亚烷基或C2-C4亚烯基桥; R1，R2，R3和R5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。

5. 发明申请

WO1998017655A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1998017655A1
公开(公告)日：1998-04-30
申请号：PCT/GB1997002891
申请日：1997-10-20
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , MARTIN, Fionna, Mitchell , MILLER, Andrew , TODD, Richard, Simon , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07D295/18
CPC分类号： C07D295/185 , C07D295/26 , Y02P20/55
摘要： Compounds of formula (I), wherein n, V, R1, R2, R3 and R4 are as defined in the specification are matrix metalloproteinase inhibitors.
摘要翻译：式（I）化合物，其中n，V，R 1，R 2，R 3和R 4如本说明书中所定义的是基质金属蛋白酶抑制剂。

6. 发明申请

WO1996016931A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1996016931A1
公开(公告)日：1996-06-06
申请号：PCT/GB1995002770
申请日：1995-11-27
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , WHITTAKER, Mark , MILLER, Andrew , MARTIN, Fionna, Mitchell
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C235/70
CPC分类号： C07C237/22 , C07C259/06 , C07D333/34
摘要： Compounds of general formula (I), principally characterized in that R4 is a polyether group, are water soluble matrix metalloproteinase inhibitors.
摘要翻译：通式（I）的化合物，其主要特征在于R4是聚醚基，是水溶性基质金属蛋白酶抑制剂。

7. 发明申请

WO1995019956A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1995019956A1
公开(公告)日：1995-07-27
申请号：PCT/GB1995000111
申请日：1995-01-20
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , WHITTAKER, Mark , MILLER, Andrew , MARTIN, Fionna, Mitchell
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07D213/75 , C07C237/22 , C07C259/06 , C07D213/89 , C07D277/46 , C07D285/135 , C07D333/34 , C07D401/12 , C07D409/12 , C07D417/12
摘要： Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a -CO2H or -CONHOH group; R4 is a phenyl or 5- or 6-membered heteroaryl ring wherein any ring nitrogen atom may be oxidised as an N-oxide, which may be optionally fused to a benzene ring or to a 5-, 6- or 7-membered heterocyclic ring, and wherein any of the rings may be optionally substituted.
摘要翻译：基质金属蛋白酶抑制性化合物（I），其中X是-CO 2 H或-CONHOH基团; R4是苯基或5-或6-元杂芳基环，其中任何环氮原子可以被氧化为N-氧化物，其可以任选地与苯环稠合，或者与5-环，6-或7-元杂环稠合，并且其中任何环可以任选被取代。

8. 发明申请

WO1999025693A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1999025693A1
公开(公告)日：1999-05-27
申请号：PCT/GB1997003132
申请日：1997-11-13
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , WHITTAKER, Mark , MILLER, Andrew , MARTIN, Fionna, Mitchell
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07D213/75
CPC分类号： C07D213/75
摘要： The compound N -[2,2-dimethyl -1S-(pyridin-2- ylcarbamoyl)-propyl] -N -hydroxy-2R- isobutyl-3S-methoxy- succinamide is a matrix metalloproteinase inhibitor.
摘要翻译：化合物N 1 - [2,2-二甲基-1S-（吡啶-2-基氨基甲酰基） - 丙基] -N 4 - 羟基-2R-异丁基-3S-甲氧基 - 琥珀酰胺是基质金属蛋白酶抑制剂。

9. 发明申请

WO1997002239A1 MATRIX METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：基质金属蛋白酶抑制剂
公开(公告)号：WO1997002239A1
公开(公告)日：1997-01-23
申请号：PCT/GB1996001578
申请日：1996-07-01
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , HUXLEY, Philip , MARTIN, Fionna, Mitchell , MILLER, Andrew , SPAVOLD, Zoe, Marie
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C259/06
摘要： Compounds of formula (I), wherein R2 represents a group R6-A- wherein A represents a divalent straight or branched, saturated or unsaturated hydrocarbon chain of up to 12 C atoms and R6 represents hydrogen or an optionally substituted aryl, heterocyclyl, cycloalkyl or cycloalkenyl group; and R4 and R5 each independently represents hydrogen, a C1-C4 alkyl group, or an aryl(C1-C4 alkyl) group, have matrix metalloproteinase inhibitory activity.
摘要翻译：式（I）化合物，其中R 2表示基团R 6 -A-，其中A表示直至12个C原子的二价直链或支链饱和或不饱和烃链，R6表示氢或任选取代的芳基，杂环基，环烷基或环烯基 R4和R5各自独立地表示氢，C1-C4烷基或芳基（C1-C4烷基）基团具有基质金属蛋白酶抑制活性。

10. 发明申请

WO1995032944A1 SUCCINYL HYDROXAMIC ACID, N-FORMYL-N-HYDROXY AMINO CARBOXYLIC ACID AND SUCCINIC ACID AMIDE DERIVATIVES AS METALLOPROTEASE INHIBITORS 审中-公开
标题翻译：亚磺酸羟基酸，N-甲醛-N-羟基氨基羧酸和作为金属蛋白酶抑制剂的磺酸酰胺衍生物
公开(公告)号：WO1995032944A1
公开(公告)日：1995-12-07
申请号：PCT/GB1995001226
申请日：1995-05-26
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , MILLER, Andrew , BECKETT, Paul, Raymond , MARTIN, Fionna, Mitchell , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C237/22
CPC分类号： C07C259/06 , C07C237/22 , C07C323/60 , Y10S514/825 , Y10S514/902 , Y10S514/925
摘要： Compounds of general formula (I) wherein X is a -CO2H, -N(OH)CHO or -CONHOH group; R1 is hydrogen; (C1-C6)alkyl; (C2-C6)alkenyl; phenyl; substituted phenyl; phenyl(C1-C6)alkyl; substituted phenyl(C1-C6)alkyl; heterocyclyl; substituted heterocyclyl; heterocyclyl(C1-C6)alkyl; substituted heterocyclyl(C1-C6)alkyl; a group BSOnA- wherein n is 0, 1 or 2 and B is hydrogen or a (C1-C6)alkyl, phenyl, substituted phenyl, heterocyclyl, (C1-C6)acyl, phenacyl or substituted phenacyl group, and A represents (C1-C6)alkyl; amino; protected amino; acylamino; OH; SH; (C1-C6)alkoxy; (C1-C6)alkylamino; di-(C1-C6)alkylamino; (C1-C6)alkylthio; aryl (C1-C6)alkyl; amino(C1-C6)alkyl; hydroxy(C1-C6)alkyl, mercapto(C1-C6)alkyl or carboxy(C1-C6)alkyl wherein the amino-, hydroxy-, mercapto- or carboxyl-groups are optionally protected or the carboxyl-group amidated; lower alkyl substituted by carbamoyl, mono(lower alkyl)carbamoyl, di(lower alkyl)carbamoyl, di(lower alkyl)amino, or carboxy-lower alkanoylamino; R2 represents a linear saturated or unsaturated C13-C24 hydrocarbon chain, which chain (i) may be interrupted by one or more non-adjacent -O- or -S- atoms or -C(=O)-, -S(}O)-, -S(=O)2- or -N(Rx)- groups wherein Rx is hydrogen, methyl or ethyl, provided that the maximum length of the chain is no more than 28 C, O, S and N atoms, and/or (ii) may be substituted with one ore more groups selected from C1-C6 alkyl, OH, OMe, halogen, NH2, NHCH3, N(CH3)2, CO2H, CO2CH3, COCH3, CHO, CONH2, CONHCH3, CON(CH3)2, CH2OH, NHCOCH3, provided that the maximum length of the chain is no more than 28 C, O, S and N atoms; R3 is the characterising side chain of a natural or non-natural alpha amino acid in which any functional groups may be protected, with the proviso that R3 does not represent hydrogen; R4 is hydrogen, C1-C6 alkyl, (C1-C4)perfluoroalkyl or a group D-(C1-C6 alkyl) wherein D represents hydroxy, (C1-C6)alkoxy, (C1-C6)alkylthio, acylamino, optionally substituted phenyl or heteroaryl, NH2, or mono- or di-(C1-C6 alkyl)amino; R5 is hydrogen or a (C1-C6)alkyl group; or a salt, hydrate or solvate thereof. The compounds are inhibitors of matrix metalloproteinases, especially gelatinases.
摘要翻译：其中X是-CO 2 H，-N（OH）CHO或-CONHOH基团的通式（I）的化合物; R1是氢; （C1-C6）烷基; （C2-C6）链烯基; 苯基; 取代的苯基; 苯基（C1-C6）烷基; 取代的苯基（C 1 -C 6）烷基; 杂环; 取代的杂环基; 杂环基（C1-C6）烷基; 取代的杂环基（C 1 -C 6）烷基; 其中n为0,1或2，B为氢或（C1-C6）烷基，苯基，取代苯基，杂环基，（C1-C6）酰基，苯甲酰甲基或取代的苯甲酰甲基，A为（C1 1 -C 6）烷基; 氨基; 保护氨基; 酰氨基; 哦; SH; （C1-C6）烷氧基; （C1-C6）烷基氨基; 二 - （C1-C6）烷基氨基; （C1-C6）烷硫基; 芳基（C 1 -C 6）烷基; 氨基（C1-C6）烷基; 羟基（C 1 -C 6）烷基，巯基（C 1 -C 6）烷基或羧基（C 1 -C 6）烷基，其中任选保护氨基，羟基，巯基或羧基或羧基酰胺基; 被低级烷基取代的低级烷基，单（低级烷基）氨基甲酰基，二（低级烷基）氨基甲酰基，二（低级烷基）氨基或羧基 - 低级烷酰基氨基; R 2表示直链饱和或不饱和C 13 -C 24烃链，其链（i）可以被一个或多个不相邻的-O-或-S-或-C（= O） - ， - S（O）） - ，-S（= O）2 - 或-N（Rx） - 基团，其中Rx是氢，甲基或乙基，条件是链的最大长度不超过28℃，O，S和N原子，和/或（ii）可以被一个或多个选自C 1 -C 6烷基，OH，OMe，卤素，NH 2，NHCH 3，N（CH 3）2，CO 2 H，CO 2 CH 3，COCH 3，CHO，CONH 2，CONHCH 3，CON （CH 3）2，CH 2 OH，NHCOCH 3，条件是链的最大长度不超过28℃，O，S和N原子; R3是天然或非天然α氨基酸的特征侧链，其中任何官能团可被保护，条件是R3不表示氢; R4是氢，C1-C6烷基，（C1-C4）全氟烷基或其中D代表羟基，（C1-C6）烷氧基，（C1-C6）烷硫基，酰基氨基，任意取代的苯基或杂芳基，NH 2或单 - 或二 - （C 1 -C 6烷基）氨基; R5是氢或（C1-C6）烷基; 或其盐，水合物或溶剂合物。这些化合物是基质金属蛋白酶，特别是明胶酶的抑制剂。

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