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21. 发明申请

WO1995019961A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1995019961A1
公开(公告)日：1995-07-27
申请号：PCT/GB1995000121
申请日：1995-01-23
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , BECKETT, Raymond, Paul , WHITTAKER, Mark , MILLER, Andrew
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C323/41
CPC分类号： C07D209/48 , C07C259/06 , C07C317/50 , C07C323/60 , C07C2601/14
摘要： Matrix metalloproteinase inhibiting compounds of formula (I), wherein X is a -CO2H or -CONHOH group; and one of the groups proximate to the amide bonds is a steric bulky group, showing enhanced oral absorption.
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; 并且接近酰胺键的一个基团是空间大体积基团，显示增强的口服吸收。

22. 发明申请

WO1998023588A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1998023588A1
公开(公告)日：1998-06-04
申请号：PCT/GB1997003258
申请日：1997-11-27
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , FLOYD, Christopher, David
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07D209/48
CPC分类号： C07K5/06078 , A61K38/00 , C07K5/0606
摘要： Compounds of formula (I) wherein R2 is a group -(Alk)m-(Q)n-(Alk )p-Ar wherein m, n and p are independently 0 or 1, Alk and Alk each independently represents a divalent (C1-C3)alkylene group, Q represents -O-, -S-, -SO-, or -SO2-, and Ar represents an optionally substituted phenyl or heteroaryl group; R1 is hydrogen or acyl; R21 is a group -(CH2)t-W wherein t represents 1, 2, 3 or 4 and W represents a 5- or 6-membered N-heterocyclic ring as defined in the specification; Z is either (a) a saturated 5- to 8-membered monocyclic or bridged N-heterocyclic ring as defined in the specification, or (b) a radical of formula (IB) wherein R3 is the side chain of a natural or non-natural alpha -amino acid in which any functional groups may be protected; R4 is one of a variety of groups defined in the specification; and R5 is hydrogen or a (C1-C6)alkyl group. The compounds are matrix metalloproteinase inhibitors.
摘要翻译：其中R2是基团 - （Alk）m-（Q）n-（Alk 1）p-Ar的式（I）化合物其中m，n和p各自独立地为0或1，Alk和Alk 1各自独立地为独立地表示二价（C1-C3）亚烷基，Q表示-O - ， - S-，-SO-或-SO2-，Ar表示任选取代的苯基或杂芳基; R1是氢或酰基; R 21是基团 - （CH 2）t-W，其中t表示1,2,3或4，W表示说明书中定义的5-或6-元N-杂环; Z是（a）如说明书中定义的饱和的5-至8-元单环或桥连的N-杂环，或（b）式（IB）的基团，其中R 3是天然或非 - 任何官能团可被保护的天然α-氨基酸; R4是规范中定义的各种组之一; 并且R 5是氢或（C 1 -C 6）烷基。这些化合物是基质金属蛋白酶抑制剂。

23. 发明申请

WO1998013495A1 HUMAN RANTES MUTANTS INCAPABLE OF AGGREGATE FORMATION 审中-公开
标题翻译：人类吞噬突变体不能形成聚集体
公开(公告)号：WO1998013495A1
公开(公告)日：1998-04-02
申请号：PCT/GB1997002605
申请日：1997-09-24
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , CZAPLEWSKI, Lloyd, George , HUNTER, Michael, George , EDWARDS, Richard, Mark , DAWSON, Keith, Martyn
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C12N15/19
CPC分类号： C07K14/523 , A61K38/00
摘要： This invention relates to mutants of human RANTES (hRANTES) which, relative to the wild-type molecule, have a reduced tendency to aggregate into large multimeric complexes at physiological ionic strength and pH, and are less pro-inflammatory.
摘要翻译：本发明涉及人RANTES（hRANTES）的突变体，其相对于野生型分子在生理离子强度和pH下具有降低的聚集成大多聚体复合物的趋势，并且较少促炎症。

24. 发明申请

WO1997018183A1 PREPARATION OF ALLYL SUCCINATE DERIVATIVES AND STARTING MATERIALS THEREFOR 审中-公开
标题翻译：制备ALLYL SUCCINATE衍生物及其起始材料
公开(公告)号：WO1997018183A1
公开(公告)日：1997-05-22
申请号：PCT/GB1996002531
申请日：1996-10-16
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , MARTIN, Fionna, Mitchell , LEWIS, Christopher, Norman , BOWLES, Stephen, Arthur , TODD, Richard, Simon
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C67/343
CPC分类号： C07C67/343 , Y02P20/55 , C07C69/593
摘要： A process for the preparation of a compound of formula (I) wherein R2 is a (C1-C6)alkyl, (C2-C6)alkenyl, (C2-C6)alkynyl, phenyl(C1-C6)alkyl, heteroaryl(C1-C6)alkyl, cycloalkyl(C1-C6)alkyl or cycloalkenyl(C1-C6)alkyl group, any one of which may be optionally substituted by one or more substituents selected from (C1-C6)alkyl, -O(C1-C6)alkyl, -S(C1-C6)alkyl, halo and cyano (-CN); and R7 is a carboxylic acid protecting group, which process comprises the internal molecular rearrangement of an allyl carboxylate compound of formula (II) wherein R2 and R7 are as defined in relation to formula (I) to form the desired compound of formula (I). Compounds (I) are intermediates for the preparation of Matrix metaloproteinase inhibitors.
摘要翻译：制备式（I）化合物的方法，其中R2是（C1-C6）烷基，（C2-C6）烯基，（C2-C6）炔基，苯基（C1-C6）烷基，杂芳基（C1- C 1 -C 6）烷基或环烯基（C 1 -C 6）烷基，其中任何一个可以任选地被一个或多个选自（C 1 -C 6）烷基，-O（C 1 -C 6）烷基，烷基，-S（C 1 -C 6）烷基，卤素和氰基（-CN）; 并且R 7是羧酸保护基，该方法包括式（II）的烯丙基羧酸酯化合物的内部分子重排，其中R 2和R 7如关于式（I）所定义，以形成所需的式（I）化合物，。化合物（I）是制备基质金属蛋白酶抑制剂的中间体。

25. 发明申请

WO1997006817A1 HAEMATOPOIETIC RECOVERY 审中-公开
公开(公告)号：WO1997006817A1
公开(公告)日：1997-02-27
申请号：PCT/GB1996002006
申请日：1996-08-19
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , LORD, Brian, Iles
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： A61K38/19
CPC分类号： A61K38/195 , A61K38/2053
摘要： Enhanced haematopoietic recovery following myelosuppressive therapy by continuous administration of a stem cell chemokine.
摘要翻译：通过连续施用干细胞趋化因子，骨髓抑制治疗后增强的造血恢复。

26. 发明申请

WO1994028917A1 PHARMACEUTICAL FORMULATIONS 审中-公开
标题翻译：药物制剂
公开(公告)号：WO1994028917A1
公开(公告)日：1994-12-22
申请号：PCT/GB1994001285
申请日：1994-06-15
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , CRAIG, Stewart , PATEL, Shilpa
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： A61K37/02
CPC分类号： C07K14/523 , A61K38/00
摘要： Metal ions such as Cu tend to promote multimerisation of stem cell inhibitors (SCIs) such as wild-type and variant macrophage inflammatory promoter-1 alpha (MIP-1 alpha ). High order multimers are unwanted in both in processing and in pharmaceutical formulations. Therefore, in pharmaceutically useful and other formulations of SCIs, monomer formation is promoted by removing metal ions, such as by the use of EDTA or another chelating agent.
摘要翻译：金属离子如Cu 2+倾向于促进干细胞抑制剂（SCI）的多聚化，例如野生型和变体巨噬细胞炎症启动子-1α（MIP-1α）。高级多聚体在加工和药物制剂中都是不需要的。因此，在药学上可用的和其它SCI制剂中，通过除去金属离子例如通过使用EDTA或另一种螯合剂来促进单体形成。

27. 发明申请

WO1997038314A1 DIAGNOSIS AND MONITORING OF NEUROLOGICAL DISEASE 审中-公开
标题翻译：诊断和监测神经病
公开(公告)号：WO1997038314A1
公开(公告)日：1997-10-16
申请号：PCT/GB1997000975
申请日：1997-04-08
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , MILLER, Karen, Margrete , GEARING, Andrew, John, Hubert , PIGOTT, Roderick
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： G01N33/573
CPC分类号： C12Q1/37 , G01N33/573 , G01N2333/96486
摘要： The invention provides a method for diagnosis or prediction of relapse or monitoring of disease activity in a patient with neurological disease, particularly multiple sclerosis, comprising quantifying the amount of MMP-9, fragments thereof or allelic variants thereof, and/or a tissue inhibitor of metalloproteinase (TIMP), fragments thereof or allelic variants thereof, present in the blood of a patient, and comparing that amount with a control.
摘要翻译：本发明提供了用于诊断或预测患有神经系统疾病，特别是多发性硬化症的患者的疾病活动的复发或监测的方法，包括定量MMP-9，其片段或其等位基因变体的量，和/或组织抑制剂存在于患者血液中的金属蛋白酶（TIMP），其片段或其等位基因变体，并将该量与对照组比较。

28. 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。

29. 发明申请

WO1996026223A1 SYNTHESIS OF HYDROXAMIC ACID DERIVATIVES 审中-公开
标题翻译：羟基酸衍生物的合成
公开(公告)号：WO1996026223A1
公开(公告)日：1996-08-29
申请号：PCT/GB1996000428
申请日：1996-02-26
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , FLOYD, Christopher, David , LEWIS, Christopher, Norman
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C08F08/30
CPC分类号： C07K1/04 , C07K1/003 , C08F8/30 , Y02P20/55
摘要： A solid phase reaction component comprising a solid substrate, substantially insoluble in aqueous or organic reaction media, carrying a plurality of covalently bound hydroxylamine or protected hydroxylamine groups of formula (A) or (B), wherein P1 is hydrogen or an amino protecting group and P2 is hydrogen or a hydroxyl protecting group, and the bond designated (a) is one which covalently links the group (A) or (B) to the residue of the solid substrate and is cleavable under acid conditions or by photolysis. Such components are useful in the solid phase synthesis of, for example, compounds which are matrix metalloproteinase inhibitors.
摘要翻译：固相反应组分，其包含基本上不溶于水或有机反应介质的固体底物，其携带多个共价键合的式（A）或（B）的羟胺或被保护的羟胺基，其中P1是氢或氨基保护基， P2是氢或羟基保护基，并且指定为（a）的键是将基团（A）或（B）共价连接到固体底物的残基上的键，并且在酸性条件下或通过光解可分解。这些组分可用于例如作为基质金属蛋白酶抑制剂的化合物的固相合成。

30. 发明申请

WO1994028916A1 RELEASE AND MOBILISATION OF HAEMATOPOIETIC CELLS 审中-公开
标题翻译：释放和移动HAEMATOPOIETIC细胞
公开(公告)号：WO1994028916A1
公开(公告)日：1994-12-22
申请号：PCT/GB1994001284
申请日：1994-06-15
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , COMER, Michael, Berisford , McCOURT, Matthew, John , WOOD, Lars, Michael , HUNTER, Michael, George , EDWARDS, Richard, Mark , GEARING, Andrew, John, Hubert
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： A61K37/02
CPC分类号： C07K14/523 , A61K38/00 , A61K38/193 , A61K39/39 , A61K2039/55522 , A61K2300/00
摘要： Stem cell inhibitors such as murine and human macrophage inflammatory protein-1 alpha (muMIP-1 alpha and huMIP-1 alpha /LD78) and their analogues and variants enhance the release and mobilisation of haematopoietic cells. This property makes them useful in enhancing responses against infection and in cell harvesting.
摘要翻译：干细胞抑制剂如鼠和人巨噬细胞炎症蛋白-1α（muMIP-1α和huMIP-1α/ LD78）及其类似物和变体增强造血细胞的释放和动员。这种性质使它们有助于增强针对感染和细胞收获的反应。

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