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1. 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。

2. 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。

3. 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。

4. 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。

5. 发明申请

WO1997006167A1 IMIDAZOPYRIDINE DERIVATIVES 审中-公开
标题翻译：咪唑吡啶衍生物
公开(公告)号：WO1997006167A1
公开(公告)日：1997-02-20
申请号：PCT/GB1996001849
申请日：1996-07-30
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , AYSCOUGH, Andrew, Paul , BLACKWELL, Christopher, Mark , LAUNCHBURY, Steven , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07D471/04
CPC分类号： C07D471/04 , C07D213/36
摘要： Compounds of formula (II), wherein L, A, X, B, R , R , W, D, E, R , R , R are as defined in the specification, are dual histamine H1 and PAF receptor antagonists.
摘要翻译：式（II）化合物，其中L，A，X，B，R 2，R 3，W，D，E，R 3，R 4，R 5如规格是双组胺H1和PAF受体拮抗剂。

6. 发明申请

WO1995035275A1 METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：金属蛋白酶抑制剂
公开(公告)号：WO1995035275A1
公开(公告)日：1995-12-28
申请号：PCT/GB1995001464
申请日：1995-06-22
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , MILLER, Andrew , WHITTAKER, Mark , BECKETT, Raymond, Paul
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C311/06
CPC分类号： C07D295/13 , C07C259/06 , C07C311/06 , C07C311/13 , C07C2601/14 , C07D285/06
摘要： Compounds of general formula (II) wherein X is a hydroxamic or carboxylic acid group, Y is carbonyl or sulphonyl and R1 and R2 are as defined in the claims, are matrix metalloproteinase inhibitors.
摘要翻译：通式（II）的化合物，其中X是异羟肟酸或羧酸基团，Y是羰基或磺酰基，R 1和R 2如权利要求中所定义，是基质金属蛋白酶抑制剂。

7. 发明申请

WO1995019957A1 HYDROXAMIC ACID DERIVATIVES AS METALLOPROTEINASE INHIBITORS 审中-公开
标题翻译：羟基酸衍生物作为金属蛋白酶抑制剂
公开(公告)号：WO1995019957A1
公开(公告)日：1995-07-27
申请号：PCT/GB1995000120
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： C07C259/06
CPC分类号： C07C259/06
摘要： The following compounds: 2S-Hydroxy-3R-[1S-(tert-butylcarbamoyl)-2,2-dimethyl-propylcarbamoyl]- 5-methyl-hexanohydroxamic acid, 2S-Hydroxy-3R-[1S-(N,N-dimethylcarbamoyl)-2,2-dimethyl-propyl-carbamoy l]-5-methyl-hexanohydroxamic acid, 2S-Hydroxy-3R-[1S-(3-hydroxy-2,2-dimethylpropylcarbamoyl)-2,2-dimethyl -propylcarbamoyl]-5-methyl-hexanohydroxamic acid, 2S-Hydroxy-3R-[1S-(methylcarbamoyl)-2,2-dimethyl-propylcarbamoyl]-6-ph enyl-hexanohydroxamic acid and 2S-Hydroxy-3R-[1S-(methylcarbamoyl)-2,2-dimethyl-butylcarbamoyl]-5-met hyl-hexanohydroxamic acid are matrix metalloproteinase inhibitors.
摘要翻译：以下化合物：2S-羟基-3R- [1S-（叔丁基氨基甲酰基）-2,2-二甲基 - 丙基氨基甲酰基] -5-甲基 - 己羟肟酸，2S-羟基-3R- [1S-（N，N-二甲基氨基甲酰基）-2,2-二甲基 - 丙基 - 氨基甲酰基l] -5-甲基 - 己羟肟酸，2S-羟基-3R- [1S-（3-羟基-2,2-二甲基丙基氨基甲酰基）-2,2-二甲基 - 丙基氨基甲酰基] -5-甲基 - 己酸异羟肟酸，2S-羟基-3R- [1S-（甲基氨基甲酰基）-2,2-二甲基 - 丙基氨基甲酰基] -6-苯基 - 己酸异羟肟酸和2S-羟基-3R- [1S-（甲基氨基甲酰基） -2,2-二甲基 - 丁基氨基甲酰基] -5-甲基己基异羟肟酸是基质金属蛋白酶抑制剂。

8. 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。

9. 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。

10. 发明申请

WO1996026918A1 SYNTHESIS OF CARBOXYLIC AND HYDROXAMIC ACID DERIVATIVES 审中-公开
标题翻译：羧酸和羟基酸衍生物的合成
公开(公告)号：WO1996026918A1
公开(公告)日：1996-09-06
申请号：PCT/GB1996000467
申请日：1996-03-01
申请人： BRITISH BIOTECH PHARMACEUTICALS LIMITED , FLOYD, Christopher, David , WHITTAKER, Mark
发明人： BRITISH BIOTECH PHARMACEUTICALS LIMITED
IPC分类号： C07C259/06
CPC分类号： C07C259/06 , C07C231/00 , Y02P20/55
摘要： A method for the preparation of carboxylic and hydroxamic acid derivatives by cocondensation in a liquid organic medium of three reaction components, namely a carboxylic acid reaction component of formula (II), an imine reaction component of formula (III), and an isonitrile reaction component of formula (IV), wherein X is hydrogen or an amino protecting group, or the residue of a solid phase reaction substrate; Y is (i) a group -CO2R5 wherein R5 is a carboxyl protecting group or the residue of a solid phase reaction substrate or (ii) a group -CONR6OR7 wherein R6 is an amino protecting group or the residue of a solid phase reaction substrate and R7 is a hydroxyl protecting group or the residue of a solid phase reaction substrate; [S1], [S2], [S3] and [S4] each represent covalently bound moieties which are substantially non reactive with the reaction components (II), (III), or (IV) defined above; provided that only one of X, R5, R6 and R7 is the residue of a solid phase reaction substrate.
摘要翻译：在三种反应组分的液体有机介质中，即式（II）的羧酸反应组分，式（III）的亚胺反应组分和异氰酸酯反应组分的缩合反应制备羧酸和异羟肟酸衍生物的方法式（Ⅳ）的化合物，其中X为氢或氨基保护基，或固相反应底物的残基; Y是（i）-CO 2 R 5基团，其中R 5是羧基保护基或固相反应底物的残基或（ii）基团-CONR 6OR 7，其中R 6是氨基保护基或固相反应底物的残基， R7是羟基保护基或固相反应底物的残基; [S1]，[S2]，[S3]和[S4]各自表示与上述定义的反应组分（II），（III）或（IV）基本上不反应的共价结合部分; 条件是X，R5，R6和R7中只有一个是固相反应底物的残基。

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