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    • 4. 发明申请
    • SYNTHESIS OF CARBOXYLIC AND HYDROXAMIC ACID DERIVATIVES
    • 羧酸和羟基酸衍生物的合成
    • WO1996026918A1
    • 1996-09-06
    • PCT/GB1996000467
    • 1996-03-01
    • BRITISH BIOTECH PHARMACEUTICALS LIMITEDFLOYD, Christopher, DavidWHITTAKER, Mark
    • BRITISH BIOTECH PHARMACEUTICALS LIMITED
    • C07C259/06
    • C07C259/06C07C231/00Y02P20/55
    • 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.
    • 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。
    • 5. 发明申请
    • METALLOPROTEINASE INHIBITORS
    • 金属蛋白酶抑制剂
    • WO1998023588A1
    • 1998-06-04
    • PCT/GB1997003258
    • 1997-11-27
    • BRITISH BIOTECH PHARMACEUTICALS LIMITEDFLOYD, Christopher, David
    • BRITISH BIOTECH PHARMACEUTICALS LIMITED
    • C07D209/48
    • C07K5/06078A61K38/00C07K5/0606
    • 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.
    • 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。