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    • 2. 发明授权
    • Peptidyl derivatives
    • 肽基衍生物
    • US5889058A
    • 1999-03-30
    • US335957
    • 1994-11-03
    • John Robert PorterThomas Andrew MillicanJohn Richard MorphyNigel Robert Arnold Beeley
    • John Robert PorterThomas Andrew MillicanJohn Richard MorphyNigel Robert Arnold Beeley
    • A61K31/19A61K31/195C07C229/04C07C229/24C07C229/28C07C233/05C07C233/08C07C237/06
    • A61K31/195
    • Methods of use for compounds of formula (I) are described wherein R represent a --CONHOH, carboxyl (--CO.sub.2 H) or esterified carboxyl group; R.sup.1 represents a hydrogen atom or an optionally substituted alkyl, alkenyl, aryl, aralkyl, heteroaralkyl or heteroarylthioalkyl group; R.sup.2 represents an optionally substituted phenylethyl, phenylpropyl or phenylbutyl group; R.sup.3 represents a hydrogen atom or an alkyl group; R.sup.4 represents a hydrogen atom or an alkyl group; R.sup.5 represents an optionally substituted alkyl or alkenyl group optionally interrupted by one or more --O-- or --S-- atoms or --N(R.sup.7)-- groups (where R.sup.7 is a hydrogen atom or a C.sub.1-6 alkyl group); X represents an amino (--NH.sub.2), or substituted amino, hydroxyl or substituted hydroxyl group; and the salts, solvates and hydrates thereof. The compounds are metalloproteinase inhibitors and in particular have a selective gelatinase action, and may be of use in the treatment of cancer to control the development of tumour metastases. ##STR1##
    • 其中R代表-CON​​HOH,羧基(-CO 2 H)或酯化的羧基;式(I)化合物的使用方法; R 1表示氢原子或任选取代的烷基,烯基,芳基,芳烷基,杂芳烷基或杂芳硫基烷基; R2表示任选取代的苯乙基,苯基丙基或苯基丁基; R3表示氢原子或烷基; R4表示氢原子或烷基; R5表示任选被一个或多个-O-或-S-原子或-N(R 7) - 基团(其中R 7是氢原子或C 1-6烷基)间隔的任选取代的烷基或烯基; X表示氨基(-NH 2)或取代的氨基,羟基或取代的羟基; 及其盐,溶剂化物和水合物。 化合物是金属蛋白酶抑制剂,特别是具有选择性明胶酶作用,并且可用于治疗癌症以控制肿瘤转移的发展。 (一)
    • 5. 发明授权
    • Conjugate compounds containing aza-macro-cycles and processes for their
preparation
    • 含有杂环 - 周期的共轭化合物及其制备方法
    • US5684135A
    • 1997-11-04
    • US451306
    • 1995-05-26
    • David ParkerNigel Robert Arnold BeeleyThomas Andrew Millican
    • David ParkerNigel Robert Arnold BeeleyThomas Andrew Millican
    • A61K49/06C07D257/02C07F9/6524C07K17/06
    • A61K49/06C07D257/02C07F9/6524
    • ##STR1## Conjugate compounds are described comprising a compound of formula (1), wherein A is a group --Alk
      3 -- or --Alk
      3 N(R
      4 )Alk
      1 --, Alk
      2 , Alk
      3 and Alk
      4 which may be the same or different is each a C
      1-4 alkylene chain optionally substituted by one or more C
      1-6 alkyl groups; and R
      1 , R
      2 , R
      3 and R
      4 , which may be the same or different, is each a hydrogen atom or a group--AlkR
      5 where Alk is an optionally substituted straight or branched C
      1-6 alkyl group and R
      5 is a hydrogen atom or a --CO
      2 H, --CONR
      6 R
      7 (where R
      6 and R
      7 , which may be the same or different is each a hydrogen atom or an alkyl group) or --P(X
      1 )(X
      2 R
      8 )L group where X
      1 and X
      2 is each an oxygen or sulphur atom. R
      8 is a hydrogen atom or an alkyl group and L is an aliphatic, aromatic, or heteroaromatic group or a linker group with the proviso that at least one of R
      1 , R
      2 , R
      3 and R
      4 is a group AlkP(X
      1 )(X
      2 R
      8 )L where L is a linker group; and a metal complexes and/or salts thereof, coupled to a protein, peptide or carbohydrate. The conjugates are useful for imaging and in the treatment of abnormal cell disorders, such as in the treatment of tumours.
    • (1)描述了包含式(1)化合物的共轭化合物,其中A是可以相同或不同的基团-Alk3-或-Alk3N(R4)Alk1,Alk2,Alk3和Alk4,各自可以相同或不同 任选被一个或多个C 1-6烷基取代的C 1-4亚烷基链; 并且可以相同或不同的R 1,R 2,R 3和R 4各自为氢原子或AlkR 5基团,其中Alk为任选取代的直链或支链C 1-6烷基,R 5为氢原子或 - CO 2 H,-CONR 6 R 7(其中R 6和R 7可以相同或不同,各自为氢原子或烷基)或-P(X1)(X2R8)L基团,其中X1和X2各自为氧或硫原子。 R8是氢原子或烷基,L是脂族,芳族或杂芳族基团或连接基团,条件是R1,R2,R3和R4中的至少一个是AlkP(X1)(X2R8)L 其中L是连接基团; 和与蛋白质,肽或碳水化合物偶联的金属络合物和/或其盐。 缀合物可用于成像和治疗异常细胞疾病,例如治疗肿瘤。