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    Prodrugs of thrombin inhibitors
    4.
    发明授权
    Prodrugs of thrombin inhibitors 有权
    凝血酶抑制剂的前药

    公开(公告)号：US07144902B1

    公开(公告)日：2006-12-05

    申请号：US09958349

    申请日：2000-04-05

    申请人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    发明人： Dorit Baucke ,  Helmut Mack ,  Werner Seitz ,  Wilfried Hornberger ,  Gisela Backfisch ,  Juergen Delzer

    IPC分类号： A61K31/425 ,  C07D277/20

    CPC分类号： C07K5/06078 ,  A61K38/00 ,  C07B43/00 ,  C07K5/0222

    摘要： The present invention relates to prodrugs of pharmacologically active five-membered heterocyclic amidines from which are produced in vivo compounds which are competitive inhibitors of trypsin-like serine proteases, in particular thrombin and kininogenases such as kallikrein, to the preparation thereof and to the use thereof as medicines. The invention also relates to pharmaceutical compositions which comprise the prodrugs of the active compounds as ingredients, and to the use of the compounds as thrombin inhibitors, anticoagulants and as antiinflammatory agents.

    摘要翻译： 本发明涉及药理活性五元杂环脒的前体药物，它们是体内化合物，其是胰蛋白酶样丝氨酸蛋白酶的竞争性抑制剂，特别是凝血酶和激肽释放酶如激肽释放酶对其制备及其用途 作为药物 本发明还涉及包含活性化合物作为成分的前药以及该化合物作为凝血酶抑制剂，抗凝剂和抗炎剂的用途的药物组合物。

    alpha/beta-adrenoceptors blockers and angiotensin converting enzyme inhibitors derived from hydroxyphenyl carboxylic acid and alcohol
    10.
    发明申请
    alpha/beta-adrenoceptors blockers and angiotensin converting enzyme inhibitors derived from hydroxyphenyl carboxylic acid and alcohol 审中-公开
    α/β受体拮抗剂和衍生自羟基苯基羧酸和酒精的血管紧张素转换酶抑制剂

    公开(公告)号：US20030040485A1

    公开(公告)日：2003-02-27

    申请号：US10136494

    申请日：2002-05-02

    发明人： Ing-Jun Chen

    IPC分类号： A61K038/05 ,  A61K031/137 ,  C07K005/062

    CPC分类号： C07K5/0222 ,  A61K38/556 ,  C07C217/20

    摘要： The invention disclosed some derivative chemically with Hydroxyphenyl carboxylic acid and Alcohol based phenoxypropanolamine and associated alanyl-proline peptide derivatives. The compounds shown as formula I, 1 whether R is a number selected from the group of hydrogen, unsaturated 2-6 straight chain carbon atoms, saturated 1-6 straight chain carbon atoms, unsaturated 2-6 straight chain of alkoxyl group, saturated 1-6 straight chain of alkoxyl group, halogen, and nullNO2; R1 is selected from the groups of nullR2OH, nullR2OR3, nullR2COCOOR4, nullR2COOR4 and R2CH(COR4)-alanylproline, R2CH(COOR4)-alanylproline; R2 is selected from the groups of unsaturated 2-6 straight chain carbon atoms, saturated 1-6 straight chain carbon atoms; R3 is selected from the ester groups consisting of proline and alanylproline; R4 is selected from the groups of hydrogen, unsaturated 2-6 straight chain carbon atoms, saturated 1-6 straight chain carbon atoms; R5 is selected from the groups of hydrogen, unsaturated 2-6 straight chain carbon atoms, saturated 1-6 straight chain carbon atoms, and 2 R may be on the meta, ortho, or para position with ethoxyl group on the bezene ring. Through in vivo experiment to prove those compounds have new generation null/null-adrenoceptor antagonist with vasorelaxant activity or angiotensin converting enzyme inhibitory activities.

    摘要翻译： 本发明公开了一些用羟基苯基羧酸和基于醇的苯氧基丙醇胺和相关的丙氨酰 - 脯氨酸肽衍生物化学衍生物。 式I化合物，无论R是选自氢，不饱和2-6直链碳原子，饱和1-6直链碳原子，不饱和2-6直链烷氧基，饱和1- 6直链烷氧基，卤素和-NO 2; R1选自-R2OH，-R2OR3，-R2COCOOR4，-R2COOR4和R2CH（COR4） - 丙氨酰脯氨酸，R2CH（COOR4） - 丙氨酰脯氨酸; R2选自不饱和2-6直链碳原子，饱和1-6直链碳原子; R3选自脯氨酸和丙氨酰脯氨酸组成的酯基; R4选自氢，不饱和2-6直链碳原子，饱和1-6直链碳原子; R5选自氢，不饱和2-6直链碳原子，饱和1-6直链碳原子，R可以在甲苯环上具有乙氧基的间位，邻位或对位。 通过体内实验证明这些化合物具有新一代α/β受体拮抗剂与血管舒张活性或血管紧张素转换酶抑制活性。