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    VERFAHREN ZUR HERSTELLUNG VON 3-PYRROLIN-2-CARBONSÄURE-DERIVATEN
    1.
    发明授权
    VERFAHREN ZUR HERSTELLUNG VON 3-PYRROLIN-2-CARBONSÄURE-DERIVATEN 失效
    用于生产3-吡咯啉-2-羧酸衍生物

    公开(公告)号：EP0915844B1

    公开(公告)日：2006-04-26

    申请号：EP97933675.7

    申请日：1997-07-14

    申请人： Abbott GmbH & Co. KG

    发明人： MACK, Helmut ,  PFEIFFER, Thomas ,  SEITZ, Werner ,  ZIERKE, Thomas ,  BALKENHOHL, Friedhelm ,  LANGE, Udo

    IPC分类号： C07D207/22 ,  C12P17/10

    CPC分类号： C07D207/22

    摘要： A process is disclosed for preparing 3-pyrroline-2-carboxylic acid derivatives of formula (I), in which R1 stands for H, C¿1?-C6-alkyl, benzyl, benzyl substituted at the phenyl radical, allyloxycarbonyl, C1-C6-alkyloxycarbonyl, benzyloxycarbonyl, in which the benzyl radical can be substituted by OCH3 radicals, or for C1-C4-alkylcarbonyl; or R?1¿ stands for an amino acid radical which can be alkylated or acylated at the nitrogen and is linked by the C-terminal; and R2 stands for OH, C¿1?-C4-alkyloxy, benzyloxy or an N?3R4¿ group, in which R?3 and R4¿ represent independently from each other H, C¿1?-C4-alkyl, benzyl, phenyl or pyridyl, in which the aromatic compounds in R?3 and R4¿ can be substituted by up to three identical or different substituents selected from the group composed of methyl, methoxy, hydroxy, cyano or halogen. According to this process, the sulphonic acid radical is eliminated by means of a base from a compound having the formula (II), in which R?1 and R2¿ have the above meanings and R5 stands for C¿1?-C6-alkyl, benzyl, trifluoromethyl, naphthyl or phenyl optionally substituted by radicals from the group composed of methyl, nitro and halogen.

    NIEDERMOLEKULARE INHIBITOREN VON SERINPROTEASEN MIT POLYHYDROXYALKYL- UND POLYHYDROXYCYCLOAKYLRESTEN
    4.
    发明公开
    NIEDERMOLEKULARE INHIBITOREN VON SERINPROTEASEN MIT POLYHYDROXYALKYL- UND POLYHYDROXYCYCLOAKYLRESTEN 审中-公开
    丝氨酸蛋白酶的低分子抑制剂WITH AND多羟基POLYHYDROXYCYCLOAKYLRESTEN

    公开(公告)号：EP1370573A2

    公开(公告)日：2003-12-17

    申请号：EP01969785.3

    申请日：2001-09-27

    申请人： Abbott GmbH & Co. KG

    发明人： HERR, Dieter ,  MACK, Helmut ,  SEITZ, Werner ,  HORNBERGER, Wilfried

    IPC分类号： C07K9/00 ,  A61K38/04 ,  A61K47/48

    CPC分类号： A61K31/155 ,  C07H7/00 ,  C07H15/00

    摘要： The invention relates to novel amidines and quanidines, the production and use thereof and the use thereof as trypsine-type serine protease competitive inhibitors, especially thrombine and compliment proteases Cls and Clr. The invention also relates to pharmaceutical compositions which contain said compounds as active ingredients, in addition to the use of the compounds as thrombine inhibitors, anticoagulants, compliment inhibitors and anti-inflammatory agents. The novel compositions are characterised by the linkage of a serine protease inhibitor having amidine or quanidine functions with an alkyl radical having two or more hydroxyl functions, whereby said alkyl radical is derived from sugar derivates. Several sugar structural components or components derived from sugar can therefore be linked to each other. Said principle of linking sugar derivates enables oral active compounds to be obtained.