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    PROCEDE DE PREPARATION DE N-CARBOXYANHYDRIDE ENANTIOMERIQUEMENT ENRICHI
    3.
    发明公开
    PROCEDE DE PREPARATION DE N-CARBOXYANHYDRIDE ENANTIOMERIQUEMENT ENRICHI 有权
    工艺生产浓缩的对映体N-羧酸酐

    公开(公告)号：EP2152680A2

    公开(公告)日：2010-02-17

    申请号：EP08805594.2

    申请日：2008-05-22

    申请人： Sanofi-Aventis

    发明人： BIGOT, Antony ,  LAMPILAS, Maxime

    IPC分类号： C07D269/02 ,  C07D269/00 ,  C07C235/12

    CPC分类号： C07D263/44

    摘要： The invention relates to a method for preparing an enantiomerically enriched N-carboxyanhydride of an amino alpha acid of the formula (IIIa) or (IIIb) : F(I) from a compound of the formula (IIa) or respectively (IIb) : F(II), wherein: R1 and R2 each represent independently an alkyl group (e.g. methyl, ethyl, isopropyl), alkenyl group (e.g. allyl), cycloalkyl group, alkyl-cycloalkyl group (e.g. -CH2-cyclohexyle), alkyl-aryl group (e.g. benzyl), aryl group; R3 is an alkyl group (e.g. methyl, ethyl, tertio-butyl) or alkyl-aryl group (e.g. benzyl); the method comprises the following steps: (i) contacting the compound of the formula (IIa) with SOCI2 in a solvent; (ii) precipitating the N-carboxyanhydride formed during step (i) using a non-solvent; (iii) recovering the N-carboxyanhydride. The method does not include any re-crystallisation nor sublimation step of the N-carboxyanhydride, and the method can be used for example in the production of (L)-N-methyl-alanine N-carboxyanhydride.

    THIENO-IMINOSAURE-DERIVATE ALS INHIBITOREN VON MATRIX-METALLOPROTEINASEN
    5.
    发明公开
    THIENO-IMINOSAURE-DERIVATE ALS INHIBITOREN VON MATRIX-METALLOPROTEINASEN 审中-公开
    噻吩并 - IMINOSAURE衍生物作为基质金属蛋白酶抑制剂

    公开(公告)号：EP1723148A2

    公开(公告)日：2006-11-22

    申请号：EP05700992.0

    申请日：2005-01-18

    申请人： Sanofi-Aventis Deutschland GmbH

    发明人： SCHUDOK, Manfred ,  MATTER, Hans ,  HOFMEISTER, Armin ,  LAMPILAS, Maxime

    IPC分类号： C07D495/04 ,  A61K31/4365

    CPC分类号： C07D495/04

    摘要： The invention relates to the compounds of formula (I), which are suitable for producing drugs for the prophylaxis and therapy of diseases, whereby the course thereof involves the increased activity of matrix metalloproteinases. Diseases belonging thereto are degenerative joint diseases, for example, osteo-arthroses, spondyloses, chondroporosis after articulation injury or a long duration of articulation immobilization after meniscus or patella injury or torn ligaments, or a disease of the connective tissue, such as collagenoses, periodontal diseases, problems with healing wounds, or a chronic disease of the locomotor system, such as inflammatory, immunological or metabolic-related acute or chronic arthrites, arthropathies, myalgies or troubles of the bone metabolism, or ulceration, atherosclerosis or stenosis. The compounds of formula (I) are also suitable for treating inflammatory diseases or cancers, metastatic tumors, cachexia, anorexia, heart failure or septic shock and in the prophylaxis of myocardial and cerebral infarction.