ANTIBODIES TO PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) AND USES THEREOF
    1.
    发明公开
    ANTIBODIES TO PLASMINOGEN ACTIVATOR INHIBITOR-1 (PAI-1) AND USES THEREOF 审中-公开
    ANTIKÖRPERGEGEN DEN PLASMINOGEN-AKTIVATOR-HEMMER 1(PAI-1)UND VERWENDUNGEN DAVON

    公开(公告)号:EP3033359A1

    公开(公告)日:2016-06-22

    申请号:EP14761451.5

    申请日:2014-08-13

    申请人: SANOFI

    IPC分类号: C07K16/38

    摘要: The invention provides antibodies that specifically bind to Plasminogen Activator inhibitor type-1 (PAI-1), The invention also provides pharmaceutical compositions, as well as nucleic acids encoding anti-PAI-1 antibodies, recombinant expression vectors and host cells for making such antibodies, or fragments thereof. Methods of using antibodies to modulate PAI-1 activity or detect PAI-1, either in vitro or in vivo, are also provided. The disclosure further provides methods of making antibodies that specifically bind to PAI-1 in the active conformational state.

    摘要翻译: 本发明提供了特异性结合纤溶酶原激活物抑制剂1型(PAI-1)的抗体。本发明还提供了药物组合物,以及编码抗PAI-1抗体的核酸,用于制备这种抗体的重组表达载体和宿主细胞 ,或其片段。 还提供了在体外或体内使用抗体调节PAI-1活性或检测PAI-1的方法。 本公开进一步提供了制备特异性结合活性构象状态的PAI-1的抗体的方法。

    DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE
    7.
    发明公开
    DÉRIVÉS DE 1-OXO-ISOINDOLINE-4-CARBOXAMIDES ET DE 1-OXO-1,2,3,4-TETRAHYDROISOQUINOLEINE-5-CARBOXAMIDES, LEUR PRÉPARATION ET LEUR APPLICATION EN THÉRAPEUTIQUE 审中-公开
    1-氧代异二氢吲哚-4-甲酰胺和1-氧代-1,2,3,4-四氢异喹啉-5-甲酰胺衍生物及其制备和治疗用途

    公开(公告)号:EP2185511A2

    公开(公告)日:2010-05-19

    申请号:EP08835551.6

    申请日:2008-07-25

    申请人: Sanofi-Aventis

    摘要: The invention relates to 1-oxo-isoindoline-4-carboxamide and 1-oxo-1,2,3,4-tetrahydroisoquinoline-5-carboxamide derivatives of general formula (I) where: R1 = H, C
    1 -C
    10 alkyl, C
    3 -C
    7 cycloalkyl, (CH
    2 )
    n -(C
    1 -C
    6 )alkenyl, (CH
    2 )n-(C
    1 -C
    6 )alkynyl, (C
    1 -C
    6 )alkyl-Z-(C
    1 -C
    6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
    m , or R1 = COOR, S(O)
    m R, aryl or aralkyl, R2 = one or more of H, halogen, C
    1 -C
    6 alkyl, C
    3 -C
    7 cycloalkyl, C
    1 -C
    6 alkenyl, C
    1 -C
    6 alkynyl, C
    1 -C
    6 alkyl-Z-(C
    1 -C
    6 )alkyl, where Z = a heteroatom chosen from O, N and S(O)
    m , or R2 = halo(C
    1 -C
    6 )alkyl, C
    1 -C
    6 alkoxy, halo(C
    1 -C
    6 )alkoxy, hydroxy, nitro, cyano, amino, NR7R8, COOR, CONR7R8, O- CO(C
    1 -C
    6 )alkyl, S(O)
    m -NR7R8, aryl; R3 = trifluoromethyl;R4 and R5 independently = H, or R4 and R5 together with the carbon to which they are attached form a saturated ring with 3 to 6 C and optionally containing O to 1 heteroatoms chosen from O, N or S; R6 = H,halogen, C
    1 - C
    6 alkyl, C
    3 -C
    7 cycloalkyl, C
    3 -C
    7 cycloalkyl-(C
    1 -C
    6 )alkyl, halo(C
    1 -C
    6 )alkyl, nitro, amino, NR7R8, COOR, NR7(SO2)R8, CONR7R8, aryl or heterocycle; X = C
    1 -C
    2 alkylene; m = a whole number from O to 2 and n = a whole number from1 to 6. The invention further relates to a method for preparation and therapeutic application thereof as ß-secretase inhibitors for the treatment of neurodegenerative disorders such as Alzheimers.