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    CYCLOALKYLSUBSTITUIERTE BENZIMIDAZOLE UND IHRE VERWENDUNG ALS PARP INHIBITOREN
    3.
    发明公开
    CYCLOALKYLSUBSTITUIERTE BENZIMIDAZOLE UND IHRE VERWENDUNG ALS PARP INHIBITOREN 有权
    环苯并咪唑类和它们作为PARP抑制剂

    公开(公告)号：EP1171424A1

    公开(公告)日：2002-01-16

    申请号：EP00918867.3

    申请日：2000-04-11

    申请人： BASF AKTIENGESELLSCHAFT

    发明人： LUBISCH, Wilfried ,  KOCK, Michael ,  HÖGER, Thomas ,  GRANDEL, Roland ,  SCHULT, Sabine ,  MÜLLER, Reinhold

    IPC分类号： C07D235/06 ,  C07D403/08 ,  C07D401/08 ,  A61K31/4184 ,  A61P25/00

    CPC分类号： C07D235/14

    摘要： The invention relates to a compound of formula (I) or (II), wherein A represents a saturated or mono-unsaturated carbocycle containing 3 to 8 carbon atoms which can also have a condensed benzol ring, whereby the rings can also be substituted with one or two different or identical radicals; R1 represents hydrogen, chlorine, fluorine, bromine, iodine, branched and unbranched C¿1?-C6-alkyl, OH, nitro, CF3, CN, NR?11R12¿, NH-CO-R13, O-C1-C4 alkyl; and R2 represents hydrogen, branched and unbranched C¿1?-C6 alkyl, C1-C4 alkyl-phenyl. The invention also relates to the tautomeric forms, possible enantiomeric and diastereomeric forms, possible cis-trans isomers on the rings in A and their prodrugs. The substituted benzimidazoles of general formulas (I) and (II) are inhibitors of poly(ADP-ribose) polymerase (PARP), or poly(ADP-ribose) synthase (PARS), as it is also known and can be used for the treatment or prophylaxis of diseases which are associated with the increased enzyme activity of this enzyme.

    HETEROZYKLISCHE VERBINDUNGEN UND DEREN ANWENDUNG ALS PARP-INHIBITOREN
    6.
    发明公开
    HETEROZYKLISCHE VERBINDUNGEN UND DEREN ANWENDUNG ALS PARP-INHIBITOREN 有权
    杂环化合物和它们作为PARP抑制剂

    公开(公告)号：EP1257551A1

    公开(公告)日：2002-11-20

    申请号：EP01911528.6

    申请日：2001-01-25

    申请人： BASF AKTIENGESELLSCHAFT

    发明人： LUBISCH, Wilfried ,  KOCK, Michael ,  HÖGER, Thomas ,  GRANDEL, Roland ,  MÜLLER, Reinhold ,  SCHULT, Sabine

    IPC分类号： C07D471/04 ,  A61K31/437 ,  A61P25/00

    CPC分类号： C07D471/04

    摘要： The invention relates to compounds of formula (I), wherein; either A1 or A2 represents CONH¿2?, and the other radical A?2 or A1¿ represents hydrogen, chlorine, fluorine, bromine, iodine C¿1?-C6 alkyl, OH, nitro, CF3, CN, NR?11R12¿, NH-CO-R13, O-C1-C4 alkyl; X1 can represent N and C-R2; X2, independent of X1, can represent N and C-R2; R2 can represent hydrogen, C¿1?-C6 alkyl, C1-C4 alkyl-phenyl, phenyl; B can represent an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 15 carbon atoms, an unsaturated, saturated or partially unsaturated monocyclic, bicyclic or tricyclic ring having a maximum of 14 carbon atoms and 0 to 5 nitrogen atoms, 0 to 2 oxygen atoms or 0 to 2 sulfur atoms, which can each still be substituted with an R?4¿ and a maximum of 3 of the same or different radicals R5, and; R?1, R4, R5, R11-R13¿ have the meanings as cited in Claim No. 1. The invention also relates to the tautomeric forms, and possible enantiomeric and diastereomeric forms of said compounds, to the prodrugs thereof and to their use as PARP inhibitors.