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    PYRROLO[2,3-D]PYRIMIDINES AND THEIR APPLICATION AS TYROSINE KINASE INHIBITORS
    4.
    发明专利
    PYRROLO[2,3-D]PYRIMIDINES AND THEIR APPLICATION AS TYROSINE KINASE INHIBITORS 未知

    公开(公告)号：BG103785A

    公开(公告)日：2000-06-30

    申请号：BG10378599

    申请日：1999-10-07

    Applicant: BASF AG

    Inventor： CALDERWOOD DAVID J ,  JOHNSTON DAVID N ,  RAFFERTY PAUL ,  TWIGGER HELEN L ,  MUNSCHAUER RAINER ,  ARNOLD LEE

    IPC: A61K31/519 ,  A61P35/00 ,  A61P37/02 ,  A61P43/00 ,  C07D487/04 ,  A61K31/505

    Abstract: The compounds are useful for the treatment of proliferative diseases and diseases of the immune system in mammals, including their pharmaceutically acceptable salts. The compounds have the formula where R1 means hydrogen, 2-phenyl-1,3-dioxan-5-yl, C1-6-alkyl group, C3-8-cycloalkyl group, C5-7-cycloalkenyl group or (optionally substituted phenyl) C1-6-alkyl where the alkyl, cycloalkyl and cycloalkenyl group are optionally substituted by one or more groups with the formula ORA where RA means hydrogen or C1-6-alkyl group provided that the group with formula ORA is not positioned at the carbon atom adjuncted to the nitrogen; R2 means hydrogen, C1-6-alkyl group, C3-8-cycloalkyl group, halogen, hydroxy (optionally substituted phenyl)-C1-6-alkyl, optionally substituted phenyl or R4; and R3 means a group with formula (a) where the phenyl ring is optionally additionally substituted and A means NH, O, NHSO2, SO2NH, C1-4-alkylen residue, NHCO, NHCO2, CONH, NHCONH, CO2 or S(O)p where p has the value of 0,1 or 2, or A is absent and R5 is adjuncted directly to the phenyl ring; and R5 optionally means substituted phenyl, and in addition when A is absent, then R5 means phthalimidogroup optionally substituted with halogen, or pyrazolylaminogroup where the pyrazol ring is optionally substituted with one or more of the following groups: hydroxy or optionally substituted phenyl; R4 is heterocyclic group. The invention also relates to methods for the preparation of these compounds and pharmaceutical compositions containing them. 30 claims

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