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    Alpha-substituted pyridazino quinoline compounds
    4.
    发明授权
    Alpha-substituted pyridazino quinoline compounds 失效
    α-取代哒嗪喹啉化合物

    公开(公告)号：US5837705A

    公开(公告)日：1998-11-17

    申请号：US617728

    申请日：1996-04-01

    申请人： Thomas Michael Bare ,  James Roy Empfield ,  Janet Marie Forst ,  Keith John Herzog ,  Richard Bruce Sparks

    发明人： Thomas Michael Bare ,  James Roy Empfield ,  Janet Marie Forst ,  Keith John Herzog ,  Richard Bruce Sparks

    IPC分类号： C07D491/147 ,  A61K31/50 ,  A61P25/00 ,  A61P25/04 ,  A61P25/28 ,  A61P25/30 ,  C07D471/04 ,  C07D471/14 ,  C07D495/14 ,  C07D491/14

    CPC分类号： C07D471/04

    摘要： The invention relates to alpha-substituted pyridazino-quinoline compounds of the formula I: ##STR1## wherein Ring A is chosen from an ortho fused aromatic or heteroaromatic five- or six-membered ring; R.sup.1 is selected from a variety of substituents including halogen, (1-4C)alkyl and nitro; R.sup.2 is selected from a group of the formula R2', R2" or R2"' wherein R2' is --CHR.sup.3 (CH.sub.2).sub.n C(O)NR.sup.5 R.sup.6 ; R2" is --CHR.sup.3 (CH.sub.2).sub.n R.sup.4 and R2"' is --CHR.sup.3 (CH.sub.2).sub.n L wherein n is 0-6; R.sup.5 is aryl or substituted aryl; R.sup.6 is (1-6C)alkyl or hydrogen; R.sup.3 is (1-6C)alkyl, (0-6C)alkylCF.sub.3 or (0-6C)alkylCOOR'; R.sup.4 is (1-6C)alkyl, (2-6C)alkyl containing a double or triple bond, or (0-6C)alkylaryl; L is a variety of substituents including phenyl, heteroaryl and CO.sub.2 R'; R' is hydrogen or (1-4C)alkyl; Z is selected from oxo, --OH, H,H--, H, (1-6C)alkyl or (1-6C)alkylaryl; and R.sup.7 is hydrogen or --(CO)R.sup.8 wherein R.sup.8 is a variety of substituents including hydrogen and (1-12C) alkyl.

    摘要翻译： 本发明涉及式I的α-取代的哒嗪 - 喹啉化合物：其中环A选自邻近稠合芳族或杂芳族五元或六元环; R1选自多种取代基，包括卤素，（1-4C）烷基和硝基; R2选自式R2'，R2“或R2”'的基团，其中R2'为-CHR3（CH2）nC（O）NR5R6; R2“是-CHR3（CH2）nR4，R2”'是-CHR3（CH2）nL，其中n是0-6; R5是芳基或取代的芳基; R6是（1-6C）烷基或氢; R3是（1-6C）烷基，（0-6C）烷基CF3或（0-6C）烷基COOR'; R4是（1-6C）烷基，含有双键或三键的（2-6C）烷基，或（0-6C）烷基芳基; L是各种取代基，包括苯基，杂芳基和CO 2 R'; R'是氢或（1-4C）烷基; Z选自氧代，-OH，H，H，H，（1-6C）烷基或（1-6C）烷基芳基; 并且R 7是氢或 - （CO）R 8，其中R 8是各种取代基，包括氢和（1-12C）烷基。

    Pyridazino quinoline compounds
    6.
    发明授权
    Pyridazino quinoline compounds 失效
    哒嗪喹啉化合物

    公开(公告)号：US06232313B1

    公开(公告)日：2001-05-15

    申请号：US09044109

    申请日：1998-03-19

    申请人： Thomas Michael Bare ,  Timothy Wayne Davenport ,  James Roy Empfield ,  Jeffrey Alan McKinney ,  Richard Bruce Sparks

    发明人： Thomas Michael Bare ,  Timothy Wayne Davenport ,  James Roy Empfield ,  Jeffrey Alan McKinney ,  Richard Bruce Sparks

    IPC分类号： A61K315025

    CPC分类号： C07D471/04 ,  C07D215/56

    摘要： The present invention relates to compounds, pharmaceutical compositions and methods of using compounds having the formula below in the treatment and prevention of certain diseases or conditions. Where the ring designated A is chosen from ortho substituted aryl or heteroaryl species, R1 and R2 are chosen independently from —(CH2)nL where L is selected from a variety of substituents including hydrogen, and aryl, heteroaryl or heterocyclic groups and R4 is chosen from a variety of substituents including halogen and alkyl groups. The compounds are useful in treating and preventing neurological disorders associated with excitatory amino acids.

    摘要翻译： 本发明涉及在治疗和预防某些疾病或病症时使用具有下式的化合物的化合物，药物组合物和方法。 当指定为A的环选自邻位取代的芳基或杂芳基时，R 1和R 2独立地选自 - （CH 2）n L，其中L选自多种取代基，包括氢和芳基，杂芳基或杂环基，并且选择R4 来自各种取代基，包括卤素和烷基。 该化合物可用于治疗和预防与兴奋性氨基酸相关的神经障碍。