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    ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS
    5.
    发明申请
    ALKYLQUINOLINE AND ALKYLQUINAZOLINE KINASE MODULATORS 有权
    烷基胆碱和碱性氨基酸激酶调节剂

    公开(公告)号：US20060281772A1

    公开(公告)日：2006-12-14

    申请号：US11422349

    申请日：2006-06-06

    申请人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

    发明人： Nand Baindur ,  Michael Gaul ,  Kevin Kreutter ,  Christian Baumann ,  Alexander Kim ,  Guozhang Xu ,  Robert Tuman ,  Dana Johnson

    IPC分类号： A61K31/517 ,  A61K31/4709 ,  C07D403/04 ,  C07D401/04

    CPC分类号： C07D401/04 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14

    摘要： The invention is directed to alkylquinoline and alkylquinazoline compounds of Formula I: wherein R1, R2, R3, B, Z, G, Q and X are as defined herein, the use of such compounds as protein tyrosine kinase modulators, particularly inhibitors of FLT3 and/or c-kit and/or TrkB, the use of such compounds to reduce or inhibit kinase activity of FLT3 and/or c-kit and/or TrkB in a cell or a subject, and the use of such compounds for preventing or treating in a subject a cell proliferative disorder and/or disorders related to FLT3 and/or c-kit and/or TrkB. The present invention is further directed to pharmaceutical compositions comprising the compounds of the present invention and to methods for treating conditions such as cancers and other cell proliferative disorders.

    摘要翻译： 本发明涉及式I的烷基喹啉和烷基喹唑啉化合物：其中R 1，R 2，R 3，B，Z，G， Q和X如本文所定义，使用这些化合物如蛋白酪氨酸激酶调节剂，特别是FLT3和/或c-kit和/或TrkB的抑制剂，使用这些化合物来降低或抑制FLT3和/或 c-kit和/或TrkB，以及这些化合物在受试者中用于预防或治疗细胞增殖性疾病和/或与FLT3和/或c-kit和/或TrkB相关的疾病的用途。 本发明进一步涉及包含本发明化合物的药物组合物和治疗诸如癌症和其它细胞增殖性疾病的病症的方法。

    Angiogenesis inhibiting pyridazinamines
    6.
    发明授权
    Angiogenesis inhibiting pyridazinamines 失效
    血管发生抑制哒嗪胺

    公开(公告)号：US5985878A

    公开(公告)日：1999-11-16

    申请号：US119075

    申请日：1998-07-09

    申请人： Raymond Antoine Stokbroekx ,  Marcel Jozef Maria Van der Aa ,  Marc Willems ,  Lieven Meerpoel ,  Marcel Gerebernus Maria Luyckx ,  Robert Tuman

    发明人： Raymond Antoine Stokbroekx ,  Marcel Jozef Maria Van der Aa ,  Marc Willems ,  Lieven Meerpoel ,  Marcel Gerebernus Maria Luyckx ,  Robert Tuman

    IPC分类号： A61K31/00 ,  A61K31/50 ,  A61K31/501 ,  A61K31/505 ,  A61K31/517 ,  A61K31/529 ,  A61K31/55 ,  A61K31/551 ,  A61P9/00 ,  C07D417/04 ,  C07D417/14 ,  C07D451/02 ,  C07D471/08

    CPC分类号： C07D417/04 ,  C07D417/14

    摘要： This invention concerns compounds of formula the N-oxide forms, the pharmaceutically acceptable acid addition salts and stereochemically isomeric forms thereof, wherein X is CH or N; m is 2 or 3 and n is 1, 2 or 3; wherein 1 or 2 C-atoms of the CH.sub.2 groups of the ##STR1## moiety which may also contain one double bond, may be substituted with C.sub.1-6 alkyl, amino, aminocarbonyl, mono- or di(C.sub.1-6 alkyl)amino, C.sub.1-6 alkyloxycarbony, C.sub.1-6 alkylcarbonylamino, hydroxy or C.sub.1-6 alkyloxy; and/or 2 C-atoms of said CH.sub.2 groups may be bridged with C.sub.2-4 alkanediyl; R.sup.1 is hydrogen, C.sub.1-6 alkyl, C.sub.1-6 alkyloxy, C.sub.1-6 alkylthio, amino, mono- or di(C.sub.1-6 alkyl)amino, Ar, ArNH--, C.sub.3-6 cycloalkyl, hydroxymethyl or benzyloxymethyl; R.sup.2 and R.sup.3 are hydrogen, or taken together may form a bivalent radical of formula --CH.dbd.CH--CH.dbd.CH--; in case X represents CH then L is a radical L.sup.1, L.sup.2 or L.sup.3 ; or in case X represents N then L is a radical L.sup.2 or L.sup.3 ; L.sup.1 is Ar-C.sub.1-6 alkyloxy, Ar-oxy, Ar-thio, Ar-carbonylamino, di-Ar-methyloxy-, N-Ar-piperazinyl, N-Ar-homopiperazinyl, 2-benzimidazolinonyl, Ar--NR.sup.4 --, Ar-Alk-NR.sup.4 --, Ar--NR.sup.4 -Alk-NR.sup.5 -- or Het-NR.sup.4 --; L.sup.2 is Ar, Ar-carbonyl, Ar--CH.dbd.CH--CH.sub.2 --, naphtalenyl or Het; L.sup.3 is C.sub.1-6 alkyl substituted with one or two radicals selected from Ar, Ar-oxy, or Ar-thio, further optionally substituted with cyano or hydroxy; 2,2-dimethyl-1,2,3,4-tetrahydro-naphtalenyl; 2,2-dimethyl-1H-2,3-dihydroindenyl;Ar-piperidinyl or Ar--NR.sup.4 -Alk-; R.sup.4 and R.sup.5 are each independently selected from hydrogen or C.sub.1-6 alkyl; Alk is C.sub.1-6 alkanediyl; their preparation, compositions containing them and their use as a medicine.

    摘要翻译： 本发明涉及N-氧化物形式的化合物，其药学上可接受的酸加成盐和立体化学异构形式，其中X是CH或N; m为2或3，n为1,2或3; 氨基，氨基羰基，一或二（C 1-6烷基）氨基，C 1-6烷氧基羰基，C 1 -C 6烷氧基羰基，C 1-6烷氧基羰基，C 1-6烷氧基羰基 -6-烷基羰基氨基，羟基或C 1-6烷氧基; 和/或所述CH 2基团的2个C原子可以与C 2-4烷二基桥接; R1是氢，C1-6烷基，C1-6烷氧基，C1-6烷硫基，氨基，一或二（C1-6烷基）氨基，Ar，ArNH-，C3-6环烷基，羟甲基或苄氧基甲基; R2和R3是氢，或者可以一起形成式-CH = CH-CH = CH-的二价基团; 在X表示CH的情况下，L是基团L 1，L 2或L 3; 或者在X表示N的情况下，则L是基团L2或L3; L 1是Ar-C 1-6烷氧基，Ar-氧基，Ar-硫代，Ar-羰基氨基，二-Ar-甲氧基 - ，N-Ar-哌嗪基，N-Ar-高哌嗪基，2-苯并咪唑啉酮基，Ar-NR4-， Alk-NR4-，Ar-NR4-Alk-NR5-或Het-NR4-; L2是Ar，Ar-羰基，Ar-CH = CH-CH 2 - ，萘基或Het; L3是被一个或两个选自Ar，Ar-氧基或Ar-硫基的基团取代的C 1-6烷基，进一步任选被氰基或羟基取代; 2,2-二甲基-1,2,3,4-四氢 - 萘基; 2,2-二甲基-1H-2,3-二氢茚基; Ar-哌啶基或Ar-NR4-Alk-; R 4和R 5各自独立地选自氢或C 1-6烷基; Alk是C1-6烷二基; 其制剂，含有它们的组合物及其作为药物的用途。