发明名称 New heterocyclylmethyl-substituted anthranilamide derivatives and analogs as KDR/FLT tyrosine kinase inhibitors, used for treating e.g. psoriasis, restenosis, leukemia, arthritis, eye or kidney disease or arteriosclerosis
摘要 N-Substituted 2-(N-(N-containing heterocyclyl-methyl)-amino)-benzamide derivatives (I) (including aza analogs) are new. Anthranilamide derivatives and analogs of formula (I) and their isomers, enantiomers and salts are new; A, B', D = CH or N, at least one being N; E = aryl or heteroaryl (both optionally substituted (os) by one or more of halo, CN, alkyl, alkoxy, haloalkyl, OR5, SR4, SOR4 or SO2R4); or COOR8, CONR2R3, SR4, SOR4, SO2R4, SCN, P(O)(OR12)(OR13), -CH=CHCOR9 or -CC-R9; G, L, M, Q = C-X or N, provided that not more than one is N; X = H or halo; or alkyl, alkoxy or carboxyalkyl (all os by one or more halo); R1 = 1-12C alkyl or 2-12C alkenyl (both os by one or more of halo, OH, alkoxy, aralkoxy (no C-number specified), alkyl and/or NR2R3); 3-10C cycloalkyl or 3-10C cycloalkenyl (both os by one or more of halo, OH, alkoxy, alkyl and/or NR2R3); or aryl or heteroaryl (both os by one or more of halo, OH, CN, alkoxy, 2-6C alkenyl, aralkoxy, alkyl, haloalkyl, =O, SO2R4, OR5, R5 or P(O)(OR12)(OR13)); R2, R3 = H; or alkyl, 3-6C cycloalkyl, 3-6C cycloalkenyl, aryl or heteroaryl (all os by one or more of CN, halo, alkyl, Ph, hydroxyalkyl, haloalkyl, aryl, NR6R7, OR5, -alkyl-OR5, SR4, SOR4 or SO2R4); NR2R3 = 3-8C ring, optionally containing a further N, O, S or NR10 in the ring (os by one or more of CN, halo, alkyl, haloalkyl, aryl, OR5, SR4, SOR4 or SO2R4); R4 = OH, alkyl, aryl, heteroaryl or NR2R3; R5 = H, 1-12C alkyl (optionally interrupted by one or more O), haloalkyl, 3-6C cycloalkyl, 3-6C cycloalkyl, CH2CH2NR2R3, CH2CN or CH2CF3; R6, R7 = H or alkyl; or NR6R7 = 5-7 membered ring, optionally containing an additional O, S or NR10 heteroatom); R8 = H; or alkyl, alkoxy, benzyl, aryl or heteroaryl (all os by halo); R9 = H, alkyl, trialkylsilyl, aryl, heteroaryl or COR11; R10 = H, alkyl or aryl; R11 = H, alkyl or NR2R3; R12, R13 = H or alkyl; Alkyl moieties have 1-6C unless specified otherwise.
申请公布号 DE10125294(A1) 申请公布日期 2002.11.21
申请号 DE20011025294 申请日期 2001.05.15
申请人 SCHERING AG 发明人 HUTH, ANDREAS;KRUEGER, MARTIN;ERNST, ALEXANDER;THIERAUCH, KARL-HEINZ;HABEREY, MARTIN;MENRAD, ANDREAS
分类号 C07D213/81;C07D401/12;C07D401/14;C07D405/12;C07D409/14;(IPC1-7):C07D401/12;C07D417/14;C07F7/10;C07F9/58;C07F9/24;A61K31/505;A61K31/53 主分类号 C07D213/81
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