首页> 外国专利> SUBSTITUTED 3-ARYLIDENE-7-AZAOXINDOLE COMPOUNDS AND PROCESS FOR THEIR PREPARATION.

SUBSTITUTED 3-ARYLIDENE-7-AZAOXINDOLE COMPOUNDS AND PROCESS FOR THEIR PREPARATION.

机译:取代的3-芳基烯烃-7-氮杂吲哚化合物及其制备方法。

摘要

The present invention relates to compound of formula (I) wherein A is benzene, naphthalene, 5,6,7,8,-tetrahydronaphthalene, quinoline, isoquinoline, indole or 7-azaindole; R1 is -H, -CN, -SO3R4, -SO2NHR5, (i), -COOR6, -CONHCH2(CHOH)nCH2OH, (ii), -NR7R8, -N(CH2CH2OH)2, -NHCH2(CHOH)nCH2OH, -NHCONH2, -NH-C(NH2)=NH, -NHCO(CH)OH)nCH2OH, (iii), -NHSO2R9, -OR10, -OCH2(CHOH)nCH2OH, -OOC(CHOH)nCH2OH, -OPO(OH)2, -CH2NH2, -C(NH2)=NH, -CH2NHC(NH2)=NH, (iv), -CH2OH, -CH2OOC(CHOH)nCH2OH, -CH2OPO(OH)2 or -PO(OH)2; R2 is C1-C6 alkyl, halogen, or hydroxy; R3 is -H or C1-C6 alkyl; R4 is -H, C1-C6 alkyl or -CH2(CHOH)nCH2OH; R5 is -H, C1-C6 alkyl, -CH2(CHOH)nCH2OH or -(CH2)mNMe2; R6 is -H, C1-C6 alkyl or -CH2(CHOH)nCH2OH; each of R7 and R8 independently is -H or C1-C6 alkyl; R9 is methyl or tolyl; R10 is -H, C1-C6 alkyl or C2-C6 alkanoyl; Z is CH2, 0, NH or NCH2CH2OH; n is zero or 1; m is 2 or 3; p is 1, 2 or 3; q is zero, 1 or 2; and the pharmaceutically acceptable salt thereof, for use as tyrosine kinase inhibitors.
机译:本发明涉及式(I)化合物,其中A是苯,萘,5,6,7,8,-四氢萘,喹啉,异喹啉,吲哚或7-氮杂吲哚; R 1是-H,-CN,-SO3R4,-SO2NHR5,(i),-COOR6,-CONHCH2(CHOH)nCH2OH,(ii),-NR7R8,-N(CH2CH2OH)2,-NHCH2(CHOH)nCH2OH,- NHCONH2,-NH-C(NH2)= NH,-NHCO(CH)OH)nCH2OH,(iii),-NHSO2R9,-OR10,-OCH2(CHOH)nCH2OH,-OOC(CHOH)nCH2OH,-OPO(OH) 2,-CH2NH2,-C(NH2)= NH,-CH2NHC(NH2)= NH,(iv),-CH2OH,-CH2OOC(CHOH)nCH2OH,-CH2OPO(OH)2或-PO(OH)2; R2是C1-C6烷基,卤素或羟基; R3是-H或C1-C6烷基; R4为-H,C1-C6烷基或-CH2(CHOH)nCH2OH; R5是-H,C1-C6烷基,-CH2(CHOH)nCH2OH或-(CH2)mNMe2; R6为-H,C1-C6烷基或-CH2(CHOH)nCH2OH; R7和R8各自独立地是-H或C1-C6烷基。 R9是甲基或甲苯基; R10为-H,C1-C6烷基或C2-C6烷酰基; Z为> CH2,> 0,> NH或> NCH2CH2OH; n为零或1; m为2或3; p是1、2或3; q为零,1或2;及其药学上可接受的盐,用作酪氨酸激酶抑制剂。

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