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首页> 外国专利> XSUP2/SUP represents a direct bond, O, -O-CSUB1-2/SUBalkyl-, CO, -CO-CSUB1-2/SUBalkyl-, NRSUP12/SUP, -NRSUP12/SUP-CSUB1-2/SUBalkyl-, -CHSUB2/SUB-, -O-N=CH- or �CSUB1-2/SUBalkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR.

XSUP2/SUP represents a direct bond, O, -O-CSUB1-2/SUBalkyl-, CO, -CO-CSUB1-2/SUBalkyl-, NRSUP12/SUP, -NRSUP12/SUP-CSUB1-2/SUBalkyl-, -CHSUB2/SUB-, -O-N=CH- or �CSUB1-2/SUBalkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR.

机译：X 2 代表一个直接键，O，-OC 1-2 烷基-，CO，-CO-C 1-2 烷基-， NR 12 ，-NR 12 -C 1-2 烷基-，-CH 2 -，-ON = CH-或C 1-2 烷基-。在受体酪氨酸激酶EGFR的酶促测定中，已经在体外证明了本发明化合物的生长抑制作用抗肿瘤活性。

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摘要

The present invention concerns the compounds of formula (I) the N-oxide forms, the pharmaceutically acceptable addition salts and the stereochemically isomeric forms thereof, wherein Z represents O, CH, NH or S; in particular Z represents NH; Y represents Calkyl-, -Calkenyl-, -Calkynyl-, -Calkyl-CO-NH- optionally substituted with amino, mono- or di(Calkyl)amino or Calkyloxycarbonylamino-, -Calkenyl-CO-NH- optionally substituted with amino, mono- or di(Calkyl)amino- or Calkyloxycarbonylamino-, Calkyl-oxy-Calkyl-, - Calkyl NR- Calkyl-, - Calkyl-NR-CO- Calkyl-, - Calkyl-CO NR- Calkyl-, -Calkyl-CO-NH-, -Calkyl-NH-CO-, -Calkyl-NH-CS-Het-, -Calkyl-NH-CO-Het-, -Calkyl-CO-Het-CO-, -Het-CH-CO-NH-Calkyl-, -CO-NH-C6alkyl-, -NH-CO-Calkyl-, -CO-Calkyl-, -Calkyl-CO-, -Calkyl-CO-Calkyl-, -Calkyl-NH-CO-CRR-NH-, -Calkyl-CO-NH-CRR-CO-, -Calkyl-CO-NR-Calkyl-CO-, Calkyl-NR-CH-CO-NH-Calkyl-, or NR-CO-Calkyl-NH-;Xrepresents a direct bond, O or -O-Calkyl-, CO, -CO-Calkyl-, NR, -NR-Calkyl-, CH-, -O-N=CH- or Calkyl-;Xrepresents a direct bond, O, -O-Calkyl-, CO, -CO-Calkyl-, NR, -NR-Calkyl-, -CH-, -O-N=CH- or Calkyl-. The growth inhibitory effect anti-tumour activity of the present compounds has been demonstrated in vitro, in enzymatic assays on the receptor tyrosine kinase EGFR.
机译：本发明涉及式（I）的化合物，其N-氧化物形式，其药学上可接受的加成盐及其立体化学异构形式，其中Z表示O，CH，NH或S; Z特别是NH; Y代表任选地被氨基，单-或二（C烷基）氨基或C烷氧基羰基氨基-，任选地被氨基取代的-C烯基-，-C烯基-，-C炔基-，-C烷基-CO-NH-，-C烯基-CO-NH- -或二（C烷基）氨基-或C烷氧基羰基氨基-，C烷基-氧基-C烷基-，-C烷基NR-C烷基-，-C烷基-NR-CO-C烷基-，-C烷基-CO NR-C烷基-，-C烷基-CO- NH-，-C烷基-NH-CO-，-C烷基-NH-CS-Het-，-C烷基-NH-CO-Het-，-C烷基-CO-Het-CO-，-Het-CH-CO-NH-烷基-，-CO-NH-C6烷基-，-NH-CO-C烷基-，-CO-烷基-，-C烷基-CO-，-C烷基-CO-C烷基-，-C烷基-NH-CO-CRR-NH- ，-C烷基-CO-NH-CRR-CO-，-C烷基-CO-NR-C烷基-CO-，C烷基-NR-CH-CO-NH-C烷基-或NR-CO-C烷基-NH-; X代表直接键，O或-O-C烷基-，CO，-CO-C烷基-，NR，-NR-C烷基-，CH-，-ON = CH-或C烷基-; X表示直接键，O，-O-C烷基-，CO，-CO-C烷基-，NR，-NR-C烷基-，-CH-，-ON = CH-或C烷基-。在受体酪氨酸激酶EGFR的酶促测定中，已经在体外证明了本发明化合物的生长抑制作用抗肿瘤活性。

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