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IMIDAZO[4,5-C]HINOLINI KAO INHIBITORI DNK-PK
专利权人:
MERCK PATENT GMBH
发明人:
FUCHSS, THOMAS,MEDERSKI, WERNER,ZENKE, FRANK,FUCHSS, Thomas,MEDERSKI, Werner,ZENKE, Frank
申请号:
RSP20150330
公开号:
RS54038B1
申请日:
2011.07.26
申请国别(地区):
RS
年份:
2015
代理人:
摘要:
The invention relates to compounds of the formulae (I) and (II) in which R1, R2, R3, R4, R5, R8, X and m have the meaning indicated in the claims, and/or physiologically acceptable salts, tautomers and stereoisomers thereof, including mixtures thereof in all ratios. The compounds of the formula (I) can be used for the inhibition of serine/threonine protein kinases and for the sensitization of cancer cells to anticancer agents and/or ionizing radiation. The invention also relates to the use of the compounds of the formula (I) in the prophylaxis, therapy or progress control of cancer, tumors, metastases or angiogenesis disorders, in combination with radiotherapy and/or an anticancer agent. The invention furthermore relates to a process for the preparation of the compounds of the formula (I).Jedinjenja molekulske strukture (I)pri čemu suR1 Y ili -(CY2)n-Ar,R2 Y, -(CY2)p-(C[YR6])s-R7 ili -Alk-R7,R3 Y ili CN,R4 Y, Hal, -(CY2)p-COOY ili -(CY2)p-CO-NYY,R5 A, Hal, -(CY2)p-OY, -(CY2)P-NYY, -(CY2)p-COOY, -(CY2)p-CO-NYY ili -(CY2)P-NY-COY,R6 Y, Hal, -(CY2)n-NYY, -(CY2)n-NY-COO-(CY2)n-SiA3, -(CY2)n-COOY, -CO-NYY, -CO-NY-(CY2)n-OY, -CO-NY-(CY2)n-NYY ili S02A,R7 -(CY2)P-Ar ili -(CY2)P-Het1,X CH2, O, S ili jednostruka veza,Y H ili A,A linearni ili račvasti alkil sa 1, 2, 3, 4, 5, 6, 7, 8, 9 ili 10 C-atoma, pri čemu 1, 2, 3, 4, 5, 6 ili 7 H-atoma nezavisno jedan od drugog može biti zamenjeno sa Hal,Alk alkilen sa 1, 2, 3, 4, 5 ili 6 C-atoma,Ar nesupstituisani iii mono-, di- ili tri-supstituisani fenil sa Hal, A, CN, -(CY2)p-OY, -(CY2)P-NYY, -(CY2)p-COOY, -(CY2)p-CO-NYY ili -(CY2)p-NY-COY,Het1 aromatični heterocikl sa jednim ili dva jezgra i sa 2, 3, 4, 5, 6, 7, 8 ili 9 C-atoma i 1, 2, 3 ili 4 N-, O- i/ili S-atoma, koji može biti mono-, di- ili tri-supstituisan sa Hal, A, CN, -(CY2)p-OY, -(CY2)P-NYY, -(CY2)p-COOY, -(CY2)p-CO-NYY, -(CY2)P-NY-COY ili -SO2-Het2,Het2 zasićeni heterocikl sa jednim jezgrom i sa 2, 3, 4, 5, 6 ili 7 C-atoma i 1, 2, 3 ili 4 N-, O- i/ili S-atoma, koji može bi
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