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Pyrimidine, pyridine and pyrazine amide derivatives substituted with thiazole or imidazole and related compounds such as inhibitors of ABL1, ABL2 and BCR-ABL1 for the treatment of cancer, specific viral infections and specific CNS disorders
专利权人:
Novartis AG
发明人:
FURET, Pascal,GROTZFELD, Robert Martin,JONES, Darryl Brynley,MANLEY, Paul,MARZINZIK, Andreas,MOUSSAOUI, Saliha,PELLE, Xavier Francois Andre,SALEM, Bahaa,SCHOEPFER, Joseph,JAHNKE, Wolfgang
申请号:
ES13730654
公开号:
ES2646777T3
申请日:
2013.05.09
申请国别(地区):
ES
年份:
2017
代理人:
摘要:
A compound of the formula (I): ** Formula ** wherein: Y in each presentation is independently selected from N and CH; Y1 is selected from N and CR5; wherein R5 is selected from hydrogen, methoxy and imidazolyl; wherein the imidazolyl is unsubstituted or substituted with methyl; R1 is a 5- to 9-membered heteroaryl ring that incorporates one to four nitrogen, oxygen or sulfur atoms, wherein no more than one of the atoms is selected from an oxygen or sulfur; wherein the heteroaryl of R1 is unsubstituted or substituted with 1 to 3 R6 groups; R2 is selected from hydrogen, halogen, hydroxyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, methoxycarbonyl, 3,6-dihydro-2H-pyran-4-yl, tetrahydro- 2H-pyran-4-yl, tetrahydro-2H-pyran-4-yloxy and cyclobutyl; wherein this alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, cyclobutyl or tetrahydro-2Hpiran-4-yl of R2 may be unsubstituted or substituted with 1 to 3 groups independently selected from halogen, hydroxyl , cyano, alkoxy of 1 to 4 carbon atoms, morpholino, piperazinyl and NR5aR5b; wherein R5a is selected from hydrogen and alkyl of 1 to 4 carbon atoms; and R5b is selected from hydroxy-ethyl; wherein the R2 piperazinyl substituent may be unsubstituted or additionally substituted with alkyl of 1 to 4 carbon atoms; R3 is selected from hydrogen and halogen; R4 is selected from -SF5 and -Y2-CF2-Y3; R6 in each presentation is independently selected from hydrogen, hydroxyl, alkyl of 1 to 4 carbon atoms, alkoxy of 1 to 4 carbon atoms, cyano, trifluoro-methyl, halogen, amino, methyl-carbonyl, methoxy carbonyl, cyclopropyl and pyrrolidinyl methyl; wherein this alkyl of 1 to 4 carbon atoms, or alkoxy of 1 to 4 carbon atoms of R6 is unsubstituted or substituted with 1 to 3 groups independently selected from halogen and hydroxyl; Y2 is selected from CF2, O and S (O) 0-2; and Y3 is selected from hydrogen, halogen, methyl, difluoro-methyl and trifluoro-methyl; Y4 is selected from N and CR2; Y5 and Y6 are independe
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