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Pyrimidine derivatives as kinase modulators and method of use
专利权人:
Inc.;Exelixis
发明人:
Mann, Lary W.,Leahy, James W.,Nuss, John,Epshteyn, Sergey,Schnepp, Kevin Luke,Noguchi, Robin Tammie,Chen, Jeff,Ibrahim, Mohamed Abdulkader,Dalrymple, Lisa Esther,Shi, Xian,Williams, Matthew Alan,Ridgw
申请号:
AU2005322855
公开号:
AU2005322855B2
申请日:
2005.12.28
申请国别(地区):
AU
年份:
2012
代理人:
摘要:
The invention provides compounds and methods for inhibition of kinases, morespecifically IGF 1 R kinases. The invention also provides compounds and methodsfor inhibition of wild­type Abl. The invention provides compounds formodulating protein kinase enzymatic activity for modulating cellular activitiessuch as proliferation, differentiation, programmed cell death, migrationand chemoinvasion. Compounds of the invention inhibit, regulate and/or modulatekinase receptor signal transduction pathways related to the changes in cellularactivities as mentioned above, and the invention includes compositions whichcontain these compounds, and methods of using them to treat kinase-dependentdiseases and conditions. A compound of formula (I), or a farmaceutically acceptablesalt, hydrate, or prodrug thereof, wherein, V is NRR,or O-R, wherein X is H, halo, C-C alkyl, NO,mono-, di-, or tri-halo substituted methyl, NRR,.C(O)O-C-C alkyl, or N(R)-C(O)-C-Calkyl; Y is H, halo, OH, C-C alkyl, C-Calkyl-NR,R, NRR,, C-Calkoxy, -N(R)-(CH)­NRR,-C(O)O-C-C alkyl, -O-(CH)-NRR,-C(O)-C-C alkyl, -C-C-alkyl-R,-O-R, -C(O)-R, -O-(CH)-R,-C(O)-NRR, -C(O)-N(R)-aryl, -C(O)-N(R)­(CH)-NRR,-C(O)-N(R)-(CH)-aryl -C(O)-N(R)-(CH)-heterocyclyl;or X and Y together with the atoms to which they are attached form a 4-7 memberedheterocyclyl or heteroaryl group containing one or two heteroatoms independentlyselected from O, N, and S. Z is H, NRR, -S-R,or -0-R
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来源网址:
http://www.ckcest.cn/home/
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