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КОМБИНИРОВАННАЯ ТЕРАПИЯ АНТАГОНИСТАМИ c-met И EGFR
专利权人:
ДЖЕНЕНТЕК; ИНК. (US)
发明人:
ФИЛВАРОФФ Эллен (US),МЕРЧАНТ Марк (US),ЙОШ Роберт Л. (US)
申请号:
RU2010140795/15
公开号:
RU2010140795A
申请日:
2009.03.06
申请国别(地区):
RU
年份:
2012
代理人:
摘要:
A method of treating cancer in an individual, comprising administering to the individual a therapeutically effective amount of a c-met antagonist and an EGFR antagonist. !! 2. The method of claim 1, wherein the EGFR antagonist has the general formula I:! !! where m is 1, 2 or 3 !! each R 1 is independently selected from the group consisting of hydrogen, halogen, hydroxy, hydroxyamino, carboxy, nitro, guanidino, ureido, cyano, trifluoromethyl and - (C1-C4 alkylene) -W- (phenyl), where W is a single bond, O, S or NH !! or each R 1 is independently selected from R 9 and C 1 -C 4 alkyl substituted with cyano, wherein R 9 is selected from the group consisting of R 5, -OR 6, -NR 6 R 6, -C (O) R 7, -NHOR 5, -OC (O) R 6, cyano , A and-YR5 R5 is C1-C4 alkyl R6 is independently hydrogen or R5 R7 is R5, -OR6 or -NR6R6 A is selected from piperidino, morpholino, pyrrolidino, 4-R6-piperazin-1-yl, imidazol-1-yl, 4-pyridon-1-yl, - (C1-C4 alkylene) (CO2H), phenoxy, phenyl, phenylsulfanyl, C2-C4 alkenyl and - (C1-C4alkylene) C (O) NR6R6 and Y is S, SO or SO2 wherein the alkyl moieties in R5, -OR6 and -NR6R6 are optionally substituted with halo substituents in an amount of one to three and the alkyl moieties in R5, -OR6 and -NR6R6 are optionally substituted with 1 or 2 R9 groups, and wherein the alkyl moieties of said optional substituents are optionally substituted with halogen or R9 with the proviso that two heteroatoms are not attached to the same carbon atom !! or each R1 is independently selected from -NHSO2R5, phthalimido (C1-C4) -alkylsulfonylamino, benzamido, benzenesulfonylamino, 3-phenylureido, 2-oxopyrrolidin-1-yl, 2,5-dioxopyrrolidin-1-yl, and R10- (C2 -C4) -alkanoylamino, wherein R10 is selected from halogen, -OR6, C2-C4 alkanoyloxy, -C (O) R7 and -NR6R6
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来源网址:
http://www.ckcest.cn/home/

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