УИКЕЛ Джеймс Г., Мл. (US),БРАУНСТЕЙН Майкл Дж. (US)
申请号：
RU2014118430/15
公开号：
RU2014118430A
申请日:
2012.10.05
申请国别(地区):
RU
年份:
2015
代理人:
摘要：
1. The antagonist Ras represented by Formula (I): where: R represents S, O, N, SO, SO or Se； and R is farnesyl or geranyl geranyl； where at least one of: R represents a 5-membered heterocyclic ring containing at least one heteroatom； and R is a 5- or 6-membered heterocyclic ring containing at least one heteroatom. 2. Ras antagonist according to claim 1, characterized in that the R or R heteroatoms are selected from the group consisting of O, N, S, SO, and SO. The Ras antagonist according to claim 1, characterized in that in the case where R is a 5-membered heterocyclic ring containing one or two heteroatoms, R is CN, C (= O) R, S (= O) (= O) R , COM, SOM or N (R) -substituted tetrazole: wherein: R is hydrogen, hydroxyl, C1-C4 alkyloxy, C2-C4 alkenyloxy, C1-C4 hydroxyalkyloxy, C1-C4 aminoalkyloxy or NRR； R is hydrogen, hydroxyl, C1 -C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl, C1-C4 hydroxyalkyl, C1-C4 alkyloxy or C1-C4 alkylamino and R4 is hydrogen, C1-C4 alkyl, C2-C4 alkenyl, C1-C4 aminoalkyl , C1-C4 hydroxyalkyl, C1-C4 alkyloxy or C1-C4 alkylamino, or where R and R together form a ring comprising morpholine, piperazine or piperidine； M is a salt that forms an organic or inorganic counterion； and R 1 is hydrogen or C 1 -C 4 alkyl. 4. The Ras antagonist according to claim 3, having the formula (3): 5. Ras antagonist according to claim 1, characterized in that in the case where R represents a 5- or 6-membered heterocyclic ring containing at least one heteroatom, R represents a phenyl ring or a possibly substituted phenyl ring. Ras antagonist according to claim 5, characterized in that R represents them1. Антагонист Ras, представленный Формулой (I):где:Rпредставляет собой S, О, N, SO, SOили Se； иRпредставляет собой фарнезил или геранил-геранил； игде по меньшей мере один из:Rпредставляет собой 5-членное гетероциклическое кольцо, содержащее по меньшей мере один гетероатом； иRпредставляет собой 5- или 6-членное гетероциклическое кольцо, содержащее по меньшей мере однии гет
