ФЛИНН Дэниел Л. (US),КАУФМАН Майкл Д. (US),ПЕТИЛЛО Питер А. (US)
申请号：
RU2014153920
公开号：
RU2014153920A
申请日:
2012.06.07
申请国别(地区):
RU
年份:
2016
代理人:
摘要：
1. A method of treating a disease caused by the kinase activity of c-KIT, its oncogenic forms or polymorphs, comprising administering a compound of formula Ia or a pharmaceutically acceptable salt thereof, wherein: A is selected from the group consisting of phenyl, naphthyl and benzothienyl； G1 is heteroaryl selected from the group consisting of pyrrolyl, furyl, thienyl, oxazolyl, thiazolyl, isoxazolyl, isothiazolyl, imidazolyl, pyrazolyl, oxadiazolyl, thiadiazolyl, triazolyl, tetrazolyl, pyrazinyl, pyridazinyl, triazinyl, pyridinyl and 4； is heterocyclyl selected from the group consisting of oxetanyl, azetadinyl, tetrahydrofuranyl, pyrrolidinyl, oxazolinyl, oxazolidinyl, imidazolonyl, pyranyl, tetrahydropyranyl, dioxalinyl, piperidinyl and morpholinyl； if A has one or more substituted carbon atoms, sp , then each corresponding sp2-hybridized carbon atom may be optionally substituted with Z3； Z1 is selected from the group consisting of -NH (R4) and -NHCOR8； if Z1 contains an alkyl or alkylene fr an agent, said fragments may be further substituted with one or more C1-C6 alkyls； each Z2 is independently selected from the group consisting of hydrogen, C1-C6 alkyl, C3-C8 carbocyclyl, C1-C6 alkoxy, hydroxyl, hydroxy-C1- C6 alkyl, cyano, (R3) N- and - (CH) R5； if Z2 contains an alkyl or alkylene fragment, these fragments may be further substituted with one or more C1-C6 alkyls； each Z3 is independently selected from the group consisting of H, methyl, ethyl, isopropyl, C3-C4 carbocyclyl, halogen, cyano, - (CH) -N (R3) and - (CH) -R5； R1 selected from the group consisting of C1-C4 alkyl, branched C3-C5 alkyl, and C3-C5 carboci1. Способ лечения заболевания, вызванного киназной активностью c-KIT, ее онкогенных форм или полиморфов, включающий введение соединения формулы Iaили его фармацевтически приемлемой соли,где:A выбран из группы, состоящей из фенила, нафтила и бензотиенила；G1 представляет собой гетероарил, выбранный из группы, состоящей из пирролила, фурила, тиенила, окса
