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1. 发明申请

US20130203822A1 COMPOUNDS FOR TREATMENT OF TUMORS BEARING DEREGULATED MYC ONCOPROTEINS 审中-公开
标题翻译：用于治疗承受破坏性MYC肿瘤的肿瘤的化合物
公开(公告)号：US20130203822A1
公开(公告)日：2013-08-08
申请号：US13806880
申请日：2011-06-22
申请人： Alessandro Quattrone , Viktoryia Sidarovich , Valentina Adami
发明人： Alessandro Quattrone , Viktoryia Sidarovich , Valentina Adami
IPC分类号： C07D213/89
CPC分类号： C07D213/89
摘要： Compound of Formula (I): wherein R1, R2 and R3, which are identical or different, are hydrogen atom or C1-4 alkyl, and R4 is a saturated C6-9 linear, branched or cyclic hydrocarbon radical or a radical of Formula (II) wherein X is S or O, Y is a hydrogen atom or up to 2 halogen atoms, Z is a single bond or a divalent radical being O, S, —CR2—, in which R is hydrogen or C1-4 alkyl, or other divalent radical with 2-10 carbon atoms and, optionally, O and/or S atoms linked in the form of a chain, wherein—if the radicals contain 2 or more O and/or S atoms—the latter are separated from one another by at least 2 carbon atoms, and it also being possible for 2 adjacent carbon atoms to be linked together by a double bond, and the free valencies of the carbon atoms being saturated by a hydrogen atom and/or C1-4 alkyl groups, Ar is an aromatic ring system which has up to two rings and which may be substituted by up to three radicals from the group of fluorine, chlorine, bromine, methoxy, C1-4 alkyl, trifluoromethyl and trifluoromethoxy, salts and/or solvates thereof, for use in the treatment of a tumor bearing deregulated MYC oncoproteins, wherein said compound is capable of increasing UTR-dependent expression of at least one MYC gene.
摘要翻译：式（I）的化合物：其中相同或不同的R 1，R 2和R 3是氢原子或C 1-4烷基，R 4是饱和的C 6-9直链，支链或环状烃基或式（ II）其中X是S或O，Y是氢原子或最多2个卤素原子，Z是单键或二价基团是O，S，-CR 2 - ，其中R是氢或C 1-4烷基，或具有2-10个碳原子的其它二价基团和任选的以链形式连接的O和/或S原子，其中 - 如果基团含有2个或更多个O和/或S原子 - 后者与一个另一个为至少2个碳原子，并且也可以通过双键将2个相邻碳原子连接在一起，碳原子的自由价饱和的氢原子和/或C 1-4烷基， Ar是具有多达两个环的芳环体系，其可被氟，氯，溴，甲氧基，C 1-4烷基中的至多三个基团取代 1，三氟甲基和三氟甲氧基，其盐和/或溶剂化物，用于治疗具有失调的MYC癌蛋白的肿瘤，其中所述化合物能够增加至少一种MYC基因的UTR依赖性表达。

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