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专利概况
专利名称 SUBSTITUTED CARBONUCLEOSIDES DERIVATIVES USED AS ANTICANCER AGENTS
申请号 RU2018142734 申请日
公开(公告)号 RU2712944C1 公开(公告)日
申请(专利权)人 ПФАЙЗЕР ИНК; PFIZER INC 发明人 КАМПФ Роберт Арнольд; КАМПФ Роберт АрнольдKUMPF Robert Arnold; МАКАЛПАЙН Индраван Джеймс; МАКАЛПАЙН Индраван ДжеймсMCALPINE Indrawan James; МАКТИГ Мишель Энн; МАКТИГ Мишель ЭннMCTIGUE Michele Ann; ПЭТМАН Райан; ПЭТМАН РайанPATMAN Ryan; ЖУЙ Юджин Яньцзинь; ЖУЙ Юджин ЯньцзиньRUI Eugene Yuanjin; ТЭТЛОК Джон Ховард; ТЭТЛОК Джон ХовардTATLOCK John Howard; ТРАН ДЬЮБ Мишелль Бич; ТРАН ДЬЮБ Мишелль БичTRAN DUBE Michelle Bich; УАЙТС Мартин Джеймс; УАЙТС Мартин ДжеймсWYTHES Martin James
专利来源 国家知识产权局 转化方式
摘要

FIELD : medicine; pharmaceuticals.SUBSTANCE : invention refers to compounds of general formula I–IV possessing property of enzyme inhibitor PRMT5, their application, pharmaceutical composition based on them, method of treating abnormal growth of cells, including various types of cancer. In general formula I R1 is selected from a group comprising (C1-C8)alkyl and N(R4)2, where each R4 independently is A-R14, where A is absent and R14 is hydrogen; R2 is hydrogen, (C1-C8)alkyl or N(R5)2, where each R5 independently is hydrogen; each R3 are independently selected from hydrogen, hydroxy, (C1-C8)alkyl, or if D is C(R3)2, R3 additionally selected from fluorine; each R9 independently is hydrogen; D is C(R3)2, O; G is phenyl or 10–12-member heteroaryl ring system with 1 to 2 nitrogen atoms or 9–11-heterocyclic ring system with 1 to 2 heteroatoms selected from nitrogen and oxygen; each R8 is absent or is independently selected from a group comprising (C1-C8)alkyl, (C1-C8)haloalkyl, hydroxy, (C1-C8)alkoxy, 5-member heteroaryl with 2-3 heteroatoms selected from N, O and S, CN, halogen and CON(R4)2, and where two R8 optionally combined with formation of carbonate; Q is absent; V is N or C, if Z is present, where if V forms a double bond, V is carbon or V is N or CH and forms a double bond with W, if Z is absent; W is C, where if W forms a double bond, if W is carbon; X is N, if Y is present, where if X forms a double bond, X is carbon or X is NR16, if Y is absent, where R16 is H or methyl; Y is absent, is CR10; Z is absent, is CR12, where each R12 independently selected from hydrogen, fluorine, chlorine, bromine. EFFECT : substituted carbonucleosides derivatives used as anticancer agents are disclosed.39 cl, 2 tbl, 216 ex

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