KUMPF, Robert Arnold (US),КАМПФ Роберт Арнольд (US),MCALPINE, Indrawan James (US),МАКАЛПАЙН Индраван Джеймс (US),MCTIGUE, Michele Ann (US),МАКТИГ Мишель Энн (US),PATMAN, Ryan (US),ПЭТМАН Райан (US),RU
申请号：
RU2018142734
公开号：
RU0002712944C1
申请日:
2017.06.03
申请国别(地区):
RU
年份:
2020
代理人:
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 exИзобретение относится к соединениям общей формулы I-IV, обладающим свойством ингибитора фермента PRMT5, их применению, фармацевтической композиции на их основе, способу лечения аномального роста клеток, в том числе различных видов рака. В общей формуле I R1 выбирают
