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Novel cycloacrylonitrile

机译:新型环丙烯腈

摘要

It refers to a compound of formula I, where: X is a 5-14 membered heteroaryl containing 1 to 3 heteroatoms; R1 is hydrogen, halogen, among others; R2a and R2b are hydrogen, halogen, cyano, among others; R4a and R4b are hydrogen, halogen, oxo, among others; R5a and R5b are hydrogen, halogen, SF5, among others; R6 and R7 are hydrogen, halogen, among others; R10 is halogen, cyano, among others; R11 is halogen, cyano, among others; y is an integer of 1, 2, 3 or 4. Preferred compounds are: 2 - {[(1aS, 6bR) -4-fluoro-1a-methyl-5- (trifluoromethoxy) -1,1a-dihydro-6bH- cyclopropa [b] [1] benzofuran-6b-yl] methyl} -7- (4-methyl-1H-imidazol-1-yl) -3,4-dihydro-2H-pyrido [1,2-a] pyrazin- 1,6-dione;2 - [(1As, 6br) - 3-fluoro-1a-methyl-5 - (trifluoromethane) - 1, 1a-dihydro-6bh-cyclopapa [b] [1] benzofuran-6b-il] methyl} - 7 - (4-methyl-1h-imidazole-1-il) - 3, 4-dihydro-2h-pyridan [1, 2-A] pyridan-1, 6-dioxin, etc. He also mentioned a pharmaceutical composer These compounds are gamma Secretariat modulators that can be used to treat neurodegenerative and neurological diseases such as Alzheimer's and Down's syndrome.
机译:它是指式I的化合物,其中:X是含有1至3个杂原子的5-14元杂芳基; R 1是氢,卤素等; R 2a和R 2b是氢,卤素,氰基等。 R4a和R4b为氢,卤素,氧代基等。 R5a和R5b是氢,卤素,SF5等。 R 6和R 7是氢,卤素等。 R 10是卤素,氰基等。 R 11为卤素,氰基等。 y是1、2、3或4的整数。优选的化合物是:2-{[((1aS,6bR)-4-fluoro-1a-methyl-5-(trifluoromethoxymethoxy)-1,1a-dihydro-6bH-cyclopropa [b] [1]苯并呋喃-6b-基]甲基} -7-(4-甲基-1H-咪唑-1-基)-3,4-二氢-2H-吡啶基[1,2-a]吡嗪-1 ,6-二酮; 2-[((1As,6br))-3-氟-1a-甲基-5-(三氟甲烷)-1,1a-二氢-6bh-环爸爸[b] [1]苯并呋喃-6b-il]甲基}-7-(4-甲基-1h-咪唑-1-il)-3,4-二氢-2h-吡啶[1,2-A]吡啶-1,6-二恶英等。他还提到了药物组合物这些化合物是伽马秘书处调节剂,可用于治疗神经退行性疾病和神经系统疾病,例如阿尔茨海默氏症和唐氏综合症。

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