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2. Oxalic acid derivatives and their use as bace inhibitors in the treatment of neurological disorders
专利权人:
NOVARTIS AG
发明人:
BADIGER, SANGAMESH,CHEBROLU, MURALI,FREDERIKSEN, MATHIAS,HOLZER, PHILIPP,HURTH, KONSTANZE,MACHAUER, RAINER,MOEBITZ, HENRIK,NEUMANN, ULF,RAMOS, RITA,RUEEGER, HEINRICH,SCHEFER, MICHAEL,TINTELNOT-BLOMLEY
申请号:
PE2012000094
公开号:
PE20121440A1
申请日:
2010.07.23
申请国别(地区):
PE
年份:
2012
代理人:
摘要:
It refers to a compound obtained from formula (I), wherein X is or s; R1 is h, cyanogen, halide, c1-8 tar, etc.; R2 is arilo, isocyanide, etc.; R3 is h, cyanogen, halide, c1-8 tar, c1-8 halide, etc.; R4 is h, halogenation, cyanogen, c1-8 toxic oxygen, c1-8 halo-8, c1-8 halo-8, c1-8 halo-8, c1-8, etc.; R5, HL, alqueno, C8, etc. C2-8, among others; R4 and R5 together are - C (H) = C (H) - C (H) = C (H) or c1-8 tar; R6 is h, c1-8 tar, c1-8 halogen tar, alcoxilo (c1-8) - tar (c1-8),E1 is - cr7r8, among other things,Among other things, E2 es-cr11r12, among others, R7 and R8 are independent h, cyanogen and halide, which together are oxo-ch2-ch2 -;R11 and R12 are independent h, cyanogen, halide, and so on. Together, they are oxo o-ch2-ch2. - [3 - [3-3]]]]]]]]]]] - [3 - [3 - [3 - [3 - [3 - [3 6-dihydro-2h - [1, 4 - [oxazin-3-il] - phenyl] - 5-trifluoro-methyl-pyridine-2-carbulin, etc. He also mentioned a drug synthesis and a preparation procedure. The compound is a beta Secretary enzyme (bace) inhibitor for the treatment of Alzheimer's disease.SE REFIERE A UN COMPUESTO DERIVADO DE OXACINA DE FORMULA (I) DONDE: X ES O O S; R1 ES H, CIANO, HALOGENO, ALQUILO C1-8, ENTRE OTROS; R2 ES ARILO, HETEROARILO, ENTRE OTROS; R3 ES H, CIANO, HALOGENO, ALQUILO C1-8, HALOALQUILO C1-8, ENTRE OTROS; R4 ES H, HALOGENO, CIANO, ALCOXILO C1-8, HALO-ALCOXILO C1-8, ENTRE OTROS; R5 ES H, CIANO, ALQUENILO C2-8, ALQUINILO C2-8, ENTRE OTROS; R4 Y R5 JUNTOS SON -C(H)=C(H)-C(H)=C(H) O ALQUILENO C1-8, ENTRE OTROS; R6 ES H, ALQUILO C1-8, HALO-ALQUILO C1-8, ALCOXILO(C1-8)-ALQUILO(C1-8), ENTRE OTROS; E1 ES -CR7R8-, ENTRE OTROS; E2 ES -CR11R12, ENTRE OTROS; R7 Y R8 SON INDEPENDIENTEMENTE H, CIANO, HALOGENO, ENTRE OTROS, JUNTOS SON OXO O -CH2-CH2-; R11 Y R12 SON INDEPENDIENTEMENTE H, CIANO, HALOGENO, ENTRE OTROS, JUNTOS SON OXO O -CH2-CH2-. SON COMPUESTOS PREFERIDOS: [3-(5-AMINO-3-METIL-3,6-DIHIDRO-2H-[1,4]-OXAZIN-3-IL)FENIL]-AMIDA DEL ACIDO FURAN-2-CARBOXILICO; 5-METIL-[3-(5-AMINO-3-METIL-3,6-DIHIDRO-2H-[1,4
来源网站:
中国工程科技知识中心
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http://www.ckcest.cn/home/

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