RAINER MARTIN LUEOEND,RAINER MACHAUER,HEINRICH RUEEGER,SIEM JACOB VEENSTRA
申请号：
ARP120103130
公开号：
AR087668A1
申请日:
2012.08.24
申请国别(地区):
AR
年份:
2014
代理人:
摘要：
This proposal relates to the grass x derivative in formula (1),And pharmaceutically acceptable salts, their pharmaceutical ingredients, their combinations, and their use as drugs, especially for the treatment of Alzheimer's disease or diabetes, through the inhibition of BACE-1 or bace-2. 1. Claim 1: a formula compound (1),or a pharmaceutically acceptable salt thereof, wherein R¹ and R² are independently hydrogen or halogen； R³ and R⁴ are independently hydrogen or C₁₋₃-alkyl；or R³ and R⁴ taken together are cyclopropyl； R⁵ is C₁₋₃ alkyl,a. Halogen - Aquilo c83216c8331237o Alcoy c83321218c8331238 for lease；R8310 is a monocyclic isomer of phenyl or 5 or 6 members, which consists of 1, 2, 3 or 4 heteroatoms independently selected from n, O and S. in this case, phenyl or isomer can be replaced by 1, 2, 3 or 4 substitutes independently selected from halogen, cyanogen, amino and hydroxyl groups, 1. Lease land No. c833218331 and 83242431；Halogen tar c8321c83318324；Halogen asphalt c8321c83318324；b. Halogen alcoxyl c8321c83318324；C₁₋₄ alkoxy,2.Alcox C83218D8331I8324； lease C83218D31832424；C₁₋₄alkoxy C₁₋₄alkoxy,2. Alcox c833218d833124； asphalt c833218d83312424；C₁₋₄alkoxy Cquealkenyl,Alcoxi c83218831s 8324； tar c83322831s 8324；hydroxy-C₁₋₄-alkyl,C₂₋₄ hydroxy-alkenyl and C₂₋₄ hydroxy-alkynyl.La presente se relaciona con derivados de oxazina de la fórmula (1), y sales farmacéuticamente aceptables de los mismos, composiciones farmacéuticas de las mismas, combinaciones de las mismas, y su uso como medicamentos, particularmente para el tratamiento de la Enfermedad de Alzheimer o diabetes a través de la inhibición de la BACE-1 o la BACE-2. Reivindicación 1: Un compuesto de la fórmula (1), o una sal farmacéuticamente aceptable del mismo, en donde R¹ y R² son independientemente hidrógeno ó halógeno； R³ y R⁴ son independientemente hidrógeno o alquilo C₁₋₃； ó R³ y R⁴ tomados juntos son ciclopropilo； R⁵ es alquilo C₁₋₃, halógeno-alquilo C₁₋₃ o alcoxi C₁₋₃alquilo C₁₋₃； y R⁶ es fenilo o un h
