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Difluoropirrolidinas as Orexin receptor modulators
专利权人:
EOLAS THERAPEUTICS; INC.
发明人:
YUANJUN HE,THEODORE KAMENECKA
申请号:
ARP150102622
公开号:
AR101558A1
申请日:
2015.08.13
申请国别(地区):
AR
年份:
2016
代理人:
摘要:
1. Requirement 1: a compound (1) with formula characteristics,X is nr8308o; R1 is a single ring or double ring heteromorphic group, in which R1 is not replaced or replaced by one or more substitutes independently selected from asphalt, halogen, halide, halide, oh-o-asphalt, cn-nr7491; r74955;-N (Rᵃ) C (O) alkyl, -N (Rᵃ) CO₂-alkyl, -N (Rᵃ) SO₂-alkyl, -C (O) alkyl, -CO₂H, -CO₂-alkyl, -CONRᵃRᵇ,-So8322 asphalt, y-so8322; nr7491; r74955;R749191 and r74955 are independent h or tar; R2 is phenyl or monocyclic heterogeneity, in which R2 is not replaced or replaced by one or more substitutes selected independently from a group of asphalt, halogen, cyclopropylsulfonyl, haloacyl fluoride, oh-o-asphalt, cn-nr75808; r74966;-N (Rᵃ) C (O) alkyl, -N (Rᶜ) CO₂-alkyl, -N (Rᶜ) SO₂-alkyl, -C (O) alkyl, -CO₂H, -CO₂-alkyl, -CONRᶜRᵈ,-So8322 asphalt, y-so8322; nr7580; r74966;R758080 and r74966 are independent h or tar; R3 is phenyl or monocyclic isomer, wherein R3 is not replaced, or replaced by one or more independent substitutes composed of asphalt, halogenated tar, halogenated Oh or asphalt-cn-nr7497; (r75844);-N (r74977) C (o) lessor, - n (r74977) co832222 lessor, - n (r74977) so8322 lessor, - C (o) lessor, - co83222; - coi83222 lessor, - conr7497; - r75844;-So8322 asphalt, y-so8322; nr7497; r75844;Among them, r74977 and r75844 are independent h or rented; r8308s is h or rented; or a salt acceptable for drugs;Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), donde X es NR⁴ ó O; R¹ es un grupo heteroarilo monocíclico o bicíclico, donde R¹ no está sustituido o está sustituido con uno o más sustituyentes seleccionados en forma independiente entre el grupo que consiste en alquilo, haloalquilo, halo, -OH, -O-alquilo, -CN, -NRᵃRᵇ, -N(Rᵃ)C(O)alquilo, -N(Rᵃ)CO₂-alquilo, -N(Rᵃ)SO₂-alquilo, -C(O)alquilo, -CO₂H, -CO₂-alquilo, -CONRᵃRᵇ, -SO₂-alquilo, y -SO₂NRᵃRᵇ; donde Rᵃ y Rᵇ son en forma independiente entre sí H o alquilo; R² es fenilo o un heteroarilo monocíclico, donde R² n
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