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PHENYL derivatives as agonists of the cannabinoid receptor 2
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
OLIVIER GAVELLE,DIDIER ROMBACH,MARK ROGERS-EVANS,STEPHAN ROEVER,MATTHIAS NETTEKOVEN,UWE GRETHER
申请号:
ARP160103752
公开号:
AR107009A1
申请日:
2016.12.07
申请国别(地区):
AR
年份:
2018
代理人:
摘要:
1. The present request is directed at phenylethanol derivatives, which are potent agents of Kanak type II steroid receptors for the treatment or prevention of pain and other disorders. 1. Claim 1: a formula compound (1),where: R¹ is cyclopropyl, alkyl or haloazetidinyl; R² is cyclopropylmethoxy, alkoxy, haloalkoxy, halopyridinyl, alkylazolyl or halopyrrolidinyl; with the proviso that at least one of R¹ and R² is cyclopropyl or cyclopropylmethoxy; R³ is -C (O) -NH-C (R⁴R⁵) -R⁶,-C (O) -R o RR83088 and r83099 are independently selected among hydrogen, hydrocarbon, cyclopentadienyl, cyclopentadienyl, cyclopentadienyl, alkylsulfonylpropyl and tar; or rc8308 and r8309 and the carbon atoms connected with them form an oxetanil or endosulfan; r8310 is aminobenzene, 5-metl-1, 2, 4-oxadiazol-3-ilo, hydroxi-hyl, dilezoyl, e. Two two, two two two two two two two two two two two two two two, two two two two two two, two two two two two two, two two two two two YesLa presente solicitud se refiere a derivados de fenilo como agonistas del receptor de canabinoides 2 útiles en el tratamiento o profilaxis del dolor entre otros trastornos. Reivindicación 1: Un compuesto de la fórmula (1), en la que: R¹ es ciclopropilo, alquilo o haloazetidinilo; R² es ciclopropilmetoxi, alcoxi, haloalcoxi, halopiridinilo, alquilazolilo o halopirrolidinilo; con la condición de que por lo menos uno de R¹ y R² sea ciclopropilo o ciclopropilmetoxi; R³ es -C(O)-NH-C(R⁴R⁵)-R⁶, -C(O)-R⁷ o R⁸; R⁴ y R⁵ se eligen con independencia entre hidrógeno, alquilo, cicloalquilo, cicloalquilalquilo, alquilsulfonilalquilo y alquiloxetanilo; o R⁴ y R⁵ junto con el átomo de carbono, al que están unidos, forman un oxetanilo o un dioxotietanilo; R⁶ es aminocarbonilo, 5-metil-1,2,4-oxadiazol-3-ilo, hidroxi-alquilo, tiazolilo, alcoxicarbonilo, carboxi, difluor-azetidinilcarbonilo, 5-amino-1,2,4-oxadiazol-3-ilo, alquilaminocarbonilo o aminocarbonilalquilo; R⁷ es (aminocarbonil)(difluor)pirrolidinilo o (amino-carbonil)azaespiro[2.4
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