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MODULADORES DE TETRAHIDROPIRIDOPIRAZINAS DE GPR6
专利权人:
TAKEDA PHARMACEUTICAL COMPANY LIMITED
发明人:
BROWN, Jason,HITCHCOCK, Stephen,HOPKINS, Maria,KIKUCHI, Shota,SUN, Hukai,MONENSCHEIN, Holger,REICHARD, Holly,SCHLEICHER, Kristin,MACKLIN, Todd
申请号:
PE0008382016
公开号:
PE07512016A1
申请日:
2014.12.19
申请国别(地区):
PE
年份:
2016
代理人:
摘要:
The present Invention relates to compounds of formula I where modulators gpr6 is cycloalkyl R1 C3 C3 C6 and C8, heterociclilo heteroaryl C1 - C10 each optionally substituted x1 and x2 is n or CH CH x1 and x2 is n or n x1 and x2 is n Z is alquileno C1 haloalquilenos C6 C1 - C6, between Other Q, s and P is 0, 1 or 2 - or \u2013nr6r7 OR5 R2 is alkyl R3 is C1 - C6Cycloalkyl C3 - C8 and trifluoromethyl alkyl R4 is C1 - C6 Hydroxy or Halo is 0 OR 1 R is alkyl R5 C1 - C3 C6 and C8 cycloalkyl alkyl Hydrogen R6 and R7 is C1 - C6, c1-c6 alkyl, cycloalkyl C3, C8, among others and X3 is CH CR4 and X4 is nr8 or vice versa and R8 is c1-c6 alkyl, haloalquilo C1 - C6, Tre.Preferred compounds are: cyclopropyl - (2 - (4 - (2 - difluorofenoxi) piperidin-1-yl) - 3 - (isopropilamino) - 7.8 - dihidropirido [3,4-b] pirazin - 6 (5H) - il) methanone 1 - (2 - (4 - (2 - difluorofenoxi) piperidin 1 - il) - 3 - (isopropilamino) - 7.8 - dihidropirido [3,4-b] pirazin - 6 (5H) - yl) - 2 - metoxietan - 1 - One among others.These compounds are derived from tetrahidropiridopirazinas being useful in the treatment of conditions associated with gpr6La presente invencion se refiere a compuestos moduladores de GPR6 de Formula I donde R1 es cicloalquilo C3-C8, heterociclilo C3-C6 y heteroarilo C1-C10 cada uno opcionalmente sustituidos X1 es N y X2 es CH o X1 es CH y X2 es N o X1 es N y X2 es N Z es alquileno C1-C6, haloalquilenos C1-C6, entre otros q, s y p son 0, 1 o 2 R2 es -OR5 o –NR6R7 R3 es alquilo C1-C6, cicloalquilo C3-C8 y trifluorometilo R4 es alquilo C1-C6, hidroxi o halo r es 0 o 1 R5 es alquilo C1-C6 y cicloalquilo C3-C8 R6 es hidrogeno y alquilo C1-C6 R7 es alquilo C1-C6, cicloalquilo C3-C8, entre otros X3 es CH y CR4 y X4 es NR8 o viceversa y R8 es alquilo C1-C6, haloalquilo C1-C6, entre otros. Son compuestos preferidos: ciclopropil-(2-(4-(2,4-difluorofenoxi)piperidin-1-il)-3-(isopropilamino)-7,8-dihidropirido[3,4-b]pirazin-6(5H)-il)metanona 1-(2-(4-(2,4-difluorofenoxi)piperidin-1-il)-3-(isop
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