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Compounds of 3,4 - dihydro - 1 - 2H - isoquinolin Ona and 2,3 dihydro - 1 - - isoindol ona
专利权人:
F. HOFFMANN-LA ROCHE AG
发明人:
JOHANNES AEBI,WENMING CHEN,BERND KUHN,YONGFU LIU,RAINER E. MARTIN,KURT AMREIN,BENOIT HORNSPERGER,DONGBO LI,HANS P. MAERKI,ALEXANDER V. MAYWEG,XUEFEI TAN,LISHA WANG,JUN WU,MINGWEI ZHOU
申请号:
ARP140102071
公开号:
AR096423A1
申请日:
2014.05.26
申请国别(地区):
AR
年份:
2015
代理人:
摘要:
Claim 1: the compound of equation (1), wherein R1,R2,R3 and r830808 were selected from h, tar and cyclopentadiene respectively; r83099;R8310,R831111 and r8313 are independently selected from h, hydrocarbon, halogen and hydrogen Xi; r831222 and R1 are added together to form - ch832222-ch8322;R1 8304es h or R1 830404 combined with R1 to form - (CH 832222) 695;A es -C (O) - o -S (O) -B is - c-o-n;R² is alkyl, cycloalkyl or substituted heteroaryl, wherein substituted heteroaryl is substituted with one to three substituents independently selected from H, alkyl, cycloalkyl, hydroxy, alkoxy, cyano and halogen; R 3 is halogen, cyano, alkoxy or haloalkoxy; R¹⁴ is H, alkyl or halogen; m, n and p are independently selected between zero and 1; w is 1, 2 or 3; with the proviso that 2- [5- (1-acetyl-pyrrolidin-3-yl) -pyridin-3-yl] -5-chloro-3,3-dimethyl-2,3-dihydro-isoindole-1 is excluded -one and 2- (1-acetyl-1,2,3,4,5,6-hexahydro- [3,4] bipyridinyl-5-yl) -5-chloro-3,3-dimethyl-2,3- dihydro-isoindole-1-one; and pharmaceutically acceptable salts thereof.Reivindicación 1: Compuestos de fórmula (1) en la que R¹, R², R³ y R⁴ se seleccionan independientemente entre H, alquilo y cicloalquilo; R⁵, R⁶, R⁷ y R⁹ se seleccionan independientemente entre H, alquilo, halógeno e hidroxi; R⁸ y R¹¹ en conjunto forman -CH₂-CH₂; R¹⁰ es H o R¹⁰ y R¹¹ en conjunto forman -(CH₂)ʷ-; A es -C(O)- o -S(O)₂-; B es -C- o -N-; R¹² es alquilo, cicloalquilo o heteroarilo sustituido, en el que heteroarilo sustituido está sustituido con uno a tres sustituyentes seleccionados independientemente entre H, alquilo, cicloalquilo, hidroxi, alcoxi, ciano y halógeno; R¹³ es halógeno, ciano, alcoxi o haloalcoxi; R¹⁴ es H, alquilo o halógeno; m, n y p se seleccionan independientemente entre cero y 1; w es 1, 2 ó 3; con la condición de que se excluyan 2-[5-(1-acetil-pirrolidin-3-il)-piridin-3-il]-5-cloro-3,3-dimetil-2,3-dihidro-isoindol-1-ona y 2-(1-acetil-1,2,3,4,5,6-hexahidro-[3,4]bipiridinil-5-il)-5-cloro-3,3-dimetil-2,
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