ES2682398T3 - Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina - Google Patents

Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina Download PDF

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ES2682398T3
ES2682398T3 ES15714957.6T ES15714957T ES2682398T3 ES 2682398 T3 ES2682398 T3 ES 2682398T3 ES 15714957 T ES15714957 T ES 15714957T ES 2682398 T3 ES2682398 T3 ES 2682398T3
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alkyl
heteroaryl
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Eva Caroff
Remy CASTRO
Thierry Kimmerlin
Emmanuel Meyer
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Idorsia Pharmaceuticals Ltd
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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Abstract

Un compuesto de Fórmula (I)**Fórmula** en el que R1 representa heteroaril-alquilo(C1-2), en el que el heteroarilo es un anillo aromático monocíclico o bicíclico de 5 a elementos que contiene 1, 2 o 3 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre y en el que el heteroarilo está no sustituido o monosustituido o disustituido con alquilo(C1-4); o heterociclilalquilo( C1-2), en el que el heterociclilo es un anillo no aromático monocíclico de 5 o 6 elementos que contiene uno o dos átomos de nitrógeno que está anillado a un anillo de fenilo o piridinilo y en el que el heterociclilo está no sustituido o monosustituido o disustituido, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en alquilo(C1-4) y oxo; R2 representa hidrógeno o metilo; R3 representa arilo, en el que el arilo es un grupo fenilo o naftilo, grupos que están independientemente no sustituidos o monosustituidos o disustituidos, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en halógeno, alquilo(C1-4), alcoxi(C1-4), fluoroalquilo(C1-2), fluoroalcoxi(C1-2) y ciano; aril-alquilo(C1-2), en el que el arilo es un grupo fenilo o naftilo, grupos que están independientemente no sustituidos o monosustituidos con halógeno; heteroarilo, en el que el heteroarilo es un anillo aromático monocíclico o bicíclico de 5 a 10 elementos que contiene 1, 2 o 3 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre y en el que el heteroarilo está no sustituido o monosustituido o disustituido, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en halógeno, alquilo(C1-4), cicloalquilo(C3-6), alcoxi(C1-4), fluoroalquilo(C1-2), fluoroalcoxi(C1-2), dialquil( C1-2)-amino, hidroxi, ciano, fenilo, piridinilo y heteroaril-alquilo(C1-2), en el que el heteroarilo es un anillo aromático monocíclico de 5 o 6 elementos que contiene 1 o 2 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre; aril-alquil(C1-2)-sulfonilo, en el que el arilo es un grupo fenilo o naftilo; o R6- carbonilo; R4 representa hidrógeno, halógeno, fluoroalquilo(C1-2) o ciano; R5 representa hidrógeno, halógeno o fluoroalquilo(C1-2); y R6 representa alquilo(C1-4); cicloalquilo(C3-6), en el que el cicloalquilo está no sustituido o monosustituido con fenilo; cicloalquilo(C5-6), en el que el cicloalquilo está anillado a un anillo de fenilo; alcoxi(C1-2)- alquilo(C1-2); arilo, en el que el arilo es un grupo fenilo o naftilo, grupos que están independientemente no sustituidos o monosustituidos o disustituidos, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en halógeno, alquilo(C1-4), alcoxi(C1-4), fluoroalquilo(C1-2) y di-alquil(C1-2)-amino; aril-alquilo(C1-2), en el que el arilo es un grupo fenilo o naftilo, grupos que están independientemente no sustituidos o monosustituidos o disustituidos, en el que los sustituyentes se seleccionan independientemente entre el grupo que consiste en halógeno y alcoxi(C1-4); ariloxi-alquilo(C1-2), en el que el arilo es un grupo fenilo o naftilo; aril-alcoxi(C1-2), en el que el arilo es un grupo fenilo o naftilo; heterociclil-alquilo(C1-2), en el que el heterociclilo es un anillo no aromático monocíclico de 5 o 6 elementos que contiene uno o dos heteroátomos seleccionados independientemente entre oxígeno y nitrógeno; heteroarilo, en el que el heteroarilo es un anillo aromático monocíclico o bicíclico de 5 a 10 elementos que contiene 1, 2 o 3 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre y en el que el heteroarilo está no sustituido o monosustituido con alquilo(C1-4); o heteroaril-alquilo(C1-2), en el que el heteroarilo es un anillo aromático monocíclico o bicíclico de 5 a 10 elementos que contiene 1, 2 o 3 heteroátomos seleccionados independientemente entre oxígeno, nitrógeno y azufre; o una sal del mismo.
ES15714957.6T 2014-03-24 2015-03-23 Derivados de 8-(piperazin-1-il)-1,2,3,4-tetrahidro-isoquinolina Active ES2682398T3 (es)

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Application Number Priority Date Filing Date Title
WOPCT/IB2014/060092 2014-03-24
IB2014060092 2014-03-24
PCT/IB2015/052098 WO2015145322A1 (en) 2014-03-24 2015-03-23 8-(piperazin-1-yl)-1,2,3,4-tetrahydro-isoquinoline derivatives

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US (1) US9951063B2 (es)
EP (1) EP3122741B1 (es)
JP (1) JP6424234B2 (es)
KR (1) KR102356410B1 (es)
CN (1) CN106103426B (es)
AR (1) AR099789A1 (es)
AU (1) AU2015237826A1 (es)
BR (1) BR112016022046A8 (es)
CA (1) CA2939893C (es)
ES (1) ES2682398T3 (es)
MX (1) MX2016012451A (es)
RU (1) RU2016141443A (es)
TW (1) TW201623280A (es)
WO (1) WO2015145322A1 (es)

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JP2017508773A (ja) 2017-03-30
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CA2939893A1 (en) 2015-10-01
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