ES2693052T3 - Compuestos de triazol como bloqueantes de los canales de calcio de tipo T - Google Patents

Compuestos de triazol como bloqueantes de los canales de calcio de tipo T Download PDF

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ES2693052T3
ES2693052T3 ES15763321T ES15763321T ES2693052T3 ES 2693052 T3 ES2693052 T3 ES 2693052T3 ES 15763321 T ES15763321 T ES 15763321T ES 15763321 T ES15763321 T ES 15763321T ES 2693052 T3 ES2693052 T3 ES 2693052T3
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alkyl
substituted
ring
cycloalkyl
alkoxy
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Olivier Bezencon
John Gatfield
Bibia HEIDMANN
Romain Siegrist
Simon STAMM
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Idorsia Pharmaceuticals Ltd
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    • C07D249/04—1,2,3-Triazoles; Hydrogenated 1,2,3-triazoles
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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  • Plural Heterocyclic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

Un compuesto de fórmula (I)**Fórmula** en la que X representa un átomo de carbono de anillo o un átomo de nitrógeno de anillo; - R1 representa - alquilo(C2-6); - alquilo(C2-4) mono-sustituido con ciano, o alcoxi(C1-3); - fluoroalquilo(C1-4); - fluoroalcoxi(C1-3); - pentafluoro-sulfanilo; - cicloalquilo(C3-6)-L1- en el que - dicho cicloalquilo(C3-6) contiene opcionalmente un átomo de oxígeno de anillo; en el que dicho cicloalquilo(C3-6) no está sustituido; o está mono-sustituido con flúor, alquilo(C1-3), alcoxi(C1-3), hidroxi, ciano, o fluoroalquilo(C1-3); o está di-sustituido con flúor, o tri-sustituido con dos sustituyentes flúor y un sustituyente alquilo (C1-3); y - el enlazador L1 representa un enlace directo, alquileno(C1-2), oxígeno, o alquilen(C1-2)-oxi; - heteroarilo de 5 o 6 miembros, independientemente y de manera opcional mono-sustituido con alquilo (C1-3); - -NR11R12, en el que - R11 y R12 representan independientemente hidrógeno, alquilo(C1-3), fluoroalquilo(C2-3), cicloalquilo(C3-6), cicloalquilo(C3-6) mono- o di-sustituido con flúor, cicloalquilo(C3-6)-alquilo(C1-3), alcoxi(C1- 3)- alquilo(C2-3); - o R11 y R12, junto con el átomo de nitrógeno al cual están unidos, forman un anillo de 4 a 6 miembros el cual está opcionalmente mono- o di-sustituido con flúor; un grupo 2-oxo-pirrolidinilo; o un grupo morfolinilo; y (R4)n representa uno o dos sustituyentes opcionales seleccionado independientemente de alquilo(C1-4), alcoxi(C1-4), fluoroalquilo(C1-3), fluoroalcoxi(C1-3), halógeno, y ciano; - o R1 junto con (R4)n forma un anillo no aromático de 5 o 6 miembros que está fusionado al anillo fenilo/ piridina; donde dicho anillo de 5 o 6 miembros contiene opcionalmente uno o dos heteroátomos seleccionados independientemente de oxígeno y nitrógeno; donde dicho anillo no aromático de 5 o 6 miembros independientemente está opcionalmente y de manera adicional mono-sustituido con oxo; o di-, tri-, o tetra-sustituido conde uno de los sustituyentes es oxo y el resto son alquilo(C1-3); - o R1 junto con (R4)n forma un anillo aromático de 5 o 6 miembros que está fusionado al anillo fenilo/ piridina; donde dicho anillo de 5 o 6 miembros contiene opcionalmente uno o dos átomos de nitrógeno, donde dicho anillo aromático fusionado de 5 o 6 miembros independientemente está opcionalmente y de forma adicional mono- o di-sustituido donde los sustituyentes son seleccionados independientemente de alquilo(C1- 4), cicloalquilo(C3-6), fluoroalquilo(C1), o ciano; Y representa un átomo de carbono de anillo o un átomo de nitrógeno de anillo; y R2 representa alquilo(C1-4); cicloalquilo(C3-6); alcoxi(C1-4); cicloalquil(C3-6)-oxi; fluoroalquilo(C1-3); fluoroalcoxi(C1-3); alcoxi(C1-3)-alcoxi(C2-3); halógeno; ciano; o -NR21R22, donde R21 y R22 representan independientemente hidrógeno, o alquilo(C1-3), o R21 y R22, junto con el átomo de nitrógeno al cual están unidos, forman un anillo de 4 a 6 miembros opcionalmente mono- o di-sustituido con flúor, o un grupo morfolinilo; y (R5)m representa uno o dos sustituyentes opcionales seleccionado independientemente de alquilo(C1-4); cicloalquilo(C3-6); alcoxi(C1-4); halógeno; ciano; fluoroalquilo(C1-3); y fluoroalcoxi(C1-3); o una sal de tal compuesto.
ES15763321T 2014-09-15 2015-09-14 Compuestos de triazol como bloqueantes de los canales de calcio de tipo T Active ES2693052T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP2014069592 2014-09-15
PCT/EP2015/070934 WO2016041892A1 (en) 2014-09-15 2015-09-14 Triazole compounds as t-type calcium channel blockers

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ES2693052T3 true ES2693052T3 (es) 2018-12-07

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US (1) US10246426B2 (es)
EP (1) EP3194374B1 (es)
JP (1) JP6500092B2 (es)
KR (1) KR102424750B1 (es)
CN (1) CN107074822B (es)
AU (1) AU2015317022B2 (es)
CA (1) CA2956816C (es)
CL (1) CL2017000616A1 (es)
EA (1) EA032873B1 (es)
ES (1) ES2693052T3 (es)
IL (1) IL251042A0 (es)
MX (1) MX367519B (es)
PH (1) PH12017500447A1 (es)
PL (1) PL3194374T3 (es)
SG (1) SG11201701998XA (es)
WO (1) WO2016041892A1 (es)

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