ES2721073T3 - Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) - Google Patents

Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) Download PDF

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ES2721073T3
ES2721073T3 ES14729373T ES14729373T ES2721073T3 ES 2721073 T3 ES2721073 T3 ES 2721073T3 ES 14729373 T ES14729373 T ES 14729373T ES 14729373 T ES14729373 T ES 14729373T ES 2721073 T3 ES2721073 T3 ES 2721073T3
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halo
group
4alkyl
substituents
bace
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Daniel Oehlrich
Henricus Gijsen
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Janssen Pharmaceutica NV
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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4985—Pyrazines or piperazines ortho- or peri-condensed with heterocyclic ring systems
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Abstract

Un compuesto de Fórmula (I)**Fórmula** o una forma estereoisomérica del mismo, en donde R1 se selecciona del grupo de hidrógeno y halo; R2 se selecciona del grupo de alquiloC1-4 o alquilo C1-4 sustituido por uno o más sustituyentes halo; R3 es en cada caso un sustituyente halo seleccionado independientemente; n es un número entero seleccionado entre 1 y 2; R4 es (a):**Fórmula** en donde R5 es heteroarilo opcionalmente sustituido por uno o más sustituyentes seleccionados cada uno independientemente del grupo de halo, -CN, alquiloC1-4 opcionalmente sustituido por uno o más sustituyentes halo y alquilC1-4oxi opcionalmente sustituido por uno o más sustituyentes halo; en donde heteroarilo es un heterociclo aromático de 5 miembros que se selecciona del grupo que consiste en oxazol y pirazol; o es un heterociclo aromático de 6 miembros que se selecciona del grupo que consiste en piridinilo, pirimidinilo y pirazinilo; o una sal de adición o un solvato farmacéuticamente aceptable del mismo.
ES14729373T 2013-06-12 2014-06-12 Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE) Active ES2721073T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP13171720 2013-06-12
PCT/EP2014/062286 WO2014198854A1 (en) 2013-06-12 2014-06-12 4-amino-6-phenyl-6,7-dihydro[1,2,3]triazolo[1,5-a]pyrazine derivatives as inhibitors of beta-secretase (bace)

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ES2721073T3 true ES2721073T3 (es) 2019-07-26

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ES14729373T Active ES2721073T3 (es) 2013-06-12 2014-06-12 Derivados de 4-amino-6-fenil-6,7-dihidro[1,2,3]triazolo[1,5 a]pirazina como inhibidores de beta-secretasa (BACE)

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Country Link
US (1) US9751886B2 (es)
EP (1) EP3008065B1 (es)
JP (1) JP6435321B2 (es)
KR (1) KR102243133B1 (es)
CN (1) CN105324383B (es)
AU (1) AU2014280125B2 (es)
BR (1) BR112015030597A2 (es)
CA (1) CA2911693C (es)
EA (1) EA028775B1 (es)
ES (1) ES2721073T3 (es)
MX (1) MX366063B (es)
WO (1) WO2014198854A1 (es)

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KR102243134B1 (ko) 2013-06-12 2021-04-22 얀센 파마슈티카 엔.브이. 베타-세크레타제(bace) 저해제로서의 4-아미노-6-페닐-5,6-디하이드로이미다조[1,5-a]피라진 유도체
ES2768823T3 (es) 2014-12-18 2020-06-23 Janssen Pharmaceutica Nv Derivados de 2,3,4,5-tetrahidropiridin-6-amina y 3,4-dihidro-2H-pirrol-5-amina útiles como inhibidores de beta-secretasa

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