AR076860A1 - Derivados de 7-aril- 1,2,4-triazolo[4,3-a]piridina moduladores alostericos positivos de receptores mglur2, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos neurologicos y siquiatricos. - Google Patents

Derivados de 7-aril- 1,2,4-triazolo[4,3-a]piridina moduladores alostericos positivos de receptores mglur2, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos neurologicos y siquiatricos.

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Publication number
AR076860A1
AR076860A1 ARP100101612A ARP100101612A AR076860A1 AR 076860 A1 AR076860 A1 AR 076860A1 AR P100101612 A ARP100101612 A AR P100101612A AR P100101612 A ARP100101612 A AR P100101612A AR 076860 A1 AR076860 A1 AR 076860A1
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Argentina
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alkyl
group
halo
substituents
substituted
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ARP100101612A
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English (en)
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Addex Pharma Sa
Ortho Mcneil Janssen Pharm
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Application filed by Addex Pharma Sa, Ortho Mcneil Janssen Pharm filed Critical Addex Pharma Sa
Publication of AR076860A1 publication Critical patent/AR076860A1/es

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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/4545—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring hetero atom, e.g. pipamperone, anabasine
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Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1) o una forma estereoquímicamente isomérica del mismo, donde A es CH o N; R1 se selecciona del grupo formado por hidrogeno; alquilo C1-6, (alquiloxi C1-3)alquilo C1-3, [(alquiloxi C1-3)-alquiloxi C1-3]alquilo C1-3; alquilo C1-3 sustituido con uno o más sustituyentes halo seleccionados independientemente; bencilo no sustituido; bencilo sustituido con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por halo, alcoxi C1-3, alquilo C1-3, alquiloxi C1-3alquilo C1-3, hidroxialquilo C1-3, ciano, hidroxilo, amino, C(=O)R', C(=O)OR', C(=O)NR'Rö, mono- o di-(alquil C1-3)amino, morfolinilo, (cicloalquil C3-7)alquiloxi C1-3, trifluormetilo y trifluormetoxi, donde R' y Rö se seleccionan independientemente entre hidrogeno y alquilo C1-6, (benciloxi)alquilo C1-3; cicloalquilo C3-7 no sustituido; cicloalquilo C3-7 sustituido con trihaloalquilo C1-3; (cicloalquil C3-7)alquilo C1-3; 4-(2,3,4,5-tetrahidro-benzo[f][1,4]oxazepin)metilo; Het1; Het1alquilo C1-3, Het2 y Het2alquilo C1-3; R2 se selecciona del grupo formado por ciano; halo; alquilo C1-3; alquilo C1-3 sustituido con uno o más sustituyentes halo; alcoxi C1-3 sustituido con uno o más sustituyentes halo; cicloalquilo C3-7 y (cicloalquil C3-7)alquilo C1-3; R3 se selecciona del grupo formado por hidrogeno; alquilo C1-3; cicloalquilo C3-7 no sustituido; cicloalquilo C3-7 sustituido con 1 o más sustituyentes cada uno seleccionado independientemente del grupo formado por hidroxilo, halo, alquilo C1-3, tri-haloalquilo C1-3 y cicloalquilo C3-7; fenilo no sustituido; fenilo sustituido con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por halo, alquilo C1-3, alcoxi C1-3, hidroxialquilo C1-3, trifluormetilo y trifluormetoxi; Het3 piridilo no sustituido; piridilo sustituido con uno o más sustituyentes cada uno seleccionado independientemente entre alquilo C1-3, alquiloxi C1-3, cicloalquilo C3-7, y halo; trihaloalquilo C1-3; e hidroxialquilo C1-3; o R3 es un radical cíclico de formula (a) donde R5 se selecciona del grupo formado por hidrogeno; alquilo C1-3; alquiloxi C1-3; e hidroxialquilo C1-3; n es 1 o 2; Z se selecciona entre CH2 o CR6(OH) donde R6 se selecciona del grupo formado por hidrogeno, alquilo C1-3 y trifluormetilo; o R5 y R6 en forma conjunta forman un radical CH2-CH2; o Z es un radical cíclico de formula (b) donde m y p se seleccionan independientemente entre 0, 1 y 2, siempre y cuando m + p >= 2; R4 se selecciona del grupo formado por hidrogeno; halo; y alquilo C1-3 sustituido con uno o más sustituyentes halo; y X se selecciona del grupo formado por un enlace covalente, alcanodiilo C1-3, O, NH, S, SO, SO2, C(OH)(CH3), CH2-O, O-CH2, CH2-NH, NH-CH2, CHF, y CF2; cada Het1 es un radical heterocíclico saturado seleccionado del grupo formado por pirrolidinilo; piperidinilo; piperazinilo; y morfolinilo; cada uno de los cuales puede estar opcionalmente sustituido con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por alquilo C1-6, alquilo C1-3 sustituido con uno o más sustituyentes halo, fenilo no sustituido y fenilo sustituido con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por halo, trifluormetilo, y trifluormetoxi; cada Het2 es piridilo o pirimidinilo no sustituido; y cada Het3 es un radical heterocíclico saturado seleccionado del grupo formado por pirrolidinilo; piperidinilo; piperazinilo; tetrahidropiranilo; y morfolinilo; cada uno de los cuales puede ser opcionalmente sustituido con uno o más sustituyentes seleccionados independientemente del grupo formado por alquilo C1-6, halo, hidroxilo, alquilo C1-3 sustituido con uno o más sustituyentes halo, fenilo no sustituido, y fenilo sustituido con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por halo, trifluormetilo, y trifluormetoxi; o una sal o solvato farmacéuticamente aceptable del mismo.
ARP100101612A 2009-05-12 2010-05-11 Derivados de 7-aril- 1,2,4-triazolo[4,3-a]piridina moduladores alostericos positivos de receptores mglur2, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos neurologicos y siquiatricos. AR076860A1 (es)

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EP09160064 2009-05-12

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AR076860A1 true AR076860A1 (es) 2011-07-13

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ARP100101612A AR076860A1 (es) 2009-05-12 2010-05-11 Derivados de 7-aril- 1,2,4-triazolo[4,3-a]piridina moduladores alostericos positivos de receptores mglur2, composiciones farmaceuticas que los contienen y uso de los mismos en el tratamiento de trastornos neurologicos y siquiatricos.

Country Status (20)

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US (2) US8716480B2 (es)
EP (1) EP2430021B1 (es)
JP (1) JP5707391B2 (es)
KR (1) KR20120039532A (es)
CN (1) CN102439009B (es)
AR (1) AR076860A1 (es)
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IL215911A0 (en) 2012-01-31
CN102439009A (zh) 2012-05-02

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