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AR076859A1 - Derivados de 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 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
AR076859A1
AR076859A1 ARP100101611A ARP100101611A AR076859A1 AR 076859 A1 AR076859 A1 AR 076859A1 AR P100101611 A ARP100101611 A AR P100101611A AR P100101611 A ARP100101611 A AR P100101611A AR 076859 A1 AR076859 A1 AR 076859A1
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AR
Argentina
Prior art keywords
alkyl
independently selected
halo
group
substituted
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ARP100101611A
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English (en)
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Ortho Mcneil Janssen Pharm
Addex Pharmaceuticals Sa
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Application filed by Ortho Mcneil Janssen Pharm, Addex Pharmaceuticals Sa filed Critical Ortho Mcneil Janssen Pharm
Publication of AR076859A1 publication Critical patent/AR076859A1/es

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    • 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
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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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    • A61K31/44—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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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
    • A61K31/553—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole having at least one nitrogen and one oxygen as ring hetero atoms, e.g. loxapine, staurosporine
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  • Animal Behavior & Ethology (AREA)
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  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Dermatology (AREA)
  • Inorganic Chemistry (AREA)
  • Dispersion Chemistry (AREA)
  • Urology & Nephrology (AREA)
  • Hospice & Palliative Care (AREA)
  • Diabetes (AREA)
  • Hematology (AREA)
  • Obesity (AREA)
  • Nutrition Science (AREA)
  • Vascular Medicine (AREA)
  • Addiction (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicacion 1: Un compuesto que tiene la formula (1) o una forma estereoquímicamente isomérica del mismo, donde el enlace dibujado hacia dentro del anillo indica que el enlace puede estar unido a cualquier átomo del anillo de carbono; 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, alquilo C1-3, alquiloxi C1-3alquilo C1-3, alquiloxi 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 uno o más alquilo C1-3 independientemente seleccionado sustituido con uno o más sustituyentes halo seleccionados independientemente; (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 sustituido con uno o más sustituyentes halo seleccionados independientemente; alquiloxi C1-3 sustituido con uno o más sustituyentes halo seleccionados independientemente; alquilo C1-3; cicloalquilo C3-7; y (cicloalquil C3-7)alquilo C1-3; -A-D- forma un radical seleccionado entre (a), (b), (c), (d) y ( e); donde el enlace dibujado dentro de (a) indica que R4 puede estar unido a cualquiera de los átomos del anillo de carbono 2 y 3; cada R3 se selecciona independientemente del grupo formado por hidrogeno; alquilo C1-6 no sustituido; alquilo C1-6 sustituido con uno o más sustituyentes seleccionados independientemente del grupo formado por halo, hidroxi, alcoxi C1-3 y trifluormetilo; cicloalquilo C3-7 no sustituido; cicloalquilo C3-7 sustituido con uno o más sustituyentes seleccionados independientemente del grupo formado por halo, alquilo C1-3, hidroxi, alcoxi C1-3, y trifluormetilo; cicloalquilo C3-7-alquilo C1-3; fenilo no sustituido; fenilo sustituido con uno o más sustituyentes seleccionados independientemente del grupo formado por halo, alquilo C1-3, alcoxi C1-3, y trifluormetilo; Het3 y Het3alquilo C1-3; o cada R3 se selecciona independientemente entre un radical cíclico de formula (f) donde R8 se selecciona entre hidrogeno, alquilo C1-3, alquiloxi C1-3 e hidroxialquilo C1-3; q es 1 o 2; X se selecciona entre O, CH2 y CR9(OH), donde R9 se selecciona entre hidrogeno, alquilo C1-3 y cicloalquilo C3-7; o X es un radical cíclico de formula (g) donde r y s se seleccionan independientemente entre 0, 1 y 2, siempre y cuando r + s >= 2; cada R4, R6 y R7 cada uno se selecciona independientemente entre alquilo C1-3 y alquilo C1-3 sustituido con uno o más sustituyentes halo seleccionados independientemente; cada R5 se selecciona independientemente del grupo formado por hidrogeno, alquilo C1-3, y alquilo C1-3 sustituido con uno o más sustituyentes halo seleccionados independientemente; n, m y p cada uno se selecciona independientemente entre 0, 1 y 2; v es 0 o 1; t y u cada uno se selecciona independientemente entre 1 y 2; W se selecciona entre N y CR10; donde R10 se selecciona entre hidrogeno, halo y trifluormetilo; cada Het1 es un radical heterocíclico saturado seleccionado entre pirrolidinilo; piperidinilo; piperazinilo; y morfolinilo; cada uno de los cuales puede ser sustituido opcionalmente con uno o más cada uno seleccionado independientemente del grupo formado por alquilo C1-6; mono-, di- y tri- haloalquilo C1-3; fenilo no sustituido; y fenilo sustituido con 1, 2 o 3 sustituyentes seleccionados independientemente del grupo formado por halo, trifluormetilo, y trifluormetoxi; cada Het2 es piridilo o pirimidinilo; y cada Het3 es un heterociclo seleccionado del grupo formado por tetrahidropirano, piridilo; y pirimidinilo; cada uno sustituido opcionalmente con uno o más sustituyentes cada uno seleccionado independientemente del grupo formado por halo, alquilo C1-3, alcoxi C1-3 y trifluormetilo; y halo se selecciona entre fluor, cloro, bromo y yodo; o una sal o solvato del mismo farmacéuticamente aceptable.
ARP100101611A 2009-05-12 2010-05-11 Derivados de 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. AR076859A1 (es)

Applications Claiming Priority (1)

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EP09160067 2009-05-12

Publications (1)

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AR076859A1 true AR076859A1 (es) 2011-07-13

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ARP100101611A AR076859A1 (es) 2009-05-12 2010-05-11 Derivados de 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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Country Link
US (1) US8946205B2 (es)
EP (1) EP2430031B1 (es)
JP (1) JP5707390B2 (es)
KR (1) KR20120035158A (es)
CN (1) CN102439015B (es)
AR (1) AR076859A1 (es)
AU (1) AU2010246607B2 (es)
BR (1) BRPI1010831A2 (es)
CA (1) CA2760259C (es)
CL (1) CL2011002837A1 (es)
EA (1) EA020671B1 (es)
ES (1) ES2409006T3 (es)
IL (1) IL215910A (es)
MX (1) MX2011011962A (es)
MY (1) MY153912A (es)
NZ (1) NZ596053A (es)
SG (1) SG176018A1 (es)
TW (1) TW201100417A (es)
WO (1) WO2010130422A1 (es)
ZA (1) ZA201107836B (es)

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