AR062210A1 - Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento - Google Patents

Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento

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Publication number
AR062210A1
AR062210A1 ARP070103439A ARP070103439A AR062210A1 AR 062210 A1 AR062210 A1 AR 062210A1 AR P070103439 A ARP070103439 A AR P070103439A AR P070103439 A ARP070103439 A AR P070103439A AR 062210 A1 AR062210 A1 AR 062210A1
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Argentina
Prior art keywords
alkylaminocarbonyl
alkylamino
alkyl
heterocyclyl
heteroaryl
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ARP070103439A
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Merz Pharma Gmbh & Co Kgaa
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Publication of AR062210A1 publication Critical patent/AR062210A1/es

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    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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Abstract

Moduladores de mGluR5 para la prevencion de trastornos neurologicos agudos y cronicos. Proceso de obtencion y composiciones farmacéuticas que los comprende. Reivindicacion 1: Un compuesto pirazolopirimidínico de formula (1) donde, Y1 representa N o C-, Y2 representa N o C-, Y3 representa N o C-, Y4 representa N o C-, mediante la cual al menos dos de los grupos Y1 a Y4 denotan un átomo de carbono, R1 representa cloro o bromo; R2 y R3 cada uno independientemente representa hidrogeno, alquilo C1- 6, cicloalquilo C3-7 o trifluorometilo; o R2 y R3 ambos junto con el átomo de carbono del anillo representan un grupo carbonilo; R4 y R5 cada uno independientemente representa hidrogeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R4 y R5 ambos junto con el átomo de carbono del anillo representan un grupo carbonilo; R6 y R7 representan independientemente hidrogeno, alquilo C1-6, cicloalquilo C3-7 o trifluorometilo; o R6 y R7 ambos junto con el átomo de carbono del anillo representan un grupo carbonilo; R2 o R3 junto con R6 y R7 también pueden formar un radical bivalente a partir del grupo CH2-CH2 o CH2-O; R10 y R11 representan independientemente hidrogeno, halogeno, amino, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, arilo, alquilo C1-6, cicloalquilo C3-7, alquenilo C2-6, alquinilo C2-6, alcoxi C1-6, cicloalquiloxi C3-7, alqueniloxi C2-6, alquiniloxi C2-6, heteroarilo, heterociclilo, ariloxi, heteroariloxi, heterocicliloxi, alquilamino C1-6, di- alquilamino C1-6, cicloalquilamino C3-7, di-cicloalquilamino C3-7, alquil C1-6-cicloalquilamino C3-7, alquenilamino C2-6, alquinilamino C2-6, di-alquenilamino C2-6, di-alquinilamino C2-6, alquil C1-6-alquenilamino C2-6, alquil C1-6-alquinilamino C2- 6, alquenil C2-6-cicloalquilamino C3-7, alquinil C2-6-cicloalquilamino C3-7, alquenil C2-6-alquinilamino C2-6, arilamino, diarilamino, aril-alquilamino C1-6, aril-alquenilamino C2-6, aril-alquinilamino C2-6, aril-cicloalquilamino C3-7, heteroarilamino, diheteroarilamino, heteroaril-alquilamino C1-6, heteroaril-alquenilamino C2-6, heteroaril-alquinilamino C2-6, heteroaril-cicloalquilamino C3-7, heteroarilarilamino, heterociclilamino, diheterociclilamino, heterociclil-alquilamino C1- 6, heterociclil-alquenilamino C2-6, heterociclil-alquinilamino C2-6, heterociclil-cicloalquilamino C3-7, heterociclilarilamino, heterociclilhetero-arilamino, acilo, aciloxi, acilamino, alcoxicarbonilo C1-6, cicloalcoxi C3-7-carbonilo, alqueniloxicarbonilo C2-6, alquiniloxicarbonilo C2-6, ariloxicarbonilo, heteroariloxicarbonilo, heterocicliloxicarbonilo, aminocarbonilo, alquilamino C1-6-carbonilo, di-alquilaminocarbonilo C1-6, cicloalquilaminocarbonilo C3-7, di- cicloalquilaminocarbonilo C3-7, alquil C1-6-cicloalquilaminocarbonilo C3-7, alquenil C2-6-aminocarbonjlo, alquinilaminocarbonilo C2-6, di-alquenilaminocarbonilo C2-6, di-alquinilaminocarbonilo C2-6, alquil C1-6-alquenilaminocarbonilo C2-6, alquil C1- 6-alquinil C2-6-aminocarbonilo, alquenil C2-6-cicloalquilaminocarbonilo C3-7, alquinil C2-6-cicloalquilaminocarbonilo C3-7, alquenil C2-6-alquinilaminocarbonilo C2-6, arilaminocarbonilo, diarilaminocarbonilo, aril-alquilaminocarbonilo C1-6, aril- alquenilaminocarbonilo C2-6, aril-alquinilaminocarbonilo C2-6, aril-cicloalquilaminocarbonil C3-7 heteroarilaminocarbonilo, diheteroarilaminocarbonilo, heteroaril-alquilaminocarbonilo C1-6, heteroaril-alquenilaminocarbonilo C2-6, heteroaril- alquinilaminocarbonilo C2-6, heteroaril-cicloalquilaminocarbonilo C3-7, heteroarilarilaminocarbonilo, heterociclilaminocarbonilo, diheterociclilaminocarbonilo, heterociclil-alquilaminocarbonilo C1-6, heterociclil-alquenilamino C2-6-carbonilo, heterociclil-alquinilaminocarbonilo C2-6, heterociclil-cicloalquil C3-7-aminocarbonilo, heterociclilarilaminocarbonilo, heterociclilheteroarilaminocarbonilo, alquilsulfinilo C1-6, cicloalquilsulfinilo C3-7, alquenilsulfinilo C2-6, alquinilsulfinilo C2-6, arilsulfinilo, heteroarilsulfinilo, heterociclilsulfinilo, alquilsulfonilo C1-6, cicloalquilsulfonilo C3-7, alquenilsulfonilo C2-6, alquinilsulfonilo C2-6, arilsulfonilo, heteroarilsulfonilo, heterociclilsulfonilo, alquilsulfonilamino C1-6, o arilsulfonilamino; o R10 y R11 junto con los dos átomos de carbono que los portan representan un heteroarilo que posee 5 o 6 miembros de anillo o un grupo heterociclilo que posee 5 o 6 miembros de anillo, que pueden ser sustituidos con uno de los siguientes grupos: halogeno, hidroxi, nitro, ciano, trifluorometilo, trifluorometoxi, alquilo C1-6 y alcoxi C1-6; e isomeros opticos, sales, hidratos, solvatos y polimorfos aceptables para uso farmacéutico de los mismos, con la condicion que el compuesto de formula (1) no representa al compuesto (6-Bromo-pirazolo[1,5-a]pirimidin-2-il)-(3,4-dihidro-1H-isoquinolin-2-il)-metanona.
ARP070103439A 2006-08-04 2007-08-03 Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento AR062210A1 (es)

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US83582006P 2006-08-04 2006-08-04
US87754406P 2006-12-28 2006-12-28

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ARP070103438A AR062209A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas moduladoras de receptores de glutamato metabotropicos mglur5, proceso para su preparacion, medicamentos que las contienen y usos en la prevencion y/o tratamiento de trastornos neurologicos agudos y cronicos.
ARP070103437A AR063680A1 (es) 2006-08-04 2007-08-03 Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.
ARP070103439A AR062210A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas sustituidas, un proceso para su preparacion y su uso como medicamento

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ARP070103438A AR062209A1 (es) 2006-08-04 2007-08-03 Pirazolopirimidinas moduladoras de receptores de glutamato metabotropicos mglur5, proceso para su preparacion, medicamentos que las contienen y usos en la prevencion y/o tratamiento de trastornos neurologicos agudos y cronicos.
ARP070103437A AR063680A1 (es) 2006-08-04 2007-08-03 Derivados de pirazolo[1, 5-a]pirimidina, metodos e intermediario para su preparacion, composiciones farmaceuticas que los comprenden y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion de mglur5.

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US (4) US7947689B2 (es)
EP (3) EP2054421B1 (es)
JP (2) JP2009545569A (es)
KR (1) KR20090047450A (es)
AR (3) AR062209A1 (es)
AT (2) ATE494289T1 (es)
AU (2) AU2007280428B2 (es)
BR (2) BRPI0714766A2 (es)
CA (2) CA2659871A1 (es)
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