AR080055A1 - Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1 - Google Patents

Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1

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Publication number
AR080055A1
AR080055A1 ARP110100295A ARP110100295A AR080055A1 AR 080055 A1 AR080055 A1 AR 080055A1 AR P110100295 A ARP110100295 A AR P110100295A AR P110100295 A ARP110100295 A AR P110100295A AR 080055 A1 AR080055 A1 AR 080055A1
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Argentina
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alkyl
aryl
optionally substituted
heteroaryl
alkoxy
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ARP110100295A
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Novartis Ag
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
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    • C07D491/044—Ortho-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
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Abstract

Utiles como antagonistas de los receptores del factor de liberacion de corticotropina (CRF1). Reivindicacion 1: Un compuesto de la formula (1), en donde R1 y R3, los cuales pueden ser iguales o diferentes, son cada uno hidrogeno, alquilo C1-6, o halogeno-alquilo C1-6; R2 es difluoro-metoxi-fenilo, en donde el fenilo puede estar opcionalmente sustituido por uno o más de alquilo C1-6, alcoxilo C1-6, halogeno, halo-alquilo C1-6, tioalquilo C1-6, -NR5R6, -CN, halo-alcoxilo C1-6, arilo o -Het, o dos átomos de carbono adyacentes están sustituidos por -O(CH2)xO(CH2)y-; Het es un heteroarilo de 5 o 6 miembros o un heterociclo de 4, 5 o 6 miembros; R4 es alquileno C2-10, hidroxi-alquilo C1-10, cada uno de los cuales puede estar opcionalmente sustituido por arilo, o es -OR7, -(CH2)mNR8R9, -COR10, un heteroarilo de 5 o 6 miembros o un heterociclo de 5 o 6 miembros, estando el heteroarilo de 5 o 6 miembros o el heterociclo de 5 o 6 miembros opcionalmente sustituido por uno o más sustituyentes seleccionados a partir del grupo alquilo C1-10, halo-alquilo C1-10, hidroxi-alquilo C1-10, alcoxilo C1-3-alquilo C1-3, halogeno, -CO2R19, -CONR20R21, arilo, o un heterociclo o heteroarilo de 5 o 6 miembros; R5 y R6, los cuales pueden ser iguales o diferentes, son cada uno hidrogeno o alquilo C1-6, o R5 y R6, junto con el átomo de nitrogeno con el que están unidos, forman un grupo cíclico saturado o insaturado opcionalmente sustituido; R7 es alquilo C1-10, cicloalquilo C3-10, opcionalmente fusionado con un arilo, alquilo C1-6-cicloalquilo C3-6-, hidroxi-alquilo C1-10, hidroxi-alquilo C1-6-(halo-alquilo C1-6), (alquilo C1-6)-oxi-alquilo C1-6, -(CH2)qCOOR22, o un heterociclo de 5 o 6 miembros; cada uno de los cuales está opcionalmente sustituido por uno o más de alquilo C1-10, alcoxilo C1-10, hidroxi-alquilo C1-10, arilo, o un heteroarilo de 5 o 6 miembros, estando el arilo o un heteroarilo de 5 o 6 miembros opcionalmente sustituido por alquilo C1-10; R8 y R9, los cuales pueden ser iguales o diferentes, son cada uno hidrogeno, alquilo C1-10, halogeno-alquilo C1-10, (alquilo C1-6)-oxi-alquilo C1-6, -COOR11, -COR12, o aril-alquilo C1-6 o, junto con el átomo de nitrogeno con el que están unidos, R8 y R9 forman un heterociclo de 5 o 6 miembros, opcionalmente sustituido por uno o más de alquilo C1-6; m es un entero 0 o 1; q es un entero de 1 a 6; x e y, los cuales pueden ser iguales o diferentes, son cada uno un entero de 1 a 6; R10 es hidrogeno, alquilo C1-6, -NR13R14, hidroxilo o alcoxilo C1-6; R12 es alquilo C1-10, arilo, o es un anillo heterocíclico insaturado de 5 o 6 miembros; R13 y R14, los cuales pueden ser iguales o diferentes, son cada uno alquilo C1-10, cicloalquilo C3-10, cicloalquilo C3-6-alquilo C1-6-, alcoxilo C1-10, halo-alquilo C1-10, arilo, un heterociclo o heteroarilo de 5 o 6 miembros que comprende 1, 2 o 3 heteroátomos; cada uno de los cuales puede estar opcionalmente sustituido por arilo o heteroarilo, o R13 y R14, junto con el átomo de nitrogeno con el que están unidos, forman un heterociclo de 5 o 6 miembros que comprende 1, 2 o 3 heteroátomos, el cual se puede fusionar opcionalmente con un grupo fenilo, estando el heterociclo y el grupo fenilo opcionalmente fusionados, opcionalmente sustituidos por uno o más de alcoxilo C1-10; R22 es hidrogeno o alquilo C1-6; R11 es alquilo C1-6 o arilo; R19 es hidrogeno o alquilo C1-10; R20 y R21, los cuales pueden ser iguales o diferentes, son cada uno alquilo C1-10; e isomeros del mismo, en forma libre o como una sal farmacéuticamente aceptable.
ARP110100295A 2010-02-01 2011-01-28 Derivados de pirazolo-[5,1-b]-oxazol como antagonistas de los receptores de crf -1 AR080055A1 (es)

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EP (1) EP2531510B1 (es)
JP (1) JP2013518085A (es)
CN (1) CN102762572A (es)
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US20110190360A1 (en) 2011-08-04
TW201130853A (en) 2011-09-16
JP2013518085A (ja) 2013-05-20
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WO2011092290A1 (en) 2011-08-04
UY33210A (es) 2011-08-31

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