AR073262A1 - Derivados de pirazolo[5, 1-b]oxazol, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por antagonistas de crf1. - Google Patents

Derivados de pirazolo[5, 1-b]oxazol, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por antagonistas de crf1.

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AR073262A1
AR073262A1 ARP090102986A ARP090102986A AR073262A1 AR 073262 A1 AR073262 A1 AR 073262A1 AR P090102986 A ARP090102986 A AR P090102986A AR P090102986 A ARP090102986 A AR P090102986A AR 073262 A1 AR073262 A1 AR 073262A1
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Argentina
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carbon atoms
alkyl
aryl
heteroaryl
optionally substituted
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Novartis Ag
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Abstract

Se describen derivados de pirazolo-[5.1-b]-oxazol utiles como antagonistas del receptor 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 de 1 a 6 átomos de carbono, o halo-alquilo de 1 a 6 átomos de carbono; R2 es fenilo, un heteroarilo de 5 o 6 miembros, o un sistema de heteroarilo bicíclico, cada uno de los cuales puede estar opcionalmente sustituido por uno o más de alquilo de 1 a 6 átomos de carbono, alcoxilo de 1 a 6 átomos de carbono, halogeno, halo-alquilo de 1 a 6 átomos de carbono, tioalquilo de 1 a 6 átomos de carbono, -NR5R6, -CN, halo-alcoxilo de 1 a 6 átomos de carbono, -O(CH2)xO(CH2)y- arilo o -Het; Het es un heteroarilo de 5 o 6 miembros, o un heterociclo de 4, 5, o 6 miembros; R4 es alquileno de 2 a 10 átomos de carbono, hidroxi-alquilo de 1 a 10 átomos de carbono, 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 que consiste en alquilo de 1 a 10 átomos de carbono, halo-alquilo de 1 a 10 átomos de carbono, hidroxi-alquilo de 1 a 10 átomos de carbono, alcoxilo (de 1 a 3 átomos de carbono)-alquilo (de 1 a 3 átomos de carbono), 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 de 1 a 6 átomos de carbono, 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 de 1 a 10 átomos de carbono, cicloalquilo de 3 a 10 átomos de carbono, opcionalmente fusionado con un arilo, alquilo (de 1 a 6 átomos de carbono)-cicloalquilo (de 3 a 6 átomos de carbono)-, hidroxi-alquilo de 1 a 10 átomos de carbono, hidroxialquilo (de 1 a 6 átomos de carbono)-(halo-alquilo de 1 a 6 átomos de carbono), alquilo (de 1 a 6 átomos de carbono)-oxi-alquilo (de 1 a 6 átomos de carbono), -(CH2)qCOOR22 o un heterociclo de 5 o 6 miembros; cada uno de los cuales esta opcionalmente sustituido por uno o más de alquilo de 1 a 10 átomos de carbono, alcoxilo de 1 a 10 átomos de carbono, hidroxi-alquilo de 1 a 10 átomos de carbono, arilo o un heteroarilo de 5 o 6 miembros, estando el arilo o heteroarilo de 5 o 6 miembros opcionalmente sustituido por alquilo de 1 a 10 átomos de carbono; R8 y R9, los cuales pueden ser iguales o diferentes, son cada uno hidrogeno, alquilo de 1 a 10 átomos de carbono, haloalquilo de 1 a 10 átomos de carbono, alquilo (de 1 a 6 átomos de carbono)-oxi-alquilo (de 1 a 6 átomos de carbono), -COOR11, -COR12 o aril-alquilo de 1 a 6 átomos de carbono 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 de 1 a 6 átomos de carbono; 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 de 1 a 6 átomos de carbono, -NR13R14, hidroxilo o alcoxilo de 1 a 6 átomos de carbono; R12 es alquilo de 1 a 10 átomos de carbono, 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 de 1 a 10 átomos de carbono, cicloalquilo de 3 a 10 átomos de carbono, cicloalquilo (de 3 a 6 átomos de carbono)-alquilo (de 1 a 6 átomos de carbono)-, alcoxilo de 1 a 10 átomos de carbono, halo-alquilo de 1 a 10 átomos de carbono, arilo, un heterociclo o heteroarilo de 5 o 6 miembros, el cual 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, el cual comprende 1, 2 o 3 heteroátomos, el cual puede estar opcionalmente fusionado con un grupo fenilo, estando este heterociclo y grupo fenilo opcionalmente fusionados, opcionalmente sustituidos por uno o más de alcoxilo de 1 a 10 átomos de carbono; R22 es hidrogeno o alquilo de 1 a 6 átomos de carbono; R11 es alquilo de 1 a 6 átomos de carbono o arilo; R19 es hidrogeno o alquilo de 1 a 10 átomos de carbono; R20 y R21, los cuales pueden ser iguales o diferentes, son cada uno alquilo de 1 a 10 átomos de carbono; e isomeros del mismo, en forma libre o como una sal farmacéuticamente aceptable.
ARP090102986A 2008-08-06 2009-08-04 Derivados de pirazolo[5, 1-b]oxazol, composiciones farmaceuticas que los comprenden y su uso en el tratamiento de enfermedades mediadas por antagonistas de crf1. AR073262A1 (es)

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US20509609P 2009-01-14 2009-01-14
EP09150553 2009-01-14

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MY152687A (en) 2008-04-15 2014-10-31 Eisai R&D Man Co Ltd 3-phenylpyrazolo[5,1-b]thiazole compound
US8273900B2 (en) 2008-08-07 2012-09-25 Novartis Ag Organic compounds
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