AR056892A1 - Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa - Google Patents

Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa

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AR056892A1
AR056892A1 ARP060105619A ARP060105619A AR056892A1 AR 056892 A1 AR056892 A1 AR 056892A1 AR P060105619 A ARP060105619 A AR P060105619A AR P060105619 A ARP060105619 A AR P060105619A AR 056892 A1 AR056892 A1 AR 056892A1
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Argentina
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heterocycloalkyl
heteroaryl
cycloalkyl
alkyl
aryl
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ARP060105619A
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Astra Ab
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Abstract

Estos compuestos se utilizan en el tratamiento o prevencion de los trastornos de la ansiedad, trastornos y/o trastornos del estado de ánimo. También son utilizados en composiciones farmacéuticas y en la fabricacion de medicamentos con actividad moduladora de GABAA. Se proveen además métodos de síntesis de los mismos. Reivindicacion 1: Un compuesto de la formula (1), o una de sus sales, tautomeros, atropisomeros o precursores hidrolizables in vivo farmacéuticamente aceptables, donde R1 es alquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 R7; R2 es H, C(=O)Rb, C(=O)NRcRd, C(O)ORa, S(O)2Rb, alquilo C1-6, haloalquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde cada uno de los alquilo C1-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 R8; R3, R4 y R5 son cada uno, de modo independiente, H, halo, Si(alquilo C1- 10)3, CN, NO2, ORa, SRa, OC(=O)Ra, OC(=O)ORb, OC(=O)NRcRCd, C(=O)Ra, C(=O)ORb, C(=O)NRcRd, NRcRd, NRcC(=O)Ra, N RcC(O)ORb, NRcS(O)2Rb, S(=O)Ra, S(=O)NRcRd, S(=O)2Ra, S(=O)2NRcRd, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con 1, 2 o 3 R9; R6 es arilo, cicloalquilo, heteroarilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 A1; R7, R8 y R9 son cada uno, de modo independiente, halo, alquilo C1-4, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(=O)Rb', C(=O)NRc'Rd', C(=O)ORa', OC(=O)Rb', OC(=O)NRc'Rd', NRc'Rd', NRc'C(=O)Rb', NRc'C(=O)ORa', NRc'S(=O)2Rb', S(=O)Rb', S(=O)NRc'Rd', S(=O)2Rb' o S(=O)2NRc'Rd'; A1 es halo, CN, NO2, ORa, SRa, C(=O)Rb, C(=O)NRcRd, C(=O)ORa, OC(=O)Rb, OC(=O)NRcRd, NRcRd, NRcC(=O)Rd, NRcC(=O)ORa, NRcS(=O)Rb, NRcS(=O)2Rb, S(=O)Rb, S(=O)NRcRd, S(=O)2Rb, S(O)2NRcRd, alcoxi C1-4, haloalcoxi C1-4, amino, alquil C1-4-amino, dialquil C2-4-amino, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, heterocicloalquilalquilo, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, donde cada uno de los alquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilalquilo, cicloalquilalquilo, heteroarilalquilo, arilo, cicloalquilo, heterocicloalquilalquilo, heteroarilo o heterocicloalquilo está opcionalmente sustituido con 1, 2, 3, 4 o 5 sustituyentes seleccionados, de modo independiente, de halo, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, haloalquilo C1-4, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(=O)Rb', C(=O)NRc'Rd', C(=O)ORa', OC(=O)Rb', OC(=O)NRc'Rd', NRc'Rd', NRc'C(=O)Rb', NRc'C(=O)ORa', NRc'S(=O)Rb', NRc'S(=O)2Rb', S(=O)Rb', S(O)NRc'Rd', S(=O)2Rb' o S(=O)2Rc'Rd'; Ra y Ra' son cada uno, de modo independiente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; Rb y Rb' son cada uno, de modo independiente, H, alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; Rc y Rd son cada uno, de modo independiente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; o Rc y Rd junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; y Rc' y Rd' son cada uno, de modo independiente, H, alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, donde el alquilo C1-10, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, arilo, heteroarilo, cicloalquilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido con OH, amino, halo, alquilo C1-6, haloalquilo C1-6, arilo, arilalquilo, heteroarilo, heteroarilalquilo, cicloalquilo o heterocicloalquilo; o Rc' y Rd' junto con el átomo de N al que están unidos forman un grupo heterocicloalquilo de 4, 5, 6 o 7 miembros; con la condicion de que, cuando R2, R3, R4 y R5 son cada uno H, entonces R6 sea distinto de fenilo no sustituido o cicloalquilo no sustituido.
ARP060105619A 2005-12-20 2006-12-19 Derivados de cinolin-3-carboxamida, metodos para su preparacion, composiciones farmaceuticas que los contienen y su uso en la fabricacion de medicamentos para el tratamiento de enfermedades mediadas por la modulacion del receptor gabaa AR056892A1 (es)

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US75213705P 2005-12-20 2005-12-20
US82369306P 2006-08-28 2006-08-28

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RU2008122405A (ru) 2010-01-27
ECSP088585A (es) 2008-07-30
UY30032A1 (es) 2007-07-31
JP5148507B2 (ja) 2013-02-20
US7425556B2 (en) 2008-09-16
IL191762A0 (en) 2008-12-29
BRPI0620126A2 (pt) 2011-11-01
SA06270474B1 (ar) 2010-12-07
NZ569607A (en) 2011-06-30
EP1966158A1 (en) 2008-09-10
JP2009520021A (ja) 2009-05-21
EP1966158B1 (en) 2012-08-08
JP2012255041A (ja) 2012-12-27
AU2006327300A1 (en) 2007-06-28
ES2391472T3 (es) 2012-11-27
CN104592128A (zh) 2015-05-06
EP1966158A4 (en) 2011-01-26
US20070142328A1 (en) 2007-06-21
NO20083197L (no) 2008-09-10
JP5474153B2 (ja) 2014-04-16
CA2634305A1 (en) 2007-06-28
WO2007073283A1 (en) 2007-06-28
KR20080080206A (ko) 2008-09-02

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