AR057978A1 - Compuestos para tratar un desorden del sistema nervioso central relacionado con o afectado por el receptor 5-ht6, composicion farmaceutica que lo contiene y metodo para la preparacion del compuesto - Google Patents

Compuestos para tratar un desorden del sistema nervioso central relacionado con o afectado por el receptor 5-ht6, composicion farmaceutica que lo contiene y metodo para la preparacion del compuesto

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AR057978A1
AR057978A1 ARP060103829A ARP060103829A AR057978A1 AR 057978 A1 AR057978 A1 AR 057978A1 AR P060103829 A ARP060103829 A AR P060103829A AR P060103829 A ARP060103829 A AR P060103829A AR 057978 A1 AR057978 A1 AR 057978A1
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Argentina
Prior art keywords
aryl
alkyl
optionally substituted
halogen
amino
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ARP060103829A
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English (en)
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Phaik-Eng Sum
David Brain How
Tarek Suhayi Mansour
Jaechul Shim
Darrin William Hooper
Matthew Douglas Vera
Joshua James Sabatini
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Wyeth Corp
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Publication of AR057978A1 publication Critical patent/AR057978A1/es

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Abstract

Reivindicacion 1: Un compuesto representado por la formula (1); caracterizado porque A es un resto de estructura de formula (2) o está ausente; R1 se selecciona de hidrogeno, -OH, amino, -NR7R8, halogeno, alquilo C1-12, opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de halogeno, amino, ciano, cicloalquilo C3-6, alquilo C1-12, fenilo, hidroxilo, alcoxi C1-12, N-alquilo C1-12, N-cicloalquilo C3-6, heterociclilo de 3 a 8 átomos en anillo, arilo, ariloxi y N-(alquilo C1-12)arilo, en donde dicho arilo, ariloxi y arilo del N(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, alquenilo C2-12 opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de fenilo, heteroarilo, halogeno, amino, ciano, alquilo, hidroxilo, alcoxi, arilo, alquinilo y N-(alquilo C1-12)-arilo, en donde dicho arilo y arilo de N-(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, ariloxi, heterociclilo y fenilo, y alquinilo C2-12 opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados del grupo halogeno, amino, ciano, alquilo, hidroxilo, y alcoxi; R2 se selecciona de hidrogeno, halogeno, alquilo C1-12, opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de halogeno, amino, ciano, cicloalquilo C3-6, alquilo C1-12, fenilo, hidroxilo, alcoxi C1-12, N-alquilo C1-12, N-cicloalquilo C3-6, heterociclilo de 3 a 8 átomos en anillo, arilo, ariloxi y N-(alquilo C1-12)-arilo, en donde dicho arilo, ariloxi y arilo del N-(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, alquenilo C2-12 opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de fenilo, heteroarilo, halogeno, amino, ciano, alquilo, hidroxilo, alcoxi, arilo, alquinilo y N-(alquilo C1-12)-arilo, en donde dicho arilo y arilo del N-(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, y alquinilo C2-12 opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados del grupo halogeno, amino, ciano, alquilo, hidroxilo, y alcoxi; R3 es una parte de R9, o un resto seleccionado del grupo de formulas (3); R4 se selecciona de hidrogeno, alquilo C1-12, opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de halogeno, amino, ciano, cicloalquilo C3-6, alquilo C1-12, fenilo, hidroxilo, alcoxi C1-12, N-alquilo C1-12, N-cicloalquilo C3-6, heterociclilo de 3 a 8 átomos en anillo, arilo, ariloxi y N-(alquilo C1-12)-arilo, en donde dicho arilo, ariloxi y arilo del N-(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, alquenilo C2-12 opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de fenilo, heteroarilo, halogeno, amino, ciano, alquilo, hidroxilo, alcoxi, arilo, alquinilo y N-(alquilo C1-12)-arilo, en donde dicho arilo y arilo del N- (alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, alquinilo C2-12 opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados del grupo halogeno, amino, ciano, alquilo, hidroxilo, y alcoxi, arilo de 6, 10 o 14 átomos de carbono dicho arilo es opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, N-(alquilo C1-12)-arilo, dicho arilo es opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, aralquilo de 7 a 16 átomos de carbono opcionalmente sustituido, aroilo de 7 a 13 átomos de carbono opcionalmente sustituidos, SR3, heteroarilo opcionalmente sustituido y heteroarilcarbonilo opcionalmente sustituido; R5 se selecciona de alquilo C1-12 opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de halogeno, amino, ciano, cicloalquilo C3-6, alquilo C1-12, fenilo, hidroxilo, alcoxi C1-12, N-alquilo C1-12, N-cicloalquilo C3-6, heterociclilo de 3 a 8 átomos en anillo, arilo de 6, 10 o 14 átomos de carbono, ariloxi y N-(alquilo C1-12)-arilo, en donde dicho arilo, ariloxi y arilo del N-(alquilo C1-12)-arilo, puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, aralquilo C7-16 opcionalmente sustituido, aroilo, -CH2-(CO)OCH2- arilo, dicho arilo es opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados entre halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, ariloxi y fenilo, alquenilo C2-12 opcionalmente sustituido, heteroarilo opcionalmente sustituido, arilo de 6, 10 o 14 átomos de carbono opcionalmente sustituido, alquinilo C2-12 opcionalmente sustituido, cicloalquilo de3 a 6 átomos en anillo, aril- CH=CH-, cicloalquil-alquilo; y adamantilo; R6 se selecciona de hidrogeno, alquilo C1-12 opcionalmente sustituidos con 1 a 3 sustituyentes independientemente seleccionados del grupo de halogeno, amino, ciano, cicloalquilo C3-6, alquilo C1-12, fenilo, hidroxilo, alcoxi C1-12, N-alquilo C1-12, N-cicloalquilo C3-6, heterociclilo de 3 a 8 átomos en anillo, arilo, ariloxi y N-(alquilo C1-12)-arilo, en donde dicho arilo, ariloxi y arilo del N-(alquilo C1-12)-arilo puede ser opcionalmente sustituido con 1 a 3 sustituyentes independientemente seleccionados de halogeno, nitro, ciano, alquenilo, hidroxilo, alquilo, haloalquilo, alcoxi, amino, alquilamino, dialquilamino, carboxilo, alcoxicarbonilo, aril-C(O)-, CH3-C(O)-NH-, aralquilo, ariloxi, heterociclilo y fenilo, y cicloalquilo C3-6; R7 y R8 son cada uno independientemente H o alquilo C1-12 o R7 y R8 cuando son opcionalmente tomados juntos con el átomo de nitrogeno al cual cada uno está sujeto forman un anillo heterociclilo de 3 a 8 miembros; R9 es aralquilo C7-16 opcionalmente sustituido o alquilo C1-12; R10 es H o alquilo C1-12; o una sal farmacéuticamente aceptable de éstos.
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