AR057543A1 - Derivados de benzofusionado sustituido utilizables como ligandos receptores de vainiloide - Google Patents

Derivados de benzofusionado sustituido utilizables como ligandos receptores de vainiloide

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AR057543A1
AR057543A1 ARP060104442A ARP060104442A AR057543A1 AR 057543 A1 AR057543 A1 AR 057543A1 AR P060104442 A ARP060104442 A AR P060104442A AR P060104442 A ARP060104442 A AR P060104442A AR 057543 A1 AR057543 A1 AR 057543A1
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Argentina
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substituted
unsubstituted
alkyl
cycloalkenyl
independently
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Laxmikant Atmaran Gharat
Uday Mukund Joshi
Neelima Khairatkar Joshi
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Glenmark Pharmaceuticals Sa
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Abstract

La presente está relacionada con derivados benzofusionados sustituidos, que pueden utilizarse como ligandos del receptor vaniloide, y procesos para su elaboracion. Tratamiento del síntoma de dolor agudo y cronico. Reivindicacion 1: Se revindica un compuesto de la formula (1), un análogo de éste, una sal farmacéuticamente aceptable de éste, un solvato farmacéuticamente aceptable de éste, un hidrato farmacéuticamente aceptable de éste, un N-oxido de éste, un tautomero de éste, un regioisomero de éste, un estereoisomero de éste, una prodroga de éste o un polímero de éste, en donde: X e Y son independientemente O, -S(O)m, NRe; R1 y R2 se unen juntos para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros opcionalmente sustituido, e cual puede incluir opcionalmente uno o más heteroátomos seleccionados de O, NR9 o S(O)m; R3 y R4 son independientemente H, ciano, halogeno, -OR9, alquilo sustituido o no sustituido o -NR9R10, o R3 y R4 forman juntos un grupo oxo; (a) R5, R6 y R7 son independientemente H, nitro, ciano, halogeno, -OR9, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -NR9R10, -C(=L)-R9, -C(O)O-R9, -C(O)NR9R10, -S(O)m-R9 o -S(O)m-NR9R10; y R8 es H, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -NR9R10, -C(=L)-R9, -C(O)O-R9, -C(O)NR9R10, -S(O)m-R9 o -S(O)m-NR9R10; o (b) R5 y R6 se definieron con anterioridad, y R7 y R8 se unen juntos para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros opcionalmente sustituido, el cual puede incluir opcionalmente hasta dos heteroátomos seleccionados de O, NRe o S; cada una de las presencias de R9 y R10 puede ser la misma o diferente y es independientemente H, -ORa, -SRa, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -NRaRb, -C(=L)-Ra, -C(O)O-Ra, -C(O)NRaRb, -S(O)m-Ra o -S(O)m-NRaRb; o R9 y R10 se unen juntos para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros opcionalmente sustituido, el cual puede incluir opcionalmente hasta dos heteroátomos seleccionados e O, NRe o S; cada una de las presencias de Ra y Rb es independientemente H, -ORc, -SRc, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, -C(=L)-Rc, -C(O)O-Rc, - C(O)NRcRd, -S(O)m-Rc, -S(O)m-NRcRd, -NRcRd, o un grupo de proteccion, o Ra y Rb tomados junto con el átomo de N al cual están unidos se juntan para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros opcionalmente sustituido, el cual puede incluir opcionalmente por lo menos dos heteroátomos seleccionados de O, NRe o S; cada uno de las presencias de Rc y Rd independientemente es H, alquilo sustituido o no sustituido, alquenilo sustituido o no sustituido, alquinilo sustituido o no sustituido, cicloalquilo sustituido o no sustituido, cicloalquilalquilo sustituido o no sustituido, cicloalquenilo sustituido o no sustituido, cicloalquenilalquilo sustituido o no sustituido, arilo sustituido o no sustituido, arilalquilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, grupo heterocíclico sustituido o no sustituido, heterociclilalquilo sustituido o no sustituido, heteroarilalquilo sustituido o no sustituido, o un grupo de proteccion, o Rc y Rd tomados junto con el átomo de N al cual están unidos pueden unirse para formar un anillo cíclico saturado o insaturado de 3 a 7 miembros opcionalmente sustituido, el cual puede incluir opcionalmente por lo menos dos heteroátomos seleccionados de O, NRe o S; cada uno de las presencias de Re independientemente es H o alquilo sustituido o no sustituido; cada uno de las presencias de L es independientemente O, S, o NRe; cada una de las presencias de m es independientemente 0, 1 o 2; y n es un entero de 0 a 4.
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