AR067602A1 - Sulfonamida como moduladores del trpm8 - Google Patents

Sulfonamida como moduladores del trpm8

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AR067602A1
AR067602A1 ARP080103108A ARP080103108A AR067602A1 AR 067602 A1 AR067602 A1 AR 067602A1 AR P080103108 A ARP080103108 A AR P080103108A AR P080103108 A ARP080103108 A AR P080103108A AR 067602 A1 AR067602 A1 AR 067602A1
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alkyl
amino
optionally substituted
alkoxycarbonyl
substituents
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Janssen Pharmaceutica Nv
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Abstract

Reivindicacion 1: Un compuesto de la formula (1) donde A es CR5 o N; B es CR6 o N; con la condicion de que A y B son C(R5) y C(R6) respectivamente, cuando G es S(O)2; Y es (i) H; (ii) isopropenilo; (iii) alquilcarbonilo C1-6 sustituido de manera opcional con 1 a 3 sustituyentes fluor; (iv) cicloalquilcarbonilo C3-6 (v) fenilcarbonilo sustituido de manera opcional con uno a tres sustituyentes seleccionados de manera independiente entre alquilo C1-4, fluor, o cloro; (vi) fenilcarbonilo sustituido con trifluormetilo y opcionalmente un sustituyente adicional seleccionado entre trifluormetilo, cloro, fluor, o alquilo C1-4 (vii) heteroarilo sustituido de manera opcional con uno a dos sustituyentes seleccionados de manera independiente entre cloro, fluor, bromo, trifluormetilo, alcoxi C1-4, hidroxi, alquilo C1-4, alcoxicarbonilo C1-3, alquiltio C1-3, ciano, amino, alquilamino C1-3, o dialquilamino C1-3; (viii) heteroarilo benzo-fusionado sustituido de manera opcional con uno a dos sustituyentes seleccionados de manera independiente entre cloro, fluor, bromo, trifluormetilo, alquilo C1-4, alcoxi C1-4, hidroxi, alcoxicarbonilo C1-4, alquiltio C1-3, ciano, amino, alquilamino C1-3, o dialquilamino C1-3; (ix) bromo; (x) cloro; (xi) fluor; (xii) yodo; (xiii) ciano; (xiv) formilo; (xv) alquilo C1-6 sustituido de manera opcional con 1 a 3 sustituyentes seleccionados de manera independiente entre hidroxi, fluor, o cloro; (xvi) C(OH) (alquilo C1-3)2, (xvii) cicloalquilo C3-6, (xviii) alquilo C1-2 sustituido con 1 sustituyente seleccionado de manera independiente entre alcoxicarbonilo C1-4, ciano, alquiltio C1-3, alcoxi C1-4, o NR7R8 donde R7 es hidrogeno, alquilo C1-4, alquilcarbonilo C1-3, o alquilsulfonilo C1-3 y R8 es hidrogeno o alquilo C1-4; o R7 y R8 se toman junto con el átomo de nitrogeno al cual están unidos para formar un anillo de 5 o 6 miembros que contiene en forma opcional un heteroátomo adicional seleccionado entre nitrogeno, oxigeno, o azufre; (xix) alcoxicarbonilo C1-4, (xx) alcoxi C1-3, (xxi) hidroxi; (xxii) arilo C6-10 sustituido de manera opcional con uno a tres sustituyentes seleccionados de manera independiente entre cloro, fluor, bromo, alcoxi C1-4, hidroxi, alcoxicarbonilo C1-3, alquiltio C1-3, ciano, amino, alquilamino C1-2, dialquilamino C1-2, o alquilo C1-6 sustituido de manera opcional con uno a tres sustituyentes halogeno; con la condicion de que no más de dos de los sustituyentes están seleccionados del grupo formado por alcoxicarbonilo C1-3, alquiltio C1-3, ciano, amino, alquilamino C1-2, dialquilamino C1-2, y alquilo C1-6 sustituido con uno a tres sustituyentes halogeno; (xxiii) NR9R10 donde R9 es hidrogeno, alquilo C1-4, alquilcarbonilo C1-3, o alquilsulfonilo C1-3 y R10 es hidrogeno o alquilo C1-4, o R9 y R10 se toman junto con el átomo de nitrogeno al cual están unidos para formar un anillo de 5 o 6 miembros que contiene en forma opcional un heteroátomo adicional seleccionado entre nitrogeno, oxígeno, o azufre; y donde ese anillo de 5 o 6 miembros está sustituido de manera opcional con un sustituyente alquilo C1-4 con la condicion de que cuando G es S y R10 es hidrogeno, R9 no es hidrogeno y alquilo C1-4; (xxiv) aminocarbonilo; (xxv) metilaminocarbonilo; (xxvi) dimetilaminocarbonilo; o (xxvii) arilhidroxialquilo C1-3; R1es (i) CF3, (ii) alquilo C1-6 sustituido de manera opcional con 1 sustituyente seleccionado entre alquilsulfonilo C1-3, alcoxicarbonilo C1-4, formulo, hidroxi, carboxi, trifluormetilo, alcoxi C1-4, alquiltio C1-3, bromo, ciano, R11, o R12; (iii) aril-alquilo C1-2 donde el anillo del grupo arilo está sustituido de manera opcional con 1 a 3 sustituyentes seleccionados de manera independiente entre alquilo C1-4, fluor, cloro, trifluormetilo, hidroxi, alcoxi C1-4, alcoxicarbonilo C1-4, o carboxi; con la condicion de que no más de dos de los sustituyentes están seleccionados del grupo formado por trifluormetilo, alcoxicarbonilo C1-4, y carboxi; (iv) heteroaril-alquilo C1-6 donde el anillo del grupo heteroarilo está unido a través de un heteroátomo de nitrogeno y está seleccionado entre imidazolilo, triazolilo, o tetrazolilo; y donde el grupo imidazolilo está sustituido de manera opcional con 1 sustituyente seleccionado entre alquilo C1-4, fluor, cloro, trifluormetilo, hidroxi, alcoxi C1-4, alcoxicarbonilo C1-4, carboxi, aminometilo, metilamino-metilo, o dimetilamino-metilo; e imidazolilo está sustituido de manera opcional con un sustituyente adicional seleccionado entre alquilo C1-4, fluor, o cloro; (v) cicloalquilo C3-8; o ciclohexilo sustituido en la posicion 4 con un sustituyente seleccionado del grupo formado por ciano, alcoxicarbonilo C1-4, carboxi, aminocarbonilo, alquilaminocarbonilo C1-3, di-alquilo C1-3-aminocarbonilo, amino-metilo, metilamino-metilo, dimetilamino-metilo, R11, y R12, (vi) cicloalquilo C5-6 benzo-fusionado ligado en la porcion benzo del sistema anular, y donde la porcion cicloalquilo C5-6 del cicloalquilo C5-6 benzofusionado está sustituido de manera opcional con amino, alquilo C1-3-amino, o di-alquilo C1-3-amino; (vii) fenilo sustituido con 3- o 4-imidazolilo, donde el punto de union del imidazolilo es a través de un heteroátomo de nitrogeno; y donde el imidazolilo está sustituido de manera opcional e independiente con uno a dos sustituyentes seleccionados del grupo formado por alquilo C1-3, 2-ciano, cloro, bromo, amino-alquilo C1-2, alquilo C1-2-amino-alquilo C1-2, y di-alquilo C1-2-amino-alquiloC1-2 donde di-alquilo C1-3 se toma en forma opcional junto con el átomo de nitrogeno al cual está unido para formar un anillo de 5 o 6 miembros que contiene en forma opcional un heteroátomo adicional seleccionado entre nitrogeno, oxigeno, o azufre; y donde el anillo formado por di-alquilo C1-3amino está sustituido de manera opcional con alquilo C1-3 con la condicion de que no más de uno de los sustituyentes es amino-alquilo C1-3, alquilo C1-2-amino-alquilo C1-2, o di-alquilo C1-2-amino-aIquilo C1-2, (viii) fenilo sustituido de manera opcional con uno a tres sustituyentes seleccionados de manera independiente entre alquilo C1-4 sustituido de manera opcional con uno a tres sustituyentes cloro o fluor o un sustituyente hidroxi, cloro, fluor, bromo, alcoxi C1-4, trifluormetoxi, 3- o 4-feniloxi, 3- o 4-heteroariloxi donde el anillo heteroarilo es un anillo de 6 miembros que contiene miembros anulares de carbono y 1 o 2 miembros anulares del heteroátomo de nitrogeno, alquilsulfonilo C1-3, alcoxicarbonilo C1-4, alquiltio C1-3, hidroxi, carboxi, ciano, nitro, 3- o 4-heteroarilo donde dicho heteroarilo no es imidazolilo, alquilcarbonilo C1-3, aminocarbonilo, alquilaminocarbonilo C1-3, dialquilaminocarbonilo C1-3, alquilsulfonilaminocarbonilo C1-3, dialquilaminosulfonilo C1-3, P(O)(Oalquilo C1-3)2, P(O)(OH)2, SO3H, C(O)NHOH, C(=N)NH2, C(=NOH)NH2, C(=N(metilcarboniloxi))NH2, ni SO2NH2; con la condicion de que no más de dos de los sustituyentes están seleccionados del grupo formado por trifluormetoxi, 3- o 4-feniloxi sustituido, 3- o 4-heteroariloxi, alquilsulfonilo C1-3, alcoxicarbonilo C1-4, alquiltio C1-3, carboxi, ciano, 3- o 4-heteroarilo, alquilcarbonilo C1-3, aminocarbonilo, alquilaminocarbonilo C1-3, dialquilaminocarbonilo C1-3, alquilsulfonilaminocarbonilo C1-3, dialquilaminosulfonilo C1-3, y P(O)(Oalquilo C1-3)2 y no más de uno de los sustituyentes está seleccionado del grupo formado por -P(O)(OH)2, -SO3H, carboxi, C(O)NHOH, C(=N)NH2, C(=NOH)NH2, C(=N(alquilcarboniloxi C1-3))NH2, y -SO2NH2 donde el feniloxi está sustituido de manera opcional con uno a dos sustituyentes seleccionados de manera independiente del grupo formado por metilo y fluor; y donde el sustituyente heteroarilo está sustituido de manera opcional e independiente con uno a dos sustituyentes seleccionados del grupo formado por alquilo C1-3, trifluormetilo, trifluormetoxi, ciano, amino, metilamino, dimetilamino, cloro, bromo, carboxi, alcoxicarbonilo C1-2, alcoxicarbonilmetilo C1-2, carboximetilo, amino-alquil C1-2, alquilo C1-2-amino-alquilo C1-2, y di-alquilo C1-2-amino-alquilo-C1-2; con la condicion de que no más de uno de los sustituyentes está seleccionado del grupo formado por carboxi, alcoxicarbonilo C1-2, alcoxicarbonilmetilo C1-2, carboximetilo, amino-alquilo C1-2, alquilo C1-2amino-alquilo C1-2, y di-alquilo C1-2-amino-alquilo C1-2, (ix) naftilo sustituido de manera opcional con un sustituyente seleccionado del grupo formado por hidroxi, cloro, fluor, bromo, alcoxicarbonilo C1-4, y carboxi; (x) arilo C6-10 sustituido con fenilo sustituido de manera opcional con uno a dos sustituyentes seleccionados entre cloro, fluor, alcoxi C1-4, alcoxicarbonilo C1-4, carboxi, hidroxi, o alquilo C1-3, (xi) fenilo sustituido con R11 o R12 en la posicion 3 o 4, y opcionalmente un sustituyente adicional seleccionado entre fluor cloro o alquilo C1-3, (xii) piridin-3-ilo sustituido en un átomo de carbono que no es el que está adyacente al carbono que porta S(O)2 con un sustituyente seleccionado entre N-imidazolilo, oxadiazolilo, tiazolilo, R11, o R12 donde piridin-3-ilo está sustituido de manera opcional con un sustituyente adicional seleccionado entre fluor, cloro, o alquilo C1-3 y además, donde el grupo N-imidazolilo está sustituido de manera opcional con uno a dos sustituyentes, y los grupos oxadiazolilo y tiazolilo están sustituidos de manera opcional con un sustituyente, estando dicho(s) sustituyente(s) seleccionado(s) de manera independiente del grupo formado por alquilo C1-4, trifluormetilo, ciano, amino, metilamino, dimetilamino, cloro, bromo, carboxi, alcoxicarbonilo C1-2, alcoxicarbonilmetilo C1-2, carboximetilo, amino-aIquiIo C1-2, alquilo C1-2-amino-alquilo C1-2, y di-alquilo C1-2-amino-alquilo C1-2; con la condicion de que no más de uno de los sustituyentes está seleccionado del grupo formado por carboxi, alcoxicarbonilo C1-2, alcoxicarbonilmetilo C1-2, carboximetilo, trifluormetilo, ciano, amino-alquilo C1-2, alquilo C1-2amino-alquilo C1-2 y di-alquilo C1-2-amino-alquilo C1-2, (xiii) imidazolilo su
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