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AR084768A1 - Moduladores de la senda de complemento y usos de los mismos - Google Patents

Moduladores de la senda de complemento y usos de los mismos

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Publication number
AR084768A1
AR084768A1 ARP120100007A ARP120100007A AR084768A1 AR 084768 A1 AR084768 A1 AR 084768A1 AR P120100007 A ARP120100007 A AR P120100007A AR P120100007 A ARP120100007 A AR P120100007A AR 084768 A1 AR084768 A1 AR 084768A1
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AR
Argentina
Prior art keywords
alkyl
alkoxy
substituted
group
halo
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ARP120100007A
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English (en)
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Novartis Ag
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Application filed by Novartis Ag filed Critical Novartis Ag
Publication of AR084768A1 publication Critical patent/AR084768A1/es

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Abstract

Un método para la elaboración de los compuestos, y sus usos terapéuticos La presente proporciona además una combinación de agentes farmacológicamente activos y una composición farmacéutica.Reivindicación 1: Un compuesto de la fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde Z1 es C, y L es un residuo divalente seleccionado a partir del grupo que consiste en -N(H)- y -C(H)-(R1)-, o Z1 es N, y L es CH2; R1 es hidrógeno, hidroxilo, o amino; Z2 es C(R2) o N; Z3 es C o N; Z4 es C(R4) o N; Z5 es C(R5) o N, o un N-óxido del mismo; Z6 es C(R6) o N, o un N-óxido del mismo; Z7 es C(R7) o N, o un N-óxido del mismo; Z8 es C o N; Z9 es C o N; en donde uno de Z1, Z3, Z8 y Z9 es N, y tres de Z1, Z3, Z8 y Z9 son C; en donde 0, 1 ó 2 ó 3 de Z2, Z4, Z5, Z6 y Z7 son N; R2 es hidrógeno o alquilo C1-6; R3 se selecciona a partir del grupo que consiste en hidrógeno, alquilo C1-4, hidroxi-alquilo C1-4, alcoxilo C1-4-alquilo C1-4, halo-alquilo C1-4, amino, o metil-amino; R4 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, y alquilo C1-6; R5 y R6 se seleccionan independientemente a partir del grupo que consiste en hidrógeno, halógeno, hidroxilo, NR8R9, ciano, CO2H, CONR10R11, SO2-alquilo C1-6, SO2NH2, SO2NR10R11, alcoxilo C1-6-carbonilo, -C(NR10)NR8R9, alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, alcoxilo C1-6, halo-alcoxilo C1-6, y alqueniloxilo C2-6, en donde cada alquilo, alquenilo, alcoxilo y alqueniloxilo está insustituido o sustituido con hasta 4 sustituyentes independientemente seleccionados a partir de halógeno, hidroxilo, ciano, tetrazol, alcoxilo C1-4, halo-alcoxilo C1-4, CO2H, alcoxilo C1-6-carbonilo, C(O)NR10R11, NR8R9, fenilo opcionalmente sustituido, heterociclo opcionalmente sustituido que tiene de 4 a 7 átomos del anillo y 1, 2, ó 3 heteroátomos del anillo seleccionados a partir de N, O ó S, heteroarilo opcionalmente sustituido que tiene 5 ó 6 átomos del anillo y 1, 2 ó 3 heteroátomos del anillo seleccionados a partir de N, O ó S, y en donde los sustituyentes opcionales de fenilo, heterociclo o heteroarilo se seleccionan a partir de halógeno, hidroxilo, alquilo C1-4, alcoxilo C1-4, y CO2H; R5 y R6, tomados en combinación con los átomos con los que están unidos, forman un ciclo que tiene de 4 a 7 átomos del anillo y 0, 1 ó 2 átomos de N, O ó S adicionales del anillo; R7 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, alquilo C1-6, alcoxilo C1-6, halo-alquilo C1-6, halo-alcoxilo C1-6alcoxilo C1-6-carbonilo, CO2H y C(O)NR10R11; R8 y R9 se seleccionan independientemente a partir del grupo que consiste en hidrógeno, y alquilo C1-6, halo-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, hidroxi-alquilo C1-6, o NR8R9, tomados en combinación, forman un heterociclo que tiene de 4 a 7 átomos del anillo y 0 ó 1 átomo de N, O ó S adicional del anillo, cuyo heterociclo está sustituido con 0, 1 ó 2 sustituyentes seleccionados independientemente a partir del grupo que consiste en alquilo C1-4, halógeno, hidroxilo, alcoxilo C1-4; R10 y R11 se seleccionan cada uno independientemente a partir del grupo que consiste en hidrógeno y alquilo C1-6, halo-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, o hidroxi-alquilo C1-6; X1 es CR14R15 o azufre; X2 es CR16R17, oxígeno, azufre, N(H) o N(alquilo C1-6), en donde cuando menos uno de X1 y X2 es carbono; o X1 y X2, en combinación, forman una olefina de la fórmula -C(R16)=C(H)- o -C(R16)=C(alquilo C1-4)-, en donde el C(R16) está unido a X3; X3 es (CR18R19)m o N(H), en donde m es 0, 1 ó 2, en donde X3 es CR18R19 o (CR18R19)2 cuando cualquiera de X1 o X2 es azufre o X2 es oxígeno; o X2 y X3, tomados en combinación, son -N=C(H)- o -N=C(alquilo C1-4)-, en donde el C(H) o C(alquilo C1-4) está unido a X1; R14 se selecciona a partir del grupo que consiste en hidrógeno, halógeno, hidroxilo, amino y alquilo C1-6; R15 se selecciona a partir del grupo que consiste en hidrógeno, hidroxilo, halógeno, alquilo C1-6, halo-alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alcoxilo C1-6, halo-alcoxilo C1-6, NR8R9, N(H)C(O)alquilo C1-6, N(H)C(O)O-alquilo C1-6 y OC(O)NR10R11, en donde cada uno de los sustituyentes de alquilo, alcoxilo, alquenilo, y alquinilo puede estar sustituido con 0, 1 ó 2 grupos independientemente seleccionados en cada presentación a partir del grupo que consiste en halógeno, hidroxilo, alquilo C1-6, alcoxilo C1-6, y NR8R9; R16 es hidrógeno, halógeno, hidroxilo, azida, ciano, COOH, alcoxilo C1-6-carbonilo, alquilo C1-6, alcoxilo C1-6, halo-alquilo C1-6, halo-alcoxilo C1-6, NR8R9, N(H)C(O)alquilo C1-6, hidroxi-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, o alquilo C1-6 sustituido con NR8R9, N(H)C(O)H o N(H)C(O)(alquilo C1-4); R17 es hidrógeno, halógeno, hidroxilo, ciano, alquilo C1-6, alcoxilo C1-6, hidroxi-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, halo-alquilo C1-6, o halo-alcoxilo C1-6; R18 se selecciona a partir del grupo que consiste en hidrógeno, fenilo y alquilo C1-6, cuyo grupo alquilo está insustituido o sustituido con hidroxilo, amino, azida, y NHC(O)-alquilo C1-6; R19 y R20 se seleccionan cada uno independientemente a partir de hidrógeno y alquilo C1-6; o CR16R17, tomados en combinación, forman un carbociclo espirocíclico de 3 a 6 miembros que está sustituido con 0, 1 ó 2 sustituyentes seleccionados independientemente a partir del grupo que consiste en halógeno y metilo; o R16 y R17, tomados en combinación, forman un metilideno exocíclico (=CH2); R15 y R16, tomados en combinación, forman un anillo de epóxido o un sistema de anillo carbocíclico de 3 a 6 miembros, cuyo anillo carbocíclico está sustituido con 0, 1 ó 2 sustituyentes seleccionados independientemente a partir del grupo que consiste en halógeno, metilo, etilo, hidroxi-alquilo C1-4, alcoxilo C1-6-alquilo C1-4, alcoxilo C1-4-carbonilo, CO2H, y alquilo C1-4 sustituido con NR8R9; R16 y R18 o R17 y R19, tomados en combinación, forman un sistema de anillo carbocíclico fusionado de 3 miembros que está sustituido con 0, 1 ó 2 sustituyentes independientemente seleccionados a partir del grupo que consiste en halógeno, metilo, etilo, hidroxi-alquilo C1-4, alcoxilo C1-6-alquilo C1-4, alcoxilo C1-4-carbonilo, CO2H, y alquilo C1-4 sustituido con NR8R9; o R14 y R20, tomados en combinación, forman un sistema de anillo carbocíclico fusionado de 3 miembros; R14 y R19, tomados en combinación, forman un enlazador de alquileno C1-3; R17 y R20, tomados en combinación, forman un enlazador de alquileno C1-3; G es un residuo divalente seleccionado a partir de C(O)-N(H), CH2-N(H)-S(O)2-, CH2-N(H)-C(O), CH2-N(H)-C(O)-O, CH2N(H), CH2-N(H)-C(O)-N(H), CH2-N(H)-C(O)-N(Me), CH2N(H)-S(O)2-N(H)-, y CH2N(H)-S(O)2-N(Me)-, en donde el residuo más a la derecha está unido a -(CR21R22)q; q es 0, 1, 2, 3 ó 4; R21 se selecciona independientemente en cada presentación a partir del grupo que consiste en hidrógeno, hidroxilo, halógeno, alquilo C1-6, halo-alquilo C1-6, ciano-alquilo C1-4, fenilo, CO2H, alcoxilo C1-6-carbonilo, C(O)NH2, hidroxi-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, alquilo C1-6 sustituido con NR8R9, imidazolil-alquilo C1-6, heterocicloalquilo C1-6, en donde el heterociclo se selecciona a partir de azetidinilo, pirrolidinilo, piperidinilo, morfolinilo, 1-oxa-6-aza-espiro-[3.3]-heptano, 2-oxa-6-aza-espiro-[3.3]-heptano, piperazinilo, 1,6-diaza-espiro-[3.3]-heptano, y 2,6-diaza-espiro-[3.3]-heptano, cada uno de los cuales está opcionalmente sustituido por 1 ó 2 sustituyentes seleccionados a partir de flúor, hidroxilo, alquilo C1-4, o alcoxilo C1-4; R22 se selecciona independientemente en cada presentación a partir de hidrógeno o alquilo C1-6; o cuando q es 1, 2, 3 ó 4, R21 y un sustituyente R22, tomados en combinación con los átomos de carbono con los que están unidos, forman un carbociclo de 3 a 6 miembros o un heterociclo de 4 a 6 miembros que tiene un átomo de oxígeno o de nitrógeno del anillo; o cuando q es 2, 3 ó 4, dos residuos R21 o R22, localizados sobre los átomos de carbono adyacentes, forman, junto con los átomos de carbono con los que están unidos, un carbociclo de 3 a 6 miembros; y Z es alquilo C1-6, halo-alquilo C1-6, fenilo, fenoxilo, naftilo, naftiloxilo, cicloalquilo C3-7, indanilo, un heterociclo monocíclico o bicíclico de 5, 6, 9 ó 10 miembros, saturado o parcialmente insaturado, que tiene 1, 2, ó 3 heteroátomos del anillo seleccionados a partir de N, O, ó S, o un heteroarilo o heteroariloxilo de 5 ó 6 miembros, cuyo heteroarilo tiene 1 ó 2 heteroátomos del anillo seleccionados a partir de N, O ó S, en el entendido de que el anillo no tiene 2 átomos de O ó S, cada residuo está insustituido o sustituido con 1, 2, 3, ó 4 sustituyentes que se seleccionan independientemente a partir del grupo que consiste en alquilo C1-6 sustituido o insustituido, cicloalquilo C3-7, halo-alquilo C1-6, halógeno, SF5, CN, hidroxilo, CO2H tetrazolilo, C(O)R25, S(O)2R26, alcoxilo C1-6 sustituido o insustituido, halo-alcoxilo C1-6, fenoxilo, NR23R24, CH2NR23R24, heteroarilo de 5 ó 6 miembros insustituido o sustituido, y fenilo insustituido o sustituido, cuyos fenilo y heteroarilo sustituidos tienen 1 ó 2 sustituyentes seleccionados independientemente a partir del grupo que consiste en ciano, halógeno, alquilo C1-6, o halo-alquilo C1-6, OH, COOH, COR25, S(O)2R26, amino, y CH2NH2, y cuyo alquilo o alcoxilo sustituido tiene un sustituyente seleccionado a partir de hidroxilo, alcoxilo C1-4, ciano, CO2H, tetrazol o NR23R24; R23 es hidrógeno o alquilo C1-6; R24 es hidrógeno, alquilo C1-6, hidroxi-alquilo C1-6, alcoxilo C1-6-alquilo C1-6, amino-alquilo C1-6, mono- y di-alquilo C1-6-amino-alquilo C1-6; o NR23R24, tomados en combinación, forman un heterociclo de 4, 5 ó 6 miembros que tiene 0 ó 1 heteroátomo adicional del anillo seleccionado a partir del grupo que consiste en N, O ó S, y que está sustituido con 0, 1 ó 2 sustituyentes independientemente seleccionados a partir de flúor, hidroxilo, alquilo C1-4, o alcoxilo C1-4; R25 se selecciona independientemente en cada presentación a partir del grupo que consiste en alcoxil
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