AR056215A1 - Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios - Google Patents

Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios

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Publication number
AR056215A1
AR056215A1 ARP060104861A ARP060104861A AR056215A1 AR 056215 A1 AR056215 A1 AR 056215A1 AR P060104861 A ARP060104861 A AR P060104861A AR P060104861 A ARP060104861 A AR P060104861A AR 056215 A1 AR056215 A1 AR 056215A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
nr9c
alkyl
heteroaryl
Prior art date
Application number
ARP060104861A
Other languages
English (en)
Original Assignee
Amira Pharmaceuticals Inc
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=37546284&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR056215(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Amira Pharmaceuticals Inc filed Critical Amira Pharmaceuticals Inc
Publication of AR056215A1 publication Critical patent/AR056215A1/es

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    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/10—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a carbon chain containing aromatic rings
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    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
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Abstract

Se describen en la presente, compuestos y composiciones farmacéuticas que contienen tales compuestos que modulan la actividad de la proteína activadora de la 5-lipoxigenasa (FLAP). También se describen en la presente la utilizacion de tales moduladores de FLAP, solos y en combinacion con otros compuestos, para tratar enfermedades respiratorias, cardiovasculares, y otras afecciones o enfermedades leucotrieno-dependientes o mediadas por leucotrienos. Reivindicacion 1: Un compuesto que tiene la estructura de formula (1), en la cual, Z se selecciona de OC(R1)2[C(R2)2]n, [C(R2)2]nC(R1)2O, [C(R2)2]nO[C(R1)2]n, [C(R1)2]nO[C(R2)2]n donde cada R1 es independientemente H, CF3, o un alquilo inferior opcionalmente substituido y dos R1 sobre el mismo carbono pueden unirse para formar un carbonilo (=O); y cada R2 es independientemente H, OH, OMe, CF3, o un alquilo inferior opcionalmente substituido y dos R2 sobre el mismo carbono pueden unirse para formar un carbonilo (=O); m es 0, 1 o 2; cada n es independientemente 0, 1, 2 o 3; Y es H, -L1-(alquilo substituido o no substituido); -L1-(alquenilo substituido o no substituido); -L1-(alquinilo substituido o no substituido); -L1-(cicloalquilo substituido o no substituido); -L1- (heteroarilo substituido o no substituido); -L1-(arilo substituido o no substituido); donde L1 es un enlace, un alquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, un heteroarilo substituido o no substituido, un cicloalquilo substituido o no substituido, un heteroalquilo substituido o no substituido, un heteroalquenilo substituido o no substituido, o un heteroalquinilo substituido o no substituido, donde cada substituyente es (LsRs)j, donde cada Ls se selecciona independientemente de un enlace, -O-, -C(=O)-, -S-, -S(=O)-, -S(=O)2-, -NHC(O)-, -C(O)NH-, S(=O)2NH-, -NHS(=O)2, -OC(O)NH-, -NHC(O)O-, -OC(O)O-, -NHC(O)NH-, -C(O)O-, - OC(O)-, alquilo C1-6, alquenilo C2-6, fluoroalquilo C1-6, heteroarilo, arilo, o grupo heteroalicíclico; y cada Rs se selecciona independientemente de H, halogeno, -N(R4)2, -CN, -NO2, N3, -S(=O)2NH2, alquilo inferior, cicloalquilo inferior, fluoroalquilo C1-6, heteroarilo o heteroalquilo; donde j s 0, 1, 2 3 o 4; cada R4 se selecciona independientemente H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo, o dos grupos R4 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; R6 es H, L2-(alquilo substituido o no substituido), L2-(cicloalquilo substituido o no substituido), L2-(alquenilo substituido o no substituido), L2-(cicloalquenilo substituido o no substituido), L2-(heterociclo substituido o no substituido), L2-(heteroarilo substituido o no substituido), o L2-(arilo substituido o no substituido), donde L2 es un enlace, O, S, -S(=O), -S(=O)2, C(O), -CH(OH), -(alquilo C1-6 substituido o no substituido), o -(alquenilo C2-6 substituido o no substituido); R7 es L3-X-L4-G2 donde L3 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, arilo substituido o no substituido, heteroarilo substituido o no substituido, heteroalicíclico substituido o no substituido; X es -NR9C(O), -C(O)NR9, -S(=O)2NR9-, -NR9S(=O)2, -OC(O)NR9-, - NR9C(O)O-, -CH=NO-, -ON=CH-, -NR9C(O)NR9-, heteroarilo, arilo, - NR9C(=NR10)NR9-, -NR9C(=NR10), -C(=NR10)NR9-, -OC(=NR10)-, o -C(=NR10)O-; L4 es un alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido; G2 es H, -NHS(=O)2R8, S(=O)2N(R9)2, -OR9, -C(=O)CF3, CN, N(R9)2, -N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, -S(=O)R8, -S(=O)2R8, -L5-(alquilo substituido o no substituido), -L5-(alquenilo substituido o no substituido), -L5-(heteroarilo substituido o no substituido), o -L5-(arilo substituido o no substituido), donde L5 es -OC(O)O-, -NHC(O)NH-, -NHC(O)O, -O(O)CNH-, -NHC(O), -C(O)NH, -C(O)O, u -OC(O); o G2 es W-G5, donde W es arilo substituido o no substituido, grupo heteroalicíclico substituido o no substituido o heteroarilo substituido o no substituido y G5 es H, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, CN, N(R9)2, - N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, -S(=O)R8, -S(=O)2R8, ; cada R8 se selecciona independientemente de alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo; cada R9 se selecciona independientemente de H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo o bencilo; o dos grupos R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; o R8 y R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros y cada R10 se selecciona independientemente de H, -S(=O)2R8, -S(=O)2NH2, -C(O)R8, - CN, -NO2, heteroarilo, o heteroalquilo; o(b) L3-X-L4-G4, donde L3 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido, arilo substituido o no substituido, heteroarilo substituido o no substituido, un grupo heteroalicíclico substituido o no substituido; X es un enlace, O, -C(=O), -CR9(OR9), S, S(=O), -S(=O)2, -NR9, -NR9C(O), -C(O)NR9, -OC(O)NR9-, - NR9C(O)O-, -CH=NO-, - ON=CH-, -NR9C(O)NR9-, heteroarilo, arilo, -NR9C(=NR10)NR9-, -NR9C(=NR10), -C(=NR10)NR9-, -OC(=NR10)-, o -C(=NR10)O-; L4 es un alquilo substituido o no substituido, cicloalquilo substituido o no substituido, alquenilo substituido o no substituido, alquinilo substituido o no substituido; G4 es -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -L5-(alquilo substituido o no substituido), -L5-(alquenilo substituido o no substituido), -L5-(heteroarilo substituido o no substituido), o -L5- (arilo substituido o no substituido), donde L5 es -NHC(O)O, -O(O)CNH-, -C(O)O, u -OC(O); o G4 es W-G5, donde W es un arilo substituido o no substituido, grupo heteroalicíclico substituido o no substituido o un heteroarilo substituido o no substituido y G5 es es H, halogeno, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, CN, N(R9)2, -N(R9)C(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, - S(=O)R8, -S(=O)2R8, con la condicion que G4 no sea un tetrazol; cada R8 se selecciona independientemente de alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo substituido o no substituido o bencilo substituido o no substituido; cada R9 se selecciona independientemente de H, alquilo inferior substituido o no substituido, cicloalquilo inferior substituido o no substituido, fenilo substituido o no substituido o bencilo substituido o no substituido; o dos grupos R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros; o R8 y R9 pueden formar juntos un anillo heterocíclico de 5, 6, 7 u 8 miembros y cada R10 se selecciona independientemente de H, -S(=O)2R8, - S(=O)2NH2, -C(O)R8, -CN, -NO2, heteroarilo, o heteroalquilo; R5 es H, halogeno, alquilo C1-6 substituido o no substituido, O-alquilo C1-6 substituido o no substituido; R11 es L7-L10-G6; donde L7 es un enlace, -O, -S, -S(=O), -S(=O)2, -NH, -C(O), - C(O)NH, -NHC(O), alquilo C1-6 substituido o no substituido, o alquenilo C2-6 substituido o no substituido; L10 es un enlace, alquilo substituido o no substituido, cicloalquilo substituido o no substituido, cicloalquenilo substituido o no substituido, heteroarilo substituido o no substituido, arilo substituido o no substituido, o grupo heteroalicíclico substituido o no substituido; G6 es H, CN, SCN, N3, NO2, halogeno, OR9, -C(O)NHR9, -NHC(O)R9, -C(=O)CF3, -C(=O)R9, -SR8, -S(=O)R8, - S(=O)2R8, N(R9)2, -NHS(=O)2R8, -S(=O)2N(R9)2, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, -C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2; R12 es H, (alquilo C1-6 substituido o no substituido), (cicloalquilo C3-6 substituido o no substituido); o su metabolito activo, o solvato, o sal aceptable para uso farmacéutico, o profármaco aceptable para uso farmacéutico.
ARP060104861A 2005-11-04 2006-11-06 Derivados de indol como inhibidores de la proteina activadora de 5-lipoxigenasa (flap), composiciones farmaceuticas que los comprenden y su uso en el tratamiento de trastornos respiratorios e inflamatorios AR056215A1 (es)

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