AR057872A1 - Inhibidores de la proteina activadora de 5-lipoxigenasa (flap) - Google Patents

Inhibidores de la proteina activadora de 5-lipoxigenasa (flap)

Info

Publication number
AR057872A1
AR057872A1 ARP060104837A ARP060104837A AR057872A1 AR 057872 A1 AR057872 A1 AR 057872A1 AR P060104837 A ARP060104837 A AR P060104837A AR P060104837 A ARP060104837 A AR P060104837A AR 057872 A1 AR057872 A1 AR 057872A1
Authority
AR
Argentina
Prior art keywords
substituted
unsubstituted
nr9c
alkyl
nhc
Prior art date
Application number
ARP060104837A
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=AR057872(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 AR057872A1 publication Critical patent/AR057872A1/es

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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • 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
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
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    • C07—ORGANIC CHEMISTRY
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    • C07D417/00—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
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    • 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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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). Estos compuestos son utiles 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 [C(R1)2]m[C(R2)2]n, [C(R2)2]n[C(R1)2]mO, O[C(R1)2]m[C(R2)2]n, [C(R2)2]nO[C(R1)2]n o [C(R1)2]nO[C(R2)2]n, donde cada R1 es independientemente H, CF3, o un alquilo inferior opcionalmente sustituido 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 sustituido 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 o -(arilo sustituido o no sustituido); o -(heteroarilo sustituido o no sustituido); donde cada sustituyente en Y o Z es (LsRs)j, donde cada Ls se selecciona independientemente en 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 sustituido o no sustituido, alquenilo C2-6, fluoroalquilo -C1-6, heteroarilo sustituido o no sustituido, arilo sustituido o no sustituido, o heterociclo sustituido o no sustituido; y cada Rs se selecciona independientemente de H, halogeno, -N(R4)2, -CN, -NO2, N3, -S(=O)2NH2, alquilo inferior sustituido o no sustituido, cicloalquilo inferior sustituido o no sustituido, fluoroalquilo C1-C6, arilo sustituido o no sustituido, heteroarilo sustituido o no sustituido, o heteroalquilo sustituido o no sustituido; donde j es 0, 1, 2, 3 o 4; R6 es H, L2-(alquilo sustituido o no sustituido, L2-(cicloalquilo sustituido o no sustituido), L2-(alquenilo sustituido o no sustituido, L2-(cicloalquenilo sustituido o no sustituido), L2-(heterociclo sustituido o no sustituido, L2-(heteroarilo sustituido o no sustituido), o L2-(arilo sustituido o no sustituido), donde L2 es un enlace, O, S, -S(=O), C(O), -CH(OH), - (alquilo C1-6 sustituido o no sustituido), o -(alquenilo C2-6sustituido o no sustituido); R7 es L3-X-L4-G1, donde, L3 es a alquilo sustituido o no sustituido; X es un enlace, O, -C(=O), -CR9(OR9), S, -S(=O)2, -NR9, -NR9C(O), -C(O)NR9, -NR9C(O)NR9-; L4 es un enlace, o un alquilo sustituido o no sustituido; G1 es H, tetrazolilo, NHS(=O)2R8, S(=O)2N(R9)2, -OR9, -C(=O)CF3, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, 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 sustituido o no sustituido), -L5-(alquenilo sustituido o no sustituido), -L5-(heteroarilo sustituido o no sustituido), o -L5-(arilo sustituido o no sustituido), 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 G1 es W-G5, donde W es un arilo sustituido o no sustituido, heterociclo sustituido o no sustituido o heteroarilo sustituido o no sustituido y G5 es H, tetrazolilo, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, 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, o -S(=O)2R8; cada R8 se selecciona independientemente de alquilo inferior sustituido o no sustituido, cicloalquilo inferior sustituido o no sustituido, fenilo sustituido o no sustituido o bencilo sustituido o no sustituido; cada R9 se selecciona independientemente de H, alquilo inferior sustitutido o no sustituido, cicloalquilo inferior sustituido o no sustituido, fenilo sustituido o no sustituido o bencilo sustituido o no sustituido; 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 C1-6sustituido o no sustituido, O-alquilo C1-6sustituido o no sustituido; R11 es L7-L10-G6, donde L7 es un enlace, -C(O), -C(O)NH, -NHC(O), o (alquilo C1-6sustituido o no sustituido); L10 es un enlace, (alquilo sustituido o no sustituido), (cicloalquilo sustituido o no sustituido), (heteroarilo sustituido o no sustituido), (arilo sustituido o no sustituido), o (heterociclo sustituido o no sustituido); G6 es OR9, -C(=O)R9, -SR8, -S(=O)R8, - S(=O)2R8, N(R9)2, tetrazolilo, -NHS(=O)2R8, -S(=O)2N(R9)2, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, -C(=O)N(R9)2, NR9C(O)R9, C(R9)2C(=O)N(R9)2-C(=NR10)N(R9)2, -NR9C(=NR10)N(R9)2, -NR9C(=CR10)N(R9)2, -L5-(alquilo sustituido o no sustituido), -L5-(alquenilo sustituido o no sustituido), -L5-(heteroarilo sustituido o no sustituido), o -L5-(arilo sustituido o no sustituido), donde L5 es -O-, C(=O), S, S(=O), S(=O)2, -NH, -NHC(O)O, -NHC(O)NH-, -OC(O)O-, -OC(O)NH-, -NHC(O), -C(O)NH, -C(O)O u -OC(O) o G6 es W-G7, donde W es (heterociclo sustituido o no sustituido), (arilo sustituido o no sustituido) o un (heteroarilo sustituido o no sustituido) y G7 es H, halogeno, CN, NO2, N3, CF3, OCF3, C1-6 alquilo, C3-6 cicloalquilo, fluoroalquilo C1-6, tetrazolilo, NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, -C(=O)CF3, -C(O)NHS(=O)2R8, -S(=O)2NHC(O)R9, 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, o -S(=O)2R8, -L5-(alquilo sustituido o no sustituido), -L5-(alquenilo sustituido o no sustituido), -L5-(heteroalquilo sustituido o no sustituido), -L5-(heteroarilo sustituido o no sustituido), -L5-(heterociclo sustituido o no sustituido), o -L5-(arilo sustituido o no sustituido), donde L5 es un enlace, -O-, C(=O), S, S(=O), S(=O)2, -NH, -NHC(O)O, NHC(O)NH-, -OC(O)O-, .OC(O)NH, -C(O)NH, -C(O)O u -OC(O); con la salvedad de que R11 comprende almenos un resto aromático (no sustituido o sustituido) y al menos un resto cíclico (no sustituido o sustituido), donde el resto cíclico (no sustituido o sustituido) es un grupo heterocíclico (no sustituido o sustituido) o un grupo heteroarilo (no sustituido o sustituido) y R11 no es un grupo tienil-fenilo; R12 es H, (alquilo C1-6sustituido o no sustituido), (cicloalquilo C3-6 sustituido o no sustituido); o su metabolito activo, o solvato, o sal aceptable para uso farmacéutico, o profármaco aceptable para uso farmacéutico.
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