AR112233A1 - Aminas cíclicas de 6 miembros o lactamas sustituidas con urea y fenilo como moduladores del fpr2 - Google Patents

Aminas cíclicas de 6 miembros o lactamas sustituidas con urea y fenilo como moduladores del fpr2

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Publication number
AR112233A1
AR112233A1 ARP170102602A AR112233A1 AR 112233 A1 AR112233 A1 AR 112233A1 AR P170102602 A ARP170102602 A AR P170102602A AR 112233 A1 AR112233 A1 AR 112233A1
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Argentina
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alkyl
cycloalkyl
membered
alkylene
heteroaryl
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Dunkern Torsten Dr
Bahrenberg Gregor Dr
Wagener Markus Dr
Rider David Dr
Nordhoff Sonja Dr
Jakob Florian Dr
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Gruenenthal Gmbh
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Abstract

Este compuesto actúa como un modulador de FPR2 y se puede usar en el tratamiento y/o la prevención de trastornos que están al menos parcialmente mediados por FPR2. Reivindicación 1: Un compuesto de acuerdo con la fórmula general (1) caracterizado porque: X² representa N(L-R⁴) y X¹, X³ y X⁴ representan CH₂; o X² representa N(L-R⁴) y X³ representa C(O) y X¹ y X⁴ representan CH₂; o X⁴ representa N(L-R⁴) y X³ representa CH₂ o C(O) y X¹ y X² representan CH₂; y n representa 0, 1 ó 2; R¹ representa fenilo o heteroarilo de 5 ó 6 miembros; R² representa H, F, Cl, Br, CN, alquilo C₁₋₆, cicloalquilo C₃₋₆, CHF₂, CH₂F, CF₃, OH, OCHF₂, OCH₂F, OCF₃, O-alquilo C₁₋₆, S-alquilo C₁₋₆, S(O)-alquilo C₁₋₆, S(O)₂-alquilo C₁₋₆, O-cicloalquilo C₃₋₆, S-cicloalquilo C₃₋₆, S(O)-cicloalquilo C₃₋₆, S(O)₂-cicloalquilo C₃₋₆, NH₂, N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, N(H)(cicloalquilo C₃₋₆), N(alquilo C₁₋₆)(cicloalquilo C₃₋₆), NC(O)(alquilo C₁₋₆), NC(O)(cicloalquilo C₃₋₆), NC(O)(heterocicloalquilo de 3 a 6 miembros); R³ representa F, Cl, Br, CHF₂, CH₂F, CF₃, alquilo C₁₋₆, cicloalquilo C₃₋₆, O-alquilo C₁₋₆, OCHF₂, OCH₂F, OCF₃, S(O)-alquilo C₁₋₆, S(O)-cicloalquilo C₃₋₆, S(O)₂-alquilo C₁₋₆, S(O)₂-cicloalquilo C₃₋₆; L representa enlace, alquileno C₁₋₆, C₍O₎, S₍O₎₂, C₍CH₃)₂; y R⁴ representa H, alquilo C₁₋₆, cicloalquilo C₃₋₆, heterocicloalquilo 3 a 6 miembros, arilo, heteroarilo de 5 ó 6 miembros, C(O)NH₂, C(O)N(H)(alquilo C₁₋₆), C(O)N(alquilo C₁₋₆)₂, C(O)N(H)(cicloalquilo C₃₋₆), C(O)N(H)(heterocicloalquilo de 3 a 6 miembros), C(O)N(H)(arilo), C(O)N(H)(heteroarilo de 5 ó 6 miembros), C(O)N(alquilo C₁₋₆)(cicloalquilo C₃₋₆), C(O)N(alquilo C₁₋₆)(heterocicloalquilo de 3 a 6 miembros), C(O)N(alquilo C₁₋₆)(arilo), C(O)N(alquilo C₁₋₆)(heteroarilo de 5 ó 6 miembros), C(O)N(cicloalquil C₃₋₆)(cicloalquilo C₃₋₆), C(O)N(cicloalquil C₃₋₆)(heterocicloalquilo de 3 a 6 miembros), C(O)N(cicloalquil C₃₋₆)(arilo), C(O)N(cicloalquil C₃₋₆)(heteroarilo de 5 ó 6 miembros), C(O)O-(alquilo C₁₋₆), C(O)O-(cicloalquilo C₃₋₆), C(O)O-(heterocicloalquilo de 3 a 6 miembros), C(O)O-(arilo), C(O)O-(heteroarilo de 5 ó 6 miembros), S(O)-alquilo C₁₋₆, S(O)₂-alquilo C₁₋₆, S(O)-cicloalquilo C₃₋₆, S(O)₂-cicloalquilo C₃₋₆, alquilen C₁₋₆-OH, alquilen C₁₋₆-O-alquilo C₁₋₆, alquilen C₁₋₆-cicloalquilo C₃₋₆, alquilen C₁₋₆-heterocicloalquilo 3 a 6 miembros, alquilen C₁₋₆-arilo, alquilen C₁₋₆-heteroarilo de 5 ó 6 miembros; en donde alquilo C₁₋₆ en cada caso de modo independiente entre sí es lineal o ramificado, saturado o insaturado; en donde alquileno C₁₋₆ es lineal y saturado o insaturado; en donde alquilo C₁₋₆, alquileno C₁₋₆, cicloalquilo C₃₋₆ y heterocicloalquilo de 3 a 6 miembros en cada caso de modo independiente entre si no están sustituidos o están mono- o polisustituidos con uno o varios sustituyentes seleccionados de F, Cl, CN, alquilo C₁₋₆, CF₃, CF₂H, CFH₂, CF₂Cl, CFCl₂, C(O)-alquilo C₁₋₆, C₍O₎₋OH, C₍O₎₋O₋ₐₗqᵘⁱₗₒ C₁₋₆, C₍O₎₋NH₂, C(O)-N(H)(alquilo C₁₋₆), C(O)-N(alquilo C₁₋₆)₂, OH, =O, OCF₃, OCF₂H, OCFH₂, OCF₂Cl, OCFCl₂, O-alquilo C₁₋₆, O-C(O)-alquilo C₁₋₆, O-C(O)-O-alquilo C₁₋₆, O-(CO)-N(H)(alquilo C₁₋₆), O-C(O)-N(alquilo C₁₋₆)₂, O-S(O)₂-NH₂, O-S(O)₂-N(H)(alquilo C₁₋₆), O-S(O)₂-N(alquilo C₁₋₆)₂, NH₂, N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, N(H)-C(O)-alquilo C₁₋₆, N(H)-C(O)-O-alquilo C₁₋₆, N(H)-C(O)-NH₂, N(H)-C(O)-N(H)(alquilo C₁₋₆), N(H)-C(O)-N(alquilo C₁₋₆)₂, N(alquilo C₁₋₆)-C(O)-alquilo C₁₋₆, N(alquilo C₁₋₆)-C(O)-O-alquilo C₁₋₆, N(alquilo C₁₋₆)-C(O)-NH₂, N(alquilo C₁₋₆)-C(O)-N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)-C(O)-N(alquilo C₁₋₆)₂, N(H)-S(O)₂OH, N(H)-S(O)₂-alquilo C₁₋₆, N(H)-S(O)₂-O-alquilo C₁₋₆, N(H)-S(O)₂-NH₂, N(H)-S(O)₂-N(H)(alquilo C₁₋₆), N(H)-S(O)₂N(alquilo C₁₋₆)₂, N(alquilo C₁₋₆)-S(O)₂-OH, N(alquilo C₁₋₆)-S(O)₂-alquilo C₁₋₆, N(alquilo C₁₋₆)-S(O)₂-O-alquilo C₁₋₆, N(alquilo C₁₋₆)-S(O)₂-NH₂, N(alquilo C₁₋₆)-S(O)₂-N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)-S(O)₂-N(alquilo C₁₋₆)₂, SCF₃, SCF₂H, SCFH₂, S-alquilo C₁₋₆, S(O)-alquilo C₁₋₆, S(O)₂-alquilo C₁₋₆, S(O)₂-OH, S(O)₂-O-alquilo C₁₋₆, S(O)₂-NH₂, S(O)₂-N(H)(alquilo C₁₋₆), S(O)₂-N(alquilo C₁₋₆)₂, cicloalquilo C₃₋₆, heterocicloalquilo 3 a 6 miembros, fenilo, heteroarilo de 5 ó 6 miembros, O-cicloalquilo C₃₋₆, O-(heterocicloalquilo de 3 a 6 miembros), O-fenilo, O-(heteroarilo de 5 ó 6 miembros), C(O)-cicloalquilo C₃₋₆, C₍O₎₋₍ₕₑₜₑʳₒᶜⁱᶜₗₒₐₗqᵘⁱₗₒ ᵈₑ ₃ ₐ ₆ ₘⁱₑₘᵇʳₒₛ₎, C₍O₎₋ᶠₑₙⁱₗₒ, C₍O₎₋₍ₕₑₜₑʳₒₐʳⁱₗₒ ᵈₑ ₅ ó ₆ ₘⁱₑₘᵇʳₒₛ₎, S₍O₎₂-(cicloalquilo C₃₋₆), S(O)₂-(heterocicloalquilo de 3 a 6 miembros), S(O)₂-fenilo o S(O)₂-(heteroarilo de 5 ó 6 miembros); en donde arilo, fenilo y heteroarilo de 5 ó 6 miembros en cada caso de modo independiente entre si no están sustituidos o están mono- o disustituidos con uno o dos sustituyentes seleccionados de F, Cl, Br, CN, alquilo C₁₋₆, CF₃, CF₂H, CFH₂, alquilen C₁₋₄-CF₃, alquilen C₁₋₄-CF₂H, alquilen C₁₋₄-CFH₂, C(O)-alquilo C₁₋₆, C₍O₎₋OH, C₍O₎₋O₋ₐₗqᵘⁱₗₒ C₁₋₆, C₍O₎₋N₍H₎₍OH₎, C₍O₎₋NH₂, C(O)-N(H)(alquilo C₁₋₆), C(O)-N(alquilo C₁₋₆)₂, OH, OCF₃, OCF₂H, OCFH₂, OCF₂Cl, OCFCl₂, O-alquilo C₁₋₆, O-cicloalquilo C₃₋₆, O-(heterocicloalquilo de 3 a 6 miembros), O-fenilo, O-(heteroarilo de 5 ó 6 miembros), NH₂, N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)₂, N(H)-C(O)-alquilo C₁₋₆, N(alquilo C₁₋₆)-C(O)-alquilo C₁₋₆, N(H)-C(O)-NH₂, N(H)-C(O)-N(H)(alquilo C₁₋₆), N(H)-C(O)-N(alquilo C₁₋₆)₂, N(alquilo C₁₋₆)-C(O)-N(H)(alquilo C₁₋₆), N(alquilo C₁₋₆)-C(O)-N(alquilo C₁₋₆)₂, N(H)-S(O)₂-alquilo C₁₋₆, SCF₃, S-alquilo C₁₋₆, S(O)-alquilo C₁₋₆, S(O)₂-alquilo C₁₋₆, S(O)₂-NH₂, S(O)₂-N(H)(alquilo C₁₋₆), S(O)₂-N(alquilo C₁₋₆)₂, cicloalquilo C₃₋₆, alquilen C₁₋₄-cicloalquilo C₃₋₆, heterocicloalquilo 3 a 6 miembros, alquilen C₁₋₄-(heterocicloalquilo de 3 a 6 miembros), fenilo o heteroarilo de 5 ó 6 miembros; en forma del compuesto libre o una de sus sales fisiológicamente aceptables.
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