AR066445A1 - Inhibidores de la proteina activadora de la 5- lipoxigenasa (flap) - Google Patents

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

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Publication number
AR066445A1
AR066445A1 ARP080101896A ARP080101896A AR066445A1 AR 066445 A1 AR066445 A1 AR 066445A1 AR P080101896 A ARP080101896 A AR P080101896A AR P080101896 A ARP080101896 A AR P080101896A AR 066445 A1 AR066445 A1 AR 066445A1
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Argentina
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substituted
unsubstituted
alkyl
nr9c
nhc
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ARP080101896A
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Amira Pharmaceuticals Inc
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Abstract

Reivindicacion 1: Un compuesto de formula (1), donde, Z es seleccionada de S(O)m, C(R1)2S(O)m, S(O)mC(R1)2, donde cada R1 es entre H, CF3, o un opcionalmente sustituido alquil C1-6; m es 0, 1 o 2; Y es un (sustituido o no-sustituido aril), o -(sustituido o no-sustituido heteroaril); R6 es H, L2-(sustituido o no-sustituido alquil), L2-(sustituido o no-sustituido cicloalquil), L2-(sustituido o no-sustituido alquenil), L2-(sustituido o no- sustituido cicloalquenil), L2-(sustituido o no-sustituido heterocicloalquil), L2-(sustituido o no-sustituido heteroaril), o L2-(sustituido o no-sustituido aril), donde L2 es un enlace, O, S, -S(=O), -S(=O)2, C(O), -CH(OH), -(sustituido o no-sustituido alquil C1-6), o -(sustituido o no-sustituidoalquenil C2-6); R7 es L3-X-L4-G1, donde, L3 es un sustituido o no-sustituido alquil; X es un enlace, O, -C(=O), -CR9(OR9), S, -S(=O), -S(=O)2, -NR9, -NR9C(=O)-, -C(O)NR9, -NR9C(O)NR9-; L4 es un enlace, un sustituido o no-sustituido alquiloramificado, un sustituido o no-sustituido alquilo de cadena recta, un sustituido o no-sustituido ciclo alquil, o un sustituido o no-sustituido heterocicloalquil; G1 es H, tetrazolil, -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(=CHR10)N(R9)2, -NR9C(=NR10)N(R9)C(=O)R9, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CHR10)N(R9)2, -CO2R9, -C(O)R9, -C(R9)2(OR9), -CON(R9)2, -SR8, -S(=O)R8, -S(=O)2R8, -L5-(sustituido o no-sustituido alquil), -L5-(sustituido o no-sustituido alquenil), -L5-(sustituido o no-sustituido heteroaril), o -L5-(sustituido o no-sustituido aril), donde L5 es -OC(O)O-, -NHC(O)NH-, -NHC(O)O, -OC(O)NH-, -NHC(O), -C(O)NH, -C(O)O, o -OC(O); o G1 es W-G5, donde W es un sustituido o no-sustituido aril, sustituido o no-sustituido heterocicloalquil sustituido o no-sustituido heteroaril y G5 es H, tetrazolil, -NHS(=O)2R8, S(=O)2N(R9)2, OH, -OR8, C(=O)CF3, -C(R9)2(OR9), -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(=CHR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -CO2R9, -C(O)R9, -CON(R9)2, -SR8, -S(=O)R8, o -S(=O)2R8, cada R8 es entreseleccionada de sustituido o no-sustituido alquil C1-6, sustituido o no-sustituido cicloalquil C3-8, sustituido o no-sustituido fenil o sustituido o no-sustituido benziI; cada R9 es seleccionada de H, sustituido o no-sustituido alquil C1-6,sustituido o no-sustituido fluoroalquil C1-6, sustituido o no-sustituido cicloalquil C3-8, sustituido o no-sustituido fenil, sustituido o no-sustituido benzil, y sustituido o no-sustituido heteroarilmetil; o dos grupos R9 pueden formar juntos un 5-,6-, 7-, u 8-membrado anillo heterocíclico; o R8 y R9 pueden juntos formar un 5-, 6-, 7-, u 8- membrado anillo heterocíclico y cada R10 es seleccionada de entre H -S(=O)2R8, -S(=O)2NH2, -C(O)R8, -CN, -NO2, heteroaril, o heteroalquil; R5 es H,halogeno, sustituido o no-sustituido alquil C1-6, sustituido o no-sustituido -O-alquil C1-6; R11 es L7-L10-G6, donde L7 es un enlace, -C(O), -C(O)NH, -NHC(O), o (sustituido o no-sustituido alquil C1-6); L10 es un enlace, (sustituido o no-sustituidoalquil), (sustituido o no-sustituido cicloalquil), (sustituido o no-sustituido heteroaril), (sustituido o no-sustituido aril), o (sustituido o no-sustituido heterocicloalquil); G6 es OR9, -C(=O)R9, -C(=O)OR9, -SR8, -S(=O)R8 -S(=O)2R8, N(R9)2,tetrazolil, -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(=CHR10)N(R9)2, -L5-(sustituido o no-sustituido alquil), -L5-(sustituido o no-sustituidoalquenil), -L5-(sustituido o no-sustituido heteroaril), o -L5-(sustituido o no- sustituido aril), 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, o -OC(O)-; o G6 es W-G7, donde Wes (sustituido o no-sustituido heterocicloalquil), (sustituido o no-sustituido aril) o un (sustituido o no-sustituido heteroaril) y G7 es H, halogeno, CN, NO2, N3, CF3, OCF3, alquil C1-6, cicloalquil C3-6, fluoroalquil C1-6, tetrazolil, -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(=CHR10)N(R9)2, -C(O)NR9C(=NR10)N(R9)2, -C(O)NR9C(=CHR10)N(R9)2, -CO2R9, -C(O)R9, -C(R9)2(OR9), -CON(R9)2, -SR8,-S(=O)R8 o -S(=O)2R8, -L5-(sustituido o no-sustituido alquil), -L5-(sustituido o no-sustituido alquenil), -5-(sustituido o no-sustituido heteroalquil), -5-(sustituido o no-sustituido heteroaril), -5-(sustituido o no-sustituido heterocicloalquil), o -5-(sustituido o no-sustituido aril), donde L5 es un enlace, -O-, C(=O), S, S(=O), S(=O)2, -H, -NHC(O)O, -NHC(O)NH-, -OC(O)O-, -OC(O)NH-, -NHC(O), -C(O)NH, -C(O)O, o -OC(O); provisto que R11 comprende al menos una (no-sustituida o sustituida) mitadaromática y al menos una (no-sustituida o sustituida) mitad cíclica, donde la (no - sustituida o sustituida) mitad cíclica es un (no-sustituido o sustituido) grupo heterocicloalquil o un (no-sustituido o sustituido) grupo heteroaril y R11 no es ungrupo tienil-fenil; y R12 es H, (sustituido o no-sustituido alquil C1-6), (sustituido o no-sustituido cicloalquil C3-6); o un metabolito glucuronido, farmacéuticamente aceptable solvato, farmacéuticamente aceptable sal, o farmacéuticamente aceptableprodroga de estos.
ARP080101896A 2007-05-08 2008-05-05 Inhibidores de la proteina activadora de la 5- lipoxigenasa (flap) AR066445A1 (es)

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US11/746,010 US20070225285A1 (en) 2005-11-04 2007-05-08 5-lipoxygenase-activating protein (flap) inhibitors

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AR066445A1 true AR066445A1 (es) 2009-08-19

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US (1) US20070225285A1 (es)
EP (1) EP2144874A4 (es)
JP (1) JP2010526818A (es)
AR (1) AR066445A1 (es)
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UY31073A1 (es) 2009-01-05
US20070225285A1 (en) 2007-09-27
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CL2008001304A1 (es) 2008-09-22
EP2144874A1 (en) 2010-01-20

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