AR054224A1 - Piperazin- piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3 - Google Patents

Piperazin- piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3

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Publication number
AR054224A1
AR054224A1 AR20060100549A ARP060100549A AR054224A1 AR 054224 A1 AR054224 A1 AR 054224A1 AR 20060100549 A AR20060100549 A AR 20060100549A AR P060100549 A ARP060100549 A AR P060100549A AR 054224 A1 AR054224 A1 AR 054224A1
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Argentina
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alkyl
cycloalkyl
aryl
alkylaryl
heterocyclyl
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AR20060100549A
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Schering Corp
Pharmacopeia Drug Discovery
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
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Abstract

La presente describe un compuesto o enantiomeros, estereoisomeros, rotámeros, tautomeros, racematos o un profármaco de dicho compuesto o sales aceptables para uso farmacéutico. También se describe un método para tratar enfermedades mediadas por quimiocinas, tales como terapia paliativa, terapia curativa, terapia profiláctica de ciertas enfermedades y afecciones tales como enfermedades inflamatorias (ejemplo(s) no limitativo(s) incluye(n), psoriasis), enfermedades autoinmunes (ejemplo(s) no limitativo(s) incluye(n), artritis reumatoidea, esclerosis multiple). Reivindicacion 1: Un compuesto que posee la estructura general de Formula (1); o sales aceptables para uso farmacéutico, solvatos o ésteres de los mismos, donde: X es N, O, alquilo, cicloalquilo, heteroarilo, heterociclilo o heterociclenilo; el anillo D es un anillo fenilo no sustituido o sustituido opcionalmente por restos R20 seleccionados independientemente segun se indica a continuacion; R1 y R2 se encuentran ausentes o presentes de manera Independiente, y si se encuentran presentes, cada uno se selecciona independientemente del grupo que consiste en H, alquilo, alcoxi, alquenilo, carbonilo, cicloalquilo, alquilcicloalquilo-, cicloalquenilo, alquilarilo, arilalquilo, arilo, amino, alquilamino, amidinilo, carboxamido, ciano, hidroxilo, urea, -NsCH, =NCN, -(CH2)qOH, (CH2)qOR31, (CH2)qNH2, (CH2)qNHR31, (CH2)qN(R31)2, (CH2)qC(=O)NHR31, (CH2)qSO2R31, (CH2)qNHSO2R31, (CH2)qSO2NHR31, -C(=S)N(H)alquilo, - N(H)-S(O)2-alquilo, -N(H)C(=O)N(H)-alquilo, -S(O)2-alquilo, -S(O)2N(H)-alquilo, -S(O)2N(alquilo)2, -S(O)2-arilo, -C(=S)N(H)-cicloalquilo, -C(=O)N(H)NH2, -C(=O)-alquilo, -heteroarilo, heterociclilo y heterociclenilo; o de manera alternativa cuando X es N, el N tomado junto con el R1 y R2 forma un heterociclilo, heteroarilo o -N=C(NH2)2; R3 y R6 restos pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquilarilo, aralquilo, -CN, CF3, haloalquilo, cicloalquilo, halogeno, hidroxialquilo, -N=CH-(R31), -C(O)N(R30)2, -N(R30)2, -OR30, -SO2(R31), -N(R30)C(=O)N(R30)2 y -N(R30)C(=O)R31; R7 y R8, son iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquilarilo, heteroarilo, hidroxilo, -CN, alcoxi, alquilamino, -N(H)S(O)2-alquilo y -N(H)C(=O)N(H)-alquilo; o de manera alternativa R7 y R8 tomados juntos son =O, S, =NH, =N(alquilo), =N(O-alquilo), =N(OH) o cicloalquilo; los restos R10 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, cicloalquilo, arilo, heteroarilo, heterociclenilo, heterociclilo, alquilarilo, arilalquilo, -CO2H, hidroxialquilo, - C(=O)N(R30)2, -(CH2)qOH, -(CH2)qOR31, -(CH2)qNHR31, (CH2)qN(R31)2, -OR30, halogeno, =O y -C(=O)R31; los restos R11 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, cicloalquilo, arilo, heteroarilo, heterociclilo, heterociclenilo, alquilarilo, arilalquilo, hidroxialquilo, carboxamida, CO2H, (CH2)qOH, (CH2)qOR31, (CH2)qNHR31, (CH2)qN(R31)2, -OR30, halogeno, =O y -C(=O)R31; R12 se selecciona del grupo que consiste en H, alquilo, -CN, -C(=O)N(R30)2, -(CH2)qOH, -(CH2)qOR31, (CH2)qNHR31, (CH2)qN(R31)2 y -S(O2)R31; los restos R20 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquenilo, alquilarilo, alquinilo, alcoxi, alquilamino, alquiltiocarboxi, alquilheteroarilo, alquiltio, alquilsulfinilo, alquilsulfonilo, alcoxicarbonilo, aminoalquilo, amidinilo, aralquilo, aralquenilo, aralcoxi, aralcoxicarbonilo, aralquiltio, arilo, aroilo, ariloxi, ciano, cicloalquilo, cicloalquenilo, formilo, guanidinilo, halogeno, haloalquilo, heteroalquilo, heteroarilo, heterociclilo, heterociclenilo, hidroxialquilo, haloalcoxi, hidroxamato, nitro, trifluorometilo, trifluorometoxi, -(CH2)qOH, -(CH2)qOR31, (CH2)qNH2, (CH2)qNHR31, (CH2)qN(R31)2, (CH2)qC(=O)NHR31, (CH2)qSO2R31, (CH2)qNHSO2R31, (CH2)qSO2NHR31, -alquinilo C(R31)2OR31, -C(=O)R30, -C(=O)NR(30)2, -C(=NR30)NHR30, -C(=NOH)N(R30)2, -C(=NOR31)N(R30)2, -C(=O)OR30, -N(R30)2, -N(R30)C(=O)R31, - NHC(=O)N(R30)2, -N(R30)C(=O)OR31, -N(R30)C(=NCN)N(R30)2, -N(R30)C(=O)N(R30)SO2(R31), -N(R30)C(=O)N(R30)2, -N(R30)SO2(R31), -N(R30)S(O)2N(R30)2, -OR30, -OC(=O)N(R30)2, -SR30, .SO2N(R30)2, SO2(R31), -OSO2(R31), O(CH2)qSO2R31 y -OSi(R30)3 o de manera alternativa dos R20 restos se unen para formar un anillo arilo, cicloalquilo, heterociclilo, heterociclenilo o heteroarilo de cinco o seis miembros donde dicho anillo arilo, cicloalquilo, heterociclilo, heterociclenilo o heteroarilo de cinco o seis miembros se fusiona al anillo D y el anillo fusionado se sustituye opcionalmente con 0-4 restos R21; los restos R21 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquenilo, alquilarilo, alquinilo, alcoxi, alquilamino, alquiltiocarboxi, alquilheteroarilo, alquiltio, alquilsulfinilo, alquilsulfonilo, alcoxicarbonilo, aminoalquilo, amidinilo, aralquilo, aralquenilo, aralcoxi, aralcoxicarbonilo, aralquiltio, arilo, aroilo, ariloxi, carboxamido, ciano, cicloalquilo, cicloalquenilo, formilo, guanidinilo, halogeno, haloalquilo, heteroalquilo, heteroarilo, heterociclilo, heterociclenilo, hidroxialquilo, hidroxamato, nitro, trifluorometoxi, -(CH2)qOH, -(CH2)qOR31, - (CH2)qNH2, -(CH2)qNHR31, -(CH2)qN(R31)2, -(CH2)C(=O)NHR31, (CH2)qSO2R31, -(CH2)qNSO2R31, -(CH2)qSO2NHR31, -alquinilo C(R31)2OR31, -C(=O)R30, -C(=O)N(R30)2, -C(=NR30)NHR30, -C(=NOH)N(R30)2, -C(=NOR31)N(R30)2, -C(=O)OR30, -N(R30)2, -N(R30)C(=O)R31, - NHC(=O)N(R30)2, -N(R30)C(=O)OR31, -N(R30)C(=NCN)N(R30)2, -N(R30)C(=O)N(R30)SO2(R31), -N(R30)C(=O)N(R30)2, -N(R30)SO2(R31), -N(R30)S(O)2N(R30)2, -OR30, -OC(=O)N(R30)2, -SR30, -SO2N(R30)2, -SO2(R31), -OSO2(R31) y -OSi(R30)3; Y se selecciona del grupo que consiste en -(CR13R13)r-, -CHR13C(=O)-, -(CHR13)rO-, (CHR13)rN(R30)-, -C(=O)-, -C(=NR30)-, -C(=N-OR30)-, -CH(C(=O)NHR30)-, CH-heteroarilo-, -C(R13R13)rC(R13)=C(R13)-, -(CHR13)rC(=O)- y -(CHR13)rN(H)C(=O)-; o de manera alternativa Y es cicloalquilo, heterociclenilo, o heterociclilo donde el cicloalquilo, heterociclenilo o heterociclilo se fusiona con el anillo fenilo con marca D; los restos R13 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo. alquilarilo, cicloalquilo, alcoxi, arilo, heteroarilo, heterociclenilo, heterociclilo, espiroalquilo, -CN, -CO2H, -C(=O)R30, -C(=O)OR31, -C(=O)N(R30)2, -(CHR30)qOH, -(CHR30)qOR31, -(CHR30)qNH2, -(CHR30)qNHR31, - (CH2)qC(=O)NHR31, -(CH2)qSO2R31, -(CH2)qNSO2R31, -(CH2)qSO2NHR31, -NH2, -N(R30)2, -N(R30)C(=O)N(R30)2, -N(R30)SO2(R31), -OH, OR30 , -SO2N(R30)2 y -SO2(R31); los restos R30 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en H, alquilo, alquilarilo, arilo, aralquilo, cicloalquilo, CN, -(CH2)qOH, -(CH2)qO-alquilo, -(CH2)qO-alquilarilo, (CH2)qO-arilo, -(CH2)qO-aralquilo, -(CH2)qO-cicloalquilo, (CH2)qNH2, (CH2)qNH-alquilo, -(CH2)qN(alquilo)2, - (CH2)qNH-alquilarilo, -(CH2)qNH-arilo, (CH2)qNH-aralquilo, -(CH2)qNH-cicloalquilo, -(CH2)qC(=O)NH-alquilo, (CH2)qC(=O)N(alquilo)2, -(CH2)qC(=O)NH-alquilarilo, -(CH2)qC(=O)NH-arilo, (CH2)qC(=O)NH-aralquilo, -(CH2)qC(=O)NH-cicloalquilo, -(CH2)qSO2- alquilo, -(CH2)SO2-alquilarilo, -(CH2)qSO2-arilo, -(CH2)qSO2-aralquilo, (CH2)qSO2-cicloalquilo, -(CH2)qNSO2-alquilo, -(CH2)qNSO2-alquilarilo, (CH2)qNSO2-arilo, -(CH2)qNSO2-aralquilo, -(CH2)qNSO2-cicloalquilo, -(CH2)qSO2NH-alquilo, -(CH2)qSO2NH- alquilarilo, -(CH2)qSO2NH-arilo, (CH2)qSO2NH-aralquilo, -(CH2)qSO2NH-cicloalquiIo, heterociclenilo, heterociclilo y heteroarilo; los restos R31 pueden ser iguales o diferentes, seleccionándose cada uno independientemente del grupo que consiste en alquilo, alquilarilo, arilo, aralquilo, cicloalquilo, -(CH2)qOH, -(CH2)qO-alquilo, -(CH2)qO-alquilarilo, -(CH2)qO-arilo, -(CH2)qO-aralquilo, -(CH2)qO-cicloalquilo, -(CH2)qNH2, -(CH2)qNH-alquiIo, (CH2)qN(alquilo)2, -(CH2)qNH-alquilarilo, -(CH2)qNH- arilo, (CH2)qNH-aralquilo, (CH2)qNH-cicloalquilo, -(CH2)qC(=O)NH-alquilo, -(CH2)qC(=O)N(alquilo)2, -(CH2)qC(=O)NH-alquilarilo, -(CH2)qC(=O)NH-arilo, -(CH2)qC(=O)NH-aralquilo, -(CH2)qC(=O)NH-cicloalquilo, -(CH2)qSO2-alquilo, (CH2)qSO2-alquilarilo, - (CH2)qSO2-arilo, -(CH2)qSO2-aralquilo, (CH2)qSO2-cicloalquilo, -(CH2)qNSO2-alquilo, -(CH2)qNSO2-alquilarilo, -(CH2)qNSO2-arilo, -(CH2)qNsO2-aralquilo, -(CH2)qNSO2-cicloalquilo, -(CH2)qSO2NH-alquilo, -(CH2)qSO2NH-alquilarilo. (CH2)qSO2NH-arilo, (CH2)qSO2NH-aralquilo, (CH2)qSO2NH-cicloalquilo, heterociclenilo, heterociclilo y heteroarilo; m es 0 a 4; n es 0 a 4; p es 0 a 5; cada q puede ser igual o diferente, seleccionándose cada uno independientemente de 1 a 5; y r es 1 a 4; con la salvedad de que no haya dos dobles enlaces adyacentes en ningun anillo y que cuando se sustituye un nitrogeno con dos grupos alquilo, dichos dos grupos alquilo se puedan unir opcionalmente entre si para formar un anillo.
AR20060100549A 2005-02-16 2006-02-15 Piperazin- piperidinas sustituidas con pirazinilo con actividad antagonista de cxcr3 AR054224A1 (es)

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EP1856098A2 (en) 2007-11-21
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EP1856098B1 (en) 2012-08-01
RU2007134260A (ru) 2009-03-27
ZA200706789B (en) 2008-11-26
CA2598458A1 (en) 2006-08-24
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BRPI0607946A2 (pt) 2009-10-20
CN101142209A (zh) 2008-03-12
PE20061164A1 (es) 2006-10-27
IL185073A0 (en) 2007-12-03
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WO2006088921A3 (en) 2006-11-02
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