AR054522A1 - Moduladores lxr basados en pirazol - Google Patents
Moduladores lxr basados en pirazolInfo
- Publication number
- AR054522A1 AR054522A1 ARP060102762A ARP060102762A AR054522A1 AR 054522 A1 AR054522 A1 AR 054522A1 AR P060102762 A ARP060102762 A AR P060102762A AR P060102762 A ARP060102762 A AR P060102762A AR 054522 A1 AR054522 A1 AR 054522A1
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- AR
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- Prior art keywords
- alkyl
- aryl
- cycloalkyl
- heteroaryl
- independently
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Abstract
Se describen composiciones farmacéuticas que contienen los compuestos, así como los métodos de utilizacion de dichos compuestos. Reivindicacion 1: Un compuesto de acuerdo con una de las formulas (1) a (4), o una sal, isomero o profármaco farmacéuticamente aceptable del mismo, en donde, A) R1 representa -L1-R5, en donde: L1 es un union, L5, L6, -L5-L6-L5-, o -L6-L5-L6-, en donde: cada L5 es independientemente -[C(R15)2]m-, donde, cada R15 es independientemente hidrogeno, halogeno, alquilo C1-6, o haloalquilo C1-6; cada L6 es independientemente -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, -NR11-, -N(R10)CO-, - N(R10)CO2-, -CON(R10)-, -CO-, -CS-, -CO2-, -OC(=O)-, -OC(=O)N(R10)-, - CONR11N(R11)2-, -CONR11-, -OCONR11-, -SO2-, -N(R10)SO2-, - SO2N(R10), -NR10CONR10-, -NR10CSNR10-, -C(=NR11)-, -C(=NOR11)-, -C(=NN(R1)2)-, arilo-, cicloalquilo C3-8, ciclo-haloalquiloC3-8, heteroarilo, heterociclilo, donde el arilo, cicloalquilo, ciclo-haloalquiloC3-8, heteroarilo, o heterociclilo son opcionalmente sustituidos con uno o más radicales de R14; o L1 representa una cadena de alidiilo C2-6 donde la cadena de alidiilo es opcionalmente interrumpida por -C(R11)2-, - C(R11)2C(R11)2-, - C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO-, -CO2-, - OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o -SO2N(R10)-; R5 representa arilo, heterociclilo, heteroarilo, alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6, cicloalquilo C3-8, -C, -B-C, -A-B-C, donde, a representa -O-; B representa -[C(R15)2]m- o cicloalquilo C3-8; C representa alquilo C1-6, haloalquilo C1-6, -SO2R11, -SR11, -SO2N(R11)2, - SO2NR11COR11, -C:::N, C(O)OR11, CON(R11)2 o N(R11)2, donde R5 es opcionalmente sustituido con uno o más R5a, en donde cada R5a es independientemente alquilo C1-6, haloalquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquiniloC3-8-alquiloC1-6-, cicloalqueniloC3-8- alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6-, halogeno, nitro, heterocicli-oxi, arilo, ariloxi, arilalquilo, ariloxiarilo, aril-alcoxiC1-6, -C', -B-C', o - A'-B'-C' en donde A' es -O-; B representa -[C(R15)2]m- o cicloalquilo C3-8-; C' es -H, halogeno, -SO2R11, -OR11, -SR11, -N3, -COR11, - SO2N(R11)2, -SO2NR11COR11, -C:::N, -C(O)OR11, -OC(=O)R11, -CON(R11)2, -CON(R11)OR11, -OCON(R11)2, -NR11COR11, -NR11CON(R11) 2, -NR11COOR11, -N(R11)2, arilo, heteroarilo, o heterociclilo; en donde cada R5 se sustituye de manera opcional con uno o más grupos que son independientemente alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8- alqueniloC2-6-, alcoxiarilo C0-6, alquilo C1-6, cicloalquilo C3-8, arilohalogeno, -C:::N, -COR11, -COOR11, -CON(R11)2, -SO2R11, -OR11, -SR11, -SO2R11, -SO2N(R11)2, -SO2NR11COR11, -OCON(R11)2; -NR11COR11, -NR11CON(R11)2, -NR11COOR11, o -N(R11)2; 2 y R21 son -L3-R7, en donde: cada L3 es independientemente un enlace o -V1-(CH2)n-V1-, -(CH2)m-V1-(CH2)n- en donde, n es 0-6; y cada V1 es independientemente -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, -S-, - NR7-, -N(R10)CO-, - N(R10)CO2-, -OCO-, -CO-, -CS-, -CONR10-, -C(=N-R11)-, -C(=N-OR11)-, -C[=N-N(R11)2], -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10) SO2-, -SO2N(R10)-, -NR10CONR10-, -NR10CSNR10-, cicloalquilo C3-8, o ciclohaloalquilo C3-8; o cada L3 es independientemente una cadena alidiilo C2-6, en donde la cadena de alidiilo es opcionalmente interrumpida por -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C(R11)2O-, - C(R11)2NR11-, -C:::C-, -O-, -S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO- , -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o - SO2N(R10)-; y cada R7 es independientemente un hidrogeno, halogeno, nitro, arilo, heteroarilo, heterociclilo, -alquiloC1-6-heterociclilo, - alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, -Z, -Y- Z, o -X-Y-Z, en donde, X es -O-; Y es -[C(R15)2]m-, -alqueniloC2-6, -cicloalquiloC3-8; Z es - H, -CN, halogeno, -OR11, -C(=O)R11, -C(=O)OR11, -C(=O)N(R11)2, -N(R11)2, -CN, -N3, -SO2R11, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, - C(=O)N(R11)(OR11), -OC(=O)- R11, -OC(=O)-N(R11)2, o -N(R11)COOR11, en donde R7 se sustituye de manera opcional con uno o más R7a, en donde, R7a es un halogeno, alquenilo C2-6, -alquiloC1-6-heterociclilo, -alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, haloarilo, ariloxi, aralquil-oxi, ariloxialquilo, alcoxiarilo C1-6, ariloC0-6-alquilocarboxi, C(R11)=C(R11)-COOOR11, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, arilo, heteroarilo, heterociclilo, cicloalquilo C3-8, heteroarilo-oxi, -Z', -Y'-Z', o-X'-Y'-Z', en donde , X' es -O-; Y' es -[C(R15)2]m- o cicloalquilo C3-8; Z' es -alquiloC1-6, -haloalquiloC1-6, -OR11, -SR11, -S(=O)2R11, -C(=O)R11, -C(=O)OR11, - C(=O)N(R11)2, -N(R11)2, -N(R11)C(=O)R11, - S(=O)2N(R11)C(=O)R11, -CN, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, -C(=O)N(R11)(OR11), - OC(=O)-R11, -OC(=O)-OR11, -N(R11)C(=O)-R11, -N(R11)S(O=)2R11; en donde cada R7a se sustituye de manera opcional con uno o más R8, en donde cada R8 es independientemente un halogeno, nitro, ciano, heteroarilo, alquilo C1-6, alcoxi C1-6, haloalquilo C1-6, haloalquiloC1- C6(OR11), alquilC0-C6OR11, alquiloC0-C6CON(R11)2, alquiloC0-6COR11, alquiloC0-C6COOR11, o alquiloC0-C6SO2R1, y en donde si dos R7a se presentan en el mismo carbono, se pueden combinar para formar un grupo heterociclilo o cicloalquilo; siempre que R2 y R21 no sean de manera simultánea -H; R3 es -L-R6, en donde, L es un enlace, -X3-(CH2)n-X3-, -(CH2)m-X3-(CH2)n- o -(CH2)1+w-Y3- (CH2)w-, en donde, n es 0-6; cada w es independientemente 0-5; y cada X3 es independientemente un enlace, -C(R11)2-, -C(R11)2C(R11)2-, -C(R11)=C(R11)-, -C:::C-, -CO-, -CS-, -CONR10-, -C(=N)(R11)-, -C(=N-OR11)-, -C[=N-N(R11)2], -CO2-, -SO2-, o - SO2N(R10)-; y Y3 es -O-, -S-, -NR7-, -N(R10)CO-, - N(R10)CO2-, -OCO-, -OC(=O)N(R10)-, -NR10CONR10-, -N(R10)SO2-, o -NR10CSNR10-; o L es una cadena de alidiilo C2-6 en donde la cadena de alidiilo se interrumpe de manera opcional por -C(R11)2-, - C(R11)2C(R11)2, -C(R11)=C(R11)-, -C(R11)2O-, -C(R11)2NR11-, -C:::C-, -O-, - S-, -N(R10)CO-, -N(R10)CO2-, -CON(R10)-, -CO-, -CO2-, -OC(=O)-, -OC(=O)N(R10)-, -SO2-, -N(R10)SO2-, o -SO2N(R10); y R6 es alquilo C1-6, haloalquilo C1-6, arilo, cicloalquilo C3-8, heteroarilo, heterociclilo, -CN, -C(=O)R11, -C(=O)OR11, -C(=O)N(R11)2, -N(R11)2, -SO2R11, -S(=O) 2N(R11)2, -C(=O)N(R11)N(R11)2, -C(=O)N(R11)(OR11), en donde el arilo, heteroarilo, cicloalquilo, o heterociclilo se sustituyen de manera opcional con uno o más R6a, en donde cada R6a es independientemente -Z'',-Y''-Z'', o -X''-Y''-Z'', en donde: X'' es -O-; Y'' es -[C(R15)2]m-, - alqueniloC2-6, cicloalquilo C3-8, heterociclilo, arilo, o heteroarilo, en donde el arilo, heteroarilo, cicloalquilo, o heterociclilo se sustituye de manera opcional con al menos un grupo independiente de Z''; Z'' es -H, -CN, halogeno, -OR11, -C(=O)R11, -C(=O)OR11, -C(O)N(R11)2, - N(R11)2, -N3, -SO2R11, -S(=O)2N(R11)2, -C(=O)N(R11)N(R11)2, - N(R11)C(=O)N(R11)2, -OC(=O)-R11, -C(=O)N(R11)(OR11), -OC(=O)-R11, - OC(=O)-N(R11)2, o -N(R11)COOR11; cada R10 es independientemente -R11, -C(=O)R11, -CO2R11, o -SO2R11; cada R11 es independientemente -hidrogeno, alqueniloC2-6, alquinilo C2-6, cicloalqueniloC3-8-alquiloC1-6-, cicloalquiloC3-8-alqueniloC2-6, N(R12)2, alquilo C1-6, -haloalquiloC1-6, -cicloalquiloC3-8, -alquiloC1-6-cicloalquiloC3-8, arilo, -alquiloC1-6-arilo, heteroarilo, -alquiloC1-6-heteroarilo, heterociclilo, o -alquiloC1- 6-heterociclilo; en donde cualquiera de los R11 se los sustituye de manera opcional con uno o más radicales R12; cada R12 es independientemente un halogeno, haloalquilo C1-6, alquilo C1-6, alcoxi C1-6, (alquiloC0-6)C=O(OR13); alquiloC0-6OR13, alquiloC0-6COR13, alquiloC0-6SO2R13, alquiloC0-6CN, alquiloC0-6CON(R13)2, alquiloC0-6CONR13OR13, alquiloC0-C6SO2N(R13)2, alquiloC0-6SR13, haloalquilC0-6OR13, ariloxi, aralquil-oxi, ariloxialquilo, alcoxiarilo C0-6, arilo-alquilcarbonC0-6-oxi, alquiloC0-6NR13SOR13, - alquiloC0-C6N(R13)2, o -OalquiloC0-6COOR13; cada R13 es independientemente un hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, cicloalquiloC3-8-alquiloC1-6-, cicloalqueniloC3-8-alquiloC1-6-, o cicloalquiloC3-8- alqueniloC2-6-; cada R14 es independientemente alquilo C1-6, alcoxi C1-6, halogeno, haloalquilo C1-6, alquiloC0-6CON(R11)2, alquiloC0-6CONR11OR11, alquiloC0-6OR11, o alquiloC0-6COOR11; G es un grupo de la formula (5), en donde: J es arilo, heteroarilo, o se encuentra ausente; K es arilo, heteroarilo, o se encuentra ausente; cada R4 es independientemente un halogeno, nitro, alquenilo C2-6, cicloalquilo C3-8, -alquiloC1-6-heterociclilo, -alquiloC1-6-heteroarilo, -alquiloC1-6-arilo, - heterociclil-arilo, -heterociclil-heteroarilo, CR11=CR11COOR11, ariloxi, -S-arilo, aralquiloxi, ariloxialquilo, alcoxiarilo C1-6, arilo- alquilcarboxiC0-6, alcoxiheteroarilo C0-6, alcoxiheterociclilo C0-6, arilo, heteroarilo, heterociclilo, -M, -E-M, o -D-E-M, en donde: D es -O-; E es -[C(R15)2]m- o -cicloalquiloC3-8; M es -alquiloC1-6, haloalquilo C1-6, -COR11, -COOR11, -OC(=O)R11, -CON(R11)2, -C:::N, -OR11, - OCON(R11)2, -OCO2-R11, -N3, -NR11COR11, -NR11SO2R11, -N(R11)2, -NR11COOR11, -SOR11, - SO2R11, -SO2NR11COR11, -SO2N(R11)2, o - SR11; en donde cada R4 se sustituye de manera opcional con uno o más R4a, en donde cada R4a es independientemente halogeno, ariloxi, aralquiloxi, ariloxialquilo, alcoxiarilo C1-6, aril-alquilcarbonoC0-C6-oxi, - M', -E'-M', o -D'-E'-M', en donde D' es -O-; E' es -[C(R15)2]m- o cicloalquilC3-C8; M' es -alquiloC1-6, haloalquilo C1-6, -COR11, -CON(R11)2, -N(R11)COOR11, -N(R11)2, COOR11, C:::N, OR11, NR11COR11, NR11SO2R11, SO2R11, SO2N(R11)2, o SR11; cada R41 es independientemente un halogeno, nitro, alquiloC1-6-heterociclilo, -alquiloC1-6- heteroarilo, -alquiloC1-6-arilo, -M'', -E''-M'',
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2006
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- 2006-06-26 JP JP2008519444A patent/JP5237799B2/ja not_active Expired - Fee Related
- 2006-06-26 WO PCT/US2006/024757 patent/WO2007002563A1/en active Application Filing
- 2006-06-26 BR BRPI0612287A patent/BRPI0612287A8/pt not_active IP Right Cessation
- 2006-06-26 AU AU2006261841A patent/AU2006261841B8/en not_active Ceased
- 2006-06-26 KR KR1020087001957A patent/KR20080028964A/ko not_active Application Discontinuation
- 2006-06-26 MX MX2008000141A patent/MX2008000141A/es active IP Right Grant
- 2006-06-26 EP EP06785558A patent/EP1910307A1/en not_active Withdrawn
- 2006-06-26 JP JP2008519445A patent/JP5244589B2/ja active Active
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- 2006-06-26 AU AU2006261845A patent/AU2006261845C1/en not_active Ceased
- 2006-06-26 WO PCT/US2006/024749 patent/WO2007002559A1/en active Application Filing
- 2006-06-26 CA CA002613522A patent/CA2613522A1/en not_active Abandoned
- 2006-06-26 ES ES06785562.7T patent/ES2525217T3/es active Active
- 2006-06-26 US US11/993,529 patent/US8569352B2/en active Active
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