AR063721A1 - Derivados de anilinopiperazina y composicion farmaceutica - Google Patents
Derivados de anilinopiperazina y composicion farmaceuticaInfo
- Publication number
- AR063721A1 AR063721A1 ARP070104809A ARP070104809A AR063721A1 AR 063721 A1 AR063721 A1 AR 063721A1 AR P070104809 A ARP070104809 A AR P070104809A AR P070104809 A ARP070104809 A AR P070104809A AR 063721 A1 AR063721 A1 AR 063721A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkylene
- alkyl
- aryl
- haloalkyl
- heterocyclyl
- Prior art date
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- C07D277/20—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members
- C07D277/32—Heterocyclic compounds containing 1,3-thiazole or hydrogenated 1,3-thiazole rings not condensed with other rings having two or three double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
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Abstract
La presente invención se refiere a derivados de anilinopiperazina, y a composiciones que comprenden los derivados de anilinopiperazina. Estos compuestos son útiles para prevenir un trastorno proliferativo, un trastorno antiproliferativo, inflamación, artritis, un trastorno del sistema nervioso central, una enfermedad cardiovascular, alopecia, una enfermedad neuronal, una lesión isquémica, una enfermedad viral, una infección fúngica o un trastorno relacionado con la actividad de una proteína quinasa. Reivindicación 1: Un compuesto que tiene la fórmula (1) o una de sus sales, solvatos, ésteres, profármacos o estereoisómeros farmacéuticamente aceptables, en donde la línea de puntos indica un enlace opcional y adicional y en donde: R1 es H, alquilo, alquenilo, alquinilo, halo, -(alquilen)m-arilo, -alquenilenarilo, -alquinilen-arilo, -(alquilen)mcicloalquilo, -(alquilen)m-heteroarilo, -(alquilen)m-heterociclilo, -(alquilen)m-heterociclenilo, en donde cualquier arilo, cicloalquilo, heteroarilo, heterociclilo o heterociclenilo puede estar opcionalmente sustituido con hasta 5 sustituyentes, que pueden ser iguales o diferentes, y están seleccionados, de modo independiente, de halo, alquilo, cicloalquilo, - (alquilen),N(R9)2, -(alquilen)m-O-alquilo, -O-arilo, -C(O)R8, -S-alquilo, -O-arilo, -(alquilen)m-CN, alquinilo, alquenilo, hidroxialquIlo, haloalquilo, -O-haloalquiLo, -C(O)OR7, -NHC(O)R7, -C(O)N(R7)2, -S(O)2N(R8)2, -NHS(O)2R8, -(alquilen)m- heteroarilo, - (alquilen)m-heterociclilo y -(alquilen)m-arilo; en donde un grupo alquilo, alquenilo o alquinilo puede estar sustituido con uno o varios sustituyentes, que pueden ser iguales o diferentes, y están seleccionados, de modo independiente, de halo, alquilo, -N(R7)2, -C(O)OH, arilo, y -O-alquilo; en donde cualquier grupo cíclico R1 puede estar opcionalmente fusionado a un grupo cicloalquilo, arilo, heteroarilo o heterociclilo; de modo que, cuando R1 es heteroarilo, heterociclilo o heterociclenilo, estos grupos están unidos al resto del compuesto de la fórmula (1) por medio de un átomo de carbono del anillo; R2 es H, alquilo, haloalquilo, hidroxialquilo, -(alquilen)m-C(O)N(R8)2, -(alquilen)-NHC(O)-R9 o -(alquilen)m-N(R9)2, o R2 y el átomo de carbono del anillo al que está unido forma un grupo carbonilo; R3 es H, -alquilo, haloalquilo, hidroxialquilo, -(alquilen),-C(O)N(R8)2, -(alquilen)m-NHC(O)-R9 o -(alquilen)m-N(R9)2, o R3 y R3a, junto con el átomo de carbono común al que están unidos, se juntan para formar un grupo carbonilo, cicloalquilo o heterociclilo; R3a es H, -alquilo, haloalquilo, hidroxialquilo, -(alquilen)m-C(O)N(R8)2, - (alquilen)m-NHC(O)-R9 o -(alquilen)m-N(R9)2; cada aparición de R4 es, de modo independiente, H, -alquilo, -(alquilen)m-arilo, -(alquilen)m-heteroarilo, -(alquilen)m-heterociclilo, -(alquilen)m-N(R8)2, -(alquilen)m-OH, -(alquilen)m-NHC(O)R8, hidroxialquilo, haloalquilo, -CH2NH2, -C(O)R5, -C(O)OR8, -C(O)-(alquilen)m-N(R8)2, - C(O)NH-alquilo, -C(O)N(alquil)2, -(alquilen)-NHC(O)R6, -NHC(O)OR8, -CR2C(O)NH2, -CR2C(O)NH(alquilo), -CR2C(O)NH(alquilo)2 o -NHS(O)2R6; R5 es H, alquilo, arilo, -heteroarilo o -NHOH; cada aparición de R6 es, de modo independiente, H, alquilo, arilo o haloalquilo; cada aparición de R7 es H, -OH, alquilo, -O-alquilo, cicloalquilo o haloalquilo; cada aparición de R8 es, de modo independiente, H, alquilo, -(alquilen)m-arilo, -(alquilen)m-heterociclilo, -(alquilen)m-heteroarilo o -(alquilen)m- cicloalquilo; cada aparición de R9 es H, aquilo, haloalquilo, hidroxialquilo, -(alquilen)m-arilo, -(alquilen)m-heterociclo, -(alquilen)m-heteroarilo o -(alquilen)m-cicloalquilo; R10 es H, -alquilo, haloalquilo, hidroxialquilo, -(alquilen)m- C(O)N(R8)2, -(alquilen)m-NHC(O)-R9 o -(alquilen)m-N(R9)2, o R10 y R10a, junto con el átomo de carbono común al que están unidos, se juntan para formar un grupo carbonilo, cicloalquilo o heterociclilo; R10a es H, -alquilo, haloalquilo, hidroxialquilo, -(alquilen)m-C(O)N(R8)2, -(alquilen)m-NHC(O)-R9 o -(alquilen)m-N(R9)2; cada aparición de R11 es, de modo independiente, H, alquilo, haloalquilo, hidroxialquilo, -(alquilen)m-C(O)N(R8)2, -(alquilen)m-NHC(O)-R9 o -(alquilen)m-N(R9)2, o cualquier R11 y el átomo de carbono del anillo al que está unido forma un grupo carbonilo; cada aparición de R12 es, de modo independiente, H, alquilo, -(alquilen)m-arilo, -(alquilen)m-heteroarilo, -(alquilen)m-heterociclilo, -S(O)2-alquilo, -S(O)2- arilo, -S(O)2-heteroarilo, hidroxialquilo, -C(O)R8, o -C(O)OR8; Ar es arileno o heteroarileno, en donde el arileno o heteroarileno se juntan a través de 2 de sus átomos de carbono del anillo adyacentes, y en donde el grupo arileno o heteroarileno puede estar opcionalmente sustituido con hasta 4 sustituyentes, que pueden ser iguales o diferentes, y están seleccionados, de modo independiente, de halo, alquilo, -OH, -OR9, -(alquilen)m-N(R6)2 -N(alquilo)2, -SR9, -S(O)R8, -S(O)2R8, -S(O)2NHR9, - C(O)R8, -C(O)OR9, -(alquilen)m-C(O)N(R8)2, -NHC(O)R9, haloalquilo, hidroxialquilo, -CN y NO2, de modo que, cuando Ar es tetrahidronaftileno, R2 y son cada uno distintos de hidrógeno; W es -N(R12)-, -S-, -O- o -C(R4)2-, en donde ambos grupos R4 y el átomo de carbono común al que están unidos se pueden combinar para formar un grupo cicloalquilo o heterociclilo, cada uno de los cuales también pueden estar sustituidos; Y es H, halo, alquilo o -CN; Z es -C(R7)- o -N-, de modo que, cuando el enlace adicional opcional está presente, Z es -C(R7)-; cada aparición de m es, de modo independiente, 0 ó 1; n es un número entero de 0 a 2; y p es 0 ó 1.
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WO2008054702A1 (en) | 2008-05-08 |
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US9206142B2 (en) | 2015-12-08 |
EP2078003A1 (en) | 2009-07-15 |
AU2007314342B2 (en) | 2013-02-21 |
TW200829583A (en) | 2008-07-16 |
IL198397A0 (en) | 2010-02-17 |
CN101578275A (zh) | 2009-11-11 |
AU2007314342A1 (en) | 2008-05-08 |
JP5063700B2 (ja) | 2012-10-31 |
CA2668210C (en) | 2013-03-12 |
EP2078003B1 (en) | 2017-03-08 |
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