AR048427A1 - Derivados de sulfonilpirroles con actividad inhibitoria de la histona deacetilasa, composiciones farmaceuticas que los contienen y el uso de las mismas para el tratamiento de enfermedades relacionadas. - Google Patents

Derivados de sulfonilpirroles con actividad inhibitoria de la histona deacetilasa, composiciones farmaceuticas que los contienen y el uso de las mismas para el tratamiento de enfermedades relacionadas.

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Publication number
AR048427A1
AR048427A1 ARP050100915A ARP050100915A AR048427A1 AR 048427 A1 AR048427 A1 AR 048427A1 AR P050100915 A ARP050100915 A AR P050100915A AR P050100915 A ARP050100915 A AR P050100915A AR 048427 A1 AR048427 A1 AR 048427A1
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Argentina
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alkyl
group
alkoxy
halogen
ring
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ARP050100915A
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English (en)
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Thomas Maier
Thomas Beckers
Thomas Bar
Petra Gimmnich
Frank Dullweber
Matthias Vennemann
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Altana Pharma Ag
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    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
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    • A61K31/4025—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil not condensed and containing further heterocyclic rings, e.g. cromakalim
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Abstract

Compuestos derivados de sulfonilpirroles como inhibidores de HDAC efectivos; composiciones farmacéuticas que los contienen utilizadas en el tratamiento de enfermedades mediadas por la actividad de la histona deacetilasa como cáncer, artropatías y condiciones inflamatorias. Reivindicacion 1: Compuestos de formula (1) caracterizados porque R1 es H, alquilo C1-4, halogeno, o alcoxi C1-4; R2 es H, alquilo C1-4, R3 es H, alquilo C1-4, R4 es H, alquilo C1-4, halogeno, o alcoxi C1-4, R5 es H, alquilo C1-4, halogeno, o alcoxi C1-4, R6 es -T1-Q1, en donde T1 es un enlace, o alquileno C1-4; Q1 es Ar1, Aa1, Hh1, o Ah1, en donde Ar1 es fenilo, o fenilo sustituido por R61 y/o R62, en dodne R61 es alquilo C1-4, o -T2-N(R611)R612, en dodne ya sea T2 es un enlace, y R611 es H, alquilo C1-4, hidroxialquilo C2-4, alcoxi C1-4, alquilo C2-4, fenilalquiolo C1-4, o Har1-alquilo C1-4, en dodne Har1 está opcionalmente sustituido por R6111 y/o R6112, y es un anillo heteroaromáticvo insaturado monocíclico o bicíclico fusionado de 5 a 10 miembros que comprende uno a tres heteroátomos, cada uno de los cuales se selecciona del grupo que consiste en N, O y sulfuro, en donde R6111 es halogeno, o alquilo C1-4, R6112 es alquilo C1-4, y R612 es H, alquilo C1-4, alcoxi C1-4 alquilo C2-4 o hidroxialquilo C2-4, o R611 y R612 en forma conjunta y con inclusion del átomo de N al cual están enlazados forman un anillo heterocíclico Het1, en donde Het 1 es morfolino, tiomorfolino, S-oxo- tiomorfolino, S,S-dioxo-tiomorfolino, piperidino, pirrolidino, piperazino, o 4N-(alquilo C1-4)-piperazino, o T2 es alquileno C1-4, o alquileno C2-4 interrumpido por O, y R611 es H, alquilo C1-4, hidroxialquilo C2-4, alcoxi C1-4 alquilo C2-4, fenilalquilo C1-4, o Har1-alquilo C1-4, en donde Har1 está opcionalmente sustituido por R6111y/o R6112, y es un anillo heteroaromático insaturado monocíclico o bicíclico fusionado de 5 a 10 miembros que comrpende uno a tres heteroátomos, cada uno de los cuales se seleciona del grupo que consiste en N, O y sulfuro, en donde R6111 es halogeno, o alquilo C1-4, R6112 es alquilo C1-4, y R612 es H, alquilo C1-4, alcoxi C1-4 alquilo C2-4 o hidroxialquilo C2-4, o R611 y R612 en forma conjunta y con inclusion del átomo de N al cual están enlazados forman un anillo heterocíclico Het1, en donde het1 es morfolino, tiomaorfolino, S-oxo-tiomorfolino, S,S-dioxo-tiomorfolino, piperidino, pirrolidino, piperazino, 4N-(alquilo C1-4)-piperazino, imidazolo, pirrolo o pirazolo, R62 es alquilo C1-4, alcoxi C1-4, halogeno, ciano, alcoxi C1-4-alquilo C1-4, alquilcarbonilamino C1-4, o alquilsulfonilamino C1-4, Aa1 es un radical bisarilo formado por dos grupos arilo, que se seleccionan independientemente de un grupo que consiste en fenilo y naftilo, y que se unen mediante un enlace simple, Hh1 es un radical bis-heteroarilo formado por dos grupos heteroarilo, que se seleccionan independientemente de un grupo que consiste en radicales heteroarilo monocíclicos de 5- o 6 miembros que comprende uno o dos heteroátomos, cada uno de los cuales se selecciona del grupo que consiste en N, O y sulfuro, y que se unen mediante un enlace simple, Ah1 es un radical heteroarilo o radical aril-heteroarilo formado por un grupo heteroarilo seleccionado del grupo que consiste en radicales heteroarilo de 5 o 6 miembros monocíclicos que comprenden uno o dos heteroátomos, cada uno de los cuales se selecciona del grupo que consiste en N, O y sulfuro, y un grupo arilo seleccioando del grupo que consiste en fenilo y naftilo, en dodne dichos grupos arilo y heteroarilo se unen mediante un enlace simple, R7 es hidroxilo, o Cic1, en donde Cic1 es un sistema de anillo de la formula (2) en donde A es C (carbono), B es C (carbono), R71 es H, halogeno, alquilo C1-4, o alcoxi C1-4, R72 es H, halogeno, alquilo C1-4, o alcoxi C1-4; M con inclusion de A y B es, ya sea un anillo Ar2 o un anillo Har2 en donde Ar2 es un anillo de benceno, Har2 es un anillo heteroaromático insaturado monocíclico de 5 o 6 miembros que comprende uno a tres heteroátomos, cada uno de los cuales se selecciona del grupo que consiste en N, O y sulfuro, y las sales de estos compuestos.
ARP050100915A 2004-03-11 2005-03-10 Derivados de sulfonilpirroles con actividad inhibitoria de la histona deacetilasa, composiciones farmaceuticas que los contienen y el uso de las mismas para el tratamiento de enfermedades relacionadas. AR048427A1 (es)

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KR101130556B1 (ko) * 2004-03-11 2012-03-30 4에스체 악티엔게젤샤프트 Ｈｄａｃ 억제제로서의 설포닐피롤
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US8404718B2 (en) 2005-01-21 2013-03-26 Astex Therapeutics Limited Combinations of pyrazole kinase inhibitors
AR054425A1 (es) 2005-01-21 2007-06-27 Astex Therapeutics Ltd Sales de adicion de piperidin 4-il- amida de acido 4-(2,6-dicloro-benzoilamino) 1h-pirazol-3-carboxilico.
EA015533B1 (ru) 2005-03-15 2011-08-30 4Сц Аг N-сульфонилпирролы и их применение в качестве ингибиторов гистондезацетилазы
AU2006232773B2 (en) * 2005-04-07 2012-04-12 4Sc Ag Sulfonylpyrroles as histone deacetylase inhibitors
NZ541788A (en) * 2005-08-11 2007-12-21 Auckland Uniservices Ltd Conducting polymers and their use in oligonucleotide (ODN) probes
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