AR033534A1 - Derivados de (hetero) arilsulfonil-1,3-tiazol-2-ilamina, utiles como inhibidores de 11-beta-hidroxi esteroide deshidrogenasa tipo 1, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y las composiciones farmaceuticas que las contienen - Google Patents

Derivados de (hetero) arilsulfonil-1,3-tiazol-2-ilamina, utiles como inhibidores de 11-beta-hidroxi esteroide deshidrogenasa tipo 1, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y las composiciones farmaceuticas que las contienen

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AR033534A1
AR033534A1 ARP010102421A ARP010102421A AR033534A1 AR 033534 A1 AR033534 A1 AR 033534A1 AR P010102421 A ARP010102421 A AR P010102421A AR P010102421 A ARP010102421 A AR P010102421A AR 033534 A1 AR033534 A1 AR 033534A1
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Argentina
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alkyl
optionally
hydrogen
aryl
substituted
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ARP010102421A
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Biovitrum Ab
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Abstract

La presente invencion se refiere a compuestos con la formula (1) y también a las composiciones farmacéuticas que contienen los compuestos, a los procesos para su preparacion, así como al uso de los compuestos (1) para la preparacion de medicamentos que actuan sobre la enzima 11-beta-hidroxiesteroide deshidrogenasa tipo 1 humana. Por lo tanto los compuestos (1) son utiles para tratar trastornos tales como la diabetes, obesidad, glaucoma, osteoporosis y trastornos cognitivos e inmunes. En la formula (2): T es un anillo de arilo o un anillo de heteroarilo o anillo de arilalquenilo C2, opcionalmente independientemente sustituido por [R]n, donde n es un entero de 0-5, y R es hidrogeno, arilo, heteroarilo, un anillo heterocíclico, alquilo C1-6 opcionalmente halogenado, alcoxi C1-6 opcionalmente halogenado, alquilsulfonilo C1-6, carboxi, ciano, nitro, halogeno, amina que está opcionalmente mono- o di-sustituida, amida que está opcionalmente mono- o di-sustituida, ariloxi, arilsulfonilo, arilamino, donde los restos arilo, heteroarilo y ariloxi y anillos heterocíclicos pueden adicionalmente estar opcionalmente sustituidos en una o más posiciones independientemente una de otra por acilo C1-6, alquiltio C1-6, ciano, nitro, hidrogeno, halogeno, alquilo C1-6 opcionalmente halogenado, alcoxi C1-6 opcionalmente halogenado, amida que está opcionalmente mono- o di-sustituida, (benzoilamino)metilo, carboxi, 2-tienilmetilamino o ({[4-(2-etoxi-2-oxoetil)-1,3-tiazol-2-il]amino}carbonilo); con la condicion de que cuando R1 sea H, X sea CH2, Y sea CO, R2 sea EtO y B sea H, entonces T no sea 2,4-dicloro-5-metilfenilo, 4-clorofenilo, 4-cloro-2,5-dimetilfenilo, 2,4-difluorfenilo, 3-nitrofenil y fenilo; R1 es hidrogeno o alquilo C1-6, X es CH2 o CO; y es CH2, CO o un enlace sencillo; B es hidrogeno, alquilo C1-6 o dimetilaminometilo; R2 se selecciona entre alquilo C1-6, azido, ariltio, heteroariltio, halogeno, hidroximetilo, 2-hidroxietilaminometilo, metilsulfoniloximetilo, 3-oxo-4-morfolinolinilmetileno, alcoxi C1-6 carbonilo, 5-metil-1,3,4-oxadiazol-2-ilo; NR3R4, donde R3 y R4 están cada uno independientemente seleccionados entre hidrogeno, alquilo C1-6, alquilo C1-6 opcionalmente halogenado sulfonilo, alcoxi C1-6, 2-metoxietilo, 2-hidroxietilo, 1-metilimidazolilsulfonilo, acilo C1-6, ciclohexilmetilo, ciclopropanocarbonilo, arilo, aril opcionalmente halogenado sulfonilo, furilcarbonilo, tetrahidro-2-furanilmetilo, N-carbetoxipiperidilo, o alquilo C1-6 sustituido con uno o más arilo o heteroarilo, o NR3R4 representa en conjunto un sistema heterocíclico que puede ser imidazol, piperidina, pirrolidina, piperazina, morfolina, oxazepina, oxazol, tiomorfolina, 1,1-dioxidotiomorfolina, 2-(3,4-dihidro-2(1H)isoquilonlinilo), (1S,4S)-2-oxa-5-azabiciclo[2,2,1]hept-5-ilo, cuyo sistema heterocíclico puede estar opcionalmente sustituido por alquilo C1-6, acilo C1-6, hidroxi, oxo, t-butoxicarbonilo; OCONR3R4, donde R3 y R4 están cada uno independientemente seleccionados entre hidrogeno, alquilo C1-6 o forman juntos un morfolinilo; R5O, donde R5 es hidrogeno, alquilo C1-6 opcionalmente halogenado, arilo, heteroarilo, acilo C1-6, alquilsulfonilo C1-6, arilcarbonilo, heteroarilcarbonilo, 2-carbometoxifenilo.
ARP010102421A 2000-05-22 2001-05-22 Derivados de (hetero) arilsulfonil-1,3-tiazol-2-ilamina, utiles como inhibidores de 11-beta-hidroxi esteroide deshidrogenasa tipo 1, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y las composiciones farmaceuticas que las contienen AR033534A1 (es)

Applications Claiming Priority (1)

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SE0001899A SE0001899D0 (sv) 2000-05-22 2000-05-22 New compounds

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AR033534A1 true AR033534A1 (es) 2003-12-26

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ARP010102421A AR033534A1 (es) 2000-05-22 2001-05-22 Derivados de (hetero) arilsulfonil-1,3-tiazol-2-ilamina, utiles como inhibidores de 11-beta-hidroxi esteroide deshidrogenasa tipo 1, procedimiento para prepararlos, el uso de los mismos para la preparacion de medicamentos y las composiciones farmaceuticas que las contienen

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JP (4) JP2003534337A (es)
KR (4) KR20030016271A (es)
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