AR045651A1 - Derivados de tiazol como moduladores del receptor de cannabinoide - Google Patents

Derivados de tiazol como moduladores del receptor de cannabinoide

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Publication number
AR045651A1
AR045651A1 ARP040103290A ARP040103290A AR045651A1 AR 045651 A1 AR045651 A1 AR 045651A1 AR P040103290 A ARP040103290 A AR P040103290A AR P040103290 A ARP040103290 A AR P040103290A AR 045651 A1 AR045651 A1 AR 045651A1
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Argentina
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group
disorders
whose
branched
atom
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ARP040103290A
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Josephus H M Lange
Cornelis G Kruse
Stuivenberg Hernan H Van
Leonardus A J M Sliedregt
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Solvay Pharm Bv
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    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
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    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
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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
    • C07D277/22—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 only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring carbon atoms
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    • 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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    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links

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Abstract

La presente se refiere a un grupo de derivados de tiazol, a métodos para la preparación de estos compuestos, a composiciones farmacéuticas que contienen al menos uno de estos compuestos como ingredientes activo, así como el uso de éstas composiciones para el tratamiento de desórdenes psiquiátricos y neurológicos y otras enfermedades que involucran neurotransmisión CB cannabinoide. Los derivados de tiazol son antagonistas del receptor (CB) cannabinoide, agonistas del receptor CB, agonistas inversos del receptor CB o agonistas parciales del receptor CB. Reivindicación 1: Un compuesto de la fórmula (1) en donde R y R1 son iguales o diferentes y representan fenilo o piridinilo, sustituidos opcionalmente con 1-3 sustituyentes Y, en donde Y representa un sustituyente del grupo metilo, etilo, propilo, metoxi, etoxi, hidroxi, hidroximetilo, hidroxietilo, Cl, I, Br, F, trifluorometilo, trifluorometoxi, metilsulfonilo, metilsulfanilo, trifluorometilsulfonilo, fenilo o ciano, con la condición de que X no representa el subgrupo (ii), o uno de los grupos moleculares R y R1 representa un grupo fenilo o piridinilo, sustituido opcionalmente con 1-3 sustituyentes Y, en donde Y tiene el significado anteriormente mencionado y el otro grupo molecular representa un átomo de H o un grupo alquilo C1-8 ramificado o lineal, un grupo heteroalquilo C3-8 ramificado o lineal que contiene un heteroátomo del grupo (N, O, S), un grupo cicloalquilo C3-7, un grupo cicloalquil C3-7-alquilo C1-3, un grupo heterocicloalquil C3-7-alquilo C1-3 cuyos grupos pueden estar sustituidos con un grupo hidroxi, metoxi, metilo, trifluorometilsulfonilo o trifluorometilo o un átomo de F y cuyo grupo heterocicloalquil C3-7-alquilo C1-3 contiene uno o dos heteroátomos del grupo (O, N, S), o dicho otro grupo molecular representa un grupo bencilo sustituido opcionalmente en su anillo fenilo con 1-3 sustituyentes Y, en donde Y tiene el significado anteriormente mencionado; X representa uno de los subgrupos (i) o (ii) en donde R2 representa un grupo alquilo C1-8 ramificado o lineal, un grupo cicloalquilo C3-7, un grupo cicloalquil C3-7-alquilo C1-2, un grupo heterocicloalquil C3-7-alquilo C1-2 cuyos grupos pueden estar sustituidos con un grupo hidroxi, metilo o trifluorometilo o un átomo de F y cuyo grupo heterocicloalquil C3-7-alquilo C1-2 contiene uno o dos heteroátomos del grupo (O, N, S), o R2 representa un grupo fenilo, bencilo, fenetilo o fenilpropilo que puede estar sustituido en su anillo fenilo con 1-3 sustituyentes Y, en donde Y tiene el significado anteriormente mencionado, o R2 representa un grupo piridilo, tienilo o naftilo, cuyo grupo naftilo puede estar sustituido con un átomo de halógeno, un grupo metilo o un grupo metoxi o trifluorometilo; R3 representa un átomo de H o un grupo alquilo C1-3 ramificado o lineal; R4 representa H, un grupo alquilo C1-10 o cicloalquil C3-8-alquilo C1-2 ramificado o lineal, alcoxi C1-10 ramificado o lineal, cicloalquilo C3-8, bicicloalquilo C5-10, bicicloalquil C5-10-alquilo C1-2, tricicloalquilo C6-10, tricicloalquil-metilo C6-10, alquenilo C3-10 ramificado o lineal, cicloalquenilo C5-8, cuyos grupos pueden contener uno o más heteroátomos del grupo (O, N, S), y cuyos grupos pueden estar sustituidos con un grupo hidroxi, 1-3 grupos metilo, un grupo etilo o 1-3 átomos de F, o R4 representa un grupo fenilo, fenilamino, fenoxi, bencilo, fenetilo o fenilpropilo, sustituido opcionalmente en su anillo fenilo con 1-3 sustituyentes Y, en donde Y tiene el significado anteriormente mencionado, o R4 representa un grupo piridilo o tienilo, o R4 representa un grupo NR5R6 en donde R5 y R6 -junto con el átomo de N al cual están unidos- forman un grupo heterocíclico monocíclico o bicíclico, saturado o insaturado, que tiene 4 a 10 átomos de anillo, cuyo grupo heterocíclico contiene uno o más heteroátomos del grupo (O, n, S) y cuyo grupo heterocíclico puede estar sustituido con un grupo alquilo C1-3 ramificado o lineal, fenilo, hidroxi o trifluorometilo o un átomo de F, o R3 y R4-junto con el átomo de N al cual están unidos- forman un grupo heterocíclico monocíclico o bicíclico, saturado o insaturado, que tiene 4 a 10 átomos de anillo, cuyo heterocíclico contiene uno o más heteroátomos del grupo (O, N, S) y cuyo grupo heterocíclico puede estar sustituido con un grupo alquilo C1-3 ramificado o lineal, fenilo, amino, hidroxi, metoxi, ciano o trifluorometilo o un átomo de F o Cl; y sales farmacológicamente aceptables de los mismos, así como prodrogas, para la preparación de una composición farmacéutica para el tratamiento de desórdenes que involucran neurotransmisión cannabinoide tales como psicosis, ansiedad, depresión, deficiencias de atención, desórdenes de memoria, desórdenes del conocimiento, desórdenes del apetito, obesidad, adicción, apetencia, dependencia de drogas y desórdenes neurológicos tales como desórdenes neurodegenerativos, demencia, distonía, espasticidad muscular, temblor, epilepsia, esclerosis múltiple, daño cerebral traumático, apoplejía, enfermedad de Parkinson, enfermedad de Alzheimer, epilepsia, enfermedad de Huntington, síndrome de Tourette, isquemia cerebral, apoplejía cerebral, trauma craneocerebral, ataque cerebral, daño a la médula espinal, desórdenes neuroinflamatorios, esclerosis de placa, encefalitis viral, desórdenes relacionados con la desmielinización, así como para el tratamiento de desórdenes de dolor, incluyendo desórdenes de dolor neuropático, y otras enfermedades que involucran neurotransmisión cannabinoide, incluyendo el tratamiento de choque séptico, glaucoma, cáncer, diabetes, emesis, náusea, asma, enfermedades respiratorias, desórdenes gastrointestinales, desórdenes sexuales, úlceras gástricas, diarrea y desórdenes cardiovasculares.
ARP040103290A 2003-09-19 2004-09-15 Derivados de tiazol como moduladores del receptor de cannabinoide AR045651A1 (es)

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