AR040791A1 - Arilcicloalquilaminas aciladas y su utilizacion como compuestos farmaceuticos - Google Patents

Arilcicloalquilaminas aciladas y su utilizacion como compuestos farmaceuticos

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Publication number
AR040791A1
AR040791A1 AR20030102804A ARP030102804A AR040791A1 AR 040791 A1 AR040791 A1 AR 040791A1 AR 20030102804 A AR20030102804 A AR 20030102804A AR P030102804 A ARP030102804 A AR P030102804A AR 040791 A1 AR040791 A1 AR 040791A1
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Argentina
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alkyl
group
heteroaryl
phenyl
alkoxy
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AR20030102804A
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Aventis Pharma Gmbh
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Abstract

Compuestos farmacológicamente activos valiosos, que son útiles en el tratamiento de varios estados de enfermedad incluyendo trastornos cardiovasculares tales como aterosclerosis, trombosis, enfermedad arterial coronaria, hipertensión e insuficiencia cardíaca. Los mismos regula hacia arriba la expresión de la enzima sintasa de óxido nítrico (NO) endotelial y pueden ser aplicados en condiciones en las cuales se desea una expresión incrementada de dicha enzima o un nivel de NO aumentado o la normalización de un nivel reducido de NO. La presente además se refiere a procesos para la preparación de compuestos de la fórmula (1), a su utilización, en particular como ingredientes activos en composiciones farmacéuticas, y a las preparaciones farmacéuticas que los contienen. Reivindicación 1: Un compuesto de la fórmula (1) en cualquiera de sus formas estereoisoméricas o una mezcla de las mismas en cualquier proporción, o una sal farmacéuticamente aceptables del mismo, en donde en la fórmula (1) es: R1 es arilo o heteroarilo, estando ambos sin sustituir o sustituidos por uno o más sustituyentes idénticos o diferentes seleccionados del grupo que consiste en alquilo C1-6, halógeno, CF3, alcoxilo C1-6, alquil(C1-6)-mercapto, -CN, COOR10, CONR11R12, NR13R14, S(O)mR15 y S(O)2NR16R17; R2 es arilo o heteroarilo, estando ambos sin sustituir o llevan uno o más sustituyentes idénticos o diferentes seleccionados del grupo que consiste en: halógenos; -CN; NH2; alquilo C1-10, alquenilo C2-10, alquinilo C2-10, alcoxilo C1-10, alquil(C1-10)-amino y di(alquil (C1-10)-amino sin sustituir o al menos monosustituidos, los sustituyentes de los cuales se seleccionan del grupo que consiste en F, OH, alcoxilo C1-8, ariloxilo, alquil(C1-8)-mercapto, NH2, alquil(C1-6)-amino y di(alquil C1-8)-amino; alcanodiílo C3-5; fenilo; heteroarilo; alquilo C1-4 sustituido por arilo o sustituido por heteroarilo; CF3; NO2; OH; fenoxilo; benciloxilo; (alquilo C1-10)-COO-; S(O)mR20; SH; fenilamino; bencilamino; (alquil (C1-10)-CONH-; (alquil C1-10)-CON-(alquilo C1-4); fenil-CONH-; fenil-CO-N(alquilo C1-4); heteroaril-CONH-; heteroaril-CON(alquilo C1-4); (alquil C1-10)-CO-; fenil-CO-; heteroaril-CO-; CF3-CO-; -OCH2O-; -OCF2O-; -OCH2CH2O-; -CH2CH2O-; COOR21; CONR22R23; C(NH)-NH2; S(O)2NR24R25; R26S(O)2NH-; R27S(O)2N(alquilo C1-6); y un radical de un heterociclo de 5 miembros a 7 miembros alifático monocíclico saturado o por lo menos monoinsaturado que contiene 1, 2 ó 3 heteroátomos seleccionados del grupo que consiste en N, O y S, heterociclo que puede estar sustituido por uno o más sustituyentes seleccionados del grupo que consiste en halógenos, alquilo C1-3, alcoxilo C1-3, OH, oxo y CF3, en donde dicho heterociclo puede estar opcionalmente condensado a dicho grupo arilo o grupo heteroarilo que representa R2; en donde todos los grupos arilo, heteroarilo, fenilo, que contienen arilo, que contienen heteroarilo y que contienen fenilo, que estén opcionalmente presentes en dichos sustituyentes de dicho grupo arilo o grupo heteroarilo que representa R2, pueden estar sustituidos por uno o más sustituyentes seleccionados del grupo que consiste en halógenos, -CN, alquilo C1-3, OH, alcoxilo C1-3 y CF3; R10 es H, alquilo C1-6 o bencilo en donde el grupo fenilo puede estar sustituido por uno o más sustituyentes idénticos o diferentes del grupo que consiste en halógenos, -CN, alquilo C1-3, alcoxilo C1-3 y CF3; R11 es seleccionado del grupo que consiste en: H, alquilo C1-6 que puede estar sustituido por fenilo; fenilo; indanilo; y heteroarilo; en donde cada uno de los grupos aromáticos está sin sustituir o lleva uno o más sustituyentes idénticos del grupo que consiste en halógenos, -CN, alquilo C1-3, alcoxilo C1-3 y CF3; R12 es H o alquilo C1-6; R13 es seleccionado del grupo que consiste en: H, alquilo C1-6; y fenilo, bencilo, heteroarilo, fenil-CO-, y heteroaril-CO- sin sustituir o sustituidos, los sustituyentes de los cuales se seleccionan del grupo que consiste en halógenos, -CN-alquilo C1-3, alcoxilo C1-3 y CF3, en donde uno o más de estos sustituyentes pueden estar presentes; R14 es H o alquilo C1-6; R15 es seleccionado del grupo que consiste en: alquilo C1-6; CF3; y fenilo y heteroarilo sin sustituir y sustituidos, los sustituyentes de los cuales se seleccionan del grupo que consiste en halógenos, -CN, alquilo C1-3, alcoxilo C1-3 y CF3; en donde uno o más de estos sustituyentes pueden estar presentes; R16, independientemente de R11, se define como R11; R17, independientemente de R12, se define como R12; R20 es seleccionado del grupo que consiste en: alquilo C1-10 que puede estar sustituido por uno o más sustituyentes seleccionados del grupo que consiste en F, OH, alcoxilo C1-8; ariloxilo, alquil(C1-8)-mercapto, alquil(C1-8)-amino y di(alquil (C1-8)-amino; CF3; y fenilo y heteroarilo sustituidos y sin sustituir, los sustituyentes de los cuales se seleccionan del grupo que consiste en halógenos, -CN, alquilo C1-3, alcoxilo C1-3 y CF3, en donde uno o más de estos sustituyentes pueden estar presentes; R21 es seleccionado del grupo que consiste en: H, alquilo C1-10 que puede estar sustituido por uno o más sustituyentes seleccionados del grupo que consiste en F, alcoxilo C1-8 y di(alquil C1-8)-amino; aril-(alquilo C1-4), y heteroaril-(alquilo C1-4), pudiendo estar ambos sustituidos por uno o más sustituyentes seleccionados del grupo que consiste en halógenos, alquilo C1-4, alcoxilo C1-4 y di(alquil C1-6)-amino; R2 es seleccionado del grupo que consiste en: H, alquilo C1-10 que puede estar sustituido por uno o más sustituyentes seleccionados del grupo que consiste en F, alcoxilo C1-8, di(alquil C1-8)-amino y fenilo; fenilo; indanilo; y heteroarilo; pudiendo estar cada uno de los grupos aromáticos sin sustituir o llevan uno o más sustituyentes seleccionados del grupo que consiste en halógenos, -CN, alquilo C1-3, alcoxilo C1-3 y CF3; R23 es H o alquilo C1-10; R24, independientemente de R22, se define como R22; R25, independientemente de R23, se define como R23; R26, independientemente de R20, se define como R20; R27, independientemente de R20, se define como R20; heteroarilo es un radical de un heterociclo de 5 miembros a 10 miembros, aromático, monocíclico o bicíclico, que contiene uno o más heteroátomos seleccionados del grupo que consiste en N, O y S; arilo es fenilo, naft-1-ilo o naft-2-ilo; m es 0, 1 ó 2; n es 1, 2, 3 ó 4; con la salvedad que, si R1 es fenilo sin sustituir, R2 no puede ser fenilo sin sustituir, 4-bromofenilo, 3-metoxifenilo, 4-H-tieno[3,2-b]pirrol-5-ilo sustituido con cloro, tienilo sin sustituir, naftiridinilo, piridinilo sin sustituir, 3-hidroxi-4-metoxipiridin-2-ilo,2,6-dicloro-piridin-4-ilo o 3,4,5-trimetoxifenilo.
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