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AR076379A1 - Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc. - Google Patents

Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc.

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Publication number
AR076379A1
AR076379A1 ARP100101340A ARP100101340A AR076379A1 AR 076379 A1 AR076379 A1 AR 076379A1 AR P100101340 A ARP100101340 A AR P100101340A AR P100101340 A ARP100101340 A AR P100101340A AR 076379 A1 AR076379 A1 AR 076379A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
phenyl
group
optionally substituted
Prior art date
Application number
ARP100101340A
Other languages
English (en)
Original Assignee
Janssen Pharmaceutica Nv
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR076379A1 publication Critical patent/AR076379A1/es

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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)

Abstract

Reivindicacion 1: Un compuesto de Formula (1) donde Y y Z se seleccionan independientemente de a) o b) de tal manera que uno de Y y Z sea seleccionado del grupo a) y el otro sea seleccionado del grupo b); El grupo a) es arilo C6-10 no sustituido, el grupo b) es i) cicloalquilo C5-7-alquilo (C1-4) benzofusionado donde cicloalquilo C5-7 está opcionalmente sustituido con 1 a 4 sustituyentes metilo; ii) aril C6-10-alquilo (C1-6); iii) aril C6-10-alquenilo (C2-6), iv) fenilalquinilo (C2-6), v) cicloalquilo C3-7 opcionalmente sustituido con uno a dos sustituyentes independientemente seleccionados del grupo integrado por alquilo C1-3, fluor, cloro, bromo, yodo, trifluorometilo, fenilo, y fenilcarbonilo; w donde el sustituyente fenilo está opcionalmente sustituido con uno a dos sustituyentes seleccionados del grupo integrado por bromo, cloro, fluor, yodo, trifluorometilo, trifluorometoxi, y trifluorometiltio; o vi) fenilo-(Q)-metilo donde Q es 0 o S; donde fenilo está opcionalmente sustituido con trifluorometilo, uno a tres sustituyentes fluor o cloro, o trifluorometoxi; donde el grupo fenilo de fenilalquinilo (C2-6); y el arilo C6-10 de aril C6-10 -alquilo (C1-6) y arilo C6-10-alquenilo (C2-6) están opcional e independientemente sustituidos, en cada caso, con uno a dos sustituyentes seleccionados del grupo integrado por i) alquilo C1-4; ii) alcoxi C1-4; iii) alquiltio C1-4; iv) -OCH2O- unido a los átomos de carbono adyacentes; v) trifluorometilo; vi) trifluorometoxi; vii) trifluorometiltio; viii) alcoxialquilaminosulfonilo C3-8; ix) alcoxicarbonilo C1-4; x) alquilcarboniloxi C1-4; xi) NRaRb donde Ra es hidrogeno o alquilo C1-6 y Rb es alquilo C1-6, fenilo, cicloalquilcarbonilo C3-8, cicloalquil C3-8-alquilo C1-2, alquilcarbonilo C1-6 opcionalmente sustituido con un a tres sustituyentes fluor, arilo C6-10-alquilo C1-2, o fenil alquilcarbonilo C1-2 donde arilo C6-10 y fenilo de Rb están opcionalmente sustituidos con uno a dos sustituyentes seleccionados de alquilo C1-4, trifluorometilo, cloro, o fluor; o Ra y Rb se toman juntos con el átomo de nitrogeno al cual están unidos para formar un anillo heterociclilo de 5 a 8 miembros, opcionalmente sustituido con oxo o alquilo C1-3 y contiene opcionalmente un heteroátomo adicional para formar morfolinilo, tiomorfolinilo, o piperazinilo; y donde dicho anillo heterociclilo está opcionalmente benzofusionado; y, el anillo heterociclilo está opcionalmente sustituido en un átomo de nitrogeno contenido en dicho anillo con alcoxicarbonilo C1-6; xii) feniloxi opcionalmente sustituido con alquilo C1-4, trifluorometilo, o uno a dos sustituyentes cloro; xiii) ciano; xiv) fluor; xv) cloro; xvi) bromo; y xvii) yodo; s es 0, 1 o 2; siempre que cuando s es 2, R1 se selecciona independientemente del grupo integrado por fenilo, alquilo C1-3, y arilo C6-10-alquilo C1-3; R1 es arilo C6-10, alquilo C1-3, benciloximetilo, hidroxi alquilo C1-3, aminocarbonilo, carboxi, trifluorometilo, ciclopropilo espirofusionado, 3-oxo o aril alquilo C1-3 o, cuando s es 2 y R1 es alquilo C1-3, los sustituyente alquilo C1-3 se toman con el anillo piperizinilo para formar un sistema anular 3,8-diaza-biciclo[3.2.1]octanilo o 2,5-diaza-biciclo[2.2.2]octanilo; siempre que cuando Y es fenilo, Z sea diferente de 2-(4-etoxifenil)etilo, 2-(3,4-difluorofenil)etil, 2-(4-dimetilaminofenil)etilo, 2-(4-metoxifenil)etilo, 4-trifluorometilfeniltio-metilo; o 2-feniletinilo; y sus enantiomeros, diastereomeros, y sales aceptables para uso farmacéutico.
ARP100101340A 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc. AR076379A1 (es)

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ARP100101343A AR076382A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.
ARP100101337A AR076376A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
ARP100101340A AR076379A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento del dolor, inflamacion y trastornos del snc.
ARP100101339A AR076378A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasas, composiciones farmaceuticas que las contienen y uso de las mismas en el tratamiento de trastornos inflamatorios asociados al dolor.
ARP100101338A AR076377A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
ARP100101341A AR076380A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasa(mgl), composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades y patologias que incluyen dolor inflamatorio.
ARP100101335A AR076374A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de lipasas de monoacil glicerol
ARP100101342A AR076381A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa

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ARP100101338A AR076377A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa
ARP100101341A AR076380A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas inhibidoras de monoacilglicerol lipasa(mgl), composiciones farmaceuticas que las contienen y uso de las mismas para el tratamiento de enfermedades y patologias que incluyen dolor inflamatorio.
ARP100101335A AR076374A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de lipasas de monoacil glicerol
ARP100101342A AR076381A1 (es) 2009-04-22 2010-04-22 Azetidinil diamidas como inhibidores de monoacilglicerol lipasa

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