AR076374A1 - Azetidinil diamidas como inhibidores de lipasas de monoacil glicerol - Google Patents

Azetidinil diamidas como inhibidores de lipasas de monoacil glicerol

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Publication number
AR076374A1
AR076374A1 ARP100101335A ARP100101335A AR076374A1 AR 076374 A1 AR076374 A1 AR 076374A1 AR P100101335 A ARP100101335 A AR P100101335A AR P100101335 A ARP100101335 A AR P100101335A AR 076374 A1 AR076374 A1 AR 076374A1
Authority
AR
Argentina
Prior art keywords
alkyl
aryl
optionally substituted
group
phenyl
Prior art date
Application number
ARP100101335A
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.)
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Publication date
Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of AR076374A1 publication Critical patent/AR076374A1/es

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    • C07D495/04—Ortho-condensed systems

Abstract

Se revelan compuestos, composiciones y métodos para tratar varias enfermedades, síndromes, afecciones y trastornos, incluyendo el dolor. Reivindicacion 1: Un compuesto de formula (1) donde Y y Z se seleccionan independientemente de a) o b) de modo que uno de Y y Z se selecciona del grupo a) y el otro se selecciona del grupo b); el grupo a) es arilo C6-10 sustituido, trifluorometilo, cicloalquilo C3-8, o heteroarilo seleccionado del grupo integrado por tienilo, furanilo, tiazolilo, isotiazolilo, oxazolilo pirrolilo, piridinilo, isoxazolilo, imidazolilo furazan-3-ilo, benzotienilo, tieno[3,2-b]tiofen-2-ilo pirazolilo, triazolilo tetrazolilo, y [1,2,3]tiadiazolilo; donde arilo C6-10 está sustituido con; y el heteroarilo está opcionalmente sustituido con; un sustituyente seleccionado del grupo integrado por fluor, cloro, bromo, alquilo C1-4, ciano alquilcarbonilamino C1-4, y trifluorometilo; el grupo b) es cicloalquilo C5-7-alquilo C1-4 benzofusionado donde cicloalquilo C5-7 está opcionalmente sustituido con 1 a 4 sustituyentes metilo; aril C6-10-alquilo C1-6; aril C6-10-alquenilo C2-6; fenil alquinilo C2-6; 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 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; fenil-(Q)-metilo donde Q es O o S; donde fenilo está opcionalmente sustituido con trifluorometilo, uno a tres sustituyentes fluor o cloro, o trifluorometoxi; pentadecanjlo; septadeca-8,11-dienilo; nonadeca-4,7,10,13-tetraeno-ilo; nonadecanilo; heptadec-8-eno-ilo; o 1-(4-cianofenil)piperidín-4-ilo; donde el grupo fenilo de fenil alquinilo C2-6; y el arilo C6-10 de aril C6-10-alquilo C1-6 y arilo C6-10-alquenilo C2-6 están cada uno de ellos opcionalmente sustituidos independientemente con uno a dos sustituyentes seleccionados del grupo integrado por alquilo C1-4; alcoxi C1-4, alquiltio C1-4, trifluorometilo; trifluorometoxi; trifluorometiltio, alcoxialquilaminosulfonilo C3-8, alcoxicarbonilo C1-4, alquilcarboniloxi C1-4, 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 uno 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; feniloxi opcionalmente sustituido con alquilo C1-4, trifluorometilo, o uno a dos sustituyentes cloro; 3,4-dimetilpirazol-1-ilo; ciano; fluor; cloro; bromo; y 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 sustituyentes 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; con la condicion de que un compuesto de formula (1) sea diferente de un compuesto donde Y es tiazol-2-ilo, Z es fenilpropilo, y s es 0; y sus enantiomeros, diastereomeros, y sales aceptables para uso farmacéutico.
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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
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.
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.
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