ES2655091T3 - Derivados del ácido pirrolidíncarboxílico como agonistas del receptor 43 acoplado a proteína G (GPR43), composición farmacéutica y métodos para su uso en el tratamiento de trastornos metabólicos - Google Patents

Derivados del ácido pirrolidíncarboxílico como agonistas del receptor 43 acoplado a proteína G (GPR43), composición farmacéutica y métodos para su uso en el tratamiento de trastornos metabólicos Download PDF

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ES2655091T3
ES2655091T3 ES10792934T ES10792934T ES2655091T3 ES 2655091 T3 ES2655091 T3 ES 2655091T3 ES 10792934 T ES10792934 T ES 10792934T ES 10792934 T ES10792934 T ES 10792934T ES 2655091 T3 ES2655091 T3 ES 2655091T3
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heteroaryl
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Hamid Hoveyda
Didier Schils
Ludivine Zoute
Julien Parcq
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Ogeda SA
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Abstract

Un compuesto de fórmula I:**Fórmula** y sales y solvatos farmacéuticamente aceptables del mismo, en donde R1 y R2 son H, D es C>=O; L2 es enlace sencillo; R es H o alquilo lineal o ramificado, arilo, dioxoleno; Ar1 es un grupo arilo o heteroarilo de 5 a 6 miembros, grupo cicloalquilo de 3 a 6 miembros, o un grupo alquilo C3-C6 lineal o ramificado, cada uno de los cuales está opcionalmente sustituido con uno o más grupos seleccionados de halo, ciano, alquilo, haloalquilo, cicloalquilo, arilo, heteroarilo, hidroxilo, alcoxi, haloalcoxilo, amino, alquilamino, carboxilo, alcoxicarbonilo, alquilcarboniloxilo, alquilcarbonilamino, haloalquilcarbonilamino, carbamoilo, hidroxicarbamoilo, alquilcarbamoilo, carbamoilamino, alquilcarbamoilamino, alquilsulfonilo, haloalquilsulfonilo, sulfamoilo, alquilsulfamoilo, alquilsulfonilamino, haloalquilsulfonilamino o dos sustituyentes forman un grupo alquilendioxi o un grupo haloalquilendioxi, cada uno de dichos sustituyentes arilo o heteroarilo está opcionalmente sustituido con uno o más sustituyentes adicionales seleccionados entre halo, ciano, alquilo, haloalquilo, hidroxilo, alcoxi, haloalcoxi; Ar2 es un grupo arilo o heteroarilo, cicloalquilo o heterociclilo monocíclico, cada uno de los cuales está opcionalmente sustituido con uno o más grupos seleccionados de halo, ciano, nitro, alquilo, haloalquilo, cicloalquilo, cicloalquilalquilo, heteroalquilo, heterociclilo, heterociclilalquilo, arilo, aralquilo, heteroarilo, benzoxazol-2-ilo, heteroarilalquilo, hidroxilo, hidroxialquilo, alcoxi, haloalcoxi, alcoxialcoxi, cicloalquiloxi, cicloalquilalquiloxi, heterocicliloxi, ariloxi, heteroariloxi, alcoxialquilo, haloalcoxialquilo, arilalquiloxi, heteroarilalquiloxi, ariloxialquilo, heteroariloxialquilo, amino, alquilamino, arilcarbonilo, carboxi, alcoxicarbonilo, ariloxicarbonilo, heteroariloxicarbonilo, alquilcarboniloxi, arilcarboniloxi, heteroarilcarboniloxi, alquilcarbonilamino, carbamoílo, hidroxicarbamoílo, alquilcarbamoílo, arilcarbamoílo, heteroarilcarbamoilo, carbamoilamino, alquilcarbamoilamino, alquilsulfonilo, arilsulfonilo, heteroarilsulfonilo, sulfamoílo, alquilsulfamoílo, arilsulfamoilo, heteroarilsulfamoiIo, alquilsulfonilamino, arilsulfonilamino, heteroarilsulfonilamino, oxo, o dos sustituyentes forman un grupo alquilendioxi o un grupo haloalquilendioxi, o condensados con el grupo arilo, heteroarilo o cicloalquilo pueden ser una o más unidades estructurales arilo o heteroarilo, cada uno de dichos sustituyentes está opcionalmente sustituido con uno o más sustituyentes seleccionados entre halo, ciano, nitro, alquilo, hidroxialquilo, haloalquilo, cianometilo, cicloalquilo, heterociclilo, arilo opcionalmente sustituido con un grupo cloro o metilo, heteroarilo, heteroalquilo, hidroxilo, alcoxilo, alcoxialquilo, alcoxialcoxilo, haloalcoxilo, cicloalquiloxilo, cicloalquilalquiloxilo, ariloxilo, aralquiloxi opcionalmente sustituido por un grupo fluoro, carboxi, alcoxicarbonilo, alquilcarboniloxi, amino, alquilamino, alquilcarbonilamino, haloalquilcarbonilamino, carbamoílo, hidroxicarbamoílo, alquilcarbamoilo, carbamoilalquiloxi, carbamoilamino, alquilcarbamoilamino, carbamimidoilo, hidroxicarbamimidoilo, alquilsulfonilo, haloalquilsulfonilo, cicloalquilsulfonilo, heterociclilsulfonilo, arilsulfonilo, sulfamoílo , alquilsulamoilo, alquilsulfonilamino, haloalquilsulfonilamino, oxo y haloalcoxialquilo; R3 es H, ciano, alquilo, hidroxialquilo, aralquilo, alcoxialquilo, acetilo, arilsulfonilo; R3' es H o alquilo C1-C4; R4 es H, ciano, alquilo C1-C4; en donde, a menos que se indique lo contrario: alquilo comprende de 1 a 6 átomos de carbono; cicloalquilo comprende de 3 a 10 átomos de carbono; heterociclilo contiene de 3 a 10 átomos en el anillo y conteniendo cada anillo un heteroátomo puede tener 1, 2, 3 o 4 heteroátomos seleccionados de átomos de N, O y/o S;
ES10792934T 2009-12-18 2010-12-17 Derivados del ácido pirrolidíncarboxílico como agonistas del receptor 43 acoplado a proteína G (GPR43), composición farmacéutica y métodos para su uso en el tratamiento de trastornos metabólicos Active ES2655091T3 (es)

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EP09306270 2009-12-18
US37337010P 2010-08-13 2010-08-13
US37601310P 2010-08-23 2010-08-23
PCT/EP2010/070040 WO2011073376A1 (en) 2009-12-18 2010-12-17 Pyrrolidine or thiazolidine carboxylic acid derivatives, pharmaceutical composition and methods for use in treating metabolic disordersas as agonists of g- protein coupled receptor 43 (gpr43)

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BR112012018374B1 (pt) * 2009-12-18 2021-09-21 Epics Therapeutics Derivados de ácido carboxílico de pirrolidina ou tiazolidina para distúrbios metabólicos como agonistas de receptor 43 acoplado à proteína g (gpr43), seu processo de preparação e composição farmacêutica
PT2800738T (pt) 2012-01-06 2020-06-23 Novartis Ag Compostos heterocíclicos e métodos para a utilização dos mesmos
AR091739A1 (es) 2012-07-11 2015-02-25 Elcelyx Therapeutics Inc Composiciones y metodos para reducir el riesgo cardiometabolico
WO2014134391A1 (en) 2013-02-28 2014-09-04 Bristol-Myers Squibb Company Phenylpyrazole derivatives as potent rock1 and rock2 inhibitors
AR094929A1 (es) 2013-02-28 2015-09-09 Bristol Myers Squibb Co Derivados de fenilpirazol como inhibidores potentes de rock1 y rock2
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