AR079236A1 - Derivados de ciclohexano y usos de los mismos - Google Patents

Derivados de ciclohexano y usos de los mismos

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Publication number
AR079236A1
AR079236A1 ARP100104441A ARP100104441A AR079236A1 AR 079236 A1 AR079236 A1 AR 079236A1 AR P100104441 A ARP100104441 A AR P100104441A AR P100104441 A ARP100104441 A AR P100104441A AR 079236 A1 AR079236 A1 AR 079236A1
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AR
Argentina
Prior art keywords
alkyl
amino
heterocyclyl
group
substituted
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ARP100104441A
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English (en)
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Novartis Ag
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    • C07D413/10Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing aromatic rings
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Abstract

La presente proporciona además una combinacion de agentes farmacologicamente activos, y una composicion farmacéutica. utiles como inhibidores de la acetil-coenzima A-carboxilasa, utiles para tratar diabetes, obesidad, síndrome metabolico. Reivindicacion 1: Un compuesto de la formula (1) o una sal farmacéuticamente aceptable del mismo, en donde: X es CH, CR1, o N; q y n son cada uno independientemente 0, 1, 2, 3, o 4; L1 es -NHSO2-, -SO2NH-, -NHSO2NH- o -NHC(O)NH-; R1, para cada presentacion, es independientemente hidroxilo, nitro, halogeno, carboxilo, formilo, alquilo C1-7, cicloalquilo C3-8, alquenilo C2-7, alquinilo C2-7, alcoxilo C1-7, tioalquilo C1-7, cicloalcoxilo C3-8, hetero-cicliloxilo, ariloxilo C6-10, amino, alquilo C1-7-amino, di-alquilo C1-7-amino, arilo C6-10, heterociclilo de 3 a 10 miembros, heteroarilo de 5 a 10 miembros, alcanoílo C1-7, alcoxilo C1-7-carbonilo, alcanoiloxilo C1-7, alquilo C1-7-amido, arilo C61-0-amido, heterociclil-amido, carbamoílo, N-alquilo C1-7-carbamoílo, N,N-di-alquilo C1-7-carbamoílo, alcoxilo C1-7-amido, alquilo C1-7-ureido, y arilo C61-0-ureido, en donde R1 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R13 independientemente seleccionados; y en donde, cuando R1 comprende un heterociclilo o un heteroarilo que comprende -NH-, el hidrogeno del grupo -NH- puede ser opcionalmente reemplazado con un alquilo C1-7; y en donde, cuando R1 comprende un heterociclilo o un heteroarilo que comprende -N=, -S-, o ambos, el -N= puede estar sustituido con -O-, y el grupo -S- puede estar sustituido con uno o dos grupos =O; R2, para cada presentacion, se selecciona independientemente a partir del grupo que consiste en hidroxilo, ciano, alquilo C1-7, alcoxilo C1-7, alquenilo C2-7, amino, alquilo C1-7-amino, di-alquilo C1-7-amino, alquilo C1-7-amido, alcoxilo C1-7-carbonil-amino, o dos o más grupos R2 sobre átomos de carbono no adyacentes forman juntos un puente alquileno C1-4; en donde R2, para cada presentacion, puede estar independientemente sustituido de manera opcional con uno o más átomos de halogeno; R2' es hidrogeno o R2; o R2' y uno o más grupos R2 forman un puente alquileno C1-4; o R2' y R6 se pueden enlazar para formar un anillo de heterociclilo espirocíclico de 5 miembros que puede estar opcionalmente sustituido con uno o más grupos alquilo C1-7; R3 se selecciona a partir del grupo que consiste en un alquilo C1-7, cicloalquilo C3-8, arilo C6-10, un heteroarilo de 5 a 10 miembros, o un heterociclilo de 3 a 10 miembros, en donde R3 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más grupos R14 independientemente seleccionados; y en donde, cuando R3 es un heteroarilo o heterociclilo que comprende -NH-, el hidrogeno del grupo -NH- puede ser opcionalmente reemplazado con un alquilo C1-7; y en donde, cuando R3 es un heteroarilo o un heterociclilo que comprende -N=, -S-, o ambos, el -N= puede estar sustituido con -O-, y el grupo -S- puede estar sustituido con uno o dos grupos =O; R4 es hidrogeno, un alquilo C1-7, o carbamoílo, en donde el alquilo puede estar opcionalmente sustituido con uno o más sustituyentes, los cuales se pueden seleccionar independientemente a partir del grupo que consiste en deuterio, hidroxilo, amino, halogeno, carboxilo, alcoxilo C1-7, alcoxilo C1-7-carbonilo, fosfono-oxilo, un péptido que tiene de 1 a 3 aminoácidos, y alcanoiloxilo C1-7, en donde el alcanoiloxilo puede estar opcionalmente sustituido con uno o más grupos carboxilo, amino, N-alquilo C1-6-amino, N,N-di-alquilo C1-6-amino, o una cadena lateral de aminoácidos; R5 es hidrogeno o un alquilo C1-7; R6 es hidrogeno o alquilo C1-7; o R6 y cualquiera de R4 o R5 se pueden enlazar para formar un heterociclilo de 3 a 7 miembros, en donde el heterociclilo puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más R15; y en donde, cuando el heterociclilo comprende -NH-, el hidrogeno del grupo -NH- puede ser opcionalmente reemplazado con R16; y en donde, cuando el heterociclilo comprende -N=, -S-, o ambos, el -N= puede estar sustituido con -O-, y el grupo -S- puede estar sustituido con uno o dos grupos =O; R13, para cada presentacion, es independientemente deuterio, halogeno, hidroxilo, oxo, carboxilo, alquilo C1-7, cicloalquilo C3-8, alcoxilo C1-7, arilo C6-10, heterociclilo de 3 a miembros, heteroarilo de 5 a 10 miembros, amino, alquilo C1-7-amino, di-alquilo C1-7-amino, alcoxilo C1-7-carbonilo, carbamoílo, en donde R13 está opcionalmente sustituido sobre uno o más átomos de carbono con uno o más grupos R17 independientemente seleccionados; y en donde, cuando R13 es un heterociclilo o un heteroarilo que comprende -NH-, el hidrogeno del grupo -NH- puede ser opcionalmente reemplazado con un alquilo C1-7; y en donde, cuando R13 es un heterociclilo o heteroarilo que comprende -N=, -S-, o ambos, el -N= puede estar sustituido con -O-, y el grupo -S- puede estar sustituido con uno o dos grupos =O; R14, para cada presentacion, es independientemente halogeno; R15, para cada presentacion, se selecciona independientemente a partir del grupo que consiste en hidroxilo, oxo, carboxilo, alquilo C1-7, y alcoxilo C1-7-carbonilo; o dos R15 sobre átomos de carbono adyacentes pueden formar un fenilo fusionado; R16, para cada presentacion, se selecciona independientemente a partir del grupo que consiste en alcanoílo C1-7, arilo C6-10-carbonilo, heteroaril-carbonilo, alcoxilo C1-7-carbonilo, heteroarilo de 5 a 10 miembros, y alquilo C1-7-sulfonilo, en donde R16 puede estar opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados a partir del grupo que consiste en carboxilo, amino, alquilo C1-7-amino, di-alquilo C1-7-amino, y alcoxilo C1-7-carbonilo; y R17, para cada presentacion, se selecciona independientemente a partir de ciano, halogeno, hidroxilo, carboxilo, alquilo C1-7, alcoxilo C1-7, amino, alquilo C1-7-amino, di-alquilo C1-7-amino, alcoxilo C1-7-carbonilo, heterociclilo de 3 a 10 miembros, en donde R17 puede estar opcionalmente sustituido sobre uno o más átomos de carbono con uno o más grupos halogeno, trifluoro-metilo, carboxilo, o alcoxilo C1-4-carbonilo independientemente seleccionados; y en donde, cuando R17 es un heterociclilo que comprende -NH-, el hidrogeno del grupo -NH- puede ser opcionalmente reemplazado con un alquilo C1-7; y en donde, cuando R17 es un heterociclilo que comprende -N=, -S-, o ambos, el -N= puede estar sustituido con -O- , y el grupo -S- puede estar sustituido con uno o dos grupos =O.
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