AR070526A1 - Derivados de urea de benzomorfanos y estructuras relacionadas, una composicion farmaceutica que incluye al compuesto y un procedimiento de preparacion del mismo - Google Patents

Derivados de urea de benzomorfanos y estructuras relacionadas, una composicion farmaceutica que incluye al compuesto y un procedimiento de preparacion del mismo

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AR070526A1
AR070526A1 ARP090100476A ARP090100476A AR070526A1 AR 070526 A1 AR070526 A1 AR 070526A1 AR P090100476 A ARP090100476 A AR P090100476A AR P090100476 A ARP090100476 A AR P090100476A AR 070526 A1 AR070526 A1 AR 070526A1
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Argentina
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alkyl
piperazin
alkyloxy
oxo
het
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ARP090100476A
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English (en)
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Matthias Eckhardt
Stefan Peters
Bradford S Hamilton
Frank Himmelsbach
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Boehringer Ingelheim Int
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Publication of AR070526A1 publication Critical patent/AR070526A1/es

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Abstract

Los compuestos son inhibidores de la 11b-hidroxiesteroide deshidrogenasa (HSD) 1 y, por lo tanto, son adecuados para el tratamiento y la prevencion de enfermedades que pueden estar influenciadas por la inhibicion de esta enzima, tales como enfermedades metabolicas, en particular diabetes de tipo 2, obesidad y dislipidemia. Reivindicacion 1: Compuestos caracterizados porque tienen la formula (1) en la que X representa CH o N; m, n, o, independientemente unos de otros, representan 0, 1 o 2; donde la estructura de nucleo C5+m+n-azacicloalqueno de formula general (1), incluyendo el grupo puente -(CH2)o-, está opcionalmente sustituida con 1, 2 o más sustituyentes independientemente seleccionados unos de otros entre el grupo que consiste en R11y R12; A representa un anillo benzo, pirido, pirrolo, furo, tieno, piridazino, pirimido o pirazino, donde cada uno de dichos anillos está opcionalmente sustituido con uno o más sustituyentes independientemente seleccionados de R1, y donde 2 átomos de C adyacentes de cada uno de dichos anillos están opcionalmente sustituidos con R2 y R3; o un anillo pirazolo, imidazo, oxazolo, tiazolo, isoxazolo o isotiazolo donde cada uno de dichos anillos está opcionalmente sustituido con R1; o un anillo 1,2,3-triazolo opcionalmente sustituido con RN; y B representa un grupo azacicloalqu-1-ilo monocíclico de 3 a 8 miembros, espirocíclico de 7 a 12 miembros, bicíclico de 6 a 12 miembros o tricíclico de 9 a 15 miembros, que está saturado o parcial o totalmente insaturado, donde 1 o 2 grupos -CH2- pueden estar reemplazados por -NRN-, en donde 1 a 4 grupos -CH2- pueden estar reemplazados independientemente unos de otros por O, S, carbonilo o sulfonilo, en donde 1 o 2 grupos -CH= pueden estar reemplazados por -N=, y en donde dicho grupo azacicloalquilo puede estar sustituido con uno o más sustituyentes independientemente seleccionados unos de otros de L1, donde dicho grupo azacicloalquilo puede estar sustituido con 1 o 2 sustituyentes independientemente seleccionados uno del otro de L2, donde 2 átomos de C adyacentes de dicho grupo azacicloalquilo pueden estar sustituidos con L3 y L4, y donde 2 átomos de C adyacentes de dicho grupo azacicloalquilo pueden estar sustituidos con L5 y L6; RN, independientemente unos de otros, representa hidrogeno, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, (het)arilo, alquilcarbonilo C1-4, alquilsulfonilo C1-4, (het)arilcarbonilo, (het)arilsulfonilo, donde cada grupo alquilo, alquenilo y alquinilo puede estar mono o polisustituido con fluor, y puede estar monosustituido con hidroxi, alcoxi C1-4, alquilsulfanilo C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, amino, alquilamino C1-4, di-(alquil C1-4)amino, alquilcarbonilamino C1-4, ciano, carboxi, alcoxicarbonilo C1-4, aminocarbonilo, alquilaminocarbonilo C1-4, di-(alquil C1-4)aminocarbonilo o (het)arilo; R1, independientemente uno de otro, representa fluor, cloro, bromo, yodo, ciano, nitro, alquilo C1-4, hidroxi, alquiloxi C1-4, difluorometilo, trifluorometilo, difluorometoxi, trifluorometoxi, trifluorometil-hidroxi-alquilo C1-2, 2,2,2-trifluoro-1-hidroxi-1-(trifluorometil)etilo, cicloalquilo C3-6, cicloalquiloxi C3-6, cicloalquil C3-6-alquilo C1-3, cicloalquil C3-6-alquiloxi C1-3, tetrahidrofurano-3-iloxi, tetrahidropiran-3-iloxi, tetrahidropiran-4-iloxi, tetrahidrofuranil-alquiloxi C1-3, tetrahidropiranil-alquiloxi C1-3, (het)arilo, (het)ariloxi, (het)aril-alquilo C1-3, (het)aril-alquiloxi C1-3, (het)ariloxi-alquilo C1-3, alquil C1-3-carbonilo, (het)aril-carbonilo, amino, alquilamino C1-4, di-(alquil C1-4)amino, pirrolidin-1-ilo, 2-oxo-pirrolidin-1-ilo, piperidin-1-ilo, 2-oxo-piperidin-1-ilo, morfolin-4-ilo, 3-oxo-morfolin-4-ilo, piperazin-1-ilo, 2-oxo-piperazin-1-ilo, 3-oxo-piperazin-1-ilo, 4-(alquil C1-4)-piperazin-1-ilo, 4-(alquil C1-4 carbonil)-piperazin-1-ilo, 4-(cicloalquilcarbonil C3-6)-piperazin-1-ilo, 4-(alquiloxicarbonil C1-4)-piperazin-1-ilo, 4-(alquilsulfonil C1-4)-piperazin-1-ilo, 2-oxo-4-(alquil C1-4)-piperazin-1-ilo, 3-oxo-4-(alquil C1-4)-piperazin-1-ilo, alquil C1-4-carbonilamino, (het)aril-carbonilamino, (het)aril-alquil C1-4-carbonilamino, alquiloxi C1-4-carbonilamino, aminocarbonilamino, alquil C1-4-aminocarbonilamino, di(alquil C1-4)aminocarbonilamino, pirrolidin-1-il-carbonilamino, piperidin-1-il-carbonilamino, morfolin-4-iI-carbonilamino, piperazin-1-il-carbonilamino, 4-(alquil C1-4)-piperazin-1-il-carbonilamino, alquil C1-4-sulfonilamino, aminosulfonilamino, alquil C1-4 amino-sulfonilamino, di-(alquil C1-4)amino-sulfonilamino, pirrolidin-1-il-sulfonilamino, piperidin-1-il-sulfonilamino, morfolin-4-il-sulfonilamino, piperazin-1-il-sulfonilamino, 4-(alquil C1-4)-piperazin-1-il-sulfonilamino, (alquiloxi C1-4-carbonilamino)carbonilamino, (het)arilsulfonilamino, (het)aril-alquil C1-4-sulfonilamino, N-(alquil C1-4)-alquil C1-4-carbonilamino, N-(alquil C1-4)-(het)arilcarbonilamino, N-(alquil C1-4)-(het)aril-alquil C1-4-carbonilamino, N-(alquil C1-4)-alquiloxi C1-4-carbonilamino, N-(aminocarbonil)-alquilamino C1-4, N-(alquil C1-4-aminocarbonil)-alquilamino C1-4, N-[di(alquil C1-4aminocarbonil]-alquilamino C1-4, N-(alquil C1-4)-alquil C1-4-sulfonilamino, N-(alquil C1-4-(het)arilsulfonilamino, N-(alquil C1-4-(het)aril-alquil C1-4-sulfonilamino, oxo-imidazolidin-1-ilo, 2,4-dioxo-imidazolidin-1-ilo, 2,5-dioxo-imidazolidin-1-ilo, 2-oxo-hexahidropirimidin-1-ilo, donde el átomo de nitrogeno de la posicion 3 de los grupos mencionados anteriormente está opcionalmente sustituido con metilo o etilo, (hidroxiimino)aminometilo, (alquiloxiimino C1-3)aminometilo, carboxi, alquiloxi C1-4-carbonilo, aminocarbonilo, alquil C1-4-aminocarbonilo, di-(alquil C1-4)-aminocarbonilo, pirrolidin-1-il-carbonilo, piperidin-1-il-carbonilo, morfolin-4-il-carbonilo, piperazin-1-iI-carbonilo, 4-(alquil C1-4-piperazin-1-il-carbonilo, carboxi-alquilo C1-4, alquiloxi C1-4-carbonil-alquilo C1-4, ciano-alquilo C1-4, aminocarbonil-alquilo C1-4, alquil C1-4-aminocarbonil-alquilo C1-4, di-(alquil C1-4)-aminocarbonil-alquilo C1-4, pirrolidin-1-il-carbonil-alquilo C1-4, piperidin-1-il-carbonilalquilo C1-4, morfolin-4-il-carbonil-alquilo C1-4, piperazin-1-il-carbonil-alquilo C1-4, 4-(alquil C1-4-piperazin-1-il-carbonil-alquilo C1-4, carboxi-alquiloxi C1-4, alquiloxi C1-4-carbonil-alquiloxi C1-4, ciano-alquiloxi C1-4, aminocarbonil-alquiloxi C1-4, alquil C1-4-aminocarbonil-alquiloxi C1-4, di-(alquil C1-4)-aminocarbonil-alquiloxi C1-4, pirrolidin-1-il-carbonil-alquiloxi C1-4, piperidin-1-il-carbonilalquiloxi C1-4, morfolin-4-iI-carbonil-alquiloxi C1-4, piperazin-1-il-carbonil-alquiloxi C1-4, 4-(alquil C1-3)-piperazin-1-il-carbonil-alquiloxi C1-4, hidroxi-alquilo C1-4, alquiloxi C1-4-alquilo C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, di-(alquil C1-4)-amino-alquilo C1-4, pirrolidin-1-il-alquilo C1-4, alquil C1-4carbonil-amino-alquilo C1-4, N-(alquil C1-4)-alquil C1-4carbonil-amino-alquilo C1-4, 2-oxo-pirrolidin-1 -il-alquilo C1-4, piperidin-1-il-alquilo C1-4, 2-oxo-piperidin-1-il-alquilo C1-4, morfolin-4-il-alquilo C1-4, 3-oxo-morfolin-4-iI-alquilo C1-4, piperazin-1-il-alquilo C1-4, 2-oxo-piperazin-1-il-alquilo C1-4, 3-oxo-piperazin-1-il-alquilo C1-4-4-(alquil C1-4)-piperazin-1-il-alquilo C1-4, 2-oxo-4-(alquil C1-4)-piperazin-1-iI-alquilo C1-4, 3-oxo-4-(alquil C1-4)-piperazin-1-il-alquilo C1-4, hidroxi-alquiloxi C1-4, alquiloxi C1-4-alquiloxi C1-4, alquilsulfanil C1-4-alquiloxi C1-4, alquilsulfinil C1-4-alquiloxi C1-4, alquilsulfonil C1-4-alquiloxi C1-4, amino-alquiloxi C1-4, alquilamino C1-4-alquiloxi C1-4, di-(alquil C1-4)-amino-alquiloxi C1-4, pirrolidin-1-il-alquiloxi C1-4, 2-oxo-pirrolidin-1-il-alquiloxi C1-4, piperidin-1-il-alquiloxi C1-4, 2-oxo-piperidin-1-il- alquiloxi C1-4, morfolin-4-iI-alquiloxi C1-4, 3-oxo-morfolin-4-il-alquiloxi C1-4, piperazin-1-il-alquiloxi C1-4, 2-oxo-piperazin-1-iI-alquiloxi C1-4, 3-oxo-piperazin-1-il-alquiloxi C1-4, 4-(alquil C1-4)-piperazin-1-il-alquiloxi C1-4, 2-oxo-4-(alquil C1-4-piperazin-1-il-alquiloxi C1-4, 3-oxo-4-(alquil C1-4)-piperazin-1-il-alquiloxi, alquilsulfanilo C1-4, alquilsulfinilo C1-4, alquilsulfonilo C1-4, alquilsulfoniloxi C1-4, (het)arilsulfonilo, (het)arilsulfoniloxi, trifluorometilsulfanilo, trifluorometilsulfinilo, trifluorometilsulfonilo, cicloalquilsulfanilo C3-6, cicloalquilsulfinilo C3-6, cicloalquilsulfonilo C3-6, cicloalquil C3-6-alquilsulfanilo C1-3, cicloalquil C3-6-alquilsulfinilo C1-3, cicloalquil C3-6-alquilsulfonilo C1-3, aminosulfonilo, alquil C1-4-aminosulfonilo, di-(alquil C1-4)-aminosulfonilo, pirrolidin-1-il-sulfonilo, piperidin-1-il-sulfonilo, morfolin-4-il-sulfonilo, piperazin-1-il-sulfonilo o 4-(alquil C1-4)-piperazin-1-il-sulfonilo, donde los anillos cicloalquilo y heterociclos saturados anteriormente mencionados están opcionalmente sustituidos con uno o dos grupos seleccionados, independientemente uno del otro, entre fluor, alquilo C1-3, alcoxi C1-3, alcoxi C1-3-alquilo C1-3, hidroxi; R2, R3 están unidos entre sí para formar un grupo puente metilenodioxi, etilenodioxi o alquileno C3-5, que puede estar mono o disustituido con metilo, y que puede estar mono o polifluorado; o R2, R3 forman, combinados con los átomos de carbono a los que están unidos, un anillo benzo, pirido, pirimido, pirazino, piridazino, pirrolo, furano, tieno, pirazolo, imidazo, triazolo, oxazolo, tiazolo, isoxazolo o isotiazolo, en donde cada uno de dichos anillos puede estar sustituido con uno o más sustituyentes seleccionados, independientemente unos de otros, de RP; RP representa halogeno, alquilo, hidroxi-alquilo C1-4, alquiloxi C1-3-alquilo C1-3, cicloalquilo C3-6, hidroxi-cicloalquilo C4-6, alquiloxi C1-3-cicloalquilo C3-6, azetidinilo, 1-(alquil C1-3)-azetidinilo, 1-(alquilcarbonil C1-3)-azetidinilo, pirrolidinilo, 1-(alquil C1-3)-pirrolidinilo, 1-(alquilcarbonil C1-3)-pirrolidinilo, piperidinilo, 1-(alquil C1-3)-piperidinilo, 1-(alquilcarbonil C1-3)piperidinilo, tetrahidrofuranilo, tetrahidropiranilo, difluorometilo, trifluorometilo, ciano, nitro, amino, alquilamino C1-3, d
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