AR059727A1 - Moduladores de 11- beta hidroxil esteriode deshidrogenasa de tipo 1, composiciones farmaceuticas de los mismos , y metodos de uso de los mismos - Google Patents

Moduladores de 11- beta hidroxil esteriode deshidrogenasa de tipo 1, composiciones farmaceuticas de los mismos , y metodos de uso de los mismos

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Publication number
AR059727A1
AR059727A1 ARP070100888A ARP070100888A AR059727A1 AR 059727 A1 AR059727 A1 AR 059727A1 AR P070100888 A ARP070100888 A AR P070100888A AR P070100888 A ARP070100888 A AR P070100888A AR 059727 A1 AR059727 A1 AR 059727A1
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Argentina
Prior art keywords
optionally substituted
cycloalkyl
heterocycloalkyl
nrc
alkyl
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ARP070100888A
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English (en)
Inventor
Jincong Zhuo
Meizhong Xu
Yun-Long Li
Chunhong He
Wenqing Yao
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Incyte Corp
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Publication of AR059727A1 publication Critical patent/AR059727A1/es

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    • C07C323/61—Thiols, sulfides, hydropolysulfides or polysulfides substituted by halogen, oxygen or nitrogen atoms, or by sulfur atoms not being part of thio groups containing thio groups and carboxyl groups bound to the same carbon skeleton having the sulfur atom of at least one of the thio groups bound to a carbon atom of a ring other than a six-membered aromatic ring of the carbon skeleton
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    • C07D233/66—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings having two double bonds between ring members or between ring members and non-ring members with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D233/72—Two oxygen atoms, e.g. hydantoin
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    • C07D401/04—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings directly linked by a ring-member-to-ring-member bond
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Abstract

Inhibidores de 11-beta hidroxil esteroide deshidrogenada de tipo 1 y composiciones farmacéuticas que los contienen. Los compuestos de la presente pueden ser utiles para el tratamiento de diversas enfermedades asociadas con la expresion o actividad de la 11-beta hidroxil esteroide deshidrogenada de tipo 1. Reivindicacion 1: Un compuesto caracterizado porque responde a la formula (1), (2), (3), (4), (5), (6) o (7), o sal aceptable para uso farmacéutico o prodroga del mismo, en donde Cy es arilo, heteroarilo, cicloalquilo, o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2, 3, 4 o 5 -W-X-Y-Z; el átomo J que forma un anillo es N o C; L se encuentra ausente, o es alquenilenilo C1-6, (CR1R2)q, (CR1R2)q1O(CR1R2)q2, (CR1R2)q1S(CR1R2)q2, (CR1R2)q1SO2(CR1R2)q2, (CR1R2)q1SO(CR1R2)q2, (CR1 R2)q1SO2NR3(CR1R2)q2, (CR1R2)q1COO(CR1R2)q2, (CR1R2)q1CO(CR1 R2)q2, (CR1R2)q1 NR3aCONR3(CR1R2)q2, o (CR1R2)q1CONR3(CR1R2)q2, en donde el alquenilenilo C1-6 está opcionalmente sustituido por 1,2, 3, 4, 5 o 6 R1a; M1 es CH, CH2, C(O), O, SO, SO2, OC(O), NH, NHC(O), o NHSO2; M2 y M3 se seleccionan en forma independiente entre ausente, C(O), SO, SO2, O, OC(O), NH, NHC(O), y NHSO2, con la salvedad de que al menos uno de M2 y M3 es distinto de ausente; T es NR8, CH2 o O; el anillo B es un grupo cicloalquilo de 3 a 14 miembros o un grupo heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2, 3, 4 o 5 -Wa-Xa-W'-X'-Y-Z'; ------ es una union simple o doble; RL es Cy o alquilo C1-6, en donde el alquilo C1-6 está opcionalmente sustituido por 1, 2, 3, 4 o 5 -W-X-Y-Z; R1 y R2 se seleccionan en forma independiente entre H, halo, alquilo C1-6, haloalquilo C1-6, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', Sra', C(O)Rb, C(O)NRc'Rd', C(O)ORa', OC(O)Rb, OC(O)NRC'Rd', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', y S(O)2NRc'Rd'; cada R1a se selecciona en forma independiente entre halo, alquilo C1-6, haloalquilo C1-6, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', Sra', C(O)Rb, C(O)NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', y S(O)2NRc'Rd'; R3 y R3a se seleccionan en forma independiente entre H, alquilo C1-8, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo y heterocicloalquilalquilo, en donde cada uno de los alquilo C1-8, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo; heterocicloalquilo y heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; R4 es H, O(O)ORb', C(O)NRc'Rd', ORb', SRb', S(O)Ra', S(O)NRc'Rd', S(O)2Ra', S(O)2NRc'Rd', alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, en donde cada uno de los alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 R11, R5 es H o alquilo C1-6, en donde el alquilo C1-6 está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R4 y R5 junto con la porcion -C-C(O)-N(R6)- interpuesta al cual están unidos forman un grupo heterocicloalquilo de 4 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z';R6 es alquilo C1-6, arilo, cicloalquilo, heteroarilo o heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2 o 3 -W'-X'-Y'-Z'; o R5 y R6 junto con el átomo de N al cual están unidos forman a un grupo heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; R7 es H, C(O)ORb', C(O)NRc'Rd', ORb', SRb', S(O)Ra', S(O)NRc'Rd', S(O)2Ra', S(O)2NRc'Rd', alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, en el alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 R11, R8 es H, alquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo o heterocicloalquilalquilo, en donde cada uno de los alquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo y heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R7 y R8 junto con los dos átomos adyacentes al cual están unidos forman a un grupo heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; R9 es H, alquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo o heterocicloalquilalquilo, en donde cada uno de los alquilo C1-6, arilalquilo, heteroarilalquilo, cicloalquilo, cicloalquilalquilo, heterocicloalquilo y heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R8 y R9 junto con los dos átomos adyacentes al cual están unidos forman a un grupo heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R7 y R9 junto con la porcion -C-T-C(O)- interpuesta al cual están unidos forman un grupo heterocicloalquilo de 4 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R4 y R9 junto con la porcion -C-S(O)2- interpuesta al cual están unidos forman un grupo heterocicloalquilo de 4 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; o R9 es NR9aR9b; R9a y R9b son cada uno, en forma independiente, H, alquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, cada uno opcionalmente sustituido con 1, 2 o 3 -W'- X'-Y'-Z'; o R9a y R9b junto con el átomo de N al cual están unidos forman a un grupo heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 -W'-X'-Y'-Z'; cada R10 es independientemente OC(O)Ra', OC(O)Orb', OC(O)NRc'Rd', C(O)ORb', C(O)NRc'Rd', NRc'Rd', NRc'C(O)Ra', NRc'C(O)ORb', NRc'S(O)2Rb', S(O)Ra', S(O)NRc'Rd', S(O)2Ra', S(O)2NRc'Rd', ORb', SRb', alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo o heterocicloalquilalquilo, en donde cada uno de los alquilo C1-10, haloalquilo C1-10, alquenilo C2-10, alquinilo C2-10, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, arilalquilo, heteroarilalquilo, cicloalquilalquilo y heterocicloalquilalquilo está opcionalmente sustituido por 1, 2 o 3 R11; o dos R10 junto con el mismo átomo de carbono al cual están unidos forman un grupo cicloalquilo o heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 R11, o dos R10 junto con el mismo átomo de carbono al cual están unidos forman un grupo carbonilo; o dos R10 adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11, o R10 y -L-Cy junto con el mismo átomo de carbono al cual están unidos forman un grupo cicloalquilo o heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o3 R11, o R10 y -L-Cy adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o R10 y -L-RL junto con el mismo átomo de carbono al cual están unidos forman un grupo cicloalquilo o heterocicloalquilo de 3 a 14 miembros el cual está opcionalmente sustituido por 1, 2 o 3 R11, o R10 y -LRL adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o r4 y R10 adyacentes junto con los das átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o R7 y R10 adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o R4 y -L-Cy adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o R7 y -L-Cy adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11, o R4 y -L-RL adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; o R7 y -L-RL adyacentes junto con los dos átomos a los cuales están unidos forman un grupo cicloalquilo fusionado de 3 a 14 miembros o un grupo heterocicloalquilo fusionado de 3 a 14 miembros el cual está opcionalmente sustituido por R11; cada R11 es independientemente halo, alquilo C1-6, haloalquilo C1-6, arilo, cicloalquilo, heteroarilo, heterocicloalquilo, CN, NO2, ORa', SRa', C(O)Rb', C(O)NRc'Rd', C(O)ORa', OC(O)Rb', OC(O)NRc'Rd', NRc'Rd', NRc'C(O)Rd', NRc'C(O)ORa', NRc'S(O)2Rb', S(O)Rb', S(O)NRc'Rd', S(O)2Rb', o S(O)2NRc'Rd'; W, W', Wö y Wa se seleccionan en forma independiente entre ausente, alquilenilo C1-6, alquenilenilo C2-6, alquinilenilo C2-6, O, S, NRe, CO, COO
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