AR085412A1 - Moduladores de los receptores de hormonas nucleares - Google Patents

Moduladores de los receptores de hormonas nucleares

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Publication number
AR085412A1
AR085412A1 ARP120100857A ARP120100857A AR085412A1 AR 085412 A1 AR085412 A1 AR 085412A1 AR P120100857 A ARP120100857 A AR P120100857A AR P120100857 A ARP120100857 A AR P120100857A AR 085412 A1 AR085412 A1 AR 085412A1
Authority
AR
Argentina
Prior art keywords
optionally substituted
alkyl
ring
heteroaryl
cycloalkyl
Prior art date
Application number
ARP120100857A
Other languages
English (en)
Inventor
K Cusak
M Hayes
D Ihle
T Gordon
G Martinez
K Mullen
L Wang
A Ericsson
E Breinlinger
A Burchat
B Lin
A Hobson
Original Assignee
Abbott Lab
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.)
Filing date
Publication date
Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=46828945&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR085412(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Abbott Lab filed Critical Abbott Lab
Publication of AR085412A1 publication Critical patent/AR085412A1/es

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    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
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    • C07D213/72—Nitrogen atoms
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Abstract

Un compuesto de la fórmula (1) y un proceso para su preparación. Los compuestos de la presente son utilizados como terapia en el rechazo de tejidos, leucemias y linfomas, hipercortisolemia, ACV, lesiones de médula espinal, hiperglucemia, trombocitopenia y enfermedad de Little, entro otras dolencias.Reivindicación 1: Un compuesto caracterizado porque es de fórmula (1), sales aceptables farmacéuticamente, prodrogas, metabolitos biológicamente activos, isómeros, y estereoisómeros, donde el Anillo A es arilo opcionalmente sustituido, carbociclilo C5-6 saturado o parcialmente insaturado opcionalmente sustituido o heteroarilo opcionalmente sustituido; el Anillo C es carbociclilo C5-6 saturado o parcialmente insaturado opcionalmente sustituido o heterociclo opcionalmente sustituido; Q y T son en forma independiente C o N, con la condición de que no sean ambos N; el Anillo B es un anillo de siete miembros, donde X es -C(R5)2-, -C(R5)-, -C(=O)-, N(Ra)-, -O-, -S-, -S(O)-, o -S(O)2-; o cuando X es -C(R5)2-, puede formar un anillo ciclopropilo espiro al átomo de carbono al cual está unido; Y es -C(R5)2C(R5)2-, -C(R5)C(R5)2-, -C(R5)2C(R5)-, -OC(R5)2-, -N(Ra)C(R5)2-, -C(R5)2N(Ra)-, -C(=O)C(R5)2-, -C(R5)2C(=O)-, -O-C(=O)-, -C(=O)-O-, o -C(R5)2-O-; o Y es -C(R5)2- cuando Q o T es N; Z es CR4 o N; o el Anillo B es un anillo de seis miembros donde Y es -C(R5)2-; Q o T debe ser N; Z es CR4 o N; o cuando X es -C(R5)2-, puede formar un anillo ciclopropilo espiro al átomo de carbono al cual está unido; con la condición de que X-Y o Y-Z no formen enlaces O-O, N-N, N-O, C(=O)-C(=O), NC-O o O-C-O; y con la condición de que en X-Y un átomo de azufre no sea adyacente a un átomo de oxígeno o -C(=O); con la condición de que X-Y no forme -O-C(R5)2-O-, -N-C(R5)2-O- o -S-C(R5)2-O-; R1 es H, Br, Cl, F, COORa, -ORa, -O-alquileno C1-3 opcionalmente sustituido-arilo opcionalmente sustituido, -O-alquileno C1-3 opcionalmente sustituido-heteroarilo opcionalmente sustituido, -O-alquileno C1-3 opcionalmente sustituido-heterociclo opcionalmente sustituido, alquilo C1-3 opcionalmente sustituido, arilo opcionalmente sustituido, cicloalquilo C3-6 opcionalmente sustituido, heteroarilo opcionalmente sustituido, heterociclo opcionalmente sustituido, -C(O)N(Ra)(CH2)r-Rb, -N(Ra)C(O)(CH2)r-Rb, -S(O)2N(Ra)-Rb-N(Ra)S(O)2-Rb, -O-S(O)2-CF3, -N(Ra)-cicloalquilo C3-6 opcionalmente sustituido, -N(Ra)-heterociclo opcionalmente sustituido, -N(Ra)-heteroarilo opcionalmente sustituido, -N(Ra)-arilo opcionalmente sustituido, o un resto del grupo de formulas (2); R2 es -(CH2)r-arilo opcionalmente sustituido, -(CH2)r-cicloalquilo C3-6 opcionalmente sustituido, alquilo C1-3 opcionalmente sustituido, o -(CH2)r-heteroarilo opcionalmente sustituido; R3 es en forma independiente H, deuterio, -CD3, -CF3, alquinilo C2-6 opcionalmente sustituido, oxo, -ORa -OP(=O)(OH)(OH), alquilo C1-4 opcionalmente sustituido, (C(Ra)2)r-cicloalquilo C3-6 opcionalmente sustituido, -(C(Ra)2)r-arilo opcionalmente sustituido, -(C(Ra)2)r-heteroarilo opcionalmente sustituido, (C(Ra)2)r-N(Ra)-heteroarilo opcionalmente sustituido, una porción carbocíclica o heterocíclica espirocíclica unida al anillo C; R4 es H, alquilo C1-3 opcionalmente sustituido, OH o -O-alquilo C1-3 opcionalmente sustituido; R5 es en forma independiente H, F, N(Ra), ORa, cicloalquilo C3-6 opcionalmente sustituido, o alquilo C1-3 opcionalmente sustituido; Ra es en forma independiente H, cicloalquilo C3-6 opcionalmente sustituido o alquilo C1-3 opcionalmente sustituido; Rb es H, alquilo C1-3 opcionalmente sustituido, arilo opcionalmente sustituido, cicloalquilo C3-6 opcionalmente sustituido, heteroarilo opcionalmente sustituido o heterociclo opcionalmente sustituido; m es 1, 2, 3 ó 4; n es 1, 2, 3 ó 4; y r es en forma independiente 0, 1 ó 2.
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