AR075005A1 - Derivados de sulfonamida - Google Patents

Derivados de sulfonamida

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Publication number
AR075005A1
AR075005A1 ARP100100053A ARP100100053A AR075005A1 AR 075005 A1 AR075005 A1 AR 075005A1 AR P100100053 A ARP100100053 A AR P100100053A AR P100100053 A ARP100100053 A AR P100100053A AR 075005 A1 AR075005 A1 AR 075005A1
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AR
Argentina
Prior art keywords
alkyl
halo
alkoxy
hydroxy
alkylamino
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ARP100100053A
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English (en)
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Icagen Inc
Pfizer Ltd
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Family has litigation
First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=41818828&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR075005(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Icagen Inc, Pfizer Ltd filed Critical Icagen Inc
Publication of AR075005A1 publication Critical patent/AR075005A1/es

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    • A61K31/445—Non condensed piperidines, e.g. piperocaine
    • A61K31/4523—Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
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    • A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
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    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
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  • Plural Heterocyclic Compounds (AREA)
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  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
  • Thiazole And Isothizaole Compounds (AREA)
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Abstract

Compuestos de formula (1), procedimientos para su preparacion, a intermedios usados en su preparacion, y a composiciones que contienen dichos compuestos y a los usos de dichos compuestos, en particular para el tratamiento del dolor. Reivindicacion 1: Compuestos de la formula (1) en la que Z es Het2, opcionalmente sustituido en un átomo de carbono del anillo con uno o más sustituyentes seleccionados entre el grupo constituido por halo, ciano, alquilo C1-4, halo-alquilo C1-4, alcoxi C1-4, halo-alcoxi C1-4, cicloalquilo C3-8, cicloalquil C3-8-alquilo C1-4, alquil C1-4-S-, amino, alquilamino C1-4, di-alquilamino C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4 y di[alquil C1-4]amino-alquilo C1-4; y/o Het2 esté opcionalmente sustituido en un átomo de nitrogeno del anillo con alquilo C1-4, halo-alquilo C1-4 y cicloalquilo C3-8; con la condicion de que Z no sea tetrazolilo; cada uno de Y1, Y2, Y3 e Y4 son independientemente CH, CR1 o N, con la condicion de que no más de dos de Y1, Y2, Y3 e Y4 sean N; cada R1 se selecciona independientemente entre el grupo constituido por halo, ciano, amino, hidroxi, alquilo C1-4, halo-alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4, halo-alcoxi C1-4, alcoxi C1-4-alquilo C1-4, C(O)H, -C(O)-alquilo C1-4 y -C(O)N(R2)2; cada R2 es independientemente hidrogeno, alquilo C1-4, halo-alquilo C1-4, hidroxi-alquilo C1-4 o cicloalquilo C3-6; o donde un nitrogeno está sustituido con dos grupos R2, cada uno independientemente seleccionado entre alquilo C1-4, halo-alquilo C1-4 o hidroxi-alquilo C1-4, que pueden tomarse junto con el átomo de N al que están unidos para formar un anillo de 4 a 6 miembros que, cuando se forman de esta manera, por lo tanto, pueden sustituirse opcionalmente con hidrogeno, alquilo, halo, hidroxi, hidroxialquilo o haloalquilo; B es fenilo o Het2, en el que, cuando B es Het2, está unido al conector oxi en un átomo de carbono del anillo y donde B además está opcionalmente sustituido en un átomo de carbono del anillo con uno o más sustituyentes seleccionados entre el grupo constituido por halo, ciano, hidroxi, alquilo C1-4, halo-alquilo C1-4, alcoxi C1-4, halo-alcoxi C1-4, ciano-alquilo C1-4, amino, alquilamino C1-4, di-alquilamino C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, di[alquil C1-4]amino-alquilo C1-4, trifluorometiltio, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, -C(O)R2, -C(O)OR2, -OC(O)R2, -C(O)-N(R2)2, -CH2-C(O)R2, -CH2C(O)OR2, -CH2-OC(O)R2, -CH2-C(O)-N(R2)2, S(O)2R2, S(O)2N(R2)2, cicloalquilo C3-8 y cicloalquil C3-8-alquilo C1-4; y/o Het2 está opcionalmente sustituido en un átomo de nitrogeno del anillo con un sustituyente seleccionado entre el grupo constituido por alquilo C1-4, halo-alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, di[alquil C1-4]amino-alquilo C1-4, -CH2-C(O)R2, -CH2-C(O)OR2, -CH2-C(O)-N(R2)2, S(O)2R2 y S(O)2N(R2)2; X está ausente, es -O-, metileno, etileno, metileno-O- o -O-metileno; C es cicloalquilo C3-8, Het1, fenilo o Het1, cada uno opcionalmente sustituido en un átomo de carbono del anillo con uno o más sustituyentes seleccionados entre el grupo constituido por halo, ciano, hidroxi, alquilo C1-4, halo-alquilo C1-4, alcoxi C1-4, halo-alcoxi C1-4, N(R2)2, (R2)2N-alquilo C1-4, trifluorometiltio, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, -C(O)R2, -C(O)OR2, -OC(O)R2, -C(O)-N(R2)2, -CH2-C(O)R2, -CH2C(O)OR2, -CH2-OC(O)R2, -CH2-C(O)-N(R2)2, S(O)2R2, S(O)2N(R2)2, cicloalquil C3-8-alquilo C1-4; cicloalcoxi C3-8, cicloalquilamino C3-8, cicloalquilamino C3-8-alquilo C1-4, cicloalquil C3-8-alquilamino C1-4, cicloalquil C3-8-alquilamino C1-4-alquilo C1-4, cicloalquil C3-8-alcoxi C1-4 y D; y/o Het2 está opcionalmente sustituido en un átomo de nitrogeno del anillo con un sustituyente seleccionado entre el grupo constituido por hidroxi, alquilo C1-4, halo-alquilo C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, di[alquil C1-4]amino-alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, -C(O)R2, -C(O)OR2, -CH2-C(O)R2, -CH2-C(O)OR2, -CH2-C(O)-N(R2)2, S(O)2R2 y S(O)2N(R2)2 y D; con la condicion de que C no sea 3,5-dioxo-4,5-dihidro-3H-[1,2,4]triazin-2-ilo; D es fenilo, bencilo, cicloalquilo C3-8 o Het1, cada uno opcionalmente sustituido en un átomo de carbono con uno o más sustituyentes seleccionados independientemente entre el grupo constituido por halo, ciano. hidroxi, alquilo C1-4, halo-alquilo C1-4, alcoxi C1-4, halo-alcoxi C1-4, amino, alquilamino C1-4, di-alquilamino C1-4, amino-alquilo C1-4, alquilamino C1-4-alquilo C1-4, di[alquil C1-4]amino-alquilo C1-4, trifluorometiltio, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, -C(O)R2, -C(O)OR2, -OC(O)R2, -C(O)-N(R2)2, -CH2-C(O)R2, -CH2-C(O)OR2, -CH2-OC(O)R2, -CH2-C(O)-N(R2)2, S(O)2R2 y S(O)2N(R2)2; Het1 es un grupo monocíclico heterocíclico saturado o parcialmente insaturado de 3 a 8 miembros que comprende uno, dos o tres miembros del anillo seleccionados entre -NR3-, -O-, -C(O)- y -S(O)p-; R3 es el punto de union a X o C para dar la estructura de formula (2), o R3 se selecciona entre el grupo constituido por hidrogeno, alquilo C1-4, halo-alquilo C1-4, hidroxi-alquilo C1-4, alcoxi C1-4-alquilo C1-4, -C(O)-alquilo C1-4, -C(O)O-alquilo C1-4, -CH2-C(O)O-alquilo C1-4, -CH2-C(O)-N(alquilo C1-4)2, S(O)2R2, S(O)2N(R2)2 y cicloalquilo C3-8; p es 0, 1 o 2;y Het2 es un grupo heterocíclico aromático de 5 o 6 miembros que comprende (a) de 1 a 4 átomos de nitrogeno, (b) un átomo de oxígeno o un átomo de azufre, o (c) 1 átomo de oxígeno o 1 átomo de azufre y 1 o 2 átomos de nitrogeno; o un tautomero del mismo, o una sal farmacéuticamente aceptable o solvato del compuesto de formula (1) o su tautomero; con la condicion de que el compuesto de formula (1) no sea el compuesto especifico de formula (3).
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