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AR078534A1 - Compuestos de dioxido de iminotiadiazina como inhibidores de bace, composiciones, y su uso - Google Patents

Compuestos de dioxido de iminotiadiazina como inhibidores de bace, composiciones, y su uso

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Publication number
AR078534A1
AR078534A1 ARP100103627A AR078534A1 AR 078534 A1 AR078534 A1 AR 078534A1 AR P100103627 A ARP100103627 A AR P100103627A AR 078534 A1 AR078534 A1 AR 078534A1
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Argentina
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alkyl
group
haloalkyl
heteroalkyl
cycloalkyl
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Schering Corp
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First worldwide family litigation filed litigation Critical https://patents.darts-ip.com/?family=43857101&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR078534(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Schering Corp filed Critical Schering Corp
Publication of AR078534A1 publication Critical patent/AR078534A1/es

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Abstract

Exhiben propiedades las cuales se espera que los convierta en ventajosos como inhibidores de BACE (Enzima de disociacion de APP de sitio b) y/o para el tratamiento y prevencion de diversas patologías relacionadas con la produccion de b-amiloides (ôAbö). También se describen composiciones farmacéuticas que comprenden uno o más de dichos compuestos (solos y en combinacion con uno o más otros agentes activos), y métodos para su preparacion y uso en el tratamiento de patologías asociadas con la proteína amiloide b (Ab), incluyendo la enfermedad de Alzheimer. Reivindicacion 1: Un compuesto, o un tautomero del mismo, o un estereoisomero de dicho compuesto o dicho tautomero, o una sal farmacéuticamente aceptable del mismo, teniendo dicho compuesto la formula estructural (1) donde: -L1- representa un enlace o un resto divalente seleccionado del grupo formado por -alquil-, -haloalquil-, -heteroalquil-, -alquenil-, y -alquinil-; -L2- representa un enlace o un resto divalente seleccionado del grupo formado por -alquil-, -haloalquil-, -heteroalquil-, -alquenil-, y -alquinil-; cada -L3- representa independientemente un enlace o un resto divalente seleccionado independientemente del grupo formado por -alquil-, -haloalquil-, -heteroalquil-, -alquenil-, -alquinil-, -N(R7)-, -NHC(O)-, -C(O)NH-, -NHS(O)2-, -S(O)2NH-, -O-alquil-, -alquil-O-, -N(R7)-alquil-, -alquil-N(R7)-, -haloalquil-NH-, y -NH-haloalquil-; m, n, y p son cada uno numeros enteros independientemente seleccionados, donde: m es 0 o más; n es 0 o más; y p es 0 o más, donde el valor máximo de la suma de m y n es el numero máximo de átomos de hidrogeno sustituibles disponibles en el anillo A, y donde el valor máximo de p es el numero máximo de átomos de hidrogeno sustituibles disponibles en el anillo B; R1 se selecciona del grupo formado por: H, alquilo, heteroalquilo, heterohaloalquilo, cicloalquilo, cicloalquilalquil-, heterocicloalquilo, heterocicloalquilalquil-, arilo, arilalquil-, heteroarilo, y heteroarilalquil-, donde cada uno de dicho alquilo, heteroalquilo, heterohaloalquilo, cicloalquilo, cicloalquilalquil-, heterocicloalquilo, heterocicloalquilalquil-, arilo, arilalquil-, heteroarilo, y heteroarilalquil- de R1 está sin sustituir o sustituido con uno o más grupos R10 independientemente seleccionados; R2 se selecciona del grupo formado por H, halo, alquilo, haloalquilo, y heteroalquilo, donde cada uno de dicho alquilo y dicho haloalquilo de R2 está sin sustituir o sustituido con uno o más grupos R10 independientemente seleccionados; R3 se selecciona del grupo formado por H, halo, alquilo, haloalquilo, y heteroalquilo, donde cada uno de dicho alquilo y dicho haloalquilo de R3 está sin sustituir o sustituido con uno o más grupos R10 independientemente seleccionados; R4 se selecciona del grupo formado por alquilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo, donde cada uno de dicho alquilo, arilo, heteroarilo, cicloalquilo, cicloalquenilo, heterocicloalquilo, y heterocicloalquenilo de R4 está sin sustituir o sustituido con uno o más grupos R10 independientemente seleccionados; el anillo A se selecciona del grupo formado por arilo monocíclico, heteroarilo monocíclico, cicloalquilo monocíclico, cicloalquenilo monocíclico, heterocicloalquilo monocíclico, heterocicloalquenilo monocíclico, y un grupo multicíclico; cada anillo B (cuando está presente) se selecciona independientemente del grupo formado por arilo monocíclico, heteroarilo monocíclico, cicloalquilo monocíclico, cicloalquenilo monocíclico, heterocicloalquilo monocíclico, heterocicloalquenilo monocíclico, y un grupo multicíclico; cada R5 (cuando está presente) se selecciona independientemente del grupo formado por halo, -CN, -SF5, -OSF5, -NO2, -Si(R6)3, -P(O)(OR7)2, -P(O)(OR7)(R7), -N(R8)2, -NR8C(O)R7, -NR8S(O)2R7, -NR8C(O)N(R8)2, -NR8C(O)OR7, -C(O)R7, -C(O)2R7, -C(O)N(R8)2, -S(O)R7, -S(O)2R7, -S(O)2N(R8)2, -OR7, -SR7, alquilo, haloalquilo, haloalcoxi, heteroalquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo, y heteroarilo, donde cada uno de dichos alquilo, haloalquilo, haloalcoxi, heteroalquilo, alquenilo, alquinilo, cicloalquilo, heterocicloalquilo, arilo, y heteroarilo de R5 (cuando está presente) está opcional e independientemente sin sustituir o sustituido adicionalmente con uno o más grupos independientemente seleccionados, seleccionados del grupo formado por alquilo inferior, alquenilo inferior, alquinilo inferior, heteroalquilo inferior, halo, -CN, -SF5, -OSF5, -NO2, -N(R8)2, -OR7, -C(O)N(R8)2, y cicloalquilo; cada R6 (cuando está presente) se selecciona independientemente del grupo formado por alquilo, arilo, arilalquil-, haloalquilo, cicloalquilo, cicloalquilalquil-, heteroarilo, y heteroarilalquil-; cada R7 (cuando está presente) se selecciona independientemente del grupo formado por H, alquilo, alquenilo, heteroalquilo, haloalquilo, arilo, arilalquil-, heteroarilo, heteroarilalquil-, cicloalquilo, cicloalquilalquil-, heterocicloalquilo, y heterocicloalquilalquil-; cada R8 (cuando está presente) se selecciona independientemente del grupo formado por H, alquilo, alquenilo, heteroalquilo, haloalquilo, haloalquenilo, arilo, arilalquil-, heteroarilo, heteroarilalquil-, cicloalquilo, cicloalquilalquil-, heterocicloalquilo, y heterocicloalquilalquil-; cada R9 (cuando está presente) se selecciona independientemente del grupo formado por: halogeno, -CN, -SF5, -OSF5, -NO2, -Si(R6)3, -P(O)(OR7)2, -P(O)(OR7)(R7), -N(R8)2, -NR8C(O)R7, -NR8S(O)2R7, -NR8C(O)N(R8)2, -NR8C(O)OR7, -C(O)R7, -C(O)2R7, -C(O)N(R8)2, -S(O)R7, -S(O)2R7, -S(O)2N(R8)2, -OR7, -SR7, alquilo, haloalquilo, heteroalquilo, alquenilo, alquinilo, arilo, arilalquil-, cicloalquilo, heteroarilo, heteroarilalquil-, y heterocicloalquilo; cada R10 (cuando está presente) se selecciona independientemente del grupo formado por halo, -CN, -NO2, -Si(R6)3, -P(O)(OR7)2, -P(O)(OR7)(R7), -N(R8)2, -NR8C(O)R7, -NR8S(O)2R7, -NR8C(O)N(R8)2, -NR8C(O)OR7, -C(O)R7, -C(O)2R7, -C(O)N(R8)2, -S(O)R7, -S(O)2R7, -S(O)2N(R8)2, -OR7, -SR7, alquilo, haloalquilo, haloalcoxi, heteroalquilo, alquenilo, alquinilo, y cicloalquilo, donde cada uno de dichos alquilo, haloalquilo, haloalcoxi, heteroalquilo, alquenilo, alquinilo, y cicloalquilo de R10 (cuando está presente) está opcional e independientemente sin sustituir o adicionalmente sustituido con uno o más grupos independientemente seleccionados del grupo formado por alquilo inferior, alquenilo inferior, alquinilo inferior, heteroalquilo inferior, halo, -CN, -NO2, -N(R8)2, -OR7, y -C(O)N(R8)2.
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