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AR057984A1 - DERIVADOS DE IMIDAZOL INHIBIDORES DE LA PROTEINA beta AMILOIDE - Google Patents

DERIVADOS DE IMIDAZOL INHIBIDORES DE LA PROTEINA beta AMILOIDE

Info

Publication number
AR057984A1
AR057984A1 ARP060105054A ARP060105054A AR057984A1 AR 057984 A1 AR057984 A1 AR 057984A1 AR P060105054 A ARP060105054 A AR P060105054A AR P060105054 A ARP060105054 A AR P060105054A AR 057984 A1 AR057984 A1 AR 057984A1
Authority
AR
Argentina
Prior art keywords
alkyl
cycloalkyl
alkynyl
alkenyl
optionally substituted
Prior art date
Application number
ARP060105054A
Other languages
English (en)
Original Assignee
Astex Therapeutics Ltd
Astrazeneca Ab
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=38049092&utm_source=google_patent&utm_medium=platform_link&utm_campaign=public_patent_search&patent=AR057984(A1) "Global patent litigation dataset” by Darts-ip is licensed under a Creative Commons Attribution 4.0 International License.
Application filed by Astex Therapeutics Ltd, Astrazeneca Ab filed Critical Astex Therapeutics Ltd
Publication of AR057984A1 publication Critical patent/AR057984A1/es

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    • C07D233/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, not condensed with other rings
    • C07D233/54—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
    • 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
    • C07D233/88—Nitrogen atoms, e.g. allantoin
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4164—1,3-Diazoles
    • A61K31/4168—1,3-Diazoles having a nitrogen attached in position 2, e.g. clonidine
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  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)

Abstract

Reivindicacion 1: Un compuesto de formula (1), en la cual R1 está seleccionada entre hidrogeno, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, cicloalquilo C3-6, cicloalquenilo C5-7, arilo, heteroarilo, heterociclilo, alquil C1-6-cicloalquilo C3-6, alquilarilo C1-6, alquilheteroarilo C1-6 o alquilheterociclilo C1-6, donde el alquilo C1-6, alquenilo C3-6, alquinilo C3-6, cicloalquilo C3-6, cicloalquenilo C5-7, arilo, heteroarilo, heterociclilo, alquil C1-6-cicloalquilo C3-6, alquilarilo C1-6, alquilheteroarilo C1-6 o alquilheterociclilo C1-6 están opcionalmente sustituidos con uno, dos o tres A; R2 está seleccionado entre hidrogeno, nitro, ciano, -Q-alquilo C1-6, -Q-alquenilo C2-6, -Q-alquinilo C2-6, -Q-cicloalquilo C3-6, -Q- cicloalquenilo C5-7, -Q-alquil C1-6cicloalquilo C3-6, -Q-arilo, -Q-heteroarilo, -Q-alquilarilo C1-6, -Q-alquilheteroarilo C1-6, -Q-heterociclilo, o -Q- alquilheterociclilo C1-6, donde dicho -Q-alquilo C1-6, -Q-alquenilo C2-6, -O-alquinilo C2-6, -Q- cicloalquilo C3-6, -Q-cicloalquenilo C5-7, -Q-alquil C1-6-cicloalquilo C3-6, -Q-arilo, -Q-heteroarilo, -Q-alquilarilo C1-6, -Q-alquiIheteroarilo C1-6, -Q-heterociclilo, o -Q-alquilheterociclilo C1-6 están opcionalmente sustituidos con uno, dos o tres R7; -Q- es un enlace directo, -CONH-, -CO-, -CON(alquilo C1-6)-, -CON(cicloalquilo C3-6)-, -SO-, -SO2-, -SO2NH-, -SO2N(alquilo C1-6)-, -SO2N(cicloalquilo C3-6)-, -NHSO2-, -N(alquilo C1-6)SO2-, -NHCO-, -N(alquilo C1-6)CO-, -N(cicloalquilo C3- 6)CO- o -N(cicloalquil C3-6)SO2-; R3 es (C(R4)(R5))nR6, alquenilo C2-4R6, alquinilo C2-4R6, cicloalquenilo C5-7R6, nitro o ciano y si n > 1 entonces cada C(R4)(R5) es independiente de los otros; R4 y R5 están independientemente seleccionados de hidrogeno, alquilo C1-6, ciano, halo o nitro; o R4 y R5 conjuntamente forman oxo, cicloalquilo C3-6 o heterociclilo; R6 está seleccionado de metilo, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo donde cada uno de dichos metilo, cicloalquilo C3-6, heterociclilo, arilo o heteroarilo está opcionalmente sustituido con entre uno y cuatro R7, y donde cualquiera de los grupos arilo o heteroarilo individuales puede estar opcionalmente fusionado con un grupo cicloalquilo, cicloalquenilo o heterociclilo de 4, 5, 6 o 7 miembros para formar un sistema de anillos bicíclico donde el sistema de anillo bicíclico está opcionalmente sustituido con entre uno y cuatro A con la condicion de que el anillo bicíclico no sea un sistema de anillo indano, benzo[1,3]dioxol o 2,3-dihidrobenzo[1,4]-dioxina; R7 está seleccionado de halogeno, nitro, CHO, alquilo C0-6CN, O-alquilo C1-6CN, alquilo C0-6OR8, O-alquilo C2-6OR8, fluorometilo, difluorometilo, trifluorometilo, fluorometoxi, difluorometoxi, trifluorometoxi, alquilo C0-6NR8R9, O-alquilo C2-6NR8R9, O-alquilo C2-6-O-alquilo C2-6NR8R9, NR8OR9, alquilo C0-6CO2R8, O-alquilo C1-6CO2R8, alquilo C0-6CONR8R9, O-alquilo C1-6CONR8R9, O-alquilo C2-6NR8(CO)R9, alquilo C0-6NR8(CO)R9, O(CO)NR8R9, NR8(CO)OR9, NR8(CO)NR8R9, O(CO)OR8, O(CO)R8, alquilo C0-6COR8, O-alquilo C1-6COR8, NR8(CO)(CO)R8, NR8(CO)(CO)NR8R9, alquilo C0-6SR8, alquilo C0-6(SO2)NR8R9, O-alquilo C1-6NR8(SO2)R9, O-alquilo C0-6(SO2)NR8R9, alquilo C0-6(SO)NR8R9, O- alquilo C1-6(SO)NR8R9, OSO2R8, SO3R8, alquilo C0-6NR8(SO2)NR8R9, alquilo C0-6NR8(SO)R9, O-alquilo C2-6NR8(SO)R8, O-alquilo C1-6SO2R8, alquilo C1-6SO2R8, alquilo C0-6SOR8, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquil C0-6cicloalquilo C3-6, alquilarilo C0-6, alquilheteroariIo C0-6, alquilheterociclilo C0-6, y O-alquilheterociclilo C2-6, donde cualquier alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C0-6cicloalquilo C3-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilheterocicliIo C0-6, y O-alquilheterociclilo C2-6 puede estar opcionalmente sustituido con uno o más R14, y donde cualquiera de los grupos arilo y heteroarilo individuales pueden estar opcionalmente fusionados con un grupo cicloalquilo, cicloalquenilo o heterociclilo de 4, 5, 6 o 7 miembros, para formar un sistema de anillo bicíclico donde el sistema de anillo bicíclico está opcionalmente sustituido con entre uno y cuatro A con la condicion de dicho sistema de anillo bicíclico no sea un sistema de anillo indano, benzo[1,3]dioxol o 2,3-dihidrobenzo[1,4]-dioxina; R14 está seleccionado entre halogeno, nitro, CHO, alquilo C0-6CN, O-alquilo C1-6CN, alquilo C0-6OR8, O-alquilo C1-6OR8, fluorometilo, difluorometilo, trifluorometilo, fluorometoxi, difluorometoxi, trifluorometoxi, alquilo C0-6NR8R9, O-alquilo C2-6NR8R9, O-alquilo C2-6O-alquilo C2-6NR8R9, NR8OR9, alquilo C0-6CO2R8, O-alquilo C1-6CO2R8, alquilo C0-6CONR8R9, O-alquilo C1-6CONR8R9, O-alquilo C2-6NR8(CO)R9, alquilo C0- 6NR8(CO)R9, O(CO)NR8R9, NR8(CO)OR9, NR8(CO)NR8R9, OR8, O(CO)OR8, O(CO)R8, alquilo C0-6COR8, O-alquilo C1-6COR8, NR8(CO)(CO)R8, NR8(CO)(CO)NR8R9, alquilo C0-6SR8, alquilo C0-6(SO2)NR8R9, O-alquilo C2-6NR8(SO2)R9, O-alquilo C0-6(SO2)NR8R9, alquilo C0- 6(SO)N R8R9, O-alquilo C1-6(SO)NR8R9, OSO2R8, OSO2R8R9, SO3R8, alquilo C0-6NR8(SO2)NR8R9, alquilo C0-6NR8(SO)R9, O-alquilo C2-6NR8(SO)R9, O-alquilo C1-6SO2R8, alquilo C1-6SO2R8, alquilo C0-6SOR8, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C0-6-cicloalquilo C3-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilheterociclilo C0-6 y O-alquilheterociclilo C2-6; donde cualquier alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C0-6-cicloalquilo C3-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilheterociclilo C0-6 y Oalquilheterociclilo C2-6 pueden estar opcionalmente sustituidos con entre uno y cuatro A; R8 y R9 están independientemente seleccionados entre hidrogeno, alquilo C1-6, alquenilo C2-6, alquinilo C2- 6, fluorometilo, difluorometilo, trifluorometilo, fluorometoxi, difluorometoxi, trifluorometoxi, alquilo C0-6-cicloalquilo C3-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquiIheterocicIilo C0-6 y alquilo C0-6NR10R11, donde el alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilo C0-6cicloalquilo C3-6, alquilarilo C0-6, alquilheteroariio C0-6 o alquilheterociclilo C0-6 están opcionalmente sustituidos con A; o R8 y R9 pueden formar conjuntamente un anillo heterocíclico de 4 a 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O o S que está opcionalmente sustituido con A; siempre que dos grupos R8 ocurren en la estructura entonces estos pueden formar opcionalmente, conjuntamente un anillo heterocíclico de 5 o 6 que contiene uno o más heteroátomos seleccionados entre N, O o S, que está opcionalmente sustituido con A; R10 y R11 están independientemente seleccionados de hidrogeno, alquilo C1-6, alquenilo C3-6, alquinilo C3-6, alquil C0-6-cicloalquilo C3-6, alquilarilo C0-6, alquilheterociclilo C0-6 y alquilheteroarilo C0-6, donde el alquilo C1-6, alquenilo C3-6, alquinilo C3-6, alquilo C0-6cicloalquilo C3-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilheterociclilo C0-6 están opcionalmente sustituidos con A; o R10 y R11 pueden formar conjuntamente un anillo heterocíclico de 4 a 6 miembros que contienen uno o más heteroátomos seleccionados entre N, O o S opcionalmente sustituidos con A; n es 0, 1, 2 o 3; A está seleccionada entre oxo, halogeno, nitro, CN, OR12, alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilo C0-6cicloalquilo C3-6, alquilheterociclilo C0-6, fluorometilo, difluorometilo, trifluorometilo, fluorometoxi, difluorometoxi, trifluorometoxi, O-alquilo C2-6NR12R13, NR12R13, CONR12R13, NR12(CO)R13, O(CO)alquilo C1-6, (CO)O-alquilo C1-6, COR12, (SO2)NR12R13, NSO2R12, SO2R12, SOR12, (CO)alquilo C1-6NR12R13, (SO2)alquilo C1-6NR12R13, OSO2R12, SO3R12 donde los grupos alquilo C1-6, alquenilo C2-6, alquinilo C2-6, alquilarilo C0-6, alquilheteroarilo C0-6, alquilheterociclilo C0-6 y alquilo C0-6cicloalquilo C3-6 pueden estar opcionalmente sustituidos con halo, OSO2R12, SO3R12, nitro, ciano, OR12, alquilo C1-6, fluorometilo, difluorometilo, trifluorometilo, fluorometoxi, difluorometoxi y trifluorometoxi; R12 y R13 están independientemente seleccionados entre hidrogeno, alquilo C1-6, cicloalquilo C3-6, arilo, heteroarilo o heterociclilo donde dicho alquilo C1-6, cicloalquilo C3-6, arilo, heteroarilo o heterociclilo está opcionalmente sustituido con uno, dos o tres hidroxi, ciano, halo o alquiloxiC1-3; o R12 y R13 pueden formar conjuntamente un anillo heterocíclico de 4 a 6 miembros que contiene uno o más heteroátomos seleccionados entre N, O o S opcionalmente sustituidos con hidroxi, alquiloxi C1-3, ciano o halo; con la condicion de que cualquiera de los grupos arilo o heteroarilo en R1, R2 o R3 está sustituido con un grupo OSO2R8, SO3R8, OSO2R12 o SO3R12; o con la condicion de cualquiera de los grupos arilo o heteroarilo individuales en R1, R2 o R3 están fusionados con un grupo cicloalquilo, cicloalquenilo o heterociclilo de 4, 5, 6 o 7 miembros para formar un sistema de anillo bicíclico donde el sistema de anillo bicíclico está opcionalmente sustituido con entre uno y cuatro A con la condicion de que el anillo bicíclico no sea un sistema de anillo indano, benzo[1,3jdioxol o 2,3- dihidrobenzo[1,4]-dioxina; o con la condicion de que R1 sea alquinilo C3-6 o cicloalquenilo C5-7 opcionalmente sustituido con uno, dos o tres A; o con la condicion de que Q esté seleccionado entre -NHSO2-, -N(alquilo C1-6)SO2-, -SO2NH-, -SO2N(alquilo C1-6)- o -SO2N(cicloalquilo C3-6)- , -SO-, -SO2- o -N(cicloalquilo C3-6)SO2-; o con la condicion de que R3 esté seleccionado entre alquenilo C2-4R6, alquinilo C2-4R6, cicloalquenilo C5-7R6, nitro o ciano; o con la condicion de que R2 esté seleccionado de un grupo que consiste en nitro, ciano, alquinillo C2-6, cicloalquenilo C5-7 o alquenilo C2-6 donde el grupo alquinilo C2-6, cicloalquenilo C5-7 o alquenilo C2-6 esté opcionalmente sustituido con uno, dos o tres R7; en forma de una base libre o una sal, solvato o solvato de una sal de éste farmacéuticamente aceptable.
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TW200738683A (en) * 2005-06-30 2007-10-16 Wyeth Corp Amino-5-(5-membered)heteroarylimidazolone compounds and the use thereof for β-secretase modulation
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WO2007058602A2 (en) 2007-05-24
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NO20082673L (no) 2008-07-23
JP2009519221A (ja) 2009-05-14
KR20080080565A (ko) 2008-09-04
EP1979324A4 (en) 2011-11-09
UY29927A1 (es) 2007-06-29
ECSP088499A (es) 2008-07-30
WO2007058602A3 (en) 2007-07-05
RU2008121756A (ru) 2009-12-27
TW200734311A (en) 2007-09-16
US20080293718A1 (en) 2008-11-27
CA2630680A1 (en) 2007-05-24
BRPI0618845A2 (pt) 2016-09-13

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