AR084553A1 - DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER - Google Patents

DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER

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AR084553A1
AR084553A1 ARP110104899A ARP110104899A AR084553A1 AR 084553 A1 AR084553 A1 AR 084553A1 AR P110104899 A ARP110104899 A AR P110104899A AR P110104899 A ARP110104899 A AR P110104899A AR 084553 A1 AR084553 A1 AR 084553A1
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Argentina
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alkyl
haloalkyl
heteroaryl
cyano
halogen
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ARP110104899A
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Astrazeneca Ab
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Publication of AR084553A1 publication Critical patent/AR084553A1/es

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    • C07D—HETEROCYCLIC COMPOUNDS
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    • C07D401/02—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
    • C07D401/10—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 linked by a carbon chain containing aromatic rings
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    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/4965—Non-condensed pyrazines
    • A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
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    • 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
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    • A61K31/4164—1,3-Diazoles
    • A61K31/4188—1,3-Diazoles condensed with other heterocyclic ring systems, e.g. biotin, sorbinil
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    • A61K31/4353—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems
    • A61K31/437—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom ortho- or peri-condensed with heterocyclic ring systems the heterocyclic ring system containing a five-membered ring having nitrogen as a ring hetero atom, e.g. indolizine, beta-carboline
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/506—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
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    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
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    • A—HUMAN NECESSITIES
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    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
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    • C07D235/00—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02—Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
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    • C07D401/00—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
    • C07D401/02—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
    • 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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    • C07D401/02—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
    • C07D401/12—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 linked by a chain containing hetero atoms as chain links
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    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
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    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D405/12—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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    • C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
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    • C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
    • C07D491/10—Spiro-condensed systems
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    • C07D491/12—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains three hetero rings
    • C07D491/20—Spiro-condensed systems
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    • C07B2200/07—Optical isomers

Abstract

Reivindicación 1: Un compuesto de acuerdo con la formula (1), donde A es -O- o -CH2-; n es 0 ó 1; R1 es alquilo C1-6 o haloalquilo C1-6; R2 es hidrógeno, alquilo C0-6-arilo, alquilo C0-6-heteroarilo, alquinilo C2-6, alquenilo C2-6, alquilo C1-6, halógeno, ciano, haloalquilo C1-6, NHC(O)R9 u OR8, donde dicho alquilo C0-6-arilo, alquilo C0-6-heteroarilo, alquinilo C2-6, alquenilo C2-6, alquilo C1-6 o haloalquilo C1-6 está opcionalmente sustituido con uno a tres R7; R5 y R6 son independientemente hidrógeno, heterociclilo, cicloalquilo C3-6, arilo, heteroarilo o alquilo C1-6, donde dicho heterociclilo, cicloalquilo C3-6, arilo, heteroarilo o alquilo C1-6 está opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre halógeno, alquilo C1-6, haloalquilo C1-6, ciano u OR8; o R5 y R6 junto con el carbono al cual están unidos, forman un anillo B, que es un anillo monocíclico cicloalquilo o heterociclilo de 3 a 14 miembros, o un anillo bicíclico cicloalquilo o heterociclilo de 9 a 14 miembros; y donde el anillo B está opcionalmente sustituido con uno o dos sustituyentes seleccionados independientemente entre oxo, halógeno, alquilo C1-6, haloalquilo C1-6, ciano, u OR8; y el anillo B esta opcionalmente fusionado con un arilo o heteroarilo para formar un sistema bicíclico o policíclico; R7 es independientemente alquilo C1-6, halógeno, ciano, alquilo C0-6-cicloalquilo C3-6, haloalquilo C1-6, O-alquilo C1-6, O-haloalquilo C1-6, alquinilo C2-6 o alquenilo C2-6, donde dicho alquilo C1-6, alquilo C0-6-cicloalquilo C3-6, haloalquilo C1-6, O-alquilo C1-6, O-haloalquilo C1-6, alquinilo C2-6 o alquenilo C2-6 está opcionalmente sustituido con 1 - 3 sustituyentes seleccionados independientemente entre halógeno, ciano, alquilo C1-6, haloalquilo C1-6, O-alquilo C1-6 y O-haloalquilo C1-6; R8 es independientemente hidrogeno, alquilo C1-6, alquinilo C2-6, haloalquilo C1-6, arilo o heteroarilo, donde dicho alquilo C1-6, haloalquilo C1-6, arilo o heteroarilo está opcionalmente sustituido con un grupo seleccionado de halógeno, ciano y alquilo C1-6; R9 es un heteroarilo, donde dicho heteroarilo está opcionalmente sustituido con halógeno, ciano, OR8, haloalquilo C1-6 o alquilo C1-6; en forma de una base libre o una sal farmacéuticamente aceptable de este.
ARP110104899A 2010-12-22 2011-12-22 DERIVADOS IMIDAZOLICOS HETEROCICLICOS INHIBIDORES DE b-SECRETASA, COMPOSICIONES FARMACEUTICAS QUE LOS CONTIENEN Y USO DE LOS MISMOS PARA TRATAR ENFERMEDADES NEURODEGENERATIVAS, EN PARTICULAR ALZHEIMER AR084553A1 (es)

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US201061425852P 2010-12-22 2010-12-22
US201161529620P 2011-08-31 2011-08-31

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KR (1) KR101916975B1 (es)
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AR (1) AR084553A1 (es)
AU (3) AU2011345389B2 (es)
BR (1) BR112013016030B1 (es)
CA (1) CA2822378C (es)
CL (1) CL2013001849A1 (es)
CO (1) CO6781485A2 (es)
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