AR065231A1 - Quinazolinas inhibidoras de pdk1, composiciones farmaceuticas que las contienen y usos para tratar enfermedades asociadas a proliferacion celular. - Google Patents

Quinazolinas inhibidoras de pdk1, composiciones farmaceuticas que las contienen y usos para tratar enfermedades asociadas a proliferacion celular.

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Publication number
AR065231A1
AR065231A1 ARP070105879A ARP070105879A AR065231A1 AR 065231 A1 AR065231 A1 AR 065231A1 AR P070105879 A ARP070105879 A AR P070105879A AR P070105879 A ARP070105879 A AR P070105879A AR 065231 A1 AR065231 A1 AR 065231A1
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AR
Argentina
Prior art keywords
substituted
heteroaryloxy
alkyl
alkoxy
heteroaryl
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ARP070105879A
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English (en)
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Novartis Vaccines & Diagnostic
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Publication of AR065231A1 publication Critical patent/AR065231A1/es

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    • C07D239/00Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72Quinazolines; Hydrogenated quinazolines
    • C07D239/78Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 2
    • C07D239/84Nitrogen atoms
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495Heterocyclic 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
    • A61K31/505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/517Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with carbocyclic ring systems, e.g. quinazoline, perimidine
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    • A61P35/00Antineoplastic agents
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    • A61P35/00Antineoplastic agents
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    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
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    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P7/00Drugs for disorders of the blood or the extracellular fluid
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00Drugs for disorders of the cardiovascular system
    • A61P9/10Drugs 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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    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D401/00Heterocyclic 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
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    • C07D401/08Heterocyclic 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 alicyclic rings
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    • C07D401/12Heterocyclic 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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    • C07D417/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings

Abstract

Reivindicacion 1: Un compuesto de formula (1), o una sal aceptable para el uso farmacéutico, un éster, o un tautomero de éste, caracterizado porque: Ar es arilo, arilo sustituido, heteroarilo, o heteroarilo sustituido; R1 es H, alquilo C1-3, halo, ciano, nitro, CF3, imidazolilo, tiazolilo, oxazolilo, o amino; R2 se selecciona del grupo que consiste en H, alcoxilo, alcoxilo sustituido, alquilo. alquilo sustituido, CN, heteroariloxilo, heteroariloxilo sustituido, heterocicliloxilo, heterocicliloxilo sustituido, y halo; R3 se selecciona del grupo que consiste en H, halo, CN, carboxilo, alquilo, alquilo sustituido, alcoxilo, alcoxilo sustituido, ariloxilo, ariloxilo sustituido, cicloalquiloxilo, cicloalquiloxilo sustituido, heterociclilalquiloxilo, heterociclilalquiloxilo sustituido, heteroariloxilo, heteroariloxilo sustituido, heteroarilalquiloxilo, heteroarilalquiloxilo sustituido, arilalquiloxilo, arilalquiloxilo sustituido, heteroarilo, heteroarilo sustituido, heterociclilo, heterociclilo sustituido, heteroarilalquilo, heteroarilalquilo sustituido, heterociclilalquilo, y heterociclilalquilo sustituido; L es un enlace covalente, carbonilo, carbonilamino, aminocarbonilo, -O-, -S- SO-, -SO2-, -NH-, alquilo C1-3, alquilo C1-3 sustituido, alquenilo C2-3, alquinilo C2-3 o un alquilo interrumpido con -O-, -S-, -SO-, o -SO2-; A1 es alquilo, alquilo sustituido, alquenilo, alquenilo sustituido, alquinilo, alquinilo sustituido, alcoxilo, alcoxilo sustituido, acilo, acilamino, aciloxilo, amino, amino sustituido, aminocarbonilo, aminotiocarbonilo, aminocarbonilamino, aminotiocarbonilamino, aminocarboniloxilo, aminosulfonilo, aminosulfoniloxilo, arninosulfonilamino, amidino, carboxilo, éster carboxílico, (éster carboxílico)amino, (éster carboxílico)oxilo, cario, halo, hidroxilo, nitro, SO3H, sulfonilo, sulfonilo sustituido, sulfoniloxilo, sulfonilamino, tioacilo, tiol, alquiltiol, alquiltiol sustituido, arilo, arilo sustituido, heteroarilo, heteroarilo sustituido, cicloalquilo, cicloalquilo sustituido, heterociclilo, o heterociclilo sustituido, con las siguientes condiciones: a) cuando R1, R2, y R3 son cada uno H, y L es un enlace covalente, entonces A1 es distinto de arilo o arilo sustituido; b) cuando R1, R2, y R5 son cada uno H, L es un enlace covalente, y A1 es Br, fenilo sustituido, o piridinilo sustituido, entonces Ar es distinto de fenilo, fenilo sustituido con piperazinilo o heterociclilalquiloxilo, o piridinilo; c) cuando R1, R2, y R3 son cada uno H, L es un enlace covalente, y A1 es hidroxilo o alcoxilo, entonces Ar es distinto de fenilo sustituido con uno o más alquilo o halo: y d) cuando R1, R2, y R3 son cada uno H, y L es O entonces A1 es distinto de piridinilo o piridinilo sustituido.
ARP070105879A 2006-12-22 2007-12-21 Quinazolinas inhibidoras de pdk1, composiciones farmaceuticas que las contienen y usos para tratar enfermedades asociadas a proliferacion celular. AR065231A1 (es)

Applications Claiming Priority (2)

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US87697206P 2006-12-22 2006-12-22
US99917007P 2007-10-15 2007-10-15

Publications (1)

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AR065231A1 true AR065231A1 (es) 2009-05-27

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ARP070105879A AR065231A1 (es) 2006-12-22 2007-12-21 Quinazolinas inhibidoras de pdk1, composiciones farmaceuticas que las contienen y usos para tratar enfermedades asociadas a proliferacion celular.

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US (1) US20100216767A1 (es)
EP (1) EP2125755A2 (es)
JP (1) JP2010514693A (es)
KR (1) KR20090092287A (es)
CN (1) CN101652352A (es)
AR (1) AR065231A1 (es)
AU (1) AU2007336893A1 (es)
BR (1) BRPI0720563A2 (es)
CA (1) CA2673003A1 (es)
CL (1) CL2007003774A1 (es)
CO (1) CO6361927A2 (es)
CR (1) CR10833A (es)
EA (1) EA200900819A1 (es)
EC (1) ECSP099445A (es)
IL (1) IL198774A0 (es)
MA (1) MA31001B1 (es)
MX (1) MX2009006627A (es)
NO (1) NO20092725L (es)
PE (1) PE20081630A1 (es)
SM (1) SMP200900055B (es)
SV (1) SV2009003307A (es)
TN (1) TN2009000255A1 (es)
TW (1) TW200829558A (es)
WO (1) WO2008079988A2 (es)
ZA (1) ZA200903233B (es)

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