AR064010A1 - Inhibidores de la actividad de la akt - Google Patents

Inhibidores de la actividad de la akt

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Publication number
AR064010A1
AR064010A1 ARP070105281A ARP070105281A AR064010A1 AR 064010 A1 AR064010 A1 AR 064010A1 AR P070105281 A ARP070105281 A AR P070105281A AR P070105281 A ARP070105281 A AR P070105281A AR 064010 A1 AR064010 A1 AR 064010A1
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AR
Argentina
Prior art keywords
aob
alkyl
cycloalkyl
heterocyclyl
aryl
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ARP070105281A
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English (en)
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Merck & Co Inc
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Publication of AR064010A1 publication Critical patent/AR064010A1/es

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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
    • C07D401/04—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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    • C07—ORGANIC CHEMISTRY
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    • C07D471/00—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
    • 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
    • C07D471/04—Ortho-condensed systems
    • 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
    • A61K31/435—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
    • A61K31/4353—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
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    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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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    • C07D—HETEROCYCLIC COMPOUNDS
    • 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
    • C07D401/06—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 only aliphatic carbon atoms
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/04—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 directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • 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
    • C07D403/06—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 carbon chain containing only aliphatic carbon atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D407/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00
    • C07D407/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings
    • C07D407/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having oxygen atoms as the only ring hetero atoms, not provided for by group C07D405/00 containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D409/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms
    • C07D409/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings
    • C07D409/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having sulfur atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
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    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic 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
    • C07D417/02—Heterocyclic 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 two hetero rings
    • C07D417/04—Heterocyclic 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 two hetero rings directly linked by a ring-member-to-ring-member bond
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D471/00—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
    • C07D471/12—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 three hetero rings
    • C07D471/14—Ortho-condensed systems

Abstract

La presente proporciona compuestos de naftiridina sustituidos que inhiben la actividad de la Akt. En particular, los compuestos descritos inhiben de manera selectiva una o dos de las isoformas de la Akt. También proporciona composiciones que comprenden tales compuestos inhibidores y procedimientos de inhibicion de la actividad de la Akt mediante la administracion del compuesto a un paciente en necesidad de tratamiento de cáncer. Reivindicacion 1: Un compuesto de acuerdo con la formula (1) en la que: a es 0 o 1; b es 0 o 1; m es 0, 1 o 2; p es 0, 1 o 2; R2 se selecciona independientemente entre alquilo C1-6, alcoxi C1-6, CO2H, halo, OH y NH2; el anillo Y es cicloalquilo C4-7; R1 se selecciona entre: H, oxo, (C=O)aOb-alquilo C1-10, (C=O)aOb-arilo, (C=O)aOb-alquenilo C2-10, (C=O)aOb-alquinilo C2-10, CO2H, halo, OH, Ob perfluoroalquilo C1-6, (C=O)aNR7R8, CN, (C=O)aOb cicloalquilo C3-8, S(O)mNR7R8, SH, S(O)m-alquilo C1-10 y (C=O)aOb-heterociclilo, dicho alquilo, arilo, alquenilo, alquinilo, cicloalquilo, y heterociclilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6 es; R6 es (C=O)aOb-alquilo C1-10, (C=O)aOb-arilo, alquenilo C2-10, alquinilo C2-10, (C=O)aOb-heterociclilo, CO2H, halo, OH, Ob perfluoroalquilo C1-6, Oa(C=O)bNR7R8, oxo, CHO, (N=O)R7R8, S(O)mNR7R8, SH, S(O)m-alquilo C1-10 o (C=O)aOb-cicloalquilo C3-8, dicho alquilo, arilo, alquenilo, alquinilo, heterociclilo, y cicloalquilo opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a; R6a se selecciona entre (C=O)aOb alquilo C1-10, Oa perfluoroalquilo C1-3, alquileno C0-6, -S(O)mRa, SH, oxo, OH, halo, CN, alquenilo C2-10, alquinilo C2-10, cicloalquilo C3-6, alquileno C0-6-arilo, alquileno C0- 6-heterociclilo, alquilen C0-6-N(Rb)2, C(O)Ra, alquilen C0-6-CO2Ra, C(O)H, y alquilen C0-6-CO2H, dicho alquilo, alquenilo, alquinilo, cicloalquilo, arilo, y heterociclilo está opcionalmente sustituido con uno a tres sustituyentes seleccionados entre Rb, OH, alcoxi C1-6, halogeno, CO2H, CN, Oa(C=O)b alquilo C1-6, oxo, y N(Rb)2, R7 y R8 se seleccionan independientemente entre: H, (C=O)aOb alquilo C1-10, (C=O)aOb cicloalquilo C3-8, (C=O)aOb-arilo, (C=O)aOb-heterociclilo, alquenilo C2-10, alquinilo C2-10, SH, SO2Ra, y (C=O)aNRb2, dicho alquilo, cicloalquilo, arilo, heterociclilo, alquenilo, y alquinilo está opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a, o R7 y R8 se pueden tomar juntos con el nitrogeno al que están unidos para formar a heterociclo monocíclico o bicíclico con 3-7 miembros en cada anillo conteniendo opcionalmente, además del nitrogeno, uno o dos heteroátomos adicionales seleccionados entre N, O y S, dicho heterociclo monocíclico o bicíclico opcionalmente sustituido con uno o más sustituyentes seleccionados entre R6a; Ra es alquilo C1-6, cicloalquilo C3-6, arilo, o heterociclilo; y Rb es independientemente: H, alquilo C1-6, arilo, heterociclilo, cicloalquilo C3-6, (C=O)aOb alquilo C1-6, o S(O)mRa; o una sal o estereoisomero farmacéuticamente aceptable de los mismos.
ARP070105281A 2006-12-06 2007-11-28 Inhibidores de la actividad de la akt AR064010A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US87319806P 2006-12-06 2006-12-06
US88066107P 2007-01-16 2007-01-16
US96787207P 2007-09-06 2007-09-06

Publications (1)

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AR064010A1 true AR064010A1 (es) 2009-03-04

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US (3) US7576209B2 (es)
EP (1) EP2104669B1 (es)
JP (2) JP4431636B1 (es)
KR (1) KR101110598B1 (es)
CN (1) CN101600706B (es)
AR (1) AR064010A1 (es)
AU (1) AU2007328286B2 (es)
BR (1) BRPI0719580A2 (es)
CA (1) CA2670760C (es)
CL (1) CL2007003495A1 (es)
CO (1) CO6190528A2 (es)
CR (1) CR10851A (es)
EA (1) EA016195B1 (es)
EC (1) ECSP099376A (es)
ES (1) ES2527567T3 (es)
GE (1) GEP20125469B (es)
GT (1) GT200900146A (es)
HK (1) HK1137758A1 (es)
HN (1) HN2009001112A (es)
IL (2) IL198826A (es)
MA (1) MA31027B1 (es)
MX (1) MX2009006052A (es)
NI (1) NI200900106A (es)
NO (1) NO20092569L (es)
NZ (2) NZ595829A (es)
PE (1) PE20081341A1 (es)
SV (1) SV2009003283A (es)
TN (1) TN2009000224A1 (es)
TW (1) TWI386410B (es)
WO (2) WO2008070041A2 (es)

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