AR062731A1 - Derivados de quinazolinona e isoquinolinona, composiciones farmaceuticas que los contienen, y su uso para tratar o prevenir trastornos relacionados con el estres o la depresion. - Google Patents

Derivados de quinazolinona e isoquinolinona, composiciones farmaceuticas que los contienen, y su uso para tratar o prevenir trastornos relacionados con el estres o la depresion.

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Publication number
AR062731A1
AR062731A1 ARP070103999A ARP070103999A AR062731A1 AR 062731 A1 AR062731 A1 AR 062731A1 AR P070103999 A ARP070103999 A AR P070103999A AR P070103999 A ARP070103999 A AR P070103999A AR 062731 A1 AR062731 A1 AR 062731A1
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AR
Argentina
Prior art keywords
alkyl
optionally substituted
heterocyclic ring
cycloalkyl
halogen
Prior art date
Application number
ARP070103999A
Other languages
English (en)
Inventor
J J Letourneau
P Jokiel
S E Napier
K K Bo
M Ohlmeyer
D R Mcarthur
Fiona Jeremiah
P D Ratcliffe
Jurgen Schulz
Original Assignee
Pharmacopeia Inc
Organon Nv
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.)
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Publication date
Application filed by Pharmacopeia Inc, Organon Nv filed Critical Pharmacopeia Inc
Publication of AR062731A1 publication Critical patent/AR062731A1/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D243/00—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms
    • C07D243/06—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4
    • C07D243/08—Heterocyclic compounds containing seven-membered rings having two nitrogen atoms as the only ring hetero atoms having the nitrogen atoms in positions 1 and 4 not condensed with other rings
    • 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
    • C07D403/04—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
    • 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
    • A61K31/47—Quinolines; Isoquinolines
    • A61K31/472—Non-condensed isoquinolines, e.g. papaverine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/22—Anxiolytics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/24—Antidepressants
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A61P25/36—Opioid-abuse
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D217/00—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems
    • C07D217/22—Heterocyclic compounds containing isoquinoline or hydrogenated isoquinoline ring systems 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 carbon atoms of the nitrogen-containing ring
    • C07D217/24—Oxygen atoms
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D239/00—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
    • C07D239/70—Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings condensed with carbocyclic rings or ring systems
    • C07D239/72—Quinazolines; Hydrogenated quinazolines
    • C07D239/86—Quinazolines; Hydrogenated quinazolines with hetero atoms directly attached in position 4
    • C07D239/88—Oxygen atoms
    • C07D239/91—Oxygen atoms with aryl or aralkyl radicals attached in position 2 or 3
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • 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
    • C07D401/04—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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—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
    • C07D405/02—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D409/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D471/02—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
    • C07D471/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente se refiere a un derivado de quinazolinona o isoquinolinona de formula (1) donde R1 es alquilo C1-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3, alquenilo C2-6, alquinilo C2-6, estando dichos alquilo C1-6, cicloalquilo C3-6 y cicloalquil C3-6-alquilo C1-3 opcionalmente sustituidos con hidroxi, alquiloxi C1-6, ciano o uno o más halogenos; R2 es arilo C1-6 opcionalmente sustituido con uno a tres sustituyentes seleccionados entre halogeno, hidroxi, ciano, alquilo C1-6, cicloalquilo C3-6, alquiloxi C1-6, cicloalquiloxi C3-6, estando dichos alquilo C1-6, cicloalquilo C3-6, alquiloxi C1-6 y cicloalquiloxi C3-6, opcionalmente sustituidos con uno o más halogenos; o R2 es un sistema de anillo heteroarilo de 5-10 miembros que comprende un heteroátomo seleccionado entre N, O y S, y está opcionalmente sustituido con un sustituyente seleccionado entre metilo, alquiloxi C1-6 y halogeno; o R2 es cicloalquilo C4-7; R3 es un sustituyente opcional seleccionado entre. alquilo C1-6, alquiloxi C1-6 y halogeno, estando dicho alquilo C1-6 y alquiloxi C1-6 opcionalmente sustituidos con uno o más halogenos; R4 es un grupo ubicado en la posicion 6 o 7 del anillo quinazolinona o isoquinolinona y tiene la formula 2, donde R5 junto con uno de R6 forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatomica adicional seleccionada entre O, S y NR9, estando dicho anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, halogeno, hidroxi y oxo, o R5 junto con uno de R7 y R8 forman un anillo heterocíclico de 6-8 miembro opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, halogeno, hidroxi y oxo; cada R6 es independientemente H, halogeno o alquilo C1-4 opcionalmente sustituido con halogeno o SO2CH3, o uno de R6 junto con R5 forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatomica adicional seleccionada entre O, S y NR9, estando dicho anillo heterocíclico opcionalmente sustituido con tino o dos sustituyentes seleccionados entre metilo, halogeno, hidroxi y oxo; R7 y R8 son independientemente H, alquilo C1-6, cicloalquilo C3-6, cicloalquil C3-6-alquilo C1-3, cianoC1-3alquilo, arilo C6-10, aril C6-10-alquilo C1-3, alquiloxi C1-3-alquilo C1-3 o acilo C1-6, estando dichos alquilo C1-6, cicloalquilo C3-6 y cicloalquil C3-6-alquilo C1-3 opcionalmente sustituidos con hidroxi, uno o más halogenos o dialquilamino C1-2; o R7 y R8, junto con el nitrogeno al cual están unidos, forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatomica adicional seleccionada entre O, S y NR10, estando dicho anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados entre alquilo C1-6, halogeno, hidroxi, alquiloxi C1-6, ciano y COOR11; o uno de R7 y R8 es Y, CH2Y o CH2CH2Y, donde Y es un anillo heterocíclico saturado de 4-6 miembros que comprende una especie heterocíclica seleccionada entre O, SO2 y NR10, estando dicho anillo opcionalmente sustituido con 1-2 sustituyentes seleccionados entre metilo o halogeno; o uno de R7 o R8 junto con R5 forman un anillo heterocíclico de 6-8 miembros que está opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, halogeno, hidroxi y oxo; o uno de R7 y R8 junto con R12 forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatomica adicional seleccionada entre O, S y NR13, estando dicho anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, hidroxi y oxo; R9 y R10 son independientemente H, alquilo C1-6 o acilo C1-6; R11 es H o alquilo C1-6; cada R12 es independientemente H o alquilo C1-4, o uno de R12 junto con uno de R7 o R8 forman un anillo heterocíclico saturado o no saturado de 4-8 miembros que opcionalmente comprende una especie heteroatomica adicional seleccionada entre O, S y NR13, estando dicho anillo heterocíclico opcionalmente sustituido con uno o dos sustituyentes seleccionados entre metilo, hidroxi y oxo; R13 es H, alquilo C1-6 o acilo C1-6; m es 2-3; y X es N o CH; o una sal o solvato farmacéuticamente aceptable del mismo.
ARP070103999A 2006-09-11 2007-09-11 Derivados de quinazolinona e isoquinolinona, composiciones farmaceuticas que los contienen, y su uso para tratar o prevenir trastornos relacionados con el estres o la depresion. AR062731A1 (es)

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US84371806P 2006-09-11 2006-09-11

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AR062731A1 true AR062731A1 (es) 2008-11-26

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Country Link
US (1) US7820649B2 (es)
EP (1) EP2069315B1 (es)
JP (1) JP5256202B2 (es)
KR (1) KR20090107994A (es)
CN (1) CN101600698B (es)
AR (1) AR062731A1 (es)
AT (1) ATE523500T1 (es)
AU (1) AU2007296634B2 (es)
CA (1) CA2663161C (es)
CL (1) CL2007002635A1 (es)
CO (1) CO6160322A2 (es)
EC (1) ECSP099177A (es)
IL (1) IL197530A0 (es)
MX (1) MX2009002686A (es)
NO (1) NO20091012L (es)
NZ (1) NZ575426A (es)
PE (1) PE20080841A1 (es)
RU (1) RU2009113612A (es)
TW (1) TW200827352A (es)
WO (1) WO2008033764A2 (es)

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