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AR075517A1 - Derivados de isoxazol-isoxazol y de isoxazol-isotiazol - Google Patents

Derivados de isoxazol-isoxazol y de isoxazol-isotiazol

Info

Publication number
AR075517A1
AR075517A1 ARP100100476A ARP100100476A AR075517A1 AR 075517 A1 AR075517 A1 AR 075517A1 AR P100100476 A ARP100100476 A AR P100100476A AR P100100476 A ARP100100476 A AR P100100476A AR 075517 A1 AR075517 A1 AR 075517A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
halogen
alkoxy
hydroxy
optionally substituted
Prior art date
Application number
ARP100100476A
Other languages
English (en)
Inventor
Maria-Clemencia Hernandez
Roland Jakob-Roetne
Andrew Thomas
Matthew C Lucas
Original Assignee
Hoffmann La Roche
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
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR075517A1 publication Critical patent/AR075517A1/es

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D261/00—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings
    • C07D261/02—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings
    • C07D261/06—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more double bonds between ring members or between ring members and non-ring members
    • C07D261/10—Heterocyclic compounds containing 1,2-oxazole or hydrogenated 1,2-oxazole rings not condensed with other rings having two or more 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
    • C07D261/18—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen
    • C—CHEMISTRY; METALLURGY
    • 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
    • C07D413/06—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 linked by a carbon chain containing only aliphatic carbon atoms
    • 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
    • A61K31/41—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
    • A61K31/42—Oxazoles
    • A61K31/422—Oxazoles not condensed and containing further heterocyclic rings
    • 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
    • A61P25/02—Drugs for disorders of the nervous system for peripheral neuropathies
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • 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
    • 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
    • C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/12—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 linked by a chain containing hetero atoms as chain links
    • 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
    • C07D487/10—Spiro-condensed systems

Landscapes

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

Abstract

La presente invencion se refiere a derivados de isoxazol-isoxazol y de isoxazol-isotiazol, que tienen afinidad y selectividad por el receptor de GABA A alfa5, a su obtencion, a composiciones farmacéuticas que los contienen y a su utilizacion como medicamentos. Los compuestos activos de la presente invencion utiles como intensificadores cognitivos o para el tratamiento terapéutico y/o profiláctico, de trastornos cognitivos como la enfermedad de Alzheimer. Reivindicacion 1: Compuestos de la formula (1), en la que es alquilo inferior, opcionalmente sustituido por halogeno, ciano, hidroxi, alcoxi inferior o halogeno-alcoxi inferior; arilo, heteroarilo, cicloalquilo, heterociclilo; cada uno de ellos está opcionalmente sustituido por halogeno, ciano, hidroxi, alquilo inferior, halogeno-alquilo inferior, ciano-alquilo inferior, hidroxi-alquilo inferior, (alquilo inferior)-C(=O)OH, (alquilo inferior)-C(=O)O-alquilo inferior, alquilo inferior)-CO-NR5R6, (alquilo inferior)-NR5R6, alcoxi inferior-alquilo inferior, -CO-alquilo inferior, -C(=O)OH, -C(=O)O-alquilo inferior, -CONR5R6, -NR5R6, alcoxi inferior, halogeno-alcoxi inferior, -SO2-alquilo inferior, -SO2-NR5R6, cicloalquilo, feniloxi o fenilo, R2 es alquilo inferior opcionalmente sustituido por halogeno, ciano, hidroxi, alcoxi inferior o halogeno-alcoxi inferior, R3 es alquilo inferior, opcionalmente sustituido por carboxi, halogeno o hidroxilo; arilo, heteroarilo, cicloalquilo, heterociclilo; cada arilo, heteroarilo, cicloalquilo, heterociclilo está opcionalmente sustituido por carboxi, halogeno, hidroxi o alquilo inferior; o -NR7R8, R4 es H o alquilo inferior, o R3 y R4 junto con el nitrogeno al que están unidos forman un anillo heterocíclico, R5 es H o alquilo inferior, R6 es H o alquilo inferior, R7 es H o alquilo inferior, R8 es H o alquilo inferior, Y es O o S, X es CH2-O- o -CH=CH-, o sus sales o ésteres farmacéuticamente activos.
ARP100100476A 2009-02-19 2010-02-18 Derivados de isoxazol-isoxazol y de isoxazol-isotiazol AR075517A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09153162 2009-02-19

Publications (1)

Publication Number Publication Date
AR075517A1 true AR075517A1 (es) 2011-04-06

Family

ID=42111584

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100100476A AR075517A1 (es) 2009-02-19 2010-02-18 Derivados de isoxazol-isoxazol y de isoxazol-isotiazol

Country Status (15)

Country Link
US (1) US8173652B2 (es)
EP (1) EP2398782B1 (es)
JP (1) JP5478640B2 (es)
KR (1) KR101361465B1 (es)
CN (1) CN102317270B (es)
AR (1) AR075517A1 (es)
AU (1) AU2010215515A1 (es)
BR (1) BRPI1016117A8 (es)
CA (1) CA2749649C (es)
ES (1) ES2431617T3 (es)
IL (1) IL213974A0 (es)
MX (1) MX2011007774A (es)
SG (1) SG173666A1 (es)
TW (1) TW201033201A (es)
WO (1) WO2010094669A1 (es)

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US10266551B2 (en) 2013-03-15 2019-04-23 Global Blood Therapeutics, Inc. Compounds and uses thereof for the modulation of hemoglobin
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US10100043B2 (en) 2013-03-15 2018-10-16 Global Blood Therapeutics, Inc. Substituted aldehyde compounds and methods for their use in increasing tissue oxygenation
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ES2993155T3 (en) 2013-03-15 2024-12-23 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
MY191087A (en) 2013-03-15 2022-05-30 Global Blood Therapeutics Inc Compounds and uses thereof for the modulation of hemoglobin
BR112015021986A2 (pt) 2013-03-15 2017-07-18 Global Blood Therapeutics Inc compostos e seus usos para a modulação de hemoglobina
EA202092627A1 (ru) 2013-11-18 2021-09-30 Глобал Блад Терапьютикс, Инк. Соединения и их применения для модуляции гемоглобина
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Also Published As

Publication number Publication date
MX2011007774A (es) 2011-08-12
US8173652B2 (en) 2012-05-08
EP2398782B1 (en) 2013-09-18
KR101361465B1 (ko) 2014-02-10
US20100210651A1 (en) 2010-08-19
KR20110120322A (ko) 2011-11-03
WO2010094669A1 (en) 2010-08-26
CN102317270B (zh) 2014-10-08
CN102317270A (zh) 2012-01-11
EP2398782A1 (en) 2011-12-28
AU2010215515A1 (en) 2011-08-11
CA2749649C (en) 2017-04-04
CA2749649A1 (en) 2010-08-26
BRPI1016117A8 (pt) 2018-01-02
IL213974A0 (en) 2011-08-31
SG173666A1 (en) 2011-09-29
JP5478640B2 (ja) 2014-04-23
JP2012518025A (ja) 2012-08-09
ES2431617T3 (es) 2013-11-27
BRPI1016117A2 (pt) 2016-04-12
TW201033201A (en) 2010-09-16

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