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AR077534A1 - Derivados de isoxazol, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades relacionadas con el receptor gaba aalfa5 - Google Patents

Derivados de isoxazol, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades relacionadas con el receptor gaba aalfa5

Info

Publication number
AR077534A1
AR077534A1 ARP100101438A ARP100101438A AR077534A1 AR 077534 A1 AR077534 A1 AR 077534A1 AR P100101438 A ARP100101438 A AR P100101438A AR P100101438 A ARP100101438 A AR P100101438A AR 077534 A1 AR077534 A1 AR 077534A1
Authority
AR
Argentina
Prior art keywords
lower alkyl
halogen
independently selected
group
cyano
Prior art date
Application number
ARP100101438A
Other languages
English (en)
Inventor
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 AR077534A1 publication Critical patent/AR077534A1/es

Links

Classifications

    • 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
    • C07D413/12—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 chain containing hetero atoms as chain links
    • 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
    • A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • 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
    • A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • A61P29/02—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID] without antiinflammatory effect
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/14—Antivirals for RNA viruses
    • A61P31/18—Antivirals for RNA viruses for HIV
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • C07D401/12—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
    • 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

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Psychiatry (AREA)
  • Pain & Pain Management (AREA)
  • Psychology (AREA)
  • Virology (AREA)
  • Cardiology (AREA)
  • Molecular Biology (AREA)
  • Rheumatology (AREA)
  • Communicable Diseases (AREA)
  • Heart & Thoracic Surgery (AREA)
  • AIDS & HIV (AREA)
  • Addiction (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Epidemiology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

Los compuestos activos que se proveen tienen afinidad y selectividad para con el receptor de GABA A alfa5. Además, la obtencion de los compuestos activos de la formula 1, la fabricacion de composiciones farmacéuticas que los contienen y su utilizacion como medicamentos. Reivindicacion 1: Un compuesto de la formula 1 en la que X es CR6 o N, en el que R6 es hidrogeno o alquilo inferior; R1 es alquilo inferior, arilo o heteroarilo, dicho alquilo inferior puede estar opcionalmente sustituido por 1- 4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, hidroxi y alcoxi inferior, y dichos arilo y heteroarilo pueden estar opcionalmente sustituidos por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, alquilo inferior, alquilo inferior sustituido por halogeno, alquilo inferior sustituido por hidroxi, (alquilo inferior)-C(O)OH, (alquilo inferior)-C(O)O-alquilo inferior, (alquilo inferior)-CO-NH2, (alquilo inferior)-CO-N(H,alquilo inferior), (alquilo inferior)-CO-N(alquilo inferior)2, (alquilo inferior)-NH2, (alquilo inferior)-N(H,alquilo inferior), (alquilo inferior)-N(alquilo inferior)2, alcoxi inferior-alquilo inferior, CO-alquilo inferior, COOH, COO-alquilo inferior, CONH2, CON(H,alquilo inferior), CON(alquilo inferior)2, cicloalquilo, heterociclilo, arilo, heteroarilo, NH2, N(H,alquilo inferior), N(alquilo inferior)2, hidroxi, alcoxi inferior, feniloxi, SO2-alquilo inferior, SO2-NH2, SO2-N(H,alquilo inferior) y SO2-N(alquilo inferior)2; R2 es hidrogeno o alquilo inferior que puede estar opcionalmente sustituido por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, alquilo inferior y alcoxi inferior; R3 es hidrogeno o alquilo inferior que puede estar opcionalmente sustituido por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, hidroxi, alquilo inferior y alcoxi inferior; R4, R5 se eligen con independencia entre sí entre el grupo formado por hidrogeno, alquilo inferior, SO2-alquilo inferior, cicloalquilo y heterociclilo, opcionalmente sustituido por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, hidroxi, alquilo inferior y alcoxi inferior, o en la que R4 y R5, junto con el átomo de nitrogeno al que están unidos forman un heterociclilo, opcionalmente sustituido por 1-4 sustituyentes elegidos con independencia entre el grupo formado por halogeno, ciano, hidroxi, oxo, alquilo inferior y alcoxi inferior; y sus sales y ésteres farmacéuticamente aceptables.
ARP100101438A 2009-04-30 2010-04-29 Derivados de isoxazol, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades relacionadas con el receptor gaba aalfa5 AR077534A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP09159150 2009-04-30

Publications (1)

Publication Number Publication Date
AR077534A1 true AR077534A1 (es) 2011-09-07

Family

ID=42229188

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100101438A AR077534A1 (es) 2009-04-30 2010-04-29 Derivados de isoxazol, un proceso para su obtencion, composiciones farmaceuticas que los contienen y su uso en el tratamiento de enfermedades relacionadas con el receptor gaba aalfa5

Country Status (15)

Country Link
US (2) US8227461B2 (es)
EP (1) EP2424863B1 (es)
JP (1) JP5478714B2 (es)
KR (1) KR101438261B1 (es)
CN (1) CN102395583B (es)
AR (1) AR077534A1 (es)
AU (1) AU2010243652B2 (es)
BR (1) BRPI1016192A8 (es)
CA (1) CA2750678C (es)
ES (1) ES2431389T3 (es)
IL (1) IL214251A0 (es)
MX (1) MX2011011303A (es)
SG (1) SG175316A1 (es)
TW (1) TW201043621A (es)
WO (1) WO2010125042A1 (es)

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ES2550994T3 (es) * 2007-12-04 2015-11-13 F. Hoffmann-La Roche Ag Derivados de isoxazol-piridina
EP2427458B1 (en) * 2009-05-05 2014-05-07 F.Hoffmann-La Roche Ag Isoxazole-pyridazine derivatives
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US20150374705A1 (en) 2012-02-14 2015-12-31 Shanghai Institues for Biological Sciences Substances for treatment or relief of pain
WO2014001280A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
IN2014DN11027A (es) 2012-06-26 2015-09-25 Aniona Aps
WO2014001279A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
JP6224097B2 (ja) 2012-06-26 2017-11-01 サニオナ・エイピイエス フェニルトリアゾール誘導体及びｇａｂａａ受受容体複合体を調節するための該フェニルトリアゾール誘導体の使用
WO2014001278A1 (en) 2012-06-26 2014-01-03 Aniona Aps A phenyl triazole derivative and its use for modulating the gabaa receptor complex
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Also Published As

Publication number Publication date
JP5478714B2 (ja) 2014-04-23
US8227461B2 (en) 2012-07-24
IL214251A0 (en) 2011-09-27
ES2431389T3 (es) 2013-11-26
CA2750678C (en) 2014-11-04
KR101438261B1 (ko) 2014-09-05
CN102395583B (zh) 2015-04-01
BRPI1016192A8 (pt) 2017-10-10
TW201043621A (en) 2010-12-16
US20100280019A1 (en) 2010-11-04
AU2010243652B2 (en) 2013-02-07
KR20120016069A (ko) 2012-02-22
WO2010125042A1 (en) 2010-11-04
MX2011011303A (es) 2011-11-18
CA2750678A1 (en) 2010-11-04
EP2424863B1 (en) 2013-09-18
SG175316A1 (en) 2011-12-29
BRPI1016192A2 (pt) 2016-04-19
EP2424863A1 (en) 2012-03-07
JP2012524762A (ja) 2012-10-18
US20100280020A1 (en) 2010-11-04
CN102395583A (zh) 2012-03-28
AU2010243652A1 (en) 2011-09-15

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