BRPI0921795B8 - inibidores radiomarcados do transportador de glicina 1 e seu uso - Google Patents

inibidores radiomarcados do transportador de glicina 1 e seu uso

Info

Publication number
BRPI0921795B8
BRPI0921795B8 BRPI0921795A BRPI0921795A BRPI0921795B8 BR PI0921795 B8 BRPI0921795 B8 BR PI0921795B8 BR PI0921795 A BRPI0921795 A BR PI0921795A BR PI0921795 A BRPI0921795 A BR PI0921795A BR PI0921795 B8 BRPI0921795 B8 BR PI0921795B8
Authority
BR
Brazil
Prior art keywords
glycine transporter
inhibitors
glycine
labeling
functionality
Prior art date
Application number
BRPI0921795A
Other languages
English (en)
Inventor
Alberati Daniela
Maurizio Borroni Edilio
Pinard Emmanuel
Norcross Roger
Hartung Thomas
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 BRPI0921795A2 publication Critical patent/BRPI0921795A2/pt
Publication of BRPI0921795B1 publication Critical patent/BRPI0921795B1/pt
Publication of BRPI0921795B8 publication Critical patent/BRPI0921795B8/pt

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/10Heterocyclic 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 carbon chain containing aromatic rings
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K51/00Preparations containing radioactive substances for use in therapy or testing in vivo
    • A61K51/02Preparations containing radioactive substances for use in therapy or testing in vivo characterised by the carrier, i.e. characterised by the agent or material covalently linked or complexing the radioactive nucleus
    • A61K51/04Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/24Antidepressants
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • GPHYSICS
    • G01MEASURING; TESTING
    • G01NINVESTIGATING OR ANALYSING MATERIALS BY DETERMINING THEIR CHEMICAL OR PHYSICAL PROPERTIES
    • G01N33/00Investigating or analysing materials by specific methods not covered by groups G01N1/00 - G01N31/00
    • G01N33/48Biological material, e.g. blood, urine; Haemocytometers
    • G01N33/50Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing
    • G01N33/58Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances
    • G01N33/60Chemical analysis of biological material, e.g. blood, urine; Testing involving biospecific ligand binding methods; Immunological testing involving labelled substances involving radioactive labelled substances

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • General Health & Medical Sciences (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Biomedical Technology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Psychiatry (AREA)
  • Immunology (AREA)
  • Physics & Mathematics (AREA)
  • Urology & Nephrology (AREA)
  • Molecular Biology (AREA)
  • Hematology (AREA)
  • Hospice & Palliative Care (AREA)
  • Pathology (AREA)
  • Cell Biology (AREA)
  • Biotechnology (AREA)
  • Food Science & Technology (AREA)
  • Pain & Pain Management (AREA)
  • Analytical Chemistry (AREA)
  • Biochemistry (AREA)
  • General Physics & Mathematics (AREA)
  • Microbiology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Optics & Photonics (AREA)
  • Epidemiology (AREA)
  • Plural Heterocyclic Compounds (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

inibidores radiomarcados do transportador de glicina 1. a presente invenção refere-se a novos inibidores radiomarcados de fórmula geral (i) para o transportador de glicina 1 (glyt1), úteis para a marcação e a formação de imagem para diagnóstico da funcionalidade do transportador de glicina 1, em que r1 isopropóxi ou 2, 2, 2-trifluoro-1-metil-etóxi; e r2 é um grupo raiomarcado ch3, em que o radionuclídeo é 3h ou 11c. foi descoberto que os compostos de fórmula (i) radiomarcados podem ser usados como marcador radioativo para pet (tomografia por emissão de pósitrons) para a marcação e a formação de imagem para diagnóstico da funcionalidade do transportador de glicina 1.
BRPI0921795A 2008-11-04 2009-10-26 inibidores radiomarcados do transportador de glicina 1 e seu uso BRPI0921795B8 (pt)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP08168229 2008-11-04
EP08168229.6 2008-11-04
PCT/EP2009/064033 WO2010052143A1 (en) 2008-11-04 2009-10-26 Radiolabelled inhibitors of the glycine 1 transporter

Publications (3)

Publication Number Publication Date
BRPI0921795A2 BRPI0921795A2 (pt) 2016-01-12
BRPI0921795B1 BRPI0921795B1 (pt) 2020-10-20
BRPI0921795B8 true BRPI0921795B8 (pt) 2021-07-27

Family

ID=41402176

Family Applications (1)

Application Number Title Priority Date Filing Date
BRPI0921795A BRPI0921795B8 (pt) 2008-11-04 2009-10-26 inibidores radiomarcados do transportador de glicina 1 e seu uso

Country Status (21)

Country Link
US (1) US8153679B2 (pt)
EP (1) EP2342197B1 (pt)
JP (1) JP5543477B2 (pt)
KR (1) KR101307671B1 (pt)
CN (1) CN102186844B (pt)
AR (1) AR074084A1 (pt)
AU (1) AU2009312891B2 (pt)
BR (1) BRPI0921795B8 (pt)
CA (1) CA2739869C (pt)
CL (1) CL2011000982A1 (pt)
DK (1) DK2342197T3 (pt)
ES (1) ES2401221T3 (pt)
IL (1) IL211804A (pt)
MX (1) MX2011004350A (pt)
PE (1) PE20110434A1 (pt)
PL (1) PL2342197T3 (pt)
RU (1) RU2512529C2 (pt)
SI (1) SI2342197T1 (pt)
TW (1) TWI449537B (pt)
WO (1) WO2010052143A1 (pt)
ZA (1) ZA201102521B (pt)

Families Citing this family (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP5618047B2 (ja) * 2010-01-29 2014-11-05 国立大学法人千葉大学 ポジトロン断層撮影法およびポジトロン放出化合物

Family Cites Families (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
UA85194C2 (ru) 2003-08-11 2009-01-12 Ф.Хоффманн-Ля Рош Аг Пиперазины с or-замещенной фенильной группой и их применение как ингибиторов glyt 1
UA91536C2 (uk) * 2005-02-07 2010-08-10 Ф. Хоффманн-Ля Рош Аг Гетероциклічні заміщені фенілметанони як інгібітори переносника гліцину 1
ES2382818T3 (es) * 2005-09-29 2012-06-13 Merck Sharp & Dohme Corp. Inhibidores de transportadores glicina radiomarcados

Also Published As

Publication number Publication date
AR074084A1 (es) 2010-12-22
SI2342197T1 (sl) 2013-05-31
PE20110434A1 (es) 2011-07-01
BRPI0921795B1 (pt) 2020-10-20
AU2009312891B2 (en) 2013-07-11
US20100111862A1 (en) 2010-05-06
JP2012507486A (ja) 2012-03-29
KR101307671B1 (ko) 2013-09-12
US8153679B2 (en) 2012-04-10
BRPI0921795A2 (pt) 2016-01-12
MX2011004350A (es) 2011-05-23
PL2342197T3 (pl) 2013-06-28
CN102186844A (zh) 2011-09-14
WO2010052143A1 (en) 2010-05-14
RU2011118230A (ru) 2012-12-20
IL211804A0 (en) 2011-06-30
ES2401221T3 (es) 2013-04-17
KR20110063861A (ko) 2011-06-14
CA2739869C (en) 2016-09-27
DK2342197T3 (da) 2013-02-18
CA2739869A1 (en) 2011-05-14
TW201019964A (en) 2010-06-01
JP5543477B2 (ja) 2014-07-09
CL2011000982A1 (es) 2012-02-03
ZA201102521B (en) 2012-09-29
EP2342197B1 (en) 2013-01-16
CN102186844B (zh) 2014-08-13
RU2512529C2 (ru) 2014-04-10
EP2342197A1 (en) 2011-07-13
IL211804A (en) 2013-11-28
AU2009312891A1 (en) 2010-05-14
TWI449537B (zh) 2014-08-21

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B07D Technical examination (opinion) related to article 229 of industrial property law [chapter 7.4 patent gazette]
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B06U Preliminary requirement: requests with searches performed by other patent offices: procedure suspended [chapter 6.21 patent gazette]
B06A Patent application procedure suspended [chapter 6.1 patent gazette]
B09A Decision: intention to grant [chapter 9.1 patent gazette]
B16A Patent or certificate of addition of invention granted [chapter 16.1 patent gazette]

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B16C Correction of notification of the grant [chapter 16.3 patent gazette]

Free format text: PRAZO DE VALIDADE: 20 (VINTE) ANOS CONTADOS A PARTIR DE 26/10/2009, OBSERVADAS AS CONDICOES LEGAIS. PATENTE CONCEDIDA CONFORME ADI 5.529/DF, QUE DETERMINA A ALTERACAO DO PRAZO DE CONCESSAO

B21F Lapse acc. art. 78, item iv - on non-payment of the annual fees in time

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B24J Lapse because of non-payment of annual fees (definitively: art 78 iv lpi, resolution 113/2013 art. 12)

Free format text: EM VIRTUDE DA EXTINCAO PUBLICADA NA RPI 2693 DE 16-08-2022 E CONSIDERANDO AUSENCIA DE MANIFESTACAO DENTRO DOS PRAZOS LEGAIS, INFORMO QUE CABE SER MANTIDA A EXTINCAO DA PATENTE E SEUS CERTIFICADOS, CONFORME O DISPOSTO NO ARTIGO 12, DA RESOLUCAO 113/2013.