BR0308945A - Derivados radiomarcados de quinolina e quinolinona e uso dos mesmos como ligantes para receptores de glutamato metabotrópicos - Google Patents

Derivados radiomarcados de quinolina e quinolinona e uso dos mesmos como ligantes para receptores de glutamato metabotrópicos

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Publication number
BR0308945A
BR0308945A BR0308945-2A BR0308945A BR0308945A BR 0308945 A BR0308945 A BR 0308945A BR 0308945 A BR0308945 A BR 0308945A BR 0308945 A BR0308945 A BR 0308945A
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Prior art keywords
alkyl
metabotropic glutamate
halo
formula
cycloalkyl
Prior art date
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BR0308945-2A
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English (en)
Inventor
Anne Simone Josephine Lesage
Francois Paul Bischoff
Cornelus Gerardus Mari Janssen
Hilde Lavreysen
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Janssen Pharmaceutica Nv
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Application filed by Janssen Pharmaceutica Nv filed Critical Janssen Pharmaceutica Nv
Publication of BR0308945A publication Critical patent/BR0308945A/pt

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    • A61K51/04Organic compounds
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    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
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    • AHUMAN NECESSITIES
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
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    • A61K51/04Organic compounds
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    • A61K51/044Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins
    • A61K51/0463Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine, rifamycins having six-membered rings with at least one nitrogen and one oxygen as the ring hetero atoms, e.g. 1,2-oxazines
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Abstract

"DERIVADOS RADIOMARCADOS DE QUINOLINA E QUINOLINONA E USO DOS MESMOS COMO LIGANTES PARA RECEPTORES DE GLUTAMATO METABOTRóPICOS". A presente invenção refere-se a derivados radiomarcados de quinolina e quinolinona de acordo com a fórmula (I-A)^ *^ ou (I-B)^ *^ que apresentam atividade antagonista de receptores de glutamato metabotrópicos, em particular atividade do receptor de mGlu1, e sua preparação; ela refere-se ainda a composições compreendendo os mesmos, bem como ao seu uso para marcar e identificar sítios de receptores de glutamato metabotrópicos e para fazer a imagem de um órgão. Em uma modalidade preferida, X representa O; R^ 1^ representa C~ 1~-C~ 6~ alquila; C~ 3~-C~ 12~ cicloalquila ou (C~ 3~-C~ 12~ cicloalquila), C~ 1~-C~ 6~ alquila, em que um ou mais átomos de hidrogênio em uma porção C~ 1~-C~ 6~ alquila ou em uma porção C~ 3~-C~ 12~ cicloalquila podem ser opcionalmente substituídos com C~ 1~-C~ 6~ alquilóxi, arila, halo ou tienila; R^ 2^ representa hidrogênio; halo; C~ 1~-C~ 6~ alquila ou amino; cada um de R^ 3^ e R^ 4^ representa, independentemente, hidrogênio ou C~ 1~-C~ 6~ alquila; ou R^ 2^ e R^ 3^ podem ser tomados juntos para formar -R^ 2^-R^ 3^, que representa um radical bivalente de fórmula -Z~ 4~-CH~ 2~-CH~ 2~-CH~ 12~- ou -Z~ 4~-CH~ 2~-CH~ 2~-, com Z~ 4~ sendo O ou NR^ 11^, em que R^ 11^ é C~ 1~-C~ 6~ alquila; e em que cada radical bivalente é opcionalmente substituído COM C~ 1~-C~ 6~ alquila; ou R^ 3^ e R^ 4^ podem ser tomados juntos para formar um radical bivalente de fórmula -CH~ 2~-CH~ 2~-CH~ 2~-CH~ 2~-; R^ 5^ representa hidrogênio; Y representa O; e arila representa fenila opcionalmente substituída com halo. Os compostos radiomarcados mais preferidos são aqueles nos quais o isótopo radioativo é selecionado do grupo de ^ 3^H, ^ 11^C e ^ 18^F. A invenção também refere-se ao uso dos mesmos em um método de diagnóstico, em particular para marcar e identificar um receptor mGluR1 em material biológico, bem como ao uso dos mesmos para fazer a imagem de um órgão, em particular usando PET.
BR0308945-2A 2002-03-29 2003-03-26 Derivados radiomarcados de quinolina e quinolinona e uso dos mesmos como ligantes para receptores de glutamato metabotrópicos BR0308945A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP02076254 2002-03-29
PCT/EP2003/003240 WO2003082350A2 (en) 2002-03-29 2003-03-26 Radiolabelled quinoline and quinolinone derivatives and their use as metabotropic glutamate receptor ligands

Publications (1)

Publication Number Publication Date
BR0308945A true BR0308945A (pt) 2005-01-04

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR0308945-2A BR0308945A (pt) 2002-03-29 2003-03-26 Derivados radiomarcados de quinolina e quinolinona e uso dos mesmos como ligantes para receptores de glutamato metabotrópicos

Country Status (19)

Country Link
US (1) US7517517B2 (pt)
EP (1) EP1492571A2 (pt)
JP (1) JP4573533B2 (pt)
KR (1) KR101061561B1 (pt)
CN (1) CN1642580B (pt)
AU (1) AU2003226737B2 (pt)
BR (1) BR0308945A (pt)
CA (1) CA2479109C (pt)
EA (1) EA009334B1 (pt)
HK (1) HK1079700A1 (pt)
HR (1) HRP20040870A2 (pt)
IL (1) IL164299A (pt)
MX (1) MXPA04009435A (pt)
NO (1) NO330688B1 (pt)
NZ (1) NZ535438A (pt)
PL (1) PL218788B1 (pt)
UA (1) UA78548C2 (pt)
WO (1) WO2003082350A2 (pt)
ZA (1) ZA200407820B (pt)

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AU2003226737A1 (en) 2003-10-13
NO20044635L (no) 2004-10-27
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US7517517B2 (en) 2009-04-14
EA009334B1 (ru) 2007-12-28
HRP20040870A2 (en) 2005-06-30
HK1079700A1 (en) 2006-04-13
CA2479109C (en) 2011-08-02
JP4573533B2 (ja) 2010-11-04
US20060083676A1 (en) 2006-04-20
UA78548C2 (en) 2007-04-10
MXPA04009435A (es) 2005-01-25
PL371607A1 (en) 2005-06-27
WO2003082350A2 (en) 2003-10-09
NO330688B1 (no) 2011-06-06
WO2003082350A3 (en) 2004-03-04
EP1492571A2 (en) 2005-01-05
JP2005524679A (ja) 2005-08-18
KR20040093711A (ko) 2004-11-08
IL164299A0 (en) 2005-12-18
PL218788B1 (pl) 2015-01-30
CA2479109A1 (en) 2003-10-09
AU2003226737B2 (en) 2008-09-04
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EA200401285A1 (ru) 2005-02-24
NZ535438A (en) 2006-08-31
ZA200407820B (en) 2005-12-28

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