Thienopyridine derivatives as modulators of metabotropic...

C - Chemistry – Metallurgy – 07 – D

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C07D 495/04 (2006.01) A61K 31/4365 (2006.01) A61P 25/28 (2006.01)

Patent

CA 2630890

The present invention relates to new mGluRl and niGluR5 receptor subtype preferring ligands of formula (I): wherein X represents a group selected from (CH2)n, CH=CH, NH, N(CH3), NHCH2, N(CH3)CH2, O, OCH2, CH2COO, NHCH2COO; n is an integer of O to 2; Y represents a subtituent selected from H, CH3, F, Cl, Br; Z is H or CH3; R is alkyl, cycloalkyl, an optionally substituted phenyl or an optionally substituted heteroaryl, and/or geometric isomers and/or salts and/or hydrates and/or solvates thereof, to the processes for producing the same, to pharmaceutical compositions containing the same and to their use in therapy and/or prevention of pathological conditions which require the modulation of mGluRl mGluR5 receptors such as neurological disorders, psychiatric disorders, acute and chronic pain and neuromuscular dysfunctions of the lower urinary tract.

La présente invention concerne de nouveaux ligands ayant une préférence pour le sous-type de récepteurs mGluR1 et mGluR5 de formule (I), dans laquelle: X représente un groupe choisi parmi (CH2)n, CH=CH, NH, N(CH3), NHCH2, N(CH3)CH2, O, OCH2, CH2COO, NHCH2COO; n est un nombre entier de 0 à 2; Y représente un substituant choisi parmi H, CH3, F, Cl, Br; Z est H ou CH3; R est alkyle, cycloalkyle, un phényle éventuellement substitué ou un hétéroaryle éventuellement substitué, et/ou des isomères géométriques et/ou des sels et/ou des hydrates et/ou des solvates de ceux-ci. L'invention concerne également des procédés pour la production de tels ligands, des compositions pharmaceutiques les contenant et leur utilisation dans le traitement et/ou la prévention de conditions pathologiques nécessitant la modulation de récepteurs mGluR1 et mGluR5 tels que des troubles neurologiques, des troubles psychiatriques, la douleur aiguë et chronique et des dysfonctionnements neuromusculaires des voies urinaires inférieures.

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