Thiazolyl mglur5 antagonists and methods for their use

C - Chemistry – Metallurgy – 07 – D

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C07D 417/06 (2006.01) C07D 417/14 (2006.01) C07D 471/04 (2006.01)

Patent

CA 2583572

The identification of a unique series of compounds which possesses special advantages in terms of drug--like properties due to their possessing advantageous properties in terms of potency and/or pharmacokinetic and/or selectivity and/or in vivo receptor occupancy properties. Specifically, the selection of a 1,3-thiazol-2-yl ring member linked by an ethynylene to the 3 position of a pyridyl ring or the 5 position of a pyrimidinyl ring, wherein the ring is substituted with selected substituents, results in a compound having superior drug-like properties. The invention includes pharmaceutically acceptable salt forms of these heterocyclic compounds, in particular chloride salts and trifluoroacetate salts.

Identification d'une série unique de composés offrant des avantages spéciaux en termes de propriétés médicamenteuses qui découlent elles-mêmes de propriétés avantageuses sur le plan de la puissance et/ou de la pharmacocinétique et/ou de la sélectivité et/ou de l'occupation de récepteur in vivo. On décrit spécifiquement la sélection d'un élément cyclique 1,3-thiazol-2-yle lié par éthynylène à la position 3 d'un cycle pyridyle ou la position 5 d'un cycle pyrimidinyle, sachant que le cycle est substitué par des substituants spécifiques, ce qui donne un composé aux propriétés médicamenteuses supérieures. On décrit enfin des formes de sel pharmaceutiquement acceptables de ces composés hétérocycliques, en particulier des sels chlorure et trifluoroacétate.

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