New substituted propiolic acid amides, useful for treatment and prevention of e.g. pain, anxiety and panic attacks, are inhibitors of the mGluR5 receptor

摘要

Propiolic acid amides (I), optionally as pure stereoisomers, particularly enantiomers or diastereomers, including racemates and mixtures in any proportion, also salts and solvates, are new. Propiolic acid amides of formula A-N(R 1>)-(CR 2>R 3>) a-(CR 4>R 5>) b-(CR 6>R 7>) c-NR 8>-CO-Ctriple boundC-R 9> (I), optionally as pure stereoisomers, particularly enantiomers or diastereomers, including racemates and mixtures in any proportion, also salts and solvates, are new a, b and c : 0 or 1, totaling 1-3; A : particular heterocyclic groups; R 1>-R 8>hydrogen or various substituents Full definitions are given in the DEFINITIONS -Full Definitions field. An independent claim is included for several methods for preparing (I). ACTIVITY : Analgesic; Antimigraine; Antidepressant; Nootropic; Neuroprotective; Antiparkinsonian; Anticonvulsant; Tranquilizer; Antitussive; Uropathic; Antidiarrheal; Antipruritic; Antiasthma; Cerebroprotective; Ophthalmological; Antialcoholic; Antismoking. MECHANISM OF ACTION : Regulation, particularly inhibition, of the mGluR5 receptor. The compound 1-(3-phenylpropiolyl)-4-(thiophen-3-yl)-piperazine has IC50 against the porcine mGluR5 receptor of 1.89 mu M.