C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 309/12 (2006.01) A61K 31/497 (2006.01) A61P 25/00 (2006.01)
Patent
CA 2697941
The present invention relates to 1-(1-methylethyl)-4-{[4-(tetrahydro-2H-pyran- 4-yloxy)phenyl]carbonyl}piperazine (Formula) or a pharmaceutically acceptable salt thereof, in particular the hydrochloride salt thereof and crystalline forms of the hydrochloride salt; to processes for the preparation of the compound or its salt; to compositions containing it; and to its use in the treatment or prophylaxis of neurological or psychiatric diseases, such as cognitive impairment, fatigue or a sleep disorder, for example in a mammal such as a human. The compound or a salt thereof has affinity for and is an antagonist and/or inverse agonist of the histamine H3 receptor.
La présente invention concerne 1-(1-méthyléthyl)-4-{[4-(tétrahydro-2H-pyran-4- yloxy)phényl]carbonyl}pipérazine (Formule) ou un sel pharmaceutiquement acceptable dudit composé, en particulier le sel de chlorhydrate de celui-ci et les formes cristallines dudit sel de chlorhydrate. L'invention concerne également des procédés de préparation du composé, ou du sel de celui-ci, des compositions le contenant et son utilisation dans le traitement ou la prophylaxie de maladies neurologiques ou psychiatriques, telles qu'un trouble cognitif, la fatigue ou un trouble du sommeil, par exemple chez un mammifère tel qu'un humain. Le composé, ou un sel de celui-ci, présente une affinité pour le récepteur H3 de l'histamine et constitue un antagoniste et/ou un agoniste inverse de celui-ci.
Best Desmond John
Mak Sing Yeung
Orlek Barry Sidney
Rassias Geracimos
Theobald Pamela Joan
Glaxo Group Limited
Gowling Lafleur Henderson Llp
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