324-41-4Relevant articles and documents
ARYL-PYRIDINE DERIVATIVES AS ALDOSTERONE SYNTHASE INHIBITORS
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Page/Page column 53, (2011/06/19)
The present invention provides a compound of formula (I) or a pharmaceutically acceptable salt thereof, wherein R1, R2, R3, R4, R5 and n are defined herein. The invention also relates to a method for manufacturing compounds of the invention, and their therapeutic uses. The present invention further provides a combination of pharmacologically active agents and a pharmaceutical composition.
Synthesis and antinociceptive activity of pyrrolidinylnaphthalenes
Collina, Simona,Azzolina, Ornella,Vercesi, Dina,Sbacchi, Massimo,Scheideler, Mark Albert,Barbieri, Annalisa,Lanza, Enrica,Ghislandi, Victor
, p. 1925 - 1930 (2007/10/03)
In this paper the synthesis of the racemates (2R,3S/2S,3R)-1,2-dimethyl-3-[2-(6-substituted naphthyl)]-3-hydroxypyrrolidine 1b-d [(2R,3S/2S,3R)-1b-d] are reported. Compounds 1b-d were prepared by reaction of the racemic 1,2-dimethyl-3-pyrrolidone 2 with the lithiation product obtained from 2-bromo-6-substituted naphthalene 3b-d. Pharmacological properties of (2R,3S/2S,3R)-1a-d are also described. Analgesic activity was investigated by the hot plate test and binding affinities towards μ, δ and κ opioid receptors were evaluated. A preliminary evaluation of the in vivo side-effects was also accomplished using the rota-rod test. Interesting antinociceptive activity was shown by all compounds and in particular by 1d, which is the most active compound, since it is six-fold more potent than morphine and has lower side effects on the locomotory activity. Copyright (C) 2000 Elsevier Science Ltd.