16098-80-9Relevant articles and documents
Fluorine-containing 1,4-disubstituted piperidine derivatives
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, (2008/06/13)
Novel fluorine-containing 1,4-disubstituted piperidine derivatives, represented by general formula ?I! STR1 such as, for example, (2R)-N-?1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl!-2-?(1R)-3,3-difluorocyclopentyl!-2-hydroxy-2-phenylacetamide or pharmaceutically acceptable salt thereof, are potent and selective antagonists for muscarinic M3 receptors with little side effects. The compounds of formula ?I! exhibit excellent oral activity, duration of activity and pharmacolkinetics. They are useful for treatment and prophylaxis of respiratory diseases, such as chronic obstructive pulmonary diseases; urinary diseases, such as urinary incontinence; and digestive diseases, such as irritable bowel syndrome, and motion sickness.
Analogues of 3-Quinuclidinyl Benzilate
Rzeszotarski, W. J.,Gibson, R. E.,Eckelman, W. C.,Simms, D. A.,Jagoda, E. M.,et al.
, p. 1103 - 1106 (2007/10/02)
A number of analogues of 3-quinuclidinyl benzilate (QNB) have been synthesized and their affinities to muscarinic receptor from rat or dog ventricular muscle measured.We have determined that the muscarinic receptor can to a different degree accomodate either a halogen in the ortho, meta, or para position of one phenyl ring or the repalcement of one phenyl ring with an alkyl group.Our in vitro competition studies show that the affinities lie within a 270-fold range, from the highest affinity compound, 3-quinuclidinyl α-hydroxy-α-cyclopentylphenylacetate (2), to the lowest affinity compound, 3-quinuclidinyl α-hydroxy-α-2-propargylphenylacetate (11).