16098-80-9Relevant academic research and scientific papers
Fluorine-containing 1,4-disubstituted piperidine derivatives
-
, (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.
1,4-di-substituted piperidine derivatives
-
, (2008/06/13)
This invention provides novel 1,4-di-substituted piperidine derivatives of the general formula ?I! STR1 and the pharmaceutically acceptable salts thereof, wherein: Ar represents a phenyl group or a five- or six-membered heteroaromatic group having one or two hetero atoms selected from the group consisting of an oxygen atom, a sulfur atom and a nitrogen atom in which one or two optional hydrogen atoms on the ring may be replaced by substituent groups selected from the group consisting of a halogen atom and a lower alkyl group; R1 represents a cycloalkyl group of 3 to 6 carbon atoms or a cycloalkenyl group of 3 to 6 carbon atoms; R2 represents a saturated or unsaturated aliphatic hydrocarbon radical of 5 to 15 carbon atoms; and X represents O or NH. These compounds have selective antagonistic activity against the muscarinic M3 receptors and can hence be used safely with a minimum of side effects.
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).
