185030-18-6Relevant academic research and scientific papers
A potent, long-acting, orally active (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamide: A novel muscarinic M3 receptor antagonist with high selectivity for M3 over M2 receptors
Mitsuya,Kobayashi,Kawakami,Satoh,Ogino,Kakikawa,Ohtake,Kimura,Hirose,Sato,Numazawa,Hasegawa,Noguchi,Mase
, p. 5017 - 5029 (2007/10/03)
A novel series of (2R)-2-[(1R)-3,3-difluorocyclopentyl]-2-hydroxy-2-phenylacetamides was designed and synthesized based on the structure and biological profiles of an active metabolite 2 of our prototype muscarinic M3 receptor selective antagon
Substituted piperidine derivatives as muscarinic M3 receptor antagonists
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, (2008/06/13)
PCT No. PCT/JP96/02904 Sec. 371 Date Apr. 9, 1998 Sec. 102(e) Date Apr. 9, 1998 PCT Filed Oct. 7, 1996 PCT Pub. No. WO97/13766 PCT Pub. Date Apr. 17, 1997This invention provides substituted heteroaromatic ring derivatives which are represented by a genera
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.
1,4-di-substituted piperidine derivatives
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, (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.
