申请人:Banyu Pharmaceutical Co., Ltd.
公开号:US05948792A1
公开(公告)日:1999-09-07
Novel fluorine-containing 1,4-disubstituted piperidine derivatives, represented by general formula \x9bI! ##STR1## such as, for example, (2R)-N-\x9b1-(6-aminopyridin-2-ylmethyl)piperidin-4-yl!-2-\x9b(1R)-3,3-difluoroc yclopentyl!-2-hydroxy-2-phenylacetamide or pharmaceutically acceptable salt thereof, are potent and selective antagonists for muscarinic M.sub.3 receptors with little side effects. The compounds of formula \x9bI! 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.
含氟的新型1,4-二取代哌啶衍生物,通式\x9bI! ##STR1##例如,(2R)-N-\x9b1-(6-氨基吡啶-2-基甲基)哌啶-4-基!-2-\x9b(1R)-3,3-二氟环戊基!-2-羟基-2-苯乙酰胺或其药用盐,是对M.sub.3受体具有强效和选择性拮抗作用的化合物,副作用很小。通式\x9bI!的化合物表现出优异的口服活性、活性持续时间和药代动力学。它们可用于治疗和预防呼吸系统疾病,如慢性阻塞性肺疾病;泌尿系统疾病,如尿失禁;以及消化系统疾病,如肠易激综合征和晕动病。