Fluorine-containing 1,4-disubstituted piperidine derivatives

Details Fluorine-containing 1,4-disubstituted piperidine derivatives Fluorine-containing 1,4-disubstituted piperidine derivatives

1997-07-31

1999-09-07

Chang, Ceila

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

514256, 514318, 514326, 544233, 544242, 546194, 546208, 546209, 546210, 546213, 546214, 546222, 546224, A61K 31445, C07D21146

Patent

active

059487925

ABSTRACT:
Novel fluorine-containing 1,4-disubstituted piperidine derivatives, ##STR1## such as, for example, yclopentyl!-2-hydroxy-2-phenylacetamide or pharmaceutically acceptable salt thereof, are potent and selective antagonists for muscarinic M.sub.3 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.

REFERENCES:
patent: 5750540 (1998-05-01), Tsuchiya et al.
Japanese language publication "Seitai no Kagaku" (biochemistry), vol. 42(5), p. 380-385, 1991 and partial English translation.
Chem. Pharm. Bull., vol. 32, No. 3, (1984), Sugai, Saburo, et al., "Studies on Spasmolytics I. Synthesis and Spasmolytic . . . piperidines", p. 967-976.
Chem. Pharm. Bull., vol. 32, No. 3, (1984), Sugai, Saburo et al., "Studies on Spasmolytics. II. Synthesis . . . Compounds", p. 977-985.
Chem. Pharm. Bull. vol. 32, No. 3, (1984), Sugai, Saburo et al, "Studies on Spasmolytics. III. Synthesis . . . Salts", p. 1126-1134.
Chem. Pharm. Bull. vol. 33, No. 2, (1985), Yoshida, Seiichiro et al., "Structure-Activity Relationship . . . piperidine Derivatives", p. 818-822 .

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