Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1999-02-04
2000-10-31
Rotman, Alan L.
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544231, 544279, 544280, 544238, 546 15, 546 16, 546112, 546113, 546192, 546225, 546226, 514278, 514318, 514320, 514329, 514330, 514331, A61K 31505, A61K 31445, C07D40900, C07D21900, C07D21130
Patent
active
061403334
ABSTRACT:
The invention relates to compounds represented by the general formula [I] ##STR1## [wherein Ar means an aryl group or a heteroaryl group which may have a substitutive group selected from a group consisting of a halogen atom, a lower alkyl group and a lower alkoxy group; R.sup.1 means a C.sub.3 -C.sub.6 cycloalkyl group which is substitutable with a fluorine atom; R.sup.2 and R.sup.4 mean hydrogen atoms, groups represented by --(A.sup.1).sub.m --NH--B or the like; R.sup.3 and R.sup.5 mean hydrogen atoms, C.sub.1 -C.sub.6 aliphatic hydrocarbon groups or the like which are substitutable with a lower alkyl group(s); n means 0 or 1; and X means an oxygen atom or a sulfur atom].
Compounds according to the invention, since they not only have potent selective antagonistic activity against muscarinic M.sub.3 receptors but also exhibit excellent oral activity, durability of action and pharmacokinetics, are very useful as safe and effective remedies against respiratory, urinary and digestive diseases with little adverse side effects.
REFERENCES:
patent: 5344835 (1994-09-01), Alker et al.
Bertram G. Katzung, MD, PhD, "Basic and Clinical Pharmacology", 4th ed. Appleton & Lange, Chapter 8, pp. 83-92 (1989).
Henri N. Doods, "Selective Muscarinic Antagonists as Bronchodilators", Drug News & Perspective, 5(6), pp. 345-352.
Kawakami Kumiko
Nishikibe Masaru
Nomoto Takashi
Ohsawa Hirokazu
Ohwaki Kenji
Banyu Pharmaceutical Co Ltd
Covington Raymond
Rotman Alan L.
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