Muscarinic antagonists

Details Muscarinic antagonists Muscarinic antagonists

1996-02-16

1999-03-16

Dees, Jose'G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514241, 514255, 514256, 514316, 514318, 514321, 544180, 544215, 544238, 544295, 544315, 544319, 544360, 546186, 546187, 546188, 546189, 546190, 546191, C07D29508, C07D30781, C07D33358, A61K 31495

Patent

active

058830960

ABSTRACT:
Di-N-substituted piperazine or 1,4 di-substituted piperadine compounds of formula I ##STR1## wherein one of Y and Z is N and the other is N, CH, or C-alkyl;
X is --O--, --SO.sub.0-2 --, amino, substituted amino, --CO--, --CH.sub.2 --, mono or di-substituted methylene, --CS--, --CONR.sup.20 --, --NR.sup.20 --SO.sub.2 --, --NR.sup.20 CO--, --SO.sub.2 NR.sup.20 --, --CH.dbd.CH--, --C.tbd.C-- or --NHC(O)NH--;
R is optionally substituted phenyl, aryl or cycloalkyl, or other substituents as defined in the specification;
R.sup.1 and R.sup.21 are H, CN or optionally substituted alkyl, or other substituents as defined in the specification;
R.sup.2 is optionally substituted cycloalkyl or piperidyl, or other substituents as defined in the specification; and
R.sup.3, R.sup.4, R.sup.5, R.sup.20, R.sup.27 and R.sup.28 are as defined in the specification; are muscarinic antagonists useful for treating cognitive disorders such as Alzheimer's disease; pharmaceutical compositions and methods of preparation are also disclosed, as well as synergistic combinations of compounds of the above formula or other compounds capable of enhancing acetylcholine release with acetylcholinesterase inhibitors.

REFERENCES:
patent: 2792398 (1957-05-01), Kyrides
patent: 2819273 (1958-01-01), Drain et al.
patent: 3772298 (1973-11-01), Bartman et al.
patent: 3852455 (1974-12-01), Carr
patent: 3988456 (1976-10-01), Nishimura et al.
patent: 4068070 (1978-01-01), Sakai et al.
patent: 4251655 (1981-02-01), Scott et al.
patent: 4525358 (1985-06-01), Balter et al.
patent: 4757074 (1988-07-01), Coker et al.
patent: 4895841 (1990-01-01), Sugimoto et al.
patent: 5010078 (1991-04-01), Abou-Gharbia et al.
patent: 5100901 (1992-03-01), Sugimoto et al.
patent: 5318967 (1994-06-01), Bruderer et al.
Baumgold et al., European Journal of Pharmacology 251 (1994) 315-317.
Melchiorre, et al., J. Med. Chem, 1993, 36, 3734-3737.
Doods, et al., Life Sciences, vol. 52, pp. 497-503 (1993).
Eberlein, et al., Trends in Pharmacol Sci. Dec. 1989 pp. 50-54.
Logemann, et al., Brit. J. Pharmacol (1961) 17, 286-296.
Wilkerson et al, J. Med. Chem., 36 (20) (1993), pp. 2899-2907.
Vidaluc et al, J. Med. Chem., 37 (5) (1994), pp. 689-695.
Drukarch et al, Eur. J. Pharmacol., 141 (1-2) (1987), pp. 153-157.
Provan et al, Brit. J. Pharmacol., 111 (4) (1994), pp. 1103-1110.
Cheng et al, Biochem. Pharmacol., 22 (1973), pp. 3099-3108.
Watson et al, J. Pharmacol. Exp. Ther., 237 (1986), pp. 411-418.
Chemical Abstracts, 70, 21 (1969), abstract 96754t.
Dankwardt et al, Tet. Let., 36, 28 (1995), pp. 4923-4926.
Protiva et al, Collect. Czech. Chem. Commun., 40, 12 (1975), pp. 3904-3923.
Chemical Abstracts, 53, abstract 20096f.
Chemical Abstracts, 53, abstracts 12306f and 12307d.
Chemical Abstracts, 53, abstract 9254b.
Chemical Abstracts, 53, abstract 8172b.
Chemical Abstracts, vol. 45, No. 12 (1951) 5153, Ochiai et al, "Electrolytic reduction of the pyridinium ion."

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