Organic compounds -- part of the class 532-570 series – Organic compounds – Heterocyclic carbon compounds containing a hetero ring...
Patent
1994-09-27
1996-06-25
Springer, David B.
Organic compounds -- part of the class 532-570 series
Organic compounds
Heterocyclic carbon compounds containing a hetero ring...
A61K 3140, C07D45102
Patent
active
055301380
ABSTRACT:
There is disclosed a compound shown by a formula of ##STR1## wherein R.sub.1 is a hydrogen atom alkyl group having 1-4 carbon atoms or acyl group having 1-4 carbon atoms: R.sub.2 and R.sub.3 are a hydrogen atom, alkyl group having 1-4 carbon atoms, phenyl radical, halogen atom, cyano radical, acyl group having 1-4 carbon atoms, nitro radical, alkoxy group having 1 or 2 carbon atoms, or substituted or non-substituted amino group, respectively; n is an integer of 1-3; and dotted line means a possible ring, and a salt thereof. The compound and salt bind with muscarinic receptor in brain to develop a powerful actuation thereof and thus those can be used as an effective ingredient for preventing and curing senile dementias, and more particularly Alzheimer's disease.
REFERENCES:
"Tetrahydropyridyloxadiazoles: Semirigid Muscarinic Ligands," J. Med. Chem. 1991, 34, pp. 1086-1094, Graham A. Showell et al.
"Synthesis and Muscarinic Activities of Quinuclidin-3-yltrizaole and -tetrazole Derivatives," J. Med. Chem. 1992, 35, pp. 1280-1290, Harry J. Wadsworth et al.
"Novel Functional M.sub.1 Selective Muscarinic Agonists. Synthesis and Structure--Activity Relationships of 3-(1,2,5-Thiadiazolyl)-1,2,5,6-tetrahydro-1-methylpyridines," J. Med. Chem. 1992, 35, pp. 2274-2283, Per Sauerberg et al.
"Muscarinic Cholinergic Binding in Rat Brain," Proc. Nat. Acad. Sci. USA, vol. 71, No. 5, pp. 1725-1729, May 1974, Henry I. Yamamura et al.
"Multiple in Vitro Interactions with and Differential in Vivo Regulation of Muscarinic Receptor Subtypes by Tetrahydroaminoacridine," The Journal of Pharmacology and Experimental Therapeutics, vol. 250, No. 2, pp. 573-581, Donna D. Flynn et al.
Baba Yutaka
Hirooka Kiyotaka
Kurono Masayasu
Sawai Kiichi
Suzuki Tomoo
Sanwa Kagaku Kenkyusho Co. Ltd.
Springer David B.
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