Cyclic carbamate analogues of (+)-pilocarpine

Details Cyclic carbamate analogues of (+)-pilocarpine Cyclic carbamate analogues of (+)-pilocarpine

1989-12-05

1991-06-18

Daus, Donald G.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

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

548229, 548344, 548342, A61K 3142, C07D26304

Patent

active

050250272

ABSTRACT:
Pilocarpine analogues are provided having the structure ##STR1## where one of R.sub.1 or R.sub.2 is an alkyl, such as methyl, ethyl, propyl, butyl, and so forth, and the corresponding secondary alkyl groups, an aralkyl, such as benzyl, phenylethyl, phenylpropyl, and the corresponding secondary aralkyl residues, or a cycloalkyl having less than about 12 carbon atoms. R.sub.3 has at least two carbon atoms but less than about 9. These pilocarpine analogues have improved duration of biological activity with respect to pilocarpine. A particularly preferred compound is a muscarinic agonist equipotent with pilocarpine, where R.sub.2 is methyl, and R.sub.3 is ethyl.

REFERENCES:
patent: 4332813 (1982-01-01), Firestone
Gonzales et al., Tetrahedron Letters, vol. 30, No. 16, pp. 2145-2148 (May 8, 1989).
Sauerberg et al., Chem. Abstr, vol. 110, Entry 231941 (p) (Jun. 1989).
Sauerberg et al., Jour. Med. Chem., vol. 32 (No. 6), pp. 1322-1326 (1989).
H. Bundgaard et al., J. Med. Chem., 28, 1985, p. 979.
Aboul-Enein et al., Meth. and Find. Exptl. Clin. Pharmacol., 4, 1982, p. 321.
Parameswaran et al., J. Med. Chem., 30, 1987, p. 936.
Gonzalez et al., "Synthesis of (+)-Pilocarpine Analogs with a 2-Oxazolidone Structure", Tetrahedron Letters, vol. 30, No. 16, 1989, pp. 2145-2148.

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