Pharmaceutical epinephrine-pilocarpine compounds

Details Pharmaceutical epinephrine-pilocarpine compounds Pharmaceutical epinephrine-pilocarpine compounds

1989-11-13

1991-10-08

Fan, Jane T.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

514397, 544133, 548336, A61K 31415, C07D23358

Patent

active

050554670

ABSTRACT:
The present invention relates to new racemic and optically active compounds containing a first moiety derived from a pilocarpine compound in which the furanone ring of pilocarpine is replaced by a hetero-ring containing a secondary nitrogen hetero-atom, and a second moiety derived from an epinephrine compound or a .beta.-adrenergic blocking compound, linked at the secondary nitrogen atom of the furanone-replacing hetero-ring of the pilocarpine compound and at the hydroxyl group of the epinephrine compound or of the .beta.-adrenergic blocking compound, via a carbonyl linker, and pharmaceutically acceptable acid addition salts thereof.
The new compounds of the present invention are potent ocular hypotensives exhibiting minimal deleterious pupillary effects.

REFERENCES:
patent: 3470197 (1969-09-01), Van Dyke
Drug and Therapeutics Bulletin, vol. 21(22):85-88 (Nov. 1983).
Gelatt, Kirk et al., Am. J. Res. 44(1):2018-2027 (Nov. 1983).
Soderstrom, Mats et al., American Journal of Ophthalmology 107:465-470 (May 1989).
Koda et al., J. Pharm. Sci., 62, 2021 (1973).

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