Pharmaceutical epinephrine-pilocarpine compounds and process of

Details Pharmaceutical epinephrine-pilocarpine compounds and process of Pharmaceutical epinephrine-pilocarpine compounds and process of

1991-10-08

1993-03-30

Ivy, C. Warren

Organic compounds -- part of the class 532-570 series

Organic compounds

Four or more ring nitrogens in the bicyclo ring system

5483147, C07D 2358

Patent

active

051985454

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, Jr.
Koda et al., J. Pharm. Sciences, vol. 62, No. 12, pp. 2021-2023 (1973).
Gelatt et al., Am. J. Vet. Res., vol. 44, No. 1, pp. 2018-2027 (1983).
Soderstrom, American Journal of Ophthalmology, vol. 107, pp. 465-470 (1989).
Drug and Therapeutics Bulletin, vol. 21 (22), pp. 85-88, (1983).

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