Bispilocarpic acid ester derivatives and process for their prepa

Details Bispilocarpic acid ester derivatives and process for their prepa Bispilocarpic acid ester derivatives and process for their prepa

1993-05-26

1995-07-25

Higel, Floyd D.

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

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

514397, 514399, 5483144, 5483415, C07D23364, C07D40514, A61K 31415

Patent

active

054363500

ABSTRACT:
The object of the invention are bispilocarpates useful in the treatment of glaucoma and having the formula ##STR1## wherein A) Y is hydrogen or the acyl group ##STR2## and W is the group --O--A--O--Z--Y', wherein Y' is hydrogen or the acyl group ##STR3## the groups R and R' having different meanings and may be the same or different and A is an aliphatic, aromatic or heterocyclic bridging group, and --Z--Y' is ##STR4## or B) W is OR, wherein R has the same meaning as above, Y is ##STR5## where R' has the same meaning as above, B means the same as A and Z'--OR' is ##STR6## or C) W and Y together mean ##STR7## where the symbols have the same meanings as above.

REFERENCES:
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"0,0'-(1,4-Xylylene) Bispilocarpic Acid Esters As New Potential Double Prodrugs Of Pilocarpine For Improved Ocular Delivery, II. Physicochemical Properties, Stability, Solubility And Enzymatic Hydrolysis," Jarvinen et al. II, International Journal of Pharmaceutics, 75 (1991) 249-258 (applicants' own publication, published after first priority date).
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Chemical Abstracts, vol. 116 (1992), Formula Index, s. 4043F.

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