Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1999-06-29
2001-04-03
Raymond, Richard L. (Department: 1624)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S422000, C514S454000, C514S467000, C514S488000, C514S643000, C546S261000, C548S559000, C549S388000, C549S448000, C560S133000, C564S286000
Reexamination Certificate
active
06211201
ABSTRACT:
FIELD OF THE INVENTION
The field of the invention is cholinergic agents.
BACKGROUND
Pyridostigmine 3-[[(Dimethylamino)-carbonyl]oxy]-1-methylpyridinium (Mestinon™), and Neostigmine 3-[[(Dimethylamino)-carbonyl]oxyl]-N,N, N-trimethylbenzeaminium (synstigmin), and Edrophonium N-Ethyl-3hydroxy-N, N-dimethylbenzenaminium are all cholinergic agents. These compounds have several known uses including treatment of mysasthenia gravis, esophageal chest pain, and pre-exposure antidote to chemical warfare nerve agents. These compounds may also be useful in treating carpel tunnel syndrome.
Pyridostigmine and neostigmine are generally administered to a patient as a bromide salt, while Edrophonium is generally administered as a chloride salt. While these known monovalent salts are generally considered to be adequate, it is now contemplated that multivalent salts would potentially be more stable, and may have better physical characteristics, especially in solid physical dosage form. There may also be advantageous pharmokinetics over the monovalent salts. Still fturther it is contemplated that compounds having multiple quaternary ammonium sites may have usefll pharmaceutical benefits.
SUMMARY OF THE INVENTION
According to the present invention quaternary ammonium cholinergic agents are complexed with a multivalent anion, or with multiple monovalent anions. The complexes may be administered orally to a patient as a cholinergic agent, or for some other purpose. Numerous modifications are contemplated, including modifications to the ring structure of the compound, and substitution and functionalization of the ring. Other contemplated modifications include the use of different anions, including various monovalent and polyvalent anions, and both organic and inorganic anions.
REFERENCES:
patent: 4246416 (1981-01-01), Sommer et al.
patent: 4672120 (1987-06-01), Sommer et al.
patent: 4677222 (1987-06-01), Sommer et al.
patent: 4686293 (1987-08-01), Sommer et al.
patent: 4692530 (1987-09-01), Sommer et al.
Granger Colin
Orr Robert
Ramasamy Kandasamy
Fish Robert D.
Fish & Associates, LLP
ICN Pharmaceuticals, Inc.
Raymond Richard L.
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