Compositions and method for treatment of cough

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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Details

C514S850000

Reexamination Certificate

active

06362197

ABSTRACT:

BACKGROUND OF THE INVENTION
Conventional cough preparations containing an effective anti-tussive agent such as codeine have long been used for the symptomatic relief of coughs. However, codeine has various side effects which are undesirable.
Accordingly, the present invention relates to compositions of matter useful as pharmaceutical compositions having anti-tussive activity, and a method of treating warm-blooded animals affected by coughs or bronchoconstriction by administering an effective amount of the pharmaceutical compositions of the invention.
SUMMARY OF THE INVENTION
The problems of the prior art have been overcome by the present invention, which provides pharmaceutical compositions possessing anti-tussive activity, and a method of administering the same to warm-blooded animals, including humans. The active anti-tussive agent in accordance with the present invention is a quaternary ammonium compound represented by the following formula (I) and its pharmaceutically acceptable salts:
wherein Y and E are independently selected from —CH
2
—R
2
or:
wherein R, R
1
and R
2
are independently selected from hydrogen, C
1
-C
8
alkyl, C
3
-C
8
alkoxyalkyl and C
7
-C
12
aralkyl; and where R
3
, R
4
and R
5
are independently selected from bromine, chlorine, fluorine, carboxy, hydrogen, hydroxy, hydroxymethyl, methanesulfonamido, nitro, sulfamyl, trifluoromethyl, C
2
-C
7
alkanoyloxy, C
1
-C
6
alkyl, C
1
-C
6
alkoxy, C
2
-C
7
alkoxycarbonyl, C
1
-C
6
thioalkyl, aryl and N(R
6
, R
7
) where R
6
and R
7
are independently selected from hydrogen, acetyl, methanesulfonyl and C
1
-C
6
alkyl, An
31
is the acid addition salt of a pharmaceutically acceptable acid or the anion from a pharmaceutically acceptable salt, and isolated enantiomeric, diastereomeric and geometric isomers thereof, and mixtures thereof, with the proviso that Y and E cannot both be —CH
2
—R
2
in the same compound.


REFERENCES:
patent: 995256 (1965-06-01), None
Caplus 100:114885, Lyttkens et al., Local anesthetics and tinnitus. Proposed peripheral mechanism of action of lidocaine, Journal for oto-rhino-laryngology and its borderlands. 46(1) see abstract, 1984.

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