Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1996-04-08
2002-10-22
Henley, III, Raymond (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
C514S653000
Reexamination Certificate
active
06469009
ABSTRACT:
The present invention is in the area of pharmaceutical compositions and methods of treatment of diseases in humans. More particularly the invention relates to combinations of two or more than two pharmaceutical substances and methods of treatment of allergic disorders.
BACKGROUND OF THE INVENTION
U.S. Pat. No. 4,525,358 discloses 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acids or amides thereof having the formula
wherein
Y is a hydroxyl group or an —NH
2
group,
X and X′ represent independently a hydrogen atom, a halogen atom, a straight or branched chain lower alkoxy radical or a trifluoromethyl radical,
m is 1 or 2, and
n is 1 or 2,
or a non-toxic, pharmaceutically acceptable salt thereof.
The compounds of formula I possess interesting pharmacological properties. In particular, they are useful as antiallergic, antihistaminic, bronchodilatory and antispasmodic agents.
Several patent documents already disclosed binary and/or ternary combinations of pharmaceutical substances in specific amounts in view of treating various disorders in humans. In particular International Patent Application published as WO 88/09656 discloses pharmaceutical compositions of matter comprising an analgesically effective amount of aspirin, sodium salicylate, salicylamide or acetaminophen, in combination with a non-sedating antihistamine, one or more active components selected from a decongestant, cough suppressant, expectorant and further optionally including pharmaceutically acceptable carriers therefor.
International Patent Application published as No. WO 92/04022 discloses compositions for the treatment of cold, cold-like flu and flu-like symptoms comprising an effective amount of a naphthalene derivative and optionally containing one or more therapeutic agents such as decongestant, an antitussive, an expectorant, an antihistamine or a bronchodilatator. Similar examples of combinations of pharmaceutically active substances may be found also in International Patent Publications No. WO 94/08551, No. WO 94/25009 and No. WO 95/07103.
Some documents also disclose the use of specific stereoisomers of pharmaceutical substances for treating disorders in humans while avoiding adverse effects associated with the corresponding racemic mixture. In particular International Patent Applications published as WO 94/06429 and WO 94/06430 disclose methods of treating a condition caused by or contributed to by eosinophilia or enhanced eosinophil function in a human, which comprises administering to a human, in need of eosinophilic therapy, an amount of (+) cetirizine (respectively (−) cetirizine), or a pharmaceutically acceptable salt thereof, substantially free of its (−) stereoisomer (respectively its (+) stereoisomer), said amount being sufficient to alleviate said eosinophilia or enhanced eosinophil function but insufficient to cause said adverse effects.
On the other hand, pseudoephedrine, its hydrochloride and sulfate are well known sympathomimetic drugs recognised as safe therapeutic agents effective in the relief of nasal congestion.
It is well known to those skilled in the art that combinations of pharmaceutical substances should always be handled with care because they are very susceptible of inducing impredictable adverse effects in humans. In some cases, they also induce an efficiency of the treatment which is lower than that of each pharmaceutical substance taken alone.
In the treatment of allergic disorders such as for example a pollen associated allergic rhino-conjunctivitis, care should be taken, when combining an antihistaminic and a decongestant, not only to increase the overall efficiency of the treatment, i.e. the percentage of days during the whole treatment period, when the symptoms of sneezing, rhinorrhea, nasal obstruction, lacrimation, nasal and ocular pruritus are absent or at the most mild, but also to avoid possible adverse effects like insomnia and headache.
Thus an objective of the present invention is to provide a useful combination of pharmaceutical substances for treating various disorders in humans, said combination being able to increase the efficiency of said treatment over the efficiency of each substance alone, while avoiding adverse effects during the said treatment.
Another objective of the present invention is to provide such a useful combination of pharmaceutical substances when the treatment in question is a therapy such as needed for rhinitis, cold, flu, cold-like and flu-like symptoms.
SUMMARY OF THE INVENTION
The present invention is based on the unexpected recognition that the combined use of pseudoephedrine, an individual optical isomer or a pharmaceutically acceptable salt thereof on the one hand and a 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivative, an individual optical isomer or a pharmaceutically acceptable salt thereof on the other hand in the treatment of rhinitis, cold, flu, cold-like and flu-like symptoms results in improved efficiency over each pharmaceutical substance alone based on the patients daily evaluation of symptoms like sneezing, rhinorrhea, nasal obstruction, nasal and ocular pruritus and lacrymation. This improved primary efficiency was obtained without increasing possible adverse effects of the treatment, like insomnia and headache.
DETAILED DESCRIPTION OF THE INVENTION
The present invention encompasses a method of treating a disorder selected from rhinitis, cold, flu, cold-like and flu-like symptoms in a human, which comprises administering to a human in need of such therapy, simultaneously or separately, an effective amount of (i)pseudoephedrine, an individual optical isomer or a pharmaceutically acceptable salt thereof and an effective amount of (ii) at least one compound selected from 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivatives, an individual optical isomer or a pharmaceutically acceptable salt thereof. When administration is effected simultaneously, it is preferably in the form of a pharmaceutical composition comprising a therapeutically effective amount of a mixture consisting essentially of compounds (i) and (ii). Such administration in a single dosage form is preferred.
The term separately as used herein means that compounds (i) and (ii) are administered separately but within a close time proximity, i.e. a lapse of time which is sufficiently short, e.g. not higher than about 3 hours, to keep advantage of their combined therapeutic effects.
The term “a method for treating a disorder selected from rhinitis, cold, flu, cold-like and flu-like symptoms in a human” as used herein means providing relief from the symptoms of sneezing, rhinorrhea, nasal obstruction, nasal and ocular pruritus, lacrymation, and the like.
The term “2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivative” as used herein means a compound having the formula
wherein
Y is a hydroxyl group or an —NH
2
group,
X and X′ represent independently a hydrogen atom, a halogen atom, a straight or branched chain lower alkoxy radical or a trifluoromethyl radical,
m is 1 or 2, and
n is 1 or 2.
The term “lower alkoxy” as used herein means residues of both straight and branched chain aliphatic alcohols having from 1 to 4 carbon atoms, such as methoxy, ethoxy, propoxy and the like. The halogen atom is preferably a chlorine or fluorine atom.
The term “pharmaceutically acceptable salts” as used herein with respect to 2-[4-(diphenylmethyl)-1-piperazinyl]-acetic acid or amide derivatives means not only their addition salts with non-toxic organic and inorganic acids, such as acetic, citric, succinic, ascorbic, hydrochloric, hydrobromic, sulfuric, and phosphoric acids and the like, but also their metal salts (for example sodium or potassium salts), ammonium salts, amine salts and aminoacid salts.
The term “pharmaceutically acceptable salt” as used herein with respect to pseudoephedrine means namely its hydrochloride and sulfate and equivalent non-toxic salts.
The term “individual optical isomer” as used herein means, when the molecule has a centre o
Martin Jean-Pierre
Van De Venne Herman
Henley III Raymond
UCB S.A.
Wenderoth , Lind & Ponack, L.L.P.
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