Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
2001-02-08
2002-04-16
Jones, Dwayne C. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Nitrogen containing other than solely as a nitrogen in an...
Reexamination Certificate
active
06372799
ABSTRACT:
TECHNICAL FIELD
This invention relates to new chemical entities as shown below and to methods of treatment of disease states modulated by allergic, inflammatory, or cholinergic activities in a mammal, using said new chemical entities.
The compounds of the invention include chemical entities of the following Formula I
where
R
1
is H and R
2
is H or methyl, and the pharmaceutically acceptable salts thereof.
The compounds of this inventions have been found to possess pharmacological properties that render said compounds to be useful in treating allergies, inflammations, various types of ocular diseases (such as for example vernal conjunctivitis and allergic conjunctivitis), different types of smooth muscle hyperreactivity (such as for example bronchial hyperreactivity) and asthma or other diseases that are mediated through histaminic receptors of various types.
More particularly, this invention relates to entities and to methods of treating allergic disorders (such as for example allergic rhinitis), motion sickness, pulmonary disorders (such as for example asthma, bronchitis, cough and bronchial hyperreactivity), skin disorders (such as for example urticaria, psoriasis and atopic dermatitis), gastrointestinal disorders (such as for example hypersecretory syndromes including Zollinger-Ellison syndrome, gastric irritation and enteritis), and other inflammatory disorders and/or allergic disorders (such as for example ocular conjunctivitis and ocular keratitis), while avoiding side effects (such as sedation, cardiac arrhythmias and ocular irritation), using said chemical entities.
The invention also refers to compositions, containing at least one of said chemical entities and combinations of the present compounds with various other chemical entities.
BACKGROUND OF THE INVENTION
This invention relates specifically to anti-allergic and anti-inflammatory compounds, having therapeutic use in various diseases, most importantly for patients suffering from allergies, including urticaria, atopic dermatitis, allergic rhinitis, ocular conjunctivitis and keratitis.
Formula 2. DIPHENHYDRAMINE
The present compounds demonstrate chemical similarities to diphenhydramine (Benadryl®) and dimenhydrinate (Dramamine®) and the secondary amine (R
1
=H; R
2
=Me; see FIG. 1) has been described in the prior art as a naturally occurring metabolites of diphenhydramine. Sedative side effects have severely limited the therapeutic usefulness of diphenhydramine and such side effects can been reduced or eliminated by using the compounds of the present invention.
SUMMARY OF THE INVENTION
The present invention is concerned with chemical entities as described below, methods of using said chemical entities for therapeutic purposes and compositions containing a therapeutically effective amount of at least one compound or a pharmaceutically acceptable acid addition salts thereof, having the formula:
where
R
1
H and R
2
is H or methyl, and the pharmaceutically acceptable salts thereof.
The compounds of the present invention have been synthesized according to methods that are well known to those skilled in the art.
The compounds of this invention have also been studied biologically. Significant differences are found between the compounds of the present invention and diphenhydramine. Thus, diphenhydramine has profound sedative side effects while the compounds of the present invention have no detectable sedative activity. The antihistaminic activities of the compounds have been investigated, using the methodology described below.
REFERENCES:
Database CA on STN AN: 106169, Andreau, Spain, “Aryl-substituted Isopropylamines” Abstract to ES 420193 A1, Jun. 16, 1976.
J. Clin. Pharmacol 1986; 26: 529-533; “Pharmacokinestics of Diphenydraine and a Demethylated Metabolite Following Intravenous and Oral Administration”; Blyden, et al.
Bridge Pharma, Inc.
Jones Dwayne C.
Nields & Lemack
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