Uses of modafinil and its D/L enantiomers

Details Uses of modafinil and its D/L enantiomers Uses of modafinil and its D/L enantiomers

2002-02-19

2002-10-15

Webman, Edward J. (Department: 1617)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

C424S451000, C424S464000

Reexamination Certificate

active

06465519

ABSTRACT:

TECHNICAL FIELD OF THE INVENTION
This invention relates to new uses of Modafinil and its D/L enantiomers, particularly the new uses in the pharmaceutical preparation field. This invention provides new uses of Modafinil and its DL enantiomers in preparing the medicine for increasing and enhancing the quantity and quality of normal spermatozoa in mate mammals, the medicine for enhancing the pregnant capacity in female mammals, the medicine for treating infertility, subfertility and sex dysfunction in male and female mammals, the medicine for enhancing the sexual function in mammals.
BACKGROUND OF THE INVENTION
As stated in the U.S. Pat. No. 4,177,290, Modafinil is a known chemical. The chemical name of Modafinil is:
2-[(Diphenylmethyl) sulfinyl]-N-Acetamide
The structure of Modafinil is shown as follows:
Modafinil's formula is C
15
H
15
NO
2
S and the molecular weight is 273.35, which is insoluble in water and cyclohexane, sparingly or slightly soluble in methanol and acetone. Modafinil and its D/L enantiomers are white or whitish crystals. The racemic compound has a melting point of 163-165° C. The racemic compound and both of the enantiomers have the same characteristics stated above.
As published in Proceedings of the Meeting of the 5
th
International Congress of Sleep Research, p.470. European Sleep Research Society. Jun. 28-Jul. 3, 1987, Copenhagen. Modafinil is a vigilance-inducing agent used in the treatment of paroxysmal narcolepsy and idiopathic hypersomnia. Modal and its D/L enantiomers have been eligible for marketing in Great Britain, France and USA, mainly used for treating paroxysmal narcolepsy and idiopathic hypersomnia. No reports regarding the new use of Modafinil as a medicine for enhancing reproductive or sexual ability as stated in this document have been found in the literature.
BRIEF DESCRIPTION OF THE INVENTION
The purpose of this invention is to provide new uses of Modafinil and its D/L enantiomers in preparing the medicine for increasing and enhancing the quantity and quality of normal spernatozoa in male mammals, the medicine for enhancing the pregnant capacity in female mammals, the medicine for treating infertility, subfertility and sex dysfunction in male and female mammals, the medicine for enhancing the sexual function in mammals.
DETAILED DESCRIPTION OF THE INVENTION
The preparation of Modafinil consists of many steps, e.g. reaction of diphenyl-methanol and thiourea and chloroacetic acid, and then oxidation and a Sedation, etc. The detailed methodology in the Example 1 is referred to the methodology of Example 1 in the U.S. Pat. No. 4,177,290.
In the following, 3 examples of pharmacological experiments in rats are described. As rat is a kind of mammal close to human being, the effects of Modafinil in rats can be deduced to have the same effects in human beings.


REFERENCES:
patent: 4177290 (1979-12-01), Lafon
patent: 6348500 (2002-02-01), Fu
B. Saletu, et al., “Differential Effects of the New Central Adrenergic Agonist Modafinil and d-Amphetamine on Sleep and Early Morning Behavior in Elderlies”, Arancim-Forsch./Drug Res. 39(II), No. 10, p. 1268 (1989).

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