Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Reexamination Certificate
1998-10-05
2001-02-27
Criares, Theodore J. (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
Reexamination Certificate
active
06194433
ABSTRACT:
FIELD OF THE INVENTION
The present invention relates to methods for improving blood flow and supply to female sexual organs, and more particularly, methods for the treatment of female erectile dysfunction. The methods of the present invention comprise the utilization of pharmaceutical compositions to induce erections in females having erectile dysfunction.
BACKGROUND
Females have sexual dysfunction. Post-menopausal women often complain of discomfort with intercourse, dryness of the vagina and diminished vaginal arousal. Studies comparing sexual dysfunction in couples have revealed 40% of the men had erectile or ejaculatory dysfunction whereas 63% of the women had arousal or orgasmic dysfunctions. Similar to male sexual dysfunction, the prevalence of female sexual dysfunction has been shown to increase with age and be associated with the presence of vascular risk factors and the development of the menopause.
The clitoris is the homologue of the penis. It is a cylindrical, erectile organ composed of the glans, corporal body and the crura. The corporal body is surrounded by a fibrous sheath, tunica albuginea, which encases cavernosal tissue consisting of sinusoids and surrounding smooth muscle. The clitoris responds to sexual excitement by tumescence and erection, although this does not occur with the degree of pressure elevation as found during penile erection. The characteristics of the clitoral blood flow, however, approximately parallel those of the male. See K. Park et al., “Vasculogenic female sexual dysfunction: The hemodynamic basis for vaginal engorgement insufficiency and clitoral erectile insufficiency,”
Int. J Impotence Res.
9:27 (1997).
Post-menopausal women and women with a history of vascular risk factors have been shown to have significantly more complaints of self-reported female vaginal and clitoral dysfunctions than pre-menopausal women or women without vascular risk factors. Such problems include, but are not limited to, atherosclerosis-induced vaginal engorgement insufficiency and clitoral erectile insufficiency syndromes.
What is needed is a pharmaceutical that is effective to treat such syndromes. Such pharmaceutical should lack in significant side effects.
SUMMARY OF THE INVENTION
The present invention relates to methods for improving blood flow and supply to female sexual organs, and more particularly, methods for the treatment of female erectile dysfunction. The methods of the present invention comprise the utilization of pharmaceutical compositions to induce erections in females having erectile dysfunction. The methods include treatment of female erectile dysfunction with quinolines and quinolones, including derivatives thereof. Quinolines and quinolones, including flosequinan, have pharmacological characteristics which improve blood flow and supply to female sexual organs.
It is not intended that the present invention be limited by the nature of the derivative. In one embodiment, the present invention contemplates halogenated quinolines (e.g., bromoquinoline) and isoquinolines (e.g., 1-methylisoquinoline and 5-nitroisoquinoline). In another embodiment, the present invention contemplates halogenated quinolones (e.g, flosequinolone). In a preferred embodiment, the quinolone is a thioquinolone or a sulphinyl or suphonyl derivatives thereof. In one embodiment, the halogenated quinolone is flosequinan (7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone).
In one embodiment, the present invention contemplates a method, comprising: a) providing: i) a female with symptoms of sexual dysfunction, and ii) flosequinan; and b) administering said flosequinan to said female. It is not intended that the present invention be limited to particular symptoms of sexual dysfunction. A variety of such symptoms are contemplated, including but not limited to, poor blood flow to the sexual organs and/or failure to achieve orgasm. In one embodiment, the present invention contemplates administering said flosequinan to said female under conditions such that blood flow to the sexual organs of said female is improved.
In another embodiment, the method comprises providing: i) a female with erectile dysfunction, and ii) flosequinan; and introducing said flosequinan to said female such that a clitoral erection is produced.
It is not intended that the present invention be limited by the method of introduction of flosequinan. In one embodiment, the flosequinan is introduced into said female orally. In a preferred embodiment, the female is an adult human and the oral dosage is in a single dose per day of fifty to seventy-five milligrams. In other embodiments said flosequinan is introduced cutaneously, transurethrally, or by standard injection.
The present invention is not limited by the degree of response by the subject. In one embodiment, the erection induced is sufficient for normal stimulation.
It is not intended that the present invention be limited by the nature of the formulation. In one embodiment, the present invention contemplates a formulation comprising a quinoline or derivative thereof in a mixture comprising lactose.
Definitions
As used herein, the term “quinoline” refers to chemical compositions comprising quinoline as set forth in the following structure:
as well as other forms of quinoline, (e.g., isoquinoline):
As used herein, the phrase “derivatives of quinoline” refers to chemical compositions comprising quinoline with a chemical group attached, including halogenated quinoline, e.g., 5-bromoquinolne:
and 1-methylisoquinoline:
As used herein, the phrase “methylsulphinyl derivatives of quinoline” refers to chemical compositions comprising quinoline with a methylsulphinyl group attached. Examples include flosequinan (7-fluoro-1-methyl-3-methylsulphinyl-4-quinolone):
and sulfone metabolites of flosequinan:
As used herein “standard injection” refers to the placement of a pharmaceutical composition into a subject (e.g., with a hypodermic needle). For example, such injection can be made subcutaneously, intravenously, intramuscularly, etc.
As used herein, “by oral administration” refers to the introduction of a pharmaceutical composition into a subject by way of the oral cavity (e.g., in aqueous liquid or solid form).
As used herein, “cutaneously” refers to the introduction of a pharmaceutical composition into a subject by application to the surface of the skin such that the composition is absorbed into the subject.
As used herein, “transurethrally” refers to the introduction of a pharmaceutical composition to the urethra of a subject such that the composition is absorbed into the subject.
As used herein “single dosage” refers to a pharmaceutical composition of a formulation that is capable of achieving its intended effect in a single application.
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Park et al., “Vasculogenic femal sexual dysfunction: The hemodynamic basis for vaginal engorgement insufficiency and clotoral erectile insufficiency,”Int. J. Impotence Res., 9:27-37 (1997).
McMurry,Organic Chemistry, 2nd Ed., Brooks/Cole Publishing, Belmont, CA (1988), pp. 1044-1045 and 1076.
Kelso, et al., “Actions of the Novel Vasodilator, Flosequinan, in Isolated Ventricular Cardiomyocytes,”J. Cardiovasc. Pharmacol.25:
Criares Theodore J.
Cutler Neal R.
Kim Jennifer
Medlen & Carroll LLP
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