Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Cyclopentanohydrophenanthrene ring system doai
Reexamination Certificate
1999-12-30
2003-04-29
Webman, Edward B. (Department: 1617)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Cyclopentanohydrophenanthrene ring system doai
C424S434000, C424S045000
Reexamination Certificate
active
06555531
ABSTRACT:
BACKGROUND OF THE INVENTION
This invention relates generally to weight promotion. Weight promotion is desirable in treating many medical and physiological conditions as well as for sports training and other activities. When weight promotion is not possible or effective in weight critical conditions, other means of treatment are used to limit the clinical effects of compromised weight.
Weight Promoting Approaches
Weight promotion can include increasing weight, maintaining weight, or slowing weight loss. There are many medical conditions which call for weight promotion. By example, in such conditions as anorexia nervosa, weight loss can lead to severe illness. Similarly, the frail elderly often suffer loss of appetite due to multiple factors such as anosmia, lack of exercise and depression. Wasting in the elderly constitutes a serious challenge in gerontology.
The depressive component of anorexia nervosa and elderly wasting can be treated, in some cases successfully, with counseling and antidepressant drugs. However, lack of appetite with resulting body emaciation often persists. Modification of body form perception in anorexia nervosa, and engaging activities for the elderly often assists in reversing these conditions. Forced feeding is resorted to in serious cases. While these and other clinical approaches are successful in some cases, disability and even death may occur in others.
Other clinical conditions benefit from weight promoting therapy. Wasting in cancer patients, especially those undergoing chemotherapy, is a challenge to oncologists. Morning sickness can be so severe as to require prolonged hospital stays, putting both the mother and unborn child at risk. Depressive conditions can lead to disinterest in food, with the resulting weight loss in turn exacerbating the underlying depression.
Carefully selected diets offered at optimal times of day are helpful in encouraging adequate food consumption in cancer patients and pregnant women suffering from morning sickness. These approaches are also useful with depressed patients, especially when coupled with anti-depressant drugs.
Low weight, especially in the frail elderly, is a contributing factor to osteoporosis and muscle wasting. The health problems attending major bone breakage and spinal cord collapse caused by these conditions are a serious public health challenge. Many therapy approaches, such as high calcium diets and exercise, provided some slowing of the effects of these challenging diseases. However, current intervention efforts are typically only partially effective in limiting the adverse effects of these conditions.
To promote weight gain among athletes, supercaloric dietary supplements are often used to provide weight gain and muscle mass increase. A disadvantage to dietary supplements is that they often satiate the appetite.
Use of systemic steroids has been previously employed to increase muscle mass. Systemically administered steroids, while highly effective in promoting body mass, have numerous side effects, including toxicity and aggressive behavior. Because of these attendant problems, systemic steroid use has been banned from most sporting events. These drugs are now strictly controlled or illegal in most jurisdictions.
Advantages of VNO Administration of Pharmaceuticals
Some of the present inventors have discovered a class of pharmaceuticals which directly stimulate the vomeronasal organ, hereinafter the VNO. Substances which act through the vomeronasal system are defined as vomeropherins. Because this class of pharmaceuticals are administered directly to the VNO, vomeropherins do not need to enter the systemic circulation in order to exert their therapeutic effects. Instead, when administered to the VNO, such as by a nasal spray, vomeropherins stimulate the VNO directly, triggering a response in the brain, such as in the hypothalamic regions.
Nasally administered vomeropherins do not need to cross the biological barriers that are associated with systemic drug absorption and distribution in order to produce the desired therapeutic effect. Consequently, this class of pharmaceuticals enjoys a rapid onset of action. In addition, because typically only minute quantities of vomeropherins are required to induce a biological response, both production costs and the potential for adverse side effects are minimized.
One characteristic of vomeropherins is that they are typically associated with reproductive factors. In certain treatment schemes, this aspect of vomeropherins is very useful. However, this gender specificity can prove a disadvantage for general applications (Monti-Bloch et al,
J. Steroid Biochem. Molec. Biol
. 39, 573-582 (1991)). Additionally, many of the reproductive effects in female patients are limited to pre-menopausal women.
There is a long standing need for a weight promoting pharmaceutical that would, be effective in weight compromised patients of different ages and genders. It would be an important advancement in the art if such a weight promoting pharmaceutical could be developed which had the advantages of VNO administration.
SUMMARY OF THE INVENTION
The present inventive weight promoting composition is an important advancement in the field of weight promotion. The inventors have unexpectedly discovered a VNO administered pharmaceutical composition which promotes weight gain in all ages and both genders, while avoiding problems of systemic administration.
The special qualities of VNO drug administration provide the weight promoting composition of the present invention with unique advantages over currently available pharmaceuticals and feeding regimens. In many cases the inventive composition acts synergistically with these prior art approaches. The activity of the inventive composition is not limited to one gender, or pre-menopausal women, and thus enjoys broad applicability.
It is an object of the present invention to provide a weight promoting composition which is effective when administered through the VNO in a broad range of individuals.
It is a further object of the present invention to provide a weight promoting composition which is effective in promoting weight in clinical conditions such as, for example, anorexia nervosa, anosmia, wasting in elderly, AIDS, cancer, morning sickness, osteoporosis, and childhood eating disorders.
It is yet a further object of the present invention to provide for increase muscle and general body mass in athletes, such as for wrestling, body building, football, hockey, weight lifting training and events.
It is an additional object of the present invention to provide a weight promoting effect by means of administration to the VNO, so as to avoid systemic exposure to the active compound.
DETAILED DESCRIPTION OF THE INVENTION
The present inventive composition, method, and product allow, for the first time, weight promotion without the disadvantages of systemic exposure to a drug. This special advantage is accomplished by administration of the pregnane vomeropherin of formula I, or a pharmaceutical composition containing it, to the VNO.
The present invention was made when the inventors unexpectedly discovered that these compounds, when administered to the VNO, promotes weight gain. The compounds of the present invention are effective in all ages and genders.
The vomeropherins which can be appropriately used in the present invention are pregnanes of the formula:
where:
R
1
=H, C
1-4
alkyl, C
1-4
alkanoyl, SO
3
H, or salts thereof,
R
2
=C
1-4
alkyl,
R
3
=H or methyl,
and one or two non-adjacent members of a, b, c, and d are optional double bonds.
The special qualities of VNO drug administration provide the weight promoting composition, method, and product of this invention with unique advantages over currently available pharmaceuticals and feeding regimens. Surprisingly, the activity of the inventive composition, method, and product is not limited by age or gender.
Target Conditions and Patient Groups
Diseases Associated with Weight Loss
Anorexia Nervosa. One important embodiment of the weight promoting method of the present inv
Berliner David L.
Jennings-White Clive L.
Monti Louis
Heller Ehrman White & McAuliffe LLP
Pherin Pharmaceuticals, Inc.
Webman Edward B.
LandOfFree
Weight promoting composition, method, and product does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with Weight promoting composition, method, and product, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Weight promoting composition, method, and product will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-3105956