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Novel compounds for use in weight loss and appetite suppression in humans

a technology of appetite suppression and compounds, applied in the field of new compounds for use in weight loss and appetite suppression in humans, can solve the problems of clinical depression, loss of productivity and relationship problems, and debilitating physical and mental health, and achieve the effects of suppressing appetite, improving mood, and improving sexual desire and performan

Inactive Publication Date: 2004-09-30
SEROCTIN RES & TECH
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Benefits of technology

[0025] A primary object of the present invention is to provide novel chemical compositions derived, isolated, and / or extracted from monocotyledonous plants or by chemical synthesis, and methods of use to achieve weight loss in mammals.
[0027] It is also an object of the present invention to provide novel chemical compositions derived, isolated, and / or extracted from monocotyledonous plants or by chemical synthesis, and methods of use to elevate mood in mammals.
[0029] In addition, it is an object of the invention to provide novel methods for growing monocotyledonous plants which results in an increased yield of 6-MBOA and other phenolic and indole-amine compounds.
[0041] Consistent with the foregoing objects, and in accordance with the invention as embodied and broadly described herein, it has been found that certain phenolic compounds and precursors of phenolic compounds, related to each other by shared structural similarities and having structural similarities with melatonin, are effective in bettering mood, improving sexual desire and performance, and as an adjunctive therapy for weight loss and substance abuse and addiction. The novel compounds of the present invention naturally exist as plant secondary metabolites in the early growth of monocotyledonous plants, become concentrated from their ingestion within certain animal parts, or can be synthesized by chemical means. The invention includes therapies using the novel compounds of the present invention for treating depression and sexual dysfunction, as well as adjunctive therapies for achieving weight loss and problems of substance abuse and addiction. The therapeutic method comprises the ingestion of the novel compounds of the present invention over a certain period of time, or other means for getting the compounds of the invention into the body. Both males and females benefit from ingesting the compounds of the invention, while still contained in dried leaves from monocotyledonous plants with such compounds or taken as purified and / or synthesized preparations. It appears that the compounds of the invention act as antidepressants without the undesirable side effects of currently used antidepressants.

Problems solved by technology

It is a serious problem that is usually or initially caused by outside stressors.
As stresses escalate or persist, a chemical imbalance can result.
Clinical depression can be very debilitating both physically and mentally and even lead to death by means of suicide.
However, lost productivity and relationship problems are also consequences of lesser depressions.
Although depressed people tend to improve when treated with antidepressants, many do not respond to the first one.
Sexual dysfunction includes lacking interest in sex, problems with arousal, not enjoying sex, and anxiety about sexual performance.
Indeed, feeling good in general has significant impact on sexual function, with those people unhappy or depressed more likely to experience difficulties.
Arousal problems affect over 20 million American males, about two in 10 adult men, with such difficulties often associated with or accompanied by some sort of depression.
Meanwhile, prescription antidepressants actually exacerbate the situation, since a frequent side effect of their use is sexual dysfunction.
These conditions may be causes of increased morbidity in overweight and obese individuals.
Being overweight is known to increase the risk of dying from many conditions, including 4 of the 10 leading causes of death: coronary heart disease, cancer, stroke and type 2 diabetes.
Poor eating habits may include excessive intake as well as poor selection of foods with nutritional value.
There are a broad range of opinions as to how successful these therapeutic approaches have been either individually or collectively, but nevertheless, incidence and prevalence of overweight and obesity continue to increase.
This compound stimulates rather than inhibits melatonin biosynthesis and does not prevent stimulation of melatonin synthesis by norepinephrine (Yuwiler et al., "Effects of 6-methoxy-2-benzoxazolinone on the pineal melatonin generating system.
However, melatonin exacerbates symptoms of dysphoria in depressed people.
Yet, the inventors are not aware of any prior art that has explored or suggested the use of 6-MBOA and related compounds as having psychotropic effects in humans, particularly with respect to depression or mood.

Method used

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  • Novel compounds for use in weight loss and appetite suppression in humans
  • Novel compounds for use in weight loss and appetite suppression in humans
  • Novel compounds for use in weight loss and appetite suppression in humans

Examples

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example 1

The Similar Physiological Effects of the Compounds of the Invention

[0068] Representative compounds of Formulas I, II, and III are shown below as compounds 1-7. The compounds of Formulas I, II and III have like physiological properties, and as such may be considered as similar or equivalent for therapeutic purposes, and were tested via a rodent model.

[0069] 1. 2-amino-5-methoxyphenol [Member of Formula I] 6

[0070] 2. 6-methoxy-2-benzoxazolinone [Member of Formula II] 7

[0071] 3. 2,4-dihydroxy-7-methoxy-1,4-(2H)-benzoxazin-3-one [Member of Formula III] 8

[0072] 4. 2-hydroxy-4-methoxyacetanilide [Member of Formula I] 9

[0073] 5. 2-hydroxy-4-ethoxyacetanilide [Member of Formula I] 10

[0074] 6. 5-methoxy-2-benzoxazolinone [Member of Formula III] 11

[0075] 7. 2-hydroxy-5-methoxyacetanilide [Member of Formula I] 12

[0076] Female montane voles, Microtis montanus, received intra peritoneal injections of representative compounds belonging to Formulas I, II and III for three consecutive days and sacr...

example 2

Compounds of the Invention as an Antidepressant and Aphrodisiac in Human Males

[0079] This component of the invention relates to a method for lessening depression and otherwise bettering mood or feelings of well-being, said method comprising the administration to human males of an effective amount of one or more of the compounds of the invention defined herein. This component of the invention also relates to a method for treating sexual dysfunction or otherwise increasing sexual desire and performance, including but not necessarily limited to lacking interest in sex, problems with arousal, not enjoying sex, and anxiety about sexual performance, said method comprising the administration of an effective amount of one or more of the active compounds of the invention.

[0080] A double-blind crossover study was done on human males to test compounds of the invention as a therapeutic agent for treating depression or otherwise elevating mood as well as bettering sexual function. The trial had ...

example 3

Compounds of the Invention as an Antidepressant in Human Females

[0087] This example further relates to a method for lessening depression and otherwise bettering mood or feelings of well-being, said method comprising the administration to human females of an effective amount of the compounds of the invention, defined above and in FIG. 1. Compounds of the invention were used to treat eight females with clinical depression, which for three females had been ongoing for at least one year. Participants took the same dose of compounds of the invention as in Example 2, 15-mg each day. A HAD was administered to participants prior to beginning daily doses. Each participant was interviewed every two weeks to check for adverse side effects and for comments on use of the compounds of the invention. A HAD Index was again administered upon completion of the six-week trial.

[0088] Referring to Table 3, the results of the study are tabulated.

3TABLE 3 HAD summary for clinically-depressed females takin...

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Abstract

Phenolic compounds with a phenolic molecule to which are covalently linked an oxygen-containing group, a nitrogen or another oxygen containing group, and a C1-C4 alkoxy group, obtainable from monocotyledonous plants, or by chemical synthesis, have been found to act as weight loss agents, appetite suppressants, mood enhancers and adjunctive therapy for arthritis, sleep apnea, fibromyalgia, diabetes and hyperglycemia. Additional chemical compounds of the present invention may include benzoxazinoids-cyclic hydroxyamic acids, lactams, and corresponding glucosides, which may serve as precursors to phenolic compounds. The phenolic compounds and precursors of phenolic compounds of the present invention, at concentrations suitable for human therapeutic use, may be obtained from monocotyledonous plants such as corn in their early growth states which are timely harvested for optimum yield.

Description

[0001] This application claims the benefit of U.S. patent application Ser. No. 09 / 834,592, filed Apr. 13, 2001, and entitled "NOVEL COMPOUNDS FOR USE AS ANTIDEPRESSANTS, APHRODISIACS AND ADJUNCTIVE THERAPIES IN HUMANS", which claims the benefit of U.S. provisional patent application Serial No. 60 / 196,829, filed Apr. 13, 2000, and entitled "ANTIDEPRESSANT, APHRODISIAC, WEIGHT-LOSS AIDE, THERAPY FOR QUITTING NICOTINE OR ADDICTIVE DRUGS AND TREATMENT OF BETTERING REPRODUCTION IN HUMANS", which are both incorporated herein by reference.[0002] 1. Field of the Invention[0003] This invention relates to compositions and methods to induce weight loss, appetite suppression and as adjunctive therapies for fibromyalgia, sleep apnea, diabetes, hyperglycemia and arthritis and more particularly, to novel compositions of phenolic and indoleamine-like compounds which are obtainable in concentrations and amounts suitable for human use from certain botanicals or from chemical synthesis, together with ...

Claims

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Application Information

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IPC IPC(8): C07D263/58C07D265/36
CPCC07D265/36C07D263/58
Inventor ROSENFELD, MARK J.FORSBERG, SCOTT R.
Owner SEROCTIN RES & TECH
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