Palatable arginine compounds and uses thereof for...

Details Palatable arginine compounds and uses thereof for... Palatable arginine compounds and uses thereof for...

2002-07-19

2004-09-21

Badio, Barbara P. (Department: 1616)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Cyclopentanohydrophenanthrene ring system doai

C426S072000, C426S073000

Reexamination Certificate

active

06794375

ABSTRACT:

FIELD OF THE INVENTION
The present invention relates to compounds, compositions, kits, and methods which are useful for providing various general health benefits including, but not limited to cardiac benefits, including lowering cholesterol in the consumer, treating, preventing, and/or inhibiting heart disease (e.g., atherosclerosis, restenosis, thrombosis) and, treating conditions such as hypercholesterolemia, hypertension, poor circulation, and complications associated with diabetes.
BACKGROUND OF THE INVENTION
Cardiovascular conditions, including heart disease, hypercholesterolemia, hypertension, poor circulation, and complications associated with diabetes, are serious medical conditions which are leading causes of mortality in humans. Various regimens have been suggested for prevention and treatment of these conditions, including pharmaceutical, dietary, and exercise regimens. Notwithstanding, they remain among the most prevalent and serious of all medical conditions.
L-arginine is a natural amino acid which has been identified to provide certain general health benefits including, for example, cardiovascular benefits, such as lowering cholesterol in the consumer, and treating, preventing, and/or inhibiting heart disease and poor circulation. See e.g., Moskowitz, U.S. Pat. No. 5,385,940, assigned to The General Hospital Corp., issued Jan. 31, 1995; Sonaka et al., EP 0,546,796, assigned to Ajinomoto Co., published Jun. 16, 1993; Cotter et al., U.S. Pat. No. 4,920,098, assigned to Baxter International Inc., issued Apr. 24, 1990; Dudrick, U.S. Pat. No. 5,032,608, issued Jul. 16, 1991; Levere et al., U.S. Pat. No. 5,217,997, issued Jun. 8, 1993; Cooke et al., U.S. Pat. No. 5,428,070, assigned to Stanford University, issued Jun. 27,1995; Chibata et al., U.S. Pat. No. 4,420,432, assigned to Tanabe Seiyaky Co., issued Dec. 13, 1983; Varma et al., U.S. Pat. No. 5,364,884, assigned to Baylor College of Medicine, issued Nov. 15, 1994; and Barbul, U.S. Pat. No. 5,157,022, issued Oct. 20, 1992.
The utility of L-arginine, particularly to advance cardiovascular health, is therefore well known in the art. However, as for any beneficial regimen, compliance must be assured in order to realize the various benefits thereof. Unfortunately, L-arginine and its close derivatives (including salts, polypeptides, and pro-forms) have a strong, bitter, and fishy flavor, making L-arginine generally unacceptable for use. This results in decreased compliance of a regimen involving L-arginine, and the requisite cardiovascular benefits are therefore not realized. Accordingly, to enhance compliance, it would be desirable to provide L-arginine in a form which diminishes and/or removes the unacceptable flavor associated with L-arginine.
Unfortunately, flavor improvement is typically associated with a decrease in the general health benefits of the component which is desired to be delivered. Additionally, because delivery of relatively large amounts of L-arginine is desirable (erg., about 3 grams to about 10 grams of L-arginine per dose), it becomes increasingly more difficult to mask the strong, bitter, and fishy flavor. Such difficulties manifest themselves in the marketplace, where it is understood that current products containing L-arginine are not acceptable to the consumer due to unacceptable flavor.
The present inventors have surprisingly discovered that the unacceptable flavor of L-arginine is significantly improved through esterification of the L-arginine with any of various components, which will be defined herein. Interestingly, and quite unexpectedly, the esterified L-arginine exhibits significantly improved flavor relative to L-arginine itself. The improvement has been found particularly significant, wherein the component is lipophilic in nature. Accordingly, such combination is acceptable to consumers which, more importantly, translates into improved regimen compliance and enhanced cardiovascular, and other health, benefits. Additionally, the in vivo hydrolysis products of the ester are biologically acceptable and, in many cases, provide unique health benefits which supplement those of L-arginine.
The foregoing findings are unexpected relative to the known literature. Accordingly, the present inventors have discovered compounds, compositions, and kits which provide general health benefits, including cardiovascular benefits. Relative to known products, compliance is improved and/or ensured through use of such compositions because the flavor is acceptable to the consumer. The compositions are easily provided as a pharmaceutical, food, or beverage product (preferably, a food or beverage product) and may be delivered in kit form, wherein the kit has the further advantage of disseminating information to the consumer regarding various health benefits and dose regimens of the compounds and compositions.
SUMMARY OF THE INVENTION
The present invention is directed to a compound having the structure:
and acceptable salts, polypeptides, and pro-forms thereof, wherein R is selected from the group consisting of:
(a) substituted glycerols; wherein n is an integer from 1 to 2;
(b) vitamins; wherein n is 1;
(c) sterols; wherein n is 1;
(d) stanols; wherein n is 1;
(e) C
6
-C
32
alkyl; wherein n is 1; and
(f) C
6
-C
32
alkenyl; wherein n is 1.
The present invention is further directed to compositions and kits comprising these compounds as well as methods of using the compounds. The compounds, compositions, kits, and methods herein are useful for providing general health benefits to the consumer, particularly cardiovascular benefits, anti-menopausal benefits and/or treating sexual dysfunction (particularly, erectile dysfunction). Most particularly, the compounds, compositions, kits, and methods herein are useful for providing cardiovascular benefits, including lowering cholesterol in the consumer, treating, preventing, and/or inhibiting heart disease (e.g., atherosclerosis, restenosis, thrombosis) and, for example, treating other conditions such as hypercholesterolemia, hypertension, poor circulation, and complications associated with diabetes.
DETAILED DESCRIPTION OF THE INVENTION
The present invention is directed to compounds, and compositions comprising such compounds, which are useful for providing general health benefits to the consumer, particularly cardiovascular benefits, anti-menopausal benefits and/or treating sexual dysfunction (particularly, erectile dysfunction). The invention herein is further directed to kits comprising the compounds and compositions and methods of their use to provide the foregoing general health benefits.
Publications, patents, and patent applications are referred to throughout this disclosure. All references cited herein are hereby incorporated by reference.
All percentages and ratios are calculated by weight unless otherwise indicated. All percentages and ratios are calculated based on the total composition unless otherwise indicated.
All component or composition levels are in reference to the active level of that component or composition, and are exclusive of impurities, for example, residual solvents or by-products, which may be present in commercially available sources.
Referred to herein are trade names for components including, but not limited to, certain fats, flavors, and other components. The inventors herein do not intend to be limited by materials under a certain trade name. Equivalent materials (e.g., those obtained from a different source under a different name or catalog (reference) number) to those referenced by trade name may be substituted and utilized in the compositions, kits, and methods herein.
In the description of the invention various embodiments and/or individual features are disclosed. As will be apparent to the ordinarily skilled practitioner, all combinations of such embodiments and features are possible and can result in preferred executions of the present invention.
The compositions, methods, and kits herein may comprise, consist essentially of, or consist of any of the elements as described herein.
Definitions
As used herein, “alkyl” is an unsubst

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