Nicotinic acid riboside or nicotinamide riboside compositions, reduced derivatives thereof, and the use thereof

A kind of technology of compound and solvate, applied in nicotinic acid riboside or nicotinamide riboside composition, its reduced derivative and use field thereof

Active Publication Date: 2018-01-02
CHROMADEX +1
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  • Summary
  • Abstract
  • Description
  • Claims
  • Application Information

AI Technical Summary

Problems solved by technology

These protective effects may be attributed to upregulated NAD+ biosynthesis, which increases the available NAD+ pool subjected to depletion during genotoxic stress

Method used

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  • Nicotinic acid riboside or nicotinamide riboside compositions, reduced derivatives thereof, and the use thereof
  • Nicotinic acid riboside or nicotinamide riboside compositions, reduced derivatives thereof, and the use thereof
  • Nicotinic acid riboside or nicotinamide riboside compositions, reduced derivatives thereof, and the use thereof

Examples

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preparation example Construction

[0122]Those skilled in the art will appreciate that the methods described are not the only means by which the compounds of the invention may be synthesized, and that a very wide range of synthetic organic reactions can potentially be used to synthesize the compounds of the invention. Those skilled in the art know how to choose and implement appropriate synthetic routes. Suitable synthetic methods can be identified by reference, including the following referenced sources such as: COMPREHENSIVE ORGANIC SYNTHESIS [Comprehensive Organic Synthesis] (eds. B.M. Trost & I. Fleming, Pergamon Press [Pergamon Press] 1991); COMPREHENSIVE ORGANIC FUNCTIONAL GROUPTRANSFORMATIONS [ COMPREHENSIVE ORGANIC FUNCTIONAL GROUP TRANSFORMATIONS II] (Editors A.R.Katritzky & R.J.K.Taylor, 2nd Edition, Elsevier [Elsevier] 2004); COMPREHENSIVE HETEROCYCLIC CHEMISTRY [Comprehensive Heterocyclic Chemistry] (edited by A.R. Katritzky & C.W. Rees, Pergamon Press [Pergamon Press] 1984); COMPREHENSIVE HETEROCYC...

example 1

[0132] In one embodiment, one or more NR, NAR, NRH or NARH derivatives (including prodrugs or salts thereof) may be used as a vehicle for transdermal delivery of compounds and / or drug products. In a preferred embodiment, the derivative is selected from NRH triacetate (2) and NARH triacetate (4a).

[0133] In another embodiment, one or more NR, NAR, NRH or NARH derivatives (including prodrugs or salts thereof) may be used to: improve signs of aging, including superficial wrinkles, coarse deep wrinkles, enlarged pores , age spots, photodamage, scaling, flaking, dryness, sagging skin, puffy skin around the eyes, puffy skin around the lower cheeks, loss of elasticity of the skin, loss of firmness of the skin, loss of firmness of the skin, loss of barrier function, deformation of the skin from loss of resiliency, depigmentation, blotchiness, sallowness, hyperpigmentation, keratosis, hyperkeratosis, elastosis or collagen breakdown, and cellulite or combinations thereof. In a prefer...

example 2

[0137] In one embodiment, one or more NR, NAR, NRH or NARH derivatives (including prodrugs, solvates or salts thereof) may optionally be used in combination with pterostilbene. A useful dosage range for topical pterostilbene is from about 0.1% by weight to about 10% by weight, based on the total weight of the composition. Another suitable dosage range for topical pterostilbene is from about 1% to 2% by weight, based on the total weight of the composition. In a preferred embodiment, the derivative is selected from NRH triacetate (2) and NARH triacetate (4a). A useful dosage range for NRH triacetate (2) and NARH triacetate (4a) is about 0.1% to about 10% by weight, based on the total weight of the composition.

[0138] In this example, combinations containing NR, NAR, NRH or NARH act as UV-induced inflammatory modulators, affecting signs of aging and damage caused by, for example, UV / radiation including skin lightening, inflammation and sunburn redness.

[0139] Furthermore, ...

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Abstract

Derivatives of nicotinic acid riboside (NAR), nicotinamide riboside (NR), and reduced NAR and NR, including 1-(2', 3', 5'-triacetyl-beta-D-ribofuranosyl)-1,4-dihydronicotinic acid (4a), and compositions containing the same and / or reduced derivative forms of nicotinamide riboside including 1-(2',3',5'-triacetyl-beta-D-ribofuranosyl)-1,4-nicotinamide (2), are provided for use in the care of treatment of skin and skin conditions. In some embodiments, the invention relates to pharmaceutical compositions and cosmetic compositions containing one or more NR, NAR, NRH, or NARH derivatives, or prodrugsor salts thereof. In further embodiments, the invention relates to methods of using one or more NR, NAR, NRH, or NARH derivatives, or prodrugs, solvates, or salts thereof, to promote the increase ofintracellular levels of nicotinamide adenine dinucleotide (NAD+) in cells and tissues for improving cell and tissue survival and overall cell and tissue health.

Description

technical field [0001] In certain embodiments, the present invention relates to pharmaceutical and cosmetic compositions comprising: derivatives of nicotinamide riboside ("NR"), including 1-(2',3',5'-triacetyl β-D-ribofuranosyl)-nicotinamide ("NR triacetate" or "NRTA"); derivatives of the reduced form of nicotinamide riboside ("NRH"), including 1-(2',3 ',5'-triacetyl-β-D-ribofuranosyl)-1,4-dihydronicotinamide ("NRH triacetate" or "NRH-TA"); nicotinic acid riboside ("NAR" ), including 1-(2',3',5'-triacetyl-β-D-ribofuranosyl)-nicotinic acid ("NAR triacetate" or "NARTA"); or nicotinic acid Derivatives of nucleoside reduced forms ("NARH"), including 1-(2',3',5'-triacetyl-β-D-ribofuranosyl)-1,4-dihydronicotinic acid ("NARH triacetate" or "NARH-TA"). In other embodiments, the present invention relates to methods of using the above compounds to promote increased intracellular levels of nicotinamide adenine dinucleotide ("NAD+") in cells and tissues to improve cell and tissue survi...

Claims

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Application Information

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Patent Type & Authority Applications(China)
IPC IPC(8): C07H19/048A61K31/706
CPCA61K31/706C07H19/048A61P17/16A61K8/675A61Q19/08A61Q19/004A61Q19/007A61Q19/00A61P17/00A61P17/18A61K2300/00A61P17/02A61P43/00
Inventor 瑞安·德林杰M·尤金妮娅·米高德P·瑞德帕斯特洛伊·鲁尼穆斯理查德·坎宁安
Owner CHROMADEX
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