CHEMICAL DERIVATIVES AND METHODS FOR SYNTHESIZING AND COMPOUNDING CHEMICAL DERIVATIVES RELATED TO CAPSAICIN PALMITATE AND CAPSAICIN PRODRUGS

Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a...

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Hauptverfasser: CARLISS, Richard Daniel, HUANG, Jianxing William
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description Capsaicin compositions and methods for enhancing hydrophobicity of a molecule useful for pharmaceutical applications, including: (1) a prodrug using a linker such as a carbamate between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (2) a prodrug using a linker such as an unsaturated carboxylic ester between capsaicin with other structures in order to optimize kinetic control of capsaicin cleavage; (3) esters of long-chain fatty acids and capsaicin where hydroxyl groups provide handles for attachment of additional capsaicin molecules; and (4) the use of carboxylic acid diesters to increase overall hydrophobicity of two or more covalently-linked capsaicin molecules. Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy. L'invention concerne des compositions à base de capsaïcine et des procédés pour améliorer l'hydrophobicité d'une molécule utile pour des applications pharmaceutiques, comprenant : (1) un promédicament utilisant un lieur tel qu'un carbamate entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (2) un promédicament utilisant un lieur tel qu'un ester carboxylique insaturé entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (3) des esters d'acides gras à longue chaîne et de la capsaïcine, des groupes hydroxyle fournissant des poignées pour la fixation de molécules de capsaïcine supplémentaires ; et (4) l'utilisation de diesters d'acide carboxylique pour augmenter l'hydrophobicité globale d'au moins deux molécules de capsaïcine liées de manière covalente. L'invention concerne également des formulations d'esters palmitates de capsaïcine, qui sont conçues pour améliorer l'hydrophobicité d'une molécule utile pour des applications pharmaceutiques, par exemple, pour fournir des mélanges composés conçus en vue d'optimiser l'efficacité analgésique.
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Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy. L'invention concerne des compositions à base de capsaïcine et des procédés pour améliorer l'hydrophobicité d'une molécule utile pour des applications pharmaceutiques, comprenant : (1) un promédicament utilisant un lieur tel qu'un carbamate entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (2) un promédicament utilisant un lieur tel qu'un ester carboxylique insaturé entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (3) des esters d'acides gras à longue chaîne et de la capsaïcine, des groupes hydroxyle fournissant des poignées pour la fixation de molécules de capsaïcine supplémentaires ; et (4) l'utilisation de diesters d'acide carboxylique pour augmenter l'hydrophobicité globale d'au moins deux molécules de capsaïcine liées de manière covalente. 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Formulations of palmitated esters of capsaicin are also described, which are designed to enhance hydrophobicity of a molecule useful for pharmaceutical applications, for example to provide compounded mixtures designed to optimize analgesic efficacy. L'invention concerne des compositions à base de capsaïcine et des procédés pour améliorer l'hydrophobicité d'une molécule utile pour des applications pharmaceutiques, comprenant : (1) un promédicament utilisant un lieur tel qu'un carbamate entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (2) un promédicament utilisant un lieur tel qu'un ester carboxylique insaturé entre la capsaïcine et d'autres structures afin d'optimiser la régulation cinétique du clivage de la capsaïcine ; (3) des esters d'acides gras à longue chaîne et de la capsaïcine, des groupes hydroxyle fournissant des poignées pour la fixation de molécules de capsaïcine supplémentaires ; et (4) l'utilisation de diesters d'acide carboxylique pour augmenter l'hydrophobicité globale d'au moins deux molécules de capsaïcine liées de manière covalente. L'invention concerne également des formulations d'esters palmitates de capsaïcine, qui sont conçues pour améliorer l'hydrophobicité d'une molécule utile pour des applications pharmaceutiques, par exemple, pour fournir des mélanges composés conçus en vue d'optimiser l'efficacité analgésique.</abstract><oa>free_for_read</oa></addata></record>
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subjects ACYCLIC OR CARBOCYCLIC COMPOUNDS
CHEMISTRY
HUMAN NECESSITIES
HYGIENE
MEDICAL OR VETERINARY SCIENCE
METALLURGY
ORGANIC CHEMISTRY
PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
title CHEMICAL DERIVATIVES AND METHODS FOR SYNTHESIZING AND COMPOUNDING CHEMICAL DERIVATIVES RELATED TO CAPSAICIN PALMITATE AND CAPSAICIN PRODRUGS
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