47 results about "Dihydrolipoic acid" patented technology

A topical composition comprising a lipoic acid, a carnitine, and a carnosine in a suitable vehicle for topical application and a method for treating skin is provided. The present compositions are useful in improving the appearance of aged skin characterized by wrinkles and loss of elasticity. Preferred components include R-lipoic acid or R-dihydrolipoic acid, acetyl-1-carnitine, and 1-carnosine.

A topical composition comprising a lipoic acid, a carnitine, and a carnosine in a suitable vehicle for topical application and a method for treating skin is provided. The present compositions are useful in improving the appearance of aged skin characterized by wrinkles and loss of elasticity. Preferred components include R-lipoic acid or R-dihydrolipoic acid, acetyl-1-carnitine, and 1-carnosine.

The invention relates to an andrographolide derivative, which has the structure as shown in a general formula I: wherein, R1, R2 and R3 are the same or different hydrogen, substituted or non-substituted organic acid radical, inorganic acid radical, alkyl, aryl or heteroaryl, while at least one of R1, R2 and R3 is R-lipoic acid or S-lipoic acid or the mixture of R-lipoic acid and S-lipoic acid or the corresponding dihydrolipoic acid or acetylcysteine radical of R-lipoic acid or S-lipoic acid; the derivative has good anti-tumor effect, and the derivative can cause apoptosis of tumor cells, directly eliminate gram positive bacteria, staphylococcus aureus and sensitivities MRSA5676 and MRSA5677, inhibit the QS system of gram negative bacteria and pseudomonas aeruginosa and inhibit and damage the formation of the bio-film of pseudomonas aeruginosa; the product has prominent hypoplycemic effect and is suitable for the preparation of the medicines that can cure cancers, inflammations, diabetes mellitus and bacterial and viral infection.

The present invention relates to compounds of the Formula (I), wherein X1 and X2 independently represent O, NH or S; R1 and R2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X1 or X2 in this case being NH, and hydrogen, both radicals R1 and R2 preferably not being H; and R3 is a residue selected from group consisting of —S—R6, wherein R6 is a C1-C30 hydrocarbyl group, at least one of R1 and R2 not being H when X1 and X2 are oxygen, —S—CH2—CH(NH2)(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group; and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug, drugs containing the same and their use for the therapy of diseases such as autoimmune disease, NF-kappaB mediated diseases, psoriasis, psoriatic arthritis, neurodermitis, enteris regionalis Crohn, cardiac insufficiency, chronic obstructive pulmonary diseases and asthma and in transplantation medicine.

The present invention relates to compounds of the formula (I) wherein X1 and X2 independently represent O, NH or S, R1 and R2 are independently selected from the group consisting of a C1-C30 hydrocarbyl group, an amino acid bonded via an amide bond or a peptide bonded via an amide bond each having up to 200 amino acids, the conjugated residue X1 or X2 in this case being NH, and hydrogen, both radicals R1 and R2 preferably not being H, wherein R3 is a residue selected from group consisting of —S—R6, wherein R6 is a C1-C30 hydrocarbyl group, at least one of R1 and R2 not being H when X1 and X2 are oxygen, —S—CH2—CH(NH2)(COOH) (cysteine-S-yl), a homologue or derivative (e.g. N-acetyl cysteine-S-yl) thereof, a peptide having up to 200 amino acids which contains at least one amino acid radical with a thiol group, preferably a cysteine radical, and is bonded via the thio sulfur, preferably via the cysteine sulfur (peptide-S-yl), coenzyme A which is bonded via a thiol group or fragments thereof, acyl carrier protein bonded via a thiol group, and dihydrolipoic acid bonded via a thiol group, and pharmaceutically acceptable salts thereof. The present invention also relates to the use of these compounds for preparing a drug and drugs containing the same.

The present invention discloses a fluorescent gold nanocluster, comprising: a dihydrolipoic acid ligand (DHLA) on the surface thereof, wherein the fluorescent gold nanocluster generates fluorescence by the interaction between the dihydrolipoic acid ligand and the nanocluster and the particle diameter of the fluorescent gold nanocluster is between 0.5 nm and 3 nm, wherein the wavelength of the emission fluorescence of the fluorescent gold nanocluster is between 400 nm and 1000 nm. In addition, the fluorescent gold nanocluster is used as bioprobes and / or applied in fluorescent biological label, clinical image as contrast medium, clinical detection, clinical trace, and clinical treatment etc.

Long term storage stable pemetrexed-containing liquid pharmaceutical compositions are disclosed. The compositions can include pemetrexed or pharmaceutically acceptable salts thereof; an antioxidant selected from lipoic acid, dihydrolipoic acid, methionine and mixtures thereof; a chelating agent selected from lactobionic acid, sodium citrate, tribasic and mixtures thereof; and a pharmaceutically acceptable fluid. The pH of the compositions is in a range of about 8 to about 9.5. The pemetrexed-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 227 nm, after at least about 18 months of storage at a temperature of from about 5° C. to about 25° C. Methods of preparing the formulation as well as methods of treatment of pemetrexed-susceptible diseases using the same are also disclosed.

Long term storage stable pemetrexed-containing liquid pharmaceutical compositions are disclosed. The compositions can include pemetrexed or pharmaceutically acceptable salts thereof; an antioxidant selected from lipoic acid, dihydrolipoic acid, methionine and mixtures thereof; a chelating agent selected from lactobionic acid, sodium citrate, tribasic and mixtures thereof; and a pharmaceutically acceptable fluid. The pH of the compositions is in a range of about 8 to about 9.5. The pemetrexed-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 227 nm, after at least about 18 months of storage at a temperature of from about 5° C. to about 25° C. Methods of preparing the formulation as well as methods of treatment of pemetrexed-susceptible diseases using the same are also disclosed.

Long term storage stable fulvestrant-containing compositions are disclosed. The compositions can include fulvestrant; a solvent selected from dimethyl sulfoxide (DMSO), glycofurol, N-methyl pyrrolidone, and mixtures thereof; an oil mixture selected from a mixture of caprylic and capric triglycerides, a mixture of caprylic, capric and linoleic triglycerides, a mixture of caprylic, capric and succinic triglycerides, and a mixture of propylene glycol dicaprylate and propylene glycol dicaprate; and a sustained release member selected from benzyl benzoate, dihydrolipoic acid, benzyl alcohol and lipoic acid. The fulvestrant-containing compositions have less than about 5% total impurities, on a normalized peak area response (“PAR”) basis as determined by high performance liquid chromatography (“HPLC”) at a wavelength of 223 nm, after at least about 24 months of storage at a temperature of from about 5° C. to about 25° C.

A stabilized dihydrolipoic acid (DHLA) compound is provided. The stabilized DHLA is derived from a microbiological culture media including at least one live probiotic organism, R-lipoic acid and at least one nutritive agent. The stabilized DHLA may be prepared by dispersing the microbiological media in distilled water to form a broth, incubating the broth at a predetermined temperature for a select period of time to induce probiotic activity, adding organic ethanol to the broth to halt the probiotic activity, and separating the derived stabilized DHLA from the broth.

The present invention discloses a fluorescent gold nanocluster, comprising: a dihydrolipoic acid ligand (DHLA) on the surface thereof, wherein the fluorescent gold nanocluster generates fluorescence by the interaction between the dihydrolipoic acid ligand and the nanocluster and the particle diameter of the fluorescent gold nanocluster is between 0.5 nm and 3 nm, wherein the wavelength of the emission fluorescence of the fluorescent gold nanocluster is between 400 nm and 1000 nm. In addition, the fluorescent gold nanocluster is used as bioprobes and / or applied in fluorescent biological label, clinical image as contrast medium, clinical detection, clinical trace, and clinical treatment etc.

The subject invention pertains to materials and methods for the prevention and treatment of disease conditions associated with oxidative stress or a compromised reducing environment, including inflammatory bowel diseases such as Crohn's disease and ulcerative colitis. Therapeutic compositions of the invention include compositions that can neutralize hydrogen peroxide, such as reducing agents and oxidizing agents. In one embodiment, a composition includes dihydrolipoic acid as a first reducing agent, an aminosalicylic acid, and a mast cell stabilizer. In another embodiment, the composition further includes a second reducing agent. Methods of the invention include administration of compounds or compositions of the invention. In one embodiment, compounds or compositions of the invention are rectally instilled in a patient.

The invention provides a cosmetic additive prepared from selenium carrageenan, dihydrolipoic acid acid and L-methionine. The selenium carrageenan and the dihydrolipoic acid in a prescription are food additives, and the L-methionine is an amino acid necessary for human beings so that the cosmetic additive does not cause allergic reactions in human bodies and has strong repairing effect on human body cells. In addition, the prescription is used for not only effectively clearing oxygen free radicals, recovering the activities of tyrosinases and preventing the poliosis, but also reconstructing the functions of the protein and recovering the skin elasticity so that the cosmetic additive has optimal effects of preventing poliosis and skin aging.

The invention discloses an andrographolidume composition and application thereof. The composition consists of a component I and a component II according to a molar ratio of between 1:10 and 10:1, wherein the component I is at least one of andrographolidume, andrographolidume derivatives and pharmaceutically acceptable salts of the andrographolidume derivatives, and the component II is at least one of lipoic acid and dihydrolipoic acid. The composition can be prepared into anticancer, anti-inflammatory, antibacterial, antivirus or hypoglycemic medicaments.

The invention relates to a pharmaceutical compound for antioxidant protection of cells, tissues and entire organism against hyperproduction of fee radicals. The inventive compound comprises an effective quantity of at least one antioxidant in the form of a main acting component. Said antioxidant is selected from a group consisting peroxiredoxine, a fragment thereof, dihydrolipoic acid and the combinations thereof with acceptable pharmaceutical additives. The inventive method for preventing and curing mammals consists in contacting the effective quantity of the compound with intercellular space of tissue, organ and entire mammal organism. Low toxicity of the compound makes it possible to increase the efficiency of treatment of multifactor actions on an organism, for example radiation, thermal, chemical burn, wounds and hurts as a result of disasters and fires.

The invention describes compositions, including soft gelatin capsules, that include dihydrolipoic acid and the reduced form of coenzyme Qn wherein the dihydrolipoic acid acts as a reducing agent for the coenzyme Qn and also, optionally, as a solvent.

Formulations comprising docetaxel or a salt thereof in combination with α-lipoic acid and / or dihydrolipoic acid and / or salts thereof in narrow concentration ranges have improved stability as concentrate liquid formulations and permit longer times between dilution from higher concentrations through completion of infusions prepared therefrom allowing for lesser waste and more efficient use of personnel in infusion preparation.

The invention relates to design and construction of a novel gold nanoparticle-anthracene ring pharmaceutical composition. The gold nanoparticle-anthracene ring pharmaceutical composition consists of gold nanoparticles serving as the core, dihydrolipoic acid serving as a connecting arm, an anthracene ring drug serving as a carried medicine and a hydrophilic polymer serving as a biocompatible molecule. The half-life period of the anthracene ring drug can be prolonged, the concentration of the drug in unit volume is increased, the drug is sensitive to acidic pH value, and the bioavailability and the drug metabolism kinetic properties of the drug are improved. The invention also discloses a method for preparing each component of the gold nanoparticle-anthracene ring pharmaceutical composition, a method for preparing the composition, in-vitro release characteristics of the drug and a drug delivery application.

The present invention related to a compound for use in prevention or treatment of a neurodegenerative disease associated with the formation of stress granules. The compound is selected from lipoic acid, lipoamide, dihydrolipoic acid, and dihydrolipoamide. The invention further relates to a method of identifying a compound that modulates a characteristic associated with one or more condensates comprising a condensate-associated molecule, comprising: (a) contacting the compound with a cellular composition comprising one or more condensates or a cellular composition capable of forming one or more condensates, and (b) determining the characteristic associated with the one or more condensates. A modulation in the characteristic, as compared to a reference, indicates that the compound modulates the characteristic associated with the one or more condensates.

The invention relates to a pharmaceutical compound for antioxidant protection of cells, tissues and entire organism against hyperproduction of fee radicals. The inventive compound comprises an effective quantity of at least one antioxidant in the form of a main acting component. Said antioxidant is selected from a group consisting peroxiredoxine, a fragment thereof, dihydrolipoic acid and the combinations thereof with acceptable pharmaceutical additives. The inventive method for preventing and curing mammals consists in contacting the effective quantity of the compound with intercellular space of tissue, organ and entire mammal organism. Low toxicity of the compound makes it possible to increase the efficiency of treatment of multifactor actions on an organism, for example radiation, thermal, chemical burn, wounds and hurts as a result of disasters and fires.

Formulations comprising docetaxel or a salt thereof in combination with α-lipoic acid and / or dihydrolipoic acid and / or salts thereof in narrow concentration ranges have improved stability as concentrate liquid formulations and permit longer times between dilution from higher concentrations through completion of infusions prepared therefrom allowing for lesser waste and more efficient use of personnel in infusion preparation.

A process for production and extraction of dihydrolipoic acid (DHLA) relates to the biotransformation of R-lipoic acid to dihydrolipoic acid. The process ferments the lipoic acid with bacteria selected from the genus of any of the following bacteria: Lactobacillus, Enterococcus, Pediococcus, or Bacillus. More particularly the present invention relates to a method for the extraction of DHLA utilizing a non-traditional solvent system, namely a food oil. Generally the DHLA that is produced in the present method is isolated from cells which have been inactivated or killed.

The invention includes novel compounds, including but not limited to formula A and formula B, and an improved delivery method. These compounds and methods are useful in preventing or treating diseases or conditions associated with or caused by the presence of free radicals, and are useful for increasing cellular metabolism while simultaneously alleviating the resultant increase in oxidative stress. Specifically, a carnitine is bound to a lipoic acid derivative or to dihydrolipoic acid or its derivatives using a hydrolysable linker to form a single compound.

The invention relates to a preparation method of R-(+)-dihydrolipoic acid, which comprises the following steps: by using R-lipoic acid as a starting raw material, carrying out Pd / H2 reduction and concentration to obtain a crude product, and finally refining the crude product to obtain the target product. The preparation method of the R-(+)-dihydrolipoic acid is simple and convenient in process, high in selectivity, single in product, short in period, low in production cost and easy to realize industrial production.

The invention relates to the technical field of in-vitro diagnosis, in particular to a sample diluent, a preparation method thereof and an immunoassay method for eliminating abnormal detection of a fresh sample. The sample diluent comprises a component A, a component B and a biological buffer solution; the component A is lipoic acid or dihydrolipoic acid; and the component B is dextran sulfate or a salt thereof. According to the invention, the lipoic acid and the dextran sulfate are combined and applied to immune clinical detection, so that the abnormality of detection results caused by different freshness degrees of samples is avoided. The diluent can effectively prevent interference in a fresh sample, and can eliminate complement, fibrin and other main interfering substances contained in the sample. The diluent can reduce non-specific reaction in immunoassay, so that the accuracy and precision of a reagent are improved. The diluent is simple in preparation method, and has safety and environmental friendliness.

A stabilized dihydrolipoic acid (DHLA) compound is provided. The stabilized DHLA is derived from a microbiological culture media including at least one live probiotic organism, R-lipoic acid and at least one nutritive agent. The stabilized DHLA may be prepared by dispersing the microbiological media in distilled water to form a broth, incubating the broth at a predetermined temperature for a select period of time to induce probiotic activity, adding organic ethanol to the broth to halt the probiotic activity, and separating the derived stabilized DHLA from the broth.

The present invention relates to a multi-step process for the production of dihydrolipoic acid, which can particularly be carried out as a one-pot reaction and without isolation of intermediates.