摘要:
The invention relates to a method for producing R- and S-lipoic acid and R-dihydrolipoic acid comprising the following steps: (a) reaction of the compound of formula (2) with sodium sulphide and sulphur in methanol, whereby Ms represents SO2R`, and R and R` independently of one another represent C¿1?-C6 alkyl, C3-C8-cycloalkyl, C3-C8-cycloalkylalkyl, aryl or aralkyl. The invention relates in particular to methods for producing pure R- or S-dihydrolipoic acid, which is either used directly or processed further to obtain R- and S-lipoic acid. The method is also used to produce medicaments. The invention also relates to a solution of sodium sulphide-trihydrate and sulphur in methanol, whereby the sulphur is present as a molar surplus in relation to the sodium sulphide-trihydrate, and to a kit that comprises the inventive solution.
摘要:
Process for the synthesis of R(+)α-lipoic acid comprising the following stages: a) Salifying of racemic 6,8-halo-octanoic acid with S(-)α-methylbenzylamine; b) separation by filtration of the crystallized diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; c) purification by re-crystallization of the diastereoisomeric salt of R(+)6,8-di-halo-octanoic acid-S(-)α-methylbenzylamine; d) separation of the diastereoisomeric salt to obtain R(+)6,8-di-halo-octanoic acid by reation of said salt with strong mineral acids in an aqueous solution with a dilution between 2 and 10% by weight; e) esterification of R(+)6,8-di-halo-octanoic acid to obtain the corresponding alkyl ester; f) reaction of the alkyl ester of R(+)6,8-di-halo-octanoic acid in an organic solvent with an aqueous solution of alkali disulfide in presence of a compound for phase transfer catalysis; g) hydolysis of the ester of R(+)α-lipoic acid.
摘要:
Active acne and acneiform scars are treated by topical application of a composition containing lipoic acid and/or a lipoic acid derivative such as dihydrolipoic acid, a lipoic or dihydrolipoic acid ester, a lipoic or dihydrolipoic acid amide, a lipoic or dihydrolipoic acid salt, and mixtures of any of these to reduce erythema, pore size, and scarring. Topical application of lipoic acid and/or a lipoic acid derivatives are advantageously used with at least one adjunct ingredient such as a retinoid, an antibiotic, or benzoyl peroxide conventionally used for acne, alone or in combination with dimethylaminoalcohol, an alpha-hydroxy acid such as glycolic acid, a tyrosine, tocotrienol, and/or a fatty acid ester of ascorbic acid. One preferred embodiment contains a combination of lipoic acid, an alpha-hydroxy acid, and dimethylaminoalcohol.
摘要:
The invention concerns novel lipoic acid derivatives, which have an inhibiting action with respect to NO-synthase enzymes producing nitrogen monoxide NO and/or are agents enabling the regeneration of antioxidants or entities trapping reactive oxygen species (ROS) and intervening in a more general manner in the redox status of thiol groups. The invention also concerns methods for preparing them, pharmaceutical compositions containing them and their use for therapeutic purposes, particularly their use as NO-synthase inhibitors and/or as agents acting more generally in the redox status of thiol groups.
摘要:
The present invention provides novel compounds having scavenging and anti-ROS properties and pharmaceutical composition comprising these compounds for treatment of conditions associated with oxidative stress or free radical injury. The compounds of the invention are of general formula (I).
摘要:
The invention relates to enantiomer-free crystalline (R) or (S) lipoic acid, where the reflection line at 2 Υ = 23° is the most intensive one in the 13° to 30° range in the 2 Υ diffractogram.
摘要:
Die vorliegende Erfindung betrifft ein Verfahren zur Herstellung trockener Thioctsäure, bei dem man ein Rohmaterial in dem Thioctsäure angereichert vorhanden ist, mit flüssigem oder überkritischem CO 2 behandelt und dadurch in einem einfachen technischen Verfahren zu Thioctsäure mit niedrigen Restlösemittelgehalten gelangt.
摘要:
Compounds of formula (I): [in which: one of m and n is 0, and the other is 0, 1 or 2; k is 0 or an integer of from 1 to 12; R 1 is hydrogen, one of substituents α, defined below, or an optionally substituted alkyl group; A is a single bond, an oxygen atom, a carbonyl group or a group of formula -N(R 2 )CO-, -N(R 2 )CS-, -N(R 2 )SO 2 -, -CON(R 2 )N(R 3 )CO-, -CON(R 2 )CO-, -CON(R 2 )CS-, -CON(R 2 )SO 2 -, -O-CO-, -ON(R 2 )CO-, -ON(R 2 )SO 2 -, -O-CON(R 2 )N(R 3 )CO-, -O-CON(R 2 )CO-, -O-CON(R 2 )SO 2 -, -CO-O-, -CO-CO-, -CO-CON(R 2 )N(R 3 )CO-, -CO-CON(R 2 )CO-, -CO-CON(R 2 )SO 2 -, -N(R 2 )O-, -N(R 2 )COCO-, -N(R 2 )N(R 3 )CO-, -N(R 2 )N(R 3 )SO 2 -, -N(R 2 )CON(R 3 )N(R 4 )CO-, -N(R 2 )CON(R 3 )CO-, -N(R 2 )CON(R 3 )SO 2 - or -N(R 2 )CON(R 3 )SO 2 N(R 4 )CO- in which R 2 , R 3 and R 4 are the same or different and each is hydrogen, alkyl, aralkyl, acyl or one of substituents α; B is a single bond, or a group of formula -N(R 5 )- or -N(R 6 )N(R 5 )- in which R 5 and R 6 are the same or different and each is hydrogen, alkyl, aralkyl, acyl or one of substituents α, or R 5 , together with R 1 and the nitrogen atom to which they are bonded, may form a heterocyclic ring having from 5 to 7 ring atoms; or R 1 may represent a group of formula -OR 7 , in which R 7 is alkyl, alkenyl, aralkyl or one of substituents α; or R 1 may represent a hydroxy group or a group of formula -OR 7 ; and said substituents α are selected from aryl groups and heterocyclic groups] and pharmaceutically acceptable salts thereof have an excellent ability to enhance the activity of glutathione reductase and can therefore be used for the treatment and prevention of a variety of diseases including cataracts.
摘要:
Die Erfindung betrifft die Herstellung und Reinigung von Salzen der 6,8-Bis(amidiniumthio)octansäure, deren Enantiomeren (+)-6,8-Bis(amidiniumthio)octansäure und (-)-6,8-Bis(amidiniumthio)octansäure und der Ester dieser Verbindungen sowie deren Verwendung zur Herstellung von Dihydroliponsäure und α-Liponsäure.