VERFAHREN ZUR HERSTELLUNG VON LIPONSÄURE UND DIHYDROLIPONSAÜRE
    111.
    发明公开
    VERFAHREN ZUR HERSTELLUNG VON LIPONSÄURE UND DIHYDROLIPONSAÜRE 有权
    用于生产硫辛酸和DIHYDROLIPONSAÜRE

    公开(公告)号:EP1339705A2

    公开(公告)日:2003-09-03

    申请号:EP01990455.6

    申请日:2001-11-29

    IPC分类号: C07D339/04

    CPC分类号: C07D339/04

    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.

    Dithiolan derivatives, their preparation and their therapeutic effect
    119.
    发明公开
    Dithiolan derivatives, their preparation and their therapeutic effect 失效
    Dithiolan Derivate,deren Herstellung und deren Heileffekt

    公开(公告)号:EP0869126A1

    公开(公告)日:1998-10-07

    申请号:EP98302532.1

    申请日:1998-04-01

    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.

    摘要翻译: 式(I)化合物:其中:m和n之一为0,另一个为0,1或2; k为0或1〜12的整数; R 1是氢,下面定义的取代基α之一或任选取代的烷基; A是单键,氧原子,羰基或式-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) -O-CON(R 2)CO-,-O-CON(R 2)SO 2 - ,-CO-O-,-CO-CO-,-CO-CON(R 2) (R 2)CO - , - CO-CON(R 2)CO-,-CO-CON(R 2)SO 2 - , - N(R 2) CO 2 - , - (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 - 或-N(R 2)CON(R 3)SO 2 N(R 4)CO-,其中R 2,R 3和R 4相同或不同, 是氢,烷基,芳烷基,酰基或取代基α之一; B是单键或式-N(R 5) - 或-N(R 6)N(R 5) - 的基团,其中R 5和R 6是 相同或不同,各自为氢,烷基,芳烷基,酰基或取代基α或R 5之一,与R 1和它们所键合的氮原子一起可以形成具有5至 7个环原子; 或R 1可以表示式-OR 7的基团,其中R 7是烷基,烯基,芳烷基或取代基α之一; 或R 1可以表示羟基或式-OR 7基团; 并且所述取代基α选自芳基和杂环基团及其药学上可接受的盐具有提高谷胱甘肽还原酶活性的优异能力,因此可用于治疗和预防各种疾病,包括白内障。