Medical application of lipid derivatives of dopamine
    62.
    发明公开
    Medical application of lipid derivatives of dopamine 有权
    医药用多巴胺的脂质衍生物

    公开(公告)号:EP2324824A3

    公开(公告)日:2011-06-15

    申请号:EP10191670.8

    申请日:2010-11-18

    CPC分类号: A61K31/165

    摘要: The subject of the present invention is the medical application of N-oleoyl-dopamine and 3'-O-methyl-N-oleoyl-dopamine for the production of a medication for treatment or prophylaxis of disturbances or states due to deficiency of dopamine, preferably chosen from the group covering oxygen deficiencies (hypoxia) in anesthetized and awake mammals, breathing with atmospheric oxygen (normoxia), for the respiratory responses to hypoxia in mammals, lack of dopamine binding to the membrane system in the mammalian brain, disturbances in metabolic pathways of dopamine metabolism, states of dopamine deficiencies provoked by morbid or genetic factors as well as under condition connected to the physiological process of aging of the organism, through the systemic introduction of the compound to the mammalian organism.
    The subject of the present invention is also the method of production of 3'-O-methyl-N-oleoyl-dopamine in vitro which consists of, according to the present invention, a reaction of 3-O-methyl-dopamine hydrochloride with oleic acid in the presence of, preferably, BOP
    (Benzotriazole-1-yl-oxy-tris-(dimethylamino)-phosphonium hexafluorophosphate), DCC ( N , N '-dicyclohexylcarbodiimide), DMAP (4-Dimethylaminopyridine) and THF (tetrahydrofuran), CH 2 Cl 2 (dichloromethane), CHCl 3 (chloroform), toluene, diethyl ether. The reaction mixture is cooled to temperature of 0-10°C, a solution of trietanolamine is added under continuous stirring and
    3'-O-methyl-N-oleoyl-dopamine is precipitated and purified by a known method.
    A variant of the method of production of 3'-O-methyl-N-oleoyl-dopamie consists of, according to the present invention, a reaction of methylation of N-oleoyl-dopamine by the catechol-O-methyltransferase (COMT) in the presence of
    S-adenosyl-L-methionine (SAM) and magnesium ions in phosphate buffered saline (PBS) solution buffered to pH of 7.0-8.0 at temperature of 25-45°C, followed by the precipitation and purification of 3'-O-methyl-N-oleoyl-dopamine by a known method.

    New cis-platinum compound and a method for pharmaceutic production
    64.
    发明公开
    New cis-platinum compound and a method for pharmaceutic production 失效
    Cis-Platin-Verbindung und Methode zur Herstellung von Arzneimitteln。

    公开(公告)号:EP0249219A1

    公开(公告)日:1987-12-16

    申请号:EP87108395.2

    申请日:1987-06-10

    IPC分类号: C07F15/00 A61K49/00

    摘要: The object of the invention is a pharmaceutic production, particularly for diagnosis of neoplasmas, based on the enclosed formula I. To the aqueous solution of potassium tetrachloroplatinate is added methionine by the molar relation of methionine to tetrachloroplatinate 2 to 1. The solution is mixed intensively. The aqueous solution of tetrachloroplatinate before the addition of methionine is enriched to a large concentration of chlo­rides, e.g. by the addition of sodium chloride and po­tassium chloride and pH of the mixture is brought to the value 3 to 5. Methionine is added to so prepared solution and in the course of further manufacturing pro­cess, to the complex of dichlorodimethionineplatinum is added metal salt. The components are mixed and pH of the solution is brought to the value about 6, 5. At last the solution is infiltrated through the sterile filter.

    摘要翻译: 本发明的目的是根据封闭的配方I进行药物生产,特别是用于诊断肿瘤。对四氯铂酸钾的水溶液通过甲硫氨酸与四氯铂酸盐的摩尔关系为2:1加入甲硫氨酸。该溶液集中混合 。 在加入甲硫氨酸之前,四氯铂酸盐的水溶液富含大量氯化物,例如氯化钠。 通过加入氯化钠和氯化钾,使混合物的pH值达到3〜5。将甲硫氨酸加入到如此制备的溶液中,在进一步制备过程中,向二氯二甲硫氨酸铂的络合物中加入金属盐。 将组分混合,使溶液的pH达到约5,6,最后将溶液通过无菌过滤器渗透。