首页> 外国专利> method for preparing a therapeutic preparation with antibiotic activity and / or cytostatic activity against tumor cells formed preparationmethod for preparing for the win and werkijze appropriate connections.

method for preparing a therapeutic preparation with antibiotic activity and / or cytostatic activity against tumor cells formed preparationmethod for preparing for the win and werkijze appropriate connections.

机译:制备具有对肿瘤细胞具有抗生素活性和/或细胞抑制活性的治疗制剂的方法,形成了制备方法,用于准备成功和成功的联系。

摘要

1,194,238. Alkyl--glyceryl ethers. ASTRA NUTRITION A.B. 15 Dec., 1967 [16 Dec., 1966], No. 57149/67. Heading C2C. The invention comprises compounds of the Formula (I) where RSP1/SP and RSP2/SP are the same or different and represent hydrogen or aliphatic acyl groups of at most 24 carbon atoms, one of RSP3/SP and RSP4/SP is hydrogen and the other is an alkoxy or alkenyloxy group of at most 7 carbon atoms and RSP5/SP represents a straight or branched, saturated or mono- or poly-unsaturated aliphatic group of 4 to 21 carbon atoms. They are extracted from naturally occurring lipid products containing -glyceryl ethers, such as liver oils from Greenland shark, dog-fish, rat-fish, by distributing the lipid product, preferably after prepurification by removal of hydrocarbons and saponifiable constituents, between two media forming separate phases comprising an operation consisting of a preferably repeated extraction using two partially miscible liquids or chromatography of the lipid product in a solvent on a solid adsorbent such as silicic acid or deactivated aluminium oxide or treating the lipid product in a solvent with a substance capable of forming inclusion compounds with some part of the glyceryl ether mixture or by fractional crystallization from a polar solvent. Compounds of Formula (I) may be prepared by reacting a compound of the formula with a compound of the formula wherein RSP3#1/SP, RSP4#1/SP and RSP5#1/SP represent RSP3/SP, RSP4/SP or RSP5/SP respectively or an atom or group capable of being transformed into RSP3/SP, RSP4/SP or RSP5/SP respectively by methods known in the literature, RSP7/SP represents an oxygen atom, a carbon-carbon bond or the group where RSPa/SP represents hydrogen or alkyl, RSPb/SP represents alkyl or aryl and RSPa/SP and RSPb/SP together may form a ring which may contain a hetero atom and X and Y are a pair representing the pairs of groups (a) hal, and -OM, (b) arylsulphonyl and -OM, (c) alkylsulphonyl and -OM, and (d) hydroxy and hydroxy, where that means halogen, preferably chlorine or bromine, and M is a positively charged atom or group, preferably K, Na or Li, to form a compound of the formula whereafter if any of RSP3#1/SP , RSP4#1/SP and RSP5#1/SP differ from RSP3/SP, RSP4/SP and RSP5/SP respectively, the differing groups are transformed into the predetermined group and whereafter the group is transformed to the group CH 2 ORSP1/SP, CHORSP2/SP- by methods known in the literature. 2-Methoxy (or 2-ethoxy) hexadecyl p-toluenesulphonate is prepared by reacting p-toluenesulphonyl chloride with 2-methoxy (or 2- ethoxy) hexadecanol. 2 - Methoxy - hexadecanol - 1 is prepared by reducing with lithium aluminium hydride methyl 2-methoxy-hexadecanoate which is prepared by methylating 2-hydroxyhexadecanoic acid. 2 - Hydroxy - hexadecanoic acid is prepared by hydrolysing 2-bromohexadecanoic acid. 2 - Ethoxy - hexadecanol - 1 is prepared by reducing ethyl - 2 - ethoxy - hexadecanoate which is prepared from ethyl 2-bromohexadecanoate and sodium ethoxide. Pharmaceutical compositions comprising as active ingredient a compound of Formula (I) together with a pharmaceutically acceptable carrier are administered orally or parenterally and have anti-biotic and anti-carcinogenic activity.
机译:1,194,238。烷基-甘油醚。 ASTRA营养A.B. 1967年12月15日[1966年12月16日],第57149/67号。标题C2C。本发明包含式(I)的化合物,其中R 1 和R 2 相同或不同,并且表示氢或最多24个碳原子的脂族酰基,一个R 3 和R 4 的一个是氢,另一个是至多7个碳原子的烷氧基或烯氧基,R 5 表示直链或4至21个碳原子的支链,饱和或单或多不饱和脂族基团。它们是通过在两种介质形成之间,最好是在通过去除烃和皂化成分的预纯化后,分配脂质产品而从脂质产品中提取的,这些脂质产品是从含有-甘油醚的天然脂质产品(例如格陵兰鲨鱼,狗鱼,大鼠鱼的肝油)中提取的。分离的相,包括优选重复使用两种部分混溶的液体进行萃取或在固体吸附剂(如硅酸或减活的氧化铝)上的溶剂中对脂质产物进行色谱分离,或在溶剂中用能够分离脂质的物质处理脂质产物的操作与一部分甘油醚混合物或通过从极性溶剂中分步结晶形成夹杂物。式(I)的化合物可以通过使所述式的化合物与下式的化合物反应来制备:其中R 3#1 ,R 4#1 和R 5#1 分别表示R 3 ,R 4 或R 5 或能够转化为R的原子或基团通过文献中已知的方法分别 3 ,R 4 或R 5 ,R 7 代表氧原子,碳-碳键或基团,其中R a 代表氢或烷基,R b 代表烷基或芳基,R a 和R b 一起可以形成一个可包含杂原子的环,X和Y是一对,分别代表以下基团:(a)hal和-OM,(b)芳基磺酰基和-OM,(c)烷基磺酰基和-OM,和(d)羟基和羟基,其中是卤素,优选氯或溴,并且M是带正电的原子或基团,优选K,Na或Li,以形成下式的化合物: R 3#1 ,R 4#1 和R 5#1 分别不同于R 3 ,R 4 和R 5 ,不同的组被转换为预定的组然后通过文献中已知的方法将该基团转化为CH 2 OR 1 ,CHOR 2 -。对甲苯磺酸2-甲氧基(或2-乙氧基)十六烷基酯是通过使对甲苯磺酰氯与2-甲氧基(或2-乙氧基)十六醇反应制备的。 2-甲氧基-十六烷醇-1通过用氢化铝锂还原2-甲氧基-十六烷酸甲酯而制得,所述2-甲氧基-十六烷酸甲酯是通过使2-羟基十六烷酸甲基化而制得的。 2-羟基十六烷酸是通过水解2-溴十六烷酸制备的。 2-乙氧基-十六烷醇-1是通过还原由2-溴十六烷酸乙酯和乙醇钠制得的乙基-2-乙氧基-十六烷酸酯而制得的。包含式(I)的化合物和药学上可接受的载体作为活性成分的药物组合物经口服或肠胃外给药,并且具有抗生和抗癌活性。

著录项

  • 公开/公告号NL160164B

    专利类型

  • 公开/公告日1979-05-15

    原文格式PDF

  • 申请/专利权人 ASTRA NUTRITION AB MOELNDAL ZWEDEN.;

    申请/专利号NL19670017165

  • 发明设计人

    申请日1967-12-15

  • 分类号A61K31/075;A61K31/21;C07C43/04;C07C69/00;

  • 国家 NL

  • 入库时间 2022-08-22 20:42:45

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