Racemic dissociation of 3-acyloxy bicyclo(3.3.0)octan-7-one-2-carboxylic
acid esters by stereospecific enzymatic or microbiological acylate
hydrolysis
    32.
    发明授权
    Racemic dissociation of 3-acyloxy bicyclo(3.3.0)octan-7-one-2-carboxylic acid esters by stereospecific enzymatic or microbiological acylate hydrolysis 失效
    3-立体特异性酶或微生物酰化物水解3-酰氧基双环(3.3.0)辛-7-酮-2-羧酸酯的外消旋解离

    公开(公告)号:US4894336A

    公开(公告)日:1990-01-16

    申请号:US237109

    申请日:1988-07-13

    Abstract: Process for the production of optically active (+)-bicyclo[3.3.0]octanol derivatives of formula (+)-I, in which R.sub.1 and R.sub.2 represent jointly an oxygen atom or the double-bond residue --O--X--O-- with X as a straight or branched-chain alkylene with 1-7 C-atoms, or R.sub.1 and R.sub.2 represent separately the residue OR.sub.5 with R.sub.5 as a straight or branched-chain alkyl with 1-7 C-atoms, and R.sub.3 the residue COOZ with Z as a hydrogen atom, straight or branched chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 atoms or R.sub.3 is the residue --(CH.sub.2).sub.n --O--COR.sub.4 with n having the meaning 1-4 and R.sub.4 as a straight or branched-chain alkyl with 1-7 C atoms, cycloalkyl with 3-6 C atoms, phenyl or aralkyl with 7-10 C atoms. The process is characterized in that racemic 3.alpha.-cyloxy-cis-bicyclo[3.3.0]-octane derivatives of formula (+)-II, wherein R.sub.1, R.sub.2 R.sub.3 and R.sub.4 have the above meanings, are subjected enzymatically or microbiologically to a stereospecific acylate hydrolsis and the (+)-bicyclo[3.3.0]-octanol derivative produced is separated from the unsaponified bicyclo[3.3.0]-octanol acylate of formula (-)-II or the unsaponified enantiomers (+)-II are separated from the saponified bicyclo[3.3.0]octanol derivative (-)-I and then subjected to chemical acylate hydrolysis.

    Abstract translation: PCT No.PCT / DE87 / 00513 Sec。 371日期:1988年7月13日 102(e)日期1988年7月13日PCT提交1987年11月12日PCT公布。 出版物WO88 / 03567 日期:1988年5月19日。制备式(+) - I的光学活性(+) - 双环[3.3.0]辛醇衍生物的方法,其中R 1和R 2共同表示氧原子或双键残基-OXO - X为具有1-7个C原子的直链或支链亚烷基,或者R1和R2分别表示残基OR5与R5作为具有1-7个C原子的直链或支链烷基,R3表示残基 具有Z作为氢原子的COOZ,具有1-7个C原子的直链或支链烷基,具有3-6个C原子的环烷基,具有7-10个原子的苯基或芳烷基或R3是残基 - (CH2)nO-COR4,其中n 具有1-4和R4为具有1-7个C原子的直链或支链烷基,具有3-6个C原子的环烷基,具有7-10个C原子的苯基或芳烷基。 该方法的特征在于其中R1,R2R3和R4具有上述含义的式(+) - II的外消旋3α-甲氧基 - 顺式 - 双 - 二环[3.3.0] - 辛烷衍生物经酶促或微生物方式进行立体特异性 将酰化物水解和(+) - 双环[3.3.0] - 辛醇衍生物与式( - ) - II的未皂化的双环[3.3.0] - 辛醇酰化物分离,或未分离的对映异构体(+) - 从皂化的双环[3.3.0]辛醇衍生物( - ) - I中,然后进行化学酰化物水解。

    Soluble phosphorylated glucan
    34.
    发明授权
    Soluble phosphorylated glucan 失效
    可溶性磷酸化葡聚糖

    公开(公告)号:US4739046A

    公开(公告)日:1988-04-19

    申请号:US767388

    申请日:1985-08-19

    CPC classification number: C08B37/0024 Y10S514/908

    Abstract: A new class of soluble phosphorylated glucans is described as well as the process for making the same. According to a preferred embodiment, the soluble phosphorylated glucan is derived from the yeast Saccharomyces cerevisiae. The soluble phosphorylated glucans are useful for prophylactic and therapeutic applications against neoplastic, bacteria, viral, fungal and parasitic diseases. Additionally, they may be administered as a non-toxic adjuvant, in combination with chemotherapy. The soluble phosphorylated glucans are also useful for stimulating macrophage cells, either in vivo or in vitro, to produce a cytotoxic/cyctostatic factor effective against cancer cells.

    Abstract translation: 描述了一类新的可溶性磷酸化葡聚糖以及其制备方法。 根据优选的实施方案,可溶性磷酸化葡聚糖衍生自酿酒酵母酿酒酵母(Saccharomyces cerevisiae)。 可溶性磷酸化葡聚糖可用于预防和治疗抗肿瘤,细菌,病毒,真菌和寄生虫病的应用。 另外,它们可以作为无毒佐剂与化学疗法组合施用。 可溶性磷酸化葡聚糖也可用于在体内或体外刺激巨噬细胞以产生对癌细胞有效的细胞毒性/细胞因子。

    Method for manufacturing liposomes
    36.
    发明授权
    Method for manufacturing liposomes 失效
    制造脂质体的方法

    公开(公告)号:US4622188A

    公开(公告)日:1986-11-11

    申请号:US684947

    申请日:1984-12-21

    CPC classification number: A61K9/1277 Y10S436/829

    Abstract: A method and apparatus for manufacturing liposomes is characterized by optically monitoring the light transmission of a liposome precursor solution and controlling the flow rate and/or temperature of the precursor solution and/or a dialysis buffer solution in accordance therewith.

    Abstract translation: 用于制造脂质体的方法和装置的特征在于通过光学监测脂质体前体溶液的光透射并根据其控制前体溶液和/或透析缓冲溶液的流速和/或温度。

    Monomethylamine-oxidizing enzyme
    39.
    发明授权
    Monomethylamine-oxidizing enzyme 失效
    单甲胺氧化酶

    公开(公告)号:US4503147A

    公开(公告)日:1985-03-05

    申请号:US435316

    申请日:1982-10-19

    CPC classification number: C12N9/0022 C12Q1/26 Y10S435/829 Y10S435/832

    Abstract: A monomethylamine-oxidizing enzyme can be obtained by cultivating in a medium a strain which belongs to Genus Bacillus and has an ability to produce a monomethylamine-oxidizing enzyme. This enzyme exhibits several beneficial properties including the ability to oxidatively deaminate the amino group of monomethylamine to produce formaldehyde, ammonia, and hydrogen peroxide. The enzyme exhibits a high substrate specificity for monomethylamine, ethylamine, and n-proplyamine while showing no substrate specificity for benzylamine, dimethylamine, trimethylamine, ethylenediamine and tryamine. In addition, the enzyme is stable through an elevated temperature range permitting faster reaction rates and therefore a shorter overall quantitative evaluation. Another property includes a low Km value which allows smaller quantities of the enzyme to be employed per sample.

    Abstract translation: 通过在培养基中培养属于芽孢杆菌属的菌株并具有产生单甲胺氧化酶的能力,可以获得单甲胺氧化酶。 该酶显示出几种有益的性质,包括使一甲胺的氨基氧化脱氨以产生甲醛,氨和过氧化氢的能力。 该酶对单甲胺,乙胺和正丙胺显示出高的底物特异性,同时对苄胺,二甲胺,三甲胺,乙二胺和试胺没有底物特异性。 此外,酶在升高的温度范围内是稳定的,允许更快的反应速率,因此较短的总体定量评估。 另一种性质包括低Km值,其允许每个样品使用较少量的酶。

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