HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF
    1.
    发明申请
    HYPERFORIN ANALOGS, METHODS OF SYNTHESIS, AND USES THEREOF 审中-公开
    HYPERFORIN ANALOGS,合成方法及其用途

    公开(公告)号:WO2012167021A3

    公开(公告)日:2013-04-25

    申请号:PCT/US2012040379

    申请日:2012-06-01

    Abstract: The present invention provides a novel 11-step enantioselective approach to the natural product hyperforin, which enables access to a wide variety of hyperforin analogs. The present invention also provides pharmaceutical compositions comprising inventive hyperforin analogs. Hyperforin analogs synthesized using the present synthetic method are envisionsed useful in the treatment of various conditions, including, but not limited to, depression and conditions characterized by depression, inflammatory skin conditions, diabetes, asthma, chronic obstructive pulmonary disease (COPD), kidney disorders, and ischemic brain damage.

    Abstract translation: 本发明提供了对天然产物hyperforin的新型11步对映选择性方法,其能够接近各种各样的hyperforin类似物。 本发明还提供包含本发明的高福林类似物的药物组合物。 使用本合成方法合成的Hyperforin类似物被设想用于治疗各种病症,包括但不限于以抑郁症,炎性皮肤病症,糖尿病,哮喘,慢性阻塞性肺病(COPD),肾脏疾病为特征的抑郁症和病症 ,和缺血性脑损伤。

    Preparation of astaxanthin
    4.
    发明申请
    Preparation of astaxanthin 审中-公开
    虾青素的制备

    公开(公告)号:WO01081301A3

    公开(公告)日:2002-04-25

    申请号:PCT/US2001/013295

    申请日:2001-04-25

    CPC classification number: C07C403/24

    Abstract: The present invention provides a method for preparing astaxanthin from zeaxanthin. Specifically, the present invention provides a method for said conversion using a halogenating agent with the salt of chloric or bromic acid in an inert solvent.

    2-ALKYLIDENE-19-NOR-VITAMIN D COMPOUNDS
    5.
    发明申请
    2-ALKYLIDENE-19-NOR-VITAMIN D COMPOUNDS 审中-公开
    2-烷基-19-异维生素D化合物

    公开(公告)号:WO98041501A1

    公开(公告)日:1998-09-24

    申请号:PCT/US1998/002976

    申请日:1998-02-11

    CPC classification number: C07C401/00 C07F7/1804 Y02P20/55

    Abstract: The invention provides a novel class of vitamin D related compounds, namely, the 2-alkylidene-19-nor-vitamin D derivatives, as well as a general method for their chemical synthesis. The compounds have the formula (I) where Y1 and Y2, which may be the same or different, are each selected from the group consisting of hydrogen and a hydroxy-protecting group, R6 and R8, which may be the same or different, are each selected from hydrogen, alkyl, hydroxyalkyl and fluoroalkyl, or when taken together represent the group -(CH2)x- where x is an integer from 2 to 5, and where the group R represents any of the typical side chains known for vitamin D type compounds. These 2-substituted compounds are characterized by low intestinal calcium transport activity and high bone calcium mobilization activity resulting in novel therapeutic agents for the treatment of diseases where bone formation is desired, particularly low bone turnover osteoporosis. These compounds also exhibit pronounced activity in arresting the proliferation of undifferentiated cells and inducing their differentiation to the monocyte thus evidencing use as anti-cancer agents and for the treatment of diseases such as psoriasis.

    Abstract translation: 本发明提供了一类维生素D相关化合物,即2-亚烷基-19-去甲维生素D衍生物,以及它们化学合成的一般方法。 化合物具有式(I),其中可以相同或不同的Y1和Y2各自选自氢和羟基保护基,R6和R8可以相同或不同,分别为 每个选自氢,烷基,羟基烷基和氟代烷基,或当它们一起表示基团 - (CH 2)x - ,其中x是2至5的整数,并且其中基团R表示维生素D已知的任何典型侧链 型化合物。 这些2-取代的化合物的特征在于低钙运输活性和高的钙钙动员活性,导致用于治疗需要骨形成,特别是低骨转换性骨质疏松症的疾病的新型治疗剂。 这些化合物在阻止未分化细胞的增殖并诱导其分化为单核细胞方面也表现出显着的活性,因此证明其用作抗癌剂并用于治疗诸如牛皮癣的疾病。

    PROCESS FOR THE HYDROGENATION OF HOP RESIN ACIDS
    10.
    发明申请
    PROCESS FOR THE HYDROGENATION OF HOP RESIN ACIDS 审中-公开
    HOP树脂酸加氢方法

    公开(公告)号:WO01036581A1

    公开(公告)日:2001-05-25

    申请号:PCT/US1999/027338

    申请日:1999-11-18

    CPC classification number: C12C3/00 C12C9/025

    Abstract: A process for the direct hydrogenation of hop resin acids in the absence of a liquid, organic solvent by reacting the hop resin acids with hydrogen in the presence of a noble metal catalyst at a temperature at which the resin acids are sufficiently fluid to allow easy mixing with the catalyst and suitably facilitate the hydrogenation reaction. Alternatively, the necessary fluidity may be achieved at relatively low temperature by subjecting the reactants to a high pressure of CO2 gas such that the quantity of this gas that dissolves into the resin is sufficient to substantially reduce its viscosity, the pressure of the CO2 gas being either less than the liquefaction pressure at temperatures below the critical temperature or less than that which would cause the density to exceed that at the critical point for temperatures above the critical temperature. A further variant allows for the hydrogenation of the resin acids as a suspension in water and is considered most appropriate for the processing of resins that are of relatively more viscous nature in circumstances where the application of a high pressure of gas may not be possible for mechanical reasons. Particularly useful applications for the process are the conversion of iso- alpha -acids to tetrahydroiso- alpha -acids and rho -iso- alpha -acids into hexahydroiso- alpha -acids. The resinous products of the hydrogenation process may be readily converted to aqueous, alkaline solutions suitable for use in brewing beer. The process may also be worked in a continuous manner, wherein hop resin acids in suitably fluid state and under high pressure are contacted with hydrogen gas and the resultant mixture passed over a bed of noble metal catalyst particles. The necessary fluidity is achieved either by heating the hop resin acid or by dissolving CO2 gas into it or a combination of both. The resinous product of the hydrogenation reaction is collected by depressurisation of the fluid exiting the catalyst bed, conveniently causing release of any excess dissolved gas.

    Abstract translation: 在树脂酸充分流动的温度下,在贵金属催化剂存在下,通过使啤酒花树脂酸与氢反应使液体有机溶剂直接氢化的方法,以便容易地混合 与催化剂合适地促进氢化反应。 或者,通过使反应物经受高压的二氧化碳气体,可以在较低的温度下实现必要的流动性,使得溶解到树脂中的这种气体的量足以显着降低其粘度,二氧化碳气体的压力为 低于临界温度以下的液化压力或低于在临界温度高于临界温度时的临界温度下的液化压力。 进一步的变体允许树脂酸作为悬浮液在水中的氢化,并且被认为是最适合加工在具有较高粘度性质的树脂中,其中施加高压气体可能不可能用于机械 原因。 该方法的特别有用的应用是将异-α-酸转化为四氢异-α-酸和正 - 异-α-酸转化为六氢异-α-酸。 氢化方法的树脂产物可以容易地转化成适用于酿造啤酒的水性碱性溶液。 该方法也可以以连续的方式进行,其中在适当的流体状态和高压下的啤酒花树脂酸与氢气接触,所得混合物通过贵金属催化剂颗粒床。 必要的流动性通过加热啤酒花树脂酸或通过将CO 2气体溶解到其中或两者的组合来实现。 通过对离开催化剂床的流体减压来收集加氢反应的树脂产物,方便地释放任何过量的溶解气体。

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