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    STABILIZED CHOLINE SOLUTIONS AND METHODS FOR PREPARING THE SAME
    25.
    发明公开
    STABILIZED CHOLINE SOLUTIONS AND METHODS FOR PREPARING THE SAME 审中-公开
    稳定CHOLINLÖSUNGEN及其制备方法

    公开(公告)号：EP2782899A1

    公开(公告)日：2014-10-01

    申请号：EP12801483.4

    申请日：2012-11-22

    申请人： Taminco

    发明人： MOONEN, Kristof ,  GERNON, Michael, David

    IPC分类号： C07C213/10 ,  C07C215/40 ,  C07C239/10 ,  C01B17/66

    摘要： A method for the stabilization of an aqueous choline hydroxide solution includes optionally, adding a first stabilizer of a dithionite salt or a dialkylhydroxylamine to an aqueous solution containing reactants that will produce an aqueous choline hydroxide solution; and after the aqueous choline hydroxide solution is formed, adding a second stabilizer of a dithionite salt or a dialkylhydroxylamine to the aqueous choline hydroxide solution. The stabilized choline hydroxide solution may include choline hydroxide, water, and a dithionite salt and/or a dialkylhydroxylamine as a stabilizer present in an amount of about 100 ppm to about 2000 ppm by weight of the stabilized choline hydroxide solution.

    POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF RETINOIDS AND RETINOID-LIKE COMPOUNDS WITH VERY HIGH SKIN PENETRATION RATES
    29.
    发明公开
    POSITIVELY CHARGED WATER-SOLUBLE PRODRUGS OF RETINOIDS AND RETINOID-LIKE COMPOUNDS WITH VERY HIGH SKIN PENETRATION RATES 有权
    带正电荷的维甲酸和RETINOIDÄHNLICHEN关系的水溶性前体药物具有非常高的皮肤渗透速率

    公开(公告)号：EP2125697A1

    公开(公告)日：2009-12-02

    申请号：EP07700593.2

    申请日：2007-01-15

    申请人： Yu, Chongxi

    发明人： Yu, Chongxi

    IPC分类号： C07C215/40

    CPC分类号： A61K47/48023 ,  A61K31/21 ,  A61K31/215 ,  A61K31/216 ,  A61K31/221 ,  A61K31/4453 ,  A61K47/54 ,  C07C219/10 ,  C07C2601/16 ,  C07C2602/10 ,  G01N33/502

    摘要： The novel positively charged pro-drugs of retinoids and retinoid-like compounds in the general formula (31) 'Structure 31' were designed and synthesized. The compounds of the general formula (31) 'Structure 31' indicated above can be prepared from retinoic acids and related compounds, by reaction with suitable alcohols, thiols, or amines and coupling reagents, such as N, N'-Dicyclohexylcarbodiimide, N,N'-Diisopropylcarbodiimide, O- (Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium tetrafluoroborate, O- (Benzotriazol-1-yl)-N,N,N',N'-tetramethyluronium hexafluorophosphate, Benzotriazol- 1-yl-oxy-tris(dimethylamino)phosphonium hexafluorophosphate, et al. The positively charged amino groups of these pro-drugs not only largely increases the solubility of the drugs in water, but also bonds to the negative charge on the phosphate head group of membranes. This bonding will disturb the membrane a little bit and may make some room for the lipophilic portion of the prodrug. When the molecules of membrane move, the membrane may 'crack' a little bit due to the bonding of the prodrug. This will let the prodrug insert into the membrane. At pH 7.4, only about 99% of amino group is protonated. When the amino group is not protonated, the bonding between the amino group of the prodrug and the phosphate head group of membrane will disassociate, and the prodrug will enter the membrane completely. When the amino group of the prodrug flips to the other side of the membrane and thus become protonated, then the prodrug is pulled into the cytosol, a semi-liquid concentrated aqueous solution or suspension. The results suggest that the pro-drugs diffuse through human skin -350 times faster than do retinoids and retinoid-like compounds. In plasma, more than 90% of these pro-drugs can change back to the parent drugs in a few minutes. The prodrugs can be used medicinally in treating any retinoids and retinoid-like compounds-treatable conditions in humans or animals. The prodrugs can be administered transdermally for any kind of medical treatments and avoid most of the side effects of retinoids and retinoid-like compounds. Controlled transdermal administration systems of the prodrug enables retinoids and retinoid-like compounds to reach constantly optimal therapeutic blood levels to increase effectiveness and reduce the side effects of retinoids and retinoid-like compounds. Another great benefit of transdermal administration of these pro-drugs is that administering medication, especially to children, will be much easier.

    摘要翻译： 本发明提供了新颖的高渗透的组合物（HPC）或类视色素和类视黄醇相关化合物的高渗透的前药（HPP），其能够穿越高穿透效率的生物屏障的的组合物。 所述HPPS能够穿越生物屏障后转化为活性母体药物或药物代谢物，因此可以使所要求的条件的处理做了母体药物或代谢物可以。 另外，所述HPPS能够到达的区域没有母体药物可能无法访问或呈现在目标区域足够的浓度，并因此呈现新颖的治疗的。 该HPPS可给予通过各种给药途径主题，E. G.，本地交付给一个条件的作用位点具有高浓度或系统给予生物样本，并用更快的速度进入普通流通。

    PROCESS FOR PREPARING DIHYDROXYTRIALKYLAMMONIUM HALIDES AND PRODUCTS THEREOF
    30.
    发明公开
    PROCESS FOR PREPARING DIHYDROXYTRIALKYLAMMONIUM HALIDES AND PRODUCTS THEREOF 审中-公开
    制备二羟基三羟基烷基吡啶鎓盐的方法及其产物

    公开(公告)号：EP1986992A1

    公开(公告)日：2008-11-05

    申请号：EP06750268.2

    申请日：2006-04-13

    申请人： DOW GLOBAL TECHNOLOGIES INC.

    发明人： DEAVENPORT, Joseph L. ,  POSEY, Rhonda C. ,  WILSON, David A.

    IPC分类号： C07C215/40 ,  C07C213/08

    CPC分类号： C07C215/40 ,  C07C213/02

    摘要： Compositions and methods for making compositions including a quaternary trialkylammonium halide compound are described. Compositions follow the formula (I): wherein the R1 groups are each individually selected from alkyl groups having from 1 to 12 carbon atoms; wherein the R2, R3, and R4 groups are each individually selected from hydrogen, hydroxide, alkyl groups having from 1 to 12 carbon atoms, and hydroxy alkyl groups having from 1 to 12 carbon atoms; wherein y ranges from O to 12; wherein X- is selected from fluoride, chloride, bromide, and iodide; wherein the quaternary trialkylammonium compound is present in an amount of at least 90 wt. percent; and wherein the composition comprises not greater than 4000 ppm of a trialkylamine or protonated form thereof.

    摘要翻译： 描述了用于制备包含季三烷基卤化铵化合物的组合物和方法。 组合物遵循式（I）：其中R 1基团各自独立地选自具有1至12个碳原子的烷基; 其中R2，R3和R4基团各自选自氢，氢氧基，具有1至12个碳原子的烷基和具有1至12个碳原子的羟烷基; 其中y的范围从0到12; 其中X-选自氟化物，氯化物，溴化物和碘化物; 其中季三烷基铵化合物的存在量为至少90wt。 百分; 并且其中所述组合物包含不超过4000ppm的三烷基胺或其质子化形式。