MONOSUBSTITUTED OR POLYSUBSTITUTED AMPHIPHILIC HYPOCRELLIN DERIVATIVE, PREPARATION METHOD THEREFOR, AND USES THEREOF
    3.
    发明申请
    MONOSUBSTITUTED OR POLYSUBSTITUTED AMPHIPHILIC HYPOCRELLIN DERIVATIVE, PREPARATION METHOD THEREFOR, AND USES THEREOF 审中-公开
    单取代或多取代的两性羟基链甾醇衍生物,其制备方法及其用途

    公开(公告)号:WO2017067497A3

    公开(公告)日:2017-08-24

    申请号:PCT/CN2016102832

    申请日:2016-10-21

    Abstract: Disclosed are a monosubstituted or polysubstituted amphiphilic hypocrellin derivative, preparation method therefor, and uses thereof. In the present invention, the amphiphilic hypocrellin derivative having substituted functional groups such as condensed ethylene glycol and quaternary ammonium salt shows in its absorption spectrum a substantial redshift and an enhanced molar extinction coefficient compared to hypocrellin precursor, and can highly effectively produce reactive oxygen species such as singlet state oxygen under light-sensitive conditions. By adjusting the hydrophobicity and hydrophilicity of said derivative, said derivative can have different amphiphilicity and enhanced biocompatibility with cells or tissues. The amphiphilic hypocrellin derivative can satisfy the requirements for different clinical medications and addresses the conflict between medicinal hydrophilicity and lipophilicity caused by different administration methods. Compared to the first and second generation commercial photosensitizer, under the same conditions, the amphiphilic hypocrellin derivative photosensitizer of the present invention has higher photodynamic capabilities in the eradication of live tumor cells.

    Abstract translation: 公开了单取代或多取代的两亲性竹红菌素衍生物,其制备方法及其用途。 在本发明中,具有取代的官能团例如缩合乙二醇和季铵盐的两亲性竹红菌素衍生物在其吸收光谱中显示出与竹红菌素前体相比显着的红移和增强的摩尔消光系数,并且可以高度有效地产生活性氧种类,例如 作为单态氧在光敏条件下。 通过调节所述衍生物的疏水性和亲水性,所述衍生物可具有不同的两亲性和增强的与细胞或组织的生物相容性。 两亲性竹红菌素衍生物可以满足不同临床药物的需要,解决了不同给药方式引起药物亲水性与亲脂性之间的矛盾。 与第一代和第二代商业光敏剂相比,在相同条件下,本发明的两亲性竹红菌素衍生物光敏剂在根除活肿瘤细胞中具有较高的光动力学能力。

    PREPARATION OF THIOALKYLAMINES WITH HIGH YIELDS
    8.
    发明申请
    PREPARATION OF THIOALKYLAMINES WITH HIGH YIELDS 审中-公开
    用高效液相色谱法制备

    公开(公告)号:WO2007022900A1

    公开(公告)日:2007-03-01

    申请号:PCT/EP2006/008060

    申请日:2006-08-16

    Inventor: PAZENOK, Sergiy

    CPC classification number: C07C303/24 C07C319/14 C07C305/06 C07C323/25

    Abstract: The present invention relates to a novel process for the preparation of compounds of the formula (I) by mixing in a first step amino alcohols of the formula (II) with sulfuric acid to yield the salt, by then reacting them in a second step in a drying device to give sulfuric acid esters of the general formula (III) and by reacting these sulfuric acid esters in a third step with mercaptans or salts thereof of the general formula (IV): RSM in each formula, where applicable, R 1 , R 2 , R 3 , R 4 , R 5 , R 6 , R, n and M have the meanings given in the description, in the presence of a diluent and in the presence of a base.

    Abstract translation: 本发明涉及一种制备式(I)化合物的新方法,其通过在第一步骤中将式(II)的氨基醇与硫酸混合以产生盐,然后在第二步中将其反应 干燥装置,得到通式(III)的硫酸酯,并通过第三步骤中的这些硫酸酯与通式(IV)的硫醇或其盐反应:各式中的RSM(如适用)R 6,R,n和M具有在描述中给出的含义,在稀释剂的存在下和在碱的存在下。

    ORGANIC NITRIC OXIDE ENHANCING SALTS OF CYCLOOXYGENASE-2 SELECTIVE INHIBITORS, COMPOSITONS AND METHODS OF USE

    公开(公告)号:WO2007016136A3

    公开(公告)日:2007-02-08

    申请号:PCT/US2006/028952

    申请日:2006-07-27

    Abstract: The invention describes compositions and kits comprising organic nitric oxide enhancing salts of cyclooxygenase 2 (COX-2) selective inhibitors, and compositions comprising at least one organic nitric oxide enhancing salt of a COX-2 selective inhibitor, and, optionally, at least one nitric oxide enhancing compound and/or at least one therapeutic agent. The invention also provides methods for (a) treating inflammation, pain and fever; (b) treating gastrointestinal disorders and/or improving the gastrointestinal properties of COX-2 selective inhibitors; (c) facilitating wound healing; (d) treating renal and/or respiratory toxicities; (e) treating disorders resulting from elevated levels of cyclooxygenase-2; (f) improving the cardiovascular profile of COX-2 selective inhibitors; (g) treating diseases resulting from oxidative stress; (h) treating endothelial dysfunctions; (j) treating diseases caused by endothelial dysfunctions; (k) treating inflammatory disease states and/or disorders; (1) treating ophthalmic disorders; and (m) treating peripheral vascular diseases. The organic nitric oxide enhancing compounds that form salts with the COX-2 selective inhibitor are organic nitrates, organic nitrites, nitrosothiols, thionitrites, thionitrates, NONOates, heterocyclic nitric oxide donors and/or nitroxides. The heterocyclic nitric oxide donors are furoxans, sydnonimines, oxatriazole-5-ones and/or oxatriazole-5-imines. The organic nitric oxide enhancing salts of cyclooxygenase 2 selective inhibitors of the invention are organic nitric oxide enhancing salts of 2(2-((2-chloro-6-fluorophenyl) amino)5- methylphenyl)acetic acid derivatives.

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