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122 条记录 (耗时 0.025 秒)

    Crystal forms of azetidinone compounds and preparing methods thereof
    55.
    发明授权
    Crystal forms of azetidinone compounds and preparing methods thereof 有权
    氮杂环丁酮化合物的结晶形式及其制备方法

    公开(公告)号：US09567298B2

    公开(公告)日：2017-02-14

    申请号：US14426085

    申请日：2013-09-05

    申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

    发明人： Hongyuan Wei ,  Chongjun Liu ,  Xuyang Zhao ,  Xiaojie Xu ,  Hua Bai ,  Yuncai Zhang

    IPC分类号： C07D205/08 ,  A61K31/397

    CPC分类号： C07D205/08 ,  A61K31/397 ,  C07B2200/13

    摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.

    摘要翻译： 本发明提供（3R，4S）-4-（4-羟基苯基）-3- [3-（4-氟苯基）-4-羟基丁-2（Z） - 烯基] -1-（ 4-氟苯基）-2-氮杂环丁酮（式A）。 可以通过X射线粉末衍射（XRPD）光谱，差示扫描量热法（DSC）光谱，红外吸收光谱等来表征晶体形态。 同时，本发明还提供了制备式A化合物的结晶形式的方法，药物组合物及其用途。

    4-((substituted phenyl) difluoromethyl) phenoxy carboxylic acid derivative, and preparation method and uses thereof
    56.
    发明授权
    4-((substituted phenyl) difluoromethyl) phenoxy carboxylic acid derivative, and preparation method and uses thereof 有权
    4 - （（取代苯基）二氟甲基）苯氧基羧酸衍生物及其制备方法和用途

    公开(公告)号：US09487470B2

    公开(公告)日：2016-11-08

    申请号：US14396455

    申请日：2013-04-25

    申请人： Zhejiang Hisun Pharmaceutical Co., Ltd.

    发明人： Hua Bai ,  Jian Hong ,  Lifeng Cai ,  Hegeng Wei ,  Xiaoyu Liu ,  Xiaohe Zheng

    IPC分类号： C07C69/712 ,  C07C59/68 ,  C07C51/363 ,  C07C59/135 ,  C07C67/307 ,  C07C69/78 ,  C07C319/16 ,  C07C323/16 ,  C07C323/56 ,  C07D307/33 ,  C07C69/94

    CPC分类号： C07C69/712 ,  C07C51/363 ,  C07C59/135 ,  C07C59/68 ,  C07C67/307 ,  C07C69/78 ,  C07C69/94 ,  C07C319/16 ,  C07C323/16 ,  C07C323/56 ,  C07D307/33

    摘要： The present invention discloses a 4-((substituted phenyl)difluoromethyl)phenoxycarboxylic acid derivative and preparation process and use thereof. More specifically, the present invention relates to a compound of the following formula I, which is defined in the specification. The compounds according to the present invention can be used as PPAR agonists, and demonstrates a strong effect on reducing the levels of total cholesterol (TC), triglyceride (TG), and low density lipoprotein cholesterol (LDL-C) in blood plasma, and thus the compound according to the present invention can be used in the preparation of a medicament for treating or preventing hyperlipoidemia or cardio-cerebrovascular diseases caused by hyperlipoidemia, such as diabetes, atherosclerosis, stroke, coronary heart disease, etc. The present invention also relates to a novel intermediate compound for the preparation of the compound of formula I and preparation method thereof.

    摘要翻译： 本发明公开了4 - （（取代苯基）二氟甲基）苯氧基羧酸衍生物及其制备方法和用途。 更具体地，本发明涉及在说明书中定义的下式I的化合物。 根据本发明的化合物可用作PPAR激动剂，并且对降低血浆中总胆固醇（TC），甘油三酯（TG）和低密度脂蛋白胆固醇（LDL-C）的水平具有很强的作用， 因此根据本发明的化合物可用于制备用于治疗或预防高脂血症引起的高脂血症或心脑血管疾病如糖尿病，动脉粥样硬化，中风，冠心病等的药物。本发明还涉及 涉及用于制备式I化合物的新型中间体化合物及其制备方法。

    TARGETING THYMIDINE KINASE PHOTOSENSITIZER AND PHARMACEUTICAL COMPOSITION AND USE FOR CANCER TREATMENT THEREOF
    57.
    发明申请
    TARGETING THYMIDINE KINASE PHOTOSENSITIZER AND PHARMACEUTICAL COMPOSITION AND USE FOR CANCER TREATMENT THEREOF 有权
    靶向噻霉素激酶和药物组合物，并用于癌症治疗

    公开(公告)号：US20160151494A1

    公开(公告)日：2016-06-02

    申请号：US14434102

    申请日：2012-11-02

    申请人： ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

    发明人： RAVINDRA K PANDEY ,  YIHUI CHEN ,  HUA BAI ,  ZHENLIANG CHEN

    IPC分类号： A61K41/00 ,  A61K31/337 ,  A61K47/48

    CPC分类号： A61K41/0057 ,  A61K31/337 ,  A61K31/706 ,  A61K31/7064 ,  A61K31/7068 ,  A61K31/7072 ,  A61K41/0071 ,  A61K47/545 ,  A61K47/546 ,  A61K47/549 ,  A61K49/0036 ,  C07D487/22

    摘要： A targeting thymidine kinase photosensitizer and pharmaceutical composition and use for cancer treatment thereof is provided, which improves the selectivity of photosensitizers to tumor cells, has better tolerance, can reach maximum blood concentration in 24 hours, has a bigger conjugated system, a longer absorption wavelength and an advantage in treating depth tumors; the wavelength area does not need to consume much energy of a light-output device and even LEDs can be used, which render PDT more practical and economical. The targeting thymidine kinase photosensitizer can be used for diagnosis and for treating prostatic carcinoma via the guidance of fluorescence imaging. The pharmaceutical composition uses a combination of a chemotherapeutic agent and the targeting thymidine kinase photosensitizer, which further improves the therapeutic effect of the PDT method, expands the application range for tumors and has good effects on metastatic tumors as well.

    摘要翻译： 提供靶向胸苷激酶光敏剂及其药物组合物及其治疗用途，提高光敏剂对肿瘤细胞的选择性，具有更好的耐受性，24小时内可达到最大血药浓度，具有较大的共轭体系，较长的吸收波长 治疗深部肿瘤有优势; 波长区域不需要消耗光输出装置的大量能量，甚至可以使用LED，这使得PDT更实用和经济。 靶向胸苷激酶光敏剂可用于诊断和通过荧光成像的指导治疗前列腺癌。 药物组合物采用化疗剂与靶向胸苷激酶光敏剂的组合，进一步提高了PDT法的治疗效果，扩大了肿瘤的应用范围，对转移性肿瘤也有很好的疗效。

    Method for Preparing Epirubicin and Intermediate Thereof
    58.
    发明申请
    Method for Preparing Epirubicin and Intermediate Thereof 有权
    制备表柔比星及其中间体的方法

    公开(公告)号：US20160137683A1

    公开(公告)日：2016-05-19

    申请号：US14900921

    申请日：2013-07-02

    申请人： ZHEJIANG HISUN PHARMACEUTICAL CO., LTD

    发明人： Wei Yan ,  Wanzeng Tong ,  Jianping Wang ,  Weiqiang Yang ,  Hongguan Qian

    IPC分类号： C07H15/252

    CPC分类号： C07H15/252

    摘要： The present invention provides a method for preparing epirubicin and an intermediate adaptive to the method. The preparation method may include: reacting tert-Butyldimethylsilyl chloride with N-trifluoroacetyl adriamycin to obtain a first compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl adriamycin; oxidizing the first compound to obtain a second compound 4′-ketone-N-trifluoroacetyl-14-O-tert-Butyldimethylsilyladriamycin; reducing the second compound to obtain a third compound N-trifluoroacetyl-14-O-tert-Butyldimethylsilyl epirubicin; and performing deprotection and hydrolysis reactions on the third compound to obtain epirubicin. The method of the present invention needs low cost, fewer reaction steps, provides high yield and high product purity, and avoids serious pollution caused by a bromination reaction in a conventional method.

    摘要翻译： 本发明提供了一种制备表柔比星的方法和适用于该方法的中间体。 制备方法可包括：使叔丁基二甲基甲硅烷基氯与N-三氟乙酰基阿霉素反应，得到第一种化合物N-三氟乙酰基-14-O-叔丁基二甲基甲硅烷基阿霉素; 氧化第一化合物以获得第二化合物4'-酮-N-三氟乙酰基-14-O-叔丁基二甲基甲硅烷基阿霉素; 还原第二化合物以获得第三化合物N-三氟乙酰基-14-O-叔丁基二甲基甲硅烷基表柔比星; 并对第三种化合物进行去保护和水解反应，得到表柔比星。 本发明的方法需要低成本，较少的反应步骤，提供高产率和高产品纯度，并且避免了常规方法中溴化反应引起的严重污染。