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91.发明公开
公开(公告)号：EP3225619A1
公开(公告)日：2017-10-04
申请号：EP15863532.6
申请日：2015-11-18
申请人： Shanghai Institute Of Materia Medica Chinese Academy of Sciences , Guangzhou Institute Of Biomedicine And Health, Chinese Academy Of Sciences
发明人： DING, Ke , DING, Jian , CHAN, Shingpan , GENG, Meiyu , REN, Xiaomei , XIE, Hua , TU, Zhengchao , CHEN, Yi
IPC分类号： C07D239/48 , C07D401/02 , C07D403/12 , C07D239/47 , A61K31/505 , A61K31/506 , A61K31/5377 , A61P35/00 , A61P35/02
CPC分类号： C07D403/12 , A61K31/4523 , A61K31/505 , A61K31/506 , A61K31/53 , A61K31/5377 , A61K31/551 , C07D239/47 , C07D239/48 , C07D401/02 , C07D401/12
摘要： Disclosed are a 2-aminopyrimidine compound and pharmaceutical composition and use thereof. The structure of the 2-aminopyrimidine compound is as represented by formula I, in the formula, R 1 , R 2 , R 3 , R 4 , R 5 , X, Y, Z, W, (i) being as defined in the specification and the claims. Such compounds effectively inhibit the growth of a variety of tumor cells and have inhibitory effects on EGFR and IGF1R protease, and can be used for preparing antineoplastic drugs and overcome the tolerance induced by the existing drugs such as gefitinib, erlotinib and the like. The compound has selectivity for tumors, in particular the wild-type non-small cell lung cancer and have good pharmacokinetic characteristics.
摘要翻译： 公开了2-氨基嘧啶化合物和药物组合物及其用途。 2-氨基嘧啶化合物的结构如式I所示，在结构式中，R 1，R 2，R 3，R 4，R 5，X，Y，Z，W，（i）如说明书和权利要求书中所定义。 这类化合物能有效抑制多种肿瘤细胞的生长，对EGFR和IGF1R蛋白酶具有抑制作用，可用于制备抗肿瘤药物，克服现有药物如吉非替尼，厄洛替尼等引起的耐受性。 该化合物对肿瘤具有选择性，特别是野生型非小细胞肺癌，并具有良好的药代动力学特征。
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公开(公告)号：EP3224248A1
公开(公告)日：2017-10-04
申请号：EP15855878.3
申请日：2015-11-01
申请人： Shanghai Fochon Pharmaceutical Co. Ltd , Shanghai Institute Of Materia Medica Chinese Academy of Sciences , Chongqing Fochon Pharmaceutical Co., Ltd.
发明人： ZHAO, Xingdong , LI, Tongshuang , ZHOU, Zuwen , CHEN, Ling , LIU, Qihong , WANG, Xianlong , YANG, Lijun , RONG, Yue , TAN, Rui , YU, Chuiliang , JIANG, Lihua , LIU, Yanxin , LINGHU, Li , SUN, Jing , WANG, Weibo , DING, Jian , MENG, Linghua , GENG, Meiyu
IPC分类号： C07D221/04 , C07D221/00 , C07D513/04 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61P43/00 , A61P35/00
CPC分类号： A61K31/437 , A61K31/4375 , A61K31/505 , A61K31/52 , A61K45/06 , C07D519/00 , A61K2300/00
摘要： Provided are certain PI3K inhibitors, pharmaceutical compositions thereof, and methods of use therefor.
摘要翻译： 提供了某些PI3K抑制剂，其药物组合物及其使用方法。
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公开(公告)号：EP3127903B1
公开(公告)日：2017-08-23
申请号：EP15774232.1
申请日：2015-03-27
发明人： NAN, Fajun , LI, Jia , XIE, Xin , GONG, Chaojun , ZHOU, Yubo , CHAI, Hui , ZHANG, Yangming , SU, Mingbo
IPC分类号： C07D277/56 , C07D277/60 , C07D417/04 , A61K31/428 , A61K31/427 , A61P37/02 , A61P35/00 , A61P35/02
CPC分类号： C07D277/56 , C07D277/60 , C07D277/66 , C07D417/04 , C07D417/14
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公开(公告)号：EP2501381B1
公开(公告)日：2017-07-26
申请号：EP10832058.1
申请日：2010-11-16
申请人： Huya Bioscience International LLC , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： ELLIOT, Gary, T. , WANG, Yiping , BAI, Donglu
IPC分类号： A61K31/4025 , A61K31/402 , A61K31/40 , A61K9/22 , A61K9/20 , A61K9/08 , A61P9/00 , A61P9/06 , A61K31/18
CPC分类号： A61K31/4025 , A61K31/18 , A61P9/00 , A61P9/06
摘要： Atrial fibrillation (AF) can be treated or prevented by administering to a subject who suffers from or is at risk of suffering from AF a composition comprised of an amount of an active agent, which is 4-methoxy-N-(3,5-bis(1-pyrrolidinyl)-4-hydroxy benzyl)benzene sulfonamide (sulcardine) or a pharmaceutically acceptable salt thereof, such that the Cmax value the active agent in the subject is in the range from about 1 muM to about 20 muM.
摘要翻译： 通过给患有或有患AF风险的受试者施用由一定量的活性剂组成的组合物来治疗或预防心房纤维性颤动（AF），所述活性剂是4-甲氧基-N-（3,5-二 - （1-吡咯烷基）-4-羟基苄基）苯磺酰胺（磺草胺）或其药学上可接受的盐，使得受试者中活性剂的C max值在约1μM至约20μM的范围内。
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95.发明公开GLECHOMA LONGITUBE EXTRACT, PREPARATION METHOD FOR SAME, AND USE THEREOF IN SUGAR REDUCTION, WEIGHT LOSS, AND LIPID REDUCTION 审中-公开GLECHOMA LONGTUBE提取物及其制备方法及其在减少糖，重量损失和脂质减少中的应用
公开(公告)号：EP3120847A1
公开(公告)日：2017-01-25
申请号：EP15765481.5
申请日：2015-03-17
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Nanjing Pailexing Pharmaceutical Technology Ltd.
发明人： ZHU, Weiliang , WANG, Heyao , ZHANG, Yong , SUN, Peng , LI, Bo , XU, Zhijian , JIANG, Hualiang , CHEN, Kaixian
CPC分类号： A61K31/7048 , A61K36/53 , A61K2236/30 , A61K2236/53
摘要： Disclosed is a Glechoma longituba (Nakai) Kupr . extract, specifically compounds I and II, a preparation method for same, and a use thereof in preparing a medicament for blood glucose decease, blood lipids decrease, weight loss, and kidney disease treatment or a method for treatment of said diseases, and a composition containing the extract.
摘要翻译： 披露是一种Glechoma longituba（Nakai）Kupr。 提取物，特别是化合物I和II，其制备方法，以及其在制备用于血糖降低，血脂降低，体重减轻和肾脏疾病治疗的药物中的用途或用于治疗所述疾病的方法， 含有提取物。
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96.发明授权NOVEL COMPOUND AS KCNQ POTASSIUM CHANNEL AGONIST, PREPARATION METHOD THEREFOR AND USE THEREOF 有权新的连接AS KCNQ KALIUMKANALAGONIST，其制造方法相同，它们的用途
公开(公告)号：EP2772481B1
公开(公告)日：2017-01-18
申请号：EP12843367.9
申请日：2012-10-23
发明人： NAN, Fajun , LI, Min , GAO, Zhaobing , CHEN, Fei , ZHANG, Yangming , ZHOU, Pingzheng , HU, Haining , XU, Haiyan , LIU, Sheng
IPC分类号： C07C271/28 , C07C269/04 , C07C233/43 , C07C231/02 , C07D235/26 , A61K31/27 , A61K31/167 , A61K31/4184 , A61P25/08 , A61P25/04 , A61P25/28 , A61P25/00 , A61P9/10
CPC分类号： C07C271/28 , C07C231/00 , C07C233/43 , C07C233/44 , C07C269/04 , C07C2601/16 , C07D235/26
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97.发明授权2-ARYLBENZOFURAN-7-FORMAMIDE COMPOUNDS, PREPARATION METHOD AND USE THEREOF 有权2-芳基苯并呋喃-7-甲酰胺，其制造方法及其用途
公开(公告)号：EP2813495B1
公开(公告)日：2016-09-28
申请号：EP13746724.7
申请日：2013-01-14
申请人： Shanghai Institute of Materia Medica, Chinese Academy of Sciences , Cisen Pharmaceutical Co., Ltd.
发明人： YANG, Chunhao , MIAO, Zehong , DING, Jian , WANG, Meng , HE, Jinxue , TAN, Cun , CHEN, Yi
IPC分类号： C07D307/81 , C07D405/04 , C07D405/12 , A61P35/00 , A61P29/00
CPC分类号： C07D307/81 , C07C67/08 , C07C67/307 , C07D405/04 , C07D405/12 , C07D407/12
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98.发明公开METHODS FOR PREPARING BREXPIPRAZOLE, KEY INTERMEDIATES THEREOF AND SALTS THEREOF 审中-公开用于生产BREXPIPRAZOL，KEY其中间体及其盐
公开(公告)号：EP3059237A1
公开(公告)日：2016-08-24
申请号：EP14854084.2
申请日：2014-10-20
申请人： Suzhou Vigonvita Life Sciences Co. Ltd. , Topharman Shanghai Co., Ltd. , Shanghai Institute Of Materia Medica Chinese Academy of Sciences
发明人： LIU, Zheng , WU, Chunhui , LIU, Yongjian , ZHANG, Rongxia , HE, Yang , TIAN, Guanghui , SHEN, Jingshan
IPC分类号： C07D409/12 , C07D333/70
CPC分类号： C07D409/12 , C07D333/54 , C07D333/70
摘要： The present invention relates to the methods for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, specifically, the present invention relates to a new method for preparing brexpiprazole, the analogs, key intermediates, and salts thereof, and the key intermediates, and salts thereof provided during the preparation. The preparation method has a mild reaction condition, stable intermediate, easy operation, and uses cheap and easy-to-get reagents, thus it saves the synthesis cost, shortens the production cycle, improves the yield and product quality, and is suitable for mass production.
摘要翻译： 本发明涉及一种用于制备brexpiprazole，所述类似物，关键中间体的方法，以及它们的盐，具体地，本发明涉及一种新的方法用于制备brexpiprazole，所述类似物，关键的中间体，以及它们的盐，以及关键中间体， 和盐在制备过程中它们提供。 该制备方法具有反应条件温和，稳定的中间，容易操作，并且使用便宜和容易获得的试剂，从而节省了合成成本，缩短生产周期，提高产量和产品质量，并且是适合于大规模 生产。
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公开(公告)号：EP3049089A1
公开(公告)日：2016-08-03
申请号：EP14849674.8
申请日：2014-09-25
申请人： Van Andel Research Institute , Shanghai Institute of Materia Medica, Chinese Academy of Sciences
发明人： XU, Huaqiang, Eric , HE, Yuanzheng , MELCHER, Karsten , YI, Wei , SHI, Jingjing
CPC分类号： C07J71/0047 , C07J3/005 , C07J5/0053
摘要： The present invention relates to novel glucocorticoid compounds. The invention also relates to methods of using these compounds, the synthesis of these compounds, and to compositions and formulations comprising the glucocorticoid compounds, and uses thereof.
摘要翻译： 本发明涉及新型糖皮质激素化合物。 本发明还涉及使用这些化合物的方法，这些化合物的合成，以及包含糖皮质激素化合物的组合物和制剂及其用途。
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100.发明公开DIARYL[A, G]QUINOLIZIDINE COMPOUND, PREPARATION METHOD THEREFOR, PHARMACEUTICAL COMPOSITION, AND USES THEREOF 审中-公开二芳基[A，G]喹啉化合物，其制备方法，药物组合物及其用途
公开(公告)号：EP2848617A1
公开(公告)日：2015-03-18
申请号：EP13787305.5
申请日：2013-05-09
发明人： LIU, Hong , ZHEN, Xuechu , SUN, Haifeng , ZHU, Liyuan , QIAN, Wangke , YU, Leiping , LI, Zeng , ZHOU, Shengbin , CAI, Wenxian , JIANG, Hualiang , CHEN, Kaixian
IPC分类号： C07D455/03 , A61K31/4375 , A61P25/00 , A61P25/18
CPC分类号： C07D471/14 , C07D455/03 , C07D491/147 , C07D491/22 , C07D495/14 , C07D495/22
摘要： The present invention relates to a diarylo[a,g]quinolizidine compound of formula (I), enantiomer, diastereoisomer, racemate, mixture, pharmaceutically acceptable salt, crystalline hydrate or solvate thereof; the preparation method thereof, and uses thereof in preparing an experimental model drugs related to dopamine receptors and 5-HT receptors or a medicament for treating or preventing a disease related to dopamine receptors and 5-HT receptors.
摘要翻译： 本发明涉及式（I）的二芳基[a，g]喹唑啉化合物，其对映体，非对映异构体，外消旋体，混合物，药学上可接受的盐，结晶水合物或溶剂化物; 其制备方法及其在制备与多巴胺受体和5-HT受体有关的实验模型药物或用于治疗或预防与多巴胺受体和5-HT受体有关的疾病的药物中的用途。
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