公开(公告)号：US20130136794A1

公开(公告)日：2013-05-30

申请号：US13642298

申请日：2011-04-21

申请人： Runtao Li ,  Zemei Ge ,  Jingrong Cui ,  Xingyl Sun ,  Zhongqing Wang ,  Xu Yan

发明人： Runtao Li ,  Zemei Ge ,  Jingrong Cui ,  Xingyl Sun ,  Zhongqing Wang ,  Xu Yan

IPC分类号： C07D213/36 ,  C07D307/52 ,  C07F5/02 ,  C07D215/12 ,  C07D405/04 ,  C07D498/04 ,  C07D213/64 ,  C07D213/75 ,  C07D263/32 ,  C07D231/12 ,  C07D239/26 ,  C07D277/28 ,  C07D241/12 ,  C07D271/10 ,  C07D239/42 ,  C07D285/12 ,  C07D207/335 ,  C07D417/06

CPC分类号： C07D213/36 ,  C07D207/335 ,  C07D213/40 ,  C07D213/64 ,  C07D213/75 ,  C07D215/12 ,  C07D231/12 ,  C07D239/26 ,  C07D239/42 ,  C07D241/12 ,  C07D263/32 ,  C07D271/10 ,  C07D277/28 ,  C07D285/12 ,  C07D307/52 ,  C07D405/04 ,  C07D417/02 ,  C07D417/06 ,  C07D417/14 ,  C07D498/04 ,  C07F5/025

摘要： Heteroaryl(alkyl)dithiocarbamate compounds represented by general formula (I) or their pharmaceutically acceptable salts, their preparing methods, and their uses for preparing antitumor medicines are disclosed, wherein each said substituent is defined as in the description. The compounds are new tyrosine kinase inhibitors useful as an anti-tumor agents, preferably useful in the preparation of medicines for treating breast cancer, liver cancer, non-small cell lung cancer, gastric cancer, colon cancer, leukaemia or nasal cancer.

摘要翻译： 公开了通式（I）表示的杂芳基（烷基）二硫代氨基甲酸酯化合物或其药学上可接受的盐，其制备方法及其用于制备抗肿瘤药物的用途，其中每个所述取代基如说明书所述定义。 该化合物是可用作抗肿瘤剂的新的酪氨酸激酶抑制剂，优选用于制备用于治疗乳腺癌，肝癌，非小细胞肺癌，胃癌，结肠癌，白血病或鼻癌的药物。

公开(公告)号：US09303001B2

公开(公告)日：2016-04-05

申请号：US14119448

申请日：2012-07-19

申请人： Shouhua Zhang ,  Zhongqing Wang ,  Zhonghua Luo

发明人： Shouhua Zhang ,  Zhongqing Wang ,  Zhonghua Luo

IPC分类号： C07D257/04 ,  C07D319/06 ,  C07D405/12 ,  C07F7/18 ,  C07B53/00

CPC分类号： C07D257/04 ,  C07B53/00 ,  C07D319/06 ,  C07D405/12 ,  C07F7/1804

摘要： The present invention relates to the field of pharmaceutical chemistry, specifically relates to a statin intermediate having formula I and preparation thereof. The advantages of the method used to prepare the chiral sulfone intermediate having formula I are that a fluorophore is introduced at the beginning of the synthesis, and the intermediates are mostly solid, which enables quality control to be easily carried out.

摘要翻译： 本发明涉及药物化学领域，具体涉及具有式I及其制备的他汀类中间体。 用于制备具有式I的手性砜中间体的方法的优点是在合成开始时引入荧光团，并且中间体大多是固体，这使得能够容易地进行质量控制。

公开(公告)号：US20140155351A1

公开(公告)日：2014-06-05

申请号：US14123109

申请日：2012-06-21

申请人： Lijun Li ,  Hailong Wang ,  Zhongqing Wang

发明人： Lijun Li ,  Hailong Wang ,  Zhongqing Wang

IPC分类号： C07F7/18 ,  C07D495/04

CPC分类号： C07F7/188 ,  C07D495/04 ,  C07F7/1804

摘要： Disclosed herein are a process or method for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride. The process comprises preparation of prasugrel by acetylation in solvents which have low boiling point and/or low toxicity, and the process not only avoids using solvents which have high boiling point and/or high toxicity such as toluene, acetonitrile and so on, but also resolves the problem about thermal instability of prasugrel, and the loss of prasugrel is reduced, as well as the yield is raised. The yield of prasugrel is higher than 85% and the purity is higher than 99.5%. The process can prepare prasugrel and its pharmaceutically acceptable salts. The novel crystalline forms of prasugrel hydrochloride are crystalline form H1, H2 and H3, and their performance in oral absorbability, activating metabolism and inhibiting platelet aggregation is excellent. They have a low toxicity and good thermal stability, and are applicable to the preparation of a drug for preventing or treating diseases caused by thrombosis or embolism.

摘要翻译： 本文公开了制备普拉格雷和几种新型的普拉格雷盐酸盐结晶形式的方法或方法。 该方法包括通过在低沸点和/或低毒性的溶剂中乙酰化制备普拉格雷，并且该方法不仅避免使用具有高沸点和/或高毒性的溶剂如甲苯，乙腈等，而且还可以 解决普拉格雷热不稳定问题，降低普拉格雷的损失，提高产量。 普拉格雷的产量高于85％，纯度高于99.5％。 该方法可以制备普拉格雷及其药学上可接受的盐。 普拉格雷盐酸盐的新型结晶形式是H1，H2和H3结晶，口服吸收性能，活化代谢和抑制血小板聚集性能优异。 它们具有低毒性和良好的热稳定性，适用于预防或治疗由血栓形成或栓塞引起的疾病的药物的制备。

公开(公告)号：US08937053B2

公开(公告)日：2015-01-20

申请号：US14123109

申请日：2012-06-21

申请人： Lijun Li ,  Hailong Wang ,  Zhongqing Wang

发明人： Lijun Li ,  Hailong Wang ,  Zhongqing Wang

IPC分类号： C07D491/02 ,  A61K31/695 ,  C07F7/18 ,  C07D495/04

CPC分类号： C07F7/188 ,  C07D495/04 ,  C07F7/1804

摘要： Disclosed herein are a process or method for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride. The process comprises preparation of prasugrel by acetylation in solvents which have low boiling point and/or low toxicity, and the process not only avoids using solvents which have high boiling point and/or high toxicity such as toluene, acetonitrile and so on, but also resolves the problem about thermal instability of prasugrel, and the loss of prasugrel is reduced, as well as the yield is raised. The yield of prasugrel is higher than 85% and the purity is higher than 99.5%. The process can prepare prasugrel and its pharmaceutically acceptable salts. The novel crystalline forms of prasugrel hydrochloride are crystalline form H1, H2 and H3, and their performance in oral absorbability, activating metabolism and inhibiting platelet aggregation is excellent. They have a low toxicity and good thermal stability, and are applicable to the preparation of a drug for preventing or treating diseases caused by thrombosis or embolism.

摘要翻译： 本文公开了制备普拉格雷和几种新型的普拉格雷盐酸盐结晶形式的方法或方法。 该方法包括通过在低沸点和/或低毒性的溶剂中乙酰化制备普拉格雷，并且该方法不仅避免使用具有高沸点和/或高毒性的溶剂如甲苯，乙腈等，而且还 解决普拉格雷热不稳定问题，降低普拉格雷的损失，提高产量。 普拉格雷的产量高于85％，纯度高于99.5％。 该方法可以制备普拉格雷及其药学上可接受的盐。 普拉格雷盐酸盐的新型结晶形式是H1，H2和H3结晶，口服吸收，活化代谢和抑制血小板聚集性能优良。 它们具有低毒性和良好的热稳定性，适用于预防或治疗由血栓形成或栓塞引起的疾病的药物的制备。