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81. 发明申请

US20160244438A1 PROCESSES FOR PREPARING DIHYDROPYRIMIDINE DERIVATIVES AND INTERMEDIATES THEREOF 有权
标题翻译：制备二氢嘧啶衍生物的方法及其中间体
公开(公告)号：US20160244438A1
公开(公告)日：2016-08-25
申请号：US15024020
申请日：2014-11-27
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Qingyun REN , Xinchang LIU , Zhifu ZOU , Guanghua YAN , Mingchao BI , Siegfried GOLDMANN , Yingjun ZHANG
IPC分类号： C07D417/04 , C07D417/14
CPC分类号： C07D417/04 , C07D417/14
摘要： The present invention relates to processes for preparing a dihydropyrimidine derivative having Formula (I) or a tautomer thereof having Formula (Ia), as well as a intermediate thereof. The processes of the invention have simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.
摘要翻译：本发明涉及制备具有式（I）的二氢嘧啶衍生物或其具有式（Ia）的互变异构体的方法及其中间体。本发明方法操作简单，产品光学纯度高，产量高，加工方便，适用于工业生产。

82. 发明授权

US09309231B2 Bridged ring compounds as hepatitis C virus (HCV) inhibitors and pharmaceutical applications thereof 有权
标题翻译：桥连环化合物作为丙型肝炎病毒（HCV）抑制剂及其药物应用
公开(公告)号：US09309231B2
公开(公告)日：2016-04-12
申请号：US14397200
申请日：2013-08-05
申请人： SUNSHINE LAKE PHARMA CO., LTD
发明人： Yingjun Zhang , Jiancun Zhang , Hongming Xie , Qingyun Ren , Yumei Tan , Huichao Luo
IPC分类号： A61K31/4178 , C07D403/14 , C07D401/14 , C07D413/14 , C07D409/14 , C07D417/14 , C07D453/06 , C07D471/08 , C07D491/056 , C07D493/08 , C07D519/00 , A61K31/4184 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/5377 , A61K45/06 , C07D491/113 , C07D405/14
CPC分类号： C07D403/14 , A61K31/4178 , A61K31/4184 , A61K31/427 , A61K31/439 , A61K31/4545 , A61K31/5377 , A61K45/06 , C07D401/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D453/06 , C07D471/08 , C07D491/056 , C07D491/113 , C07D493/08 , C07D519/00
摘要： Provided herein is a compound having Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, which can be used for treating HCV infection or a HCV disorder. Also provided herein are pharmaceutical compositions comprising the compounds disclosed herein, which can be used for treating HCV infection or a HCV disorder.
摘要翻译：本文提供的是具有式（I）化合物或其立体异构体，几何异构体，互变异构体，N-氧化物，水合物，溶剂合物，代谢物，药学上可接受的盐或前药，其可用于治疗HCV感染或HCV病症。本文还提供了包含本文公开的化合物的药物组合物，其可用于治疗HCV感染或HCV病症。

83. 发明申请

US20160039838A1 AMINOQUINAZOLINE DERIVATIVES AND THEIR SALTS AND METHODS OF USE THEREOF 有权
标题翻译：氨基喹啉衍生物及其用途及其使用方法
公开(公告)号：US20160039838A1
公开(公告)日：2016-02-11
申请号：US14774702
申请日：2014-04-28
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Yingjun ZHANG , Bing LIU , Jinlei LIU , Jiancun ZHANG , Changchung CHENG
IPC分类号： C07D491/056 , C07D413/12 , A61K31/553 , C07D417/12 , A61K31/5415 , C07D498/04 , A61K31/5383 , A61K31/538 , C07D491/048 , C07D495/04 , C07D497/04 , C07D401/12 , C07D403/12 , C07D491/044 , C07D519/00 , A61K31/5377 , A61K33/24 , A61K31/7008 , A61K39/395 , A61K38/21 , A61K31/573 , A61K38/12 , A61K31/282 , A61K31/704 , A61K31/4545 , A61K31/337 , A61K31/517
CPC分类号： C07D491/056 , A61K31/196 , A61K31/198 , A61K31/255 , A61K31/282 , A61K31/337 , A61K31/4545 , A61K31/475 , A61K31/517 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/5415 , A61K31/553 , A61K31/573 , A61K31/675 , A61K31/7008 , A61K31/704 , A61K33/24 , A61K38/12 , A61K38/212 , A61K39/39558 , A61K2039/505 , C07D401/12 , C07D403/12 , C07D413/12 , C07D417/12 , C07D491/044 , C07D491/048 , C07D495/04 , C07D497/04 , C07D498/04 , C07D519/00 , A61K2300/00
摘要： Provided herein are aminoquinazoline compounds, salts and uses thereof. The compounds have Formula (I), or a stereoisomer, a geometric isomer, a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof. Also provided herein are pharmaceutical compositions containing the compounds disclosed herein, and uses of the compounds or the compositions for preventing, managing, treating or lessening the severity of a proliferative disorder in a patient and for modulating the protein tyrosine kinase activity.
摘要翻译：本文提供氨基喹唑啉化合物，其盐和用途。化合物具有式（I）或立体异构体，几何异构体，互变异构体，N-氧化物，水合物，溶剂合物，代谢物，药学上可接受的盐或前药。本文还提供含有本文公开的化合物的药物组合物，以及化合物或组合物用于预防，控制，治疗或减轻患者中增殖性疾病的严重性并调节蛋白酪氨酸激酶活性的用途。

84. 发明申请

US20150299215A1 SPIRO RING COMPOUND AS HEPATITIS C VIRUS (HCV) INHIBITOR AND USES THEREOF 有权
标题翻译：螺旋环化合物作为丙型肝炎病毒（HCV）抑制剂及其用途
公开(公告)号：US20150299215A1
公开(公告)日：2015-10-22
申请号：US14647445
申请日：2013-11-28
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Jiancun Zhang , Yingjun Zhang , Hongming Xie , Qingyun Ren , Bailin Hu , Changping Fu , Xiwei Wu , Shifeng Li , Chenglin Wang , Zhikeng Zhang
IPC分类号： C07D491/113 , A61K31/517 , C07D401/14 , A61K31/4709 , C07D491/107 , A61K45/06 , A61K31/549 , C07D405/14 , C07D409/14 , A61K31/435 , C07D413/14 , A61K31/423 , C07D403/14 , C07D417/14
CPC分类号： C07D491/113 , A61K31/4184 , A61K31/423 , A61K31/435 , A61K31/4709 , A61K31/517 , A61K31/527 , A61K31/549 , A61K38/2013 , A61K38/204 , A61K38/208 , A61K38/21 , A61K45/06 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14 , C07D413/14 , C07D417/14 , C07D491/107 , A61K2300/00
摘要： A compound of formula (I) or a stereoisomer, a geometric isomer. a tautomer, an N-oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof is provided, which can be used for treating HCV infection or a HCV disorder. Also a pharmaceutical composition comprising the compound and the use of the compound and the pharmaceutical composition thereof are provided, which can also be used for treating HCV infection or a HCV disorder.
摘要翻译：式（I）化合物或立体异构体，几何异构体。提供了可用于治疗HCV感染或HCV病症的互变异构体，N-氧化物，水合物，溶剂化物，代谢物，药学上可接受的盐或前药。还提供了包含该化合物的药物组合物和该化合物及其药物组合物的用途，其也可用于治疗HCV感染或HCV病症。

85. 发明申请

US20150152096A1 DIHYDROPYRIMIDINE COMPOUNDS AND THEIR APPLICATION IN PHARMACEUTICALS 有权
标题翻译：二氢咪嗪化合物及其在药物中的应用
公开(公告)号：US20150152096A1
公开(公告)日：2015-06-04
申请号：US14416061
申请日：2013-08-23
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Yingjun ZHANG , Qingyun REN , Xinchang LIU , Siegfried GOLDMANN
IPC分类号： C07D417/14 , A61K45/06 , C07D413/14 , A61K31/5377 , A61K31/506
CPC分类号： C07D417/14 , A61K31/505 , A61K31/506 , A61K31/5377 , A61K45/06 , C07D413/14 , A61K2300/00
摘要： Provided herein are dihydropyrimidine compounds and their pharmaceutical applications, especially for use in treating and preventing HBV diseases. Specifically, provided herein are compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof, wherein the variables of the formulas are as defined in the specification. Also provided herein is the use of the compounds having Formula (I) or (Ia), or an enantiomer, a diastereoisomer, a tautomer, a hydrate, a solvate, or a pharmaceutically acceptable salt thereof for treating and preventing HBV diseases.
摘要翻译：本文提供了二氢嘧啶化合物及其药物应用，特别是用于治疗和预防HBV疾病。具体地，本文提供了具有式（I）或（Ia）的化合物或其对映体，非对映异构体，互变异构体，水合物，溶剂合物或其药学上可接受的盐，其中式的变量如规范。本文还提供了具有式（I）或（Ia）的化合物或其对映体，非对映异构体，互变异构体，水合物，溶剂化物或其药学上可接受的盐在治疗和预防HBV疾病中的用途。

86. 发明申请

US20150141463A1 SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE 有权
公开(公告)号：US20150141463A1
公开(公告)日：2015-05-21
申请号：US14601207
申请日：2015-01-20
申请人： CALITOR SCIENCES, LLC , SUNSHINE LAKE PHARMA CO., LTD.
发明人： Ning Xi , Yanjun Wu , Min Liao , Yanming Feng
IPC分类号： A61K31/4439 , A61K31/444
CPC分类号： A61K31/4439 , A61K31/444 , A61K45/06 , C07D401/12 , C07D401/14 , A61K2300/00
摘要： The present invention provides novel substituted pyrazolone compounds, pharmaceutical acceptable salts and formulations thereof useful in modulating the protein tyrosine kinase activity, and in modulating cellular activities such as proliferation, differentiation, apoptosis, migration and invasion. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.

87. 发明授权

US08937053B2 Process for the preparation of prasugrel and several novel crystalline forms of prasugrel hydrochloride 有权
标题翻译：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
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。

88. 发明申请

US20140056849A1 SUBSTITUTED AZAINDOLE COMPOUNDS, SALTS, PHARMACEUTICAL COMPOSITIONS THEREOF AND METHODS OF USE 有权
标题翻译：取代的AZAINDOLE化合物，SALTS，药物组合物及其使用方法
公开(公告)号：US20140056849A1
公开(公告)日：2014-02-27
申请号：US13975371
申请日：2013-08-26
申请人： Sunshine Lake Pharma Co., Ltd. , Calitor Sciences, LLC
发明人： Ning Xi , Tingjin Wang , Yin Tang , Mingming Sun , Qian Wang
IPC分类号： C07D471/04 , A61K45/06 , A61K31/437
CPC分类号： C07D471/04 , A61K31/437 , A61K45/06 , A61K2300/00
摘要： The present invention provides substituted azaindole prodrugs, methods of making said prodrugs, pharmaceutical compositions of said prodrugs and methods of using said prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer.
摘要翻译：本发明提供取代的氮杂吲哚前药，制备所述前药的方法，所述前药的药物组合物和使用所述前药的方法及其药物组合物治疗或预防疾病或病症如癌症。

89. 发明授权

US08426585B2 Compounds comprising a spiro-ring 有权
标题翻译：包含螺环的化合物
公开(公告)号：US08426585B2
公开(公告)日：2013-04-23
申请号：US13587936
申请日：2012-08-17
申请人： Ning Xi
发明人： Ning Xi
IPC分类号： A61P35/04 , C07D403/14 , C07D413/14 , C07D471/04
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D471/04 , C07D491/107 , C07D493/10 , C07D495/04 , C07D498/04 , C07D519/00
摘要： The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
摘要翻译：本发明提供了可用于调节蛋白酪氨酸激酶活性和调节细胞间和/或细胞内信号传导的新化合物。本发明还提供包含这些化合物的药学上可接受的组合物和使用该组合物治疗哺乳动物，特别是人类中过度增殖性疾病的方法。

90. 发明申请

US20120315247A1 COMPOUNDS COMPRISING A SPIRO-RING AND METHODS OF USE 有权
标题翻译：包含螺旋环的化合物及其使用方法
公开(公告)号：US20120315247A1
公开(公告)日：2012-12-13
申请号：US13587936
申请日：2012-08-17
申请人： Ning Xi
发明人： Ning Xi
IPC分类号： A61K31/4709 , C07D401/12 , A61K31/704 , A61K31/664 , A61K31/573 , A61K31/7048 , A61K31/513 , A61K31/506 , A61K31/517 , A61K31/5377 , A61K38/21 , A61K31/4745 , A61K39/395 , A61K31/4995 , A61P35/00 , A61P9/10 , A61P35/04 , C12N9/99 , C07D401/14
CPC分类号： A61K31/437 , A61K31/444 , A61K31/4709 , A61K31/5377 , A61K45/06 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D413/14 , C07D471/04 , C07D491/107 , C07D493/10 , C07D495/04 , C07D498/04 , C07D519/00
摘要： The present invention provides novel compounds useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
摘要翻译：本发明提供了可用于调节蛋白酪氨酸激酶活性和调节细胞间和/或细胞内信号传导的新化合物。本发明还提供包含这些化合物的药学上可接受的组合物和使用该组合物治疗哺乳动物，特别是人类中过度增殖性疾病的方法。

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