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31. 发明授权

US09617252B2 Processes for preparing dihydropyrimidine derivatives and intermediates thereof 有权
公开(公告)号：US09617252B2
公开(公告)日：2017-04-11
申请号：US15023676
申请日：2014-11-27
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Xinchang Liu , Qingyun Ren , Zhifu Zou , Jinsheng Liang , Linjin Tu , 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 refers to processes for preparing a dihydropyrimidine compound having Formula (I), or a tautomer thereof having Formula (1a), as well as a intermediate thereof. The process of the invention has simple operation, high optical purity of product, high yield and convenient work-up, which is suitable for industrial production.

32. 发明授权

US09598401B2 Substituted heteroaryl compounds and methods of use thereof 有权
公开(公告)号：US09598401B2
公开(公告)日：2017-03-21
申请号：US14787774
申请日：2014-07-28
申请人： Sunshine Lake Pharma Co., Ltd.
发明人： Yingjun Zhang , Chuanfei Jin , Rongqi Zhou
IPC分类号： A61K31/506 , C07D403/12 , A61K31/496 , C07D417/12 , A61K45/06 , C07D403/14 , C07D417/14
CPC分类号： C07D403/12 , A61K31/496 , A61K31/506 , A61K45/06 , C07D403/14 , C07D417/12 , C07D417/14 , A61K2300/00
摘要： Provided herein are novel heteroaryl compounds, pharmaceutically acceptable salts and pharmaceutical formulations thereof for selectively inhibiting serotonin reuptake and/or acting as 5-HT1A receptor agonists. Also provided herein are pharmaceutical compositions comprising the heteroaryl compounds and methods of using the pharmaceutical compositions in treating central nervous system (CNS) dysfunction in a mammal, especially a human being.

33. 发明授权

US09556191B2 Aminoquinazoline derivatives and their salts and methods of use thereof 有权
标题翻译：氨基喹唑啉衍生物及其盐及其使用方法
公开(公告)号：US09556191B2
公开(公告)日：2017-01-31
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： A01N43/54 , A61K31/517 , C07D239/72 , C07D491/056 , A61K31/5415 , A61K31/553 , C07D413/12 , C07D417/12 , C07D403/12 , C07D401/12 , C07D495/04 , C07D497/04 , C07D498/04 , C07D519/00 , A61K31/196 , A61K31/198 , A61K31/255 , A61K31/475 , A61K31/675 , A61K31/282 , A61K31/337 , A61K31/4545 , A61K31/5377 , A61K31/538 , A61K31/5383 , A61K31/573 , A61K31/7008 , A61K31/704 , A61K33/24 , A61K38/12 , A61K38/21 , A61K39/395 , C07D491/044 , C07D491/048 , A61K39/00
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。

34. 发明授权

US09434695B2 Nitrogenous heterocyclic derivatives and their application in drugs 有权
标题翻译：氮杂环衍生物及其在药物中的应用
公开(公告)号：US09434695B2
公开(公告)日：2016-09-06
申请号：US14396754
申请日：2013-07-18
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Yingjun Zhang , Jiancun Zhang , Xiaojun Wang , Runfeng Lin , Shengtian Cao , Zhaohe Wang , Jing Li
IPC分类号： C07D239/36 , C07D403/12 , C07D401/12 , C07D403/06 , C07D405/12 , C07D417/04 , C07D498/04 , C07D213/64
CPC分类号： C07D239/36 , C07D213/64 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07D417/04 , C07D498/04
摘要： The present invention relates to the field of medicine, provided herein are novel nitrogenous heterocyclic compounds, their preparation methods and their uses as drugs, especially for treatment and prevention of tissue fibrosis. Also provided herein are pharmaceutically acceptable compositions comprising the nitrogenous heterocyclic compounds and the uses of the compositions in the treatment of human or animal tissue fibrosis, especially for human or animal renal interstitial fibrosis, glomerular sclerosis, liver fibrosis, pulmonary fibrosis, peritoneal fibrosis, myocardial fibrosis, dermatofibrosis, postsurgical adhesion, benign prostatic hyperplasia, skeletal muscle fibrosis, scleroderma, multiple sclerosis, pancreatic fibrosis, cirrhosis, myosarcoma, neurofibroma, pulmonary interstitial fibrosis, diabetic nephropathy, alzheimer disease or vascular fibrosis.

35. 发明授权

US09403801B2 Substituted heteroaryl compounds and methods of use 有权
公开(公告)号：US09403801B2
公开(公告)日：2016-08-02
申请号：US14670421
申请日：2015-03-27
申请人： Calitor Sciences, LLC , Sunshine Lake Pharma Co., Ltd.
发明人： Ning Xi , Minxiong Li , Haiyang Hu , Weilong Dai
IPC分类号： A61K31/506 , C07D403/14 , A61K31/527 , C07D401/14 , A61K45/06 , C07D493/04 , C07D403/12
CPC分类号： C07D403/14 , A61K31/506 , A61K31/527 , A61K45/06 , C07D401/14 , C07D403/12 , C07D493/04
摘要： The present invention provides novel heteroaryl compounds, pharmaceutical acceptable salts and formulations thereof useful in preventing, treating or lessening the severity of a protein kinase-mediated disease. The invention also provides pharmaceutically acceptable compositions comprising such compounds and methods of using the compositions in the treatment of protein kinase-mediated disease.

36. 发明授权

US09326975B2 Substituted pyrazolone compounds and methods of use 有权
公开(公告)号：US09326975B2
公开(公告)日：2016-05-03
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： C07D401/14 , A61K31/444 , A61K31/4439 , C07D401/12 , A61K45/06
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.

37. 发明授权

US09181277B2 Aminoquinazoline derivatives and their salts and methods of use 有权
标题翻译：氨基喹唑啉衍生物及其盐及使用方法
公开(公告)号：US09181277B2
公开(公告)日：2015-11-10
申请号：US14346741
申请日：2012-11-14
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Jiancun Zhang , Yingjun Zhang , Weihong Zhang , Bing Liu , Jiquan Zhang , Jinlei Liu , Lu Zhang
IPC分类号： A61K31/517 , A61K31/5383 , C07D403/12 , C07D487/04 , C07D491/052 , C07D491/056 , C07D491/048 , C07D513/04 , C07D498/04 , C07D401/12 , C07D471/04 , C07D495/04 , A61K45/06 , A61K31/519
CPC分类号： C07D513/04 , A61K31/517 , A61K31/519 , A61K31/5383 , A61K45/06 , C07D401/12 , C07D403/12 , C07D471/04 , C07D487/04 , C07D491/048 , C07D491/052 , C07D491/056 , C07D495/04 , C07D498/04 , A61K2300/00
摘要： The present invention relates to the field of medicine. Provided herein are aminoquinazoline derivatives, their salts and pharmaceutical formulations useful in modulating the protein tyrosine kinase activity, and in modulating inter- and/or intra-cellular signaling. Also provided herein are pharmaceutically acceptable compositions comprising the aminoquinazoline compounds and methods of using the compositions in the treatment of hyperproliferative disorders in mammals, especially humans.
摘要翻译：本发明涉及药物领域。本文提供的氨基喹唑啉衍生物，其盐和药物制剂可用于调节蛋白质酪氨酸激酶活性，以及调节细胞间和/或细胞内信号传导。本文还提供了包含氨基喹唑啉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。

38. 发明申请

US20150299118A1 HEXAHYDROPENTALENO DERIVATIVES, PREPARATION METHOD AND USE IN MEDICINE THEREOF 有权
标题翻译：六氢叶酸衍生物，其制备方法和用途
公开(公告)号：US20150299118A1
公开(公告)日：2015-10-22
申请号：US14378975
申请日：2013-06-25
申请人： SUNSHINE LAKE PHARMA CO., LTD.
发明人： Zheng Gu , Guanpeng Qiu , Wuyong Wu , Panpan Kang , Zongyuan Zhang , Gang Chen , Chengsheng Lan , Yonggang Wei , Jiaping Wen , Guozhi Zhu , Yonghua Lu , Heran Wang , Yincai Wang , Mingyun Yuan , Kangzhi Ye , Guizhuan Su , PengCho Tang
IPC分类号： C07D207/16 , A61K31/40 , C07D405/12 , C07D209/52 , A61K31/403 , C07C217/52 , A61K45/06
CPC分类号： C07D207/16 , A61K31/40 , A61K31/4025 , A61K31/403 , A61K45/06 , C07C213/02 , C07C217/52 , C07C249/08 , C07C253/30 , C07C255/47 , C07C2601/02 , C07C2602/22 , C07C2603/94 , C07D209/52 , C07D405/12 , C07C251/34 , A61K2300/00
摘要： The invention relates to hexahydropentaleno derivatives, the preparation method and use in medicine thereof, and in particular to hexahydropentaleno derivatives or stereo-isomers or pharmaceutically acceptable salts thereof as shown in general formula (I), and to the preparation method therefor and pharmaceutical compositions comprising the derivatives, and to the use thereof as a therapeutical agent, especially as a DPP-IV inhibitor. The definition of each substituent in formula (I) is the same as the definition in the description.
摘要翻译：本发明涉及六氢蛇嘌呤衍生物，其制备方法及其药物用途，特别是通式（I）所示的六氢蛇嘌呤衍生物或立体异构体或其药学上可接受的盐及其制备方法和药物组合物，其包含衍生物和其作为治疗剂的用途，特别是作为DPP-IV抑制剂。式（I）中每个取代基的定义与描述中的定义相同。

39. 发明申请

US20150037280A1 SUBSTITUTED PYRAZOLONE COMPOUNDS AND METHODS OF USE 有权
公开(公告)号：US20150037280A1
公开(公告)日：2015-02-05
申请号：US13945924
申请日：2013-07-19
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： C07D401/12 , A61K31/4439 , A61K45/06 , 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.

40. 发明申请

US20140364464A1 CRYSTALLINE FORMS OF AZILSARTAN MEDOXOMIL POTASSIUM AND PREPARATION AND USES THEREOF 有权
标题翻译：亚硫酸钾溶液的结晶形式及其制备及其用途
公开(公告)号：US20140364464A1
公开(公告)日：2014-12-11
申请号：US14371737
申请日：2013-01-14
申请人： SUNSHINE LAKE PHARMA CO., LTD. , RUYUAN HEC PHARM CO., LTD.
发明人： Xin Lei , Zhiqing Lv , Tianming Wang
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to the field of pharmaceutical chemistry. Disclosed herein is a crystalline form of azilsartan medoxomil potassium, which is substantially pure. The crystalline form is crystalline form A, form B, form C, form D, form E, form F, form G, form H, form I, form J, form K or form L. The substantially pure crystalline forms of azilsartan medoxomil potassium of the invention generally have good properties such as high solubility, high bioavailability, good stability, long shelf life and good antistatic property. The crystalline forms of azilsartan medoxomil potassium generally exhibit an excellent performance in reducing clinical systolic blood pressure (SBP) and average 24-hour SBP. Disclosed herein are methods of preparing the substantially pure crystalline forms of azilsartan medoxomil potassium, pharmaceutical compositions comprising the crystalline forms, and preparation methods and uses thereof.
摘要翻译：本发明涉及药物化学领域。本文公开的是基本上纯的吖唑烷酮莫昔米尔钾的结晶形式。结晶形式为晶型A，B型，C型，D型，E型，F型，G型，H型，I型，J型，K型或L型。本发明通常具有高溶解性，高生物利用度，良好的稳定性，长保存期和良好的抗静电性等良好的性能。吖唑烷酮莫昔米尔钾的结晶形式通常表现出降低临床收缩压（SBP）和平均24小时SBP的优异表现。本文公开了制备基本上纯的结晶形式的吖唑烷酮莫昔米尔钾的方法，包含结晶形式的药物组合物及其制备方法和用途。

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