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1.发明公开
公开(公告)号：EP3766870A1
公开(公告)日：2021-01-20
申请号：EP19761595.8
申请日：2019-03-01
发明人： GONG, Feng , HUANG, Ticong , ZANG, Haishan , ZHANG, Shibo , ZHAO, Rui , LIU, Fei
IPC分类号： C07D215/22 , A61K31/47 , A61P35/00 , A61P29/00 , A61P37/06
摘要： The present application falls within the field of medicinal chemistry, relates to the crystalline of a compound as a c-Met kinase inhibitor, and specifically relates to the crystalline of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fluorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystalline for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystalline of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.
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2.发明公开
公开(公告)号：EP4279138A3
公开(公告)日：2024-03-27
申请号：EP23198543.3
申请日：2019-03-01
发明人： GONG, Feng , HUANG, Ticong , ZANG, Haishan , ZHANG, Shibo , ZHAO, Rui , LIU, Fei
IPC分类号： C07D215/22 , A61K31/47 , A61P35/00
摘要： The present application falls within the field of medicinal chemistry, relates to the crystal of a compound as a c-Met kinase inhibitor, and specifically relates to the crystal of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fl uorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystal for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystal of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.
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3.发明公开
公开(公告)号：EP4279138A2
公开(公告)日：2023-11-22
申请号：EP23198543.3
申请日：2019-03-01
发明人： GONG, Feng , HUANG, Ticong , ZANG, Haishan , ZHANG, Shibo , ZHAO, Rui , LIU, Fei
IPC分类号： A61P35/00
摘要： The present application falls within the field of medicinal chemistry, relates to the crystal of a compound as a c-Met kinase inhibitor, and specifically relates to the crystal of N-(4-((7-((1-(cyclopentylamino)cyclopropyl)methoxy)-6-methoxyquinolin-4-yl)oxy)-3-fl uorophenyl)-N-(4-fluorophenyl)cyclopropane-1,1-dicarboxamide, and a preparation method therefor, a crystalline composition thereof, and a pharmaceutical composition thereof, as well as the use of the crystal for treating diseases associated with the inhibition of growth factor receptor protein tyrosine kinase activity. The crystal of the present application has excellent properties in at least one of the following aspects: pharmacokinetics, bioavailability, hygroscopicity, stability, solubility, purity, ease of preparation, etc.
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4.发明公开
公开(公告)号：EP3816161A1
公开(公告)日：2021-05-05
申请号：EP19826745.2
申请日：2019-06-24
发明人： DONG, Ping , HE, Xiongxiong , LIU, Lei , ZHAO, Rui
IPC分类号： C07D401/12 , A61K31/4709 , A61P35/00 , A61K9/14
摘要： The present application relates to the field of pharmaceutical technology, specifically to the crystal habit and crystalline powder preparation of quinoline derivatives, and more specifically, to the crystal habit and crystalline powder preparation of anlotinib dihydrochloride. The compound of formula II disclosed herein is a crystalline powder with a flaky crystal habit having a specific surface area ≥ 10 m 2 /g and a particle-size distribution of X 50 ≤ 50 µm and/or X 90 ≤ 500 µm, such that a large specific surface area is provided without reducing the particle size of the drug by a physical method under the condition of a broad particle-size distribution, and the drug can rapidly dissolving. In addition to excellent dissolution property, the crystalline powder is also beneficial to industrial manufacturing, featuring simplified process and cost-efficiency.
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5.发明公开
公开(公告)号：EP3502103A1
公开(公告)日：2019-06-26
申请号：EP17848166.9
申请日：2017-09-08
发明人： DING, Charles Z. , CHEN, Shuhui , HU, Lihong , XU, Zhaobing , LIU, Yingchun , REN, Bingjie , LI, Weidong , LI, Zongbin , ZHAO, Rui , ZHANG, Xiquan
IPC分类号： C07D401/14 , A61K31/506 , A61P35/00
摘要： A crystal form and a salt type of a substituted 2-hydro-pyrazole derivative, preparation method therefor, and use of the crystal form and the salt type in preparation of a medicament for treating cancers such as breast cancer, lung cancer and the like.
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公开(公告)号：EP3176160A1
公开(公告)日：2017-06-07
申请号：EP15826817.7
申请日：2015-07-31
申请人： Chia Tai Tianqing Pharmaceutical Group Co.,Ltd , Lianyungang Runzhong Pharmaceutical Co., Ltd. , Centaurus BioPharma Co., Ltd.
发明人： GONG, Feng , LI, Xinlu , ZHAO, Rui , ZHANG, Xiquan , XU, Xinhe , LIU, Xijie , XIAO, Dengming , HAN, Yongxin
IPC分类号： C07D401/14 , C07D213/73 , A61K31/496 , A61K31/444 , A61P35/00
CPC分类号： C07D401/14 , A61K31/444 , A61K31/496 , C07D213/73
摘要： The present invention discloses pharmaceutically acceptable acid salts of pyridine-substituted 2-aminopyridine derivatives as protein kinase inhibitors, preparation methods, pharmaceutical compositions thereof, and use thereof for the treatment of diseases associated with protein kinase.
摘要翻译： 本发明公开了作为蛋白激酶抑制剂的吡啶取代的2-氨基吡啶衍生物的药学上可接受的酸式盐，其制备方法，药物组合物及其用于治疗与蛋白激酶相关的疾病的用途。
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公开(公告)号：EP3919485A1
公开(公告)日：2021-12-08
申请号：EP20749295.0
申请日：2020-01-31
发明人： ZHANG, Xiquan , WANG, Shanchun , GENG, Wenjun , LIU, Yanlong , ZHANG, Huihui , LIU, Fei , ZHU, Shanliang , LI, Xinlu , ZHAO, Rui , GU, Hongmei
IPC分类号： C07D401/12 , A61P35/00 , A61K31/4709
摘要： The present application relates to the field of medicine, and relates to crystals of quinoline derivatives, and in particular, to crystals of a quinoline derivative anhydride and a solvate, as well as a method for preparing the crystals, pharmaceutical compositions containing the crystals, and a use thereof in the field of medicine. The present application further provides a preparation method therefor, which has a high yield, has mild crystallization conditions, is suitable for industrial production, and may better meet the needs of the pharmaceutical industry.
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公开(公告)号：EP3412673B1
公开(公告)日：2020-11-25
申请号：EP17747006.9
申请日：2017-02-04
发明人： DING, Zhaozhong , SUN, Fei , HU, Yinghu , ZHOU, Yilong , ZHAO, Rui , YANG, Ling
IPC分类号： C07D487/04
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9.发明公开
公开(公告)号：EP3572409A1
公开(公告)日：2019-11-27
申请号：EP18742199.5
申请日：2018-01-22
申请人： Chia Tai Tianqing Pharmaceutical Group Co., Ltd. , Lianyungang Runzhong Pharmaceutical Co., Ltd. , Centaurus BioPharma Co., Ltd.
发明人： HUANG, Ticong , XIAO, Huifeng , ZHAO, Rui , LIU, fei , WEI, Wei , XU, Hongjiang , WANG, Xiaojin , WU, Jingli
IPC分类号： C07D401/14 , A61K31/5377 , A61P35/00
摘要： The invention discloses a crystal of 4-(tert-butoxyamino)-6-(6-(trifluoromethyl)pyridin-2-yl) -N-(2-(trifluoromethyl)pyridin-4-yl)-1,3,5-triazin-2-amine compound, a mesylate salt and crystal thereof, a preparation method thereof, a composition containing thereof, and a use thereof for inhibiting activity of mutant IDH2 and treating cancer.
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公开(公告)号：EP3828192A1
公开(公告)日：2021-06-02
申请号：EP19841191.0
申请日：2019-07-24
发明人： LIU, Lin , ZHAO, Rui , SANG, Guangming , ZHOU, Xingjian , GUO, Xiaopeng , ZHANG, Aiming , WU, Gang , XIA, Chunguang , ZHANG, Xiquan
IPC分类号： C07H19/073 , C07H1/00
摘要： The present application relates to a method for preparing trifluridine, comprising reacting a compound of formula III with a compound of formula IV in a first solvent in the presence of an acid to obtain a compound of formula II, and performing further reaction to obtain trifluridine.
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