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公开(公告)号：EP2816039A1
公开(公告)日：2014-12-24
申请号：EP13749142.9
申请日：2013-02-08
发明人： ZHANG, Fuli , YANG, Chunbo , LIANG, Bin , QIU, Pengcheng , LUO, Hairong , LI, Jiang , CHAI, Jian , CAI, Qingfeng
IPC分类号： C07D263/20 , C07D265/30 , C07D303/36 , C07D205/12 , C07D413/10 , C07D295/155 , C07D413/00
CPC分类号： C07D263/20 , C07D413/06
摘要： Disclosed is a new method for preparing a methyl substitute of a linezolid intermediate, (S)-2-(3-(3-fluoro-4-morpholinophenyl)-2-oxo-5-oxazoline) ( I ), wherein the intermediate (I) is obtained by the cyclization of 3-fluoro-4-morpholinophenyl isocyanate (II) and epoxy compound (III). This process has a short process route, low cost, easy operation, and high yield, so is suitable for a large-scale industrial production.
摘要翻译： 公开了用于制备（（S）-2-（3-（3-氟-4-吗啉代苯基）-2-氧代-5-恶唑啉）（I）的利奈唑胺中间体的甲基取代物的新方法，其中中间体 I）通过3-氟-4-吗啉代异氰酸酯（II）和环氧化合物（III）的环化获得。 该工艺工艺路线短，成本低，操作方便，收率高，适合大规模工业化生产。
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52.发明公开BENZAMIDE DERIVATIVE WITH ANTICANCER ACTIVITY AND PREPARATION METHOD AND USE THEREOF 审中-公开BENZAMIDDERIVAT MIT ANTIKREBSWIRKUNG SOWIE HERSTELLUNGSVERFAHRENDAFÜRUND VERWENDUNG DAVON
公开(公告)号：EP2636667A1
公开(公告)日：2013-09-11
申请号：EP11837396.8
申请日：2011-11-03
发明人： BAI, Hua , ZHAO, Xuyang , GONG, Yongxiang , ZHONG, Jinqing , ZHU, Qifeng , LIU, Xiaoyu , LIU, Lifei , ZHOU, Qixian
IPC分类号： C07C233/65 , C07C233/92 , C07C231/02 , C07C231/12 , C07C271/64 , C07C269/04 , C07C255/57 , C07C253/30 , A61K31/166 , A61K31/27 , A61K31/277 , A61P35/00 , A61P35/02
CPC分类号： C07C255/60 , C07C231/02 , C07C233/65 , C07C233/92 , C07C253/30 , C07C255/57 , C07C271/64 , C07D295/192
摘要： Provided are a benzamide derivative as shown in formula (I) or a pharmaceutically acceptable salt thereof, and the preparation method and use thereof for preparing a medicine for treating cancer, wherein the group definitions of formula (I) are as set out in the description.
摘要翻译： 提供式（I）所示的苯甲酰胺衍生物或其药学上可接受的盐及其制备用于治疗癌症的药物的制备方法和用途，其中式（I）的基团定义如说明书所述 。
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公开(公告)号：EP2241566B1
公开(公告)日：2013-08-21
申请号：EP08714810.2
申请日：2008-02-01
发明人： WANG, Jidong , ZHANG, Hui , WANG, Haibin , YING, Lingping , WANG, Sheng , GUAN, Xufang , BAI, Hua
IPC分类号： C07D417/06 , C07D493/04
CPC分类号： C07D417/06 , C07D493/04
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公开(公告)号：EP1845092B1
公开(公告)日：2010-09-01
申请号：EP05824250.4
申请日：2005-12-23
发明人： YAO, Hui
IPC分类号： C07D239/36 , A61K31/505 , A61K31/513 , A61P3/06 , A61P3/10 , A61P19/10 , A61P25/28 , C07D405/06
CPC分类号： C07D239/36 , C07D405/06 , C07F9/65122
摘要： Pyrimidinone compounds, their preparation and use thereof are disclosed. The said compounds are HMG-CoA reductase inhibitors, and can be used for the treatment and prophylaxis of cardiovascular disease, senile dementia, diabetes, osteoporosis and cancer, and shows anti-viral activity and immunity-enchancing activity, especially suitable for the treatment of hyperlipidemics-related diseases.
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公开(公告)号：EP4361144A1
公开(公告)日：2024-05-01
申请号：EP22827556.6
申请日：2022-06-21
发明人： ZHAO, Meiyu , CHEN, Lianwei , LI, Na , SHI, Zhenjuan , ZHENG, Jianfeng , SU, Di
IPC分类号： C07D403/12 , C07D471/10 , C07D487/10 , A61K31/506 , A61P35/00
CPC分类号： C07D403/12 , C07D471/10 , C07D487/10 , A61P35/00 , A61K31/506
摘要： The present invention relates to the field of chemical pharmacy, relates to a crystal form of a pyrimidine derivative and a preparation method therefor, and specifically relates to crystal forms A, B, C, D, and E of a compound of formula (I), a preparation method therefor, and a pharmaceutical composition and use thereof. The present invention solves the problems of small granularity, poor fluidity, poor stability and the like of the compound of formula (I) present in an amorphous form. The crystal form prepared by the present invention and the pharmaceutical composition thereof can be used for preparing a drug for treating a cancer disease.
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公开(公告)号：EP4357333A1
公开(公告)日：2024-04-24
申请号：EP22824244.2
申请日：2022-06-15
发明人： LI, Xufei , WU, Jinlong , ZHANG, Yong , ZHANG, Yuncai , XU, Xiaojie , CHEN, Lei , WANG, Xiaoming , CHEN, Yanan , JIN, Meichun , ZHOU, Yaqian , ZHAN, Dongkai
IPC分类号： C07C303/40
CPC分类号： C07C303/40
摘要： The present invention provides a hybutimibe intermediate and a preparation method therefor. The method comprises the steps of: reacting an easily available raw material of p-fluorobenzoyl butyrate with cheap sulfonylhydrazide to obtain sulfonylhydrazone valerate, then reacting sulfonylhydrazone valerate with carbon dioxide under an alkaline condition to obtain a compound of formula VI with a Z configuration, followed by subjecting the compound of formula VI to acylation, reduction and hydrolysis to obtain the hybutimibe intermediate of (Z)-5-(4-fluorophenyl)-6-hydroxy-hex-4-enoic acid. The preparation method involves readily available and cheap raw materials, has mild reaction conditions, simple and safe operation, a good stereoselectivity, a high yield and low costs, and is suitable for industrial mass production.
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57.发明授权
公开(公告)号：EP3342778B1
公开(公告)日：2022-01-12
申请号：EP16840785.6
申请日：2016-08-26
发明人： YANG, Zhiqing , ZHANG, Liang , ZHANG, Xiangyang , SHI, Zhenjuan , SU, Di , LUO, Hairong , LUO, Hongying , FU, Dejin
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公开(公告)号：EP3459952B1
公开(公告)日：2022-01-05
申请号：EP17798784.9
申请日：2017-05-19
发明人： CHEN, Lei , GUAN, Dongliang , BAI, Hua , GOU, Jun , ZHAO, Weifeng , WANG, Zhongli , LING, Long , MA, Yutao
IPC分类号： C07D471/10 , C07D487/10 , C07D401/12 , C07D403/12 , A61K31/506 , A61K31/505 , A61P35/00
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公开(公告)号：EP3406619B1
公开(公告)日：2020-11-25
申请号：EP16885495.8
申请日：2016-01-18
发明人： YIN, Mingxing , WU, Dongdong , WEN, Weijiang
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公开(公告)号：EP3483165A1
公开(公告)日：2019-05-15
申请号：EP17823604.8
申请日：2017-07-04
发明人： TENG, Yun , XU, Hongbing , JIANG, Lianqing , CHEN, Zhengjie , BAI, Hua
IPC分类号： C07D493/22 , A01N43/90 , A01P7/02 , A01P7/04
摘要： The present invention relates to the field of pharmaceuticals, especially to the field of veterinary drugs, and more particularly to a crystal form of milbemycin A3 oxime, able to be characterized by the X-ray powder diffraction spectrogram, infrared absorption (IR) spectrogram, differential scanning calorimetry (DSC), and thermogravimetric analysis (TGA), etc. Furthermore, the present invention also relates to a method for preparing the crystal form of milbemycin A3 oxime and to a use of the crystal form of milbemycin A3 oxime as an insecticidal and acaricidal agent.
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