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公开(公告)号：US11421255B2
公开(公告)日：2022-08-23
申请号：US16070497
申请日：2016-01-20
发明人： Dejin Fu , Yong Yang , Wei Yan , Weijiang Wen , Xiande Gu , Hua Chen , Xiaojun Ma , Ling Zhang , Kaijun Wang
摘要： A method for enzymatic preparation of fludarabine phosphate, comprising reaction of fludarabine with a high-energy phosphate compound under the action of deoxyribonucleic acid kinase. According to said method, acetate kinase and acetyl phosphate free acid or acetyl phosphate are also added. The technical problems present in the existing processes are successfully addressed by employing the enzymatic process to prepare the fludarabine phosphate. The usage of the high-energy phosphate compound is reduced by means of adding acetate kinase to recycle and regenerate a small amount of the high-energy phosphate compound, thereby reducing the generation of by-products having similar structures to the fludarabine phosphate, enhancing the operation convenience of purification steps in the industrial production of the fludarabine phosphate. The process is environment friendly, the reaction conditions are moderate, the cost is low, and the yield and the purity of the product obtained are high.
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公开(公告)号：US20220177450A1
公开(公告)日：2022-06-09
申请号：US17602758
申请日：2020-04-09
发明人： Panpan ZHANG , Sunli YAN , Ying LI , Chenli GUO , Wenjian QIAN , Cheng YE , Zhengzheng SHI , Taishan HU , Lei CHEN
IPC分类号： C07D401/14 , C07D487/08 , C07D498/08 , C07D403/14
摘要： The present invention relates to a piperazine amide derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and use of same as a therapeutic agent, especially as a selective Rearranged During Transfection (RET) kinase inhibitor. Ring a, ring e, X1, X2, X3, X4, R1, R2, R3, R4, R4′, R5, R5′, R6, R6′, R7, R7′, R8, m and n have the same definitions as those in the specification.
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公开(公告)号：US20210277021A1
公开(公告)日：2021-09-09
申请号：US17254273
申请日：2019-06-18
发明人： Yanghui GUO , Xiangui HUANG , Weiwei LIAO , Lichen MENG , Taishan HU , Lei CHEN , Guoping JIANG
IPC分类号： C07D498/04 , C07D413/04 , C07D401/04 , C07D417/04 , C07D413/14
摘要： Provided are a tetrahydroisoquinoline derivative, a preparation method therefor and an application thereof in medicine. In particular, provided are a tetrahydroisoquinoline derivative represented by general formula (I), a preparation method therefor and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as an angiotensin II type 2 receptor (AT2R) antagonist, wherein definitions of substituent groups in the general formula (I) are the same as definitions in the description.
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公开(公告)号：US20190152986A1
公开(公告)日：2019-05-23
申请号：US16314748
申请日：2017-07-04
发明人： Yun TENG , Hongbing XU , Lianqing JIANG , Zhengjie CHEN , Hua BAI
IPC分类号： C07D493/22 , A01N43/90
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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公开(公告)号：US20190023681A1
公开(公告)日：2019-01-24
申请号：US16070658
申请日：2016-01-18
发明人： Mingxing Yin , Dongdong Wu , Weijiang Wen
IPC分类号： C07D315/00
CPC分类号： C07D315/00 , C07H1/00 , C07H1/06 , C07H17/00
摘要： A method and an intermediate for preparing a tulathromycin. The method includes the following step: in an organic solvent, subjecting a compound represented by formula (II) and an n-propylamine to a ring-opening addition shown below to obtain a tulathromycin represented by formula (I), wherein the organic solvent is a 1,2-propandiol. Tulathromycin obtained using the method has a high purity, with an HPLC purity being 95% and above, and up to 99% and above, satisfying a required purity for preparing a tulathromycin as a pharmaceutical formulation. The method has a high yield, is simple to operate, and is more suitable for industrial production.
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公开(公告)号：US09982314B2
公开(公告)日：2018-05-29
申请号：US15028577
申请日：2014-10-14
发明人： Hao Xu , Fei Tang , Peijun Zhan , Jianhong Hu , Huijun Ren , Hongmei Fan , Linghui Zheng , Hua Bai
摘要： A bacterial strain of Actinoplanes sp. and and the use thereof. The bacterial strain is named Actinoplanes sp. HS-16-20, whose preservation number is CGMCC (China General Microbiological Culture Collection Center) No. 7294. The bacterial strain can be used to generate Fidaxomicin or analogs thereof or compositions containing Fidaxomicin, such as by aerobically fermenting the strain in nutrient medium containing assimilable carbon and/or nitrogen sources. Fidaxomicin has an inhibitory effect on various gram positive bacteria pathogens, and in particular, on Clostridium difficile.
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公开(公告)号：US20180099930A1
公开(公告)日：2018-04-12
申请号：US15835649
申请日：2017-12-08
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07D205/08 , C07C59/56 , C07C51/367 , C07C67/327 , C07C69/65 , C07C67/343 , C07C67/30 , C07C69/732
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09926268B2
公开(公告)日：2018-03-27
申请号：US15317297
申请日：2015-06-05
发明人： Hua Bai , Xuyang Zhao , Yuncai Zhang , Xufei Li , Yong Zhang , Dezhou Xu , Li Zhang , Xiaojie Xu , Qifeng Zhu , Xiaoming Wang , Zhiqing Yang , Zehua Zhong , Jian Zhang
IPC分类号： C07C51/367 , C07C67/327 , C07D205/08 , C07C67/30 , C07C67/343 , C07C69/65 , C07C69/732 , C07C59/56
CPC分类号： C07D205/08 , C07C51/367 , C07C59/56 , C07C67/30 , C07C67/327 , C07C67/343 , C07C69/65 , C07C69/732
摘要： Disclosed is a new method for preparing an azetidinone compound represented by formula (I). The carboxylic ketoester represented by formula (II) serves as the raw material and is subjected to Grignard addition, stereoselective dehydration, ester group reduction, hydroxyl group protection, addition with imine after condensation with a chiral auxiliary, cyclization and deprotection to obtain the compound represented by formula (I). The present invention has advantages of easily available raw material, a few synthetic steps, simple operation, high yield, good stereoselectivity and low cost, and can be used for industrial production.
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公开(公告)号：US09802891B2
公开(公告)日：2017-10-31
申请号：US15386349
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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公开(公告)号：US09776959B2
公开(公告)日：2017-10-03
申请号：US15386147
申请日：2016-12-21
发明人： Hongyuan Wei , Chongjun Liu , Xuyang Zhao , Xiaojie Xu , Hua Bai , Yuncai Zhang
IPC分类号： C07D205/08 , A61K31/397
CPC分类号： C07D205/08 , A61K31/397 , C07B2200/13
摘要： The present invention provides crystal forms of the compound of (3R,4S)-4-(4-hydroxyphenyl)-3-[3-(4-fluorophenyl)-4-hydroxybut-2(Z)-enyl]-1-(4-fluorophenyl)-2-azetidinone (formula A). The crystal forms can be characterized by X-ray powder diffraction (XRPD) spectra, differential scanning calorimetry (DSC) spectra, infrared absorption spectra and so on. Meanwhile, the present invention also provides methods for preparing the crystal forms of the compound of formula A, pharmaceutical compositions and uses thereof.
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