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91.发明申请公开(公告)号：US20150087828A1
公开(公告)日：2015-03-26
申请号：US14394041
申请日：2013-04-15
发明人： Fuli Zhang , Chonghao Liu , Pengcheng Qiu , Jian Chai , Qingfeng Cai
IPC分类号： C07D265/32 , C07D413/06
CPC分类号： C07D265/32 , C07D413/06
摘要： A molecule with neural activities, especially 4-substituent-2-hydroxymorpholin-3-one, as a new intermediate of neurokinin-1 receptor antagonist aprepitant, and preparation method thereof.
摘要翻译： 具有神经活性的分子，特别是4-取代基-2-羟基吗啉-3-酮作为神经激肽-1受体拮抗剂阿维他啶的新中间体及其制备方法。
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92.发明申请4-SUBSTITUTED-(3-SUBSTITUTED-1H-PYRAZOLE-5-AMINO)-PYRIMIDINE DERIVATIVES HAVING ACTIVITY OF INHIBITING PROTEIN KINASE AND USE THEREOF 有权具有抑制性蛋白激酶活性的4-取代的（3-取代的1H-吡唑-5-氨基） - 吡啶衍生物及其用途公开(公告)号：US20140378488A1
公开(公告)日：2014-12-25
申请号：US14342656
申请日：2011-09-05
发明人： Yili Ding , Xuan Yang , Qingyan Yan , Hua Bai , Lifeng Cai , Kenneth Smith , Jian Chai
IPC分类号： C07D403/12
CPC分类号： C07D403/12 , A61K31/4155 , C07D401/14 , C07D403/14 , C07D405/14 , C07D409/14
摘要： Provided are derivatives substituted by urea associated with 4-substituted-(3-substituted-1H-pyrazole-5-amino)-pyrimidine-2-amino of formula (I), wherein these compounds may selectively regulate or inhibit an information transmission process controlled by natural or variant tyrosine kinase. Also provided are preparation methods and uses of the compounds.
摘要翻译： 提供的是由与式（I）的4-取代的 - （3-取代的-1H-吡唑-5-氨基） - 嘧啶-2-氨基相关的脲取代的衍生物，其中这些化合物可以选择性地调节或抑制控制的信息传递过程 通过天然或变体酪氨酸激酶。 还提供了化合物的制备方法和用途。
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公开(公告)号：US20240287045A1
公开(公告)日：2024-08-29
申请号：US18571216
申请日：2022-06-21
发明人： Meiyu ZHAO , Lianwei CHEN , Na LI , Zhenjuan SHI , Jianfeng ZHENG , Di SU
IPC分类号： C07D403/12 , A61K31/506
CPC分类号： C07D403/12 , 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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94.发明公开公开(公告)号：US20240287044A1
公开(公告)日：2024-08-29
申请号：US18571213
申请日：2022-06-01
发明人： Jinqing ZHONG , Xinlong ZHANG , Yongxiang GONG , Lei CHEN , Xiaohe ZHENG , Lifei MAO , Yi LI
IPC分类号： C07D403/12 , A61K31/506 , A61P35/00
CPC分类号： C07D403/12 , A61K31/506 , A61P35/00
摘要： The present invention relates to a mesylate or ethanesulfonate salt of the compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition comprising the salt, and an application of the salt.
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公开(公告)号：US20230348467A1
公开(公告)日：2023-11-02
申请号：US17791283
申请日：2021-01-12
发明人： Xiangui Huang , Yanghui Guo , Zongxing Qiu , Pingyan Bie , Weiwei Liao , Qingyan Yan , Weichao Shen , Hai Cao , Qingna Xing , Xin Wang , Qi Cao , Lichen Meng , Nuoyi Wu , Wenpeng Li , Cheng Ye , Taishan Hu , Lei Chen
IPC分类号： C07D487/04 , C07D519/00 , A61P35/00
CPC分类号： C07D487/04 , C07D519/00 , A61P35/00
摘要： The present invention relates to heteroaryl derivatives, preparation methods therefor, and applications thereof in medicine. Specifically, the present invention relates to a heteroaryl derivative represented by general formula (AI), a preparation method therefor, and a pharmaceutically acceptable salt, and use thereof as a therapeutic agent, in particular, as an SHP2 allosteric inhibitor, wherein the definition of substituents in general formula (AI) is the same as that in the description.
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96.发明公开公开(公告)号：US20230242522A1
公开(公告)日：2023-08-03
申请号：US18012269
申请日：2021-06-25
发明人： Yanghui GUO , Lichen MENG , Xiangui HUANG , Weiwei LIAO , Yongxiang GONG , Daiwang XU , Taishan HU , Lei CHEN
IPC分类号： C07D413/14
CPC分类号： C07D413/14
摘要： The present invention relates to a pharmaceutically acceptable salt of (S)-2-(6-fluorobenzo[d]oxazol-2-yl)-6-methoxy-5-((5-methoxypyridin-2-yl))methoxy)-1,2,3,4-tetrahydroisoquinoline-3-carboxylic acid, a preparation method therefor, a pharmaceutical composition comprising the pharmaceutically acceptable salt thereof, and the use thereof as a therapeutic agent, in particular as an angiotensin II type-2 receptor antagonist.
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公开(公告)号：US20220235070A1
公开(公告)日：2022-07-28
申请号：US17612315
申请日：2020-05-20
发明人： Youxi CHEN , Liang GONG , Xingwu ZHU , Qing XIANG , Wentao MAO , Cheng YE , Taishan HU , Lei CHEN , Guoping JIANG
IPC分类号： C07D498/22 , C07D487/04 , A61P35/00
摘要： Provided are a macrolide derivative represented by formula (I), a preparation method thereof, and an application of the macrolide derivative as an inhibitor of one or more protein kinases of TRK, ALK and ROS1,
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公开(公告)号：US11384097B2
公开(公告)日：2022-07-12
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 , C07D401/04 , C07D413/04 , C07D413/14 , C07D417/04
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：US11371026B2
公开(公告)日：2022-06-28
申请号：US16301377
申请日：2017-05-08
发明人： Min Zhou , Xing Jiang , Shuang Han , Yingying He , Linghui Zheng
摘要： The present invention relates to a DoxA protein mutant having an amino acid sequence set forth in SEQ ID NO: 16, and coding gene thereof. The protein mutant or the coding gene thereof can be used for producing epirubicin. The present invention further relates to a Streptomyces capable of efficiently expressing epirubicin, which is constructed by replacing the dnmV gene of a starting Streptomyces in situ with the avrE gene and mutating the doxA gene of the starting Streptomyces into a gene encoding the protein set forth in SEQ ID NO: 16. The fermentation broth of this Streptomyces has an epirubicin potency of up to 102.0 μg/ml.
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公开(公告)号：US20200207745A1
公开(公告)日：2020-07-02
申请号：US16800057
申请日：2020-02-25
发明人： Lei Chen , Dongliang Guan , Hua Bai , Jun Gou , Weifeng Zhao , Zhongli Wang , Long Ling , Yutao Ma
IPC分类号： C07D403/14 , C07D403/12 , C07D471/10 , C07D487/10 , A61K31/506 , A61P35/00 , C07D403/04
摘要： The present invention relates to a pyrimidine derivative, a method for preparing same and use thereof in medicine. In particular, the present invention relates to a pyrimidine derivative represented by general formula (I), a method for preparing same and a pharmaceutically acceptable salt thereof as well as use thereof as a therapeutic agent, in particular as a FGFR4 kinase inhibitor, definitions of each substituent in the general formula (I) being the same as those defined in the description.
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