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公开(公告)号：US10434098B2
公开(公告)日：2019-10-08
申请号：US15579429
申请日：2016-05-27
发明人： Wenbao Li , Tianwen Sun , Shixiao Wang , Jianchun Zhao , Bing Cai , Huashi Guan
IPC分类号： C07D233/64 , C07D403/06 , A61K31/496 , C07B59/00 , A61P35/00
摘要： Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehydrophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
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2.发明公开公开(公告)号：US20240327418A1
公开(公告)日：2024-10-03
申请号：US18293840
申请日：2022-08-01
申请人： OCEAN UNIVERSITY OF CHINA , QINGDAO HIGENE BIOPHARMACEUTICAL CO., LTD , MARINE BIOMEDICAL RESEARCH INSTITUTE OF QINGDAO CO., LTD
发明人： Xiaoyang LI , Zhongren ZHOU , Yuqi JIANG , Kairui YUE , Wenfang XU
IPC分类号： C07D491/048 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4406 , A61K31/4439 , A61K31/655 , A61P35/00 , A61P35/02 , C07C247/12 , C07D209/42 , C07D213/40 , C07D213/56 , C07D307/85 , C07D333/70 , C07D401/04 , C07D471/04 , C07D495/04
CPC分类号： C07D491/048 , A61K31/343 , A61K31/381 , A61K31/404 , A61K31/4355 , A61K31/4365 , A61K31/437 , A61K31/4406 , A61K31/4439 , A61K31/655 , A61P35/00 , A61P35/02 , C07C247/12 , C07D209/42 , C07D213/40 , C07D213/56 , C07D307/85 , C07D333/70 , C07D401/04 , C07D471/04 , C07D495/04
摘要： A compound targeting HDAC and NAD synthesis and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof, as well as preparation and application thereof. Specifically, a compound shown in structural general formula (I) and a pharmaceutically acceptable salt, hydrate, deuterate, isomer or prodrug thereof are provided. The compound of the structural general formula (I) is a multi-target inhibitor, targeting HDAC and NAD targets, and exhibiting significant HDAC inhibitory activity, while representative compounds exhibit certain NAD inhibitory activity.
Ring E-B-L-C (O)—(NH)r-R (General formula I)-
公开(公告)号：US20190185506A1
公开(公告)日：2019-06-20
申请号：US16324679
申请日：2017-08-04
发明人： Wenbao LI , Xianjun QU , Feng LI , Liang ZHANG , Shixiao WANG , Zhiyu SONG , Feng WANG , Chong YANG , Huashi GUAN
IPC分类号： C07H17/07 , C07D311/64 , C07H1/00 , A61P1/04 , A61P35/00
CPC分类号： C07H17/07 , A61K31/7048 , A61P1/00 , A61P1/04 , A61P35/00 , C07D311/64 , C07H1/00 , Y02P20/55
摘要： The present invention provides a myricetin derivative, a preparation method thereof, a pharmaceutical composition containing the same, an application thereof for treating colitis, preventing and treating colitis-associated tumorigenesis and treating colorectal cancer, and an application thereof in preparing a composition for modulating activities of endoplasmic reticulum stress signaling molecules. The myricetin derivative disclosed herein has excellent water solubility, and has biological activities including inhibition of colitis, prevention and treatment of colitis-associated tumorigenesis, and treatment of colorectal cancer. The preparation method disclosed herein uses myricetrin as starting material which is economical and easily available. With the merits of low cost, high yield, high product purity and suitability for large-scale industrial production, the preparation method disclosed herein represents significant market value and economic prospects.
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公开(公告)号：US20220218666A1
公开(公告)日：2022-07-14
申请号：US17604795
申请日：2020-04-17
发明人： Jinbo YANG , Qiaoling SONG , Chenyang ZHAO , Lijuan WU , Jun ZHAO , Dan YAO , Yu TANG , Ximing XU , Menglin YANG
IPC分类号： A61K31/4045 , A61P35/00 , A61K9/00
摘要： The present disclosure discloses the use of Tegaserod or a pharmaceutically acceptable salt thereof as a JAK-STAT3 signaling pathway inhibitor and an immunomodulator in the preparation of an anti-tumor drug. Tegaserod and the pharmaceutically acceptable salt thereof show a very excellent inhibitory effect on the growth of various tumor cells in vivo and in vitro, and are expected to be used in the treatment of various cancers.
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公开(公告)号：US11021507B2
公开(公告)日：2021-06-01
申请号：US16324679
申请日：2017-08-04
发明人： Wenbao Li , Xianjun Qu , Feng Li , Liang Zhang , Shixiao Wang , Zhiyu Song , Feng Wang , Chong Yang , Huashi Guan
IPC分类号： C07H17/07 , A61K31/7048 , A61P35/00 , A61P1/00 , A61P1/04 , C07D311/64 , C07H1/00
摘要： The present invention provides a myricetin derivative, a preparation method thereof, a pharmaceutical composition containing the same, an application thereof for treating colitis, preventing and treating colitis-associated tumorigenesis and treating colorectal cancer, and an application thereof in preparing a composition for modulating activities of endoplasmic reticulum stress signaling molecules. The myricetin derivative disclosed herein has excellent water solubility, and has biological activities including inhibition of colitis, prevention and treatment of colitis-associated tumorigenesis, and treatment of colorectal cancer. The preparation method disclosed herein uses myricetrin as starting material which is economical and easily available. With the merits of low cost, high yield, high product purity and suitability for large-scale industrial production, the preparation method disclosed herein represents significant market value and economic prospects.
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6.发明申请公开(公告)号：US20190177302A1
公开(公告)日：2019-06-13
申请号：US16325166
申请日：2017-07-24
发明人： Wenbao LI , Shixiao WANG , Zhongpeng DING , Yingwei HOU , Huashi GUAN
IPC分类号： C07D403/06 , A61P35/00
摘要： A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
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7.发明申请公开(公告)号：US20180140600A1
公开(公告)日：2018-05-24
申请号：US15579429
申请日：2016-05-27
发明人： Wenbao LI , Tianwen SUN , Shixiao WANG , Jianchun ZHAO , Bing CAI , Huashi GUAN
IPC分类号： A61K31/496 , C07B59/00 , C07D233/64 , C07D403/06 , A61P35/00
CPC分类号： A61K31/496 , A61P35/00 , C07B59/00 , C07B59/002 , C07D233/64 , C07D403/06
摘要： Provided are a deuterium-substituted dehydrophenylahistin-like compound, preparation method thereof and use in a preparation of antitumor drugs. The deuterium-substituted dehydrophenylahistin-like compound has a structure of general formula (I), and a synthesis method thereof comprises: firstly conducting a condensation reaction of diacetyldiketopiperazine and an aldehyde intermediate a or a deuterated aldehyde compound b to form a heterocyclic compound c or a deuterium-containing heterocyclic compound d, which is then subjected to a condensation reaction with benzaldehyde and a deuterium-substituted benzaldehyde-like compound to form the deuterium-substituted dehydrophenylahistin-like compound. Also provided are a highly effective deuterated aldehyde intermediate with a high deuterium substitution rate and a deuterium-containing heterocycle intermediate, and a synthesis method thereof. An experiment shows that the deuterium-substituted dehyd-rophenylahistin-like compound provided by the present invention has an effect on tubulin depolymerization and can treat a refractory solid tumor or lymphoma. The present invention provides a method for researching and developing antitumor drugs of the related compound.
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公开(公告)号：US20220177485A1
公开(公告)日：2022-06-09
申请号：US17251583
申请日：2019-06-11
发明人： Tao JIANG , Guanzhao WU , Xiong HE
IPC分类号： C07D491/22 , A61P35/00
摘要： The present invention is directed to compounds according to Formula I as well as to stereoisomer, tautomer or pharmaceutically acceptable salts of such compounds. The invention also is directed to pharmaceutically acceptable compositions containing such compounds and associated methods for preparing and effect dose in treatment as well as the application in preparing medicine for preventing and/or treating cancers. The invention provides the novel derivatives which introduce methylenedioxy in the position of 10,11 and different groups in the position of 7. The derivatives of novel structure, and the raw materials are easily to obtain. In addition, the compounds in this invention have good cytotoxic activity in vitro and anti-tumor activity in vivo. Therefore, this kind of compounds have broad application foreground. The structure of derivatives are as follows:
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公开(公告)号：US20210070738A1
公开(公告)日：2021-03-11
申请号：US16995098
申请日：2020-08-17
发明人： Wenbao LI , Shixiao WANG , Zhongpeng DING , Yingwei HOU , Huashi GUAN
IPC分类号： C07D403/06 , A61K31/496 , A61P35/00 , A61P31/10
摘要： A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
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公开(公告)号：US10851086B2
公开(公告)日：2020-12-01
申请号：US16325166
申请日：2017-07-24
发明人： Wenbao Li , Shixiao Wang , Zhongpeng Ding , Yingwei Hou , Huashi Guan
IPC分类号： C07D403/06 , A61P35/00 , A61K31/496 , A61P31/10
摘要： A polycrystalline form of a dehydrophenylahistin-like compound, and a manufacturing and purification method and application thereof. A (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)deuteromethylene]piperazine-2,5-dione monohydrate crystal and a (3Z,6Z)-3-benzylidene-6-[(5-tert-butyl-1H-imidazol-4-yl)methylene]piperazine-2,5-dione monohydrate crystal are more competitive crystalline forms with stable quality. The manufacturing and purification method is simple and easy to operate, and can effectively control the generation of a trans-isomer contaminant to obtain a high purity product. The polycrystalline form of the dehydrophenylahistin-like compound has a certain value in an application for manufacturing an antitumor pharmaceutical product.
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