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Patent Agency Ranking
公开(公告)号：US20190185506A1
公开(公告)日：2019-06-20
申请号：US16324679
申请日：2017-08-04
Inventor： Wenbao LI , Xianjun QU , Feng LI , Liang ZHANG , Shixiao WANG , Zhiyu SONG , Feng WANG , Chong YANG , Huashi GUAN
IPC: C07H17/07 , C07D311/64 , C07H1/00 , A61P1/04 , A61P35/00
CPC classification number: C07H17/07 , A61K31/7048 , A61P1/00 , A61P1/04 , A61P35/00 , C07D311/64 , C07H1/00 , Y02P20/55
Abstract: 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：US20210070738A1
公开(公告)日：2021-03-11
申请号：US16995098
申请日：2020-08-17
Inventor： Wenbao LI , Shixiao WANG , Zhongpeng DING , Yingwei HOU , Huashi GUAN
IPC: C07D403/06 , A61K31/496 , A61P35/00 , A61P31/10
Abstract: 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：US20210002259A1
公开(公告)日：2021-01-07
申请号：US16995045
申请日：2020-08-17
Inventor： Wenbao LI , Shixiao WANG , Zhongpeng DING , Yingwei HOU , Huashi GUAN
IPC: C07D403/06 , A61P35/00 , A61K31/496 , A61P31/10
Abstract: 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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4.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
Inventor： Wenbao LI , Shixiao WANG , Zhongpeng DING , Yingwei HOU , Huashi GUAN
IPC: C07D403/06 , A61P35/00
Abstract: 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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5.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
Inventor： Wenbao LI , Tianwen SUN , Shixiao WANG , Jianchun ZHAO , Bing CAI , Huashi GUAN
IPC: A61K31/496 , C07B59/00 , C07D233/64 , C07D403/06 , A61P35/00
CPC classification number: A61K31/496 , A61P35/00 , C07B59/00 , C07B59/002 , C07D233/64 , C07D403/06
Abstract: 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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