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公开(公告)号:US20220324868A1
公开(公告)日:2022-10-13
申请号:US17623001
申请日:2020-08-28
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Qian WANG , Guoyong HUO , Guangxin XIA , Jiangsong LOU , Sijie SHU , Hui GE , Lin ZHANG , Chen SHI , Zhihui ZHANG , Yu MAO , Bingbin ZHANG , Jianxin YU , Yanjun LIU , Ying KE , Chi ZHANG
IPC: C07D487/04
Abstract: Disclosed in the present invention are a pyrazolone-fused pyrimidine compound, and a preparation method and a use therefor. Provided in the present invention is a pyrazolone-fused pyrimidine compound as in formula (I), said compound having better inhibitory activity towards WEE1 kinase.
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公开(公告)号:US20190010153A1
公开(公告)日:2019-01-10
申请号:US16067158
申请日:2016-12-30
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Guangxin XIA , Qian WANG , Chen SHI , Xiong ZHAI , Hui GE , Xuemei LIAO , Yu MAO , Zhixiong XIANG , Yanan HAN , Guoyong HUO , Yanjun LIU
IPC: C07D471/04 , A61P35/00 , C07F9/6561 , C07F9/6584 , C07F7/08 , C07F5/02
CPC classification number: C07D471/04 , A61P35/00 , C07F5/025 , C07F7/0812 , C07F7/0816 , C07F7/083 , C07F9/6561 , C07F9/65842 , Y02P20/55
Abstract: The present invention discloses a nitrogen-containing fused heterocyclic compound, as well as a preparation method, intermediate, composition and application thereof. The nitrogen-containing fused heterocyclic compound of the present invention as represented by formula (I), as well as the pharmaceutically acceptable salt, enantiomer, diastereomer, tautomer, solvate, metabolite or drug precursor thereof, exhibit a high selectivity and a high inhibitory activity with respect to CDK4 and CDK6 at a molecular level, an excellent inhibitory activity with respect to breast cancer cells at a cellular level, and significant inhibition of tumor cell proliferation associated with cyclin-dependent kinase activity at an animal level. The invention also exhibits a good stability with respect to human or mouse liver microsomes without significant inhibition of metabolic enzymes, good in vivo absorption in mice and rats, a high bioavailability and good druggability.
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3.
公开(公告)号:US20220259210A1
公开(公告)日:2022-08-18
申请号:US17622579
申请日:2020-06-28
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Qian WANG , Sijie SHU , Guangxin XIA , Hui GE , Bingbin ZHANG , Guoyong HUO , Lin ZHANG , Chen SHI , Jiangsong LOU , Chi ZHANG , Zhihui ZHANG , Yu MAO , Jianxin YU , Ying KE , Yanjun LIU
IPC: C07D487/04 , A61K31/519 , A61K45/06 , A61P35/00
Abstract: Disclosed are a pyrazolone-fused pyrimidine compound, a preparation method for same and applications thereof. Provided in the present invention is the pyrazolone-fused pyrimidine compound as represented by formula (II). The compound has improved inhibitory activity with respect to WEE1 kinase.
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公开(公告)号:US20200239470A1
公开(公告)日:2020-07-30
申请号:US16848942
申请日:2020-04-15
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Guangxin XIA , Qian WANG , Chen SHI , Xiong ZHAI , Hui GE , Xuemei LIAO , Yu MAO , Zhixiong XIANG , Yanan HAN , Guoyong HUO , Yanjun LIU
IPC: C07D471/04 , C07F9/6584 , C07F9/6561 , C07F7/08 , C07F5/02 , A61P35/00
Abstract: The present invention discloses a substituted pyridine compound represented by formula I, and a pharmaceutically acceptable salt, stereoisomer and tautomer thereof. The compounds of the present invention are useful in the treatment of cancers.
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公开(公告)号:US20190300491A1
公开(公告)日:2019-10-03
申请号:US16335622
申请日:2017-09-22
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Guangxin XIA , Di LI , Ning ZHOU , Ao CHEN , Liang ZHAO , Jiansheng HAN , Yanjun LIU
IPC: C07D239/94 , A61P35/00 , C07C59/265 , C07C309/05 , C07C309/29 , C07C59/105 , C07C59/255 , C07C65/11 , C07C309/35 , C07C59/305 , C07C69/38 , C07C69/40 , C07C59/347 , C07C57/145 , C07C55/08 , C07C55/10 , C07C309/39
Abstract: A salt of a quinazoline derivative (N-[4-(3-chlorine-4-fluoanilino)]-7-(3-morpholinepropanol)-6-(2-fluoroacrylamide)-quinazoline, the structure thereof is as represented by formula I). Compared with a known quinazoline derivative, the salt of the quinazoline derivative has one or more improved properties and at least has better water solubility, wherein a citrate, a benzene sulfonate, and an ethanedisulphonate thereof further have better crystallinity and are not easy to absorb moisture.
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6.
公开(公告)号:US20240307346A1
公开(公告)日:2024-09-19
申请号:US18606090
申请日:2024-03-15
Inventor: Taisheng LI , Yanjun LIU
IPC: A61K31/365 , A61P31/18 , A61P37/06
CPC classification number: A61K31/365 , A61P31/18 , A61P37/06
Abstract: Disclosed in the present invention is a method for treating or preventing a disease of incomplete immune reconstitution in aids using (5R)-5-hydroxytriptolide, in particular a method for treating or preventing a disease of incomplete immune reconstitution in AIDS in a subject in need thereof, comprising administering a therapeutically effective amount of a medicament comprising (5R)-5-hydroxytriptolide to the subject. The present invention uses (5R)-5-hydroxytriptolide (T8) in experiments and finds that (5R)-5-hydroxytriptolide has an immunosuppressive activity against incomplete immune reconstitution in AIDS, is characterized by high efficiency and low toxicity, and has a good safety treatment index.
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7.
公开(公告)号:US20190091226A1
公开(公告)日:2019-03-28
申请号:US16081558
申请日:2017-03-01
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Guangxin XIA , Di LI , Hongjian ZUO , Guangsheng WU , Lingjun DUAN , Jing ZHANG , Yu MAO , Yanjun LIU
IPC: A61K31/519 , A61K31/541 , A61K31/5355 , A61K31/5377 , A61P35/00
Abstract: Disclosed are a nitrogenous heterocyclic compound, intermediates, a preparation method, a composition and use thereof. The nitrogenous heterocyclic compound in the present invention is as shown in formula I. The compound has a high inhibitory activity towards ErbB2 tyrosine kinase and a relatively good inhibitory activity towards human breast cancer BT-474 and human gastric cancer cell NCI-N87 which express ErbB2 at a high level, and at the same time has a relatively weak inhibitory activity towards EGFR kinase. Namely, the compound is a highly selective small-molecule inhibitor targeted at ErbB2, and hence it has a high degree of safety, and can effectively enlarge the safety window in the process of taking the drug.
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公开(公告)号:US20220380433A1
公开(公告)日:2022-12-01
申请号:US17776537
申请日:2020-11-12
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Xuemei LIAO , Jingwei HUANG , Zhuo CHEN , Yang LIU , Xiaocui CHENG , Manman XIE , Rongfang SUN , Yingying LI , Guangxin XIA , Ying KE , Yanjun LIU
IPC: C07K14/705 , C07K14/725 , A61P35/00 , A61K35/17 , C07K16/28
Abstract: The present invention relates to an immune cell, which contains a TMEM59 protein and/or a functional fragment thereof, a chimeric antigen receptor (CAR) and/or a coding element thereof, as well as a use of the immune cell in the preparation of a drug for treating tumors. Further provided are a method for promoting the proliferation of immune cells and a method for promoting the production of memory cells.
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公开(公告)号:US20220195397A1
公开(公告)日:2022-06-23
申请号:US17600904
申请日:2020-04-03
Applicant: SHANGHAI PHARMACEUTICALS HOLDING CO., LTD.
Inventor: Xuemei LIAO , Jingwei HUANG , Zhuo CHEN , Manman XIE , Andi LI , Yang LIU , Guangxin XIA , Yanjun LIU , Ying KE
IPC: C12N5/10 , A61K39/00 , A61P35/00 , C07K16/30 , C07K14/725
Abstract: A modified immune effector cell and a use thereof, a cell population containing the immune effector cell, and a pharmaceutical composition. The expression and/or activity of an S1PR1 protein of the modified immune effector cell is up-regulated.
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公开(公告)号:US20210052541A1
公开(公告)日:2021-02-25
申请号:US16969594
申请日:2018-12-14
Inventor: Taisheng LI , Yanjun LIU
IPC: A61K31/343 , A61K9/20
Abstract: Disclosed in the present invention is an application of (5R)-5-hydroxytriptolide in the preparation of drugs, in particular an application in the preparation of drugs for treating and/or preventing acquired immune deficiency syndrome (AIDS) abnormal immune activation or incomplete immune reconstitution associated with AIDS abnormal immune activation. The present invention uses (5R)-5-hydroxytriptolide (T8) in experiments and finds that (5R)-5-hydroxytriptolide has an immunosuppressive activity against AIDS abnormal immune activation or incomplete immune reconstitution associated with AIDS abnormal immune activation, is characterized by high efficiency and low toxicity, and has a good safety treatment index.
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