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公开(公告)号:US20220125788A1
公开(公告)日:2022-04-28
申请号:US17418678
申请日:2019-12-24
发明人: Wu DU , Yu LI , Kun WEN , Xinghai LI , Yuanwei CHEN
IPC分类号: A61K31/506 , A61K39/395 , A61P35/00 , C07D403/12
摘要: A deuterated compound as represented by formula (I) or an optical isomer, a tautomer, a pharmaceutically acceptable salt, a prodrug, a hydrate, or a solvate thereof are presented. Compared with a compound before deuteration, the deuterated compound shows better pharmacokinetics, higher maximum plasma drug concentration, higher exposure, and longer half-life, and has more excellent metabolic performance. The deuterated compound can effectively inhibit FAK activity, and has good application prospect in preparation of FAK inhibitors and/or drugs for treating cancer. In addition, the use of the deuterated compound in combination with an anti-cancer drug (such as a PD-1 inhibitor) can achieve a synergistic effect, thereby significantly improving the tumor suppression effect, and providing a better choice for clinical cancer treatment.
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公开(公告)号:US20210292304A1
公开(公告)日:2021-09-23
申请号:US17255231
申请日:2019-06-21
发明人: Wu DU , Yu LI , Haibo LI , Yuanwei CHEN , Chengzhi ZHANG , Xinghai LI
IPC分类号: C07D403/12
摘要: Disclosed are a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof, wherein R1-R10 are independently selected from H and D, respectively, and not all are H. Compared to the undeuterated control compound MGL3 196, the compound of formula (I) or the optical isomers, pharmaceutically acceptable salts, prodrugs, hydrates or solvates thereof has/have better agonistic activity on thyroid hormone receptor p (THR-p), has/have a longer half-life and a lower clearance rate, has/have better metabolic stability and pharmacokinetic properties, and has/have excellent application prospects in the preparation of THR-p agonists and drugs for treating indications to which THR-p agonists are applicable, including dyslipidemia, hypercholesterolemia, nonalcoholic steatohepatitis (NASH) and nonalcoholic fatty liver disease (NAFLD).
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公开(公告)号:US20230091225A1
公开(公告)日:2023-03-23
申请号:US17594474
申请日:2020-04-16
发明人: Wu DU , Kun WEN , Yiwei FU , Haibin LV , Jinyun HE , Dekun QIN , Yu LI , Jingyi DUAN , Yong LI , Chaowu AI , Zhilin TU , Yuanwei CHEN , Xinghai LI , Haibo LI
IPC分类号: C07D417/12 , C07D413/12 , C07D403/12 , C07D403/06 , C07D401/04 , C07D471/04 , C07D487/04 , C07D413/14 , C07D519/00 , C07D498/22 , C07D491/18 , C07D491/08 , C07D487/10 , C07D487/08 , C07D471/10 , C07D417/14
摘要: Bifunctional chimeric heterocyclic compounds of formula (I) is effective for targeted degradation of androgen receptors and use thereof. The compound of formula (I) also has an isotopic compound, an optical isomer, a tautomer, pharmacologically acceptable salt, a prodrug thereof, or a solvate. In formula (I), ARB is an androgen receptor recognition/binding part, L is a link part, and U is a ubiquitin protease recognition/binding part; and the three parts are connected by means of chemical bonds. The compound can perform targeted degradation on androgen receptors in prostate cancer cells, and suppress proliferation of the prostate cancer cells, and also show good metabolic stability and pharmacokinetic properties. The compound has good application prospect in preparation of targeted chimeras for protein degradation of androgen receptors and in the preparation of drugs for treating related diseases regulated by the androgen receptors.
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公开(公告)号:US20210198247A1
公开(公告)日:2021-07-01
申请号:US16956581
申请日:2018-12-20
发明人: Wu DU , Chaowu AI , Yu LI , Kun WEN , Haibin LV , Wen REN , Jinyun HE , Dekun QIN , Xinghai LI , Yuanwei CHEN
IPC分类号: C07D413/12 , A61P35/00
摘要: Provided is a compound represented by formula (I). Also provided are a pharmaceutical composition containing the compound of formula (I) and use of the compound in preparing indoleamine-2,3-dioxygenase (IDO) inhibitor drugs. The compound or the pharmaceutical composition thereof can be used for preparing drugs for preventing and/or treating diseases having pathological features of IDO-mediated tryptophan metabolic pathways.
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公开(公告)号:US10450274B2
公开(公告)日:2019-10-22
申请号:US15781997
申请日:2016-12-06
发明人: Lei Fan , Wu Du , Xinghai Li , Yuanwei Chen , Kexin Xu , Ke Chen , Shaohua Zhang , Tongchuan Luo
IPC分类号: C07D215/36 , A61K31/47 , A61K31/4709 , C07D401/04 , C07D401/12
摘要: Quinoline compounds and salts, hydrates or solvates serving as a selective uric acid reabsorption inhibitor, can be used in the treatment of hyperuricemia and gout by promoting uric acid to excrete from the body and reducing serum uric acid. Such compounds have the effect of reducing the uric acid in the animal body and human body.
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公开(公告)号:US20210238166A1
公开(公告)日:2021-08-05
申请号:US17054080
申请日:2019-05-06
发明人: Wu DU , Yu LI , Kun WEN , Xinghai LI , Yuanwei CHEN
IPC分类号: C07D403/12
摘要: This disclosure provides a compound as shown in formula (I) or optical isomers, pharmaceutically acceptable salts, hydrates or solvates thereof. In formula (I). R1-R18 are independently selected from hydrogen and deuterium respectively, but not all are hydrogen at the same time. The compound and salts, hydrates or solvates thereof can be used as FAR inhibitors, and used in the preparation of anti-cancer drugs, and compared with the undeuterated control compound Defactinib, the compound has significantly improved metabolic stability and pharmacokinetic properties.
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公开(公告)号:US20210137890A1
公开(公告)日:2021-05-13
申请号:US17142440
申请日:2021-01-06
发明人: Xinghai Li , Yuanwei Chen
IPC分类号: A61K31/4166 , A61P35/00
摘要: Provided herein is a compound of Formula I having androgen receptor antagonistic properties and methods of using the compound to more efficiently and efficaciously reduce the concentration of prostate specific antigen (PSA) and treat male hormone-related diseases such as prostate cancer, breast cancer, alopecia, hair loss, acne and adolescent acne. Also provided are methods of reducing the plasma concentration of prostate specific antigen (PSA) in a subject with elevated PSA comprising administering to the subject a therapeutically effective amount of the compound.
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公开(公告)号:US20210047281A1
公开(公告)日:2021-02-18
申请号:US16967077
申请日:2019-01-31
发明人: Wu DU , Wen REN , Haibin LV , Haibo LI , Kun WEN , Jinyun HE , Dekun QIN , Xinghai LI , Yuanwei CHEN
IPC分类号: C07D271/08 , C07D413/12
摘要: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.
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公开(公告)号:US09708289B2
公开(公告)日:2017-07-18
申请号:US14889032
申请日:2014-05-27
发明人: Yuanwei Chen , Yu Gong
IPC分类号: A61K31/44 , C07D211/00 , C07D401/04
CPC分类号: C07D401/04
摘要: Provided are imidazolidinedione compounds of formula (I), processes for preparation, uses and pharmaceutically compositions thereof. Said imidazolidinedione compounds possess androgen receptor antagonist activity and can be used for preventing and treating diseases and disorders related to androgen receptor, such as prostate cancer, alopecia, hair regeneration, acne and adolescent acne.
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公开(公告)号:US11591301B2
公开(公告)日:2023-02-28
申请号:US16967077
申请日:2019-01-31
发明人: Wu Du , Wen Ren , Haibin Lv , Haibo Li , Kun Wen , Jinyun He , Dekun Qin , Xinghai Li , Yuanwei Chen
IPC分类号: C07D271/08 , C07D413/12
摘要: A compound is represented by formula (I). A pharmaceutical composition contains the compound of formula (I). The compound is used in the preparation of an indoleamine-2,3-dioxygenase (IDO) inhibitor drug. The compound exhibits inhibition effect on IDO protease and metabolizes stably in the body. The compound or pharmaceutical composition thereof can be used for preparing an IDO inhibitor drug, and can also be used for preparing a drug for preventing and/or treating diseases having IDO-mediated tryptophan metabolic pathway pathological features.
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