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公开(公告)号：US12122784B2
公开(公告)日：2024-10-22
申请号：US17283012
申请日：2019-08-26
发明人： Jiandong Yuan , Xinliang Fu , Zhanli Sun , Xiaopei Xing , Jingcheng Hui , Qilei Cong
IPC分类号： C07D487/18 , C07D515/22
CPC分类号： C07D487/18 , C07D515/22
摘要： The present invention provides a method for preparing an ecteinascidin compound and an intermediate thereof, and specifically provides a preparation method for a novel compound QT9, and a method of using QT9 to prepare an ecteinascidin compound. The method provided by the present invention has high reaction selectivity and high yield, the obtained compound is easy to purify, and defects in the prior art that multiple intermediates are oily substances, and the reaction selectivity is poor are solved. The method of the present invention is particularly applicable to industrial production.
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公开(公告)号：US10913756B2
公开(公告)日：2021-02-09
申请号：US16706315
申请日：2019-12-06
发明人： Jiandong Yuan , Yangqing Huang , Linfeng Miao , Jianing Gu , Chaohua Liang , Zhengye Wang , Zhanli Sun
摘要： The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.
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公开(公告)号：US10759905B2
公开(公告)日：2020-09-01
申请号：US16064317
申请日：2016-12-21
发明人： Jiandong Yuan , Fenghua Meng , Yan Zou , Yuan Fang , Zhiyuan Zhong
IPC分类号： C08G64/18 , C08G64/30 , A61K49/18 , A61K47/62 , A61K47/68 , A61K9/127 , A61K47/34 , C08G64/02 , C08G64/08 , B82Y5/00
摘要： Disclosed in the present disclosure is a biodegradable amphiphilic polymer containing disulfide in the side chain, a self-crosslinked polymeric vesicle thereof and an application in the targeted therapy of lung cancer. The polymer is obtained by an activity-controllable ring-opening polymerization based on a cyclic carbonate monomer containing a functional group of dithiolane ring, which has a controllable molecular weight and a narrow molecular weight distribution, and does not require processes of protection and deprotection; the polymer obtained by the ring-opening polymerization of the cyclic carbonate monomer of the present disclosure has biodegradability and can be used to control the drug release system, the prepared lung cancer-targeted reduction-sensitive reversibly-crosslinked polymeric vesicle as a nanomedicine carrier supports stable long circulation in vivo. However, it is highly enriched in lung cancer tissues, enter cells efficiently, and rapidly decrosslinks in the cells to release drugs, so as to kill cancer cells with high potency and specificity and inhibit the growth of tumor effectively without causing toxic and side effects.
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公开(公告)号：US20240209056A1
公开(公告)日：2024-06-27
申请号：US18283164
申请日：2022-03-23
发明人： Jiandong YUAN , Yunsong SONG , Wenteng ZHEN , Yue CAI , Jianing GU , Yangqing HUANG
IPC分类号： C07K14/605 , A61K38/00 , A61P3/04 , A61P3/10
CPC分类号： C07K14/605 , A61P3/04 , A61P3/10 , A61K38/00
摘要： A GIP and GLP-1 dual receptor agonist, a pharmaceutical composition, and the use. In particular, the present application relates to a compound represented by formula I, a pharmaceutical composition comprising the compound, and the use of the compound as a GIP and GLP-1 dual receptor agonist in the field of medicine. The compound represented by formula I exhibits excellent GIPR and GLP-1R agonist activity and excellent pharmaceutical activity in reducing blood sugar and controlling body weight, is a therapeutic drug having a clinical application prospect, and can be used for preventing and treating diseases such as diabetes, diabetes complications, obesity, or obesity complications.
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公开(公告)号：US20220096644A1
公开(公告)日：2022-03-31
申请号：US17431541
申请日：2020-02-17
发明人： Jiandong Yuan , Yangqing Huang , Yunsong Song
IPC分类号： A61K47/60 , A61K31/4745 , A61K47/64
摘要： Disclosed is a class of multi-branched drug conjugates capable of specifically targeting CD44. The class of compounds specifically binds to CD44, and may target tumor cells and tissues having high expression of CD44, so that the concentration of the conjugate in a target tissue is high, the clinical treatment effect thereof is improved, and toxicity is reduced. The compound of the present invention is suitable for treating all tumors having high expression of CD44, comprising but not limited to gastric cancer, pancreatic cancer, small cell lung cancer, colon cancer, breast cancer, lung adenocarcinoma, liver cancer, nasopharyngeal carcinoma, malignant glioma, lymphoma, renal carcinoma, ovarian cancer, head and neck cancer, squamous cell carcinoma, and the like.
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公开(公告)号：US20200000797A1
公开(公告)日：2020-01-02
申请号：US16300428
申请日：2017-05-15
发明人： Jiandong Yuan , Yangqing Huang , Yunsong Song , Fang Yuan
摘要： Disclosed is a multi-arm targeting drug conjugate modified by a water-soluble polymer; the drug conjugate has the structural formula of (III). In formula (III), R is an organic core, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is a camptothecin-based drug, and q is any integer between 3 and 8. The drug conjugate may improve the poor water solubility, high toxicity and low bioavailability of camptothecin-based drugs.
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公开(公告)号：US20180244710A1
公开(公告)日：2018-08-30
申请号：US15754009
申请日：2016-09-13
发明人： Jiandong Yuan , Yangqing Huang , Lingfeng Miao , Jianing Gu , Chaohua Liang , Zhengye Wang , Zhanli Sun
摘要： Provided is a preparation method of a composition enriched in compound Sp-1. The method performs isomer separation on a reaction product from the first step, and then performs a two-step chemical synthesis, so as to prepare a composition comprising high-purity compound Sp-1, wherein the HPLC purity of the single isomer Sp-1 is 90% or more. Provided is a composition enriched in compound Sp-1. The composition has an inhibitory effect on tumor cell proliferation in vitro significantly higher than that of NUC-1031 and compound Rp-1. Also provided are the use of the composition, and a pharmaceutical composition comprising the composition and at least one pharmaceutically acceptable excipient.
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公开(公告)号：US11191843B2
公开(公告)日：2021-12-07
申请号：US16498765
申请日：2018-04-19
发明人： Jiandong Yuan , Yangqing Huang , Yunsong Song , Haifeng Ding
IPC分类号： A61K47/64 , A61K47/60 , A61K47/65 , A61P35/00 , A61K31/4745
摘要： A multi-branched drug conjugate of formula (I) or a pharmaceutically acceptable salt thereof. In the formula, R is an organic center, POLY is a polymer, L is a multivalent linker, T is a targeting molecule, D is an active agent, and q is any integer between 3 and 8. The symbol “*” in L represents a junction point of the multivalent linker L and the targeting molecule T, “#” represents a junction point of the multivalent linker L and the active agent D, and “%” represents a junction point of the multivalent linker L and POLY. 1 is any integer between 2 and 20, and m and n are each an integer between 0 and 10. T is iRGD, cRGD, tLyp-1, Lyp-1, RPARPAR, Angiopep2, or GE11. D is a camptothecin drug.
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公开(公告)号：US10689413B2
公开(公告)日：2020-06-23
申请号：US15754009
申请日：2016-09-13
发明人： Jiandong Yuan , Yangqing Huang , Linfeng Miao , Jianing Gu , Chaohua Liang , Zhengye Wang , Zhanli Sun
IPC分类号： C07H19/10 , A61K31/7068 , C07H1/02 , A61P35/00
摘要： Provided is a preparation method of a composition enriched in compound Sp-1. The method performs isomer separation on a reaction product from the first step, and then performs a two-step chemical synthesis, so as to prepare a composition comprising high-purity compound Sp-1, wherein the HPLC purity of the single isomer Sp-1 is 90% or more. Provided is a composition enriched in compound Sp-1. The composition has an inhibitory effect on tumor cell proliferation in vitro significantly higher than that of NUC-1031 and compound Rp-1. Also provided are the use of the composition, and a pharmaceutical composition comprising the composition and at least one pharmaceutically acceptable excipient.
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公开(公告)号：US10538541B2
公开(公告)日：2020-01-21
申请号：US15754318
申请日：2016-09-13
发明人： Jiandong Yuan , Yangqing Huang , Linfeng Miao , Jianing Gu , Chaohua Liang , Zhengye Wang , Zhanli Sun
摘要： The present disclosure involves a composition enriched in compound 61501b, wherein the compound 61501b has a purity of not less than 90% or more. The composition has a significant advantage in preparing a high-purity compound Sp-1. In addition, the present disclosure also provides a preparation method of the composition enriched in compound 61501b. The method adopts a crystallization technique to perform separation and purification, has a simple and convenient operation and good reproducibility, and therefore the compound 61501b in the prepared composition has high purity and quality. Further, the present disclosure also involves a novel crystal form of compound 61501b.
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