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公开(公告)号：US20210198275A1
公开(公告)日：2021-07-01
申请号：US17058151
申请日：2019-05-10
Inventor： Yuguang WANG , Nong ZHANG , Pingjing ZHANG
IPC: C07D495/04
Abstract: Disclosed are a salt of a fused ring pyrimidine compound, a crystal form thereof and a preparation method therefor and the use thereof. The fused ring pyrimidine compound is N-[7-(4-fluoro-2-methoxyphenyl)-6-methylthieno[3,2-d]pyrimidin-2-yl]-1-(piperidin-4-yl)-1H-pyrazol-4-amine, having a structure as shown in formula 1. The preparation methods in the invention for the salt of the fused ring pyrimidine compound and the crystal form thereof are simple; and the salt of the fused ring pyrimidine compound and the crystal form thereof at least have the characteristics of having a better stability, not easily absorbing moisture, being of a polycrystalline type, having a chemical stability and pharmacokinetics, and having an improved solubility.
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公开(公告)号：US20230046904A1
公开(公告)日：2023-02-16
申请号：US17761097
申请日：2020-09-17
Inventor： Yuguang WANG , Feilan WANG , Nong ZHANG
IPC: A61K31/198 , A61K39/395 , A61K45/06
Abstract: The invention provides methods for treating a cancer, comprising administering to a subject in need thereof a therapeutically effective amount of a small molecule inhibitor of the PD-1/PD-L1 interaction or a pharmaceutically acceptable salt or prodrug thereof in combination with a therapeutically effective amount of an anti-PD-1 antibody, wherein the small molecule inhibitor of the PD-1/PD-L1 interaction is not a protein.
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公开(公告)号：US11352368B2
公开(公告)日：2022-06-07
申请号：US17058151
申请日：2019-05-10
Inventor： Yuguang Wang , Nong Zhang , Pingjing Zhang
IPC: C07D495/04 , A61K31/519 , A61P35/00 , A61P35/02 , C07C57/15
Abstract: Disclosed are a salt of a fused ring pyrimidine compound, a crystal form thereof and a preparation method therefor and the use thereof. The fused ring pyrimidine compound is N-[7-(4-fluoro-2-methoxyphenyl)-6-methylthieno[3,2-d]pyrimidin-2-yl]-1-(piperidin-4-yl)-1H-pyrazol-4-amine, having a structure as shown in formula 1. The preparation methods in the invention for the salt of the fused ring pyrimidine compound and the crystal form thereof are simple; and the salt of the fused ring pyrimidine compound and the crystal form thereof at least have the characteristics of having a better stability, not easily absorbing moisture, being of a polycrystalline type, having a chemical stability and pharmacokinetics, and having an improved solubility.
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公开(公告)号：US10259816B2
公开(公告)日：2019-04-16
申请号：US15568999
申请日：2016-04-22
Inventor： Nong Zhang , Zusheng Xu , Tinghan Wang , Yuguang Wang
IPC: C07D487/04 , C07D401/14 , C07D405/14 , A61K31/517 , A61K31/519 , A61K31/5377 , C07D401/12 , C07D405/12 , C07D495/04 , C07D239/78 , A61P35/00 , C07D409/14
Abstract: Disclosed are a condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b′ to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.
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公开(公告)号：US20230192653A1
公开(公告)日：2023-06-22
申请号：US17911053
申请日：2021-03-08
Inventor： Yuguang WANG , Zhenhua FENG , Feilan WANG
IPC: C07D401/14 , C07K16/28 , A61P35/00
CPC classification number: C07D401/14 , C07K16/2896 , A61P35/00 , C07B2200/13
Abstract: The disclosure provides new therapeutic uses for certain fused ring pyrimidine compounds, in particular for treating patients having a cancer which expresses elevated fibroblast growth factor receptor oncogene partner 2 (FGFR1OP2) and/or elevated FGFR1, or expresses a FGFR1-FGFR1OP2 fusion protein, and for treating patients who are being treated with an immune checkpoint inhibitor.
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Patent Agency Ranking
公开(公告)号：US20220313626A1
公开(公告)日：2022-10-06
申请号：US17621576
申请日：2020-06-23
Inventor： Yugang WANG , Feilan WANG , Nong ZHANG
IPC: A61K31/137 , A61K31/198 , A61K31/357 , A61K31/277 , A61K31/397 , A61K31/401 , A61K31/454 , A61K31/4196 , A61K31/4025 , A61K31/423 , A61K31/4545 , A61P35/02
Abstract: Provided herein are methods for treating a cancer in a subject having a tumor with interstitial fluid pressure (IFP) of at least 10 mmHg, comprising administering to the subject a therapeutically effective amount of a compound or a pharmaceutically acceptable salt or prodrug thereof, which is an inhibitor of the interaction between the PD-1 receptor and its ligand PD-L1 and which is not a protein, alone, or in combination with other agents, e.g., in combination with the use of anti-PD-1/PD-L1 antibodies, in combination with an inhibitor of the CTLA-4/B7 interaction, or in combination with an inhibitor binding to VEFG.
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公开(公告)号：US11078192B2
公开(公告)日：2021-08-03
申请号：US16315307
申请日：2017-07-04
Inventor： Yuguang Wang , Zusheng Xu , Tianzhi Wu , Min He , Nong Zhang
IPC: C07D405/10 , C07D405/04 , C07D207/08 , C07D211/60 , C07D213/38 , C07D213/48 , C07D231/10 , C07D231/12 , C07D319/18 , A61P35/00 , C07C22/04 , C07C22/08 , C07C25/24 , C07C43/225 , C07C47/548 , C07C47/55 , C07C47/575 , C07C69/94 , C07C215/10 , C07C217/58 , C07C229/22 , C07C229/24 , C07C229/64 , C07C233/18 , C07C235/84 , C07C237/30 , C07C255/56
Abstract: Disclosed are an aromatic acetylene or aromatic ethylene compound, an intermediate, a preparation method, a pharmaceutical composition and a use thereof. The aromatic acetylene or aromatic ethylene compound has a significant inhibitory effect on PD-1 and PD-L1, and can effectively relieve or treat cancers and other related diseases.
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公开(公告)号：US20180127420A1
公开(公告)日：2018-05-10
申请号：US15568999
申请日：2016-04-22
Inventor： Nong ZHANG , Zusheng XU , Tinghan WANG , Yuguang WANG
IPC: C07D487/04 , C07D239/78 , C07D401/12 , C07D401/14 , C07D405/12 , C07D495/04 , A61P35/00 , C07D409/14
CPC classification number: C07D487/04 , A61K31/517 , A61K31/519 , A61K31/5377 , A61P35/00 , C07D239/78 , C07D401/12 , C07D401/14 , C07D405/12 , C07D405/14 , C07D409/14 , C07D495/04
Abstract: Disclosed area condensed-ring pyrimidylamino derivative, a preparation method therefor, and an intermediate, a pharmaceutical composition and applications thereof. The method for preparing the condensed-ring pyrimidylamino derivative comprises: in a solvent, in the presence of a palladium-containing catalyst, allowing a compound represented by formula I-a and a compound represented by formula I-b′ to have a coupling reaction, and then preparing a compound represented by formula I by means of a deprotection reaction. Also disclosed applications of the condensed-ring pyrimidylamino derivative in the preparation of drugs for preventing, relieving and/or treating tumors or diseases caused by an anaplastic lymphoma kinase. The condensed-ring pyrimidylamino derivative of the present invention has an obvious restraint effect on the anaplastic lymphoma kinase.
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公开(公告)号：US20230144170A1
公开(公告)日：2023-05-11
申请号：US17909753
申请日：2021-02-26
Inventor： Yuguang WANG , Tianzhi WU , Nong ZHANG
IPC: C07D495/04 , C07D401/04 , C07D211/46 , B01J23/42 , B01J21/18 , B01J31/28 , B01J31/24
CPC classification number: C07D495/04 , C07D401/04 , C07D211/46 , B01J23/42 , B01J21/18 , B01J31/28 , B01J31/2404
Abstract: Disclosed are a thienopyrimidine derivative and a preparation method therefor. Provided is a method for preparing a compound as shown in formula B, which method is characterized by comprising the following steps: subjecting a compound as shown in formula C with a compound as shown in formula K to a coupling reaction as shown below under a protective gas atmosphere, in a solvent and in the presence of a catalyst and a base, wherein the catalyst comprises a palladium compound and a phosphine ligand. The preparation method of the present invention can improve the yield of products, and reduce the production cost; in addition, the preparation method has simple reaction conditions and a strong process operability, which is beneficial to industrial production and the reduction of the generation of three wastes.
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10.发明申请公开(公告)号：US20230115605A1
公开(公告)日：2023-04-13
申请号：US17912142
申请日：2021-03-02
Inventor： Yuguang WANG , Nong ZHANG , Pingjing ZHANG
IPC: C07C229/22 , C07C227/42
Abstract: Disclosed in the present invention are a crystal form of aromatic vinyl derivatives, and a preparation method therefor and the use thereof. Specifically disclosed in the present invention are crystal form A, crystal form B and crystal form C of a compound as shown in formula I. The crystal forms of the present invention have a good stability, are less hygroscopic and are easy to prepare, and have an important value in terms of the optimization and development of drugs.
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