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1.发明申请公开(公告)号：US20250066360A1
公开(公告)日：2025-02-27
申请号：US18728864
申请日：2023-01-16
Inventor： Jiaqiang Dong , Xinxian Deng , Wensheng Yu , Fangfang Jin , Zhen Gong
IPC: C07D471/14 , A61K31/444 , A61K31/506 , C07D401/14
Abstract: The present invention relates to a pyridine-containing polycyclic derivative, and a preparation method therefor and the use thereof. In particular, the present invention relates to a compound as represented by general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and the use thereof as a biological regulator in the preparation of a medicament for the treatment of autoimmune diseases, chronic inflammatory diseases, acute inflammatory diseases, autoinflammatory diseases, atherosclerosis, diabetes, fibrotic diseases, metabolic diseases, cancers, tumors, leukemia and lymphoma, wherein the definition of each substituent in general formula (I) is the same as that in the description.
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公开(公告)号：US20240376108A1
公开(公告)日：2024-11-14
申请号：US18569184
申请日：2022-06-09
Inventor： Hua Dong , Linsong Guo
IPC: C07D471/14 , A61K31/519
Abstract: An acid salt and a crystal form of a pyrazole-containing polycyclic derivative represented by formula (I-a), and a preparation method therefor, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and an intermediate for preparing the derivative. In particular, the present invention relates to the use of the salt and the crystal form of the compound represented by general formula (I-a) as a P2X3 inhibitor in the preparation of a drug for treating neurogenic diseases.
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3.发明公开公开(公告)号：US20240254109A1
公开(公告)日：2024-08-01
申请号：US18558165
申请日：2022-04-27
Inventor： Jinyao Chen , Yuanyuan Li
IPC: C07D403/12 , A61K31/496 , A61K31/551 , A61P25/18 , C07D241/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC classification number: C07D403/12 , A61K31/496 , A61K31/551 , A61P25/18 , C07D241/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
Abstract: Provided are a salt containing a piperazine polycyclic derivative, a crystal form thereof, a preparation method therefor, and the use thereof. In particular, the present invention relates to a salt containing a compound of general formula (I) and a stereoisomer thereof, a crystal form of the salt, a preparation method, a pharmaceutical composition containing a therapeutically effective amount of the crystal form, and the use as a G protein-coupled receptor regulator in treatment or prevention of central nervous system diseases and/or mental diseases.
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公开(公告)号：US20240165252A1
公开(公告)日：2024-05-23
申请号：US18263091
申请日：2022-01-26
Inventor： Haiqing Hua , Dongjie Mao , Yan Luo , Yuejun Xie
IPC: A61K47/68 , A61P35/00 , C07D491/22 , C07K16/28
CPC classification number: A61K47/68037 , A61K47/6849 , A61P35/00 , C07D491/22 , C07K16/2878
Abstract: An anti-BCMA antibody-drug conjugate, or a pharmaceutically acceptable salt or solvent compound thereof, and the medical use thereof. Specifically, the antibody-drug conjugate is formed by connecting an anti-BCMA antibody or an antigen-binding fragment thereof and an exatecan derivative by using a linker, and the antibody-drug conjugate or the pharmaceutically acceptable salt or solvent compound thereof has a significant anti-tumor effect and good safety.
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公开(公告)号：US11661437B2
公开(公告)日：2023-05-30
申请号：US16969137
申请日：2019-01-31
Inventor： Yidong Su , Xiaopo Chen , Jun Wang , Rudi Bao
CPC classification number: C07J43/003 , A61P25/08 , A61P25/24 , C07J7/009 , C07J41/005 , C07J41/0094 , C07J53/004
Abstract: Steroid derivative regulators, a method for preparing the same, and uses thereof are described. Specifically, a compound as shown in formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and uses thereof as a regulator of GABA A receptor for treating depression, convulsion, Parkinson's disease, and nervous system diseases are described, wherein the substituents of the formula (I) are as defined in the description.
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Patent Agency Ranking
公开(公告)号：US20230118497A1
公开(公告)日：2023-04-20
申请号：US17784256
申请日：2020-12-07
Inventor： Hualing XIAO , Qiang LIU , Xingyun LU , Jiaqiang CAI , Rudi BAO
IPC: C07D471/14 , C07D513/14 , C07D498/14
Abstract: Provided are a pyrazole-containing polycyclic derivative inhibitor, a preparation method therefor and an application thereof. In particular, provided are a compound as represented by formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, and an application thereof as a P2X3 inhibitor in treatment of P2X3 receptor function disorders, particularly in treatment of neurogenic diseases, wherein the substituents in the formula (I) are the same as those in the description in definition.
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公开(公告)号：US10428081B2
公开(公告)日：2019-10-01
申请号：US16207968
申请日：2018-12-03
Inventor： Mingsong Wei , Guangjun Sun , Songliang Tan , Peng Gao , Shaobao Wang , Wenhua Xiu , Fujun Zhang , Rudi Bao
IPC: C07D471/04 , C07D491/107 , C07D403/12 , C07D405/14 , A61K31/505 , A61K31/506 , A61K31/675 , C07F9/53 , C07D403/04 , C07D405/12 , C07D239/48 , C07D471/10 , C07D413/14 , C07D471/06 , C07D491/10
Abstract: Epidermal growth factor receptor (EGFR) inhibitors are provided. In particular, 4-substituted-2-(N-(5-substituted ally amide)phenyl)amino)pyrimidine derivatives of formula (I), a preparation method and use thereof as an EGFR inhibitor are provided. The 4-substituted-2-(N-(5-substituted ally amide)phenyl)amino)pyrimidine derivatives of formula (I) have inhibitory activity against the L858R EGFR mutant, the T790M EGFR mutant and the exon 19 deletion activating mutant, and can be used to treat diseases mediated alone or in part by EGFR mutant activity. The derivatives of formula (I) can be used to treat and/or prevent cancers, particularly non-small cell lung cancer.
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公开(公告)号：US20190284220A1
公开(公告)日：2019-09-19
申请号：US16317636
申请日：2017-07-21
Inventor： Xiang LI , Jun YU , Haizhou YU , Jinjia WANG , Lei HE , Zuyin DU
IPC: C07H7/04
Abstract: Disclosed are a crystal form of a dapagliflozin intermediate and a preparation method therefor, and specifically disclosed are a crystal form of the dapagliflozin intermediate (2S,3R,4S,5S,6R)-2-(4-chloro-3 -(4-ethoxybenzyOphenyl)-2-ethoxy-6-(methylhydroxyl) tetrahydro-2H-pyran-3,4,5-triol and a preparation method therefor. The advantages thereof lie in that an intermediate can be highly purified to obtain a sample with a purity of 99.3% or more, which has an important significance for improving the quality of the dapagliflozin, and the preparation process is simple and suitable for industrial production.
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公开(公告)号：US20180280392A1
公开(公告)日：2018-10-04
申请号：US15524394
申请日：2015-11-06
Inventor： Jin ZENG , Ruijun WANG , Xiaolei WANG
IPC: A61K31/519 , A61K9/20 , A61K9/28 , A61K9/48
Abstract: Disclosed is a pharmaceutical preparation having 6-acetyl-8-cyclopentyl-5-methyl-2-(5-piperazine-1-yl-pyridine-2-yl amino group)-8H-pyrido[2,3-d]pyrimidine-7-one or salt thereof as an active ingredient, the salt comprising hydrochloride or isethionate, and the dosage form thereof comprising tablets and capsules both having good stability and excellent dissolution performance.
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10.发明申请公开(公告)号：US20170210760A1
公开(公告)日：2017-07-27
申请号：US15328795
申请日：2015-07-30
IPC: C07D519/00
CPC classification number: C07D519/00 , A61K31/5383 , C07B2200/13
Abstract: Crystalline free bases and crystalline acid salts of 9-((8-fluoro-6-(1-methyl-1H-pyrazol-4-yl)-[1,2,4]triazolo[4,3-a]pyridine-3-yl)thio)-4-methyl-2H-[1,4]oxaazido [3,2-c]quinoline-3(4H)-one are disclosed as C-Met inhibitors. Their preparation methods and uses are also described. In particular, crystal forms I, II, III and IV of the free base; crystal form I of the hydrochloride salt; crystal forms I and II of the sulfate salt; crystal forms I, II, III and IV of the phosphate salt; crystal forms I, II, III, IV and V of the mesylate salt; crystal forms I, and III of the p-toluenesulfonate salt; and crystal forms I, II and III of the 1,5-naphthalenedisulfonate salt are disclosed. Also disclosed are methods for preparing the above-mentioned crystal forms, pharmaceutical compositions thereof, methods for regulating the catalytic activity of a protein kinase, and methods of treating protein kinase-related diseases.
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