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1.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
发明人： Jinyao Chen , Yuanyuan Li
IPC分类号： C07D403/12 , A61K31/496 , A61K31/551 , A61P25/18 , C07D241/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
CPC分类号： C07D403/12 , A61K31/496 , A61K31/551 , A61P25/18 , C07D241/04 , C07D401/12 , C07D405/12 , C07D409/12 , C07D413/12 , C07D417/12
摘要： 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
发明人： Haiqing Hua , Dongjie Mao , Yan Luo , Yuejun Xie
IPC分类号： A61K47/68 , A61P35/00 , C07D491/22 , C07K16/28
CPC分类号： A61K47/68037 , A61K47/6849 , A61P35/00 , C07D491/22 , C07K16/2878
摘要： 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
发明人： Yidong Su , Xiaopo Chen , Jun Wang , Rudi Bao
CPC分类号： C07J43/003 , A61P25/08 , A61P25/24 , C07J7/009 , C07J41/005 , C07J41/0094 , C07J53/004
摘要： 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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公开(公告)号：US20230118497A1
公开(公告)日：2023-04-20
申请号：US17784256
申请日：2020-12-07
发明人： Hualing XIAO , Qiang LIU , Xingyun LU , Jiaqiang CAI , Rudi BAO
IPC分类号： C07D471/14 , C07D513/14 , C07D498/14
摘要： 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
发明人： Mingsong Wei , Guangjun Sun , Songliang Tan , Peng Gao , Shaobao Wang , Wenhua Xiu , Fujun Zhang , Rudi Bao
IPC分类号： 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
摘要： 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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6.发明公开公开(公告)号：US20240228490A1
公开(公告)日：2024-07-11
申请号：US18555468
申请日：2022-04-22
发明人： Peng Gao , Mi Zeng , Shaobao Wang , Wensheng Yu
IPC分类号： C07D471/04 , A61P35/00 , C07D401/14 , C07D413/14 , C07D498/04 , C07D519/00
CPC分类号： C07D471/04 , A61P35/00 , C07D401/14 , C07D413/14 , C07D498/04 , C07D519/00
摘要： A heterocyclic derivative inhibitor and a preparation method therefor and an application thereof. Specifically, the present invention relates to a compound represented by general formula (I), a preparation method therefor, a pharmaceutical composition comprising said compound, and an application of same as an inhibitor for treatment of cancers, wherein substituents in general formula (I) are as defined in the description.
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7.发明公开公开(公告)号：US20230271969A1
公开(公告)日：2023-08-31
申请号：US18017666
申请日：2021-07-30
发明人： Yidong Su , Feng Wang , Kailong Li , Wu Zhang , Rudi Bao
IPC分类号： C07D487/04 , C07D519/00
CPC分类号： C07D487/04 , C07D519/00 , C07B2200/05
摘要： A nitrogen-containing fused ring derivative inhibitor, a preparation method therefor and the use thereof. The present invention particularly relates to a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition thereof, and the use thereof as an NK inhibitor in the treatment of depression, anxiety, schizophrenia, sex hormone-dependent diseases and other related diseases. The various substituents in general formula (I) have the same definition as that in the description.
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公开(公告)号：US20230072897A1
公开(公告)日：2023-03-09
申请号：US17596239
申请日：2020-06-08
发明人： Haiqing HUA , Suxia LIU , Rudi BAO
摘要： Provided are an anti-B7-H4 antibody-drug conjugate and medicinal use thereof. Specifically, provided is an anti-B7-H4 antibody or antigen-binding fragment thereof, a humanized antibody comprising the CDR region of the anti-B7-H4 antibody, and antibody-drug conjugate thereof or pharmaceutically acceptable salt or solvent compound thereof, and the aforesaid antibody-drug conjugate thereof or pharmaceutical composition of a pharmaceutically acceptable salt or solvent compound thereof, and use thereof as an anti-cancer drug, particularly the use in the preparation of a drug for treating diseases or disorders having high expression of B7-H4.
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9.发明申请公开(公告)号：US20230043863A1
公开(公告)日：2023-02-09
申请号：US17298578
申请日：2019-11-29
IPC分类号： C07D519/00 , C07D451/04 , C07D471/04 , C07D495/04 , C07D401/14
摘要： The present invention relates to heteroaromatic derivatives for use as a regulator, a preparation method therefor and a use thereof. In particular, disclosed are compounds represented by general formula (I), preparation methods therefor, pharmaceutical compositions comprising said compounds, and a use thereof as Janus kinase inhibitors in treating inflammatory diseases and tumor-related diseases.
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公开(公告)号：US11472882B2
公开(公告)日：2022-10-18
申请号：US16967016
申请日：2019-02-01
发明人： Rudi Bao , Haiqing Hua , Suxia Liu , Fujun Zhang , Ting Wang
IPC分类号： A61K39/395 , A61K39/00 , C07K16/00 , C07K16/46 , C07H21/04 , G01N33/53 , C12N5/20 , C12N15/00 , C07K16/28
摘要： An anti-B7-H4 antibody, an antigen-binding fragment thereof and pharmaceutical use thereof. A chimeric antibody and a humanized antibody comprising a CDR region of the anti-B7-H4 antibody, a pharmaceutical composition comprising the anti-B7-H4 antibody and the antigen-binding fragment thereof, and use thereof as an anti-cancer medicament. A humanized anti-B7-H4 antibody and use thereof in the preparation of a medicament for treating diseases or conditions mediated by B7-H4.
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