公开(公告)号：US11447512B2

公开(公告)日：2022-09-20

申请号：US16955482

申请日：2018-12-06

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： A61K31/675 ,  C07F9/6561 ,  A61P31/20 ,  A61P31/18

摘要： An antiviral nucleoside reverse transcriptase inhibitor compound as shown in formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form or an isotopic derivative of the compound. A preparation method therefor, a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV).

公开(公告)号：US11319317B2

公开(公告)日：2022-05-03

申请号：US17098675

申请日：2020-11-16

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao ,  Yixin Ai

IPC分类号： C07D417/14 ,  A61P35/00 ,  C07D401/14

摘要： Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition including the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase, for preparing a plurality of drugs including an anti-tumour drug.

公开(公告)号：US20210093650A1

公开(公告)日：2021-04-01

申请号：US16954824

申请日：2018-12-04

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： A61K31/675 ,  C07F9/6561 ,  A61P31/14 ,  A61P31/18

摘要： The present invention relates to a compound of a novel antiviral nucleoside reverse transcriptase inhibitor, a pharmaceutical composition containing the compound, and preparation and application of the compound. Specifically, disclosed in the present invention are a fused pyrimidine compound as represented by formula (I) and a pharmaceutical composition comprising the compound, or a pharmaceutically acceptable salt, stereoisomer, solvate, hydrate, crystal form, prodrug or isotopic derivative of the compound. The compound of the present invention can be used for treatment and/or prevention of infectious diseases caused by viruses, such as human immunodeficiency virus (HIV), hepatitis B virus (HBV).

公开(公告)号：US11453672B2

公开(公告)日：2022-09-27

申请号：US16956057

申请日：2018-12-18

申请人： SHENZHEN TARGETRX, INC.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： A61K31/519 ,  C07D487/04

摘要： Provided are pharmaceutical compositions comprising substituted pyrazolo[1,5-a]pyrimidine compounds and the use thereof. The compositions may comprise the substituted pyrazolo[1,5-a]pyrimidine compound or a pharmaceutically acceptable salt, prodrug, hydrate or solvate, polymorph, stereoisomer or isotopic variant thereof, and can be used for treating diseases treatable with Trk kinase inhibitors.

公开(公告)号：US20200369696A1

公开(公告)日：2020-11-26

申请号：US16955482

申请日：2018-12-06

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： C07F9/6561 ,  A61P31/18 ,  A61P31/20 ,  A61K31/675

摘要： An antiviral nucleoside reverse transcriptase inhibitor compound as shown in formula (I), and a pharmaceutically acceptable salt, a stereoisomer, a solvate, a hydrate, a crystal form or an isotopic derivative of the compound. A preparation method therefor, a pharmaceutical composition thereof, and a use thereof in the preparation of a drug for treating and/or preventing viral infectious diseases, such as human immunodeficiency virus (HIV) and hepatitis B virus (HBV).

公开(公告)号：US20230322717A1

公开(公告)日：2023-10-12

申请号：US17920001

申请日：2021-04-20

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： C07D401/14 ,  A61K9/20

CPC分类号： C07D401/14 ,  A61K9/2009 ,  A61K9/2013 ,  A61K9/2018 ,  A61K9/2054 ,  C07B2200/13

摘要： Provided are a crystal form of a free base or a pharmaceutically acceptable salt of (R)-N-(4-(chlorodifluoromethoxy)phenyl)-6-(3-fluoropyrrolidin-1-yl)-5-(pyrazin-2-yl)nicotinamide (compound A), a preparation method therefor, and use of the compound in preparation of drugs for treating diseases mediated by Bcr-Abl kinase and mutants thereof, such as chronic granulocytic leukemia. Also provided are a method for preparing compound A, and a preparation containing compound A.

公开(公告)号：US11358973B2

公开(公告)日：2022-06-14

申请号：US17047877

申请日：2019-04-10

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao ,  Yixin Ai

IPC分类号： C07D471/22 ,  C07D487/04 ,  C07D487/22 ,  C07D498/22 ,  A61K31/04 ,  A61K31/519 ,  A61P29/00 ,  A61P25/04 ,  A61P25/28 ,  A61P35/00 ,  C07D487/18 ,  C07D498/18

摘要： A di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation and the use thereof. Specifically, disclosed are a di(hetero)aryl macrocyclic compound represented by formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug or an active metabolite thereof, a pharmaceutical composition comprising said compound and the derivative thereof, and methods of using the same, including methods of treating cancers, pain, neurological diseases, autoimmune diseases and inflammation.

公开(公告)号：US11345703B2

公开(公告)日：2022-05-31

申请号：US16964069

申请日：2019-01-23

申请人： SHENZHEN TARGETRX, INC.

发明人： Yihan Wang ,  Jiuyang Zhao

IPC分类号： C07D471/22

摘要： Provided are a pharmaceutical composition of a substituted pyrazolo[1,5-a]pyrimidine macrocyclic compound and the use thereof. The pyrazolo[1,5-a]pyrimidine macrocyclic compound is a compound as shown in formula (Aa), or a pharmaceutically acceptable salt, a prodrug, a hydrate or a solvate, a crystal form, a stereoisomer or an isotopic variant thereof. The compound of the present invention is an inhibitor of the Trk kinase, and can be used for treating pain, cancers, inflammation, neurodegenerative diseases and certain infectious diseases.

公开(公告)号：US20210171542A1

公开(公告)日：2021-06-10

申请号：US17047877

申请日：2019-04-10

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao ,  Yixin Ai

IPC分类号： C07D498/22 ,  A61P35/00 ,  C07D498/18 ,  C07D487/18 ,  C07D487/22 ,  C07D471/22

摘要： A di(hetero)aryl macrocyclic compound having an inhibitory effect on protein kinase activity, preparation therefor and the use thereof. Specifically, disclosed are a di(hetero)aryl macrocyclic compound represented by formula (I), or a pharmaceutically acceptable salt, an enantiomer, a diastereomer, a racemate, a solvate, a hydrate, a polymorph, a prodrug or an active metabolite thereof a pharmaceutical composition comprising said compound and the derivative thereof, and methods for using same, including methods for treating cancers, pain, neurological diseases, autoimmune diseases and inflammation.

公开(公告)号：US11091462B2

公开(公告)日：2021-08-17

申请号：US16479299

申请日：2018-01-19

申请人： Shenzhen TargetRx, Inc.

发明人： Yihan Wang ,  Jiuyang Zhao ,  Yixin Ai

IPC分类号： A61K31/4439 ,  A61K31/444 ,  A61K49/00 ,  A61P31/00 ,  A61P35/00 ,  A61P35/02 ,  C07D401/04 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14

摘要： Provided are a (hetero)arylamide compound as shown in formula (I) having an inhibitory effect on protein kinase activity, a pharmaceutically acceptable salt, a stereoisomer, a solvate or hydrate thereof, a pharmaceutical composition including the compound or a derivative thereof, and a method for preparing the compound. The compound can be used as an irreversible inhibitor for protein kinase for preparing a plurality of drugs including an anti-tumour drug.