公开(公告)号：US12122775B1

公开(公告)日：2024-10-22

申请号：US18413246

申请日：2024-01-16

申请人： KING FAISAL UNIVERSITY

发明人： Michelyne Haroun ,  Christophe Tratrat

IPC分类号： A61K31/4985 ,  A61P35/00 ,  C07D471/14 ,  C07D487/04

CPC分类号： C07D471/14 ,  A61K31/4985 ,  A61P35/00

摘要： Pyrido[4,3-e]pyrrolo[1,2-a]pyrazine compounds, a method of synthesizing the compounds, a pharmaceutical composition comprising the compounds and a suitable carrier, and a method of using the compounds. The pyrido[4,3-e]pyrrolo[1,2-a]pyrazine compounds, identified as CK2 inhibitors, are useful as anticancer and/or antitumor agents, and as agents for treating other kinase-associated conditions including inflammation, pain, and certain immunological disorders, and other types of diseases such as diabetes, viral infection, neurodegenerative diseases. The pyrido[4,3-e]pyrrolo[1,2-a]pyrazine compounds having the formula:

公开(公告)号：US20240336629A1

公开(公告)日：2024-10-10

申请号：US18276269

申请日：2022-01-26

申请人： JACOBIO PHARMACEUTICALS CO., LTD.

发明人： Haijun LI ,  Mingming CHEN ,  Di KANG ,  Qinglong LI ,  Lei ZHANG ,  Man YAN ,  Wei LONG ,  Yanping WANG ,  Hao ZHANG ,  Cunbo MA ,  Amin LI

IPC分类号： C07D513/14 ,  C07D471/14 ,  C07D498/14 ,  C12N9/99

CPC分类号： C07D513/14 ,  C07D471/14 ,  C07D498/14 ,  C12N9/99

摘要： Provided are a compound of formula (I) that inhibit the activity of PARP7, a stereoisomer thereof, a deuterated derivative thereof, or a pharmaceutically acceptable salt thereof, an intermediate to prepare the compound, a process to prepare the compound, a composition comprising the same, and the methods of using the same.

公开(公告)号：US12108665B2

公开(公告)日：2024-10-01

申请号：US17639348

申请日：2020-08-31

申请人： Merck Patent GmbH

发明人： Amir Parham ,  Philipp Stoessel ,  Christian Ehrenreich

IPC分类号： H10K85/60 ,  C07D251/20 ,  C07D251/22 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C09K11/06 ,  H10K50/11 ,  H10K101/10

CPC分类号： H10K85/654 ,  C07D251/20 ,  C07D251/22 ,  C07D403/10 ,  C07D403/14 ,  C07D405/04 ,  C07D405/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00 ,  C09K11/06 ,  H10K85/615 ,  H10K85/622 ,  H10K85/624 ,  H10K85/626 ,  H10K85/657 ,  H10K85/6572 ,  H10K85/6574 ,  H10K85/6576 ,  C09K2211/1018 ,  H10K50/11 ,  H10K2101/10

摘要： The invention relates to compounds which are suitable for use in electronic devices, and to electronic devices, in particular organic electroluminescent devices, containing said compounds.

公开(公告)号：US12103929B2

公开(公告)日：2024-10-01

申请号：US17129983

申请日：2020-12-22

申请人： JACOBIO PHARMACEUTICALS CO., LTD.

发明人： Haiquan Fang ,  Mingming Chen ,  Guiqun Yang ,  Yuelei Du ,  Yanping Wang ,  Tong Wu ,  Qinglong Li ,  Lei Zhang ,  Shaojing Hu

IPC分类号： C07D471/14 ,  A61P35/00

CPC分类号： C07D471/14 ,  A61P35/00 ,  C07B2200/05

摘要： Disclosed are tricyclic compounds as bromodomain and extra-terminal (BET) inhibitors which are shown as formula I, their synthesis and their use for treating diseases. More particularly, disclosed are fused heterocyclic derivatives useful as inhibitors of BET, methods for producing such compounds and methods for treating diseases and conditions wherein inhibition of one or more BET bromodomains provides a benefit.

公开(公告)号：US20240317753A9

公开(公告)日：2024-09-26

申请号：US17998030

申请日：2021-05-05

申请人： Merck Patent GmbH ,  Cancer Research Technology Ltd.

发明人： Timo HEINRICH ,  Sarah Schlesiger ,  Jakub Gunera ,  Emma Carswell ,  Lisa Koetzner ,  Andreas Blum

IPC分类号： C07D487/04 ,  A61P35/00 ,  C07D471/14 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00 ,  C07F5/02 ,  C07H15/26

CPC分类号： C07D487/04 ,  A61P35/00 ,  C07D471/14 ,  C07D498/04 ,  C07D513/04 ,  C07D513/14 ,  C07D519/00 ,  C07F5/025 ,  C07H15/26

摘要： Tricyclic heterocycles are disclosed. These heterocyclic compounds are useful as TEAD binders and/or inhibitors of YAP-TEAD and TAZ-TEAD protein-protein interaction or binding and for the prevention and/or treatment of several medical conditions including hyperproliferative disorders and diseases, in particular cancer.

公开(公告)号：US20240317749A1

公开(公告)日：2024-09-26

申请号：US18572411

申请日：2022-06-21

申请人： TAXIS PHARMACEUTICALS, INC.

发明人： Ajit K. PARHI ,  Yi YUAN ,  Yongzheng ZHANG ,  Jesus ROSADO ,  Pratik DATTA

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P31/04 ,  C07D487/04

CPC分类号： C07D471/14 ,  A61K31/519 ,  A61P31/04 ,  C07D487/04

摘要： Disclosed herein are compounds of formula I: and salts thereof. Also disclosed are compositions comprising compounds of formula I and methods using compounds of formula I.

公开(公告)号：US20240279238A1

公开(公告)日：2024-08-22

申请号：US18630561

申请日：2024-04-09

申请人： Shionogi & Co., Ltd. ,  ViiV Healthcare Company

发明人： Brian A. JOHNS ,  Takashi KAWASUJI ,  Teruhiko TAISHI ,  Yoshiyuki TAODA

IPC分类号： C07D498/14 ,  A61K9/00 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/551 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D498/04 ,  C07D498/20 ,  C07D498/22

CPC分类号： C07D498/14 ,  A61K9/0053 ,  A61K31/4985 ,  A61K31/519 ,  A61K31/5365 ,  A61K31/551 ,  A61K45/06 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D498/04 ,  C07D498/20 ,  C07D498/22

摘要： Substituted 1,2,3,3a,4,5,7,9,13,13a-decahydropyrido[1′,2′:4,5]pyrazino[1,2-a]pyrrolo[1,2-c]pyrimidines having the anti-virus activity, particularly the HIV integrase inhibitory activity, and a pharmaceutical composition containing the same, particularly an anti-HIV pharmaceutical composition.

公开(公告)号：US20240270747A1

公开(公告)日：2024-08-15

申请号：US18523284

申请日：2023-11-29

申请人： Genentech, Inc.

发明人： James John CRAWFORD ,  Daniel Fred ORTWINE ,  BinQing WEI ,  Wendy B. YOUNG

IPC分类号： C07D487/04 ,  A61K9/20 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC分类号： C07D487/04 ,  A61K9/20 ,  A61K31/495 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/4995 ,  A61K31/501 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/53 ,  A61K31/5377 ,  A61K31/5383 ,  A61K45/06 ,  A61P35/00 ,  A61P37/00 ,  C07D471/04 ,  C07D471/14 ,  C07D487/08 ,  C07D487/14 ,  C07D495/04 ,  C07D495/14 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： Heteroaryl pyridone and aza-pyridone compounds are provided, including stereoisomers, tautomers, and pharmaceutically acceptable salts thereof, useful for inhibiting Btk kinase, and for treating immune disorders such as inflammation mediated by Btk kinase. Methods of using heteroaryl pyridone and aza-pyridone compounds for in vitro, in situ, and in vivo diagnosis, and treatment of such disorders in mammalian cells, or associated pathological conditions, are disclosed.

公开(公告)号：US20240270745A1

公开(公告)日：2024-08-15

申请号：US18569434

申请日：2022-06-15

申请人： SHANGHAI INSTITUTE OF MATERIA MEDICA, CHINESE ACADEMY OF SCIENCES ,  LANZHOU INSTITUTE OF CHEMICAL PHYSICS, CHINESE ACADEMY OF SCIENCES

发明人： Zhaobing GAO ,  Junli YANG ,  Xianhua MENG ,  Yueming ZHENG ,  Tian CHAI ,  Yin ZHANG

IPC分类号： C07D471/14 ,  A61K31/519 ,  A61P29/00

CPC分类号： C07D471/14 ,  A61K31/519 ,  A61P29/00

摘要： Provided in the present invention are an isoquinoline alkaloid compound selected from the group consisting of the compounds represented by the following structural formulas, and a preparation method therefor and the use thereof. The present invention proves for the first time that the isoquinoline alkaloid compound is an inhibitor of the IK potassium current and the background potassium current in the nervous system, the cardiovascular system and the pancreas, especially an inhibitor of the Kv2.1 channel and the TRESK channel, and can be used for treating a disease such as stroke, arrhythmia, atrial fibrillation, diabetes, pain, hypoventilation, and depression.

公开(公告)号：US20240262828A1

公开(公告)日：2024-08-08

申请号：US18543151

申请日：2023-12-18

申请人： Enanta Pharmaceuticals, Inc.

发明人： Joseph D. PANARESE ,  Dexter DAVIS ,  Samuel BARTLETT ,  Katherine CHONG ,  Nathaniel Thomas KENTON ,  Yat Sun OR

IPC分类号： C07D471/14 ,  A61K45/06

CPC分类号： C07D471/14 ,  A61K45/06

摘要： The present invention discloses compounds of Formula (I), or pharmaceutically acceptable salts, thereof:




which inhibit the protein(s) encoded by hepatitis B virus (HBV) or interfere with the function of the HBV life cycle of the hepatitis B virus and are also useful as antiviral agents. The present invention further relates to pharmaceutical compositions comprising the aforementioned compounds for administration to a subject suffering from HBV infection. The invention also relates to methods of treating an HBV infection in a subject by administering a pharmaceutical composition comprising the compounds of the present invention.