公开(公告)号：USRE50082E1

公开(公告)日：2024-08-20

申请号：US17579990

申请日：2022-01-20

申请人： NETHERLANDS TRANSLATIONAL RESEARCH CENTER B.V.

发明人： Adrianus Petrus Antonius De Man ,  Rogier Christian Buijsman ,  Jan Gerard Sterrenburg ,  Joost Cornelis Marinus Uitdehaag ,  Joeri Johannes Petrus De Wit ,  Guido Jenny Rudolf Zaman

IPC分类号： C07D471/14 ,  C07D471/22

CPC分类号： C07D471/14 ,  C07D471/22

摘要： A compound of Formula I:




wherein, R1 and R2 independently are selected from the group consisting of optionally substituted (6-10C)aryl and (1-5C)heteroaryl groups. The compounds can be used in pharmaceutical compositions, in particular in the treatment of cancer.

公开(公告)号：US12054498B2

公开(公告)日：2024-08-06

申请号：US17834135

申请日：2022-06-07

申请人： Nuvalent, Inc.

发明人： Joshua Courtney Horan ,  Xinxing Tang ,  Scot Richard Mente ,  Henry Efrem Pelish ,  Matthew D. Shair ,  Anupong Tangpeerachaikul

IPC分类号： A61K31/4427 ,  A61P35/00 ,  C07D471/22 ,  C07D498/22 ,  C07D513/22

CPC分类号： C07D498/22 ,  A61P35/00 ,  C07D513/22

摘要： Disclosed are heterocyclic heteroaromatic macrocyclic ether compounds of Formula (I):




pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof. The disclosure further relates to methods of treating or preventing cancer using the heterocyclic heteroaromatic macrocyclic ether compounds, pharmaceutically acceptable salts of the compounds and pharmaceutical compositions thereof.

公开(公告)号：US12024528B2

公开(公告)日：2024-07-02

申请号：US18334611

申请日：2023-06-14

申请人： Gilead Sciences, Inc.

发明人： Hang Chu ,  Ana Z. Gonzalez Buenrostro ,  Xiaochun Han ,  Anna E. Hurtley ,  Lan Jiang ,  Jiayao Li ,  Gregg M. Schwarzwalder ,  Devleena M. Shivakumar ,  Matthew J. Von Bargen ,  Qiaoyin Wu ,  Hong Yang

IPC分类号： C07D498/20 ,  A61K45/06 ,  A61P31/18 ,  C07D471/22 ,  C07D491/22 ,  C07D497/22 ,  C07D498/22 ,  C07D513/22 ,  C07D515/22

CPC分类号： C07D498/20 ,  A61K45/06 ,  A61P31/18 ,  C07D471/22 ,  C07D491/22 ,  C07D497/22 ,  C07D498/22 ,  C07D513/22 ,  C07D515/22 ,  C07B2200/05

摘要： The present disclosure relates generally to compounds, of Formula I:




Also disclosed are pharmaceutical compositions comprising said compounds and methods of making said compounds. The compounds of the disclosure are useful in treating or preventing human immunodeficiency virus (HIV) infection.

公开(公告)号：US20240208972A1

公开(公告)日：2024-06-27

申请号：US18512306

申请日：2023-11-17

申请人： NEURON23, INC.

发明人： Ming Yu ,  Gyanendra Kumar ,  Zhonghua Pei ,  Scott Savage ,  Kejia Wu ,  Jim X. Zheng

IPC分类号： C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D519/00

CPC分类号： C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D519/00

摘要： The invention provides compounds that modulate the activity of protein kinases that are associated with human diseases, disorders, and conditions. In particular, compounds of the invention inhibit LRRK2.

公开(公告)号：US11976070B1

公开(公告)日：2024-05-07

申请号：US18392679

申请日：2023-12-21

申请人： KING FAISAL UNIVERSITY

发明人： Michelyne Haroun ,  Christophe Tratrat

IPC分类号： C07D487/22 ,  A61P35/00 ,  A61P35/02 ,  C07D471/22

CPC分类号： C07D471/22 ,  A61P35/00 ,  A61P35/02

摘要： Novel 5-substituted aminopyrimido[6′,1′:2,3]imidazo[4,5-c][1,6]naphthyridine compounds having the formula I below with all substituents as defined in the instant specification, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 5-substituted aminopyrimido[6′,1′:2,3]imidazo[4,5-c][1,6]naphthyridine 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.

公开(公告)号：US20240140950A1

公开(公告)日：2024-05-02

申请号：US18398201

申请日：2023-12-28

申请人： Hebei University of Science & Technology

发明人： Huajie ZHU

IPC分类号： C07D471/22 ,  A61P35/00

CPC分类号： C07D471/22 ,  A61P35/00

摘要： The present application provides a nitrogen-containing polycyclic aromatic compound and its preparation method and application. The nitrogen-containing polycyclic aromatic compound has a structure of Formula I, has an excellent broad-spectrum anti-tumor activity, and shows an inhibitory activity comparable to cisplatin on cervical cancer cells, breast cancer cells, melanoma cells, lung cancer cells and myeloma cells. Compared with cisplatin, the compound also has lower toxicity, and may be used as a lead compound for the development of new anti-tumor drugs.

公开(公告)号：US11964975B1

公开(公告)日：2024-04-23

申请号：US18236390

申请日：2023-08-21

申请人： KING FAISAL UNIVERSITY

发明人： Michelyne Haroun ,  Christophe Tratrat

IPC分类号： C07D471/22 ,  A61P35/00

CPC分类号： C07D471/22 ,  A61P35/00

摘要： Novel 5-substituted aminopyrimido[6′,1′:2,3]imidazo[4,5-c][2,6]naphthyridine compounds, a method of synthesizing said compounds, a pharmaceutical composition comprising said compounds and a suitable carrier, and a method of using the compounds. The 5-substituted aminopyrimido[6′,1′:2,3]imidazo[4,5-c][2,6]naphthyridine 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.

公开(公告)号：US11963442B2

公开(公告)日：2024-04-16

申请号：US17196712

申请日：2021-03-09

申请人： Merck Patent GmbH

发明人： Amir Hossain Parham ,  Tobias Grossmann ,  Anja Jatsch ,  Thomas Eberle ,  Jonas Kroeber ,  Christof Pflumm ,  Lars Dobelmann-Mara

IPC分类号： C07D405/14 ,  A61B18/20 ,  A61N5/06 ,  C07D409/14 ,  C07D471/04 ,  C07D471/14 ,  C07D471/22 ,  C07D487/04 ,  C07D487/14 ,  C07D491/048 ,  C07D491/052 ,  C07D491/056 ,  C07D495/04 ,  C07D498/04 ,  C07D513/04 ,  C09B57/00 ,  C09K11/02 ,  H10K50/11 ,  H10K50/16 ,  H10K71/12 ,  H10K85/60 ,  H10K85/30 ,  H10K101/10

CPC分类号： H10K85/6572 ,  A61B18/203 ,  A61N5/0616 ,  C07D405/14 ,  C07D409/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/048 ,  C09B57/00 ,  C09K11/025 ,  H10K85/654 ,  H10K85/657 ,  H10K85/6574 ,  H10K85/6576 ,  H10K50/11 ,  H10K50/16 ,  H10K71/12 ,  H10K85/342 ,  H10K85/346 ,  H10K2101/10 ,  Y02E10/549 ,  Y02P70/50

摘要： The application relates to compounds having functional substituents in a specific spatial arrangement, to devices comprising same, and to the preparation and use thereof.

公开(公告)号：US11939341B2

公开(公告)日：2024-03-26

申请号：US17161692

申请日：2021-01-29

申请人： WUHAN TIANMA MICROELECTRONICS CO., LTD. ,  WUHAN TIANMA MICROELECTRONICS CO., LTD. SHANGHAI BRANCH

发明人： Quan Ran ,  Wei Gao ,  Lei Zhang ,  Wenpeng Dai

IPC分类号： C07D495/20 ,  C07D471/04 ,  C07D471/20 ,  C07D471/22 ,  C07D493/20 ,  C07D493/22 ,  C07D495/22 ,  C07D519/00 ,  H01L51/00 ,  H10K85/60 ,  H10K50/18

CPC分类号： C07D495/20 ,  C07D471/04 ,  C07D471/20 ,  C07D471/22 ,  C07D493/20 ,  C07D493/22 ,  C07D495/22 ,  C07D519/00 ,  H10K85/633 ,  H10K85/653 ,  H10K85/654 ,  H10K85/656 ,  H10K85/6572 ,  H10K85/6574 ,  H10K85/6576 ,  H10K50/18

摘要： Provided are an organic compound, an electroluminescent material and an application thereof. The organic compound has a structure represented by Formula I. With the design of the spiro parent structure and the introduction of specific substituents, the organic compound can prevent materials from stacking and reduce the crystallinity of the molecule. The design of the spiro structure and substituents make the organic material have a high triplet state energy level Ti, and the nitrogen heterocycle and its linking groups make the organic compound have characteristics of good electron and hole transport performances. The organic compound has suitable HOMO and LUMO energy levels, facilitating the coordination of adjacent layers in terms of energy level. The organic compound also has advantages of high glass-transition temperature and good molecular thermal stability. Therefore, the organic compound can effectively improve the light emitting efficiency and lifetime of the device.

公开(公告)号：US11891404B2

公开(公告)日：2024-02-06

申请号：US17940617

申请日：2022-09-08

申请人： Bayer Aktiengesellschaft ,  Bayer Pharma Aktiengesellschaft ,  The Broad Institute, Inc.

发明人： Kai Thede ,  Anne Mengel ,  Clara Christ ,  Joachim Kuhnke ,  Sarah Anna Liesa Johannes ,  Philipp Buchgraber ,  Ulrich Klar ,  Ulrike Rauh ,  Stefan Kaulfuss ,  Amaury Ernesto Fernandez-Montalvan ,  Nicolas Werbeck ,  Ursula Moenning ,  Katrin Nowak-Reppel ,  Sven Wittrock ,  David McKinney ,  Michael H. Serrano-Wu ,  Chris Lemke ,  Mark Fitzgerald ,  Christopher Nasveschuk ,  Kiel Lazarski ,  Steven James Ferrara ,  Laura Furst ,  Guo Wei ,  Patrick Ryan McCarren ,  Rebecca Ann Harvey

IPC分类号： C07D498/14 ,  A61P35/02 ,  A61P35/00 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/22 ,  C07D487/14 ,  C07D487/22 ,  C07D498/22

CPC分类号： C07D498/14 ,  A61K31/4162 ,  A61K31/437 ,  A61K31/496 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  A61P35/02 ,  C07D471/22 ,  C07D487/14 ,  C07D487/22 ,  C07D498/22

摘要： The present invention relates to substituted macrocyclic indole derivatives of general formula (I):




in which R1, R2, R3, R4, R5, R6, A and L are as defined herein, methods of preparing said compounds, intermediate compounds useful for preparing said compounds, pharmaceutical compositions and combinations comprising said compounds, and the use of said compounds for manufacturing pharmaceutical compositions for the treatment or prophylaxis of diseases, in particular of hyperproliferative disorders, as a sole agent or in combination with other active ingredients.