公开(公告)号：US20240124422A1

公开(公告)日：2024-04-18

申请号：US18128117

申请日：2023-03-29

申请人： Prelude Therapeutics Incorporated

发明人： Chun Chen ,  Ryan Holmes ,  Soham Maity ,  Andrew P. Combs ,  Andrew W. Buesking ,  Sarah Pawley

IPC分类号： C07D403/04 ,  C07D239/95 ,  C07D401/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

CPC分类号： C07D403/04 ,  C07D239/95 ,  C07D401/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/08

摘要： The disclosure is directed to compounds of Formula I






Pharmaceutical compositions comprising compounds of Formula I, as well as methods of their use and preparation, are also described.

公开(公告)号：US11951189B2

公开(公告)日：2024-04-09

申请号：US17046053

申请日：2019-04-11

申请人： THE UNIVERSITY OF MELBOURNE

发明人： Paul Stephen Donnelly ,  Nicholas Alan Zia

IPC分类号： A61B5/00 ,  A61B8/00 ,  A61B10/00 ,  A61K51/04 ,  C07D487/08

CPC分类号： A61K51/0482 ,  A61K51/044 ,  C07D487/08

摘要： The present invention is directed to sarcophagine based compounds of formula (I). The compounds can complex a radioisotope, such as 64-copper and hence are useful in radioimaging and radiotherapy of cancers, e.g. colorectal cancer. The compounds work via a pre-targeting imaging approach in which the tetrazine reacts via click chemistry with a functional group such as a transcyclooctene which is pre-bound to a ligand such as a tumour specific antibody.

公开(公告)号：US20240109889A1

公开(公告)日：2024-04-04

申请号：US18370186

申请日：2023-09-19

申请人： C4 Therapeutics, Inc.

发明人： Roger Norcross ,  Annick Goergler ,  Fabian Dey ,  Eric Andre Kusznir

IPC分类号： C07D471/04 ,  C07D235/26 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/10 ,  C07D487/08

CPC分类号： C07D471/04 ,  C07D235/26 ,  C07D401/10 ,  C07D401/14 ,  C07D403/10 ,  C07D403/14 ,  C07D405/12 ,  C07D405/14 ,  C07D417/10 ,  C07D487/08

摘要： The present invention provides selected dihydrobenzimidazolones which bind to the ubiquitously expressed E3 ligase protein cereblon (CRBN) and alter the substrate specificity of the CRBN E3 ubiquitin ligase complex, resulting in breakdown of intrinsic downstream proteins. The disclosed compounds are useful for the treatment of cancer.

公开(公告)号：US11945812B2

公开(公告)日：2024-04-02

申请号：US17335620

申请日：2021-06-01

申请人： Boehringer Ingelheim International GmbH ,  Vanderbilt University

发明人： Jason Abbott ,  Joachim Broeker ,  Jianwen Cui ,  Steve W. Fesik ,  Andreas Gollner ,  Tim Hodges ,  Jale Karolyi-Oezguer ,  Andrew Little ,  Andreas Mantoulidis ,  Jason Phan ,  Dhruba Sarkar ,  Christian Alan Paul Smethurst ,  Qi Sun ,  Matthias Treu ,  Alex Waterson

IPC分类号： C07D521/00 ,  A61K31/381 ,  A61K31/506 ,  A61P35/00 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10

CPC分类号： C07D413/14 ,  A61K31/506 ,  A61P35/00 ,  C07D409/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D487/10

摘要： The present invention encompasses compounds of formula (I)




wherein R1a, R1b, R2a, R2b, Z, R3 to R5, A, p, U, V, W, L and E have the meanings given in the claims and specification, their use as inhibitors of mutant Ras family proteins, pharmaceutical compositions and preparations containing such compounds and their use as medicaments/medical uses, especially as agents for treatment and/or prevention of oncological diseases.

公开(公告)号：US20240101567A1

公开(公告)日：2024-03-28

申请号：US18262399

申请日：2022-01-24

申请人： Merck Sharp & Dohme LLC

发明人： John S. Debenham ,  Cheng Zhu ,  Amjad Ali ,  Sung-Sau So ,  Ying-Duo Gao

IPC分类号： C07D487/08

CPC分类号： C07D487/08

摘要： The present invention provides a compound of Formula I and pharmaceutical compositions comprising one or more said compounds, and methods for using said compounds for treating or preventing thromboses, embolisms, hypercoagulability or fibrotic changes. The compounds are selective Factor XIa inhibitors or dual inhibitors of Factor XIa and plasma kallikrein.

公开(公告)号：US11918592B2

公开(公告)日：2024-03-05

申请号：US16962809

申请日：2019-01-16

申请人： Syros Pharmaceuticals, Inc.

发明人： Jason J. Marineau ,  Claudio Edmundo Chuaqui ,  Stephane Ciblat ,  Anzhelika Kabro ,  Henri Piras ,  Kenneth Matthew Whitmore ,  Kate-Lyn Lund ,  Michael Bradley

IPC分类号： C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  A61P35/00 ,  A61K31/675 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  C07D471/04 ,  C07D487/08 ,  C07F9/6558

CPC分类号： A61K31/675 ,  A61K31/506 ,  A61K31/5377 ,  A61K45/06 ,  A61P35/00 ,  C07D403/04 ,  C07D403/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/08 ,  C07F9/65583

摘要： The present invention provides, inter alia, compounds having the structures of formulas described herein; pharmaceutically acceptable salts, solvates, hydrates, tautomers, and isotopic forms thereof; and compositions (e.g., pharmaceutical compositions and kits) containing one or more of the foregoing. Also provided are methods of administering and uses involving the compounds and/or pharmaceutical compositions for treating or preventing disease. The disease can be a proliferative disease, such as a cancer (e.g., a blood cancer (e.g., a leukemia or lymphoma), a brain cancer, a breast cancer, melanoma, multiple myeloma, or an ovarian cancer) a benign neoplasm, pathologic angiogenesis, or a fibrotic disease. While no aspect of the invention is limited by the biological events that may transpire, administering a compound or other composition described herein may selectively inhibit the aberrant expression or activity of cyclin-dependent kinase 7 (CDK7) and, thereby, induce cellular apoptosis and/or inhibit the transcription of disease-related genes in the patient (or in a biological sample).

公开(公告)号：US11912713B2

公开(公告)日：2024-02-27

申请号：US17532413

申请日：2021-11-22

申请人： Trevena, Inc.

发明人： Aimee Crombie Speerschneider ,  Dennis Shinji Yamashita ,  Philip Michael Pitis ,  Michael John Hawkins ,  Guodong Liu ,  Tamara Ann Miskowski Daubert ,  Catherine C. K. Yuan ,  Robert Borbo Kargbo ,  Robert Jason Herr ,  Donna Romero

IPC分类号： C07D487/08 ,  A61P25/22 ,  A61P23/00 ,  A61P25/24 ,  C07D223/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

CPC分类号： C07D487/08 ,  A61P23/00 ,  A61P25/22 ,  A61P25/24 ,  C07D223/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/14 ,  C07D417/14

摘要： The present embodiments are directed, in part, to compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof for modulating the activity of delta opioid receptor, biased and/or unbiased, and/or methods for treating pain, migraines, headaches, depression, Parkinsons Disease, anxiety, and/or overactive bladder, and other disorders and conditions described herein or any combination thereof.

公开(公告)号：US11884647B2

公开(公告)日：2024-01-30

申请号：US17072844

申请日：2020-10-16

申请人： THE REGENTS OF THE UNIVERSITY OF CALIFORNIA ,  ATENGEN, INC.

发明人： Hui Sun ,  Pu Sun ,  Guo Cheng ,  Adrian Chichuen Au ,  Ming Zhong

IPC分类号： C07D401/14 ,  A61P35/00 ,  C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07D487/08 ,  C07D491/113 ,  C07D498/04 ,  C07H15/26

CPC分类号： C07D401/14 ,  A61P35/00 ,  C07D215/42 ,  C07D215/44 ,  C07D215/46 ,  C07D401/04 ,  C07D401/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D417/12 ,  C07D487/08 ,  C07D491/113 ,  C07D498/04 ,  C07H15/26

摘要： The disclosure provides compounds, and compositions, including pharmaceutical compositions, kits that include the compounds, and methods of using (or administering) and making the compounds. The disclosure further provides compounds or compositions thereof for use in a method of modulating PLXDC1 (TEM7) and/or PLXDC2 or killing pathogenic blood vessles. The disclosure further provides compounds or compositions thereof for use in a method of treating a disease, disorder, or condition that is mediated, at least in part, by PEDF receptors or by angiogenesis.

公开(公告)号：US11834455B2

公开(公告)日：2023-12-05

申请号：US16822478

申请日：2020-03-18

申请人： Epizyme, Inc.

发明人： Richard Chesworth ,  Oscar Miguel Moradei ,  Gideon Shapiro ,  Lei Jin ,  Robert E. Babine

IPC分类号： C07D487/10 ,  C07D403/12 ,  C07D405/14 ,  C07D413/14 ,  C07D401/04 ,  C07D403/04 ,  C07D405/04 ,  C07D405/12 ,  C07D239/42 ,  C07D409/14 ,  C07D413/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/08 ,  C07D493/04 ,  C07D493/10 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10 ,  C07D413/04 ,  C07D487/04

CPC分类号： C07D487/10 ,  C07D239/42 ,  C07D401/04 ,  C07D403/04 ,  C07D403/12 ,  C07D405/04 ,  C07D405/12 ,  C07D405/14 ,  C07D409/14 ,  C07D413/04 ,  C07D413/12 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/08 ,  C07D493/04 ,  C07D493/10 ,  C07D495/04 ,  C07D498/04 ,  C07D498/10

摘要： Provided herein are compounds of Formula (I):




and pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof; wherein X, R1, R1a, R2a, R2b, R2c, R2d, are as defined herein, and Ring HET is a 6-membered monocyclic heteroaryl ring system of Formula:





wherein L2, R13, G8, G10, G11, and G12 are as defined herein. Compounds of the present invention are useful for inhibiting CARM1 activity. Methods of using the compounds for treating CARM1-mediated disorders are also described.

公开(公告)号：US20230365572A1

公开(公告)日：2023-11-16

申请号：US18027890

申请日：2021-09-23

申请人： ATROGI AB

发明人： Ilga Mutule ,  Benjamin Pelcman ,  Tore Bengtsson

IPC分类号： C07D487/08

CPC分类号： C07D487/08

摘要： There is provided herein a compound of formula I or a pharmaceutically acceptable salt thereof, wherein R1 and the ring comprising Q1 to Q5 have meanings provided in the description.