公开(公告)号：US20240343744A1

公开(公告)日：2024-10-17

申请号：US18757341

申请日：2024-06-27

申请人： THE GOVERNING COUNCIL OF THE UNIVERSITY OF TORONTO

发明人： Andrei K. YUDIN ,  Aleksandra HOLOWNIA

IPC分类号： C07F5/02 ,  C07F5/04

CPC分类号： C07F5/025 ,  C07F5/04

摘要： There is provide herein a compound of Formula (3):






wherein R1, R2, R3, R4, R5, R6, and R7 are each independently H or an organic group.

公开(公告)号：US20240336634A1

公开(公告)日：2024-10-10

申请号：US18580944

申请日：2022-07-22

申请人： The Government of the United States of America as represented by the Department of Veterans Affairs

发明人： Bhaskar Das ,  John Cijiang He

IPC分类号： C07F5/02 ,  A61K31/426 ,  A61K31/69 ,  A61K45/06 ,  C07D277/34

CPC分类号： C07F5/025 ,  A61K31/426 ,  A61K31/69 ,  A61K45/06 ,  C07D277/34

摘要： The present disclosure is concerned with small molecule modulators of TYR03 signaling useful for treating various disorders such as, for example, kidney disease (e.g, chronic kidney disease, acute kidney injury (AKI), diabetic kidney disease (DKD), focal segmental glomemlosclerosis (FSGS)) and a neurodegenerative disease (e.g, amyotrophic lateral sclerosis (ALS), Alzheimer's disease, Parkinson's disease, spinal muscular atrophy, traumatic brain injury, vascular dementia, Huntington's disease, mental retardation, and attention deficit and hyperactivity disorder (ADHD)). This abstract is intended as a scanning tool for purposes of searching in the particular art and is not intended to be limiting of the present invention.

公开(公告)号：US20240309001A1

公开(公告)日：2024-09-19

申请号：US18675780

申请日：2024-05-28

申请人： Incyte Corporation

发明人： Shili Chen ,  Zhongjiang Jia ,  Pingli Liu ,  Lei Qiao ,  Yongzhong Wu ,  Jiacheng Zhou ,  Qun Li

IPC分类号： C07D471/04 ,  A01M31/06 ,  C07D471/02 ,  C07F5/02

CPC分类号： C07D471/04 ,  A01M31/06 ,  C07D471/02 ,  C07F5/025 ,  C07B2200/13

摘要： The present application relates to crystalline solid forms of an inhibitor of BET proteins such as BRD2, BRD3, BRD4, and BRD-t, including methods of preparation thereof, and intermediates in the preparation thereof, where the compound is useful in the treatment of diseases such as cancer.

公开(公告)号：US20240287102A1

公开(公告)日：2024-08-29

申请号：US18291703

申请日：2022-07-28

申请人： Merck Patent GmbH

发明人： Delia-Maria GRUIA ,  Markus Klein ,  Michael Lange

IPC分类号： C07F5/02 ,  A61K31/69

CPC分类号： C07F5/025 ,  A61K31/69 ,  C07B2200/13

摘要： A solid form of [(1R)-2-(1-benzofuran-3-yl)-1-{[(1S,2R,4R)-7-oxabicyclo[2.2.1]heptan-2-yl]formamido}ethyl]boronic acid, hydrates, solvates, and/or adducts thereof can be used as LMP7 inhibitors. The solid form can be a trimeric crystalline anhydrous form characterized by two or more 2θ XRPD peaks at 6.5±0.2°, 11.2±0.2°, 17.1±0.2°, 19.6±0.2°, and 21.9±0.2° degrees.

公开(公告)号：US20240287051A1

公开(公告)日：2024-08-29

申请号：US18568772

申请日：2022-06-10

申请人： Otsuka Pharmaceutical Co., Ltd.

发明人： Prabhubas BODHURI ,  Hem Raj KHATRI ,  Ian SCOTT ,  Michael READER ,  David Charles LATHBURY ,  Nipun DAVAR ,  Matthew JOHNSON

IPC分类号： C07D405/14 ,  C07C67/10 ,  C07C217/70 ,  C07C271/16 ,  C07C313/06 ,  C07D209/46 ,  C07D405/12 ,  C07F5/02 ,  C12N9/10

CPC分类号： C07D405/14 ,  C07C67/10 ,  C07C217/70 ,  C07C271/16 ,  C07C313/06 ,  C07D209/46 ,  C07D405/12 ,  C07F5/025 ,  C12N9/1096 ,  C12Y206/01029

摘要： The present disclosure relates generally to methods for the preparation of Compound (I).

公开(公告)号：US20240279247A1

公开(公告)日：2024-08-22

申请号：US18605444

申请日：2024-03-14

申请人： SHANGHAI MICURX PHARMACEUTICALS CO., LTD.

发明人： Xinghai Wang ,  Jinqian Liu ,  Mikhail Fedorovich Gordeev

IPC分类号： C07F5/02 ,  A61K31/69 ,  A61P31/04

CPC分类号： C07F5/025 ,  A61K31/69 ,  A61P31/04

摘要： Described herein are prodrugs of antimicrobial organoboron compounds of Formula I, or salts thereof, and pharmaceutical compositions thereof, methods for their use, and methods for preparing the same.

公开(公告)号：US20240279201A1

公开(公告)日：2024-08-22

申请号：US18565426

申请日：2022-06-01

申请人： Fengtian Xue ,  Yan Shu ,  Yong Ai

发明人： Fengtian Xue ,  Yan Shu ,  Yong Ai

IPC分类号： C07D401/12 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/517 ,  A61K31/69 ,  A61K45/06 ,  A61K47/55 ,  A61K47/60 ,  A61P1/16 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07F5/02

CPC分类号： C07D401/12 ,  A61K31/423 ,  A61K31/427 ,  A61K31/428 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/517 ,  A61K31/69 ,  A61K45/06 ,  A61K47/551 ,  A61K47/60 ,  A61P1/16 ,  A61P35/00 ,  C07D401/14 ,  C07D403/12 ,  C07D413/12 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07F5/025

摘要： Compounds and compositions are provided as inhibitors of the Wnt/beta-catenin pathway and/or activators of the adenosine monophosphate-activated kinase (AMPK) pathway for the treatment of diseases that implicate the same. Such diseases include cancer or a metabolic disease. Cancers that may be treated by these compounds and compositions include adrenocortical cancer, hepatocellular cancer, hepatoblastoma, malignant melanoma, ovarian cancer, Wilm's tumor, Barrett's esophageal cancer, prostate cancer, colon cancer, colorectal cancer, rectal cancer, pancreatic cancer, bladder cancer, breast cancer (e.g. triple negative breast cancer), gastric cancer, head & neck cancer, lung cancer, mesothelioma, cervical cancer, uterine cancer, myeloid leukemia cancer, lymphoid leukemia cancer, pilometricoma cancer, medulloblastoma cancer, glioblastoma, and familial adenomatous polyposis. Metabolic diseases include type 2 diabetes, obesity, hyperlipidemia, alcoholic or non-alcoholic fatty liver disease, and liver fibrosis.

公开(公告)号：US20240247252A1

公开(公告)日：2024-07-25

申请号：US18405421

申请日：2024-01-05

申请人： The Trustees of Boston College

发明人： Jianmin Gao

IPC分类号： C12N15/10 ,  C07F5/02 ,  C07K7/50

CPC分类号： C12N15/1037 ,  C07F5/025 ,  C07K7/50

摘要： This patent document provides novel compounds as warheads for therapeutic or diagnostic agents. Advantages of the agents modified with the warheads include low off-target conjugation and minimized immunogenicity due to the reversible covalent bonding between the warheads and the targets.

公开(公告)号：US20240239816A1

公开(公告)日：2024-07-18

申请号：US18563110

申请日：2022-04-20

申请人： STELLA PHARMA CORPORATION

发明人： Yusuke MURATA ,  Hiroshi TAKENAKA ,  Yoichiro OHTA ,  Aya SUDANI ,  Miki ISHIMURA ,  Kensuke SUZUKI ,  Hiroyuki KAI

IPC分类号： C07F5/02 ,  A61K41/00 ,  A61K51/04

CPC分类号： C07F5/025 ,  A61K41/0095 ,  A61K51/0402

摘要： Provided are new compounds that can have the property of being specifically taken up into cancer cells. In the present invention, novel 4-borono-phenylalanine derivatives, borono-phenylalanine derivatives having a heterocyclic skeleton, borono-phenylalanine derivatives having a fused ring structure, or pharmaceutically acceptable salts thereof are prepared. These compounds have the property of being taken up specifically by LAT1 and thus easily taken up specifically by cancer cells in the evaluation of LAT1 and LAT2 selective uptake, and can be conveniently used for neutron capture therapy and the like. A typical example is a compound represented by the following formula (I) or a pharmaceutically acceptable salt thereof.

公开(公告)号：US20240209005A1

公开(公告)日：2024-06-27

申请号：US18550601

申请日：2022-03-15

申请人： RIBOSCIENCE LLC

发明人： Ronald HAWLEY

IPC分类号： C07F5/02 ,  A61K31/69 ,  A61K45/06

CPC分类号： C07F5/025 ,  A61K31/69 ,  A61K45/06

摘要： The present disclosure provides certain bicyclic heteroaryl boronate compounds that inhibit ectonucleotide pyrophosphatase/phosphodiesterase 1 (ENPP1) enzymatic activity and are therefore useful for the treatment of diseases and conditions modulated at least in part by ENPP1. In some embodiments, the bicyclic heteroaryl compounds includes those of Formula (I). Also provided herein are pharmaceutical compositions containing such compounds and processes for preparing such compounds.