公开(公告)号：US20240360104A1

公开(公告)日：2024-10-31

申请号：US18553988

申请日：2022-04-26

申请人： Dana-Farber Cancer Institute, Inc.

发明人： Nathanael S. Gray ,  Tinghu Zhang ,  Mengyang Fan ,  Jianwei Che ,  Wenchao Lu ,  Sirano Dhe-Paganon ,  Nicholas Paul Kwiatkowski

IPC分类号： C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

CPC分类号： C07D403/12 ,  A61K31/40 ,  A61K31/4155 ,  A61K31/4178 ,  A61K31/4192 ,  A61K31/422 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/551 ,  C07D207/14 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/14 ,  C07D405/14 ,  C07D495/04

摘要： Provided herein are compounds of Formula (I′), Formula (II), Formula (III), Formula (IV), Formula (V), Formula (VI), Formula (VII), or Formula (VIII) and pharmaceutically acceptable salts, solvates, hydrates, polymorphs, co-crystals, tautomers, stereoisomers, isotopically labeled derivatives, or prodrugs thereof. Also provided are methods and kits involving the inventive compounds or compositions for treating and/or preventing diseases (e.g., proliferative diseases (e.g., cancers, such as carcinoma, sarcoma, lung cancer, thyroid cancer, skin cancer, ovarian cancer, colorectal cancer, prostate cancer, pancreatic cancer, esophageal cancer, liver cancer, breast cancer)) in a subject. Provided are methods of inhibiting a TEAD transcription factors (e.g., TEAD1, TEAD2, TEAD3, TEAD4) in a subject.

公开(公告)号：US20240350460A1

公开(公告)日：2024-10-24

申请号：US18685925

申请日：2022-08-18

申请人： NANJING SHIJIANG MEDICINE TECHNOLOGY CO., LTD

发明人： Yufeng SHI ,  Wenjiang MA

IPC分类号： A61K31/422 ,  A61K31/345 ,  A61P35/00 ,  C12Q1/6886

CPC分类号： A61K31/422 ,  A61K31/345 ,  A61P35/00 ,  C12Q1/6886 ,  C12Q2600/136 ,  C12Q2600/154 ,  C12Q2600/158

摘要： The present invention relates to an application of a hydrazide compound in tumor treatment, and, in particular, the present invention provides a use of a compound represented by formula I, an optical isomer or a racemate thereof, or a solvate thereof, or a pharmaceutically acceptable salt thereof, being used for the preparation of a composition or formulation, said composition or formulation being used for the prevention and/or treatment of tumors. The compound of the present invention has significant and exceptional therapeutic effects on tumors having low or no expression of the NNMT gene, high expression of DNA methylase, high expression of UHRF1, high methylation level at the NNMT gene nucleotide site, and/or high methylation level at a DNA CpG site in the NNMT gene region.

公开(公告)号：US12121511B2

公开(公告)日：2024-10-22

申请号：US17159485

申请日：2021-01-27

申请人： Gilead Sciences, Inc.

发明人： Stephen E. Ammann ,  Gediminas J. Brizgys ,  James S. Cassidy ,  Elbert Chin ,  Chienhung Chou ,  Jeromy J. Cottell ,  Chao-I Hung ,  Kavoos Kolahdouzan ,  Daniel G. Shore ,  Suzanne M. Szewczyk ,  James G. Taylor ,  Rhiannon Thomas-Tran ,  Nathan E. Wright ,  Zheng-Yu Yang

IPC分类号： A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D471/04 ,  C07D493/04 ,  C07D493/10 ,  C07D498/04

CPC分类号： A61K31/4184 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/424 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K45/06 ,  C07D405/10 ,  C07D405/14 ,  C07D409/14 ,  C07D413/10 ,  C07D471/04 ,  C07D493/04 ,  C07D493/10 ,  C07D498/04

摘要： The present disclosure provides GLP-1R agonists, and compositions, methods, and kits thereof. Such compounds are generally useful for treating a GLP-1R mediated disease or condition.

公开(公告)号：US20240299360A1

公开(公告)日：2024-09-12

申请号：US17760169

申请日：2021-02-03

申请人： Jiangsu Hengrui Pharmaceuticals Co., Ltd.

发明人： Dong Liu ,  Peng Zhao ,  Jian Liu ,  Linghang Zhuang ,  Fengqi Zhang ,  Xinzhu Zhang ,  Chunying Song ,  Suxing Liu ,  Jing Li

IPC分类号： A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

CPC分类号： A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/497 ,  A61K31/506 ,  A61K31/55 ,  C07D401/06 ,  C07D401/14 ,  C07D403/06 ,  C07D403/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

摘要： Compounds of formula (I) useful as inhibitors of ADAMTS-5 and/or ADAMTS-4, pharmaceutical compositions thereof, and use of them as therapeutic agents for the treatment of diseases involving degradation of cartilage or disruption of cartilage homeostasis, in particular osteoarthrosis and/or rheumatoid arthritis, are disclosed.

公开(公告)号：US20240294541A1

公开(公告)日：2024-09-05

申请号：US18681141

申请日：2022-08-05

申请人： FILECLO SPOLKA Z OGRANICZONA ODPOWIEDZIALNOSCIA

发明人： Dominika CZERWONKA ,  Julia KRZYWIK ,  Tomasz SOBIERAJSKI ,  Greta KLEJBOROWSKA ,  Malgorzata ULLRICH ,  Witold MOZGA ,  Adam HUCZYNSKI ,  Przemyslaw PILASZEK

IPC分类号： C07D493/20 ,  A61K31/351 ,  A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4433 ,  A61K31/453 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/64 ,  A61P35/00

CPC分类号： C07D493/20 ,  A61K31/351 ,  A61K31/381 ,  A61K31/397 ,  A61K31/4025 ,  A61K31/4178 ,  A61K31/422 ,  A61K31/427 ,  A61K31/4433 ,  A61K31/453 ,  A61K31/496 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/64 ,  A61P35/00

摘要： The invention relates to compounds constituting C20-N-modified salinomycin derivatives, a method for obtaining the same, a composition containing the same, and their use as a medicament, particularly as an anti-cancer agent.

公开(公告)号：US20240287006A1

公开(公告)日：2024-08-29

申请号：US18570555

申请日：2022-06-16

申请人： The Regents of the University of California

发明人： Michael Rape ,  Julia Sabine Schaletzky ,  Edward Eric Wehri ,  Andrew Garrett Manford

IPC分类号： C07D263/58 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K45/06 ,  C07D215/26 ,  C07D413/04 ,  C07D471/04

CPC分类号： C07D263/58 ,  A61K31/422 ,  A61K31/423 ,  A61K31/437 ,  A61K45/06 ,  C07D215/26 ,  C07D413/04 ,  C07D471/04

摘要： The present disclosure provides pharmaceutical compositions and drug delivery devices comprising a compound of formula I, II, III, or IV. Methods are provided for inhibiting activity of an E3 ligase, involving contacting the E3 ligase with a compound of formula I, II, III, or IV. The present disclosure provides various treatment methods involving administration of such compounds.

公开(公告)号：US20240287005A1

公开(公告)日：2024-08-29

申请号：US18569408

申请日：2022-06-15

申请人： Elanco Tiergesundheit AG ,  Bayer Animal Health GmbH

发明人： Pierre DUCRAY ,  Denise RAGEOT ,  Andreas TURBERG

IPC分类号： C07D261/04 ,  A01N43/80 ,  A01P7/02 ,  A01P7/04 ,  A61K31/42 ,  A61K31/422 ,  A61P33/14 ,  C07D413/12

CPC分类号： C07D261/04 ,  A01N43/80 ,  A01P7/02 ,  A01P7/04 ,  A61K31/42 ,  A61K31/422 ,  A61P33/14 ,  C07D413/12

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




which are useful for long-lasting treatment and control of pests, for example fleas and ticks, in companion animals and livestock, and pharmaceutical compositions and methods of using the same.

公开(公告)号：US20240262916A1

公开(公告)日：2024-08-08

申请号：US18561127

申请日：2022-05-16

申请人： METANOIA BIO INC.

发明人： Slavica TUDZAROVA-TRAJKOVSKA ,  Oppel GREEFF ,  Abraham VAN WYK

IPC分类号： C07K16/28 ,  A61K31/196 ,  A61K31/198 ,  A61K31/245 ,  A61K31/26 ,  A61K31/352 ,  A61K31/357 ,  A61K31/37 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/501 ,  A61K31/519 ,  A61K31/661 ,  A61K38/06 ,  A61K38/08 ,  C12N15/113

CPC分类号： C07K16/2857 ,  A61K31/196 ,  A61K31/198 ,  A61K31/245 ,  A61K31/26 ,  A61K31/352 ,  A61K31/357 ,  A61K31/37 ,  A61K31/381 ,  A61K31/403 ,  A61K31/41 ,  A61K31/416 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/498 ,  A61K31/501 ,  A61K31/519 ,  A61K31/661 ,  A61K38/06 ,  A61K38/08 ,  C12N15/1138 ,  C07K2317/569 ,  C12N2310/11

摘要： The disclosure provides methods and compositions for treating cardiovascular disease with HIF1-a Pathway Inhibitors and PFKFB3 Inhibitors. Exemplary cardiovascular diseases ns treated using the provided methods and compositions include acute coronary syndrome, coronary artery disease, myocardial infarction, coronary heart disease, carditis or cardiomyopathy, an ischemic cardiovascular disease, heart failure, stroke, peripheral vascular disease peripheral arterial disease, and ischemia/reperfusion injury.

公开(公告)号：US20240254089A1

公开(公告)日：2024-08-01

申请号：US18245700

申请日：2021-09-16

申请人： ESCIENT PHARMACEUTICALS, INC.

发明人： Brandon SELFRIDGE ,  Liming HUANG ,  Adam YEAGER ,  Marcos SAINZ ,  Marion LANIER ,  Esther MARTINBOROUGH ,  Marcus BOEHM

IPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

CPC分类号： C07D231/56 ,  A61K31/416 ,  A61K31/4192 ,  A61K31/4196 ,  A61K31/422 ,  A61K31/423 ,  A61K31/4245 ,  A61K31/427 ,  A61K31/428 ,  A61K31/429 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/4709 ,  A61K31/497 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D407/12 ,  C07D409/12 ,  C07D413/12 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D513/04

摘要： Methods are provided for modulating MRGPR X4 generally, or for treating a MRGPR X4-dependent condition more specifically, by contacting MRGPR X4 or administering to a subject in need thereof, respectively, an effective amount of a compound having structure (I): or a pharmaceutically acceptable salt, isomer, hydrate, solvate or isotope thereof, wherein E, Q, W, Z, R1, R2, R3, and R4 are as defined herein. Pharmaceutical compositions containing such compounds, as well as compounds themselves, are also provided.

公开(公告)号：US20240208993A1

公开(公告)日：2024-06-27

申请号：US18544546

申请日：2023-12-19

申请人： HANGZHOU POLYMED BIOPHARMACEUTICALS, INC.

发明人： Jason Shaoyun XIANG ,  Lei WU ,  Rui XU ,  Qiang ZHANG ,  Gang YANG ,  Michael XIANG ,  Mixue TONG ,  Camille XIANG ,  Yuxin LIU ,  Suyue WANG ,  Rui YANG

IPC分类号： C07D498/08 ,  A61K31/422 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61P35/02 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  C07D493/08 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

CPC分类号： C07D498/08 ,  A61K31/422 ,  A61K31/437 ,  A61K31/439 ,  A61K31/4439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/5377 ,  A61K31/5386 ,  A61P35/02 ,  C07D401/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D491/107 ,  C07D493/08 ,  C07D498/04 ,  C07D513/04 ,  C07D519/00

摘要： A five-membered-fused six-membered compound, and a preparation method therefor and a pharmaceutical composition and the use thereof. The five- and six-membered compound is a compound as shown in formula I, II or III. The compound has an inhibitory effect on FLT3 and/or IRAK4.