公开(公告)号：US20240360145A1

公开(公告)日：2024-10-31

申请号：US18770694

申请日：2024-07-12

申请人： LISEN THERAPEUTICS, INC.

发明人： Ning ZHOU ,  Tong CHENG ,  Yingjiao XU ,  Chengtao LI ,  Wuxin ZOU

IPC分类号： C07D487/08 ,  A61K31/506 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

CPC分类号： C07D487/08 ,  A61K31/506 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/12

摘要： Provided are pyrimidine-2,4-diamine derivatives and use thereof. Specifically, the pyrimidine-2,4-diamine derivative are as represented by Formula 1, and a racemate, tautomer, enantiomer, diastereomer, isotope-substituted compound, prodrug or pharmaceutically acceptable salt thereof, a preparation method thereof, and use thereof in the preparation of a medicament

公开(公告)号：US20240360085A1

公开(公告)日：2024-10-31

申请号：US18672406

申请日：2024-05-23

申请人： Kadmon Corporation, LLC

发明人： Kevin G. Liu ,  Kellen Olszewski ,  Ji-In Kim ,  Masha V. Poyurovsky ,  Koi Morris ,  Xuemei Yu ,  Christophe Lamarque

IPC分类号： C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

CPC分类号： C07D239/42 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D403/04 ,  C07D403/12 ,  C07D405/12 ,  C07D405/14 ,  C07D409/12 ,  C07D413/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D473/34 ,  C07D491/048 ,  C07D491/052 ,  C07D495/04 ,  C07D519/00

摘要： This invention provides compounds that modulate glucose uptake activity and cellular transport/uptake of glucose, and particularly GLUT3, but also including but not limited to GLUT1-14 (SLC2A1-SLC2A14). Compounds of the invention are useful for treating diseases, including cancer, autoimmune diseases and inflammation, infectious diseases, and metabolic diseases.

公开(公告)号：US12128040B2

公开(公告)日：2024-10-29

申请号：US17254991

申请日：2019-07-11

申请人： Eli Lilly and Company

发明人： Jeffrey Daniel Cohen ,  Daniel Jon Sall

IPC分类号： A61K31/4709 ,  A61K9/00 ,  A61P35/00 ,  C07D401/12

CPC分类号： A61K31/4709 ,  A61K9/0053 ,  A61P35/00 ,  C07D401/12

摘要： Novel selective estrogen receptor degraders (SERDs) according to the formula: pharmaceutically acceptable salts, pharmaceutical compositions, uses, and methods of use thereof are provided.

公开(公告)号：US20240351987A1

公开(公告)日：2024-10-24

申请号：US18615563

申请日：2024-03-25

申请人： Escient Pharmaceuticals, Inc.

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

IPC分类号： C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

CPC分类号： C07D215/44 ,  C07D239/94 ,  C07D401/12 ,  C07D401/14 ,  C07D405/12 ,  C07D409/12 ,  C07D413/14 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04

摘要： Methods are provided for modulating MRGPR X2 generally, or for treating a MRGPR X2 dependent condition more specifically, by contacting the MRGPR X2 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 W, Z, R1, R2, R3, R4, R5, R6 and Rx are as defined herein. Pharmaceutical compositions containing such compounds, as well as the compounds themselves, are also provided.

公开(公告)号：US20240343682A1

公开(公告)日：2024-10-17

申请号：US18755058

申请日：2024-06-26

申请人： City of Hope

发明人： Linda H. Malkas ,  David Horne ,  Robert J. Hickey ,  Long Gu

IPC分类号： C07C233/76 ,  A61K31/167 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4725 ,  A61K33/243 ,  A61P35/00 ,  A61P35/02 ,  C07C237/22 ,  C07D213/68 ,  C07D217/26 ,  C07D401/12

CPC分类号： C07C233/76 ,  A61K31/167 ,  A61K31/4409 ,  A61K31/4418 ,  A61K31/4725 ,  A61K33/243 ,  A61P35/00 ,  A61P35/02 ,  C07C237/22 ,  C07D213/68 ,  C07D217/26 ,  C07D401/12

摘要： Described herein, inter alia, are compositions of PCNA modulators and methods for treating or preventing cancer.

公开(公告)号：US12116356B2

公开(公告)日：2024-10-15

申请号：US18106103

申请日：2023-02-06

申请人： CHIA TAI TIANQING PHARMACEUTICAL GROUP CO., LTD.

发明人： Yinsheng Zhang ,  Wangwei Ao ,  Yuan Li ,  Hui Wang ,  Hangzhou Shen ,  Jie Ni ,  Huan Zhang ,  Jie Wu ,  Li Zhang ,  Kai Cao ,  Peng Lu ,  Xushi Liu ,  Jie Wang ,  Tianxiao Zhao ,  Xingfeng Ge ,  Dandan Lu ,  Shuo Chen ,  Xueqin Ma ,  Wei Shi ,  Xiaojin Wang ,  Hongjiang Xu

IPC分类号： C07D401/12 ,  C07D207/34 ,  C07D405/12 ,  C07D409/12

CPC分类号： C07D401/12 ,  C07D207/34 ,  C07D405/12 ,  C07D409/12

摘要： A N-heterocyclic five-membered ring-containing capsid protein assembly inhibitor, and a pharmaceutical composition and use thereof, specifically relating to a compound as represented by formula I, a stereoisomer, a tautomer, a geometrical isomer, a solvate, an active metabolite, a hydrate, a prodrug or a pharmaceutically acceptable salt thereof, a pharmaceutical composition thereof, and a medical use thereof. The medical use comprises the use in treating diseases benefiting from the capsid protein assembly inhibitor, and in particular, diseases caused by hepatitis B virus infection.

公开(公告)号：US12116343B2

公开(公告)日：2024-10-15

申请号：US17161474

申请日：2021-01-28

申请人： Vertex Pharmaceuticals Incorporated

发明人： Leslie A. Dakin ,  Timothy J. Senter ,  Jingrong Cao ,  Jon H. Come ,  Francois Denis ,  Warren A. Dorsch ,  Anne Fortier ,  Martine Hamel ,  Elaine B. Krueger ,  Brian Ledford ,  Francois Maltais ,  Suganthini S. Nanthakumar ,  Olivier Nicolas ,  Camil E. Sayegh ,  Tiansheng Wang ,  Stephane Dorich ,  Lee Fader ,  Claudio Sturino ,  Janek Szychowski

IPC分类号： C07D209/18 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D491/107

CPC分类号： C07D209/18 ,  C07D401/12 ,  C07D403/04 ,  C07D403/12 ,  C07D403/14 ,  C07D405/12 ,  C07D413/12 ,  C07D451/02 ,  C07D491/107

摘要： The disclosure provides at least one entity chosen from compounds of Formula (I)






pharmaceutically acceptable salts thereof, solvates of any of the foregoing, and deuterated derivatives of any of the foregoing, compositions comprising the same, and methods of using the same, including use in treating APOL1 mediated kidney disease.

公开(公告)号：US12115228B2

公开(公告)日：2024-10-15

申请号：US17189135

申请日：2021-03-01

申请人： Concortis Biosystems, Corp.

发明人： Zhenwei Miao ,  Yufeng Hong ,  Tong Zhu ,  Alexander Wilhelm Chucholowski

IPC分类号： A61K47/68 ,  A61K38/07 ,  C07D207/08 ,  C07D207/09 ,  C07D277/593 ,  C07D401/12 ,  C07D403/12 ,  C07F5/02 ,  C07K5/06 ,  C07K5/062 ,  C07K5/103 ,  C07K7/06

CPC分类号： A61K47/6855 ,  A61K38/07 ,  A61K47/6803 ,  A61K47/6811 ,  A61K47/6849 ,  A61K47/6889 ,  C07D207/08 ,  C07D207/09 ,  C07D277/593 ,  C07D401/12 ,  C07D403/12 ,  C07F5/025 ,  C07K5/06008 ,  C07K5/06034 ,  C07K5/06052 ,  C07K5/1008 ,  C07K7/06

摘要： In one aspect, an active agent-conjugate, methods of preparing the active agent-conjugate, and uses thereof is provided.

公开(公告)号：US20240336592A1

公开(公告)日：2024-10-10

申请号：US18294014

申请日：2022-08-15

申请人： Redx Pharma PLC

发明人： Inder Bhamra ,  Clifford D. Jones ,  Ana Varela Rodriguez

IPC分类号： C07D401/12 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08

CPC分类号： C07D401/12 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/506 ,  A61K31/5377 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D471/04 ,  C07D487/04 ,  C07D491/08

摘要： This invention relates to novel compounds and pharmaceutical compositions comprising novel isoquinolone compounds. More specifically, the invention relates to compounds useful as inhibitors of discoidin domain receptor 1 (DDR1) and discoidin domain receptor 2 (DDR2). The compounds are particularly useful in the treatment of cancer and fibrotic diseases.

公开(公告)号：US12110278B2

公开(公告)日：2024-10-08

申请号：US17500622

申请日：2021-10-13

申请人： YALE UNIVERSITY

发明人： William L. Jorgensen ,  Joseph Schlessinger

IPC分类号： C07D249/14 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

CPC分类号： C07D249/14 ,  A61K31/4196 ,  A61K31/4245 ,  A61K31/4439 ,  A61K45/06 ,  C07D401/12 ,  C07D405/12 ,  C07D413/12

摘要： The compounds of Formula I described herein regulate activity of JAK2 by specifically binding to the JAK2 pseudokinase domain, JH2, and are useful as therapeutic agents in the treatment or amelioration of myeloproliferative disorders. Also provided herein are methods of treating myeloproliferative disorders, and methods of making compounds of Formula I.