公开(公告)号：US20250066379A1

公开(公告)日：2025-02-27

申请号：US18716280

申请日：2022-12-05

Applicant: Merck Sharp & Dohme LLC ,  The Walter and Eliza Hall Institute of Medical Research ,  MSD R&D (China) Co., Ltd.

Inventor： John A. McCauley ,  Manuel De Lera Ruiz ,  Zhuyan Guo ,  Philippe Nantermet ,  Michael J. Kelly, III ,  Alvaro Gutierrez Bonet ,  Lianyun Zhao ,  Zhiyu Lei ,  Bin Hu ,  Dongmei Zhan ,  Anthony Hodder

IPC: C07D491/22 ,  A61K31/519 ,  A61K45/06 ,  C07D487/08 ,  C07D491/048 ,  C07D491/052 ,  C07D519/00

Abstract: Provided are methods of treating malaria comprising administration of compounds of Formula (I), or a pharmaceutically acceptable salt thereof, to a subject in need thereof, wherein the variables are as defined herein. Also provided are uses of the compounds of Formula (I), as defined herein, for inhibiting plasmepsin X, plasmepsin IX or plasmepsin X and IX activity, for treating a Plasmodium infection, and for treating malaria. Also provided are methods of treatment further comprising administration of one or more additional anti-malarial compounds.

公开(公告)号：US12234222B2

公开(公告)日：2025-02-25

申请号：US17602758

申请日：2020-04-09

Applicant: ZHEJIANG HISUN PHARMACEUTICAL CO., LTD.

Inventor： Panpan Zhang ,  Sunli Yan ,  Ying Li ,  Chenli Guo ,  Wenjian Qian ,  Cheng Ye ,  Zhengzheng Shi ,  Taishan Hu ,  Lei Chen

IPC: C07D401/14 ,  C07D403/14 ,  C07D487/08 ,  C07D498/08

Abstract: The present invention relates to a piperazine amide derivative as represented by formula (I) or a pharmaceutically acceptable salt thereof, and a pharmaceutical composition thereof, and use of same as a therapeutic agent, especially as a selective Rearranged During Transfection (RET) kinase inhibitor. Ring a, ring e, X1, X2, X3, X4, R1, R2, R3, R4, R4′, R5, R5′, R6, R6′, R7, R7′, R8, m and n have the same definitions as those in the specification.

公开(公告)号：US20250059205A1

公开(公告)日：2025-02-20

申请号：US18696946

申请日：2022-04-28

Applicant: AMGEN INC.

Inventor： Brian Alan Lanman ,  Ryan Paul Wurz ,  Wei Zhao ,  Xiaofen Li ,  Michael M. Yamano ,  Yunxiao Li ,  Ning Chen ,  Birgitte Weinreich Husemoen ,  Sebastian Leth-Petersen ,  Jose M. Medina ,  Kexue Li ,  Liping Pettus ,  Rene Rahimoff ,  Primali Vasundera Navaratne ,  Huan Rui ,  Christopher P. Mohr

IPC: C07D519/00 ,  A61K31/4995 ,  A61K31/517 ,  C07D487/08

Abstract: The present disclosure provides compounds useful for the inhibition of KRAS G12D. The compounds have a general Formula I: (I) wherein the variables of Formula I are defined herein. This disclosure also provides pharmaceutical compositions comprising the compounds, uses of the compounds, and compositions for treatment of, for example, cancer.

公开(公告)号：US20250059198A1

公开(公告)日：2025-02-20

申请号：US18710130

申请日：2022-11-23

Applicant: Arvinas Operations, Inc. ,  Genentech, Inc.

Inventor： Michael Berlin ,  Fabio Broccatelli ,  Huifen Chen ,  Peter Scott Dragovich ,  Jing Wang

IPC: C07D487/08 ,  A61K31/501 ,  A61K31/5377 ,  A61K31/5386 ,  A61K31/551 ,  C07D413/14 ,  C07D417/14 ,  C07D498/10

Abstract: The present disclosure relates to bifunctional compounds, which find utility as modulators of SMARCA2 or BRM (target protein). In particular, the present disclosure is directed to bifunctional compounds, which contain on one end a ligand that binds to the Von Hippel-Lindau E3 ubiquitin ligase, and on the other end a moiety which binds the target protein, such that the target protein is placed in proximity to the ubiquitin ligase to effect degradation (and inhibition) of target protein. The present disclosure exhibits a broad range of pharmacological activities associated with degradation/inhibition of target protein. Diseases or disorders that result from aggregation or accumulation of the target protein are treated or prevented with compounds and compositions of the present disclosure.

公开(公告)号：US20250026762A1

公开(公告)日：2025-01-23

申请号：US18712270

申请日：2022-11-28

Applicant: Merck Sharp & Dohme LLC

Inventor： Mark E. Fraley ,  Tao Liang ,  H. Marie Loughran ,  Anthony J. Roecker ,  Kathy M. Schirripa ,  Ling Tong ,  Ashwin U. Rao

IPC: C07D487/08 ,  A61K31/551 ,  C07D519/00

Abstract: The present invention relates to Compounds of Formula (I) and pharmaceutically acceptable salts or prodrug thereof. The present invention also relates to compositions comprising at least one compound of Formula (I), and methods of using the compounds of Formula (I) for treatment or prophylaxis of lysosomal storage diseases, neurodegenerative disease, cystic disease, cancer, or a diseases or disorders associated with elevated levels of glucosylceramide (GlcCer), glucosylsphingosine (GlcSph) and/or other glucosylceramide-based glycosphingolipids (GSLs).

公开(公告)号：US12180243B2

公开(公告)日：2024-12-31

申请号：US17752960

申请日：2022-05-25

Applicant: BEIJING TIDE PHARMACEUTICAL CO., LTD.

Inventor： Yanping Zhao ,  Hongjun Wang ,  Yeming Wang ,  Xiang Li ,  Yuanyuan Jiang ,  Huai Huang ,  Fajie Li ,  Liying Zhou ,  Ning Shao ,  Fengping Xiao ,  Zhenguang Zou

IPC: C07D241/38 ,  A61K31/4995 ,  C07D471/08 ,  C07D487/08 ,  C07F9/6561

Abstract: The present invention discloses a receptor inhibitor of formula (I), a pharmaceutical composition comprising the same and the use thereof.

公开(公告)号：US20240425493A1

公开(公告)日：2024-12-26

申请号：US18740140

申请日：2024-06-11

Applicant: THE TRUSTEES OF INDIANA UNIVERSITY ,  KOVINA THERAPEUTICS INC.

Inventor： Elliot J. ANDROPHY ,  Samy MEROUEH ,  Anne RIETZ ,  Zhijian LU

IPC: C07D413/14 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  C07D403/04 ,  C07D403/14 ,  C07D471/04 ,  C07D487/08 ,  C07D487/10 ,  C07D495/04

Abstract: Compositions and methods are provided for treating HPV infections including pre-malignant and cancers. Compounds that specifically bind to the HPV E6 protein and inactivate the protein are disclosed.

公开(公告)号：US20240415851A1

公开(公告)日：2024-12-19

申请号：US18605319

申请日：2024-03-14

Applicant: The University of Chicago ,  The United States of America, as Represented by the Secretary, Department of Health and Human ,  President and Fellows of Harvard College ,  IIT Research Institute ,  Beth Israel Deaconess Medical Center, Inc.

Inventor： Julian SOLWAY ,  Nickolai DULIN ,  Marsha ROSNER ,  Gokhan MUTLU ,  Diane LUCI ,  David MALONEY ,  Chan Young PARK ,  Jeffrey FREDBERG ,  David MCCORMICK ,  Ramaswamy KRISHNAN

IPC: A61K31/635 ,  A61K31/18 ,  A61K31/63 ,  A61P35/04 ,  C07C311/16 ,  C07C311/21 ,  C07D207/48 ,  C07D211/34 ,  C07D211/96 ,  C07D239/42 ,  C07D241/04 ,  C07D265/30 ,  C07D277/52 ,  C07D279/12 ,  C07D295/13 ,  C07D295/26 ,  C07D309/14 ,  C07D401/12 ,  C07D471/04 ,  C07D487/08 ,  C07D491/113

Abstract: Disclosed herein is a class of molecules termed remodilins that inhibit serum response factor (SRF). By inhibiting SRF, a number of downstream pathways can be targeted. The remodilins can be used to treat glaucoma, inhibit tumor cell growth, inhibit tumor metastasis, inhibit hypoxia-induced response, and/or reduce cellular metabolism.

公开(公告)号：US12157730B2

公开(公告)日：2024-12-03

申请号：US17701478

申请日：2022-03-22

Applicant: VORONOI INC.

Inventor： Youn Ho Lee ,  Ju Hee Kang ,  Se In Kang ,  Yi Kyung Ko ,  Eun Hwa Ko ,  Hwan Geun Choi ,  Jung Beom Son ,  Nam Doo Kim

IPC: C07D413/14 ,  A61P35/00 ,  C07D413/04 ,  C07D487/08 ,  C07D498/08

Abstract: The present invention relates to a 6-(isooxazolidin-2-yl)-N-phenylpyrimidin-4-amine derivative, and a pharmaceutical composition for preventing or treating cancer comprising the compound as an effective component. The compound exhibits high inhibitory activity against an epidermal growth factor receptor (EGFR) variant, or wild-type or variants of one or more of ERBB2 and ERBB4, and thus may be usefully used in the treatment of cancers in which same are expressed. In particular, the compound exhibits excellent inhibitory activity on proliferation of lung cancer cell lines, and thus can be usefully used in the treatment of lung cancer.

公开(公告)号：US12152015B2

公开(公告)日：2024-11-26

申请号：US18109705

申请日：2023-02-14

Applicant: Stingray Therapeutics, Inc.

Inventor： Srinivas Rao Kasibhatla ,  Raman Kumar Kalakuntla ,  Alexis Weston ,  Trason Thode ,  Sunil Sharma ,  Mohan R. Kaadige

IPC: C07D403/04 ,  A61P35/00 ,  C07D215/54 ,  C07D239/74 ,  C07D239/88 ,  C07D239/94 ,  C07D401/04 ,  C07D401/14 ,  C07D403/14 ,  C07D487/08

Abstract: Compounds and methods for their preparation and use as therapeutic or prophylactic agents, for example for treatment of cancer, bacterial or viral diseases by targeting Ectonucleotide Pyrophosphatase/Phosphodiesterase-1 (ENPP1).