公开(公告)号：US20250066358A1

公开(公告)日：2025-02-27

申请号：US18718012

申请日：2022-12-09

Applicant: Bala Therapeutics, Inc.

Inventor： Ruben Abagyan ,  Vladislav Zenonovich Parchinsky ,  Alexander Khvat ,  Alexandre Vasilievich Ivachtchenko ,  Nikolay Savchuk

IPC: C07D471/10 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/538 ,  A61K31/5415 ,  A61K31/554 ,  C07D401/12 ,  C07D403/12 ,  C07D519/00

Abstract: The present invention is directed to the compounds of Formula (I)—inhibitors of the interaction of menin and MLL. The inhibitors described herein can be useful in the treatment of diseases or disorders associated with menin-MLL interaction, such as cancer. In particular, the invention is concerned with compounds and pharmaceutical compositions inhibiting/blocking menin-MLL interaction, methods of treating diseases or disorders associated with menin-MLL interaction, and methods of synthesizing these compounds.

公开(公告)号：US20250064967A1

公开(公告)日：2025-02-27

申请号：US18724710

申请日：2022-12-27

Applicant: AstraZeneca UK Limited ,  DAIICHI SANKYO COMPANY , LIMITED

Inventor： Matthew Simon SUNG ,  Alan Yin Kai LAU ,  Yann WALLEZ ,  Jerome Thomas METTETAL, II ,  Theresa Angela PROIA ,  Suzanne Jane RANDLE ,  Mark John ANDERTON

IPC: A61K47/68 ,  A61K31/5377 ,  A61P35/00

Abstract: A pharmaceutical product for administration of an anti TROP2 antibody-drug conjugate in combination with an ATR inhibitor is provided. The anti-TROP2 antibody-drug conjugate is an antibody-drug conjugate in which a drug linker represented by the following formula (wherein A represents the connecting position to an anti-TROP2 antibody) is conjugated to an anti-TROP2 antibody via a thioether bond. Also provided is a therapeutic use and method wherein the anti-TROP2 antibody-drug conjugate and the ATR inhibitor are administered in combination to a subject: Formula (I).

公开(公告)号：US20250064732A1

公开(公告)日：2025-02-27

申请号：US18825795

申请日：2024-09-05

Applicant: PFIZER INC.

Inventor： James Joseph HUSSEY ,  Andrew Gilbert Bright

IPC: A61K9/08 ,  A61K9/00 ,  A61K9/19 ,  A61K31/5377 ,  A61K47/02 ,  A61K47/12 ,  A61K47/26 ,  A61K47/40 ,  A61P35/00

Abstract: The present invention relates to a pharmaceutical aqueous formulation comprising 1-(4-{[4-(dimethylamino)piperidin-1-yl]carbonyl}phenyl)-3-[4-(4,6-dimorpholin-4-yl-1,3,5-triazin-2-yl)phenyl]urea, or a pharmaceutically acceptable organic or inorganic acid salt thereof, a pharmaceutically acceptable organic or inorganic acid, a pharmaceutically acceptable beta- or gamma-cyclodextrin and water, that is a clear solution, with the proviso that the organic or inorganic acid (including a salt thereof) is not a sulphonic acid. Such a formulation is particularly suitable for intravenous or parenteral administration to a patient.

公开(公告)号：US20250059201A1

公开(公告)日：2025-02-20

申请号：US18720569

申请日：2022-12-16

Applicant: MABWELL (SHANGHAI) BIOSCIENCE CO., LTD. ,  JIANGSU MABWELL HEALTH PHARMACEUTICAL R&D CO., LTD.

Inventor： Wei ZHOU ,  Hui XU ,  Huikai ZHU ,  Zhenzhen WANG ,  Xiaoding TAN

IPC: C07D491/22 ,  A61K31/4745 ,  A61K31/506 ,  A61K31/5377 ,  A61K47/54 ,  A61P35/00 ,  C07D495/22

Abstract: Provided is a camptothecin compound, which is a compound represented by structural formula I or a pharmaceutically acceptable salt, stereoisomer, solvate or prodrug thereof. An antibody-drug conjugate comprising the camptothecin compound is also provided.

公开(公告)号：US20250059188A1

公开(公告)日：2025-02-20

申请号：US18722104

申请日：2022-12-22

Applicant: Anaxis Pharma Pty Ltd

Inventor： Martin Brzozowski ,  Christophe Poitevin ,  Jean-Marc Daniel Garnier ,  Christopher Gardner ,  Guillaume Laurent Lessene ,  Peter Edward Czabotar ,  Carole Annie Schuster-Klein ,  Katherine Davies ,  Angus Cowan ,  Wilhelmus Johannes Antonius Kersten

IPC: C07D471/04 ,  A61K31/4355 ,  A61K31/437 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/55 ,  C07D487/04 ,  C07D491/08 ,  C07D519/00

Abstract: This invention relates to compounds of formula (I) and salts, solvates, tautomers, N-oxides, stereoisomers, polymorphs and/or prodrugs thereof. Also disclosed is the use of the compounds of formula (I) to treat necroptosis and/or inhibit MLKL.

公开(公告)号：US20250059179A1

公开(公告)日：2025-02-20

申请号：US18696948

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 ,  Sebastian Leth-Petersen ,  Kexue Li ,  Liping Pettus ,  Rene Rahimoff ,  Primali Vasundera Navaratne ,  Huan Rui

IPC: C07D417/14 ,  A61K31/517 ,  A61K31/5377 ,  A61K31/5383 ,  A61K31/5386 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  C07D471/04 ,  C07D471/08 ,  C07D487/04 ,  C07D487/10 ,  C07D487/20 ,  C07D498/04 ,  C07D498/10 ,  C07D519/00

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：US20250059164A1

公开(公告)日：2025-02-20

申请号：US18751286

申请日：2024-06-23

Applicant: Kymera Therapeutics, Inc.

Inventor： Xiaozhang ZHENG ,  Nello Mainolfi ,  Matthew M. Weiss

IPC: C07D401/14 ,  A61K31/4545 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5377 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D519/00

Abstract: The present invention provides compounds, compositions thereof, and methods of using the same.

公开(公告)号：US20250057930A1

公开(公告)日：2025-02-20

申请号：US18936652

申请日：2024-11-04

Applicant: The Children's Medical Center Corporation

Inventor： Roberto Chiarle ,  Rafael Blasco-Patino

IPC: A61K39/00 ,  A61K31/439 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/501 ,  A61K31/506 ,  A61K31/5377 ,  A61K31/7084 ,  A61K39/395 ,  C12N9/12

Abstract: The invention features compositions and methods for treating anaplastic lymphoma kinase (ALK)-rearranged neoplasias including Non-Small Cell Lung Cancers (NSCLCs). The methods involve administering to a subject ALK peptides and/or polynucleotides encoding the ALK peptides, optionally in combination with an immune checkpoint inhibitor (ICI) and/or an ALK tyrosine kinase inhibitor (TKI).

公开(公告)号：US12226420B2

公开(公告)日：2025-02-18

申请号：US18433881

申请日：2024-02-06

Applicant: HMI MEDICAL INNOVATIONS, LLC

Inventor： Gerard M. Housey

IPC: A61K31/5377 ,  A61K31/166 ,  A61K31/175 ,  A61K31/195 ,  A61K31/27 ,  A61K31/415 ,  A61K31/4196 ,  A61K31/44 ,  A61K31/4436 ,  A61K31/444 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/495 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/53 ,  C07C243/38 ,  C07D213/77 ,  C07D213/81 ,  C07D213/86 ,  C07D213/87 ,  C07D215/38 ,  C07D215/50 ,  C07D231/14 ,  C07D239/42 ,  C07D239/48 ,  C07D239/84 ,  C07D253/065 ,  C07D253/075 ,  C07D401/12 ,  C07D403/12 ,  C07D405/12 ,  C07D409/12 ,  G01N33/50 ,  G01N33/573 ,  G01N33/574

Abstract: This invention relates to agents that are inhibitors or activators of variant forms of endogenous proteins and novel methods of identifying such variants. Of particular interest are inhibitors and activators of endogenous protein variants, encoded by genes which have mutated, which variants often arise or are at least first identified as having arisen following exposure to a chemical agent which is known to be an inhibitor or activator of the corresponding unmutated endogenous protein.

公开(公告)号：US12226414B2

公开(公告)日：2025-02-18

申请号：US17274781

申请日：2019-09-16

Applicant: SUZHOU ZANRONG PHARMA LIMITED

Inventor： Ding Zhou ,  Ziqiang Cheng

IPC: A61K31/5025 ,  A61K31/5377 ,  C07D487/04

Abstract: The present application relates to novel substituted imidazo[4,5-c]cinnolin-2-one compounds and pharmaceutically acceptable salts thereof, which selectively modulate ataxia telangiectasia mutated (“ATM”) kinase. The present application also relates to pharmaceutical compositions comprising one or more of the compounds and salts thereof as an active ingredient, and to the use of the compounds and salts thereof in the treatment of ATM-associated diseases or conditions, including cancers.