公开(公告)号：US20250064808A1

公开(公告)日：2025-02-27

申请号：US18942238

申请日：2024-11-08

Applicant: The Regents of the University of California

Inventor： Michael Karin ,  Hongxu Xian

IPC: A61K31/517 ,  A61P37/06 ,  C12N15/113

Abstract: Provided herein are methods for treating a disease or condition associated with one or more of: mtDNA fragmentation; cytostolic Ox-mtDNA; mtDNA release; or Casp1 activation and IL-1β production by administering an effective amount of an inhibitor of human flap endonuclease-1 (FEN1). These diseases include without limitation, an inflammatory or a neurodegenerative disease, such as Alzheimer's, disease, Parkinson's disease, atherosclerosis, NASH, asthma, inflammatory bowel disease, melanoma, metabolic pathologies, including obesity, type 2 diabetes, atherosclerosis, inflammatory bowel diseases, gout, and periodic fevers.

公开(公告)号：US20250059196A1

公开(公告)日：2025-02-20

申请号：US18723812

申请日：2022-12-29

Applicant: SHANGHAI HANSOH BIOMEDICAL CO., LTD. ,  JIANGSU HANSOH PHARMACEUTICAL GROUP CO., LTD.

Inventor： Jianrui Wu ,  Jiaqiang Dong ,  Fangfang Jin ,  Wensheng Yu ,  Lipu Zhang

IPC: C07D487/04 ,  A61K31/4155 ,  A61K31/4192 ,  A61K31/437 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/4725 ,  A61K31/473 ,  A61K31/4745 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61P35/00 ,  C07D401/12 ,  C07D401/14 ,  C07D403/14 ,  C07D405/14 ,  C07D409/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04

Abstract: The invention relates to a tricyclic derivative inhibitor, a preparation method therefor, and application thereof. In particular, the present invention relates to a compound as shown in general formula (I), a preparation method therefor, a pharmaceutical composition containing the compound, as well as a use thereof in the treatment of cancer and autoimmune diseases, wherein each substituent in general formula (I) is the same as the definition in the description.

公开(公告)号：US20250059162A1

公开(公告)日：2025-02-20

申请号：US18723083

申请日：2022-12-22

Applicant: SUZHOU KINTOR PHARMACEUTICALS, INC.

Inventor： Zhaohui YANG ,  Songying LIU ,  Jie PAN ,  Dong CHEN ,  Ruo XU ,  Liandong MA ,  Youzhi TONG

IPC: C07D401/14 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/513 ,  A61K31/517 ,  A61K31/53 ,  A61P35/00 ,  C07D405/14 ,  C07D471/04 ,  C07D487/04 ,  C07D495/04

Abstract: Provided is a multi-protein degradation agent having an imide skeleton, which can degrade multiple proteins comprising c-Myc, GSPT1, CK1α and IKZF (1/2/3) proteins, and therefore can be used for treating diseases or disorders related thereto, such as cancer.

公开(公告)号：US20250041226A1

公开(公告)日：2025-02-06

申请号：US18722868

申请日：2022-12-20

Applicant: PALAU PHARMA, S.L.U.

Inventor： MONTSERRAT SURIOL FERRER ,  MARTA BUSQUETS BAQUÉ

IPC: A61K9/16 ,  A61K31/517

Abstract: The present invention provides an oral solid pharmaceutical composition in the form of a multiparticulate composition comprising albaconazole, a process for the preparation of the composition of the invention, and its use in therapy.

公开(公告)号：US20250032788A1

公开(公告)日：2025-01-30

申请号：US18759109

申请日：2024-06-28

Applicant: NOVOCURE GMBH

Inventor： Eyal Dor-On ,  Spencer J. Collis ,  Callum George Jones ,  Ola Rominiyi ,  Lilach Avigdor

IPC: A61N1/36 ,  A61K31/4985 ,  A61K31/506 ,  A61K31/517

Abstract: Disclosed herein is the use of alternating electric fields and a DNA-dependent PK inhibitor to treat cancer. Disclosed herein is the use of alternating electric fields and a DNA-dependent PK inhibitor for inducing cell death. Disclosed herein is the use of alternating electric fields and a DNA-dependent PK inhibitor for inhibiting DNA repair in a cancer cell having double stranded DNA breaks. Disclosed herein is the use of alternating electric fields and a DNA-dependent PK inhibitor for increasing efficacy of radiation therapy.

公开(公告)号：US20250032501A1

公开(公告)日：2025-01-30

申请号：US18580831

申请日：2022-07-21

Applicant: Memorial Sloan-Kettering Cancer Center ,  Memorial Hospital for Cancer and Allied Diseases ,  Sloan-Kettering Institute for Cancer Research

Inventor： Frederic Geissmann ,  Rocio Vicario

IPC: A61K31/5377 ,  A61K31/166 ,  A61K31/18 ,  A61K31/365 ,  A61K31/404 ,  A61K31/4184 ,  A61K31/437 ,  A61K31/44 ,  A61K31/4412 ,  A61K31/4418 ,  A61K31/4439 ,  A61K31/4523 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/505 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61P25/28

Abstract: The present technology relates to methods for treating, preventing, and/or ameliorating Alzheimer's disease, in a subject in need thereof. In particular aspects, the present technology relates to the use of MAPK inhibitors to treat, prevent, and/or ameliorate Alzheimer's disease.

公开(公告)号：US20250026748A1

公开(公告)日：2025-01-23

申请号：US18696850

申请日：2022-09-29

Applicant: Repare Therapeutics Inc.

Inventor： Bingcan LIU ,  Alexander PERRYMAN ,  Philippe MOCHIRIAN ,  Michel GALLANT ,  David BENDAHAN ,  Simon SURPRENANT ,  Janek SZYCHOWSKI ,  Evelyne DIETRICH ,  Boubacar SOW ,  Monica BUBENIK

IPC: C07D417/14 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/5355 ,  A61K31/5377 ,  A61K31/541 ,  A61K31/55 ,  A61K31/551 ,  C07D417/12 ,  C07D471/04 ,  C07D487/04 ,  C07D491/107

Abstract: Disclosed are compounds of formula (I), wherein V is N or CR; W is optionally substituted alkylene, alkenylene, alkynylene, cycloalkylene, or arylene; X is optionally substituted heterocyclylene, heteroarylene, arylene, wherein X may be substituted with -L1-Rx, wherein L1 is —O—, —NRX1—, optionally substituted heterocyclylene, heteroarylene, or cycloalkylene, Rx is optionally substituted alkyl, heteroalkyl, heterocyclyl, heteroaryl, cycloalkyl C1-6 alkyl, or heteroaryl C1-6alkyl, and RX1 is hydrogen or optionally substituted alkyl; Y is optionally substituted heterocyclyl, heteroaryl, or aryl; Z is a H, optionally substituted alkyl, alkynyl, alkoxy, cycloalkyl, heterocyclyl, heteroaryl, or aryl; and R is hydrogen, halogen, optionally substituted alkyl, CN, cycloalkyl, alkoxy, cycloalkoxy, N(R1)2, or C(O)NHz, wherein each R1 is hydrogen alkyl, or cycloalkyl. The compounds of formula (I) are useful for inhibiting human Polymerase Theta (Polθ) and for treating cancers, such as carcinoma, sarcoma, adenocarcinoma, leukemia, lymphoma, and melanoma.

公开(公告)号：US12201635B2

公开(公告)日：2025-01-21

申请号：US17441618

申请日：2019-11-27

Applicant: GUANGZHOU LIUSHUN BIOTECHNOLOGY CO., LTD. ,  BEIJING BEIKEHUAXIA BIO-MEDICAL TECHNOLOGY CO., LTD.

Inventor： Bing Liu ,  Jingsi Dai ,  Yan Wang ,  Xueqi Qian ,  Junjun Dong ,  Xihong Liu ,  Lianwu Deng ,  Shuang Xie ,  Daping Li ,  Nengan Chen ,  Jin Ma

IPC: A61K31/517 ,  A61P35/00

Abstract: A multi-target kinase inhibitor is shown in formula (I), in which R is selected from formula (a), formula (b), formula (c), formula (d), formula (e) and formula (f). The multi-target kinase inhibitor can effectively inhibit the enzymatic activities of RET, VEGFR3 and PDGFRA, and can effectively treat diseases that are regulated and controlled by multi-target kinases and are related to abnormal signal transduction pathways of the multi-target kinases, including cancers of breast, respiratory tract, brain, reproductive organ, digestive tract, urinary tract, eye, liver, skin, head and/or neck and distant metastatic cancers thereof, and lymphoma, sarcoma, leukemia and the like. The active ingredients of the pharmaceutical composition of the present invention comprise a multi-target kinase inhibitor, which accounts for 1-50 wt % of the composition.

公开(公告)号：US12201592B2

公开(公告)日：2025-01-21

申请号：US17159798

申请日：2021-01-27

Applicant: TYRNOVO LTD.

Inventor： Hadas Reuveni ,  Izhak Haviv ,  Lana Kupershmidt

IPC: A61K31/165 ,  A61K31/436 ,  A61K31/4375 ,  A61K31/505 ,  A61K31/517 ,  A61K31/519 ,  A61K39/395 ,  C07K16/28

Abstract: Provided is a treatment of cancer using a dual modulator of Insulin Receptor Substrate (IRS) and signal transducer and activator of transcription 3 (Stat3), as well with other agents. The combination can be used to treat a tumor that has developed resistance to an EGFR inhibitor, EGFR antibody, mTOR inhibitor, MEK inhibitor, mutated B-Raf inhibitor, chemotherapeutic agents, and certain combinations thereof, or to prevent acquired resistance of a tumor to any of said inhibitors or agents, or to prevent tumor recurrence following cease of treatment with any of said inhibitors or agents or a combination thereof. The subject matter further provides a treatment of cancer using combination therapy comprising a dual modulator of IRS and Stat3, in combination with an immunotherapy agent. The combination can be used to sensitize a tumor to immunotherapy.

公开(公告)号：US20250018055A1

公开(公告)日：2025-01-16

申请号：US18902040

申请日：2024-09-30

Applicant: L.E.A.F. HOLDINGS GROUP LLC

Inventor： Clet NIYIKIZA ,  Victor Mandla MOYO

IPC: A61K47/69 ,  A61K9/127 ,  A61K31/517 ,  A61K31/519 ,  A61K45/06 ,  A61K47/10 ,  A61K47/54 ,  A61K47/64 ,  A61K47/68 ,  A61P19/02 ,  A61P35/00 ,  B82Y5/00 ,  C07K16/28

Abstract: The disclosure relates generally to polyglutamated antifolates, formulations containing liposomes filled with alpha or D-gamma polyglutamated antifolates, methods of making the polyglutamated antifolates and liposome containing formulations, and methods of using polyglutamated antifolates and liposome containing formulations to treat hyerproliferative disorders (e.g., cancer) and disorders of the immune system (e.g., an autoimmune disease such as rheumatoid arthritis).