公开(公告)号：US20250066504A1

公开(公告)日：2025-02-27

申请号：US18847463

申请日：2023-03-16

Applicant: CANARIABIO INC.

Inventor： Christopher F. NICODEMUS ,  Ragupathy MADIYALAKAN

IPC: C07K16/30 ,  A61K31/454 ,  A61K39/00

Abstract: The present document describes a method for improving likelihood of survival in a stage III-IV ovarian cancer patient. The method comprises at least steps of (a) administering daily to a stage III-IV ovarian cancer patient a therapeutically effective dose of Niraparib, for at least 12 weeks; and (b) administering to the patient a therapeutically effective dose of monoclonal antibody mAb-B43.13 during week 1, week 4, week 7, week 12 and week 20 of a treatment period, wherein (a) is performed first and step (b) is performed second, to increase the patient's likelihood of survival in comparison with a control patient who has been diagnosed with stage III-IV ovarian cancer and has received standard of care chemotherapy treatment.

公开(公告)号：US20250066501A1

公开(公告)日：2025-02-27

申请号：US18825958

申请日：2024-09-05

Applicant: Janssen Biotech, Inc.

Inventor： Tahamtan Ahmadi ,  Tineke Casneuf ,  Henk Lokhorst ,  Tuna Mutis ,  Amy Sasser ,  Niels van de Donk

IPC: C07K16/28 ,  A61K31/454 ,  A61K31/573 ,  A61K38/47 ,  A61K39/00 ,  A61K39/395 ,  A61K45/06 ,  C07K16/40

Abstract: The present invention relates to methods of immunomodulation and treating patients having solid tumors with antibodies that specifically bind CD38.

公开(公告)号：US20250066318A1

公开(公告)日：2025-02-27

申请号：US18717613

申请日：2022-12-09

Applicant: Prothena Biosciences Limited

Inventor： Stéphane DE LOMBAERT

IPC: C07D401/04 ,  A61K31/415 ,  A61K31/4155 ,  A61K31/427 ,  A61K31/437 ,  A61K31/4439 ,  A61K31/444 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/4725 ,  A61K31/496 ,  A61K31/497 ,  A61K31/4985 ,  A61K31/501 ,  A61K31/502 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/5377 ,  A61K31/5415 ,  C07D231/40 ,  C07D277/46 ,  C07D401/12 ,  C07D403/12 ,  C07D405/14 ,  C07D413/04 ,  C07D417/04 ,  C07D417/06 ,  C07D417/12 ,  C07D417/14 ,  C07D471/04 ,  C07D471/14 ,  C07D487/04 ,  C07D491/08 ,  C07D493/04 ,  C07D493/08 ,  C07D519/00

Abstract: This disclosure provides compounds and pharmaceutically acceptable salts thereof, that inhibit Dual specificity tyrosine-phosphorylation-regulated kinase 1A (DYRK1A). These chemical entities are useful, e.g., for treating a condition, disease or disorder in which increased (e.g., excessive) DYRK1A activation contributes to the pathology and/or symptoms and/or progression of the condition, disease or disorder (e.g., a neurological disorder) in a subject (e.g., a human). This disclosure also provides compositions containing the same as well as methods of using and making the same.

公开(公告)号：US20250066308A1

公开(公告)日：2025-02-27

申请号：US18696807

申请日：2022-09-29

Applicant: YUHAN CORPORATION

Inventor： Eun-Kyung KIM ,  Cheol-Hee LIM ,  Kang-Yo LEE ,  Hyun-Ho CHOI

IPC: C07D235/14 ,  A61K31/4184 ,  A61K31/4192 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/496 ,  A61K31/506 ,  A61K31/52 ,  A61K31/5377 ,  A61K31/675 ,  C07D249/18 ,  C07D403/10 ,  C07D403/12 ,  C07D487/04 ,  C07F9/6506 ,  C07F9/6518

Abstract: Provided are a bicyclic fused ring such as for example, benzo[d]imidazole, benzo[d][1,2,3]triazole, or 8-oxo-8,9-dihydro-7H-purine derivatives or pharmaceutically acceptable salt thereof, a process for the preparation thereof, a pharmaceutical composition comprising the same and a use thereof, wherein the bicyclic fused ring derivative or pharmaceutically acceptable salt thereof has an inhibitory activity against the lysyl oxidase family and can be usefully applied for preventing or treating various diseases associated with the lysyl oxidase family, such as idiopathic pulmonary fibrosis (IPF), non-alcoholic steatohepatitis (NASH), chronic kidney disease (CKD), or liver cirrhosis.

公开(公告)号：US20250064833A1

公开(公告)日：2025-02-27

申请号：US18719194

申请日：2022-12-13

Applicant: SAGE THERAPEUTICS, INC.

Inventor： Michael C. Quirk ,  Aaron Michael Koenig

IPC: A61K31/575 ,  A61K31/4365 ,  A61K31/4375 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/47 ,  A61K31/4709 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/517 ,  A61K31/519 ,  A61K31/538 ,  A61K31/58

Abstract: The present disclosure relates to compositions, kits, and methods of treating CNS diseases and disorders using a combination of a muscarinic receptor positive modulator and an NMDA receptor positive allosteric modulator.

公开(公告)号：US20250059156A1

公开(公告)日：2025-02-20

申请号：US18799037

申请日：2024-08-09

Applicant: Sensorium Therapeutics, Inc.

Inventor： Jacob M. Hooker ,  Michael S. Placzek

IPC: C07D401/04 ,  A61K31/404 ,  A61K31/407 ,  A61K31/4155 ,  A61K31/454 ,  A61K31/5377 ,  C07D209/12 ,  C07D209/70 ,  C07D403/04 ,  C07D413/04 ,  C07D491/044 ,  C07D491/107

Abstract: Disclosed are compounds that are derivatives of mesembrine or mesembrenone, and related methods of preparing and using the compounds. The disclosed compounds inhibit PDE4.

公开(公告)号：US12226424B2

公开(公告)日：2025-02-18

申请号：US17046690

申请日：2019-04-09

Applicant: ShanghaiTech University

Inventor： Xiaobao Yang ,  Biao Jiang ,  Renhong Sun ,  Chaowei Ren ,  Ning Sun ,  Ying Kong ,  Yan Li ,  Jinju Chen ,  Qianqian Yin ,  Xiaoling Song ,  Quanju Zhao ,  Xing Qiu

IPC: A61K31/675 ,  A61K31/138 ,  A61K31/454 ,  A61K31/496 ,  A61K31/5025 ,  A61K31/506 ,  A61K31/519 ,  A61K31/5517 ,  A61K45/06 ,  A61K47/54 ,  A61K47/60 ,  A61P35/00

Abstract: The present disclosure relates to compounds of formula (I) and their anti-tumor uses, and their intermediates of formula (III), intermediates of formula (IV), and uses of the intermediates. The compound of formula (I) has a degrading effect on a specific target protein, which is mainly composed of three parts. The first part is a small molecule compound (SMBP, Small Molecules Binding Protein) that can bind to a protein, the second part LIN is a linker, and the three-part ULM is a ubiquitin ligand (ULM, Ubiquitin Ligase Binding Moiety), wherein SMBP is covalently bound to LIN, and LIN is covalently bound to ULM. A series of compounds designed and synthesized in the present disclosure have a wide range of pharmacological activities, including the functions of degrading specific proteins and/or inhibiting activities of specific proteins, and thus can be used in related tumor treatments.

公开(公告)号：US20250051347A1

公开(公告)日：2025-02-13

申请号：US18293289

申请日：2022-07-29

Applicant: Hinova Pharmaceuticals, Inc.

Inventor： Wu Du ,  Xinghai Li ,  Kun Wen ,  Dekun Qin ,  Shaohua Zhang ,  Song Chen ,  Jingyi Duan ,  Haibin Lv ,  Haibo Li ,  Yu Li ,  Jinyun He ,  Muyang Chen ,  Shijuan Liu ,  Yiwei Fu ,  Yikai Guan ,  Zhilin Tu

IPC: C07D491/107 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/496 ,  A61K31/497 ,  A61K31/501 ,  A61K31/506 ,  A61K31/517 ,  A61K31/519 ,  A61K31/53 ,  A61K31/5377 ,  A61P35/00 ,  C07D401/14 ,  C07D405/14 ,  C07D413/14 ,  C07D417/14 ,  C07D471/04 ,  C07D471/10 ,  C07D487/04 ,  C07D487/10 ,  C07D519/00

Abstract: A compound as shown in formula I, or an optical isomer thereof, a solvate thereof, a pharmaceutically acceptable salt thereof, a prodrug thereof, a tautomer thereof, a mesomer thereof, a racemate thereof, an enantiomer thereof, a diastereomer thereof, a mixture form thereof, a metabolite thereof, a metabolic precursor thereof, or an isotope substitute form thereof. TB is a target recognition/binding portion, L is a linking portion, and U is a ubiquitin protease recognition/binding portion, the three portions being connected by means of chemical bonds. The compound can significantly down-regulate mutated androgen receptor (AR) proteins, and has good inhibitory activity on prostate cancer cell lines. The compound of formula I can be used for preparation of a protein degradation targeted chimera for targeted regulation of androgen receptors, and a drug for treating diseases correlated with regulation by androgen receptors, and has particularly good application prospects in drugs for treating prostate cancers and breast cancers.

公开(公告)号：US20250049777A1

公开(公告)日：2025-02-13

申请号：US18721934

申请日：2022-12-23

Applicant: JIANGSU HENGRUI PHARMACEUTICALS CO., LTD. ,  SHANGHAI HENGRUI PHARMACEUTICAL CO., LTD.

Inventor： Weidong LU ,  Gujun XU ,  Junran YANG ,  Qiyun SHAO ,  Zhenxing DU ,  Jun FENG ,  Feng HE

IPC: A61K31/454 ,  C07D405/14

Abstract: Provided are a pharmaceutically acceptable salt and a crystalline form of a GLP-1 receptor agonist and a preparation method therefor. Specifically, provided are a pharmaceutically acceptable salt and a crystalline form of a compound 2-((4-((S)-3-(4-chloro-2-fluorophenyl)-2,3-dihydrobenzo[b][1,4]dioxane-5-yl)piperidin-1-yl)methyl)-1-(((S)-oxe-tane-2-yl)methyl)-1H-benzo[d]imidazole-6-formic acid.

公开(公告)号：US20250041208A1

公开(公告)日：2025-02-06

申请号：US18717160

申请日：2022-12-08

Applicant: NANEXA AB

Inventor： Anders JOHANSSON ,  Mårten ROOTH ,  Joel HELLRUP ,  David WESTBERG

IPC: A61K9/00 ,  A61K9/50 ,  A61K31/192 ,  A61K31/196 ,  A61K31/405 ,  A61K31/407 ,  A61K31/4439 ,  A61K31/454 ,  A61K31/4545 ,  A61K31/5415 ,  A61K31/569 ,  A61K31/635 ,  A61K31/706

Abstract: There is provided a pharmaceutical or veterinary formulation comprising: (a) a biologically-active agent in admixture with a pharmaceutically- or veterinarily-acceptable extended-release component; (b) an antiinflammatory agent; and (c) a pharmaceutically- or veterinarily-acceptable injectable carrier. An extended-release component may also be applied to the antiinflammatory agent. The formulation may provide for the delayed or sustained release of biologically active ingredient without producing an inflammatory response after injection, and s preferably provided in the form of: (1) a plurality of particles having a weight-, number-, or volume-based mean diameter that is between about 10 nm and about 700 μm, which particles comprise solid corms comprising a biologically-active agent coated with a coating comprising at least one coating material applied by way of a gas phase deposition technique; (2) which particles are suspended in a carrier system comprising a pharmaceutically-acceptable or veterinarily-acceptable vehicle; and (3) which formulation further includes an antiinflammatory agent, which is optionally in the form of particles that are coated with a coating comprising at least one coating material applied by way of a gas phase deposition technique. Said coated particles are preferably synthesized via atomic layer deposition.