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公开(公告)号:US20250026739A1
公开(公告)日:2025-01-23
申请号:US18895915
申请日:2024-09-25
Applicant: Full-Life Technologies HK Limited
Inventor: Fa LIU
IPC: C07D403/12 , A61K31/4155 , A61K51/04 , A61P35/00
Abstract: The present application relates to a compound of Formula I or a pharmaceutically acceptable salt and/or solvate thereof, or a radionuclide complex comprising a compound of Formula I or a pharmaceutically acceptable salt and/or solvate thereof, and one or more radionuclides, and to compositions thereof. The present application also includes methods of using the compounds, complexes and compositions for targeting neurotensin receptors, and further to their use in the imaging, diagnosis and treatment of diseases, disorders or conditions such as cancer. The present application relates to a compound of Formula II or a pharmaceutically acceptable salt and/or solvate thereof, and to compositions and uses thereof, for example, in the treatment of diseases, disorders or conditions such as cancer.
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公开(公告)号:US20250018068A1
公开(公告)日:2025-01-16
申请号:US18709187
申请日:2022-11-10
Applicant: AC IMMUNE SA
Inventor: Jérôme Molette
IPC: A61K51/04 , C07D487/04
Abstract: The present invention relates to novel compounds of formula (I), or a detectably labelled compound, stereoisomer, racemic mixture, pharmaceutically acceptable salt, hydrate, or solvate thereof, that can be employed in the imaging of alpha-synuclein aggregates and determining an amount thereof. Furthermore, the compounds can be used for diagnosing a disease, disorder or abnormality associated with an alpha-synuclein aggregates, including, but not limited to, Lewy bodies and/or Lewy neurites (such as Parkinson's disease), determining a predisposition to such a disease, disorder or abnormality, prognosing such a disease, disorder or abnormality, monitoring the evolution of the disease in a patient suffering from such a disease, disorder or abnormality, monitoring the progression of such a disease, disorder or abnormality and predicting responsiveness of a patient suffering from such a disease, disorder or abnormality to a treatment thereof.
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公开(公告)号:US20250009917A1
公开(公告)日:2025-01-09
申请号:US18696307
申请日:2022-09-29
Inventor: Katherine Anne Morgan , Paul Stephen Donnelly , Christian Werner Wichmann , Andrew Mark Scott
Abstract: The present invention relates to compounds of formula (I) that have the ability to be used as metal complexes in radiotherapy. wherein A is selected from the group consisting of CO2R1, and PO3R1; B is selected from the group consisting of CO2R2, and PO3R2; R1, R2 and R3 are each independently selected from the group consisting of H and C1-C12alkyl; each Ra is independently selected from the group consisting of H, F, Cl, Br, I, CH3, CH2CH3, CH(CH3)2, OH, OCH3, OCH2CH3, CF3, OCF3, NO2, NH2, and CN; each Rb is independently selected from the group consisting of H, F, Cl, Br, I, CH3, CH2CH3, CH(CH3)2, OH, OCH3, OCH2CH3, CF3, OCF3, NO2, NH2, and CN; L is a linker having from 1 to 20 atoms in the normal chain; or a pharmaceutically acceptable salt thereof.
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公开(公告)号:US20250009913A1
公开(公告)日:2025-01-09
申请号:US18754452
申请日:2024-06-26
Applicant: NORTH CAROLINA STATE UNIVERSITY
Inventor: Qihui Liu , Zhiyuan Wu , Jonathan S. Lindsey
Abstract: Compounds comprising a tetrapyrrole macrocycle that includes a radionuclide; a hydrogelator attached to the tetrapyrrole macrocycle; a water solubilizing group attached to the hydrogelator; and a cleavage site that is between the hydrogelator and the water solubilizing group are described herein along with their methods of use. Two or more compounds of the present invention may two or more compounds may self-assemble (e.g., aggregate), optionally in vivo.
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15.
公开(公告)号:US20250009911A1
公开(公告)日:2025-01-09
申请号:US18886598
申请日:2024-09-16
Inventor: Guillermina FERRO FLORES , Blanca Elí OCAMPO GARCÍA , Myrna Alejandra LUNA GUTIÉRREZ , Clara Leticia SANTOS CUEVAS , Erika Patricia AZORÍN VEGA , Nallely Patricia JIMÉNEZ MANCILLA , Tania HERNÁNDEZ JIMÉNEZ , Flor de María RAMÍREZ DE LA CRUZ , Khaled Ahmed Adly Ibrahim ATTIA
Abstract: The invention relates to a new therapeutic radiopharmaceutical as an inhibitor of prostate-specific membrane antigen (iPSMA), wherein 1,4,7,10-tetraazacyclododecane-N, N′, N″, N″″ -tetraacetic acid (DOTA) bonded to the heterocyclic molecule hydrazinonicotinamide (HYNIC), generates a rigid chemical structure that minimises the number of conformers and intramolecular hydrogen bonds, thereby producing a favourable spatial orientation of the active site (Lys(Nal)—NH—CO—NH-Glu) in the molecule, for biological recognition by the PSMA protein. The new DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic or radiodiagnostic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the detection and treatment of tumours with PSMA overexpression. Radiolabelling of the new molecule is demonstrated with lutetium-177, actinium-225, terbium-161, gallium-67 or gallium-68 isotopes.
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公开(公告)号:US20250002497A1
公开(公告)日:2025-01-02
申请号:US18826736
申请日:2024-09-06
Applicant: Bristol-Myers Squibb Company , Université De Montréal
Inventor: Jacques Banville , Roger Rémillard , Edward H. Ruediger , Daniel H. Deon , Marc Gagnon , Laurence Dubé , Julia Guy , Eldon Scott Priestley , Shoshana L. Posy , Brad D. Maxwell , Pancras C. Wong , R. Michael Lawrence , Michael M. Miller
IPC: C07D487/04 , A61K31/433 , A61K31/435 , A61K31/4439 , A61K31/454 , A61K31/496 , A61K31/497 , A61K31/5025 , A61K31/5377 , A61K31/5386 , A61K31/541 , A61K31/55 , A61K31/553 , A61K45/06 , A61K51/04 , C07B59/00 , C07D513/04 , C07D519/00
Abstract: The present invention provides thiazole compounds of Formula I wherein W, Y, R0, R2, R4, R1, R6, R7, X1, X2, X3 and X4 are as defined herein, or a stereoisomer, tautomer, pharmaceutically acceptable salt, prodrug ester or solvate form thereof, wherein all of the variables are as defined herein. These compounds are inhibitors of platelet aggregation and thus can be used as medicaments for treating or preventing thromboembolic disorders.
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公开(公告)号:US20240415988A1
公开(公告)日:2024-12-19
申请号:US18805445
申请日:2024-08-14
Applicant: NORROY BIOSCIENCE CO., LTD.
Inventor: Peng FANG , Shanyou YU , Chenglong YAN , Wai-si ENG
IPC: A61K51/04 , A61K49/10 , C07D417/12 , C07D417/14
Abstract: The present application relates to a carbonic anhydrase IX-targeting radioactive diagnostic and therapeutic medicament and a preparation method thereof. Specifically, the present disclosure relates to a compound, or a pharmaceutically acceptable salt, ester, or solvate thereof. The compound has a structure represented by Formula (I). The compound can be used for diagnosing and/or treating one or more tumors, cancers, or cells expressing carbonic anhydrase IX.
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公开(公告)号:US12168063B2
公开(公告)日:2024-12-17
申请号:US18640917
申请日:2024-04-19
Applicant: Advanced Accelerator Applications SA
Inventor: Donato Barbato , Clementina Brambati , Daniela Chicco , Francesco de Palo , Lorenza Fugazza , Maurizio Mariani , Giovanni Tesoriere
Abstract: The present invention relates to radionuclide complex solutions of high concentration and of high chemical stability, that allows their use as drug product for diagnostic and/or therapeutic purposes. The stability of the drug product is achieved by at least one stabilizer against radiolytic degradation. The use of two stabilizers introduced during the manufacturing process at different stages was found to be of particular advantage.
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公开(公告)号:US20240409580A1
公开(公告)日:2024-12-12
申请号:US18809625
申请日:2024-08-20
Applicant: Siemens Medical Solutions USA, Inc.
Inventor: Eric Wang , Hartmuth C. Kolb , Anna Katrin Szardenings , Changhui Liu , Joseph C. Walsh , Gang Chen , Anjana Sinha , Dhanalakshmi Kasi , Chul Yu , Umesh B. Gangadharmath , Wei Zhang , Tieming Zhao , Vani P. Mocharla
IPC: C07K5/02 , A61K38/00 , A61K51/04 , A61K51/08 , C07D207/16 , C07D209/48 , C07D213/81 , C07D213/82 , C07D233/78 , C07D233/96 , C07D239/60 , C07D249/04 , C07D249/06 , C07D251/30 , C07D263/34 , C07D277/56 , C07D401/12 , C07D403/06 , C07D403/12 , C07D405/12 , C07K5/062 , C07K5/072
Abstract: Compounds for targeting and agents for imaging, prostate-specific membrane antigen (PSMA) are disclosed. Methods of synthesizing compounds and imaging agents, as well as methods for imaging PSMA are also disclosed. The imaging agents disclosed are suitable for PET and SPECT imaging.
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公开(公告)号:US20240408247A1
公开(公告)日:2024-12-12
申请号:US18566733
申请日:2022-06-08
Applicant: CRINETICS PHARMACEUTICALS, INC.
Inventor: R. Scott STRUTHERS , Jian ZHAO , Yunfei ZHU
Abstract: Described herein are non-peptide drug conjugates (NPDCs) that target tumor cells expressing cell surface peptide and protein G protein-coupled receptors and their use in the treatment and/or diagnosis of cancer.
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