公开(公告)号：US12161733B2

公开(公告)日：2024-12-10

申请号：US16969673

申请日：2019-02-22

Applicant: THE UNITED STATES OF AMERICA, AS REPRESENTED BY THE SECRETARY, DEPARTMENT OF HEALTH AND HUMAN SERVICES

Inventor： Xiaoyuan Chen ,  Orit Jacobson Weiss

IPC: A61K51/04 ,  A61K31/40 ,  A61K31/4025 ,  A61K45/06 ,  A61K47/54 ,  A61K49/00

Abstract: A compound of Formula I or a pharmaceutically acceptable ester, amide, solvate, or salt thereof, or a salt of such an ester or amide or a solvate of such an ester amide or salt: wherein the definitions of R1-R13 and L1-L4 are provided in the disclosure, and wherein R14 is a group capable of binding to prostate-specific membrane antigen (PSMA).

公开(公告)号：US12161732B2

公开(公告)日：2024-12-10

申请号：US18640907

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

IPC: A61K51/00 ,  A61K33/24 ,  A61K51/04 ,  A61M36/14 ,  C22B59/00

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.

公开(公告)号：US12161731B2

公开(公告)日：2024-12-10

申请号：US17312949

申请日：2019-09-19

Applicant: SHANGHAI UNIVERSITY OF MEDICINE&HEALTH SCIENCES

Inventor： Gang Huang ,  Bin Li

IPC: A61K51/04 ,  C07B59/00 ,  C07D487/04

Abstract: The invention relates to a radioactive I-labeled Larotrectinib compound and a preparation method and application thereof, including a radioactive I-labeled Larotrectinib compound having the following structural formula and its analogs: where R1 and R2 are respectively H, F, Cl, Br, 123I, 124I, 125I, 130I or 131I, and at least one of R1 and R2 is a radioactive iodine element. The invention provides a preparation method of a radioiodinated pyrazolo[1,5-a]pyrimidine compound base. Radioiodinated pyrazolo[1,5-a]pyrimidine compounds with long half-life and different ray energy can be used for PET tomography and clinical diagnostic research of SPECT. Moreover, the high-energy radioiodinated pyrazolo[1,5-a]pyrimidine can act as a TrK receptor ligand to inhibit the activity of TRK and kill tumor cells; and due to high-energy I-131 ray energy carried, the radioiodinated pyrazolo[1,5-a]pyrimidine can coordinate to shoot tumor cells and thus achieve an accurate radiotherapy effect.

公开(公告)号：US12156920B2

公开(公告)日：2024-12-03

申请号：US17889655

申请日：2022-08-17

Applicant: Deutsches Krebsforschungszentrum

Inventor： Ann-Christin Eder ,  Matthias Eder ,  Klaus Kopka ,  Martin Schaefer ,  Ulrike Bauder-Wuest ,  Uwe Haberkorn

IPC: A61K51/04 ,  C07D403/14

Abstract: The present invention relates to a compound or a pharmaceutically acceptable salt thereof having a chemical structure comprising: A compound or a pharmaceutically acceptable salt thereof of formula (I): (A)-x1-(B)-x2-(C), wherein (A) is at least one motif specifically binding to cell membranes of neoplastic cells; (B) at least one chelator moiety of radiometals; (C) a dye moiety; x1 is a spacer covalently connecting (A) and (B); x2 is a spacer or a chemical single bond connecting (B) and (C); wherein (C) has the formula wherein R1 to R4, R9, a, b, Y and X1 to X4 have the meaning as indicated in the claims and description. The invention further relates to compositions comprising said compounds as well as a method for detecting neoplastic cells in a sample in vitro with the aid of the compounds or composition.

公开(公告)号：US20240391883A1

公开(公告)日：2024-11-28

申请号：US18791751

申请日：2024-08-01

Applicant: The University of British Columbia ,  British Columbia Cancer Agency Branch

Inventor： Raymond John ANDERSEN ,  Javier Garcia FERNANDEZ ,  Kunzhong JIAN ,  Marianne Dorothy SADAR ,  Nasrin R. MAWJI ,  Carmen Adriana BANUELOS

IPC: C07D249/04 ,  A61K31/4164 ,  A61K31/4192 ,  A61K31/5375 ,  A61K45/06 ,  A61K51/04 ,  A61P35/00 ,  C07B59/00 ,  C07D233/60 ,  C07D265/30 ,  C07D295/084 ,  C07D295/088

Abstract: Compounds having a structure of Formula I: or a pharmaceutically acceptable salt, tautomer or stereoisomer thereof, wherein R1, R2, R3, R11a, R11b, R11c, R11d, X, n1, n2, and n3 are as defined herein, are provided. Uses of such compounds for modulating androgen receptor activity, imaging diagnostics in cancer and therapeutics, and methods for treatment of subjects in need thereof, including prostate cancer are also provided.

公开(公告)号：US12145926B2

公开(公告)日：2024-11-19

申请号：US18604397

申请日：2024-03-13

Applicant: Full-Life Technologies HK Limited

Inventor： Fa Liu

IPC: C07D403/12 ,  A61K31/41 ,  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.

公开(公告)号：US12138322B2

公开(公告)日：2024-11-12

申请号：US18610095

申请日：2024-03-19

Applicant: Vector Vitale IP LLC

Inventor： Peter Novak ,  Max Temnik ,  Oleksandr Balakin

IPC: A61K51/04 ,  A61K31/164 ,  A61K33/30 ,  A61P35/00

Abstract: A method for treating melanoma or preventing the development of melanoma comprising administration of a composition comprising 64Zne(Asp)2 in a therapeutically effective amount. Such administration may be via injection such as intratumoral and/or intravenous injection and may be once a day or more than once a day. A composition for the treatment of or prevention of melanoma comprising 64Zne(Asp)2 in a therapeutically effective amount. The composition may be a liquid suitable for injection.

公开(公告)号：US20240366808A1

公开(公告)日：2024-11-07

申请号：US18569180

申请日：2022-06-16

Applicant: GE Healthcare Limited

Inventor： Torgrim ENGELL ,  Graeme MCROBBIE ,  Alan CLARKE ,  Julian GRIGG ,  Imtiaz Ahmed KHAN ,  Kristine WIKENE ,  Jonathan Robert SHALES ,  Alexander JACKSON

IPC: A61K51/04 ,  C07B59/00

Abstract: The invention relates to a method of preparing an [18F] radio-labelled compound, wherein the water content is controlled. Controlling the water content and the origin of the water within the reaction process has a significant effect on both the yield and the purity of the product of the radio-labelling process.

公开(公告)号：US20240366807A1

公开(公告)日：2024-11-07

申请号：US18683663

申请日：2022-08-18

Applicant: Trustees of tufts college

Inventor： William W. Bachovchin ,  Hung-sen Lai ,  Wengen Wu

IPC: A61K51/04 ,  A61P35/00 ,  C07B59/00 ,  C12N9/99

Abstract: Disclosed are compounds useful for imaging cells that overexpress FAP, and for treating cancer. Also disclosed are methods of making said compounds.

公开(公告)号：US12128114B2

公开(公告)日：2024-10-29

申请号：US16980252

申请日：2019-03-07

Applicant: INSTITUTO NACIONAL DE INVESTIGACIONES NUCLEARES

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

IPC: A61K51/00 ,  A61K51/04 ,  A61M36/14

CPC classification number: A61K51/041

Abstract: The invention relates to a new lutetium-177 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 177Lu-DOTA-HYNIC-iPSMA radiopharmaceutical accumulates, with high affinity in vivo, in tumours that overexpress the PSMA protein, acting as a radiotherapeutic agent. The purpose of the invention is to provide a new specific radiopharmaceutical (molecular target radiopharmaceutical) for the treatment of tumours with PSMA overexpression.