公开(公告)号：US12128114B2

公开(公告)日：2024-10-29

申请号：US16980252

申请日：2019-03-07

申请人： INSTITUTO NACIONAL DE INVESTIGACIONES NUCLEARES

发明人： 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分类号： A61K51/00 ,  A61K51/04 ,  A61M36/14

CPC分类号： A61K51/041

摘要： 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.

公开(公告)号：US12053532B2

公开(公告)日：2024-08-06

申请号：US17114195

申请日：2020-12-07

申请人： Purdue Research Foundation

发明人： Sumith A. Kularatne ,  Sakkarapalayam M. Mahalingam ,  Philip S. Low ,  Mohammad Noshi

IPC分类号： A61K51/00 ,  A61B5/00 ,  A61K49/00 ,  A61M36/14 ,  G01N33/574 ,  G01N33/58

CPC分类号： A61K49/0052 ,  A61B5/0071 ,  A61K49/0032 ,  G01N33/57411 ,  G01N33/57415 ,  G01N33/57423 ,  G01N33/57426 ,  G01N33/57449 ,  G01N33/582

摘要： The present disclosure relates to compounds that are useful as near-infrared fluorescence probes, wherein the compounds include i) a pteroyl ligand that binds to a target receptor protein, ii) a dye molecule, and iii) a linker molecule that comprises an amino acid or derivative thereof. The disclosure further describes methods and compositions for incorporating the compounds as used for the targeted imaging of tumors. Conjugation of the amino acid linking groups increase specificity and detection of the compound. Methods and compositions for use thereof in diagnostic imaging are contemplated.

公开(公告)号：US11938201B2

公开(公告)日：2024-03-26

申请号：US18354282

申请日：2023-07-18

申请人： The Johns Hopkins University

发明人： Xing Yang ,  Sridhar Nimmagadda ,  Steven Rowe ,  Stephanie Slania ,  Martin G. Pomper

IPC分类号： A61K51/00 ,  A61K47/54 ,  A61K51/04 ,  A61M36/14

CPC分类号： A61K51/0485 ,  A61K47/545 ,  A61K51/0478 ,  A61K51/0482

摘要： Imaging and radiotherapeutics agents targeting fibroblast-activation protein-α (FAP-α) and their use in imaging and treating FAP-α related diseases and disorders are disclosed.

公开(公告)号：US11904027B2

公开(公告)日：2024-02-20

申请号：US16827606

申请日：2020-03-23

申请人： Advanced Accelerator Applications

发明人： Francesco de Palo ,  Lorenza Fugazza ,  Donato Barbato ,  Maurizio Mariani ,  Daniela Chicco ,  Giovanni Tesoriere ,  Clementina Brambati

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

CPC分类号： A61K51/048 ,  A61K33/24 ,  C22B59/00 ,  A61K51/0482

摘要： 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：US11813339B2

公开(公告)日：2023-11-14

申请号：US16484706

申请日：2018-02-06

申请人： IGL Pharma, Inc.

发明人： Jaime Simon ,  R. Keith Frank

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  A61P35/00 ,  A61P35/04 ,  A61P19/08 ,  A61P7/00 ,  G21G1/02

CPC分类号： A61K51/0482 ,  A61K51/0478 ,  A61P35/00 ,  A61P7/00 ,  A61P19/08 ,  A61P35/04 ,  G21G1/02

摘要： This invention relates to radioactive, bone-seeking, pharmaceutical compositions that are administered multiple times to a patient, have a lower impurity profile, a longer shelf life, and are less expensive to prepare.

公开(公告)号：US11661402B2

公开(公告)日：2023-05-30

申请号：US17718812

申请日：2022-04-12

申请人： The Johns Hopkins University

发明人： Martin G. Pomper ,  Ronnie C. Mease ,  Ying Chen ,  Sangeeta Ray

IPC分类号： A61K51/00 ,  A61M36/14 ,  C07D257/02 ,  C07D209/14 ,  C07D213/04 ,  C07D249/04 ,  C07D255/02 ,  C07D311/14 ,  C07D311/82 ,  A61K49/00 ,  C07D209/24 ,  A61K51/04 ,  C07D209/12 ,  C07D311/20 ,  C07F5/02 ,  C07F13/00 ,  G01N33/50 ,  A61P35/00

CPC分类号： C07D257/02 ,  A61K49/0032 ,  A61K49/0052 ,  A61K51/044 ,  A61K51/0421 ,  A61K51/0446 ,  A61K51/0453 ,  A61K51/0472 ,  C07D209/12 ,  C07D209/14 ,  C07D209/24 ,  C07D213/04 ,  C07D249/04 ,  C07D255/02 ,  C07D311/14 ,  C07D311/20 ,  C07D311/82 ,  C07F5/027 ,  C07F13/005 ,  G01N33/5091 ,  A61P35/00 ,  G01N2800/342

摘要： Compositions and methods for visualizing tissue under illumination with near-infrared radiation, including compounds comprising near-infrared, closed chain, sulfo-cyanine dyes and prostate specific membrane antigen ligands are disclosed.

公开(公告)号：US11554184B2

公开(公告)日：2023-01-17

申请号：US17697416

申请日：2022-03-17

申请人： Vyripharm Enterprises, Inc.

发明人： Jerry L. Bryant, Jr.

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

摘要： Compositions and methods for the personalized and targeted therapeutic treatment of diseases and disorders, including the treatment of pain, inflammation, and infectious diseases in a subject. In particular, labeled synthetic cannabinoid therapeutic compositions are provided that include a conjugate of a synthetic cannabinoid compound, a chelator, and a label, that when coupled with imaging may be used to determine in real time optimal dosing and targeting of particular pathways and tissues to provide personalized therapies. Combination therapies are also provided that include one or more synthetic cannabinoid compound and at least one active pharmaceutical ingredient.

公开(公告)号：US11497819B2

公开(公告)日：2022-11-15

申请号：US16765729

申请日：2018-12-11

申请人： Technische Universität München

发明人： Hans-Jurgen Wester ,  Alexander Schmidt ,  Mara Parzinger

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  A61P35/00 ,  C07D257/02

摘要： The present invention relates to compounds which bind and/or inhibit prostate-specific membrane antigen (PSMA) comprising at least one group electron dense substituent (EDS), and at least one moiety which is amenable to radiolabeling; and therapeutic and diagnostic uses thereof.

公开(公告)号：US11439714B2

公开(公告)日：2022-09-13

申请号：US17461860

申请日：2021-08-30

申请人： Centre for Probe Development and Commercialization (CPDC)

发明人： Joe McCann ,  Justyna Kelly ,  Paul Billone

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K51/04 ,  A61K51/12 ,  A61K47/12 ,  A61K47/02 ,  A61K47/22 ,  A61K9/00

摘要： A radiopharmaceutical 177Lu-DOTATATE compound, a composition, and a kit are provided. Further provided are methods of synthesis of a 177Lu-DOTATATE compound and methods of treatment that comprise a 177Lu-DOTATATE compound.

公开(公告)号：US11433064B2

公开(公告)日：2022-09-06

申请号：US16919562

申请日：2020-07-02

申请人： Exelixis, Inc.

发明人： Dana T. Aftab ,  Thomas Mueller ,  Aaron Weitzman ,  Jaymes Holland

IPC分类号： A61K51/00 ,  A61M36/14 ,  A61K31/47 ,  A61K31/4706 ,  A61K41/00 ,  A61K45/06 ,  A61K31/495 ,  A61K31/4188 ,  A61N5/10 ,  A61K31/015 ,  A61P43/00 ,  A61K31/517 ,  A61P35/00 ,  C07D215/22

摘要： Methods of treating cancer by administering a compound of Formula I, or a pharmaceutically acceptable salt or solvate thereof, in combination with other cancer treatments are described, wherein R1 is halo; R2 is halo; and Q is CH or N.