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1. 发明授权

US10398791B2 Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer 有权
公开(公告)号：US10398791B2
公开(公告)日：2019-09-03
申请号：US16114988
申请日：2018-08-28
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： Matthias Eder , Klaus Kopka , Martin Schäfer , Ulrike Bauder-Wüst , Uwe Haberkorn , Michael Eisenhut , Walter Mier , Martina Benesova
IPC分类号： A61K51/04 , C07B59/00 , C07D295/145 , C07D257/02
摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

2. 发明授权

US10471160B2 Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer 有权
公开(公告)号：US10471160B2
公开(公告)日：2019-11-12
申请号：US16038729
申请日：2018-07-18
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： Matthias Eder , Klaus Kopka , Martin Schäfer , Ulrike Bauder-Wüst , Uwe Haberkorn , Michael Eisenhut , Walter Mier , Martina Benesova , Hans-Christian Kliem , Clemens Kratochwil
IPC分类号： A61K51/04 , C07D257/02 , C07B59/00 , C07D295/145
摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer. Thus, the present invention concerns compounds that are represented by the general Formulae (Ia) or (Ib).

3. 发明授权

US10016519B2 18F-tagged inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer 有权
公开(公告)号：US10016519B2
公开(公告)日：2018-07-10
申请号：US15463059
申请日：2017-03-20
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： Klaus Kopka , Martina Benesova , Jens Cardinale , Matthias Eder , Martin Schäfer , Ulrike Bauder-Wüst , Uwe Haberkorn , Michael Eisenhut
IPC分类号： A61K31/04 , C07B59/00 , C07C275/16 , C07D213/82 , A61K51/04
摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

4. 发明申请

US20170246327A1 18F-TAGGED INHIBITORS OF PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA), THEIR USE AS IMAGING AGENTS AND PHARMACEUTICAL AGENTS FOR THE TREATMENT OF PROSTATE CANCER 有权
公开(公告)号：US20170246327A1
公开(公告)日：2017-08-31
申请号：US15463059
申请日：2017-03-20
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITÄT HEIDELBERG
发明人： Klaus KOPKA , Martina Benesova , Jens Cardinale , Matthias Eder , Martin SCHÄFER , Ulrike BAUDER-WÜST , Uwe Haberkorn , Michael Eisenhut
IPC分类号： A61K51/04 , C07B59/00 , C07C275/16 , C07D213/82
CPC分类号： A61K51/0455 , A61K51/0402 , A61K51/06 , C07B59/001 , C07B59/002 , C07B2200/05 , C07C275/16 , C07D213/82
摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers, imaging agents and for the treatment of various disease states of prostate cancer.

5. 发明申请

US20220118121A1 PROSTATE SPECIFIC MEMBRANE ANTIGEN (PSMA) LIGANDS WITH IMPROVED TISSUE SPECIFICITY 有权
公开(公告)号：US20220118121A1
公开(公告)日：2022-04-21
申请号：US17431396
申请日：2020-02-14
申请人： Ruprecht-Karls-Universität Heidelberg , Deutsches Krebsforschungszentrum
发明人： Matthias Eder , Ann-Christin Baranski , Michael Eisenhut , Uwe Haberkorn
IPC分类号： A61K51/08 , A61K51/04 , A61P35/00
摘要： The present invention relates to a compound of formula (1), and to a complex comprising said compound and a radionuclide, and to the respective pharmaceutical composition, the compound having the following structure or a pharmaceutically acceptable salt or solvate thereof, wherein R1 is H or —CH3, preferably H, wherein R2, R3 and R4 are independently of each other, selected from the group consisting of —CO2H, —SO2H, —SO3H, —OSO3H, —PO2H, —PO3H and —OPO3H2, Q1 is selected from the group consisting of alkylaryl, arylalkyl, aryl, alkylheteroaryl, heteroarylalkyl and heteroaryl, Q2 is selected from the group consisting of aryl, alkylaryl, arylalkyl, cycloalkyl, heterocycloalkyl, heteroaryl, heteroarylalkyl and alkylheteroaryl, A is a chelator residue derived from a chelator selected from the group consisting of 1,4,7,10-tetraazacyclododecane-N,N′,N″,N′″-tetraacetic acid (=DOTA), N,N″-bis[2-hydroxy-5-(carboxyethyl)benzyl]ethylenediamine-N,N″-diacetic acid, 1,4,7-triazacyclononane-1,4,7-triacetic acid (=NOTA), 2-(4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl)pentanedioic acid, (NODAGA), 2-(4,7, 10-tris(carboxymethyl)-1,4,7,10-tetraazacyclododecan-1-yl)pentanedioic acid (DOTAGA), 1,4,7-riazacyclononane phosphinic acid (TRAP), 1,4,7-triazacyclononane phosphinic acid (TRAP), 1,4,7-triazacyclononane-1-[methyl(2-carboxyethyl)phosphinic acid]-4,7-bis[methyl(2-hydroxymethyl)phosphinic acid](NOPO), 3,6,9, 15-tetraazabicyclo[9.3.1.]pentadeca-1(15),11,13-triene-3,6,9-triacetic acid (=PCTA), N′-{5-[Acetyl(hydroxy)amino]pentyl}-N-[5-({4-[(5-aminopentyl)(hydroxy)amino]-4-oxobutanoyl}amino)pentyl]-N-hydroxysuccinamide (DFO), Diethylenetriaminepentaacetic acid (DTPA), Trans-cyclohexyl-diethylenetriaminepentaacetic acid (CHX-DTPA), 1-oxa-4,7, 10-triazacyclododecane-4,7, 10-triacetic acid (oxo-Do3A) p-isothiocyanatobenzyl-DTPA (SCN-Bz-DTPA), 1-(p-isothiocyanatobenzyl)-3-methyl-DTPA (1 B3M), 2-(p-isothiocyanatobenzyl)-4-methyl-DTPA (1 M3B) and 1-(2)-methyl-4-isocyanatobenzyl-DTPA (MX-DTPA), X1, X2, Y1, Y2, Z1 and Z2, are independently of each other, charged amino acids, q is an integer of from 0-3, n, m and p, are independently of each other an integer of from 0 to 9, n1, n2, m1, m2, p1, p2, are independently of ach other, an integer of from 0 to 3, and wherein n1+n2>0, m1+m2>0 and p1+p2>0, and wherein n+m+p>0. Further, the present invention relates to the compound, the complex, and the pharmaceutical composition for use in treating, ameliorating or preventing PSMA-expressing cancers, in particular prostate cancer, and/or metastases thereof.

6. 发明申请

US20190351069A1 Coating of Nanoparticle Surfaces with Cyclopeptides for Improving Delivery of Agents Via the Oral Route 审中-公开
公开(公告)号：US20190351069A1
公开(公告)日：2019-11-21
申请号：US16329534
申请日：2017-09-19
申请人： Ruprecht-Karls-Universität Heidelberg
发明人： Philipp Uhl , Walter Mier , Uwe Haberkorn , Max Sauter
IPC分类号： A61K47/69 , A61K9/19 , A61K9/00 , A61K9/48 , A61K38/12 , A61K31/704 , A61K38/28 , A61K38/26
摘要： The present invention relates to a surface-coated nanoparticle comprising biodegradable polymer chains and cyclopeptides, wherein the cyclopeptides are covalently attached to the biodegradable polymer chains forming the nanoparticle, thereby coating the surface of the nanoparticle. The present invention further relates to the use of said surface-coated nanoparticle as a capsule for an agent for improving the oral delivery thereof. In another aspect, the present invention relates to the surface-coated nanoparticle for use in the treatment or prevention of a disorder or disease in a patient, wherein the treatment or prevention is achieved by mucosal uptake of the surface-coated nanoparticle via the oral route.

7. 发明申请

US20140356284A1 HYDROPHOBIC MODIFIED PEPTIDES FOR LIVER SPECIFIC DIAGNOSIS 审中-公开
标题翻译：用于肝脏特异性诊断的疏水性修饰肽
公开(公告)号：US20140356284A1
公开(公告)日：2014-12-04
申请号：US13984715
申请日：2012-02-10
申请人： Ruprecht-Karls-Universität Heidelberg
发明人： Walter Mier , Stephan Urban , Stefan Mehrle , Uwe Haberkorn , Thomas Müller , Vasileios Askoxylakis
IPC分类号： A61K51/08 , C12N7/00 , C07K14/005
CPC分类号： A61K51/088 , A61K38/00 , A61K49/0056 , A61K49/085 , A61K49/14 , C07K14/005 , C07K2319/50 , C12N7/00 , C12N2730/10122 , Y02A50/409 , Y02A50/411 , Y02A50/423 , Y02A50/463
摘要： The present invention relates to hydrophobic modified peptides for the specific delivery of labels to the liver, preferably to hepatocytes, in vitro as well as in vivo. The present invention relates to pharmaceutical compositions comprising said hydrophobic modified peptide(s) and the label(s) to be specifically delivered to the liver. The present invention furthermore relates to the diagnostic use of the inventive hydrophobic modified peptides as well as to a method for the diagnosis of liver diseases or disorders.
摘要翻译：本发明涉及在体外和体内特异性递送给肝脏，优选肝细胞的疏水性修饰肽。本发明涉及包含所述疏水性修饰肽和特异性递送至肝脏的标签的药物组合物。本发明还涉及本发明的疏水性修饰肽的诊断用途以及用于诊断肝脏疾病或病症的方法。

8. 发明授权

US11638765B2 Double-labeled probe for molecular imaging and use thereof 有权
公开(公告)号：US11638765B2
公开(公告)日：2023-05-02
申请号：US16765927
申请日：2018-11-20
申请人： Deutsches Krebsforschungszentrum , Ruprecht-Karls-Universitaet Heidelberg
发明人： Matthias Eder , Klaus Kopka , Martin Schaefer , Ulrike Bauder-Wuest , Uwe Haberkorn , Ann-Christin Eder , Jens Cardinale , Martina Benesova
IPC分类号： A61K51/00 , A61M36/14 , A61K51/04 , A61K49/00 , G01N33/574 , G01N33/58 , G01N33/60 , A61K49/10 , C07D403/14 , C09B23/01 , C09B23/08
摘要： The present invention relates to a compound of a pharmaceutically acceptable salt thereof of formula (I) 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 or a chemical single bond covalently connecting (A) to the rest of the molecule; x2 is a spacer or a chemical single bond covalently connecting (C) to the rest of the molecule. 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.

9. 发明授权

US11452786B2 Double-labeled probe for molecular imaging and use thereof 有权
公开(公告)号：US11452786B2
公开(公告)日：2022-09-27
申请号：US16763667
申请日：2018-11-12
申请人： Deutsches Krebsforschungszentrum , Ruprecht-Karls-Universitaet Heidelberg
发明人： Ann-Christin Eder , Matthias Eder , Klaus Kopka , Martin Schaefer , Ulrike Bauder-Wuest , Uwe Haberkorn
IPC分类号： A61K51/04 , C07D403/14
摘要： 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.

10. 发明授权

US10815200B2 18F—tagged inhibitors of prostate specific membrane antigen (PSMA) and their use as imaging agents for prostate cancer 有权
公开(公告)号：US10815200B2
公开(公告)日：2020-10-27
申请号：US15915978
申请日：2018-03-08
申请人： DEUTSCHES KREBSFORSCHUNGSZENTRUM , RUPRECHT-KARLS-UNIVERSITAET HEIDELBERG
发明人： Jens Cardinale , Martin Schaefer , Klaus Kopka , Matthias Eder , Ulrike Bauder-Wuest , Michael Eisenhut , Martina Benesova , Uwe Haberkorn , Frederik L. Giesel
IPC分类号： A61K38/00 , C07D213/61 , A61K51/04 , C07B59/00 , G01N33/574 , C07K7/02 , A61P35/00
摘要： The present invention generally relates to the field of radiopharmaceuticals and their use in nuclear medicine as tracers and imaging agents for various disease states of prostate cancer.

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