公开(公告)号：US20240181094A1

公开(公告)日：2024-06-06

申请号：US18552124

申请日：2021-10-29

Applicant: UNIVERSITÄT BASEL ,  PAUL SCHERRER INSTITUT

Inventor： Cristina MÜLLER ,  Roger SCHIBLI ,  Nicolas VAN DER MEULEN ,  Francesca BORGNA ,  Damian WILD ,  Fani MELPOMENI

IPC: A61K51/08 ,  A61K47/22 ,  A61K51/12 ,  A61P35/00

CPC classification number: A61K51/083 ,  A61K47/22 ,  A61K51/088 ,  A61K51/121 ,  A61P35/00

Abstract: A radiopeptide is provided which comprises (a) a radionuclide, wherein the radionuclide is terbium-161, (b) a chelator coordinating terbium-161, and (c) a peptide or peptide analogue, which is a somatostatin receptor (SSTR) antagonist. The radiopeptide is suitable for use in the treatment of tumor diseases.

公开(公告)号：US20230414796A1

公开(公告)日：2023-12-28

申请号：US18035662

申请日：2021-11-05

Applicant: ITM ISOTOPEN TECHNOLOGIEN München AG

Inventor： Marian MECKEL ,  Theresa OSL ,  Konstantin ZHERNOSEKOV

IPC: A61K51/08 ,  A61K31/198 ,  A61P35/00

CPC classification number: A61K51/088 ,  A61K51/083 ,  A61P35/00 ,  A61K31/198

Abstract: The present invention provides a combination comprising (a) a radiolabeled complex comprising a radionuclide and a targeting molecule linked to a chelating agent, and (b) para-aminohippuric acid (PAH) or a salt or derivate thereof for the treatment of cancer. Moreover, a pharmaceutical composition comprising (a) a radiolabeled complex comprising a radionuclide and a targeting molecule linked to a chelating agent, and (b) para-aminohippuric acid (PAH) or a salt or derivate thereof is provided for the treatment of cancer. The radiolabeled complex and PAH may be used in a combination therapy for the treatment of cancer.

公开(公告)号：US11723992B2

公开(公告)日：2023-08-15

申请号：US17265138

申请日：2019-08-02

Applicant: Board of Regents, The University of Texas System

Inventor： Mai Lin ,  Carlos E. Gonzalez-Lepera

IPC: A61K51/04 ,  B01J41/12 ,  B01J47/02 ,  C01G15/00 ,  G21G1/00 ,  A61K51/08 ,  G21G1/10

CPC classification number: A61K51/088 ,  A61K51/0402 ,  A61K51/048 ,  A61K51/0482 ,  A61K51/08 ,  A61K51/082 ,  A61K51/083 ,  B01J41/12 ,  B01J47/02 ,  C01G15/003 ,  G21G1/001 ,  G21G1/10 ,  C01P2006/88 ,  G21G2001/0021

Abstract: Disclosed herein are methods preparing a purified, carrier-free 68Ga solution. Tire present disclosure also provides systems for preparing a purified, carrier-free 68Ga solution. The present disclosure also provides compositions comprising the purified, carrier-free 68Ga solutions disclosed herein. Also provided are methods of administering compositions of the present disclosure to a patient in need thereof, for example, for imaging a disease or disorder, such as cancer.

公开(公告)号：US20180193495A1

公开(公告)日：2018-07-12

申请号：US15832371

申请日：2017-12-05

Applicant: CURASIGHT APS

Inventor： Andreas Kjaer ,  Morten Persson ,  Jacob Madsen

IPC: A61K51/08 ,  A61K38/08

CPC classification number: A61K51/088 ,  A61K38/08 ,  A61K51/08 ,  A61K51/083

Abstract: There is provided a positron-emitting radionuclide labelled peptide for non-invasive PET imaging of the Urokinase-type Plasminogen Activator Receptor (uPAR) in humans. More specifically the invention relates to human uPAR PET imaging of any solid cancer disease for diagnosis, staging, treatment monitoring and especially as an imaging biomarker for predicting prognosis, progression and recurrence.

公开(公告)号：US09919065B2

公开(公告)日：2018-03-20

申请号：US14949473

申请日：2015-11-23

Applicant: The Regents of the University of California

Inventor： Murray Goodman ,  Sandra Blaj Moore

IPC: A61K49/00 ,  A61K51/08 ,  C07K14/655 ,  A61K38/08

CPC classification number: A61K51/083 ,  A61K38/08 ,  A61K51/08 ,  C07K14/6555

Abstract: Provided are therapeutic and diagnostic somatostatin analogs including radiotherapeutic and radiodiagnostic reagents, and methods of making and use thereof.

公开(公告)号：US09884131B2

公开(公告)日：2018-02-06

申请号：US14649113

申请日：2013-11-29

Applicant: Curasight ApS

Inventor： Andreas Kjaer ,  Morten Persson ,  Jacob Madsen

IPC: A61K51/00 ,  A61M36/14 ,  A61K51/08 ,  A61K38/08

CPC classification number: A61K51/088 ,  A61K38/08 ,  A61K51/08 ,  A61K51/083

Abstract: There is provided a positron-emitting radionuclide labelled peptide for non-invasive PET imaging of the Urokinase-type Plasminogen Activator Receptor (uPAR) in humans. More specifically the invention relates to human uPAR PET imaging of any solid cancer disease for diagnosis, staging, treatment monitoring and especially as an imaging biomarker for predicting prognosis, progression and recurrence.

公开(公告)号：US09566246B2

公开(公告)日：2017-02-14

申请号：US15044949

申请日：2016-02-16

Applicant: CHIASMA INC.

Inventor： Roni Mamluk ,  Moshe Tzabari ,  Karen Marom ,  Paul Salama ,  Irina Weinstein

IPC: A61K9/00 ,  A61K9/48 ,  A61K9/10 ,  A61K31/70 ,  A61K38/21 ,  A61K38/27 ,  A61K38/28 ,  A61K38/29 ,  A61K47/14 ,  A61K47/44 ,  A61K38/12 ,  A61K47/12 ,  A61K47/32 ,  A61K38/09 ,  A61K38/11 ,  A61K38/14 ,  A61K38/22 ,  A61K38/26 ,  A61K51/10 ,  A61K51/08 ,  A61K9/16

CPC classification number: A61K47/44 ,  A61K9/0031 ,  A61K9/0053 ,  A61K9/10 ,  A61K9/1623 ,  A61K9/4858 ,  A61K9/4866 ,  A61K9/4891 ,  A61K31/70 ,  A61K31/7036 ,  A61K31/713 ,  A61K31/721 ,  A61K38/08 ,  A61K38/09 ,  A61K38/11 ,  A61K38/12 ,  A61K38/14 ,  A61K38/212 ,  A61K38/22 ,  A61K38/26 ,  A61K38/27 ,  A61K38/28 ,  A61K38/29 ,  A61K47/12 ,  A61K47/14 ,  A61K47/24 ,  A61K47/26 ,  A61K47/32 ,  A61K51/083 ,  A61K51/1021 ,  A61K51/1024 ,  A61K51/1045

Abstract: The pharmaceutical compositions described herein include a suspension which comprises an admixture in solid form of a therapeutically effective amount of a therapeutic agent and at least one salt of a medium chain fatty acid and a hydrophobic medium, e.g. castor oil or glyceryl tricaprylate or a mixture thereof. The pharmaceutical compositions described herein contain medium chain fatty acid salts and are substantially free of alcohols. The pharmaceutical compositions may be encapsulated in a capsule. Methods of treating or preventing diseases by administering such compositions to affected subjects are also disclosed.

Abstract translation: 本文所述的药物组合物包括悬浮液，其包含固体形式的治疗有效量的治疗剂和至少一种中链脂肪酸和疏水性介质的盐的混合物，例如， 蓖麻油或三辛酸甘油酯或其混合物。 本文所述的药物组合物含有中链脂肪酸盐，并且基本上不含醇。 药物组合物可以被包封在胶囊中。 还公开了通过将这些组合物施用于受影响的受试者来治疗或预防疾病的方法。

公开(公告)号：US09421283B2

公开(公告)日：2016-08-23

申请号：US14402036

申请日：2013-05-14

Applicant: ZENTRALKLINIK BAD BERKA GMBH

Inventor： Dirk Muller

IPC: C07K1/13 ,  C07F19/00 ,  B01L3/00 ,  C07F5/00 ,  A61K51/08

CPC classification number: A61K51/083 ,  C07K1/13

Abstract: A kit for producing a radiopharmaceutical, having: a cation exchange cartridge; a reaction vial having a marker precursor; a solution vial having a solvent; an elution vial having a sterile solution including common salt (NaCl) and hydrochloric acid (HCl); and a buffer salt. A method for producing a radiopharmaceutical is also disclosed.

Abstract translation: 一种用于生产放射性药物的试剂盒，具有：阳离子交换盒; 具有标记物前体的反应小瓶; 具有溶剂的溶液小瓶; 具有无菌溶液的洗脱小瓶包括常见的盐（NaCl）和盐酸（HCl）; 和缓冲盐。 还公开了放射性药物的制造方法。

公开(公告)号：US09266084B2

公开(公告)日：2016-02-23

申请号：US13916599

申请日：2013-06-13

Applicant: Ming-Hsin Li ,  Hsin-Han Hsieh

Inventor： Ming-Hsin Li ,  Hsin-Han Hsieh

IPC: A61K51/00 ,  A61M36/14 ,  B01J19/00 ,  A61K51/08 ,  C07B59/00

CPC classification number: B01J19/0053 ,  A61K51/083 ,  C07B59/00

Abstract: The invention provides an automatic synthesizer apparatus and method for producing radiopharmaceutical tumor imaging agent Gallium-68-DOTATATE with one button control process to effectively isolate the medication in vials from the contamination of environment and manual operations, saving the costs of investment in production with alleviation of the critical standard required for the environmental equipments to be used for production.

Abstract translation: 本发明提供一种用于制造放射性药物肿瘤成像剂Gallium-68-DOTATATE的自动合成装置和方法，其具有一个按钮控制过程，以有效地将小瓶中的药物与环境污染和手动操作隔离，从而节省了生产投资的成本，减轻了 环境设备用于生产所需的关键标准。

公开(公告)号：US20160045626A1

公开(公告)日：2016-02-18

申请号：US14922619

申请日：2015-10-26

Applicant: Immunomedics, Inc.

Inventor： William J. McBride ,  David M. Goldenberg

IPC: A61K51/08 ,  A61K45/06

CPC classification number: A61K51/083 ,  A61K45/06 ,  C07B59/002 ,  C07B2200/05 ,  C07D255/02 ,  C07D403/12 ,  C07D405/12 ,  C07D475/04 ,  C07F5/069

Abstract: The present application discloses compositions and methods of synthesis and use of labeled targeting peptides, such as octreotide, octreotate, or other somatostatin analogs or derivatives. The targeting peptide may be labeled with a therapeutic or diagnostic isotope, such as 61Cu, 62Cu, 64Cu, 67Cu, 18F, 19F, 66Ga, 67Ga, 68Ga, 72Ga, 111In, 177Lu, 44Sc, 47Sc, 86Y, 88Y, 90Y, 45Ti or 89Zr, preferably 18F or 19F. More preferably, the targeting peptide is NOTA-octreotate, NOTA-MPAA-octreotate, pyridine-NOTA-octreotate or triazole-NOTA-octreotate. The labeled targeting peptides may be used for detection, diagnosis, imaging and/or treatment of sst2+ tumors, such as neuroendocrine tumors.

Abstract translation: 本申请公开了合成和使用标记的靶向肽的组合物和方法，例如奥曲肽，奥曲肽或其它生长抑素类似物或衍生物。 靶向肽可用治疗或诊断同位素标记，例如61Cu，62Cu，64Cu，67Cu，18F，19F，66Ga，67Ga，68Ga，72Ga，111In，177Lu，44Sc，47Sc，86Y，88Y，90Y，45Ti 或89Zr，优选18F或19F。 更优选地，靶向肽是NOTA-八羟甲基吗啉，NOTA-MPAA-八羟甲酸酯，吡啶-NTA-八羟甲酸酯或三唑-NTA-八羟甲酸酯。 标记的靶向肽可用于sst2 +肿瘤如神经内分泌肿瘤的检测，诊断，成像和/或治疗。