公开(公告)号：US20240254092A1

公开(公告)日：2024-08-01

申请号：US18610927

申请日：2024-03-20

申请人： ACTINIUM PHARMACEUTICALS, INC.

发明人： Le-Cun XU ,  Denis BECKFORD VERA

IPC分类号： C07D257/02 ,  A61K51/04 ,  A61K51/10 ,  C07K16/28

CPC分类号： C07D257/02 ,  A61K51/0482 ,  A61K51/1093 ,  C07K16/283 ,  C07B2200/05

摘要： Provided are new bifunctional chelators for use in the manufacture of radiolabeled targeting agents for therapeutic or diagnostic use. Also provided are conjugates of the new bifunctional chelators with various cancer antigen targeting agents.

公开(公告)号：US20240174622A1

公开(公告)日：2024-05-30

申请号：US18548716

申请日：2022-03-02

申请人： NIHON MEDI-PHYSICS CO., LTD. ,  KYOTO UNIVERSITY

发明人： Yoshifumi MAYA ,  Hiroaki ICHIKAWA ,  Yusuke HIGAKI ,  Masahiro ONO ,  Shimpei IIKUNI

IPC分类号： C07D257/02 ,  A61K31/395 ,  A61K51/04 ,  C07B59/00

CPC分类号： C07D257/02 ,  A61K31/395 ,  A61K51/0482 ,  C07B59/004 ,  C07B2200/05

摘要： The compound of the present invention includes a structure having: a chelating part capable of coordinating with a radioactive metal ion; a first atomic group containing an albumin-binding part; and a second atomic group containing a PSMA molecule-binding part, wherein the first atomic group and the second atomic group are bonded with each other through the chelating part, or the chelating part is bonded from between the first atomic group and the second atomic group so that it makes a branch. The present invention also provides: a radiolabeled compound in which the compound is coordinated with a radioactive metal ion; and a method for manufacturing a radiolabeled compound.

公开(公告)号：US11975081B2

公开(公告)日：2024-05-07

申请号：US18481844

申请日：2023-10-05

申请人： ACTINIUM PHARMACEUTICALS, INC.

发明人： Le-Cun Xu ,  Denis Beckford Vera

IPC分类号： C07D257/02 ,  A61K51/04 ,  A61K51/10

CPC分类号： A61K51/1093 ,  A61K51/0482 ,  C07D257/02

摘要： Provided are new bifunctional chelators for use in the manufacture of radiolabeled targeting agents for therapeutic or diagnostic use. Also provided are conjugates of the new bifunctional chelators with various cancer antigen targeting agents.

公开(公告)号：US20240025866A1

公开(公告)日：2024-01-25

申请号：US18253306

申请日：2021-11-19

申请人： NOVARTIS AG

发明人： Fritz ANDREAE

IPC分类号： C07D257/02

CPC分类号： C07D257/02

摘要： The present disclosure relates to the synthesis of prostate specific membrane antigen (PSMA) ligands that are useful in the treatment of diseases like cancer. In particular, the disclosure relates to a method for synthesizing PSMA ligands having a glutamate-urea-lysine (GUL) moiety and a chelating agent that can comprise a radiometal.

公开(公告)号：US20240018110A1

公开(公告)日：2024-01-18

申请号：US18267987

申请日：2021-12-16

申请人： THE UNIVERSITY OF BRITISH COLUMBIA ,  PROVINCIAL HEALTH SERVICES AUTHORITY ,  ALPHA-9 THERANOSTICS INC.

发明人： François BÉNARD ,  Kuo-Shyan LIN ,  Chengcheng ZHANG ,  David PERRIN ,  Aron ROXIN ,  Zhengxing ZHANG ,  Antoine DOUCHEZ ,  Pargol DANESHMANDKASHANI ,  Samson LAI

IPC分类号： C07D257/02 ,  C07C235/78 ,  A61K51/04

CPC分类号： C07D257/02 ,  C07C235/78 ,  A61K51/0482 ,  A61K2123/00 ,  C07B2200/07 ,  A61K2121/00 ,  C07B2200/05

摘要： The present invention relates to radiolabelled compounds for in vivo imaging or treatment of diseases or conditions characterized by expression of prostate-specific membrane antigen.

公开(公告)号：US20230356105A1

公开(公告)日：2023-11-09

申请号：US18027283

申请日：2021-11-12

申请人： Ustav Organicke Chemie a Biochemie AV CR V.V.I.

发明人： Miloslav POLASEK ,  Kelsea Grace JONES ,  Tomas DAVID

IPC分类号： B01D9/00 ,  C01F17/13 ,  C07D257/02 ,  C22B59/00 ,  B01D15/32 ,  B01D61/14

CPC分类号： B01D9/005 ,  C01F17/13 ,  C07D257/02 ,  C22B59/00 ,  B01D15/327 ,  B01D61/145 ,  B01D2009/0086

摘要： The present invention related to the use of compounds of general formula (I) for separations of rare earth elements (lanthanides) by precipitation, wherein R is selected from the group consisting of H; —CH2COOH; R2, R3, R4, R5 and R6 areindependently selected from the group consisting of H; OH; —NO2; —COOH; phenyl; and/or R2 and R3 or R3 and R4 or R4 and R5 or R5 and R6 The invention further relates to a method of separation of rare earth elements by precipitation. together with two neighbouring carbon atoms of the aromatic ring form a six-membered aromatic ring.

公开(公告)号：US11701440B2

公开(公告)日：2023-07-18

申请号：US17047859

申请日：2019-04-15

申请人： NIHON MEDI-PHYSICS CO., LTD. ,  National University Corporation Kagoshima University ,  National University Corporation Chiba University

发明人： Shota Komoto ,  Yu Ogawa ,  Yoshinari Shoyama ,  Tadashi Hatano ,  Yuji Ito ,  Yasushi Arano ,  Hiroyuki Suzuki ,  Tomoya Uehara

IPC分类号： A61K47/68 ,  A61K51/10 ,  C07K5/065 ,  C07K5/087 ,  A61K51/04 ,  A61K51/08 ,  C07D257/02 ,  C07K7/08 ,  C07K16/32

CPC分类号： A61K51/1093 ,  A61K47/6887 ,  A61K47/6889 ,  A61K51/0482 ,  A61K51/088 ,  A61K51/1096 ,  C07D257/02 ,  C07K5/06078 ,  C07K5/0812 ,  C07K7/08 ,  C07K16/32 ,  C07K2317/21

摘要： Described is a labeling technique which can facilitate the metabolism in the liver after administration to patients without the reduction in the antibody function, thereby reducing accumulation of radionuclides in an organ such as the liver, and a modified antibody containing an IgG antibody and an IgG-binding peptide bound to the IgG antibody. The IgG-binding peptide has an amino acid sequence consisting of 13 to 17 amino acid residues, such as GPDCAYH(Xaa1)GELVWCTFH (SEQ ID NO: 2) wherein Xaa1 represents a lysine residue, a cysteine residue, an aspartic acid residue, a glutamic acid residue, 2-aminosuberic acid, or diaminopropionic acid, and a compound represented by the following formula (II-1) is linked at a position of the lysine residue via a modification linker to the N terminus of the IgG-binding peptide.

公开(公告)号：US20180354915A1

公开(公告)日：2018-12-13

申请号：US16060297

申请日：2016-06-06

申请人： ZHEJIANG TIANYU PHARMACEUTICAL CO., LTD.

发明人： Guorong ZHU ,  Yongjun TU ,  Wenlong XIE ,  Zhen WANG ,  Shaojun XU

IPC分类号： C07D257/02 ,  B01D9/00

CPC分类号： C07D257/02 ,  A61P9/12 ,  B01D9/0054 ,  B01D9/0063 ,  C07C231/02 ,  C07C233/47 ,  C07D257/04

摘要： The present invention discloses a method for preparing an anti-heart-failure medicine LCZ696. The preparing method comprises the following step (formula (I)): in an organic solvent, a Sacubitril dicyclohexylamine salt reacts with valsartan under the effect of a sodium hydroxide aqueous solution, and the anti-heart-failure medicine LCZ696 is obtained. The preparing method of the present invention is simple in process and omits the procedures of ion exchange from a sodium salt to a calcium salt and hydrochloric acid dissociation in an existing production process, residues of calcium ions are avoided, and the production efficiency is effectively improved.

公开(公告)号：US20170340757A1

公开(公告)日：2017-11-30

申请号：US15534352

申请日：2015-12-10

申请人： RF Therapeutics Inc.

发明人： ZHANG Jidong ,  CURRY Ken

IPC分类号： A61K49/10 ,  A61K49/08

CPC分类号： A61K49/101 ,  A61K49/085 ,  A61K49/10 ,  A61K49/108 ,  C07C243/38 ,  C07D209/42 ,  C07D249/04 ,  C07D257/02 ,  C07D403/12 ,  C07D403/14

摘要： Described herein is a contrast agent for administration to a subject. The contrast agent includes a targeting portion that includes a hydrazide functional group; a metal ion bound to a metal-complexable portion; and a linker joining the targeting portion and the metal-complexable portion of the contrast agent. The portion that is not bound to a metal ion localizes the contrast agent to necrotic tissue in the subject.

公开(公告)号：US09822084B2

公开(公告)日：2017-11-21

申请号：US15511882

申请日：2015-09-07

申请人： ST PHARM CO., LTD.

发明人： Geun Jho Lim ,  Sun Ki Chang ,  Chang Ho Byeon ,  Hoe Jin Yoon ,  Moon Soo Kim

IPC分类号： C07D257/02

CPC分类号： C07D257/02 ,  C07F3/04

摘要： Disclosed is a novel method of preparing highly pure calcobutrol using an intermediate (butrol) of gadobutrol without using highly pure gadobutrol. This method is capable of obtaining calcobutrol at high purity and high yield through a simple and environmentally friendly process, and thus can be easily applied to mass production.