JP2020520902A5 - - Google Patents
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- JP2020520902A5 JP2020520902A5 JP2019562312A JP2019562312A JP2020520902A5 JP 2020520902 A5 JP2020520902 A5 JP 2020520902A5 JP 2019562312 A JP2019562312 A JP 2019562312A JP 2019562312 A JP2019562312 A JP 2019562312A JP 2020520902 A5 JP2020520902 A5 JP 2020520902A5
- Authority
- JP
- Japan
- Prior art keywords
- acid
- branched
- hydrocarbyl
- independently
- compound according
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Granted
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- 150000001875 compounds Chemical class 0.000 claims 30
- 229910052757 nitrogen Inorganic materials 0.000 claims 21
- 125000001183 hydrocarbyl group Chemical group 0.000 claims 18
- 125000004122 cyclic group Chemical group 0.000 claims 15
- -1 (carboxymethyl) -1,4,7-triazonan-1-yl Chemical group 0.000 claims 11
- 229910052794 bromium Inorganic materials 0.000 claims 11
- 229910052740 iodine Inorganic materials 0.000 claims 11
- 150000002148 esters Chemical class 0.000 claims 10
- 125000005842 heteroatom Chemical group 0.000 claims 10
- 150000003839 salts Chemical class 0.000 claims 10
- 239000012453 solvate Substances 0.000 claims 10
- JHALWMSZGCVVEM-UHFFFAOYSA-N 2-[4,7-bis(carboxymethyl)-1,4,7-triazonan-1-yl]acetic acid Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CC1 JHALWMSZGCVVEM-UHFFFAOYSA-N 0.000 claims 9
- QPCDCPDFJACHGM-UHFFFAOYSA-N N,N-bis{2-[bis(carboxymethyl)amino]ethyl}glycine Chemical compound OC(=O)CN(CC(O)=O)CCN(CC(=O)O)CCN(CC(O)=O)CC(O)=O QPCDCPDFJACHGM-UHFFFAOYSA-N 0.000 claims 9
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 229910052801 chlorine Inorganic materials 0.000 claims 9
- 229910052731 fluorine Inorganic materials 0.000 claims 9
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 9
- 229960003330 pentetic acid Drugs 0.000 claims 9
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 8
- 125000001147 pentyl group Chemical group C(CCCC)* 0.000 claims 8
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 8
- 125000006850 spacer group Chemical group 0.000 claims 8
- 125000005647 linker group Chemical group 0.000 claims 7
- 125000000008 (C1-C10) alkyl group Chemical group 0.000 claims 6
- 239000002253 acid Substances 0.000 claims 6
- ACHQFNGCBWWVRR-UHFFFAOYSA-N NOPO Chemical compound NOPO ACHQFNGCBWWVRR-UHFFFAOYSA-N 0.000 claims 5
- 125000000753 cycloalkyl group Chemical group 0.000 claims 5
- 229910052760 oxygen Inorganic materials 0.000 claims 5
- 239000008194 pharmaceutical composition Substances 0.000 claims 5
- ACVYVLVWPXVTIT-UHFFFAOYSA-N phosphinic acid Chemical compound O[PH2]=O ACVYVLVWPXVTIT-UHFFFAOYSA-N 0.000 claims 5
- 229910052717 sulfur Inorganic materials 0.000 claims 5
- 125000006657 (C1-C10) hydrocarbyl group Chemical group 0.000 claims 4
- WDLRUFUQRNWCPK-UHFFFAOYSA-N Tetraxetan Chemical compound OC(=O)CN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 WDLRUFUQRNWCPK-UHFFFAOYSA-N 0.000 claims 4
- 125000002777 acetyl group Chemical group [H]C([H])([H])C(*)=O 0.000 claims 4
- 125000002877 alkyl aryl group Chemical group 0.000 claims 4
- 239000002738 chelating agent Substances 0.000 claims 4
- JFCQEDHGNNZCLN-UHFFFAOYSA-N glutaric acid Chemical compound OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 4
- 125000006832 (C1-C10) alkylene group Chemical group 0.000 claims 3
- 125000006710 (C2-C12) alkenyl group Chemical group 0.000 claims 3
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 3
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 3
- 125000000539 amino acid group Chemical group 0.000 claims 3
- 229910052799 carbon Inorganic materials 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 229910052739 hydrogen Inorganic materials 0.000 claims 3
- 230000001404 mediated effect Effects 0.000 claims 3
- 125000006711 (C2-C12) alkynyl group Chemical group 0.000 claims 2
- DZTVAULYUGBHSF-UHFFFAOYSA-N 2-[4,7,10-tris(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]pentanedioic acid Chemical compound OC(=O)CCC(C(O)=O)N1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 DZTVAULYUGBHSF-UHFFFAOYSA-N 0.000 claims 2
- ZCYVEMRRCGMTRW-UHFFFAOYSA-N 7553-56-2 Chemical compound [I] ZCYVEMRRCGMTRW-UHFFFAOYSA-N 0.000 claims 2
- WKBOTKDWSSQWDR-UHFFFAOYSA-N Bromine atom Chemical compound [Br] WKBOTKDWSSQWDR-UHFFFAOYSA-N 0.000 claims 2
- 239000007983 Tris buffer Substances 0.000 claims 2
- 125000003118 aryl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- GDTBXPJZTBHREO-UHFFFAOYSA-N bromine Substances BrBr GDTBXPJZTBHREO-UHFFFAOYSA-N 0.000 claims 2
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 2
- 229910052736 halogen Inorganic materials 0.000 claims 2
- 150000002367 halogens Chemical class 0.000 claims 2
- 239000011630 iodine Substances 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 239000000203 mixture Substances 0.000 claims 2
- 125000000143 2-carboxyethyl group Chemical group [H]OC(=O)C([H])([H])C([H])([H])* 0.000 claims 1
- 102000009027 Albumins Human genes 0.000 claims 1
- 108010088751 Albumins Proteins 0.000 claims 1
- 206010005003 Bladder cancer Diseases 0.000 claims 1
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- CKLJMWTZIZZHCS-REOHCLBHSA-N L-aspartic acid Chemical compound OC(=O)[C@@H](N)CC(O)=O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 claims 1
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical compound NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims 1
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 1
- 239000004472 Lysine Substances 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 208000007097 Urinary Bladder Neoplasms Diseases 0.000 claims 1
- 125000000304 alkynyl group Chemical group 0.000 claims 1
- 235000003704 aspartic acid Nutrition 0.000 claims 1
- 125000001164 benzothiazolyl group Chemical group S1C(=NC2=C1C=CC=C2)* 0.000 claims 1
- OQFSQFPPLPISGP-UHFFFAOYSA-N beta-carboxyaspartic acid Natural products OC(=O)C(N)C(C(O)=O)C(O)=O OQFSQFPPLPISGP-UHFFFAOYSA-N 0.000 claims 1
- 239000004305 biphenyl Substances 0.000 claims 1
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 1
- 239000000032 diagnostic agent Substances 0.000 claims 1
- 229940039227 diagnostic agent Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 235000013922 glutamic acid Nutrition 0.000 claims 1
- 239000004220 glutamic acid Substances 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 235000018977 lysine Nutrition 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 125000001624 naphthyl group Chemical group 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 238000002600 positron emission tomography Methods 0.000 claims 1
- 210000002307 prostate Anatomy 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 210000001519 tissue Anatomy 0.000 claims 1
- 201000005112 urinary bladder cancer Diseases 0.000 claims 1
- 0 CC(C)I*N* Chemical compound CC(C)I*N* 0.000 description 5
- MWFDFYUDGPZYTC-UHFFFAOYSA-N CC(C)C(C(Cc1cc2ccccc2cc1)NC(C1CCC(CNC(C)=O)CC1)=O)=O Chemical compound CC(C)C(C(Cc1cc2ccccc2cc1)NC(C1CCC(CNC(C)=O)CC1)=O)=O MWFDFYUDGPZYTC-UHFFFAOYSA-N 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP17000891.6 | 2017-05-24 | ||
| EP17000891 | 2017-05-24 | ||
| PCT/EP2017/000717 WO2018233798A1 (en) | 2017-06-20 | 2017-06-20 | Novel psma-binding agents and uses thereof |
| EPPCT/EP2017/000717 | 2017-06-20 | ||
| PCT/EP2018/063734 WO2018215627A1 (en) | 2017-05-24 | 2018-05-24 | Novel psma-binding agents and uses thereof |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2020520902A JP2020520902A (ja) | 2020-07-16 |
| JP2020520902A5 true JP2020520902A5 (enExample) | 2021-07-26 |
| JP7340459B2 JP7340459B2 (ja) | 2023-09-07 |
Family
ID=62200468
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2019562312A Active JP7340459B2 (ja) | 2017-05-24 | 2018-05-24 | 新規ｐｓｍａ結合剤及びその使用 |
Country Status (9)
| Country | Link |
|---|---|
| US (1) | US11629201B2 (enExample) |
| EP (1) | EP3630204A1 (enExample) |
| JP (1) | JP7340459B2 (enExample) |
| KR (1) | KR102843240B1 (enExample) |
| CN (1) | CN110740757B (enExample) |
| AU (1) | AU2018274184B2 (enExample) |
| CA (1) | CA3060143A1 (enExample) |
| WO (1) | WO2018215627A1 (enExample) |
| ZA (1) | ZA201906832B (enExample) |
Families Citing this family (28)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US20200339625A1 (en) * | 2017-10-22 | 2020-10-29 | Provincial Health Services Authority | Novel radiometal-binding compounds for diagnosis or treatment of prostate specific membrane antigen-expressing cancer |
| US12228480B2 (en) * | 2018-11-30 | 2025-02-18 | Revvity Health Sciences, Inc. | Biological sample preparation using electric fields |
| AU2020208492A1 (en) * | 2019-01-17 | 2021-08-12 | Case Western Reserve University | Peptide PET/SPECT probes specific to oncoproteins in tumor extracellular matrix |
| US12472272B2 (en) | 2019-04-17 | 2025-11-18 | Provincial Health Services Authority | Radiolabelled compounds for diagnosis or treatment of prostate-specific membrane antigen- expressing cancer |
| EP3976025A4 (en) * | 2019-05-24 | 2023-05-17 | Clarity Pharmaceuticals Limited | PSMA IMAGING AGENT FORMULATIONS |
| AU2020296488A1 (en) | 2019-06-21 | 2022-01-20 | Provincial Health Services Authority | Radiolabeled compounds targeting the prostate-specific membrane antigen |
| TWI803688B (zh) * | 2019-08-26 | 2023-06-01 | 行政院原子能委員會核能研究所 | 一種psma靶向放射診療藥物備製方法 |
| KR102269315B1 (ko) * | 2019-10-24 | 2021-06-24 | 서울대학교산학협력단 | 전립선 암의 영상 또는 치료를 위한 동위원소 표지 화합물 |
| CN113350531A (zh) * | 2020-03-02 | 2021-09-07 | 上海核力星医药科技有限公司 | 前列腺特异性膜抗原结合配体偶联物及其应用 |
| WO2022096103A1 (en) | 2020-11-05 | 2022-05-12 | ITM Isotopen Technologien München AG | Combination of para-aminohippuric acid (pah) and radiolabeled complexes for treating cancer |
| WO2022111800A1 (en) | 2020-11-25 | 2022-06-02 | Itm Solucin Gmbh | Stable formulations for radionuclide complexes |
| CA3210294A1 (en) * | 2021-03-04 | 2022-09-09 | Yoshifumi Maya | Compound and radioactive labeling compound |
| CA3223227A1 (en) * | 2021-05-21 | 2022-11-24 | NorthStar Medical Technologies, LLC | Urokinase plasminogen activator receptor-targeted radiopharmaceutical |
| WO2023030509A1 (zh) * | 2021-09-03 | 2023-03-09 | 晶核生物医药科技(南京)有限公司 | 一种肽脲素衍生物、含其的药物组合物及其应用 |
| TW202321204A (zh) * | 2021-11-10 | 2023-06-01 | 大陸商蘇州瑞核醫藥科技有限公司 | 靶向前列腺特異性膜抗原的配體化合物及其螯合物與用於前列腺癌診斷和治療的應用 |
| EP4436979A1 (en) * | 2021-11-26 | 2024-10-02 | Full-Life Technologies HK Limited | Cleavable radioligands for targeting cell surface receptors and uses thereof |
| AU2023226956A1 (en) * | 2022-03-04 | 2024-09-12 | Provincial Health Services Authority | Radiolabeled compounds targetng the prostate-specific membrane antigen |
| CN115010629B (zh) * | 2022-06-07 | 2024-02-23 | 西南医科大学附属医院 | 前列腺特异性膜抗原抑制剂、其核素标记物及制法和应用 |
| KR20250057886A (ko) * | 2022-09-07 | 2025-04-29 | 쓰리비 파마슈티컬스 게엠베하 | 전립선 특이적 막 항원 (psma) 리간드 및 그의 용도 |
| WO2024051794A1 (zh) * | 2022-09-09 | 2024-03-14 | 同宜医药（苏州）有限公司 | 放射性核素偶联药物及其药物组合物和应用 |
| CN120282804A (zh) * | 2022-09-23 | 2025-07-08 | 核素迪姆股份公司 | 高纯度铜放射性药物组合物及其诊断和治疗用途 |
| TW202426433A (zh) | 2022-09-23 | 2024-07-01 | 瑞士商紐利迪姆股份公司 | 成纖維細胞活化蛋白（ｆａｐ）抑制劑、ｆａｐ結合物及其診斷與治療用途 |
| KR20250148672A (ko) * | 2023-02-16 | 2025-10-14 | 노로이 바이오사이언스 씨오., 엘티디. | Psma 표적 방사성 약물 및 그 합성과 응용 |
| WO2024245421A1 (en) * | 2023-05-31 | 2024-12-05 | Full-Life Technologies Hk Limited | Radioligands for targeting cell surface receptors and uses thereof |
| AU2024282453A1 (en) * | 2023-05-31 | 2025-12-04 | Full-Life Technologies Hk Limited | Conjugates and uses thereof |
| CN120265331A (zh) | 2023-07-31 | 2025-07-04 | 美国锔责任有限公司 | [177Lu]镥-PSMA I&T组合物及其剂量测定、试剂盒、制备方法和使用方法 |
| WO2025088147A1 (en) * | 2023-10-27 | 2025-05-01 | Deutsches Krebsforschungszentrum Stiftung des öffentlichen Rechts | Theranostic psma-targeting ligands for the diagnosis and treatment of psma-expressing cancers and their solid phase synthesis |
| WO2025218879A1 (en) | 2024-04-15 | 2025-10-23 | Itm Technologies Munich Se | Stable formulations comprising 225-actinium labeled complexes and methods for preparing the same |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0621973D0 (en) | 2006-11-03 | 2006-12-13 | Philogen Spa | Binding molecules and uses thereof |
| US9687572B2 (en) * | 2010-12-06 | 2017-06-27 | Molecular Insight Pharmaceuticals, Inc. | PSMA-targeted dendrimers |
| ES2732060T3 (es) | 2011-08-05 | 2019-11-20 | Molecular Insight Pharm Inc | Inhibidores radiomarcados del antígeno de membrana específico de la próstata |
| HUE068833T2 (hu) | 2011-08-17 | 2025-01-28 | Merck & Cie Kmg | Albumint megkötõ egységek folát konjugátjai |
| ES2743433T3 (es) | 2013-03-15 | 2020-02-19 | Cancer Targeted Tech Llc | Agentes para imágenes de pet dirigidos a psma marcados con 18F |
| AU2014336638C1 (en) * | 2013-10-18 | 2020-09-17 | Novartis Ag | Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer |
| EP2862857A1 (en) | 2013-10-18 | 2015-04-22 | Deutsches Krebsforschungszentrum | Labeled inhibitors of prostate specific membrane antigen (PSMA), their use as imaging agents and pharmaceutical agents for the treatment of prostate cancer |
| WO2018031809A1 (en) | 2016-08-10 | 2018-02-15 | Cancer Targeted Technology Llc | Chelated psma inhibitors |
-
2018
- 2018-05-24 KR KR1020197038065A patent/KR102843240B1/ko active Active
- 2018-05-24 CN CN201880034324.3A patent/CN110740757B/zh active Active
- 2018-05-24 JP JP2019562312A patent/JP7340459B2/ja active Active
- 2018-05-24 AU AU2018274184A patent/AU2018274184B2/en active Active
- 2018-05-24 EP EP18725856.1A patent/EP3630204A1/en active Pending
- 2018-05-24 WO PCT/EP2018/063734 patent/WO2018215627A1/en not_active Ceased
- 2018-05-24 US US16/616,744 patent/US11629201B2/en active Active
- 2018-05-24 CA CA3060143A patent/CA3060143A1/en active Pending
-
2019
- 2019-10-16 ZA ZA2019/06832A patent/ZA201906832B/en unknown
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