JPWO2022212958A5 - - Google Patents
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- JPWO2022212958A5 JPWO2022212958A5 JP2023560919A JP2023560919A JPWO2022212958A5 JP WO2022212958 A5 JPWO2022212958 A5 JP WO2022212958A5 JP 2023560919 A JP2023560919 A JP 2023560919A JP 2023560919 A JP2023560919 A JP 2023560919A JP WO2022212958 A5 JPWO2022212958 A5 JP WO2022212958A5
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- JP
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- group
- compound
- cancer
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- 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.)
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- 150000001875 compounds Chemical class 0.000 claims 26
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 14
- 125000000217 alkyl group Chemical group 0.000 claims 9
- 102100041003 Glutamate carboxypeptidase 2 Human genes 0.000 claims 8
- 101000892862 Homo sapiens Glutamate carboxypeptidase 2 Proteins 0.000 claims 8
- 201000010099 disease Diseases 0.000 claims 8
- 239000008194 pharmaceutical composition Substances 0.000 claims 7
- 208000035475 disorder Diseases 0.000 claims 6
- -1 1,8-diamino-3,6,10,13,16,19-hexazabicyclo(6,6,6)eicosane-3,6,10,13,16,19-hexazabicyclo[6.6.6]eicosane-1,8-diamine Chemical compound 0.000 claims 5
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 claims 5
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims 4
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 102100023832 Prolyl endopeptidase FAP Human genes 0.000 claims 3
- 206010060862 Prostate cancer Diseases 0.000 claims 3
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 3
- 125000002877 alkyl aryl group Chemical group 0.000 claims 3
- 108010072257 fibroblast activation protein alpha Proteins 0.000 claims 3
- 238000003384 imaging method Methods 0.000 claims 3
- 125000005647 linker group Chemical group 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- 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 2
- WBRUPBYQJCBBBL-UHFFFAOYSA-N 2-[4-(carboxymethyl)-1,4,7-triazonan-1-yl]acetic acid Chemical compound OC(=O)CN1CCNCCN(CC(O)=O)CC1 WBRUPBYQJCBBBL-UHFFFAOYSA-N 0.000 claims 2
- SYFGLWDDLZQFNI-UHFFFAOYSA-N 2-[4-(carboxymethyl)-1,4,8,11-tetrazabicyclo[6.6.2]hexadecan-11-yl]acetic acid Chemical compound C1CN(CC(O)=O)CCCN2CCN(CC(=O)O)CCCN1CC2 SYFGLWDDLZQFNI-UHFFFAOYSA-N 0.000 claims 2
- OOLRAQKFMNOZBV-UHFFFAOYSA-N 8-n-[(4-aminophenyl)methyl]-3,6,10,13,16,19-hexazabicyclo[6.6.6]icosane-1,8-diamine Chemical compound C1=CC(N)=CC=C1CNC1(CNCCNC2)CNCCNCC2(N)CNCCNC1 OOLRAQKFMNOZBV-UHFFFAOYSA-N 0.000 claims 2
- 206010006187 Breast cancer Diseases 0.000 claims 2
- 208000026310 Breast neoplasm Diseases 0.000 claims 2
- 206010009944 Colon cancer Diseases 0.000 claims 2
- 208000001333 Colorectal Neoplasms Diseases 0.000 claims 2
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 2
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 2
- UBQYURCVBFRUQT-UHFFFAOYSA-N N-benzoyl-Ferrioxamine B Chemical compound CC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCNC(=O)CCC(=O)N(O)CCCCCN UBQYURCVBFRUQT-UHFFFAOYSA-N 0.000 claims 2
- 206010033128 Ovarian cancer Diseases 0.000 claims 2
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 2
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 2
- 206010038389 Renal cancer Diseases 0.000 claims 2
- JVHROZDXPAUZFK-UHFFFAOYSA-N TETA Chemical compound OC(=O)CN1CCCN(CC(O)=O)CCN(CC(O)=O)CCCN(CC(O)=O)CC1 JVHROZDXPAUZFK-UHFFFAOYSA-N 0.000 claims 2
- 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 2
- 235000011054 acetic acid Nutrition 0.000 claims 2
- 230000001588 bifunctional effect Effects 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 229910052799 carbon Inorganic materials 0.000 claims 2
- 125000000753 cycloalkyl group Chemical group 0.000 claims 2
- 229960000958 deferoxamine Drugs 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 208000014829 head and neck neoplasm Diseases 0.000 claims 2
- 125000001072 heteroaryl group Chemical group 0.000 claims 2
- 201000010982 kidney cancer Diseases 0.000 claims 2
- 201000005202 lung cancer Diseases 0.000 claims 2
- 208000020816 lung neoplasm Diseases 0.000 claims 2
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 2
- 238000000034 method Methods 0.000 claims 2
- 201000002528 pancreatic cancer Diseases 0.000 claims 2
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 2
- 230000002062 proliferating effect Effects 0.000 claims 2
- 239000000126 substance Substances 0.000 claims 2
- 125000000547 substituted alkyl group Chemical group 0.000 claims 2
- 125000005346 substituted cycloalkyl group Chemical group 0.000 claims 2
- 230000008685 targeting Effects 0.000 claims 2
- QBPPRVHXOZRESW-UHFFFAOYSA-N 1,4,7,10-tetraazacyclododecane Chemical compound C1CNCCNCCNCCN1 QBPPRVHXOZRESW-UHFFFAOYSA-N 0.000 claims 1
- ITWBWJFEJCHKSN-UHFFFAOYSA-N 1,4,7-triazonane Chemical compound C1CNCCNCCN1 ITWBWJFEJCHKSN-UHFFFAOYSA-N 0.000 claims 1
- FQVAEMASBCTTJN-UHFFFAOYSA-N 2-[4,7-bis(2-sulfanylethyl)-1,4,7-triazonan-1-yl]ethanethiol Chemical compound SCCN1CCN(CCS)CCN(CCS)CC1 FQVAEMASBCTTJN-UHFFFAOYSA-N 0.000 claims 1
- HOFAGEWOGCQDAL-UHFFFAOYSA-N 2-[4-[2-[bis(carboxymethyl)amino]ethyl]-7,10-bis(carboxymethyl)-1,4,7,10-tetrazacyclododec-1-yl]acetic acid Chemical compound OC(=O)CN(CC(O)=O)CCN1CCN(CC(O)=O)CCN(CC(O)=O)CCN(CC(O)=O)CC1 HOFAGEWOGCQDAL-UHFFFAOYSA-N 0.000 claims 1
- WQMDWBJCGNFKRK-UHFFFAOYSA-N 2-[4-[2-[bis(carboxymethyl)amino]ethyl]-7-(carboxymethyl)-1,4,7-triazonan-1-yl]acetic acid Chemical compound OC(=O)CN(CC(O)=O)CCN1CCN(CC(O)=O)CCN(CC(O)=O)CC1 WQMDWBJCGNFKRK-UHFFFAOYSA-N 0.000 claims 1
- UQQQAKFVWNQYTP-UHFFFAOYSA-N 3,6,10,13,16,19-hexazabicyclo[6.6.6]icosane-1,8-diamine Chemical compound C1NCCNCC2(N)CNCCNCC1(N)CNCCNC2 UQQQAKFVWNQYTP-UHFFFAOYSA-N 0.000 claims 1
- JZGOMSHZCWYDBB-UHFFFAOYSA-N 4-[[(1-amino-3,6,10,13,16,19-hexazabicyclo[6.6.6]icosan-8-yl)amino]methyl]benzoic acid Chemical compound C1NCCNCC(N)(CNCCNC2)CNCCNCC12NCC1=CC=C(C(O)=O)C=C1 JZGOMSHZCWYDBB-UHFFFAOYSA-N 0.000 claims 1
- 208000003200 Adenoma Diseases 0.000 claims 1
- 206010001233 Adenoma benign Diseases 0.000 claims 1
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010008342 Cervix carcinoma Diseases 0.000 claims 1
- 206010053567 Coagulopathies Diseases 0.000 claims 1
- 101100294331 Drosophila melanogaster nod gene Proteins 0.000 claims 1
- 208000001976 Endocrine Gland Neoplasms Diseases 0.000 claims 1
- 208000000461 Esophageal Neoplasms Diseases 0.000 claims 1
- 201000008808 Fibrosarcoma Diseases 0.000 claims 1
- 208000008999 Giant Cell Carcinoma Diseases 0.000 claims 1
- 206010025323 Lymphomas Diseases 0.000 claims 1
- 241001181114 Neta Species 0.000 claims 1
- 206010030155 Oesophageal carcinoma Diseases 0.000 claims 1
- 238000012879 PET imaging Methods 0.000 claims 1
- 208000006265 Renal cell carcinoma Diseases 0.000 claims 1
- 208000000453 Skin Neoplasms Diseases 0.000 claims 1
- 208000021712 Soft tissue sarcoma Diseases 0.000 claims 1
- 208000005718 Stomach Neoplasms Diseases 0.000 claims 1
- 208000006105 Uterine Cervical Neoplasms Diseases 0.000 claims 1
- 208000002495 Uterine Neoplasms Diseases 0.000 claims 1
- 208000009956 adenocarcinoma Diseases 0.000 claims 1
- 239000002671 adjuvant Substances 0.000 claims 1
- 125000002947 alkylene group Chemical group 0.000 claims 1
- JFCQEDHGNNZCLN-UHFFFAOYSA-N anhydrous glutaric acid Natural products OC(=O)CCCC(O)=O JFCQEDHGNNZCLN-UHFFFAOYSA-N 0.000 claims 1
- 125000003118 aryl group Chemical group 0.000 claims 1
- 230000023555 blood coagulation Effects 0.000 claims 1
- 206010006007 bone sarcoma Diseases 0.000 claims 1
- 150000001721 carbon Chemical group 0.000 claims 1
- 125000002057 carboxymethyl group Chemical group [H]OC(=O)C([H])([H])[*] 0.000 claims 1
- 201000010881 cervical cancer Diseases 0.000 claims 1
- 239000002738 chelating agent Substances 0.000 claims 1
- 208000037976 chronic inflammation Diseases 0.000 claims 1
- 230000006020 chronic inflammation Effects 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 108700013553 diamsar chelate Proteins 0.000 claims 1
- 230000001079 digestive effect Effects 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 239000003814 drug Substances 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000004064 dysfunction Effects 0.000 claims 1
- 230000002124 endocrine Effects 0.000 claims 1
- 201000004101 esophageal cancer Diseases 0.000 claims 1
- 206010017758 gastric cancer Diseases 0.000 claims 1
- 229910052736 halogen Inorganic materials 0.000 claims 1
- 150000002367 halogens Chemical class 0.000 claims 1
- 208000032839 leukemia Diseases 0.000 claims 1
- 239000003446 ligand Substances 0.000 claims 1
- 201000000014 lung giant cell carcinoma Diseases 0.000 claims 1
- 208000029559 malignant endocrine neoplasm Diseases 0.000 claims 1
- 208000026037 malignant tumor of neck Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 239000002184 metal Substances 0.000 claims 1
- 229910052751 metal Inorganic materials 0.000 claims 1
- YACKEPLHDIMKIO-UHFFFAOYSA-N methylphosphonic acid Chemical compound CP(O)(O)=O YACKEPLHDIMKIO-UHFFFAOYSA-N 0.000 claims 1
- UXDAWVUDZLBBAM-UHFFFAOYSA-N n,n-diethylbenzeneacetamide Chemical compound CCN(CC)C(=O)CC1=CC=CC=C1 UXDAWVUDZLBBAM-UHFFFAOYSA-N 0.000 claims 1
- 229910052757 nitrogen Inorganic materials 0.000 claims 1
- 238000012634 optical imaging Methods 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims 1
- 125000002943 quinolinyl group Chemical group N1=C(C=CC2=CC=CC=C12)* 0.000 claims 1
- 230000002285 radioactive effect Effects 0.000 claims 1
- 238000001959 radiotherapy Methods 0.000 claims 1
- 238000002603 single-photon emission computed tomography Methods 0.000 claims 1
- 201000000849 skin cancer Diseases 0.000 claims 1
- 206010041823 squamous cell carcinoma Diseases 0.000 claims 1
- 201000011549 stomach cancer Diseases 0.000 claims 1
- 125000003107 substituted aryl group Chemical group 0.000 claims 1
- 239000001384 succinic acid Substances 0.000 claims 1
- 230000007838 tissue remodeling Effects 0.000 claims 1
- 150000003852 triazoles Chemical group 0.000 claims 1
- 230000002485 urinary effect Effects 0.000 claims 1
- 206010046766 uterine cancer Diseases 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US202163170035P | 2021-04-02 | 2021-04-02 | |
| US63/170,035 | 2021-04-02 | ||
| PCT/US2022/023374 WO2022212958A1 (en) | 2021-04-02 | 2022-04-04 | Heterobivalent and homobivalent agents targeting fibroblast activation protein alpha and/or prostate-specific membrane antigen |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2024514528A JP2024514528A (ja) | 2024-04-02 |
| JP2024514528A5 JP2024514528A5 (https=) | 2025-04-14 |
| JPWO2022212958A5 true JPWO2022212958A5 (https=) | 2025-04-14 |
Family
ID=83459940
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2023560919A Pending JP2024514528A (ja) | 2021-04-02 | 2022-04-04 | 線維芽細胞活性化タンパク質アルファおよび／または前立腺特異的膜抗原を標的とするヘテロ二価およびホモ二価薬剤 |
Country Status (11)
| Country | Link |
|---|---|
| US (1) | US20240382629A1 (https=) |
| EP (1) | EP4313049A4 (https=) |
| JP (1) | JP2024514528A (https=) |
| KR (1) | KR20230165818A (https=) |
| CN (1) | CN117255685A (https=) |
| AU (1) | AU2022252419A1 (https=) |
| BR (1) | BR112023020123A2 (https=) |
| CA (1) | CA3214070A1 (https=) |
| IL (1) | IL307405A (https=) |
| MX (2) | MX2023011599A (https=) |
| WO (1) | WO2022212958A1 (https=) |
Families Citing this family (13)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| AU2023347470A1 (en) | 2022-09-23 | 2025-04-10 | Nuclidium Ag | High-purity copper radiopharmaceutical compositions and diagnostic and therapeutic uses thereof |
| CN117883585A (zh) * | 2022-10-14 | 2024-04-16 | 无锡诺宇医药科技有限公司 | 靶向成纤维细胞活化蛋白的药物及其应用 |
| WO2024222888A1 (zh) * | 2023-04-27 | 2024-10-31 | 中国科学院上海药物研究所 | 一种fap抑制剂和靶向fap核素探针及其应用 |
| US12440585B2 (en) * | 2023-09-12 | 2025-10-14 | Curadel Surgical Innovations, Inc. | Zwitterionic metal chelators |
| WO2025087229A1 (zh) * | 2023-10-27 | 2025-05-01 | 四川科伦博泰生物医药股份有限公司 | 一类喹啉结构的配体化合物及其放射性或非放射性标记物以及应用 |
| KR20250062978A (ko) * | 2023-10-31 | 2025-05-08 | 서울대학교병원 | 신규한 전립선 특이적 막 항원 리간드 및 이의 용도 |
| WO2025119908A1 (en) * | 2023-12-06 | 2025-06-12 | Bracco Imaging Spa | Psma-targeting fluorescent probes |
| WO2025163029A1 (en) | 2024-01-31 | 2025-08-07 | Bracco Imaging Spa | Psma-targeting bimodal and heterobivalent fluorescent agents |
| CN117700485B (zh) * | 2024-02-04 | 2024-04-16 | 山东大学 | 一种同时靶向psma和fap的化合物及其制备方法与应用 |
| WO2025167951A1 (zh) * | 2024-02-07 | 2025-08-14 | 苏州博锐创合医药有限公司 | 一种成纤维细胞活化蛋白抑制剂 |
| CN118271393B (zh) * | 2024-05-31 | 2024-09-03 | 中国药科大学 | 一种靶向fap的二聚化合物及其探针和应用 |
| CN119080743B (zh) * | 2024-08-30 | 2026-01-06 | 北京师范大学 | 靶向psma和fap的双重靶向化合物及其应用 |
Family Cites Families (6)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2013107820A1 (en) * | 2012-01-17 | 2013-07-25 | Universiteit Antwerpen | Novel fap inhibitors |
| EA202090776A1 (ru) * | 2017-10-23 | 2020-07-27 | Дзе Джонс Хопкинс Юниверсити | Визуализирующие и радиотерапевтические агенты, нацеленные на фибробласт-активирующий белок-альфа (fapalpha) |
| SG11202007180QA (en) * | 2018-02-06 | 2020-08-28 | Univ Heidelberg | Fap inhibitor |
| CA3093694A1 (en) * | 2018-03-12 | 2019-09-19 | Memorial Sloan Kettering Cancer Center | Bispecific binding agents and uses thereof |
| US11279698B2 (en) * | 2018-11-20 | 2022-03-22 | Cornell University | Macrocyclic complexes of alpha-emitting radionuclides and their use in targeted radiotherapy of cancer |
| CN113292538A (zh) * | 2021-05-10 | 2021-08-24 | 北京肿瘤医院(北京大学肿瘤医院) | 靶向肿瘤相关成纤维细胞激活蛋白的化合物及其制备方法和应用与靶向fap的肿瘤显影剂 |
-
2022
- 2022-04-04 BR BR112023020123A patent/BR112023020123A2/pt unknown
- 2022-04-04 MX MX2023011599A patent/MX2023011599A/es unknown
- 2022-04-04 US US18/553,092 patent/US20240382629A1/en active Pending
- 2022-04-04 JP JP2023560919A patent/JP2024514528A/ja active Pending
- 2022-04-04 CN CN202280032772.6A patent/CN117255685A/zh active Pending
- 2022-04-04 EP EP22782372.1A patent/EP4313049A4/en active Pending
- 2022-04-04 IL IL307405A patent/IL307405A/en unknown
- 2022-04-04 WO PCT/US2022/023374 patent/WO2022212958A1/en not_active Ceased
- 2022-04-04 KR KR1020237037723A patent/KR20230165818A/ko active Pending
- 2022-04-04 AU AU2022252419A patent/AU2022252419A1/en active Pending
- 2022-04-04 CA CA3214070A patent/CA3214070A1/en active Pending
-
2023
- 2023-09-29 MX MX2026000948A patent/MX2026000948A/es unknown
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