JP2019519491A5 - - Google Patents
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- JP2019519491A5 JP2019519491A5 JP2018558662A JP2018558662A JP2019519491A5 JP 2019519491 A5 JP2019519491 A5 JP 2019519491A5 JP 2018558662 A JP2018558662 A JP 2018558662A JP 2018558662 A JP2018558662 A JP 2018558662A JP 2019519491 A5 JP2019519491 A5 JP 2019519491A5
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- 150000001875 compounds Chemical class 0.000 claims 51
- 229910052739 hydrogen Inorganic materials 0.000 claims 7
- 239000001257 hydrogen Substances 0.000 claims 7
- 150000001408 amides Chemical class 0.000 claims 6
- 150000002148 esters Chemical class 0.000 claims 6
- 150000003839 salts Chemical class 0.000 claims 6
- 125000000171 (C1-C6) haloalkyl group Chemical group 0.000 claims 5
- 108090000765 processed proteins & peptides Proteins 0.000 claims 5
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 claims 4
- 229920000858 Cyclodextrin Polymers 0.000 claims 4
- 239000013522 chelant Substances 0.000 claims 4
- 150000003983 crown ethers Chemical class 0.000 claims 4
- 229940097362 cyclodextrins Drugs 0.000 claims 4
- 150000002431 hydrogen Chemical class 0.000 claims 4
- 150000004032 porphyrins Chemical class 0.000 claims 4
- 239000012453 solvate Substances 0.000 claims 4
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 claims 3
- 125000004737 (C1-C6) haloalkoxy group Chemical group 0.000 claims 3
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical class [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000004093 cyano group Chemical group *C#N 0.000 claims 3
- 229910052736 halogen Inorganic materials 0.000 claims 3
- 150000002367 halogens Chemical class 0.000 claims 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 claims 3
- 108010069514 Cyclic Peptides Proteins 0.000 claims 2
- 102000001189 Cyclic Peptides Human genes 0.000 claims 2
- AOJJSUZBOXZQNB-TZSSRYMLSA-N Doxorubicin Chemical compound O([C@H]1C[C@@](O)(CC=2C(O)=C3C(=O)C=4C=CC=C(C=4C(=O)C3=C(O)C=21)OC)C(=O)CO)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 AOJJSUZBOXZQNB-TZSSRYMLSA-N 0.000 claims 2
- 239000004480 active ingredient Substances 0.000 claims 2
- 125000000217 alkyl group Chemical group 0.000 claims 2
- 210000004027 cell Anatomy 0.000 claims 2
- 239000003937 drug carrier Substances 0.000 claims 2
- 239000000314 lubricant Substances 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- OZFJRKAKSNINHF-KKUMJFAQSA-N (2s)-2-[[[(4s)-4-[[(4s)-4-(6-aminohexanoylamino)-4-carboxybutanoyl]amino]-4-carboxybutoxy]-hydroxyphosphoryl]amino]pentanedioic acid Chemical compound NCCCCCC(=O)N[C@H](C(O)=O)CCC(=O)N[C@H](C(O)=O)CCCOP(O)(=O)N[C@H](C(O)=O)CCC(O)=O OZFJRKAKSNINHF-KKUMJFAQSA-N 0.000 claims 1
- 108091023037 Aptamer Proteins 0.000 claims 1
- IYMAXBFPHPZYIK-BQBZGAKWSA-N Arg-Gly-Asp Chemical compound NC(N)=NCCC[C@H](N)C(=O)NCC(=O)N[C@@H](CC(O)=O)C(O)=O IYMAXBFPHPZYIK-BQBZGAKWSA-N 0.000 claims 1
- 108010051479 Bombesin Proteins 0.000 claims 1
- 102000013585 Bombesin Human genes 0.000 claims 1
- KLWPJMFMVPTNCC-UHFFFAOYSA-N Camptothecin Natural products CCC1(O)C(=O)OCC2=C1C=C3C4Nc5ccccc5C=C4CN3C2=O KLWPJMFMVPTNCC-UHFFFAOYSA-N 0.000 claims 1
- 102000004269 Granulocyte Colony-Stimulating Factor Human genes 0.000 claims 1
- 108010017080 Granulocyte Colony-Stimulating Factor Proteins 0.000 claims 1
- 102000006992 Interferon-alpha Human genes 0.000 claims 1
- 108010047761 Interferon-alpha Proteins 0.000 claims 1
- 241000124008 Mammalia Species 0.000 claims 1
- 102400000740 Melanocyte-stimulating hormone alpha Human genes 0.000 claims 1
- 101710200814 Melanotropin alpha Proteins 0.000 claims 1
- ZDZOTLJHXYCWBA-VCVYQWHSSA-N N-debenzoyl-N-(tert-butoxycarbonyl)-10-deacetyltaxol Chemical compound O([C@H]1[C@H]2[C@@](C([C@H](O)C3=C(C)[C@@H](OC(=O)[C@H](O)[C@@H](NC(=O)OC(C)(C)C)C=4C=CC=CC=4)C[C@]1(O)C3(C)C)=O)(C)[C@@H](O)C[C@H]1OC[C@]12OC(=O)C)C(=O)C1=CC=CC=C1 ZDZOTLJHXYCWBA-VCVYQWHSSA-N 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- BPEGJWRSRHCHSN-UHFFFAOYSA-N Temozolomide Chemical compound O=C1N(C)N=NC2=C(C(N)=O)N=CN21 BPEGJWRSRHCHSN-UHFFFAOYSA-N 0.000 claims 1
- 229940120638 avastin Drugs 0.000 claims 1
- 239000011230 binding agent Substances 0.000 claims 1
- DNDCVAGJPBKION-DOPDSADYSA-N bombesin Chemical compound C([C@@H](C(=O)N[C@@H](CC(C)C)C(=O)N[C@@H](CCSC)C(N)=O)NC(=O)CNC(=O)[C@@H](NC(=O)[C@H](C)NC(=O)[C@H](CC=1NC2=CC=CC=C2C=1)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H](CC(N)=O)NC(=O)CNC(=O)[C@H](CC(C)C)NC(=O)[C@H](CCCNC(N)=N)NC(=O)[C@H](CCC(N)=O)NC(=O)[C@H]1NC(=O)CC1)C(C)C)C1=CN=CN1 DNDCVAGJPBKION-DOPDSADYSA-N 0.000 claims 1
- VSJKWCGYPAHWDS-FQEVSTJZSA-N camptothecin Chemical compound C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-FQEVSTJZSA-N 0.000 claims 1
- 229940127093 camptothecin Drugs 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- DQLATGHUWYMOKM-UHFFFAOYSA-L cisplatin Chemical compound N[Pt](N)(Cl)Cl DQLATGHUWYMOKM-UHFFFAOYSA-L 0.000 claims 1
- 229960004316 cisplatin Drugs 0.000 claims 1
- 239000003086 colorant Substances 0.000 claims 1
- 238000003745 diagnosis Methods 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- VSJKWCGYPAHWDS-UHFFFAOYSA-N dl-camptothecin Natural products C1=CC=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)C5(O)CC)C4=NC2=C1 VSJKWCGYPAHWDS-UHFFFAOYSA-N 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003995 emulsifying agent Substances 0.000 claims 1
- 229940082789 erbitux Drugs 0.000 claims 1
- 239000000796 flavoring agent Substances 0.000 claims 1
- 235000019634 flavors Nutrition 0.000 claims 1
- 229940022353 herceptin Drugs 0.000 claims 1
- 239000003906 humectant Substances 0.000 claims 1
- 239000000203 mixture Substances 0.000 claims 1
- CFODQUSMSYDHBS-UHFFFAOYSA-N octreotate Chemical compound O=C1NC(CC=2C=CC=CC=2)C(=O)NC(CC=2[C]3C=CC=CC3=NC=2)C(=O)NC(CCCCN)C(=O)NC(C(C)O)C(=O)NC(C(=O)NC(C(O)C)C(O)=O)CSSCC1NC(=O)C(N)CC1=CC=CC=C1 CFODQUSMSYDHBS-UHFFFAOYSA-N 0.000 claims 1
- 229960001592 paclitaxel Drugs 0.000 claims 1
- 239000008194 pharmaceutical composition Substances 0.000 claims 1
- 239000003755 preservative agent Substances 0.000 claims 1
- 230000002335 preservative effect Effects 0.000 claims 1
- 239000003381 stabilizer Substances 0.000 claims 1
- 239000004094 surface-active agent Substances 0.000 claims 1
- RCINICONZNJXQF-MZXODVADSA-N taxol Chemical compound O([C@@H]1[C@@]2(C[C@@H](C(C)=C(C2(C)C)[C@H](C([C@]2(C)[C@@H](O)C[C@H]3OC[C@]3([C@H]21)OC(C)=O)=O)OC(=O)C)OC(=O)[C@H](O)[C@@H](NC(=O)C=1C=CC=CC=1)C=1C=CC=CC=1)O)C(=O)C1=CC=CC=C1 RCINICONZNJXQF-MZXODVADSA-N 0.000 claims 1
- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims 1
- 229960004964 temozolomide Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- WHNFPRLDDSXQCL-UAZQEYIDSA-N α-msh Chemical compound C([C@@H](C(=O)N[C@@H](CO)C(=O)N[C@@H](CCSC)C(=O)N[C@@H](CCC(O)=O)C(=O)N[C@@H](CC=1NC=NC=1)C(=O)N[C@@H](CC=1C=CC=CC=1)C(=O)N[C@@H](CCCNC(N)=N)C(=O)N[C@@H](CC=1C2=CC=CC=C2NC=1)C(=O)NCC(=O)N[C@@H](CCCCN)C(=O)N1[C@@H](CCC1)C(=O)N[C@@H](C(C)C)C(N)=O)NC(=O)[C@H](CO)NC(C)=O)C1=CC=C(O)C=C1 WHNFPRLDDSXQCL-UAZQEYIDSA-N 0.000 claims 1
- WJLROCPIZOQIAS-UHFFFAOYSA-N CN(CCN(CCN(CC(O)=O)CC(O)=O)CC(O)=O)CC(O)=O Chemical compound CN(CCN(CCN(CC(O)=O)CC(O)=O)CC(O)=O)CC(O)=O WJLROCPIZOQIAS-UHFFFAOYSA-N 0.000 description 1
- ZJBDNCHDNHMUKT-QWRGUYRKSA-N C[C@@H](CCC(N[C@@H](CCCOP(NCCCC(O)=O)(O)=O)C(O)=O)=O)C(O)=O Chemical compound C[C@@H](CCC(N[C@@H](CCCOP(NCCCC(O)=O)(O)=O)C(O)=O)=O)C(O)=O ZJBDNCHDNHMUKT-QWRGUYRKSA-N 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662333427P | 2016-05-09 | 2016-05-09 | |
| US62/333,427 | 2016-05-09 | ||
| PCT/US2017/031696 WO2017196806A1 (en) | 2016-05-09 | 2017-05-09 | Chemical conjugates of evans blue derivatives and their use as radiotherapy and imaging agents |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019519491A JP2019519491A (ja) | 2019-07-11 |
| JP2019519491A5 true JP2019519491A5 (enExample) | 2020-05-28 |
| JP6946342B2 JP6946342B2 (ja) | 2021-10-06 |
Family
ID=60267260
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018558662A Active JP6946342B2 (ja) | 2016-05-09 | 2017-05-09 | エバンスブルー誘導体の化学的コンジュゲート、ならびに放射線治療剤およびイメージング剤としてのそれらの使用 |
Country Status (6)
| Country | Link |
|---|---|
| US (1) | US10696631B2 (enExample) |
| EP (1) | EP3455206B1 (enExample) |
| JP (1) | JP6946342B2 (enExample) |
| CN (1) | CN109153641B (enExample) |
| SG (1) | SG11201809982RA (enExample) |
| WO (1) | WO2017196806A1 (enExample) |
Families Citing this family (22)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10709790B2 (en) | 2015-06-22 | 2020-07-14 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Chemical conjugates of Evans Blue derivatives and their use in the production of long-acting therapeutics |
| US10981866B2 (en) * | 2017-10-03 | 2021-04-20 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents |
| JP7449864B2 (ja) * | 2018-02-22 | 2024-03-14 | ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ | エバンスブルー誘導体の化学結合体ならびに前立腺癌を標的とするための放射線療法および造影剤としてのその使用 |
| TWI745616B (zh) * | 2018-09-10 | 2021-11-11 | 行政院原子能委員會核能研究所 | 放射線標誌長效型靶向性胜肽藥物及其生產方法 |
| CN109485642A (zh) * | 2018-11-21 | 2019-03-19 | 希施生物科技（上海）有限公司 | 一种制备伊文氏蓝衍生物的方法 |
| WO2020160222A2 (en) | 2019-01-30 | 2020-08-06 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Conjugates of bivalent evans blue dye derivatives and methods of use |
| US12357712B2 (en) * | 2019-05-24 | 2025-07-15 | Beijing Giluntide Pharmaceutical Co., Ltd. | Targeted radiopharmaceutical for tumor and its use in the imaging-guided combination therapy of targeted radiotherapy and immunotherapy |
| CN115210240A (zh) * | 2020-03-04 | 2022-10-18 | 日本医事物理股份有限公司 | 化合物及放射性标记化合物 |
| KR20230027004A (ko) * | 2020-05-06 | 2023-02-27 | 코넬 유니버시티 | 구리-함유 테라그노스틱 화합물 및 사용 방법 |
| CN114790193B (zh) * | 2020-12-21 | 2024-05-10 | 苏州药明博锐生物科技有限公司 | 成纤维细胞活化蛋白抑制剂 |
| KR102648429B1 (ko) * | 2021-02-10 | 2024-03-18 | 옌타이 란나청 바이오테크놀로지 컴퍼니 리미티드 | 절단형 에반스 블루 변형의 섬유아세포 활성화 단백질 억제제 및 이의 제조 방법과 응용 |
| CN114369084B (zh) * | 2021-02-10 | 2023-02-03 | 烟台蓝纳成生物技术有限公司 | 一种截短型伊文思蓝修饰的成纤维细胞活化蛋白抑制剂及其制备方法和应用 |
| CN113004371A (zh) | 2021-03-01 | 2021-06-22 | 上海蓝纳成生物技术有限公司 | 一种长循环半衰期的前列腺特异性膜抗原靶向化合物及其制备方法和应用 |
| CN114796532A (zh) * | 2022-04-20 | 2022-07-29 | 北京先通国际医药科技股份有限公司 | 放射性标记的伊文思蓝衍生物药物水溶液及其用途 |
| AU2023283882A1 (en) * | 2022-06-10 | 2025-01-30 | Peking University | Trifunctional compound and use thereof |
| CN115433261B (zh) * | 2022-11-07 | 2023-01-13 | 烟台蓝纳成生物技术有限公司 | 一种rgd二聚体化合物及其制备方法和应用 |
| CN115583989B (zh) * | 2022-12-09 | 2023-02-28 | 烟台蓝纳成生物技术有限公司 | 一种靶向sstr2的化合物及其制备方法和应用 |
| CN115611779A (zh) * | 2022-12-21 | 2023-01-17 | 北京先通国际医药科技股份有限公司 | 一种放射性药物前体的中间体的制备方法及其用途 |
| CN115838393B (zh) * | 2023-02-16 | 2023-05-05 | 烟台蓝纳成生物技术有限公司 | 用于fapi合成的中间体及其制备方法和应用 |
| CN115850367B (zh) * | 2023-03-02 | 2023-05-23 | 北京先通国际医药科技股份有限公司 | Psma抑制剂的纯化方法及其用途 |
| CN115947775B (zh) * | 2023-03-13 | 2023-06-09 | 北京先通国际医药科技股份有限公司 | 一种制备化合物（i）的方法和化合物（i）及其用途 |
| AU2024276915A1 (en) * | 2023-05-24 | 2026-01-15 | Beijing Changping Laboratory | Novel trifunctional compound and use thereof |
Family Cites Families (12)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2004075925A1 (ja) | 2003-02-27 | 2004-09-10 | Kyushu Tlo Company Limited | Ｍｒｉ用造影剤 |
| WO2006025304A1 (ja) | 2004-08-30 | 2006-03-09 | Kyushu University, National University Corporation | 動脈硬化検知用ｍｒｉ造影剤 |
| CN101848668A (zh) * | 2007-09-14 | 2010-09-29 | 健康研究有限公司 | 用于肿瘤显像和治疗的多模态试剂 |
| US8143219B2 (en) * | 2008-02-26 | 2012-03-27 | Cornell University | Methods for prevention and treatment of acute renal injury |
| CN101623504A (zh) * | 2008-07-07 | 2010-01-13 | 中国人民解放军军事医学科学院放射与辐射医学研究所 | 伊文思蓝作为实体肿瘤着色剂的用途 |
| CN103242255B (zh) * | 2013-04-28 | 2015-01-14 | 厦门大学 | 伊文氏蓝配合物及其制备方法和应用 |
| CN104650217B (zh) * | 2015-01-26 | 2018-08-10 | 莎穆(上海)生物科技有限公司 | 伊文氏蓝或其衍生物修饰的Exendin-4及其制备方法和应用 |
| US20160287730A1 (en) | 2015-03-31 | 2016-10-06 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv | Labeled evans blue dye derivative for in vivo serum albumin labeling |
| US10709790B2 (en) | 2015-06-22 | 2020-07-14 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Chemical conjugates of Evans Blue derivatives and their use in the production of long-acting therapeutics |
| US20190298824A1 (en) | 2016-05-04 | 2019-10-03 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Serv | Albumin-binding immunomodulatory compositions and methods of use thereof |
| US10981866B2 (en) | 2017-10-03 | 2021-04-20 | The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Chemical conjugates of Evans Blue derivatives and their use as radiotherapy and imaging agents |
| JP7449864B2 (ja) | 2018-02-22 | 2024-03-14 | ザ ユナイテッド ステイツ オブ アメリカ， アズ リプレゼンテッド バイ ザ セクレタリー， デパートメント オブ ヘルス アンド ヒューマン サービシーズ | エバンスブルー誘導体の化学結合体ならびに前立腺癌を標的とするための放射線療法および造影剤としてのその使用 |
-
2017
- 2017-05-09 SG SG11201809982RA patent/SG11201809982RA/en unknown
- 2017-05-09 JP JP2018558662A patent/JP6946342B2/ja active Active
- 2017-05-09 US US16/099,488 patent/US10696631B2/en active Active
- 2017-05-09 WO PCT/US2017/031696 patent/WO2017196806A1/en not_active Ceased
- 2017-05-09 CN CN201780029003.XA patent/CN109153641B/zh active Active
- 2017-05-09 EP EP17796666.0A patent/EP3455206B1/en active Active
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