JP2020532496A5 - - Google Patents
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- Publication number
- JP2020532496A5 JP2020532496A5 JP2020504380A JP2020504380A JP2020532496A5 JP 2020532496 A5 JP2020532496 A5 JP 2020532496A5 JP 2020504380 A JP2020504380 A JP 2020504380A JP 2020504380 A JP2020504380 A JP 2020504380A JP 2020532496 A5 JP2020532496 A5 JP 2020532496A5
- Authority
- JP
- Japan
- Prior art keywords
- ipr
- lys
- selective binding
- binding ligand
- high affinity
- 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.)
- Pending
Links
- 102100031650 C-X-C chemokine receptor type 4 Human genes 0.000 claims 21
- 101000922348 Homo sapiens C-X-C chemokine receptor type 4 Proteins 0.000 claims 21
- 239000003446 ligand Substances 0.000 claims 21
- 239000000863 peptide conjugate Substances 0.000 claims 20
- -1 D-Dab Chemical compound 0.000 claims 7
- 229960001592 paclitaxel Drugs 0.000 claims 7
- 206010028980 Neoplasm Diseases 0.000 claims 6
- FFFHZYDWPBMWHY-VKHMYHEASA-N L-homocysteine Chemical class OC(=O)[C@@H](N)CCS FFFHZYDWPBMWHY-VKHMYHEASA-N 0.000 claims 5
- 201000011510 cancer Diseases 0.000 claims 5
- 235000018417 cysteine Nutrition 0.000 claims 5
- XUJNEKJLAYXESH-UHFFFAOYSA-N cysteine Natural products SCC(N)C(O)=O XUJNEKJLAYXESH-UHFFFAOYSA-N 0.000 claims 5
- PECYZEOJVXMISF-UWTATZPHSA-N 3-amino-D-alanine Chemical compound NC[C@@H](N)C(O)=O PECYZEOJVXMISF-UWTATZPHSA-N 0.000 claims 4
- AHLPHDHHMVZTML-SCSAIBSYSA-N D-Ornithine Chemical compound NCCC[C@@H](N)C(O)=O AHLPHDHHMVZTML-SCSAIBSYSA-N 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 238000003384 imaging method Methods 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- 125000004434 sulfur atom Chemical group 0.000 claims 4
- XUJNEKJLAYXESH-REOHCLBHSA-N L-Cysteine Chemical compound SC[C@H](N)C(O)=O XUJNEKJLAYXESH-REOHCLBHSA-N 0.000 claims 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 3
- 125000003107 substituted aryl group Chemical group 0.000 claims 3
- 229940124597 therapeutic agent Drugs 0.000 claims 3
- DKIDEFUBRARXTE-UHFFFAOYSA-N 3-mercaptopropanoic acid Chemical compound OC(=O)CCS DKIDEFUBRARXTE-UHFFFAOYSA-N 0.000 claims 2
- LLUXQOVDMQZMPJ-KKUMJFAQSA-N Cys-Tyr-Lys Chemical compound NCCCC[C@@H](C(O)=O)NC(=O)[C@@H](NC(=O)[C@@H](N)CS)CC1=CC=C(O)C=C1 LLUXQOVDMQZMPJ-KKUMJFAQSA-N 0.000 claims 2
- ODKSFYDXXFIFQN-SCSAIBSYSA-N D-arginine Chemical compound OC(=O)[C@H](N)CCCNC(N)=N ODKSFYDXXFIFQN-SCSAIBSYSA-N 0.000 claims 2
- WHUUTDBJXJRKMK-GSVOUGTGSA-N D-glutamic acid Chemical compound OC(=O)[C@H](N)CCC(O)=O WHUUTDBJXJRKMK-GSVOUGTGSA-N 0.000 claims 2
- KDXKERNSBIXSRK-RXMQYKEDSA-N D-lysine Chemical compound NCCCC[C@@H](N)C(O)=O KDXKERNSBIXSRK-RXMQYKEDSA-N 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
- 150000001945 cysteines Chemical class 0.000 claims 2
- 239000000032 diagnostic agent Substances 0.000 claims 2
- 125000000524 functional group Chemical group 0.000 claims 2
- 239000002835 hiv fusion inhibitor Substances 0.000 claims 2
- 239000012216 imaging agent Substances 0.000 claims 2
- 150000003839 salts Chemical class 0.000 claims 2
- STQGQHZAVUOBTE-UHFFFAOYSA-N 7-Cyan-hept-2t-en-4,6-diinsaeure Natural products C1=2C(O)=C3C(=O)C=4C(OC)=CC=CC=4C(=O)C3=C(O)C=2CC(O)(C(C)=O)CC1OC1CC(N)C(O)C(C)O1 STQGQHZAVUOBTE-UHFFFAOYSA-N 0.000 claims 1
- 108010006654 Bleomycin Proteins 0.000 claims 1
- 206010006187 Breast cancer Diseases 0.000 claims 1
- 208000026310 Breast neoplasm Diseases 0.000 claims 1
- 238000009007 Diagnostic Kit Methods 0.000 claims 1
- 208000031886 HIV Infections Diseases 0.000 claims 1
- 108010078851 HIV Reverse Transcriptase Proteins 0.000 claims 1
- 208000037357 HIV infectious disease Diseases 0.000 claims 1
- 229940099797 HIV integrase inhibitor Drugs 0.000 claims 1
- 208000008839 Kidney Neoplasms Diseases 0.000 claims 1
- 206010058467 Lung neoplasm malignant Diseases 0.000 claims 1
- 208000028018 Lymphocytic leukaemia Diseases 0.000 claims 1
- 208000034578 Multiple myelomas Diseases 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
- 206010029260 Neuroblastoma Diseases 0.000 claims 1
- 208000015914 Non-Hodgkin lymphomas Diseases 0.000 claims 1
- 206010033128 Ovarian cancer Diseases 0.000 claims 1
- 206010061535 Ovarian neoplasm Diseases 0.000 claims 1
- 229930012538 Paclitaxel Natural products 0.000 claims 1
- 206010061902 Pancreatic neoplasm Diseases 0.000 claims 1
- DBNGDEAQXGFGRA-ACRUOGEOSA-N Phe-Tyr-Lys Chemical compound C1=CC=C(C=C1)C[C@@H](C(=O)N[C@@H](CC2=CC=C(C=C2)O)C(=O)N[C@@H](CCCCN)C(=O)O)N DBNGDEAQXGFGRA-ACRUOGEOSA-N 0.000 claims 1
- 206010035226 Plasma cell myeloma Diseases 0.000 claims 1
- 206010060862 Prostate cancer Diseases 0.000 claims 1
- 208000000236 Prostatic Neoplasms Diseases 0.000 claims 1
- 208000015634 Rectal Neoplasms Diseases 0.000 claims 1
- 206010038389 Renal cancer Diseases 0.000 claims 1
- 229940122803 Vinca alkaloid Drugs 0.000 claims 1
- 125000000217 alkyl group Chemical group 0.000 claims 1
- 150000001408 amides Chemical class 0.000 claims 1
- 125000000539 amino acid group Chemical group 0.000 claims 1
- 125000003710 aryl alkyl group Chemical group 0.000 claims 1
- 230000001588 bifunctional effect Effects 0.000 claims 1
- 229960001561 bleomycin Drugs 0.000 claims 1
- OYVAGSVQBOHSSS-UAPAGMARSA-O bleomycin A2 Chemical compound N([C@H](C(=O)N[C@H](C)[C@@H](O)[C@H](C)C(=O)N[C@@H]([C@H](O)C)C(=O)NCCC=1SC=C(N=1)C=1SC=C(N=1)C(=O)NCCC[S+](C)C)[C@@H](O[C@H]1[C@H]([C@@H](O)[C@H](O)[C@H](CO)O1)O[C@@H]1[C@H]([C@@H](OC(N)=O)[C@H](O)[C@@H](CO)O1)O)C=1N=CNC=1)C(=O)C1=NC([C@H](CC(N)=O)NC[C@H](N)C(N)=O)=NC(N)=C1C OYVAGSVQBOHSSS-UAPAGMARSA-O 0.000 claims 1
- 230000001684 chronic effect Effects 0.000 claims 1
- 230000000112 colonic effect Effects 0.000 claims 1
- 239000000562 conjugate Substances 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 229960000975 daunorubicin Drugs 0.000 claims 1
- STQGQHZAVUOBTE-VGBVRHCVSA-N daunorubicin 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(C)=O)[C@H]1C[C@H](N)[C@H](O)[C@H](C)O1 STQGQHZAVUOBTE-VGBVRHCVSA-N 0.000 claims 1
- 229940039227 diagnostic agent Drugs 0.000 claims 1
- 239000003085 diluting agent Substances 0.000 claims 1
- 229960003668 docetaxel Drugs 0.000 claims 1
- 229960004679 doxorubicin Drugs 0.000 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- BEBCJVAWIBVWNZ-UHFFFAOYSA-N glycinamide Chemical group NCC(N)=O BEBCJVAWIBVWNZ-UHFFFAOYSA-N 0.000 claims 1
- 239000003084 hiv integrase inhibitor Substances 0.000 claims 1
- 239000004030 hiv protease inhibitor Substances 0.000 claims 1
- 208000033519 human immunodeficiency virus infectious disease Diseases 0.000 claims 1
- 229960004768 irinotecan Drugs 0.000 claims 1
- UWKQSNNFCGGAFS-XIFFEERXSA-N irinotecan Chemical compound C1=C2C(CC)=C3CN(C(C4=C([C@@](C(=O)OC4)(O)CC)C=4)=O)C=4C3=NC2=CC=C1OC(=O)N(CC1)CCC1N1CCCCC1 UWKQSNNFCGGAFS-XIFFEERXSA-N 0.000 claims 1
- 201000010982 kidney cancer Diseases 0.000 claims 1
- 201000005202 lung cancer Diseases 0.000 claims 1
- 208000020816 lung neoplasm Diseases 0.000 claims 1
- 208000003747 lymphoid leukemia Diseases 0.000 claims 1
- 208000015486 malignant pancreatic neoplasm Diseases 0.000 claims 1
- 201000001441 melanoma Diseases 0.000 claims 1
- 201000002528 pancreatic cancer Diseases 0.000 claims 1
- 208000008443 pancreatic carcinoma Diseases 0.000 claims 1
- 125000001151 peptidyl group Chemical group 0.000 claims 1
- 239000000546 pharmaceutical excipient Substances 0.000 claims 1
- 208000005069 pulmonary fibrosis Diseases 0.000 claims 1
- 206010038038 rectal cancer Diseases 0.000 claims 1
- 201000001275 rectum cancer Diseases 0.000 claims 1
- 206010039073 rheumatoid arthritis Diseases 0.000 claims 1
- 239000003419 rna directed dna polymerase inhibitor 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
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 229960000303 topotecan Drugs 0.000 claims 1
- UCFGDBYHRUNTLO-QHCPKHFHSA-N topotecan Chemical compound C1=C(O)C(CN(C)C)=C2C=C(CN3C4=CC5=C(C3=O)COC(=O)[C@]5(O)CC)C4=NC2=C1 UCFGDBYHRUNTLO-QHCPKHFHSA-N 0.000 claims 1
- 0 CNC(CSCc1ccccc1CSCC(C(*)=O)N*)C(*)=O Chemical compound CNC(CSCc1ccccc1CSCC(C(*)=O)N*)C(*)=O 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201762554354P | 2017-09-05 | 2017-09-05 | |
| US62/554,354 | 2017-09-05 | ||
| PCT/US2018/018530 WO2019050564A1 (en) | 2017-09-05 | 2018-02-17 | CXCR4 SELECTIVE BINDING CONJUGATE WITH HIGH AFFINITY AND METHOD OF USING THE SAME |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2020532496A JP2020532496A (ja) | 2020-11-12 |
| JP2020532496A5 true JP2020532496A5 (cg-RX-API-DMAC10.html) | 2021-02-04 |
Family
ID=65635072
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020504380A Pending JP2020532496A (ja) | 2017-09-05 | 2018-02-17 | 高親和性ｃｘｃｒ４選択的結合抱合体およびその使用方法 |
Country Status (6)
| Country | Link |
|---|---|
| EP (1) | EP3679053A4 (cg-RX-API-DMAC10.html) |
| JP (1) | JP2020532496A (cg-RX-API-DMAC10.html) |
| KR (2) | KR20230145543A (cg-RX-API-DMAC10.html) |
| CN (1) | CN111183146A (cg-RX-API-DMAC10.html) |
| CA (1) | CA3065086A1 (cg-RX-API-DMAC10.html) |
| WO (1) | WO2019050564A1 (cg-RX-API-DMAC10.html) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US11123437B2 (en) | 2017-09-05 | 2021-09-21 | Mainline Biosciences, Inc. | Selective CXCR4 binding peptide conjugate and methods for making and using the same |
| JP2021165234A (ja) * | 2018-07-03 | 2021-10-14 | 富士フイルム富山化学株式会社 | Ｃｘｃｒ４結合性化合物もしくはその塩またはそれらと金属との錯体 |
| EP3956346A4 (en) * | 2019-04-18 | 2023-01-18 | Provincial Health Services Authority | NEW RADIOLABALED DIAGNOSTIC AND THERAPEUTIC COMPOUNDS TARGETING CXCR4 |
| WO2021150258A1 (en) * | 2020-01-26 | 2021-07-29 | Mainline Biosciences Llc | Isotopically labelled selective cxcr4 binding peptide conjugate and methods for making and using the same |
| WO2022082312A1 (en) | 2020-10-21 | 2022-04-28 | Provincial Health Services Authority | Novel cxcr4-targeting compounds |
| EP4321526A4 (en) | 2022-02-11 | 2026-04-15 | C Biomex Co Ltd | Peptide ligand targeting carbonic anhydrase IX, peptide construction comprising it, and associated uses |
| CN114832113B (zh) * | 2022-03-22 | 2023-06-20 | 重庆医科大学 | 疏水药物-马来酰亚胺衍生物及其主动载药脂质体和应用 |
| EP4511384A4 (en) * | 2022-04-20 | 2026-07-29 | Provincial Health Services Authority | Compounds targeting CXCR4, and their manufacturing and use processes |
| CN116023438B (zh) * | 2023-02-06 | 2025-07-11 | 中国药科大学 | 一种cxcr4靶向多肽及其应用 |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2007096662A2 (en) * | 2006-02-27 | 2007-08-30 | Technische Universität München | Cancer imaging and treatment |
| HRP20110551T1 (hr) * | 2007-05-30 | 2011-09-30 | Eli Lilly & Company | Antagonisti cikličkog peptida cxcr4 |
| IT1397901B1 (it) * | 2010-01-26 | 2013-02-04 | Consiglio Nazionale Ricerche | Peptidi ciclici che legano il recettore cxcr4 e relativi usi in campo medico e diagnostico. |
| CN102626522B (zh) * | 2012-04-12 | 2014-09-10 | 韩彦江 | 基于趋化因子受体cxcr4多肽类拮抗剂的多肽放射性诊断与治疗药物 |
| MX355396B (es) * | 2012-06-06 | 2018-04-18 | Polyphor Ag | Peptido - mimeticos de la horquilla beta. |
| US9790286B2 (en) * | 2013-01-02 | 2017-10-17 | Lucia Irene Gonzalez | Stereoisomer peptides, their polymer conjugates, their encapsulation into nanoparticles, and uses thereof for the treatment of diseases caused by abnormal angiogenesis |
| CN106573959B (zh) * | 2014-06-06 | 2022-03-25 | 慕尼黑工业大学 | 修饰的环五肽及其用途 |
-
2018
- 2018-02-17 KR KR1020237034343A patent/KR20230145543A/ko not_active Ceased
- 2018-02-17 JP JP2020504380A patent/JP2020532496A/ja active Pending
- 2018-02-17 CA CA3065086A patent/CA3065086A1/en active Pending
- 2018-02-17 WO PCT/US2018/018530 patent/WO2019050564A1/en not_active Ceased
- 2018-02-17 EP EP18852912.7A patent/EP3679053A4/en not_active Withdrawn
- 2018-02-17 CN CN201880049498.7A patent/CN111183146A/zh active Pending
- 2018-02-17 KR KR1020207000227A patent/KR20200043970A/ko not_active Ceased
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