JPWO2021028686A5 - - Google Patents
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- JPWO2021028686A5 JPWO2021028686A5 JP2022508564A JP2022508564A JPWO2021028686A5 JP WO2021028686 A5 JPWO2021028686 A5 JP WO2021028686A5 JP 2022508564 A JP2022508564 A JP 2022508564A JP 2022508564 A JP2022508564 A JP 2022508564A JP WO2021028686 A5 JPWO2021028686 A5 JP WO2021028686A5
- Authority
- JP
- Japan
- Prior art keywords
- binding complex
- multimeric binding
- seq
- conh2
- attachment
- 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
- YBJHBAHKTGYVGT-ZKWXMUAHSA-N (+)-Biotin Chemical compound N1C(=O)N[C@@H]2[C@H](CCCCC(=O)O)SC[C@@H]21 YBJHBAHKTGYVGT-ZKWXMUAHSA-N 0.000 claims description 6
- 229960002685 biotin Drugs 0.000 claims description 3
- 235000020958 biotin Nutrition 0.000 claims description 3
- 239000011616 biotin Substances 0.000 claims description 3
- 108090000765 processed proteins & peptides Proteins 0.000 claims 15
- 239000003446 ligand Substances 0.000 claims 12
- 239000003607 modifier Substances 0.000 claims 10
- 125000006850 spacer group Chemical group 0.000 claims 9
- 101000851370 Homo sapiens Tumor necrosis factor receptor superfamily member 9 Proteins 0.000 claims 7
- 125000002619 bicyclic group Chemical group 0.000 claims 7
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims 3
- 229940079593 drug Drugs 0.000 claims 3
- 239000003814 drug Substances 0.000 claims 3
- 239000002062 molecular scaffold Substances 0.000 claims 3
- 229920001184 polypeptide Polymers 0.000 claims 3
- 102000004196 processed proteins & peptides Human genes 0.000 claims 3
- 239000000700 radioactive tracer Substances 0.000 claims 3
- 150000003839 salts Chemical class 0.000 claims 3
- LRQKBLKVPFOOQJ-YFKPBYRVSA-N L-norleucine Chemical compound CCCC[C@H]([NH3+])C([O-])=O LRQKBLKVPFOOQJ-YFKPBYRVSA-N 0.000 claims 2
- 125000003275 alpha amino acid group Chemical group 0.000 claims 2
- 150000001875 compounds Chemical class 0.000 claims 2
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 claims 2
- 150000002632 lipids Chemical class 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- UORVCLMRJXCDCP-UHFFFAOYSA-N propynoic acid Chemical group OC(=O)C#C UORVCLMRJXCDCP-UHFFFAOYSA-N 0.000 claims 2
- MRTPISKDZDHEQI-YFKPBYRVSA-N (2s)-2-(tert-butylamino)propanoic acid Chemical group OC(=O)[C@H](C)NC(C)(C)C MRTPISKDZDHEQI-YFKPBYRVSA-N 0.000 claims 1
- FYBFGAFWCBMEDG-UHFFFAOYSA-N 1-[3,5-di(prop-2-enoyl)-1,3,5-triazinan-1-yl]prop-2-en-1-one Chemical compound C=CC(=O)N1CN(C(=O)C=C)CN(C(=O)C=C)C1 FYBFGAFWCBMEDG-UHFFFAOYSA-N 0.000 claims 1
- PECYZEOJVXMISF-UHFFFAOYSA-N 3-aminoalanine Chemical compound [NH3+]CC(N)C([O-])=O PECYZEOJVXMISF-UHFFFAOYSA-N 0.000 claims 1
- BXRLWGXPSRYJDZ-UHFFFAOYSA-N 3-cyanoalanine Chemical group OC(=O)C(N)CC#N BXRLWGXPSRYJDZ-UHFFFAOYSA-N 0.000 claims 1
- 239000012099 Alexa Fluor family Substances 0.000 claims 1
- OYPRJOBELJOOCE-UHFFFAOYSA-N Calcium Chemical compound [Ca] OYPRJOBELJOOCE-UHFFFAOYSA-N 0.000 claims 1
- 108010055196 EphA2 Receptor Proteins 0.000 claims 1
- 102100030340 Ephrin type-A receptor 2 Human genes 0.000 claims 1
- DGAQECJNVWCQMB-PUAWFVPOSA-M Ilexoside XXIX Chemical compound C[C@@H]1CC[C@@]2(CC[C@@]3(C(=CC[C@H]4[C@]3(CC[C@@H]5[C@@]4(CC[C@@H](C5(C)C)OS(=O)(=O)[O-])C)C)[C@@H]2[C@]1(C)O)C)C(=O)O[C@H]6[C@@H]([C@H]([C@@H]([C@H](O6)CO)O)O)O.[Na+] DGAQECJNVWCQMB-PUAWFVPOSA-M 0.000 claims 1
- DGYHPLMPMRKMPD-UHFFFAOYSA-N L-propargyl glycine Natural products OC(=O)C(N)CC#C DGYHPLMPMRKMPD-UHFFFAOYSA-N 0.000 claims 1
- 102100035486 Nectin-4 Human genes 0.000 claims 1
- 101710043865 Nectin-4 Proteins 0.000 claims 1
- ZLMJMSJWJFRBEC-UHFFFAOYSA-N Potassium Chemical compound [K] ZLMJMSJWJFRBEC-UHFFFAOYSA-N 0.000 claims 1
- 239000002253 acid Substances 0.000 claims 1
- 238000007792 addition Methods 0.000 claims 1
- 235000001014 amino acid Nutrition 0.000 claims 1
- 150000001413 amino acids Chemical class 0.000 claims 1
- 150000003863 ammonium salts Chemical class 0.000 claims 1
- 238000004458 analytical method Methods 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 239000011575 calcium Substances 0.000 claims 1
- 229910052791 calcium Inorganic materials 0.000 claims 1
- 201000010099 disease Diseases 0.000 claims 1
- 208000035475 disorder Diseases 0.000 claims 1
- 239000012636 effector Substances 0.000 claims 1
- GNBHRKFJIUUOQI-UHFFFAOYSA-N fluorescein Chemical compound O1C(=O)C2=CC=CC=C2C21C1=CC=C(O)C=C1OC1=CC(O)=CC=C21 GNBHRKFJIUUOQI-UHFFFAOYSA-N 0.000 claims 1
- 125000000524 functional group Chemical group 0.000 claims 1
- 102000050327 human TNFRSF9 Human genes 0.000 claims 1
- 230000001404 mediated effect Effects 0.000 claims 1
- 125000001312 palmitoyl group Chemical group O=C([*])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 239000011591 potassium Substances 0.000 claims 1
- 229910052700 potassium Inorganic materials 0.000 claims 1
- 230000002265 prevention Effects 0.000 claims 1
- 239000011734 sodium Substances 0.000 claims 1
- 229910052708 sodium Inorganic materials 0.000 claims 1
- 230000001629 suppression Effects 0.000 claims 1
- 239000011541 reaction mixture Substances 0.000 description 2
- JGFZNNIVVJXRND-UHFFFAOYSA-N N,N-Diisopropylethylamine (DIPEA) Chemical compound CCN(C(C)C)C(C)C JGFZNNIVVJXRND-UHFFFAOYSA-N 0.000 description 1
- 229940125904 compound 1 Drugs 0.000 description 1
- 229940125782 compound 2 Drugs 0.000 description 1
- 239000012043 crude product Substances 0.000 description 1
- 238000004895 liquid chromatography mass spectrometry Methods 0.000 description 1
- 239000000203 mixture Substances 0.000 description 1
- 238000002600 positron emission tomography Methods 0.000 description 1
- 238000002953 preparative HPLC Methods 0.000 description 1
- 239000007787 solid Substances 0.000 description 1
- 238000006467 substitution reaction Methods 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201962885947P | 2019-08-13 | 2019-08-13 | |
| US62/885,947 | 2019-08-13 | ||
| GBPCT/GB2020/051831 | 2020-07-30 | ||
| PCT/GB2020/051831 WO2021019246A1 (en) | 2019-07-30 | 2020-07-30 | Heterotandem bicyclic peptide complexes |
| PCT/GB2020/051923 WO2021028686A1 (en) | 2019-08-13 | 2020-08-13 | Modified multimeric bicyclic peptide ligands |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022544246A JP2022544246A (ja) | 2022-10-17 |
| JPWO2021028686A5 true JPWO2021028686A5 (https=) | 2023-08-25 |
| JP2022544246A5 JP2022544246A5 (https=) | 2023-08-25 |
Family
ID=74570355
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022508564A Pending JP2022544246A (ja) | 2019-08-13 | 2020-08-13 | 修飾された多量体二環式ペプチドリガンド |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US20220275053A1 (https=) |
| EP (1) | EP4013501A1 (https=) |
| JP (1) | JP2022544246A (https=) |
| CN (1) | CN114787197A (https=) |
| WO (1) | WO2021028686A1 (https=) |
Families Citing this family (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP6882978B2 (ja) | 2014-10-29 | 2021-06-02 | バイスクルアールディー・リミテッド | Ｍｔ１−ｍｍｐに特異的な二環性ペプチドリガンド |
| JP7301757B2 (ja) | 2017-06-26 | 2023-07-03 | バイスクルアールディー・リミテッド | 検出可能部分を持つ二環式ペプチドリガンドおよびその使用 |
| CN111183147B (zh) | 2017-08-04 | 2024-07-05 | 拜斯科技术开发有限公司 | Cd137特异性的双环肽配体 |
| TWI825046B (zh) | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
| JP2021514953A (ja) | 2018-02-23 | 2021-06-17 | バイスクルテクス・リミテッド | 多量体二環式ペプチドリガンド |
| IL279489B2 (en) | 2018-06-22 | 2025-10-01 | Bicycletx Ltd | Bicyclic peptide ligands specific for nectin-4, a drug conjugate containing the peptide ligands and a pharmaceutical composition containing the drug conjugate |
| GB201820295D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for MT1-MMP |
| GB201820288D0 (en) | 2018-12-13 | 2019-01-30 | Bicycle Tx Ltd | Bicycle peptide ligaands specific for MT1-MMP |
| GB201820325D0 (en) | 2018-12-13 | 2019-01-30 | Bicyclerd Ltd | Bicyclic peptide ligands specific for psma |
| US12551567B2 (en) | 2018-12-21 | 2026-02-17 | Bicyclerd Limited | Bicyclic peptide ligands specific for PD-L1 |
| JP2022514618A (ja) | 2018-12-21 | 2022-02-14 | バイスクルテクス・リミテッド | Ｐｄ－ｌ１に特異的な二環式ペプチドリガンド |
| GB201900529D0 (en) | 2019-01-15 | 2019-03-06 | Bicycletx Ltd | Bicyclic peptide ligands specific for CD38 |
| TWI860386B (zh) | 2019-07-30 | 2024-11-01 | 英商拜西可泰克斯有限公司 | 異質雙環肽複合物 |
| ES3033517T3 (en) * | 2019-10-03 | 2025-08-05 | Bicycletx Ltd | Heterotandem bicyclic peptide complexes |
| IL300248A (en) | 2020-08-03 | 2023-03-01 | Bicycletx Ltd | peptide-based linkers |
| GB202016331D0 (en) * | 2020-10-15 | 2020-12-02 | Bicyclerd Ltd | Bicyclic peptide ligand drug conjugates |
| US20250186539A2 (en) * | 2021-01-11 | 2025-06-12 | Bicycletx Limited | Methods for treating cancer |
| EP4308586A1 (en) * | 2021-03-19 | 2024-01-24 | BicycleTX Limited | Bicyclic peptide ligands specific for trem2 |
| MX2024003876A (es) | 2021-09-29 | 2024-04-19 | Conjustar Zhuhai Biologics Co Ltd | Conjugado farmaco-polipeptido triciclico y sus aplicaciones. |
| CN114133434B (zh) * | 2021-12-01 | 2022-11-15 | 北京大学第一医院 | 靶向Nectin-4的双环肽核素配体与探针 |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1452868A2 (en) | 2003-02-27 | 2004-09-01 | Pepscan Systems B.V. | Method for selecting a candidate drug compound |
| DK1844337T3 (da) | 2005-01-24 | 2013-09-30 | Pepscan Systems Bv | Bindingsforbindelser, immunogene forbindelser og peptidmimetika |
| JP4030067B2 (ja) * | 2005-03-22 | 2008-01-09 | ロート製薬株式会社 | 新規ペプチド |
| AU2009211253B2 (en) | 2008-02-05 | 2014-11-06 | Bicyclerd Limited | Methods and compositions |
| EP3181146A1 (en) * | 2015-12-16 | 2017-06-21 | Ruprecht-Karls-Universität Heidelberg | Cyclic ntcp-targeting peptides and their uses as entry inhibitors |
| TWI825046B (zh) * | 2017-12-19 | 2023-12-11 | 英商拜西可泰克斯有限公司 | Epha2特用之雙環胜肽配位基 |
| JP2021514953A (ja) * | 2018-02-23 | 2021-06-17 | バイスクルテクス・リミテッド | 多量体二環式ペプチドリガンド |
| JP7551500B2 (ja) * | 2018-04-04 | 2024-09-17 | バイスクルテクス・リミテッド | ヘテロタンデム二環式ペプチド複合体 |
-
2020
- 2020-08-13 WO PCT/GB2020/051923 patent/WO2021028686A1/en not_active Ceased
- 2020-08-13 JP JP2022508564A patent/JP2022544246A/ja active Pending
- 2020-08-13 EP EP20757655.4A patent/EP4013501A1/en not_active Withdrawn
- 2020-08-13 US US17/630,754 patent/US20220275053A1/en active Pending
- 2020-08-13 CN CN202080064375.8A patent/CN114787197A/zh active Pending
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