JPWO2020132655A5 - - Google Patents
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- Publication number
- JPWO2020132655A5 JPWO2020132655A5 JP2021535547A JP2021535547A JPWO2020132655A5 JP WO2020132655 A5 JPWO2020132655 A5 JP WO2020132655A5 JP 2021535547 A JP2021535547 A JP 2021535547A JP 2021535547 A JP2021535547 A JP 2021535547A JP WO2020132655 A5 JPWO2020132655 A5 JP WO2020132655A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- antibody
- adc
- mla
- tmc1
- 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
- 150000001875 compounds Chemical class 0.000 claims description 49
- 125000005647 linker group Chemical group 0.000 claims description 46
- 229940079593 drug Drugs 0.000 claims description 40
- 239000003814 drug Substances 0.000 claims description 40
- 101000801040 Homo sapiens Transmembrane channel-like protein 1 Proteins 0.000 claims description 34
- 102100033690 Transmembrane channel-like protein 1 Human genes 0.000 claims description 34
- 101000638069 Homo sapiens Transmembrane channel-like protein 2 Proteins 0.000 claims description 30
- 102100032054 Transmembrane channel-like protein 2 Human genes 0.000 claims description 30
- 125000004434 sulfur atom Chemical group 0.000 claims description 28
- 150000003573 thiols Chemical class 0.000 claims description 26
- 125000000151 cysteine group Chemical group N[C@@H](CS)C(=O)* 0.000 claims description 22
- 229910052717 sulfur Inorganic materials 0.000 claims description 20
- 229920001223 polyethylene glycol Polymers 0.000 claims description 14
- 125000006242 amine protecting group Chemical group 0.000 claims description 12
- 238000005698 Diels-Alder reaction Methods 0.000 claims description 10
- 238000006352 cycloaddition reaction Methods 0.000 claims description 10
- KZNICNPSHKQLFF-UHFFFAOYSA-N succinimide Chemical group O=C1CCC(=O)N1 KZNICNPSHKQLFF-UHFFFAOYSA-N 0.000 claims description 10
- 125000000524 functional group Chemical group 0.000 claims description 9
- 239000002202 Polyethylene glycol Substances 0.000 claims description 8
- 235000001014 amino acid Nutrition 0.000 claims description 6
- 150000001413 amino acids Chemical class 0.000 claims description 6
- 229940127089 cytotoxic agent Drugs 0.000 claims description 6
- -1 PEG6 Chemical compound 0.000 claims description 4
- NINIDFKCEFEMDL-UHFFFAOYSA-N Sulfur Chemical compound [S] NINIDFKCEFEMDL-UHFFFAOYSA-N 0.000 claims description 4
- 230000000340 anti-metabolite Effects 0.000 claims description 4
- 229940049595 antibody-drug conjugate Drugs 0.000 claims description 4
- 229940100197 antimetabolite Drugs 0.000 claims description 4
- 239000002256 antimetabolite Substances 0.000 claims description 4
- 239000002246 antineoplastic agent Substances 0.000 claims description 4
- UCMIRNVEIXFBKS-UHFFFAOYSA-N beta-alanine Chemical group NCCC(O)=O UCMIRNVEIXFBKS-UHFFFAOYSA-N 0.000 claims description 4
- 230000000973 chemotherapeutic effect Effects 0.000 claims description 4
- 229960002173 citrulline Drugs 0.000 claims description 4
- 125000002228 disulfide group Chemical group 0.000 claims description 4
- 125000003827 glycol group Chemical group 0.000 claims description 4
- 230000002209 hydrophobic effect Effects 0.000 claims description 4
- 239000002777 nucleoside Substances 0.000 claims description 4
- 150000003833 nucleoside derivatives Chemical class 0.000 claims description 4
- 239000011593 sulfur Substances 0.000 claims description 4
- 125000001399 1,2,3-triazolyl group Chemical group N1N=NC(=C1)* 0.000 claims description 2
- KXSKAZFMTGADIV-UHFFFAOYSA-N 2-[3-(2-hydroxyethoxy)propoxy]ethanol Chemical compound OCCOCCCOCCO KXSKAZFMTGADIV-UHFFFAOYSA-N 0.000 claims description 2
- DJQYYYCQOZMCRC-UHFFFAOYSA-N 2-aminopropane-1,3-dithiol Chemical compound SCC(N)CS DJQYYYCQOZMCRC-UHFFFAOYSA-N 0.000 claims description 2
- BWGNESOTFCXPMA-UHFFFAOYSA-N Dihydrogen disulfide Chemical compound SS BWGNESOTFCXPMA-UHFFFAOYSA-N 0.000 claims description 2
- 108010016626 Dipeptides Proteins 0.000 claims description 2
- 239000004471 Glycine Substances 0.000 claims description 2
- DHMQDGOQFOQNFH-UHFFFAOYSA-N Glycine Natural products NCC(O)=O DHMQDGOQFOQNFH-UHFFFAOYSA-N 0.000 claims description 2
- 101000693243 Homo sapiens Paternally-expressed gene 3 protein Proteins 0.000 claims description 2
- QNAYBMKLOCPYGJ-REOHCLBHSA-N L-alanine Chemical group C[C@H](N)C(O)=O QNAYBMKLOCPYGJ-REOHCLBHSA-N 0.000 claims description 2
- KDXKERNSBIXSRK-YFKPBYRVSA-N L-lysine Chemical group NCCCC[C@H](N)C(O)=O KDXKERNSBIXSRK-YFKPBYRVSA-N 0.000 claims description 2
- 239000004472 Lysine Chemical group 0.000 claims description 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Chemical group NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims description 2
- 102100025757 Paternally-expressed gene 3 protein Human genes 0.000 claims description 2
- 235000004279 alanine Nutrition 0.000 claims description 2
- 150000001345 alkine derivatives Chemical group 0.000 claims description 2
- 125000000539 amino acid group Chemical group 0.000 claims description 2
- 239000000611 antibody drug conjugate Substances 0.000 claims description 2
- 150000001540 azides Chemical class 0.000 claims description 2
- 229940000635 beta-alanine Drugs 0.000 claims description 2
- 239000000562 conjugate Substances 0.000 claims description 2
- 239000002254 cytotoxic agent Substances 0.000 claims description 2
- 231100000599 cytotoxic agent Toxicity 0.000 claims description 2
- 125000003630 glycyl group Chemical group [H]N([H])C([H])([H])C(*)=O 0.000 claims description 2
- 125000002924 primary amino group Chemical group [H]N([H])* 0.000 claims description 2
- 125000006239 protecting group Chemical group 0.000 claims description 2
- 150000003839 salts Chemical class 0.000 claims description 2
- PSVXZQVXSXSQRO-UHFFFAOYSA-N undecaethylene glycol Chemical compound OCCOCCOCCOCCOCCOCCOCCOCCOCCOCCOCCO PSVXZQVXSXSQRO-UHFFFAOYSA-N 0.000 claims description 2
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 125000005439 maleimidyl group Chemical group C1(C=CC(N1*)=O)=O 0.000 description 1
- 238000000034 method Methods 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2024163811A JP2024178320A (ja) | 2018-12-21 | 2024-09-20 | チオール多重リンカーを有するａｄｃ |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862783582P | 2018-12-21 | 2018-12-21 | |
| US201862783707P | 2018-12-21 | 2018-12-21 | |
| US62/783,582 | 2018-12-21 | ||
| US62/783,707 | 2018-12-21 | ||
| PCT/US2019/068178 WO2020132655A1 (en) | 2018-12-21 | 2019-12-20 | Adcs with thiol multiplex linkers |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024163811A Division JP2024178320A (ja) | 2018-12-21 | 2024-09-20 | チオール多重リンカーを有するａｄｃ |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2022514348A JP2022514348A (ja) | 2022-02-10 |
| JPWO2020132655A5 true JPWO2020132655A5 (https=) | 2022-12-20 |
| JP2022514348A5 JP2022514348A5 (https=) | 2022-12-20 |
Family
ID=71101991
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021535547A Ceased JP2022514348A (ja) | 2018-12-21 | 2019-12-20 | チオール多重リンカーを有するａｄｃ |
| JP2024163811A Pending JP2024178320A (ja) | 2018-12-21 | 2024-09-20 | チオール多重リンカーを有するａｄｃ |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2024163811A Pending JP2024178320A (ja) | 2018-12-21 | 2024-09-20 | チオール多重リンカーを有するａｄｃ |
Country Status (12)
| Country | Link |
|---|---|
| US (1) | US20220040320A1 (https=) |
| EP (1) | EP3897734A4 (https=) |
| JP (2) | JP2022514348A (https=) |
| KR (1) | KR20210141918A (https=) |
| CN (1) | CN113543812A (https=) |
| AU (1) | AU2019403552A1 (https=) |
| CA (1) | CA3122316A1 (https=) |
| IL (1) | IL284147A (https=) |
| MX (1) | MX2021007548A (https=) |
| SG (1) | SG11202106122QA (https=) |
| TW (1) | TW202039008A (https=) |
| WO (1) | WO2020132655A1 (https=) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2021207701A1 (en) * | 2020-04-10 | 2021-10-14 | Seagen Inc. | Charge variant linkers |
| CA3254333A1 (en) * | 2022-05-18 | 2025-07-04 | Systimmune, Inc. | Ligand-drug conjugate and use thereof |
| AR132368A1 (es) | 2023-04-18 | 2025-06-18 | Astrazeneca Ab | Conjugados que comprenden enlazadores escindibles |
Family Cites Families (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| ATE234635T1 (de) * | 1995-12-22 | 2003-04-15 | Bristol Myers Squibb Co | Verzweigte hydrazongruppen enthaltende kuppler |
| JP2001505194A (ja) * | 1996-11-05 | 2001-04-17 | ブリストル―マイヤーズ・スクイブ・カンパニー | 分枝ペプチド・リンカー |
| DE10048417A1 (de) * | 2000-09-29 | 2002-04-11 | Roche Diagnostics Gmbh | Verbindungen mit verzweigtem Linker |
| US6821529B2 (en) * | 2001-09-05 | 2004-11-23 | Deanna Jean Nelson | Oligo(ethylene glycoll)-terminated 1,2-dithiolanes and their conjugates useful for preparing self-assembled monolayers |
| KR100889587B1 (ko) * | 2006-05-12 | 2009-03-19 | 한국생명공학연구원 | 기질표면 처리 및 특이적 단백질 고정용 링커분자, 및 그제조방법 |
| US9056129B2 (en) * | 2007-02-09 | 2015-06-16 | Northeastern University | Precision-guided nanoparticle systems for drug delivery |
| US20130195799A1 (en) * | 2010-08-19 | 2013-08-01 | Peg Biosciences, Inc. | Synergistic biomolecule-polymer conjugates |
| EP3842074A1 (en) * | 2010-09-29 | 2021-06-30 | Philogen S.p.A. | Protein-drug conjugates |
| US9981046B2 (en) * | 2012-05-15 | 2018-05-29 | Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. | Drug-conjugates, conjugation methods, and uses thereof |
| KR102557309B1 (ko) * | 2012-05-15 | 2023-07-20 | 씨젠 인크. | 자가-안정화 링커 접합체 |
| PL2872157T3 (pl) * | 2012-07-12 | 2020-07-13 | Hangzhou Dac Biotech Co., Ltd | Koniugaty wiążących komórkę cząsteczek ze środkami cytotoksycznymi |
| AU2014312215B2 (en) * | 2013-08-28 | 2020-02-27 | Abbvie Stemcentrx Llc | Site-specific antibody conjugation methods and compositions |
| TW201511774A (zh) * | 2013-09-18 | 2015-04-01 | Iner Aec Executive Yuan | 放射性標誌之主動標靶性醫藥組合物及其用途 |
| ES2826398T3 (es) * | 2013-10-15 | 2021-05-18 | Seagen Inc | Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco |
| WO2016025752A1 (en) * | 2014-08-14 | 2016-02-18 | Prolynx Llc | Reagents for thiol conjugation and conjugates formed therefrom |
| US11135307B2 (en) * | 2016-11-23 | 2021-10-05 | Mersana Therapeutics, Inc. | Peptide-containing linkers for antibody-drug conjugates |
| WO2021207701A1 (en) * | 2020-04-10 | 2021-10-14 | Seagen Inc. | Charge variant linkers |
-
2019
- 2019-12-20 EP EP19900437.5A patent/EP3897734A4/en not_active Withdrawn
- 2019-12-20 AU AU2019403552A patent/AU2019403552A1/en not_active Abandoned
- 2019-12-20 US US17/311,508 patent/US20220040320A1/en not_active Abandoned
- 2019-12-20 KR KR1020217022058A patent/KR20210141918A/ko not_active Abandoned
- 2019-12-20 WO PCT/US2019/068178 patent/WO2020132655A1/en not_active Ceased
- 2019-12-20 MX MX2021007548A patent/MX2021007548A/es unknown
- 2019-12-20 JP JP2021535547A patent/JP2022514348A/ja not_active Ceased
- 2019-12-20 CA CA3122316A patent/CA3122316A1/en active Pending
- 2019-12-20 SG SG11202106122QA patent/SG11202106122QA/en unknown
- 2019-12-20 CN CN201980085333.XA patent/CN113543812A/zh active Pending
- 2019-12-23 TW TW108147276A patent/TW202039008A/zh unknown
-
2021
- 2021-06-17 IL IL284147A patent/IL284147A/en unknown
-
2024
- 2024-09-20 JP JP2024163811A patent/JP2024178320A/ja active Pending
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