JP2023129495A5 - - Google Patents
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- Publication number
- JP2023129495A5 JP2023129495A5 JP2023116253A JP2023116253A JP2023129495A5 JP 2023129495 A5 JP2023129495 A5 JP 2023129495A5 JP 2023116253 A JP2023116253 A JP 2023116253A JP 2023116253 A JP2023116253 A JP 2023116253A JP 2023129495 A5 JP2023129495 A5 JP 2023129495A5
- Authority
- JP
- Japan
- Prior art keywords
- alkyl
- alkylene
- unsubstituted
- substituted
- absent
- 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
- 125000000217 alkyl group Chemical group 0.000 claims 86
- 150000003839 salts Chemical class 0.000 claims 46
- 150000001875 compounds Chemical class 0.000 claims 40
- 125000004432 carbon atom Chemical group C* 0.000 claims 39
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 38
- 125000004452 carbocyclyl group Chemical group 0.000 claims 37
- 229910052739 hydrogen Inorganic materials 0.000 claims 36
- 239000001257 hydrogen Substances 0.000 claims 34
- 150000001408 amides Chemical group 0.000 claims 30
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 28
- UFHFLCQGNIYNRP-UHFFFAOYSA-N Hydrogen Chemical compound [H][H] UFHFLCQGNIYNRP-UHFFFAOYSA-N 0.000 claims 27
- 125000002947 alkylene group Chemical group 0.000 claims 24
- 229910052757 nitrogen Inorganic materials 0.000 claims 24
- 239000003446 ligand Substances 0.000 claims 21
- KXDHJXZQYSOELW-UHFFFAOYSA-N Carbamic acid Chemical group NC(O)=O KXDHJXZQYSOELW-UHFFFAOYSA-N 0.000 claims 19
- 239000003814 drug Substances 0.000 claims 19
- 229940079593 drug Drugs 0.000 claims 19
- 125000006239 protecting group Chemical group 0.000 claims 19
- 125000004433 nitrogen atom Chemical group N* 0.000 claims 17
- 229910052799 carbon Inorganic materials 0.000 claims 16
- 125000003275 alpha amino acid group Chemical group 0.000 claims 13
- 150000001412 amines Chemical class 0.000 claims 13
- -1 auristatin F compound Chemical class 0.000 claims 13
- 125000003998 beta-amino acid group Chemical group 0.000 claims 13
- 239000002253 acid Substances 0.000 claims 12
- 125000001424 substituent group Chemical group 0.000 claims 12
- 235000008206 alpha-amino acids Nutrition 0.000 claims 11
- 125000002843 carboxylic acid group Chemical group 0.000 claims 11
- 230000002209 hydrophobic effect Effects 0.000 claims 11
- 150000003335 secondary amines Chemical class 0.000 claims 10
- 125000005263 alkylenediamine group Chemical group 0.000 claims 9
- IJGRMHOSHXDMSA-UHFFFAOYSA-N Atomic nitrogen Chemical compound N#N IJGRMHOSHXDMSA-UHFFFAOYSA-N 0.000 claims 8
- 108010016626 Dipeptides Proteins 0.000 claims 8
- 125000001449 isopropyl group Chemical group [H]C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 8
- 150000003512 tertiary amines Chemical group 0.000 claims 8
- 210000004899 c-terminal region Anatomy 0.000 claims 7
- 150000002431 hydrogen Chemical class 0.000 claims 7
- 125000002924 primary amino group Chemical class [H]N([H])* 0.000 claims 7
- 125000003118 aryl group Chemical group 0.000 claims 6
- CREXVNNSNOKDHW-UHFFFAOYSA-N azaniumylideneazanide Chemical group N[N] CREXVNNSNOKDHW-UHFFFAOYSA-N 0.000 claims 6
- VILAVOFMIJHSJA-UHFFFAOYSA-N dicarbon monoxide Chemical group [C]=C=O VILAVOFMIJHSJA-UHFFFAOYSA-N 0.000 claims 6
- 108090000765 processed proteins & peptides Proteins 0.000 claims 6
- 125000004434 sulfur atom Chemical group 0.000 claims 5
- 101000629400 Homo sapiens Mesoderm-specific transcript homolog protein Proteins 0.000 claims 4
- 102100026821 Mesoderm-specific transcript homolog protein Human genes 0.000 claims 4
- CKLJMWTZIZZHCS-REOHCLBHSA-N aspartic acid group Chemical group N[C@@H](CC(=O)O)C(=O)O CKLJMWTZIZZHCS-REOHCLBHSA-N 0.000 claims 4
- 125000004429 atom Chemical group 0.000 claims 4
- 125000000291 glutamic acid group Chemical group N[C@@H](CCC(O)=O)C(=O)* 0.000 claims 4
- 125000001072 heteroaryl group Chemical group 0.000 claims 4
- QJGQUHMNIGDVPM-UHFFFAOYSA-N nitrogen group Chemical group [N] QJGQUHMNIGDVPM-UHFFFAOYSA-N 0.000 claims 4
- 229910052717 sulfur Inorganic materials 0.000 claims 4
- WHUUTDBJXJRKMK-UHFFFAOYSA-N Glutamic acid Natural products OC(=O)C(N)CCC(O)=O WHUUTDBJXJRKMK-UHFFFAOYSA-N 0.000 claims 3
- 125000002015 acyclic group Chemical group 0.000 claims 3
- 239000003795 chemical substances by application Substances 0.000 claims 3
- 125000000524 functional group Chemical group 0.000 claims 3
- 235000013922 glutamic acid Nutrition 0.000 claims 3
- 239000004220 glutamic acid Substances 0.000 claims 3
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 3
- 230000008685 targeting Effects 0.000 claims 3
- 125000006479 2-pyridyl methyl group Chemical group [H]C1=C([H])C([H])=C([H])C(=N1)C([H])([H])* 0.000 claims 2
- 125000003143 4-hydroxybenzyl group Chemical group [H]C([*])([H])C1=C([H])C([H])=C(O[H])C([H])=C1[H] 0.000 claims 2
- KDXKERNSBIXSRK-UHFFFAOYSA-N Lysine Natural products NCCCCC(N)C(O)=O KDXKERNSBIXSRK-UHFFFAOYSA-N 0.000 claims 2
- 239000004472 Lysine Substances 0.000 claims 2
- ONIBWKKTOPOVIA-UHFFFAOYSA-N Proline Natural products OC(=O)C1CCCN1 ONIBWKKTOPOVIA-UHFFFAOYSA-N 0.000 claims 2
- DGYIJVNZSDYBOE-UHFFFAOYSA-N [CH2]C1=CC=NC=C1 Chemical group [CH2]C1=CC=NC=C1 DGYIJVNZSDYBOE-UHFFFAOYSA-N 0.000 claims 2
- 150000001370 alpha-amino acid derivatives Chemical class 0.000 claims 2
- 238000010976 amide bond formation reaction Methods 0.000 claims 2
- 239000000427 antigen Substances 0.000 claims 2
- 102000036639 antigens Human genes 0.000 claims 2
- 108091007433 antigens Proteins 0.000 claims 2
- 125000002393 azetidinyl group Chemical group 0.000 claims 2
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 2
- 239000000470 constituent Substances 0.000 claims 2
- 125000000113 cyclohexyl group Chemical group [H]C1([H])C([H])([H])C([H])([H])C([H])(*)C([H])([H])C1([H])[H] 0.000 claims 2
- 125000004427 diamine group Chemical group 0.000 claims 2
- 230000002708 enhancing effect Effects 0.000 claims 2
- 230000007062 hydrolysis Effects 0.000 claims 2
- 238000006460 hydrolysis reaction Methods 0.000 claims 2
- 125000005647 linker group Chemical group 0.000 claims 2
- 125000004108 n-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000000740 n-pentyl group Chemical group [H]C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])* 0.000 claims 2
- 125000003386 piperidinyl group Chemical group 0.000 claims 2
- 125000000719 pyrrolidinyl group Chemical group 0.000 claims 2
- 125000002914 sec-butyl group Chemical group [H]C([H])([H])C([H])([H])C([H])(*)C([H])([H])[H] 0.000 claims 2
- 125000006850 spacer group Chemical group 0.000 claims 2
- 125000000999 tert-butyl group Chemical group [H]C([H])([H])C(*)(C([H])([H])[H])C([H])([H])[H] 0.000 claims 2
- OKTJSMMVPCPJKN-UHFFFAOYSA-N Carbon Chemical compound [C] OKTJSMMVPCPJKN-UHFFFAOYSA-N 0.000 claims 1
- 206010028980 Neoplasm Diseases 0.000 claims 1
- 201000011510 cancer Diseases 0.000 claims 1
- 150000001732 carboxylic acid derivatives Chemical class 0.000 claims 1
- 210000004027 cell Anatomy 0.000 claims 1
- 125000004122 cyclic group Chemical group 0.000 claims 1
- 150000004985 diamines Chemical class 0.000 claims 1
- 238000006073 displacement reaction Methods 0.000 claims 1
- 239000012634 fragment Substances 0.000 claims 1
- 239000012038 nucleophile Substances 0.000 claims 1
- 230000000269 nucleophilic effect Effects 0.000 claims 1
- 239000002243 precursor Substances 0.000 claims 1
- 229920006395 saturated elastomer Polymers 0.000 claims 1
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201862633059P | 2018-02-20 | 2018-02-20 | |
| US62/633,059 | 2018-02-20 | ||
| PCT/US2019/018825 WO2019164987A1 (en) | 2018-02-20 | 2019-02-20 | Hydrophobic auristatin f compounds and conjugates thereof |
| JP2020543847A JP2021513990A (ja) | 2018-02-20 | 2019-02-20 | 疎水性アウリスタチンｆ化合物およびそのコンジュゲート |
Related Parent Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020543847A Division JP2021513990A (ja) | 2018-02-20 | 2019-02-20 | 疎水性アウリスタチンｆ化合物およびそのコンジュゲート |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2023129495A JP2023129495A (ja) | 2023-09-14 |
| JP2023129495A5 true JP2023129495A5 (https=) | 2024-01-31 |
Family
ID=65904522
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020543847A Pending JP2021513990A (ja) | 2018-02-20 | 2019-02-20 | 疎水性アウリスタチンｆ化合物およびそのコンジュゲート |
| JP2023116253A Pending JP2023129495A (ja) | 2018-02-20 | 2023-07-14 | 疎水性アウリスタチンｆ化合物およびそのコンジュゲート |
Family Applications Before (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2020543847A Pending JP2021513990A (ja) | 2018-02-20 | 2019-02-20 | 疎水性アウリスタチンｆ化合物およびそのコンジュゲート |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US11857565B2 (https=) |
| EP (1) | EP3755707A1 (https=) |
| JP (2) | JP2021513990A (https=) |
| KR (1) | KR20200122351A (https=) |
| CN (1) | CN111989339A (https=) |
| AU (1) | AU2019225845B2 (https=) |
| CA (1) | CA3090805A1 (https=) |
| IL (1) | IL276546B2 (https=) |
| MX (1) | MX2020008267A (https=) |
| SG (1) | SG11202007540SA (https=) |
| TW (1) | TWI838358B (https=) |
| WO (1) | WO2019164987A1 (https=) |
Families Citing this family (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AU2022238571A1 (en) | 2021-03-18 | 2023-09-14 | Seagen Inc. | Selective drug release from internalized conjugates of biologically active compounds |
| JP7717832B2 (ja) | 2021-04-10 | 2025-08-04 | ジェンマブ エー／エス | Ｆｏｌｒ１結合剤、そのコンジュゲートおよびこれを使用する方法 |
| WO2022226317A1 (en) | 2021-04-23 | 2022-10-27 | Profoundbio Us Co. | Anti-cd70 antibodies, conjugates thereof and methods of using the same |
| TW202320857A (zh) | 2021-07-06 | 2023-06-01 | 美商普方生物製藥美國公司 | 連接子、藥物連接子及其結合物及其使用方法 |
| MX2024002571A (es) | 2021-09-03 | 2024-03-20 | Toray Industries | Composicion farmaceutica para tratamiento y/o prevencion de cancer. |
| AU2024353316A1 (en) | 2023-09-26 | 2026-03-26 | Genmab A/S | Ptk7 binding agents, conjugates thereof and methods of using the same |
| WO2025149661A1 (en) | 2024-01-10 | 2025-07-17 | Genmab A/S | Slitrk6 binding agents, conjugates thereof and methods of using the same |
| WO2025181219A1 (en) | 2024-02-29 | 2025-09-04 | Genmab A/S | Egfr and c-met bispecific binding agents, conjugates thereof and methods of using the same |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB2036891B (en) | 1978-12-05 | 1983-05-05 | Windsor Smith C | Change speed gear |
| GB8308235D0 (en) | 1983-03-25 | 1983-05-05 | Celltech Ltd | Polypeptides |
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| JPS6147500A (ja) | 1984-08-15 | 1986-03-07 | Res Dev Corp Of Japan | キメラモノクロ−ナル抗体及びその製造法 |
| EP0173494A3 (en) | 1984-08-27 | 1987-11-25 | The Board Of Trustees Of The Leland Stanford Junior University | Chimeric receptors by dna splicing and expression |
| GB8422238D0 (en) | 1984-09-03 | 1984-10-10 | Neuberger M S | Chimeric proteins |
| JPS61134325A (ja) | 1984-12-04 | 1986-06-21 | Teijin Ltd | ハイブリツド抗体遺伝子の発現方法 |
| JPS63501765A (ja) | 1985-11-01 | 1988-07-21 | インタ−ナショナル、ジェネティック、エンジニアリング インコ−ポレ−テッド | 抗体遺伝子のモジュ−ル組立体、それにより産生された抗体及び用途 |
| US5225539A (en) | 1986-03-27 | 1993-07-06 | Medical Research Council | Recombinant altered antibodies and methods of making altered antibodies |
| US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
| JP4046354B2 (ja) | 1996-03-18 | 2008-02-13 | ボード オブ リージェンツ，ザ ユニバーシティ オブ テキサス システム | 増大した半減期を有する免疫グロブリン様ドメイン |
| 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 |
| SI1545613T1 (sl) * | 2002-07-31 | 2011-11-30 | Seattle Genetics Inc | Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni |
| US7498298B2 (en) | 2003-11-06 | 2009-03-03 | Seattle Genetics, Inc. | Monomethylvaline compounds capable of conjugation to ligands |
| JP5171621B2 (ja) | 2005-07-07 | 2013-03-27 | シアトル ジェネティックス， インコーポレイテッド | フェニルアラニン側鎖修飾をｃ末端に有するモノメチルバリン化合物 |
| WO2007086083A1 (en) | 2006-01-24 | 2007-08-02 | Tecnoimage Srl | Supporting frame for covering elements |
| US8257706B2 (en) | 2006-08-25 | 2012-09-04 | Seattle Genetics, Inc. | CD30 binding agents and uses thereof |
| CA2678514A1 (en) | 2007-02-21 | 2008-08-28 | Medarex, Inc. | Chemical linkers with single amino acids and conjugates thereof |
| EP2265283B1 (en) | 2008-03-18 | 2014-09-03 | Seattle Genetics, Inc. | Auristatin drug linker conjugates |
| JP6105481B2 (ja) | 2010-12-06 | 2017-03-29 | シアトル ジェネティクス，インコーポレーテッド | Ｌｉｖ−１に対するヒト化抗体および癌治療のためのその使用 |
| CN104220094A (zh) | 2012-02-17 | 2014-12-17 | 西雅图基因公司 | 针对整联蛋白αvβ6的抗体和使用该抗体治疗癌症 |
| JP6280031B2 (ja) | 2012-03-29 | 2018-02-14 | 中外製薬株式会社 | 抗ｌａｍｐ５抗体およびその利用 |
| 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 |
| US20130309223A1 (en) | 2012-05-18 | 2013-11-21 | Seattle Genetics, Inc. | CD33 Antibodies And Use Of Same To Treat Cancer |
| SG10202001468UA (en) | 2014-02-17 | 2020-04-29 | Seattle Genetics Inc | Hydrophilic antibody-drug conjugates |
-
2019
- 2019-02-20 CN CN201980025734.6A patent/CN111989339A/zh active Pending
- 2019-02-20 US US16/968,749 patent/US11857565B2/en active Active
- 2019-02-20 MX MX2020008267A patent/MX2020008267A/es unknown
- 2019-02-20 KR KR1020207026764A patent/KR20200122351A/ko not_active Ceased
- 2019-02-20 WO PCT/US2019/018825 patent/WO2019164987A1/en not_active Ceased
- 2019-02-20 TW TW108105691A patent/TWI838358B/zh not_active IP Right Cessation
- 2019-02-20 JP JP2020543847A patent/JP2021513990A/ja active Pending
- 2019-02-20 CA CA3090805A patent/CA3090805A1/en active Pending
- 2019-02-20 AU AU2019225845A patent/AU2019225845B2/en not_active Ceased
- 2019-02-20 SG SG11202007540SA patent/SG11202007540SA/en unknown
- 2019-02-20 IL IL276546A patent/IL276546B2/en unknown
- 2019-02-20 EP EP19713233.5A patent/EP3755707A1/en not_active Withdrawn
-
2023
- 2023-07-14 JP JP2023116253A patent/JP2023129495A/ja active Pending
- 2023-11-02 US US18/500,858 patent/US20240216420A1/en not_active Abandoned
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