JP2012503621A5 - - Google Patents
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- Publication number
- JP2012503621A5 JP2012503621A5 JP2011528309A JP2011528309A JP2012503621A5 JP 2012503621 A5 JP2012503621 A5 JP 2012503621A5 JP 2011528309 A JP2011528309 A JP 2011528309A JP 2011528309 A JP2011528309 A JP 2011528309A JP 2012503621 A5 JP2012503621 A5 JP 2012503621A5
- Authority
- JP
- Japan
- Prior art keywords
- group
- allyl
- halogen
- compound according
- alkoxy
- 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
- 125000001997 phenyl group Chemical group [H]C1=C([H])C([H])=C(*)C([H])=C1[H] 0.000 claims 9
- 150000001875 compounds Chemical class 0.000 claims 7
- 125000000217 alkyl group Chemical group 0.000 claims 5
- 229910052736 halogen Inorganic materials 0.000 claims 5
- 150000002367 halogens Chemical class 0.000 claims 5
- PEDCQBHIVMGVHV-UHFFFAOYSA-N Glycerol Natural products OCC(O)CO PEDCQBHIVMGVHV-UHFFFAOYSA-N 0.000 claims 4
- 125000003545 alkoxy group Chemical group 0.000 claims 4
- 239000003814 drug Substances 0.000 claims 4
- 125000001424 substituent group Chemical group 0.000 claims 4
- 125000003903 2-propenyl group Chemical group [H]C([*])([H])C([H])=C([H])[H] 0.000 claims 3
- -1 alkylene diol Chemical class 0.000 claims 3
- 125000001797 benzyl group Chemical group [H]C1=C([H])C([H])=C(C([H])=C1[H])C([H])([H])* 0.000 claims 3
- 125000000951 phenoxy group Chemical group [H]C1=C([H])C([H])=C(O*)C([H])=C1[H] 0.000 claims 3
- 229920006395 saturated elastomer Polymers 0.000 claims 3
- 206010028980 Neoplasm Diseases 0.000 claims 2
- 201000011510 cancer Diseases 0.000 claims 2
- 150000002148 esters Chemical class 0.000 claims 2
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 claims 2
- 238000004519 manufacturing process Methods 0.000 claims 2
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims 2
- 125000001624 naphthyl group Chemical group 0.000 claims 2
- 239000008194 pharmaceutical composition Substances 0.000 claims 2
- LFQSCWFLJHTTHZ-UHFFFAOYSA-N Ethanol Chemical compound CCO LFQSCWFLJHTTHZ-UHFFFAOYSA-N 0.000 claims 1
- COLNVLDHVKWLRT-QMMMGPOBSA-N L-phenylalanine Chemical compound OC(=O)[C@@H](N)CC1=CC=CC=C1 COLNVLDHVKWLRT-QMMMGPOBSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-BYPYZUCNSA-N L-valine Chemical compound CC(C)[C@H](N)C(O)=O KZSNJWFQEVHDMF-BYPYZUCNSA-N 0.000 claims 1
- KZSNJWFQEVHDMF-UHFFFAOYSA-N Valine Natural products CC(C)C(N)C(O)=O KZSNJWFQEVHDMF-UHFFFAOYSA-N 0.000 claims 1
- 125000003342 alkenyl group Chemical group 0.000 claims 1
- 239000003080 antimitotic agent Substances 0.000 claims 1
- 230000006907 apoptotic process Effects 0.000 claims 1
- 210000004899 c-terminal region Anatomy 0.000 claims 1
- 125000003178 carboxy group Chemical group [H]OC(*)=O 0.000 claims 1
- 230000001939 inductive effect Effects 0.000 claims 1
- COLNVLDHVKWLRT-UHFFFAOYSA-N phenylalanine Natural products OC(=O)C(N)CC1=CC=CC=C1 COLNVLDHVKWLRT-UHFFFAOYSA-N 0.000 claims 1
- 125000001436 propyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])[H] 0.000 claims 1
- 125000006239 protecting group Chemical group 0.000 claims 1
- 150000003839 salts Chemical class 0.000 claims 1
- 150000005846 sugar alcohols Polymers 0.000 claims 1
- 239000004474 valine Substances 0.000 claims 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08165147.3 | 2008-09-25 | ||
| EP08165147A EP2174947A1 (en) | 2008-09-25 | 2008-09-25 | Bioactive pre-tubulysins and use thereof |
| PCT/EP2009/062282 WO2010034724A1 (en) | 2008-09-25 | 2009-09-22 | Bioactive pre-tubulysins and use thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| JP2012503621A JP2012503621A (ja) | 2012-02-09 |
| JP2012503621A5 true JP2012503621A5 (enExample) | 2012-11-08 |
Family
ID=39952267
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011528309A Pending JP2012503621A (ja) | 2008-09-25 | 2009-09-22 | 生物活性プレチューブリシンおよびその使用 |
Country Status (5)
| Country | Link |
|---|---|
| US (1) | US8791098B2 (enExample) |
| EP (2) | EP2174947A1 (enExample) |
| JP (1) | JP2012503621A (enExample) |
| CA (1) | CA2738091A1 (enExample) |
| WO (1) | WO2010034724A1 (enExample) |
Families Citing this family (36)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| EP1789391B1 (en) | 2004-07-23 | 2017-06-28 | Endocyte, Inc. | Bivalent linkers and conjugates thereof |
| CN104127878A (zh) | 2007-03-14 | 2014-11-05 | 恩多塞特公司 | 结合配体连接的微管溶素递药缀合物 |
| WO2009002993A1 (en) | 2007-06-25 | 2008-12-31 | Endocyte, Inc. | Conjugates containing hydrophilic spacer linkers |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| US8394922B2 (en) | 2009-08-03 | 2013-03-12 | Medarex, Inc. | Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof |
| EP2409983A1 (en) | 2010-07-19 | 2012-01-25 | Leibniz-Institut für Pflanzenbiochemie (IPB) | Tubulysin analogues |
| MX2013014583A (es) | 2011-06-10 | 2014-03-31 | Mersana Therapeutics Inc | Conjugados de proteina-polimero-farmaco. |
| US10080805B2 (en) | 2012-02-24 | 2018-09-25 | Purdue Research Foundation | Cholecystokinin B receptor targeting for imaging and therapy |
| US20140080175A1 (en) | 2012-03-29 | 2014-03-20 | Endocyte, Inc. | Processes for preparing tubulysin derivatives and conjugates thereof |
| ES2887208T3 (es) | 2012-05-15 | 2021-12-22 | Concortis Biosystems Corp | Conjugados de fármacos y usos de los mismos |
| PT2872157T (pt) | 2012-07-12 | 2020-04-30 | Hangzhou Dac Biotech Co Ltd | Conjugados de moléculas de ligação celular com agentes citotóxicos |
| KR20150070318A (ko) | 2012-10-16 | 2015-06-24 | 엔도사이트, 인코포레이티드 | 비천연 아미노산을 함유하는 약물 전달 컨쥬게이트 및 사용 방법 |
| AU2012395148B2 (en) | 2012-11-24 | 2016-10-27 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to cell binding molecules |
| JP6334553B2 (ja) | 2012-12-10 | 2018-05-30 | メルサナ セラピューティクス，インコーポレイティド | タンパク質−高分子−薬剤コンジュゲート |
| WO2014093640A1 (en) | 2012-12-12 | 2014-06-19 | Mersana Therapeutics,Inc. | Hydroxy-polmer-drug-protein conjugates |
| MX356698B (es) | 2013-02-14 | 2018-06-11 | Bristol Myers Squibb Co | Compuestos de tubulisina, metodos para obtenerlos y uso. |
| WO2014160360A1 (en) * | 2013-03-14 | 2014-10-02 | Mersana Therapeutics Inc. | Tubulysin compounds and conjugates thereof |
| WO2015057585A1 (en) * | 2013-10-14 | 2015-04-23 | Regents Of The University Of Minnesota | Therapeutic compounds |
| US10836821B2 (en) | 2013-10-15 | 2020-11-17 | Sorrento Therapeutics, Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| CA3187392A1 (en) | 2013-10-15 | 2015-04-23 | Seagen Inc. | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| CN106414465B (zh) | 2014-02-28 | 2021-11-16 | 杭州多禧生物科技有限公司 | 带电荷链接体及其在共轭反应上的应用 |
| US10077287B2 (en) | 2014-11-10 | 2018-09-18 | Bristol-Myers Squibb Company | Tubulysin analogs and methods of making and use |
| CA2975383C (en) | 2015-01-28 | 2023-09-12 | Sorrento Therapeutics, Inc. | Antibody drug conjugates comprising dolastatin derivatives |
| CN107529754A (zh) * | 2015-02-25 | 2018-01-02 | 威廉马歇莱思大学 | 去乙酰氧基微管溶素h及其类似物 |
| AU2015242213A1 (en) | 2015-07-12 | 2018-03-08 | Hangzhou Dac Biotech Co., Ltd | Bridge linkers for conjugation of cell-binding molecules |
| US9839687B2 (en) | 2015-07-15 | 2017-12-12 | Suzhou M-Conj Biotech Co., Ltd. | Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule |
| US11793880B2 (en) | 2015-12-04 | 2023-10-24 | Seagen Inc. | Conjugates of quaternized tubulysin compounds |
| SG10202010590UA (en) | 2015-12-04 | 2020-12-30 | Seattle Genetics Inc | Conjugates of quaternized tubulysin compounds |
| US11844839B2 (en) | 2016-03-25 | 2023-12-19 | Seagen Inc. | Process for the preparation of pegylated drug-linkers and intermediates thereof |
| KR20220147720A (ko) | 2016-11-14 | 2022-11-03 | 항저우 디에이씨 바이오테크 씨오, 엘티디 | 결합 링커, 그러한 결합 링커를 함유하는 세포 결합 분자-약물 결합체, 링커를 갖는 그러한 결합체의 제조 및 사용 |
| JP7527787B2 (ja) | 2017-03-24 | 2024-08-05 | シージェン インコーポレイテッド | グルクロニド薬物－リンカーの調製のためのプロセスおよびその中間体 |
| WO2019108685A1 (en) | 2017-11-29 | 2019-06-06 | William March Rice University | Tubulysin analogues as anticancer agents and payloads for antibody-drug conjugates and methods of treatment therewith |
| MA53765B2 (fr) | 2018-12-21 | 2025-04-30 | Regeneron Pharmaceuticals, Inc. | Tubulysines et conjugués tubulysines-protéines |
| CA3145050A1 (en) | 2019-06-29 | 2021-01-07 | Robert Zhao | Conjugates of tubulysin derivatives and cell binding molecules and methods of making |
| CN111647040B (zh) * | 2020-05-11 | 2022-02-22 | 深圳市老年医学研究所 | 一种天然活性多肽Tubulysin U的制备方法 |
| EP4426727A2 (en) | 2021-11-03 | 2024-09-11 | Hangzhou Dac Biotech Co., Ltd. | Specific conjugation of an antibody |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE10254439A1 (de) * | 2002-11-21 | 2004-06-03 | GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) | Tubulysine, Herstellungsverfahren und Tubulysin-Mittel |
| US20100047841A1 (en) * | 2007-02-27 | 2010-02-25 | University Of Pittsburgh-Of The Commonwealth System Of Higher Education | Synthesis of desacetoxytubulysin h and analogs thereof |
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2008
- 2008-09-25 EP EP08165147A patent/EP2174947A1/en not_active Withdrawn
-
2009
- 2009-09-22 EP EP09783296A patent/EP2331559A1/en not_active Withdrawn
- 2009-09-22 WO PCT/EP2009/062282 patent/WO2010034724A1/en not_active Ceased
- 2009-09-22 US US13/120,497 patent/US8791098B2/en not_active Expired - Fee Related
- 2009-09-22 JP JP2011528309A patent/JP2012503621A/ja active Pending
- 2009-09-22 CA CA2738091A patent/CA2738091A1/en not_active Abandoned