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 |
|---|---|---|---|---|
| WO2006012527A1 (en) | 2004-07-23 | 2006-02-02 | Endocyte, Inc. | Bivalent linkers and conjugates thereof |
| AU2008224988A1 (en) | 2007-03-14 | 2008-09-18 | Endocyte, Inc. | Binding ligand linked drug delivery conjugates of tubulysins |
| US9877965B2 (en) | 2007-06-25 | 2018-01-30 | Endocyte, Inc. | Vitamin receptor drug delivery conjugates for treating inflammation |
| RU2523909C2 (ru) | 2007-06-25 | 2014-07-27 | Эндосайт, Инк. | Конъюгаты, содержащие гидрофильные спейсеры линкеров |
| 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 |
| EP2850059A4 (en) | 2012-05-15 | 2016-06-29 | Concortis Biosystems Corp | CONJUGATES OF MEDICATION, METHODS OF CONJUGATION AND USE THEREOF |
| US10501412B2 (en) | 2012-07-12 | 2019-12-10 | Hangzhou Dac Biotech Co., Ltd. | Conjugates of cell binding molecules with cytotoxic agents |
| WO2014062697A2 (en) | 2012-10-16 | 2014-04-24 | Endocyte, Inc. | Drug delivery conjugates containing unnatural amino acids and methods for using |
| JP6133431B2 (ja) | 2012-11-24 | 2017-05-24 | ハンジョウ ディーエーシー バイオテック シーオー．，エルティディ．Ｈａｎｇｚｈｏｕ Ｄａｃ Ｂｉｏｔｅｃｈ Ｃｏ．，Ｌｔｄ． | 親水性連結体及び薬物分子と細胞結合分子との共役反応における親水性連結体の使用 |
| 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 |
| EP2931316B1 (en) | 2012-12-12 | 2019-02-20 | Mersana Therapeutics, Inc. | Hydroxyl-polymer-drug-protein conjugates |
| KR102215954B1 (ko) | 2013-02-14 | 2021-02-15 | 브리스톨-마이어스 스큅 컴퍼니 | 튜부리신 화합물, 그의 제조 및 사용 방법 |
| 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 |
| EP3756663A1 (en) | 2013-10-15 | 2020-12-30 | Seagen Inc. | Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics |
| EP3057610B1 (en) | 2013-10-15 | 2021-09-22 | Sorrento Therapeutics, Inc. | Drug-conjugates with a targeting molecule and two different drugs |
| CA2938919C (en) | 2014-02-28 | 2020-12-29 | Hangzhou Dac Biotech Co., Ltd | Charged linkers and their uses for conjugation |
| 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 |
| US10808007B2 (en) * | 2015-02-25 | 2020-10-20 | William Marsh Rice University | Desacetoxytubulysin H and analogs thereof |
| 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 |
| MX2018006218A (es) | 2015-12-04 | 2018-09-05 | Seattle Genetics Inc | Conjugados de compuestos de tubulisina cuaternizada. |
| EA201892040A1 (ru) | 2016-03-25 | 2019-04-30 | Сиэтл Дженетикс, Инк. | Способ получения пегилированных соединений лекарственный препарат - линкер и их промежуточных соединений |
| MX2019005583A (es) | 2016-11-14 | 2019-10-21 | Hangzhou Dac Biotech Co Ltd | Vinculantes de conjugacion, conjugados de molecula de union a celulas que contienen los vinculantes, metodos de creacion y usos de dichos conjugados con los vinculantes. |
| MX2019010769A (es) | 2017-03-24 | 2019-12-11 | Seattle Genetics Inc | Proceso para la preparacion de enlazadores de farmacos de glucuronidos y compuestos intermediarios de los mismos. |
| 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 |
| WO2020132658A2 (en) | 2018-12-21 | 2020-06-25 | Regeneron Pharmaceuticals, Inc. | Tubulysins and protein-tubulysin conjugates |
| US20230025327A1 (en) | 2019-06-29 | 2023-01-26 | Hangzhou Dac Biotech Co., Ltd. | 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 |
| CN117980327A (zh) | 2021-11-03 | 2024-05-03 | 杭州多禧生物科技有限公司 | 抗体的特异性偶联 |
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 |
| WO2008106080A2 (en) * | 2007-02-27 | 2008-09-04 | University Of Pittsburgh - Of The Commonwealth System Of Higher Education | Synthesis of desacetoxytubulysin h and analogs thereof |
-
2008
- 2008-09-25 EP EP08165147A patent/EP2174947A1/en not_active Withdrawn
-
2009
- 2009-09-22 JP JP2011528309A patent/JP2012503621A/ja active Pending
- 2009-09-22 CA CA2738091A patent/CA2738091A1/en not_active Abandoned
- 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 EP EP09783296A patent/EP2331559A1/en not_active Withdrawn