JP2018058822A - ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 - Google Patents
ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 Download PDFInfo
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- JP2018058822A JP2018058822A JP2017147506A JP2017147506A JP2018058822A JP 2018058822 A JP2018058822 A JP 2018058822A JP 2017147506 A JP2017147506 A JP 2017147506A JP 2017147506 A JP2017147506 A JP 2017147506A JP 2018058822 A JP2018058822 A JP 2018058822A
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- cancer
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- 0 CC1=S*N=C1 Chemical compound CC1=S*N=C1 0.000 description 15
- YQHWKNRGTQXVEC-UHFFFAOYSA-N CC(C)/C(/C1CCCCC1)=[O]\C Chemical compound CC(C)/C(/C1CCCCC1)=[O]\C YQHWKNRGTQXVEC-UHFFFAOYSA-N 0.000 description 1
- SPLYUVSOZYIHFB-SSDOTTSWSA-N CC(C)[C@@H](C)NC(C(C)(C)N)=O Chemical compound CC(C)[C@@H](C)NC(C(C)(C)N)=O SPLYUVSOZYIHFB-SSDOTTSWSA-N 0.000 description 1
- LNADHOIWAYQWPG-UHFFFAOYSA-N CS(c(nc1)ncc1C(O)=O)(=O)=O Chemical compound CS(c(nc1)ncc1C(O)=O)(=O)=O LNADHOIWAYQWPG-UHFFFAOYSA-N 0.000 description 1
- MVKKBCWXFIIUMT-XLDIYJRPSA-N C[C@]1(C(CCNCN)C1)C(Nc1ccc(COC(Oc(cc2)ccc2[N+]([O-])=O)=O)cc1)=O Chemical compound C[C@]1(C(CCNCN)C1)C(Nc1ccc(COC(Oc(cc2)ccc2[N+]([O-])=O)=O)cc1)=O MVKKBCWXFIIUMT-XLDIYJRPSA-N 0.000 description 1
- HFIYAQAMRNTEQI-LBPRGKRZSA-N Cc1ccc(C[C@@H](c2ncc[s]2)NC=O)cc1 Chemical compound Cc1ccc(C[C@@H](c2ncc[s]2)NC=O)cc1 HFIYAQAMRNTEQI-LBPRGKRZSA-N 0.000 description 1
- ACBQROXDOHKANW-UHFFFAOYSA-N [O-][N+](c(cc1)ccc1OC(Oc(cc1)ccc1[N+]([O-])=O)=O)=O Chemical compound [O-][N+](c(cc1)ccc1OC(Oc(cc1)ccc1[N+]([O-])=O)=O)=O ACBQROXDOHKANW-UHFFFAOYSA-N 0.000 description 1
- CZPWVGJYEJSRLH-UHFFFAOYSA-N c1cncnc1 Chemical compound c1cncnc1 CZPWVGJYEJSRLH-UHFFFAOYSA-N 0.000 description 1
- KYQCOXFCLRTKLS-UHFFFAOYSA-N c1nccnc1 Chemical compound c1nccnc1 KYQCOXFCLRTKLS-UHFFFAOYSA-N 0.000 description 1
Classifications
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- A61K47/6889—Conjugates wherein the antibody being the modifying agent and wherein the linker, binder or spacer confers particular properties to the conjugates, e.g. peptidic enzyme-labile linkers or acid-labile linkers, providing for an acid-labile immuno conjugate wherein the drug may be released from its antibody conjugated part in an acidic, e.g. tumoural or environment
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- Pharmacology & Pharmacy (AREA)
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- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Priority Applications (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2022102984A JP7555998B2 (ja) | 2016-08-03 | 2022-06-27 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
| JP2024157625A JP2024174998A (ja) | 2016-08-03 | 2024-09-11 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
Applications Claiming Priority (4)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662370270P | 2016-08-03 | 2016-08-03 | |
| US62/370,270 | 2016-08-03 | ||
| US201762530554P | 2017-07-10 | 2017-07-10 | |
| US62/530,554 | 2017-07-10 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022102984A Division JP7555998B2 (ja) | 2016-08-03 | 2022-06-27 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
Publications (2)
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| JP2018058822A true JP2018058822A (ja) | 2018-04-12 |
| JP2018058822A5 JP2018058822A5 (enExample) | 2020-08-13 |
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Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
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| JP2017147506A Withdrawn JP2018058822A (ja) | 2016-08-03 | 2017-07-31 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
| JP2022102984A Active JP7555998B2 (ja) | 2016-08-03 | 2022-06-27 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
| JP2024157625A Withdrawn JP2024174998A (ja) | 2016-08-03 | 2024-09-11 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2022102984A Active JP7555998B2 (ja) | 2016-08-03 | 2022-06-27 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
| JP2024157625A Withdrawn JP2024174998A (ja) | 2016-08-03 | 2024-09-11 | ヘテロアリールスルホンをベースとするコンジュゲーションハンドル、これらの調製のための方法、および抗体薬物コンジュゲートの合成におけるこれらの使用 |
Country Status (5)
| Country | Link |
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| US (1) | US11712480B2 (enExample) |
| EP (1) | EP3493853A1 (enExample) |
| JP (3) | JP2018058822A (enExample) |
| CA (1) | CA3032559C (enExample) |
| WO (1) | WO2018025168A1 (enExample) |
Cited By (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023068325A1 (ja) * | 2021-10-20 | 2023-04-27 | 国立研究開発法人産業技術総合研究所 | 抗ガン剤、抗ガン剤のプロドラッグ、体外でガン細胞を死滅させる方法、ガンの治療方法、及びガンの治療装置 |
Families Citing this family (10)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JP2015502397A (ja) | 2011-12-23 | 2015-01-22 | ファイザー・インク | 部位特異的コンジュゲーションのための操作された抗体定常領域、ならびにそのための方法および使用 |
| US11364303B2 (en) | 2017-09-29 | 2022-06-21 | Pfizer Inc. | Cysteine engineered antibody drug conjugates |
| EP4667495A3 (en) * | 2017-12-15 | 2026-03-11 | Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. | Bioactive molecule conjugate, preparation method and use thereof |
| TW202317205A (zh) * | 2021-06-29 | 2023-05-01 | 美國公爵大學 | 用於癌症治療之經放射性標記之parp抑制劑結合物 |
| AU2022380909A1 (en) * | 2021-11-03 | 2024-06-06 | Adcentrx Therapeutics Inc. | Drug conjugates and methods of preparing and using the same |
| US20240207425A1 (en) | 2022-12-14 | 2024-06-27 | Merck Sharp & Dohme Llc | Auristatin linker-payloads, pharmaceutical compositions, and uses thereof |
| CN120957753A (zh) * | 2023-03-23 | 2025-11-14 | 广州百济神州生物制药有限公司 | 生物活性结合物、其制备方法和其用途 |
| AR133125A1 (es) * | 2023-06-29 | 2025-08-27 | Beigene Switzerland Gmbh | Conjugados bioactivos, método de preparación y uso de estos |
| WO2025002368A1 (en) * | 2023-06-29 | 2025-01-02 | Beigene, Ltd. | Bioactive conjugates, preparation method and use thereof |
| WO2025261478A1 (en) * | 2024-06-21 | 2025-12-26 | Biotheus Inc. | Antibody drug conjugates and applications thereof |
Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014144878A2 (en) * | 2013-03-15 | 2014-09-18 | The Scripps Research Institute | Novel thiol & amino modifying reagents for protein chemistry and methods of use thereof |
Family Cites Families (37)
| 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 |
| US5225530A (en) | 1986-07-16 | 1993-07-06 | Eniricerche S.P.A. | Polypeptide useful for the preparation of antimalarial vaccines and of diagnostic kits for the detection of malarial affections |
| US5530101A (en) | 1988-12-28 | 1996-06-25 | Protein Design Labs, Inc. | Humanized immunoglobulins |
| DE3920358A1 (de) | 1989-06-22 | 1991-01-17 | Behringwerke Ag | Bispezifische und oligospezifische, mono- und oligovalente antikoerperkonstrukte, ihre herstellung und verwendung |
| US5545806A (en) | 1990-08-29 | 1996-08-13 | Genpharm International, Inc. | Ransgenic non-human animals for producing heterologous antibodies |
| US5633425A (en) | 1990-08-29 | 1997-05-27 | Genpharm International, Inc. | Transgenic non-human animals capable of producing heterologous antibodies |
| US5661016A (en) | 1990-08-29 | 1997-08-26 | Genpharm International Inc. | Transgenic non-human animals capable of producing heterologous antibodies of various isotypes |
| ES2108048T3 (es) | 1990-08-29 | 1997-12-16 | Genpharm Int | Produccion y utilizacion de animales inferiores transgenicos capaces de producir anticuerpos heterologos. |
| US5625126A (en) | 1990-08-29 | 1997-04-29 | Genpharm International, Inc. | Transgenic non-human animals for producing heterologous antibodies |
| JPH07501451A (ja) | 1991-11-25 | 1995-02-16 | エンゾン・インコーポレイテッド | 多価抗原結合タンパク質 |
| US6214345B1 (en) | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
| US5773001A (en) | 1994-06-03 | 1998-06-30 | American Cyanamid Company | Conjugates of methyltrithio antitumor agents and intermediates for their synthesis |
| AU728657B2 (en) | 1996-03-18 | 2001-01-18 | Board Of Regents, The University Of Texas System | Immunoglobulin-like domains with increased half-lives |
| US20050287596A9 (en) * | 1998-06-26 | 2005-12-29 | Braisted Andrew C | Novel ligands and libraries of ligands |
| RU2402548C2 (ru) | 2004-05-19 | 2010-10-27 | Медарекс, Инк. | Химические линкеры и их конъюгаты |
| JP2005330229A (ja) * | 2004-05-20 | 2005-12-02 | Ube Ind Ltd | 4−トリフルオロメトキシフェニル(オキシ)エチルアミン誘導体及び抗菌剤 |
| DK1912671T3 (da) | 2005-07-18 | 2017-11-27 | Seattle Genetics Inc | Beta-glucuronid-linker-lægemiddelkonjugater |
| EP2942346B1 (en) | 2009-02-17 | 2020-05-06 | Syntrix Biosystems, Inc. | Pyridinecarboxamides as cxcr2 modulators |
| CA2813411C (en) | 2010-11-05 | 2016-08-02 | Rinat Neuroscience Corporation | Engineered polypeptide conjugates and methods for making thereof using transglutaminase |
| CA2851155C (en) | 2011-10-14 | 2021-02-23 | Ambit Biosciences Corporation | Heterocyclic compounds and methods of use thereof |
| AR088693A1 (es) | 2011-11-11 | 2014-06-25 | Rinat Neuroscience Corp | Anticuerpos especificos para trop-2 y sus usos |
| CN104185477B (zh) | 2011-11-17 | 2017-05-24 | 辉瑞公司 | 细胞毒性肽及其抗体‑药物缀合物 |
| JP2015502397A (ja) | 2011-12-23 | 2015-01-22 | ファイザー・インク | 部位特異的コンジュゲーションのための操作された抗体定常領域、ならびにそのための方法および使用 |
| CA2890569C (en) | 2012-11-05 | 2019-03-05 | Pfizer Inc. | Spliceostatin analogs |
| WO2015015448A2 (en) | 2013-07-31 | 2015-02-05 | Rinat Neuroscience Corp. | Engineered polypeptide conjugates |
| KR101871088B1 (ko) | 2014-01-27 | 2018-06-25 | 화이자 인코포레이티드 | 이관능성 세포독성제 |
| US11602525B2 (en) | 2014-04-25 | 2023-03-14 | Rinat Neuroscience Corp. | Antibody-drug conjugates with high drug loading |
| SI3185908T1 (sl) | 2014-08-28 | 2020-08-31 | Pfizer Inc. | Linkerji za modulacijo stabilnosti, ki se uporabljajo s konjugati zdravil s protitelesi |
| BR112017018706B1 (pt) | 2015-03-20 | 2023-01-24 | Pfizer Inc | Agentes citotóxicos bifuncionais contendo o farmacoforo cti, composição farmacêutica e uso dos mesmos |
-
2017
- 2017-07-31 JP JP2017147506A patent/JP2018058822A/ja not_active Withdrawn
- 2017-07-31 WO PCT/IB2017/054675 patent/WO2018025168A1/en not_active Ceased
- 2017-07-31 US US16/321,695 patent/US11712480B2/en active Active
- 2017-07-31 CA CA3032559A patent/CA3032559C/en active Active
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-
2022
- 2022-06-27 JP JP2022102984A patent/JP7555998B2/ja active Active
-
2024
- 2024-09-11 JP JP2024157625A patent/JP2024174998A/ja not_active Withdrawn
Patent Citations (1)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2014144878A2 (en) * | 2013-03-15 | 2014-09-18 | The Scripps Research Institute | Novel thiol & amino modifying reagents for protein chemistry and methods of use thereof |
Non-Patent Citations (2)
| Title |
|---|
| ANGEWANDTE CHEMIE INTERNATIONAL EDITION, vol. 52, no. 48, JPN6021027080, 2013, pages 12592 - 12596, ISSN: 0004560497 * |
| BIOCONJUGATE CHEMISTRY, vol. 25, JPN6021027081, 2014, pages 1402 - 1407, ISSN: 0004560498 * |
Cited By (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2023068325A1 (ja) * | 2021-10-20 | 2023-04-27 | 国立研究開発法人産業技術総合研究所 | 抗ガン剤、抗ガン剤のプロドラッグ、体外でガン細胞を死滅させる方法、ガンの治療方法、及びガンの治療装置 |
| JPWO2023068325A1 (enExample) * | 2021-10-20 | 2023-04-27 | ||
| JP7455316B2 (ja) | 2021-10-20 | 2024-03-26 | 国立研究開発法人産業技術総合研究所 | 抗ガン剤、抗ガン剤のプロドラッグ、体外でガン細胞を死滅させる方法、ガンの治療方法、及びガンの治療装置 |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3493853A1 (en) | 2019-06-12 |
| JP2022126826A (ja) | 2022-08-30 |
| US11712480B2 (en) | 2023-08-01 |
| CA3032559A1 (en) | 2018-02-08 |
| WO2018025168A1 (en) | 2018-02-08 |
| JP7555998B2 (ja) | 2024-09-25 |
| JP2024174998A (ja) | 2024-12-17 |
| US20210308276A1 (en) | 2021-10-07 |
| CA3032559C (en) | 2022-04-19 |
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