CN105102455B - 亲水性自消耗连接子及其缀合物 - Google Patents
亲水性自消耗连接子及其缀合物 Download PDFInfo
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- CN105102455B CN105102455B CN201380073519.6A CN201380073519A CN105102455B CN 105102455 B CN105102455 B CN 105102455B CN 201380073519 A CN201380073519 A CN 201380073519A CN 105102455 B CN105102455 B CN 105102455B
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- alkyl
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- connexon
- heterocycle
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- 0 CC(CC(N1*)=O)(CC1=O)SC Chemical compound CC(CC(N1*)=O)(CC1=O)SC 0.000 description 11
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D241/00—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings
- C07D241/36—Heterocyclic compounds containing 1,4-diazine or hydrogenated 1,4-diazine rings condensed with carbocyclic rings or ring systems
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- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
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- A61K31/407—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with other heterocyclic ring systems, e.g. ketorolac, physostigmine
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Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| CN201810460861.6A CN108546283A (zh) | 2012-12-21 | 2013-12-20 | 亲水性自消耗连接子及其缀合物 |
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261745448P | 2012-12-21 | 2012-12-21 | |
| US61/745,448 | 2012-12-21 | ||
| US201361785027P | 2013-03-14 | 2013-03-14 | |
| US61/785,027 | 2013-03-14 | ||
| PCT/US2013/077306 WO2014100762A1 (en) | 2012-12-21 | 2013-12-20 | Hydrophilic self-immolative linkers and conjugates thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810460861.6A Division CN108546283A (zh) | 2012-12-21 | 2013-12-20 | 亲水性自消耗连接子及其缀合物 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN105102455A CN105102455A (zh) | 2015-11-25 |
| CN105102455B true CN105102455B (zh) | 2018-05-25 |
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Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201380073519.6A Expired - Fee Related CN105102455B (zh) | 2012-12-21 | 2013-12-20 | 亲水性自消耗连接子及其缀合物 |
| CN201810460861.6A Pending CN108546283A (zh) | 2012-12-21 | 2013-12-20 | 亲水性自消耗连接子及其缀合物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201810460861.6A Pending CN108546283A (zh) | 2012-12-21 | 2013-12-20 | 亲水性自消耗连接子及其缀合物 |
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Families Citing this family (98)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CN101098854B (zh) | 2004-07-23 | 2012-12-05 | 恩多塞特公司 | 二价连接体及其轭合物 |
| NZ599239A (en) | 2007-03-14 | 2013-10-25 | Endocyte Inc | Binding ligand linked drug delivery conjugates of tubulysins |
| US9138484B2 (en) | 2007-06-25 | 2015-09-22 | 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 |
| BR112013031819B1 (pt) | 2011-06-10 | 2022-05-03 | Mersana Therapeutics, Inc | Suporte polimérico, composição farmacêutica, composto, e, uso do suporte |
| US8815226B2 (en) | 2011-06-10 | 2014-08-26 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| WO2013126797A1 (en) | 2012-02-24 | 2013-08-29 | 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 |
| US9662402B2 (en) | 2012-10-16 | 2017-05-30 | Endocyte, Inc. | Drug delivery conjugates containing unnatural amino acids and methods for using |
| MX379355B (es) | 2012-12-21 | 2025-03-11 | Altrubio Inc | Enlazadores autodestructivos hidrofilos y conjugados de los mismos. |
| AU2014228489B2 (en) | 2013-03-15 | 2018-11-15 | Zymeworks Bc Inc. | Cytotoxic and anti-mitotic compounds, and methods of using the same |
| ES2754397T3 (es) | 2013-10-11 | 2020-04-17 | Asana Biosciences Llc | Conjugados de proteína-polímero-fármaco |
| KR102087850B1 (ko) | 2013-10-11 | 2020-03-12 | 메르사나 테라퓨틱스, 인코포레이티드 | 단백질-고분자-약물 접합체 |
| BR112016015105A8 (pt) | 2013-12-27 | 2018-04-24 | Var2 Pharmaceuticals Aps | conjugados var2csa-droga |
| KR102384740B1 (ko) | 2013-12-27 | 2022-04-07 | 자임워크스 인코포레이티드 | 약물 접합체를 위한 설폰아마이드-함유 연결 시스템 |
| SG11201610620UA (en) | 2014-06-20 | 2017-01-27 | Bioalliance Cv | Anti-folate receptor aplha (fra) antibody-drug conjugates and methods of using thereof |
| EP3157560A4 (en) * | 2014-06-20 | 2018-02-21 | Abgenomics International Inc. | Her2 antibody-drug conjugates |
| RU2017101681A (ru) * | 2014-06-20 | 2018-07-20 | Биоэллаенс К.В. | Конъюгаты анти-cd22 антитело - лекарственное средство и способы их применения |
| MX384379B (es) * | 2014-08-28 | 2025-03-14 | Pfizer | Ligadores que modulan la estabilidad para usar con conjugados anticuerpo-fármaco. |
| RS62860B1 (sr) | 2014-09-17 | 2022-02-28 | Zymeworks Inc | Citotoksična i antimitotička jedinjenja, i postupci upotrebe istih |
| CN107106701B (zh) | 2014-10-03 | 2020-11-06 | 西纳福克斯股份有限公司 | 磺酰胺接头、其缀合物及制备方法 |
| AU2015358532C1 (en) * | 2014-12-03 | 2020-10-29 | Genentech, Inc. | Quaternary amine compounds and antibody-drug conjugates thereof |
| EP3277305B1 (en) | 2015-03-31 | 2021-07-21 | F. Hoffmann-La Roche AG | Antigen binding molecules comprising a trimeric tnf family ligand |
| CA2985823A1 (en) | 2015-05-12 | 2016-11-17 | Blinkbio, Inc. | Silicon based drug conjugates and methods of using same |
| US11173213B2 (en) * | 2015-06-29 | 2021-11-16 | Daiichi Sankyo Company, Limited | Method for selectively manufacturing antibody-drug conjugate |
| AR106188A1 (es) | 2015-10-01 | 2017-12-20 | Hoffmann La Roche | Anticuerpos anti-cd19 humano humanizados y métodos de utilización |
| EP3165237B1 (en) | 2015-11-03 | 2018-12-19 | Industrial Technology Research Institute | Antibody-drug conjugate (adc) and method for forming the same |
| AU2017206074B2 (en) | 2016-01-08 | 2023-09-07 | Altrubio Inc. | Tetravalent anti-PSGL-1 antibodies and uses thereof |
| WO2017137456A1 (en) | 2016-02-08 | 2017-08-17 | Synaffix B.V. | Bioconjugates containing sulfamide linkers for use in treatment |
| US11590239B2 (en) | 2016-02-08 | 2023-02-28 | Synaffix B.V. | Antibody-conjugates with improved therapeutic index for targeting CD30 tumours and method for improving therapeutic index of antibody-conjugates |
| WO2017137457A1 (en) | 2016-02-08 | 2017-08-17 | Synaffix B.V. | Antibody-conjugates with improved therapeutic index for targeting cd30 tumours and method for improving therapeutic index of antibody-conjugates |
| EP3413916A1 (en) | 2016-02-08 | 2018-12-19 | Synaffix B.V. | Antibody-conjugates with improved therapeutic index for targeting cd30 tumours and method for improving therapeutic index of antibody-conjugates |
| WO2017137423A1 (en) | 2016-02-08 | 2017-08-17 | Synaffix B.V. | Improved sulfamide linkers for use in bioconjugates |
| US20190307904A1 (en) | 2016-03-30 | 2019-10-10 | Convatec Technologies Inc. | Modified wound dressings |
| MA45328A (fr) | 2016-04-01 | 2019-02-06 | Avidity Biosciences Llc | Compositions acide nucléique-polypeptide et utilisations de celles-ci |
| UY37278A (es) | 2016-06-08 | 2018-01-31 | Abbvie Inc | Anticuerpos anti-b7-h3 y conjugados de fármaco y anticuerpos |
| JP2019517564A (ja) | 2016-06-09 | 2019-06-24 | ブリンクバイオ インコーポレイテッド | シラノール系治療的ペイロード |
| US11419944B2 (en) | 2016-10-11 | 2022-08-23 | Byondis B.V. | Non-linear self-immolative linkers and conjugates thereof |
| KR102562760B1 (ko) * | 2016-11-25 | 2023-08-04 | 맵웰 (상하이) 바이오사이언스 컴퍼니, 리미티드 | 항체-약물 접합을 위한 이-치환된 말레익 아미드 링커 및 이의 제조 방법 및 용도 |
| CN108101825B (zh) * | 2016-11-25 | 2022-02-22 | 迈威(上海)生物科技股份有限公司 | 用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途 |
| CN109810039B (zh) * | 2017-11-22 | 2021-11-12 | 迈威(上海)生物科技股份有限公司 | 一种用于抗体-药物偶联的双取代马来酰胺类连接子及其制备方法和用途 |
| MX2019008199A (es) | 2017-01-06 | 2019-11-25 | Avidity Biosciences Llc | Composiciones de acido nucleico polipeptido y metodos de induccion de la omision de exon. |
| JP2020507584A (ja) | 2017-02-10 | 2020-03-12 | ザ ボード オブ トラスティーズ オブ ザ ユニヴァーシティ オブ イリノイThe Board Of Trustees Of The University Of Illinois | 癌選択的標識および標的化のためのトリガー活性化可能な糖コンジュゲート |
| AU2018289581C1 (en) | 2017-06-23 | 2025-01-30 | VelosBio Inc. | ROR1 antibody immunoconjugates |
| JP7325341B2 (ja) | 2017-07-11 | 2023-08-14 | シンソークス,インク. | 非天然ヌクレオチドの組み込み及びその方法 |
| GB201711809D0 (en) | 2017-07-21 | 2017-09-06 | Governors Of The Univ Of Alberta | Antisense oligonucleotide |
| WO2019023247A1 (en) | 2017-07-25 | 2019-01-31 | Immutics, Inc. | TREATMENT OF CANCER BY BLOCKING THE INTERACTION OF TIM-3 AND ITS LIGAND |
| BR112020002272A2 (pt) | 2017-08-03 | 2020-07-28 | Synthorx, Inc. | conjugados de citocina para o tratamento de doenças autoimunes |
| WO2019071028A1 (en) | 2017-10-04 | 2019-04-11 | Avidity Biosciences Llc | NUCLEIC ACID-POLYPEPTIDE COMPOSITIONS AND USES THEREOF |
| WO2019113393A1 (en) | 2017-12-06 | 2019-06-13 | Avidity Biosciences Llc | Compositions and methods of treating muscle atrophy and myotonic dystrophy |
| KR102812714B1 (ko) | 2018-02-26 | 2025-05-27 | 신톡스, 인크. | Il-15 접합체 및 이의 용도 |
| WO2019183270A1 (en) * | 2018-03-23 | 2019-09-26 | The Regents Of The University Of California | Puromycin-based probes and methods of use thereof |
| WO2019185586A1 (en) | 2018-03-26 | 2019-10-03 | Universidad Complutense De Madrid | Ligands for enhanced imaging and drug delivery to neuroblastoma cells |
| SG11202011739SA (en) | 2018-05-29 | 2020-12-30 | Bristol Myers Squibb Co | Modified self-immolating moieties for use in prodrugs and conjugates and methods of using and making |
| JP7636323B2 (ja) | 2018-11-08 | 2025-02-26 | シンソークス, インコーポレイテッド | インターロイキン10コンジュゲートおよびその使用 |
| IL319265A (en) | 2018-12-21 | 2025-04-01 | Avidity Biosciences Inc | Anti-transferrin receptor antibodies and their uses |
| EP3918323A4 (en) | 2019-01-30 | 2022-12-28 | TrueBinding, Inc. | ANTI-GAL3 ANTIBODIES AND USES THEREOF |
| CN113660946A (zh) | 2019-02-06 | 2021-11-16 | 新索思股份有限公司 | Il-2缀合物及其使用方法 |
| AU2020263487A1 (en) | 2019-04-25 | 2021-12-16 | Avidity Biosciences, Inc. | Nucleic acid compositions and methods of multi-exon skipping |
| JP2022533215A (ja) * | 2019-05-20 | 2022-07-21 | ノバルティス アーゲー | 親水性基を含むリンカーを有する抗体薬剤コンジュゲート |
| US11578090B2 (en) | 2019-06-06 | 2023-02-14 | Avidity Biosciences, Inc. | Nucleic acid-polypeptide compositions and uses thereof |
| JP7581252B2 (ja) | 2019-06-06 | 2024-11-12 | アビディティー バイオサイエンシーズ,インク. | Unaアミダイトおよびその使用 |
| JP7758662B2 (ja) | 2019-09-10 | 2025-10-22 | シンソークス, インコーポレイテッド | Il-2コンジュゲートおよび自己免疫疾患を治療するための使用方法 |
| KR20220097445A (ko) | 2019-11-04 | 2022-07-07 | 신톡스, 인크. | 인터류킨 10 접합체 및 이의 용도 |
| TW202144572A (zh) | 2020-03-19 | 2021-12-01 | 美商亞維代堤生物科學公司 | 治療臉肩胛肱骨肌肉失養症之組合物及方法 |
| WO2021195469A1 (en) | 2020-03-27 | 2021-09-30 | Avidity Biosciences, Inc. | Compositions and methods of treating muscle dystrophy |
| WO2021242776A2 (en) | 2020-05-26 | 2021-12-02 | Truebinding, Inc. | Methods of treating inflammatory diseases by blocking galectin-3 |
| WO2021249228A1 (zh) * | 2020-06-08 | 2021-12-16 | 四川百利药业有限责任公司 | 一种带有高稳定性亲水连接单元的喜树碱类药物及其偶联物 |
| PE20231104A1 (es) | 2020-07-21 | 2023-07-19 | Genentech Inc | Inductores quimicos de degradacion conjugados con anticuerpo de brm y metodos de estos |
| JP2023548310A (ja) | 2020-10-30 | 2023-11-16 | アバクタ・ライフ・サイエンシーズ・リミテッド | Fap活性化血清半減期延長型治療用コンジュゲート |
| TW202241516A (zh) | 2020-12-17 | 2022-11-01 | 美商杜夫特學院信託管理公司 | 經fap活化之放射性治療診斷(radiotheranostics),與其相關用途 |
| AR124681A1 (es) | 2021-01-20 | 2023-04-26 | Abbvie Inc | Conjugados anticuerpo-fármaco anti-egfr |
| JP2024522388A (ja) * | 2021-04-29 | 2024-06-19 | ハイスリンク セラピューティクス | 抗体薬物複合体の調製方法および使用 |
| WO2022234003A1 (en) | 2021-05-07 | 2022-11-10 | Avacta Life Sciences Limited | Cd33 binding polypeptides with stefin a protein |
| JP2024526764A (ja) | 2021-07-13 | 2024-07-19 | トゥルーバインディング,インコーポレイテッド | タンパク質凝集を防止する方法 |
| CN118265544A (zh) | 2021-09-16 | 2024-06-28 | 艾维迪提生物科学公司 | 治疗面肩肱型肌营养不良的组合物和方法 |
| JP7658450B2 (ja) * | 2021-09-30 | 2025-04-08 | 味の素株式会社 | 抗体および機能性物質の位置選択的なコンジュゲートまたはその塩、ならびにその製造に用いられる抗体誘導体および化合物またはそれらの塩 |
| WO2023054706A1 (ja) * | 2021-09-30 | 2023-04-06 | 味の素株式会社 | 抗体および機能性物質のコンジュゲートまたはその塩、ならびにその製造に用いられる抗体誘導体および化合物またはそれらの塩 |
| KR102793244B1 (ko) | 2021-10-06 | 2025-04-07 | 주식회사 엘지에너지솔루션 | 안전성이 향상된 배터리 팩 |
| WO2023057567A1 (en) | 2021-10-07 | 2023-04-13 | Avacta Life Sciences Limited | Pd-l1 binding affimers |
| EP4412711A1 (en) | 2021-10-07 | 2024-08-14 | Avacta Life Sciences Limited | Serum half-life extended pd-l1 binding polypeptides |
| WO2023086768A1 (en) | 2021-11-09 | 2023-05-19 | Truebinding, Inc. | Methods of treating or inhibiting cardiovascular diseases |
| KR20240107151A (ko) | 2021-11-17 | 2024-07-08 | 알트루바이오 인코퍼레이티드 | T-세포 매개 염증 질환 또는 암을 치료하기 위해 jak 억제제와 조합하여 항-psgl-1 항체를 사용하는 방법 |
| WO2023122347A2 (en) | 2021-12-23 | 2023-06-29 | Mirecule, Inc. | Compositions for delivery of polynucleotides |
| AR128331A1 (es) | 2022-01-26 | 2024-04-17 | Genentech Inc | Inductores químicos de degradación conjugados con anticuerpos y métodos de estos |
| AR128330A1 (es) | 2022-01-26 | 2024-04-17 | Genentech Inc | Inductores químicos de degradación conjugados con anticuerpo y métodos de estos |
| WO2023153876A1 (ko) | 2022-02-10 | 2023-08-17 | 주식회사 아피셀테라퓨틱스 | Cd40l에 특이적으로 결합하는 스테핀 a 단백질 변이체 및 이의 용도 |
| US12071621B2 (en) | 2022-04-05 | 2024-08-27 | Avidity Biosciences, Inc. | Anti-transferrin receptor antibody-PMO conjugates for inducing DMD exon 44 skipping |
| JP2025511684A (ja) | 2022-04-07 | 2025-04-16 | ツインピッグ バイオラブ インコーポレイテッド | 新規ペプチドベースの免疫抗癌剤 |
| WO2023218243A1 (en) | 2022-05-12 | 2023-11-16 | Avacta Life Sciences Limited | Lag-3/pd-l1 binding fusion proteins |
| KR20250054842A (ko) | 2022-07-29 | 2025-04-23 | 리제너론 파마슈티칼스 인코포레이티드 | 뇌 및 근육으로의 트랜스페린 수용체(tfr)-매개 전달을 위한 조성물 및 방법 |
| JP2025531299A (ja) * | 2022-09-16 | 2025-09-19 | 上海君▲実▼生物医▲薬▼科技股▲分▼有限公司 | 抗体薬物複合体に用いられるリンカー及びその応用 |
| WO2024077212A2 (en) * | 2022-10-06 | 2024-04-11 | The Regents Of The University Of California | Site-specific covalent ligation of human serum albumin |
| WO2024107765A2 (en) | 2022-11-14 | 2024-05-23 | Regeneron Pharmaceuticals, Inc. | Compositions and methods for fibroblast growth factor receptor 3-mediated delivery to astrocytes |
| KR20250169306A (ko) | 2023-04-18 | 2025-12-02 | 아스트라제네카 아베 | 절단가능한 링커를 포함하는 접합체 |
| US12491257B2 (en) | 2023-06-27 | 2025-12-09 | Avidity Biosciences, Inc. | Compositions and methods of using PRKAG2-targeting antibody-oligonucleotide conjugates |
| US12409230B2 (en) | 2023-06-30 | 2025-09-09 | Avidity Biosciences, Inc. | Compositions comprising PLN-targeting anti-transferrin receptor antibody-polynucleotides and methods of use thereof to treat cardiomyopathy |
| WO2025158385A1 (en) | 2024-01-25 | 2025-07-31 | Genzyme Corporation | Pegylated il-2 for suppressing adaptive immune response to gene therapy |
Family Cites Families (88)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4816567A (en) | 1983-04-08 | 1989-03-28 | Genentech, Inc. | Recombinant immunoglobin preparations |
| GB8823869D0 (en) | 1988-10-12 | 1988-11-16 | Medical Res Council | Production of antibodies |
| US5198560A (en) | 1990-04-27 | 1993-03-30 | Bristol-Myers Squibb Company | Cytotoxic bicyclo[7.3.1]tridec-4-ene-2,6-diyne compounds and process for the preparation thereof |
| US5633425A (en) | 1990-08-29 | 1997-05-27 | Genpharm International, Inc. | Transgenic non-human animals capable of producing heterologous antibodies |
| JP2938569B2 (ja) | 1990-08-29 | 1999-08-23 | ジェンファーム インターナショナル,インコーポレイティド | 異種免疫グロブリンを作る方法及びトランスジェニックマウス |
| US5625126A (en) | 1990-08-29 | 1997-04-29 | Genpharm International, Inc. | Transgenic non-human animals for 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 |
| US5545806A (en) | 1990-08-29 | 1996-08-13 | Genpharm International, Inc. | Ransgenic non-human animals for producing heterologous antibodies |
| WO1992009690A2 (en) | 1990-12-03 | 1992-06-11 | Genentech, Inc. | Enrichment method for variant proteins with altered binding properties |
| US6214345B1 (en) * | 1993-05-14 | 2001-04-10 | Bristol-Myers Squibb Co. | Lysosomal enzyme-cleavable antitumor drug conjugates |
| DE69534530T2 (de) | 1994-08-12 | 2006-07-06 | Immunomedics, Inc. | Für b-zell-lymphom und leukämiezellen spezifische immunkonjugate und humane antikörper |
| US6548530B1 (en) | 1995-10-03 | 2003-04-15 | The Scripps Research Institute | CBI analogs of CC-1065 and the duocarmycins |
| DE69733942T2 (de) | 1996-03-08 | 2006-06-08 | The Scripps Research Institute, La Jolla | Mcbi analoge von cc-1065 und die duocarmycine |
| EP0934269A4 (en) | 1996-05-31 | 2000-01-12 | Scripps Research Inst | ANALOGS OF CC-1065 AND DUOCARMYCINE |
| DE69825048D1 (de) | 1997-05-22 | 2004-08-19 | Scripps Research Inst | Analoga von duocarmycin and cc-1065 |
| IL135616A0 (en) | 1997-10-14 | 2001-05-20 | Scripps Research Inst | Iso-cbi and iso-ci analogs of cc-1065 and the duocarmycins |
| GB9809951D0 (en) | 1998-05-08 | 1998-07-08 | Univ Cambridge Tech | Binding molecules |
| US20020106728A1 (en) | 2000-06-20 | 2002-08-08 | Genentech, Inc. | NS4 nucleic acids and polypeptides and methods of use for the treatment of body weight disorders |
| US6762020B1 (en) | 1999-03-15 | 2004-07-13 | Protein Design Labs, Inc. | Methods of diagnosing breast cancer |
| DE19926154A1 (de) | 1999-06-09 | 2000-12-14 | Ktb Tumorforschungs Gmbh | Verfahren zur Herstellung einer injizierbaren Arzneimittelzubereitung |
| US20070258987A1 (en) | 2000-11-28 | 2007-11-08 | Seattle Genetics, Inc. | Recombinant Anti-Cd30 Antibodies and Uses Thereof |
| US7090843B1 (en) | 2000-11-28 | 2006-08-15 | Seattle Genetics, Inc. | Recombinant anti-CD30 antibodies and uses thereof |
| EP1243276A1 (en) | 2001-03-23 | 2002-09-25 | Franciscus Marinus Hendrikus De Groot | Elongated and multiple spacers containing activatible prodrugs |
| US20030083263A1 (en) | 2001-04-30 | 2003-05-01 | Svetlana Doronina | Pentapeptide compounds and uses related thereto |
| US6884869B2 (en) | 2001-04-30 | 2005-04-26 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| US7256257B2 (en) | 2001-04-30 | 2007-08-14 | Seattle Genetics, Inc. | Pentapeptide compounds and uses related thereto |
| KR100788092B1 (ko) | 2001-06-20 | 2007-12-21 | 제넨테크, 인크. | 종양의 진단 및 치료를 위한 방법 및 이를 위한 조성물 |
| US7091186B2 (en) | 2001-09-24 | 2006-08-15 | Seattle Genetics, Inc. | p-Amidobenzylethers in drug delivery agents |
| US8877901B2 (en) | 2002-12-13 | 2014-11-04 | Immunomedics, Inc. | Camptothecin-binding moiety conjugates |
| US7591994B2 (en) | 2002-12-13 | 2009-09-22 | Immunomedics, Inc. | Camptothecin-binding moiety conjugates |
| KR20040101502A (ko) | 2002-04-16 | 2004-12-02 | 제넨테크, 인크. | 종양의 진단 및 치료 방법 및 이를 위한 조성물 |
| PL224001B1 (pl) | 2002-05-02 | 2016-11-30 | Wyeth Corp | Sposób wytwarzania stabilnej liofilizowanej kompozycji obejmującej monomeryczne koniugaty pochodna kalicheamycyny/przeciwciało anty-CD22, kompozycja otrzymana tym sposobem oraz jej zastosowanie |
| US20090068178A1 (en) | 2002-05-08 | 2009-03-12 | Genentech, Inc. | Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin |
| JP4741838B2 (ja) | 2002-07-31 | 2011-08-10 | シアトル ジェネティクス,インコーポレーテッド | 癌、自己免疫疾患または感染症を治療するための薬物結合体およびその使用 |
| JP2006507322A (ja) | 2002-11-14 | 2006-03-02 | シンタルガ・ビーブイ | 多重自己脱離放出スペーサーとして構築されたプロドラッグ |
| US8420086B2 (en) | 2002-12-13 | 2013-04-16 | Immunomedics, Inc. | Camptothecin conjugates of anti-CD22 antibodies for treatment of B cell diseases |
| US7332164B2 (en) | 2003-03-21 | 2008-02-19 | Enzon Pharmaceuticals, Inc. | Heterobifunctional polymeric bioconjugates |
| CN104998273A (zh) | 2003-11-06 | 2015-10-28 | 西雅图基因公司 | 能够与配体偶联的单甲基缬氨酸化合物 |
| WO2005080431A2 (en) | 2004-02-12 | 2005-09-01 | Morphotek, Inc. | Monoclonal antibodies that specifically bind to folate receptor alpha |
| AU2005216251B2 (en) | 2004-02-23 | 2011-03-10 | Genentech, Inc. | Heterocyclic self-immolative linkers and conjugates |
| MXPA06010782A (es) | 2004-03-23 | 2007-03-28 | Complex Biosystems Gmbh | Ligador de profarmaco. |
| JP4861308B2 (ja) | 2004-04-07 | 2012-01-25 | ジェネンテック, インコーポレイテッド | 抗体結合体の質量分析 |
| US7691962B2 (en) | 2004-05-19 | 2010-04-06 | Medarex, Inc. | Chemical linkers and conjugates thereof |
| EP3088004B1 (en) | 2004-09-23 | 2018-03-28 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
| WO2008020827A2 (en) | 2005-08-01 | 2008-02-21 | Biogen Idec Ma Inc. | Altered polypeptides, immunoconjugates thereof, and methods related thereto |
| WO2007103288A2 (en) | 2006-03-02 | 2007-09-13 | Seattle Genetics, Inc. | Engineered antibody drug conjugates |
| US8524865B2 (en) | 2006-05-30 | 2013-09-03 | Genentech, Inc. | Antibodies and immunoconjugates and uses therefor |
| BRPI0712850A8 (pt) | 2006-06-07 | 2018-05-02 | Bioalliance Cv | anticorpos que reconhecem um epitopo contendo carboidrato em cd-43 e cea expressados em células cancerígenas e métodos de uso dos mesmos |
| CA2663375A1 (en) | 2006-09-15 | 2008-03-20 | Onconova Therapeutics, Inc. | Activated cytotoxic compounds for attachment to targeting molecules for the treatment of mammalian disease conditions |
| GB0619291D0 (en) | 2006-09-29 | 2006-11-08 | Ucb Sa | Altered antibodies |
| PT2099823E (pt) | 2006-12-01 | 2014-12-22 | Seattle Genetics Inc | Agentes de ligação ao alvo variantes e suas utilizações |
| TWI412367B (zh) | 2006-12-28 | 2013-10-21 | Medarex Llc | 化學鏈接劑與可裂解基質以及其之綴合物 |
| US9216228B2 (en) | 2007-02-16 | 2015-12-22 | KTB Tumorforschungsgesellschaft MBM | Receptor and antigen targeted prodrug |
| BRPI0820452A2 (pt) | 2007-12-18 | 2015-06-16 | Bioalliance Cv | Anticorpos que reconhecendo um epítopo contendo um carboidrato em cd-43 e cea expressos em células cancerosas e métodos de uso dos mesmos. |
| ES2613963T3 (es) | 2008-01-18 | 2017-05-29 | Medimmune, Llc | Anticuerpos manipulados con cisteína para conjugación específica de sitio |
| US8742076B2 (en) | 2008-02-01 | 2014-06-03 | Genentech, Inc. | Nemorubicin metabolite and analog reagents, antibody-drug conjugates and methods |
| US8309093B2 (en) | 2009-03-06 | 2012-11-13 | Agensys, Inc. | Antibody drug conjugates (ADC) that bind to 24P4C12 proteins |
| AU2010256410B2 (en) | 2009-06-04 | 2016-10-20 | Massachusetts Institute Of Technology | Methods for identification of sites for IgG conjugation |
| EP2711018A1 (en) | 2009-06-22 | 2014-03-26 | MedImmune, LLC | Engineered Fc regions for site-specific conjugation |
| GB0920127D0 (en) | 2009-11-17 | 2009-12-30 | Ucb Pharma Sa | Antibodies |
| SMT201700139T1 (it) | 2010-02-24 | 2017-05-08 | Immunogen Inc | Immunoconiugati contro il recettore 1 del folato e relativi usi |
| HRP20130953T1 (hr) | 2010-04-15 | 2013-11-22 | Spirogen Sàrl | Pirolobenzodiazepini i njihovi konjugati |
| NO3056203T3 (enExample) | 2010-04-21 | 2018-05-12 | ||
| CA2799540A1 (en) | 2010-06-08 | 2011-12-15 | Genentech, Inc. | Cysteine engineered antibodies and conjugates |
| SMT201900181T1 (it) | 2011-02-15 | 2019-05-10 | Immunogen Inc | Metodi di preparazione di coniugati |
| CN114441757A (zh) | 2011-04-01 | 2022-05-06 | 伊缪诺金公司 | 用于增加folr1癌症治疗的功效的方法 |
| US8852599B2 (en) | 2011-05-26 | 2014-10-07 | Bristol-Myers Squibb Company | Immunoconjugates, compositions for making them, and methods of making and use |
| BR112013032928A2 (pt) | 2011-06-21 | 2017-01-24 | Immunogen Inc | "derivados de maitansinoide com ligante de peptídeo e conjugados dos mesmos, composição farmacêutica que os compreende e uso dos mesmos" |
| CA3111357A1 (en) | 2011-12-23 | 2013-06-27 | Pfizer Inc. | Engineered antibody constant regions for site-specific conjugation and methods and uses therefor |
| AU2013203422A1 (en) | 2012-01-06 | 2013-07-18 | Bioalliance C.V. | Anti-transferrin receptor antibodies and methods using same |
| WO2013173391A1 (en) | 2012-05-15 | 2013-11-21 | Concortis Biosystems, Corp | Drug-conjugates, conjugation methods, and uses thereof |
| WO2013181597A2 (en) | 2012-05-31 | 2013-12-05 | Synchem, Inc. | Thiol-ene click chemistry for drug conjugates |
| BR112015000439A2 (pt) | 2012-07-09 | 2017-12-19 | Genentech Inc | imunoconjugado , formulação farmacêutica e métodos de tratamento de um indivíduo e de inibição da proliferação |
| PL2872157T3 (pl) | 2012-07-12 | 2020-07-13 | Hangzhou Dac Biotech Co., Ltd | Koniugaty wiążących komórkę cząsteczek ze środkami cytotoksycznymi |
| CN103566377A (zh) * | 2012-07-18 | 2014-02-12 | 上海博笛生物科技有限公司 | 癌症的靶向免疫治疗 |
| WO2014057118A1 (en) | 2012-10-12 | 2014-04-17 | Adc Therapeutics Sarl | Pyrrolobenzodiazepine-anti-cd22 antibody conjugates |
| US9107960B2 (en) | 2012-12-13 | 2015-08-18 | Immunimedics, Inc. | Antibody-SN-38 immunoconjugates with a CL2A linker |
| DK2900277T3 (da) | 2012-12-13 | 2022-04-04 | Immunomedics Inc | Doser af immunokonjugater af antistoffer og sn-38 til forbedret effektivitet og reduceret toksicitet |
| MX379355B (es) | 2012-12-21 | 2025-03-11 | Altrubio Inc | Enlazadores autodestructivos hidrofilos y conjugados de los mismos. |
| US9814784B2 (en) | 2013-01-03 | 2017-11-14 | Celltrion, Inc. | Antibody-linker-drug conjugate, preparation method therefor, and anticancer drug composition containing same |
| SI2953976T1 (sl) | 2013-02-08 | 2021-08-31 | Novartis Ag | Specifična mesta z modificiranje protiteles za izdelavo imunokonjugatov |
| CA2902872A1 (en) | 2013-03-15 | 2014-09-18 | Regeneron Pharmaceuticals, Inc. | Biologically active molecules, conjugates thereof, and therapeutic uses |
| WO2014197871A2 (en) | 2013-06-06 | 2014-12-11 | Igenica Biotherapeutics, Inc. | Antibody-drug conjugates, compositions and methods of use |
| ES2668984T3 (es) | 2014-01-10 | 2018-05-23 | Synthon Biopharmaceuticals B.V. | CAF de duocarmicina para su uso en el tratamiento del cáncer de vejiga |
| EP3157560A4 (en) | 2014-06-20 | 2018-02-21 | Abgenomics International Inc. | Her2 antibody-drug conjugates |
| SG11201610620UA (en) | 2014-06-20 | 2017-01-27 | Bioalliance Cv | Anti-folate receptor aplha (fra) antibody-drug conjugates and methods of using thereof |
| RU2017101681A (ru) | 2014-06-20 | 2018-07-20 | Биоэллаенс К.В. | Конъюгаты анти-cd22 антитело - лекарственное средство и способы их применения |
| AU2017206074B2 (en) | 2016-01-08 | 2023-09-07 | Altrubio Inc. | Tetravalent anti-PSGL-1 antibodies and uses thereof |
-
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-
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- 2018-03-13 US US15/920,229 patent/US20180264131A1/en not_active Abandoned
-
2020
- 2020-12-10 US US17/118,228 patent/US20210113710A1/en not_active Abandoned
Non-Patent Citations (2)
| Title |
|---|
| 《Antibody-Drug Conjugates: Linking Cytotoxic Payloads to Monoclonal Antibodies》;Laurent Ducry and Bernhard Stump;《Bioconjugate Chem.》;20100921;第21卷(第1期);5-13 * |
| 《Elongated Multiple Electronic Cascade and Cyclization Spacer Systems in Activatible Anticancer Prodrugs for Enhanced Drug Release》;Franciscus M. H. de Groot等;《J. Org. Chem.》;20011127;第66卷;8815-8830 * |
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