JP2019502746A5 - - Google Patents
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- JP2019502746A5 JP2019502746A5 JP2018538743A JP2018538743A JP2019502746A5 JP 2019502746 A5 JP2019502746 A5 JP 2019502746A5 JP 2018538743 A JP2018538743 A JP 2018538743A JP 2018538743 A JP2018538743 A JP 2018538743A JP 2019502746 A5 JP2019502746 A5 JP 2019502746A5
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- 150000001875 compounds Chemical class 0.000 claims description 189
- 125000000217 alkyl group Chemical group 0.000 claims description 53
- 125000003545 alkoxy group Chemical group 0.000 claims description 37
- 125000005843 halogen group Chemical group 0.000 claims description 37
- 125000000592 heterocycloalkyl group Chemical group 0.000 claims description 37
- 125000001188 haloalkyl group Chemical group 0.000 claims description 35
- 239000011230 binding agent Substances 0.000 claims description 25
- 238000000034 method Methods 0.000 claims description 22
- 125000004438 haloalkoxy group Chemical group 0.000 claims description 19
- 125000003342 alkenyl group Chemical group 0.000 claims description 18
- 125000002877 alkyl aryl group Chemical group 0.000 claims description 18
- 125000000304 alkynyl group Chemical group 0.000 claims description 18
- 125000003710 aryl alkyl group Chemical group 0.000 claims description 18
- 125000003118 aryl group Chemical group 0.000 claims description 18
- 150000001540 azides Chemical class 0.000 claims description 18
- 125000004093 cyano group Chemical group *C#N 0.000 claims description 18
- 125000001072 heteroaryl group Chemical group 0.000 claims description 18
- 125000000449 nitro group Chemical group [O-][N+](*)=O 0.000 claims description 18
- 125000004404 heteroalkyl group Chemical group 0.000 claims description 16
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- 125000005549 heteroarylene group Chemical group 0.000 claims description 14
- 101710104624 Proline/betaine transporter Proteins 0.000 claims description 12
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- 125000001309 chloro group Chemical group Cl* 0.000 claims description 12
- 239000002184 metal Substances 0.000 claims description 12
- 125000002496 methyl group Chemical group [H]C([H])([H])* 0.000 claims description 12
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- LMBFAGIMSUYTBN-MPZNNTNKSA-N teixobactin Chemical compound C([C@H](C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H](CCC(N)=O)C(=O)N[C@H]([C@@H](C)CC)C(=O)N[C@@H]([C@@H](C)CC)C(=O)N[C@@H](CO)C(=O)N[C@H]1C(N[C@@H](C)C(=O)N[C@@H](C[C@@H]2NC(=N)NC2)C(=O)N[C@H](C(=O)O[C@H]1C)[C@@H](C)CC)=O)NC)C1=CC=CC=C1 LMBFAGIMSUYTBN-MPZNNTNKSA-N 0.000 claims description 10
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- ALBODLTZUXKBGZ-JUUVMNCLSA-N (2s)-2-amino-3-phenylpropanoic acid;(2s)-2,6-diaminohexanoic acid Chemical compound NCCCC[C@H](N)C(O)=O.OC(=O)[C@@H](N)CC1=CC=CC=C1 ALBODLTZUXKBGZ-JUUVMNCLSA-N 0.000 claims description 2
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| WO2017190079A1 (en) | 2016-04-28 | 2017-11-02 | Regeneron Pharmaceuticals, Inc. | Methods of making multispecific antigen-binding molecules |
| TWI782930B (zh) | 2016-11-16 | 2022-11-11 | 美商再生元醫藥公司 | 抗ｍｅｔ抗體，結合ｍｅｔ之雙特異性抗原結合分子及其使用方法 |
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| FI3635009T3 (fi) | 2017-06-07 | 2026-04-07 | Regeneron Pharma | Koostumuksia ja menetelmiä entsyymien internalisoimiseksi |
| MX2020004691A (es) | 2017-11-07 | 2020-08-20 | Regeneron Pharma | Enlazadores hidrofilicos para conjugados anticuerpo-farmaco. |
| MX2020011487A (es) | 2018-04-30 | 2020-12-07 | Regeneron Pharma | Anticuerpos y moleculas biespecificas de union al antigeno que se unen a her2 y/o aplp2, conjugados y usos de estos. |
| EP3793591A1 (en) | 2018-05-17 | 2021-03-24 | Regeneron Pharmaceuticals, Inc. | Anti-cd63 antibodies, conjugates, and uses thereof |
| JP2022500454A (ja) * | 2018-09-17 | 2022-01-04 | ストロ バイオファーマ インコーポレーテッド | 抗葉酸受容体抗体コンジュゲートによる併用療法 |
| JP7591503B2 (ja) | 2018-12-21 | 2024-11-28 | リジェネロン ファーマシューティカルズ，インク． | リファマイシンアナログおよびその抗体薬物コンジュゲート |
| US20220040319A1 (en) | 2019-02-21 | 2022-02-10 | Regeneron Pharmaceuticals, Inc. | Methods of treating ocular cancer using anti-met antibodies and bispecific antigen binding molecules that bind met |
| US11896682B2 (en) | 2019-09-16 | 2024-02-13 | Regeneron Pharmaceuticals, Inc. | Radiolabeled MET binding proteins for immuno-PET imaging and methods of use thereof |
| US11814428B2 (en) | 2019-09-19 | 2023-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-PTCRA antibody-drug conjugates and uses thereof |
| AU2020381495A1 (en) | 2019-11-15 | 2022-05-19 | Seagen Inc. | Methods of treating HER2 positive breast cancer with tucatinib in combination with an anti-HER2 antibody-drug conjugate |
| IL295312A (en) | 2020-02-28 | 2022-10-01 | Regeneron Pharma | Bispecific antigen binding molecules that bind her2, and methods of use thereof |
| IL319200A (en) | 2020-04-16 | 2025-04-01 | Regeneron Pharma | Antibody-drug conjugates prepared using Diels-Alder compression methods |
| KR20240038138A (ko) | 2020-07-13 | 2024-03-22 | 리제너론 파마슈티칼스 인코포레이티드 | 단백질에서 글루타민 잔기에 접합된 캄토테신 유사체 및 그의 용도 |
| CA3191304A1 (en) | 2020-09-14 | 2022-03-17 | Amy Han | Antibody-drug conjugates comprising glp1 peptidomimetics and uses thereof |
| AU2021366691B2 (en) | 2020-10-22 | 2024-06-06 | Regeneron Pharmaceuticals, Inc. | Anti-FGFR2 antibodies and methods of use thereof |
| CA3198294A1 (en) | 2020-11-10 | 2022-05-19 | Thomas Nittoli | Selenium antibody conjugates |
| CA3241734A1 (en) | 2022-01-12 | 2023-07-20 | Amy Han | Camptothecin analogs conjugated to a glutamine residue in a protein, and their use |
| AU2023231305A1 (en) | 2022-03-11 | 2024-09-12 | Regeneron Pharmaceuticals, Inc. | Anti-GLP1r antibody-tethered drug conjugates comprising GLP1 peptidomimetics and uses thereof |
| IL321285A (en) | 2022-12-21 | 2025-08-01 | Regeneron Pharma | Topoisomerase I inhibitor prodrugs for ADC conjugates and a regimen for their use |
| CN116239607B (zh) * | 2023-01-04 | 2024-04-09 | 山东大学 | 一种美登素衍生物及其生物合成方法与应用 |
| US20250171516A1 (en) | 2023-11-03 | 2025-05-29 | Regeneron Pharmaceuticals, Inc. | Peptide acids as a glp1r agonist and antibody-drug conjugates thereof |
| CN117257977A (zh) * | 2023-11-07 | 2023-12-22 | 正大天晴药业集团南京顺欣制药有限公司 | 用于制备抗体药物偶联物的方法 |
Family Cites Families (81)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4307016A (en) * | 1978-03-24 | 1981-12-22 | Takeda Chemical Industries, Ltd. | Demethyl maytansinoids |
| JPS5566585A (en) | 1978-11-14 | 1980-05-20 | Takeda Chem Ind Ltd | Novel maytansinoid compound and its preparation |
| US4263294A (en) * | 1978-11-20 | 1981-04-21 | Takeda Chemical Industries, Ltd. | Maytansinoids, pharmaceutical compositions thereof and method of use thereof |
| JPS55102583A (en) * | 1979-01-31 | 1980-08-05 | Takeda Chem Ind Ltd | 20-acyloxy-20-demethylmaytansinoid compound |
| CA2026147C (en) | 1989-10-25 | 2006-02-07 | Ravi J. Chari | Cytotoxic agents comprising maytansinoids and their therapeutic use |
| US5208020A (en) | 1989-10-25 | 1993-05-04 | Immunogen Inc. | Cytotoxic agents comprising maytansinoids and their therapeutic use |
| US5714586A (en) | 1995-06-07 | 1998-02-03 | American Cyanamid Company | Methods for the preparation of monomeric calicheamicin derivative/carrier conjugates |
| US7087411B2 (en) | 1999-06-08 | 2006-08-08 | Regeneron Pharmaceuticals, Inc. | Fusion protein capable of binding VEGF |
| US6596541B2 (en) | 2000-10-31 | 2003-07-22 | Regeneron Pharmaceuticals, Inc. | Methods of modifying eukaryotic cells |
| US20070258987A1 (en) | 2000-11-28 | 2007-11-08 | Seattle Genetics, Inc. | Recombinant Anti-Cd30 Antibodies and Uses Thereof |
| US20090068178A1 (en) | 2002-05-08 | 2009-03-12 | Genentech, Inc. | Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin |
| DK2105135T3 (da) * | 2002-05-17 | 2014-11-03 | Celgene Corp | Farmaceutiske sammensætninger til behandling af cancer |
| SI1545613T1 (sl) * | 2002-07-31 | 2011-11-30 | Seattle Genetics Inc | Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni |
| US20110250133A1 (en) | 2003-01-13 | 2011-10-13 | Bracco Imaging S.P.A. | Gastrin releasing peptide compounds |
| US8088387B2 (en) | 2003-10-10 | 2012-01-03 | Immunogen Inc. | Method of targeting specific cell populations using cell-binding agent maytansinoid conjugates linked via a non-cleavable linker, said conjugates, and methods of making said conjugates |
| US7276497B2 (en) | 2003-05-20 | 2007-10-02 | Immunogen Inc. | Cytotoxic agents comprising new maytansinoids |
| CN102558352A (zh) | 2003-06-27 | 2012-07-11 | 艾默根佛蒙特有限公司 | 针对表皮生长因子受体的缺失突变体的抗体及其使用 |
| GB0316294D0 (en) | 2003-07-11 | 2003-08-13 | Polytherics Ltd | Conjugated biological molecules and their preparation |
| AR048098A1 (es) | 2004-03-15 | 2006-03-29 | Wyeth Corp | Conjugados de caliqueamicina |
| CN1997402B (zh) * | 2004-05-19 | 2014-04-02 | 梅达雷克斯有限责任公司 | 化学连接基团及其缀合物 |
| KR20120064120A (ko) | 2004-06-01 | 2012-06-18 | 제넨테크, 인크. | 항체 약물 접합체 및 방법 |
| EP1817341A2 (en) | 2004-11-29 | 2007-08-15 | Seattle Genetics, Inc. | Engineered antibodies and immunoconjugates |
| NZ563370A (en) | 2005-06-20 | 2010-10-29 | Genentech Inc | Compositions and methods for the diagnosis and treatment of tumor |
| NZ565075A (en) | 2005-06-20 | 2011-05-27 | Psma Dev Company Llc | PSMA antibody-drug conjugates |
| US7750116B1 (en) | 2006-02-18 | 2010-07-06 | Seattle Genetics, Inc. | Antibody drug conjugate metabolites |
| KR20140116546A (ko) | 2006-10-27 | 2014-10-02 | 제넨테크, 인크. | 항체 및 면역접합체 및 이들의 용도 |
| NO347649B1 (no) | 2006-12-14 | 2024-02-12 | Regeneron Pharma | Humant antistoff eller antistoff fragment som spesifikt binder human deltaliknende ligand 4 (hDII4), nukleinsyremolekyl som koder for slike og vektor og vert-vektorsystemer, samt fremgangsmåte for fremstilling, sammensetning og anvendelse. |
| WO2008122039A2 (en) | 2007-04-02 | 2008-10-09 | The Government Of The United States Of America, As Represented By The Secretary, Department Of Health And Human Services | Selenocysteine mediated hybrid antibody molecules |
| EP2144628B1 (en) | 2007-05-08 | 2012-10-17 | Genentech, Inc. | Cysteine engineered anti-muc16 antibodies and antibody drug conjugates |
| JP2010528285A (ja) | 2007-05-23 | 2010-08-19 | ベンタナ・メデイカル・システムズ・インコーポレーテツド | 免疫組織化学およびｉｎｓｉｔｕハイブリダーゼーションのためのポリマー担体 |
| NZ602675A (en) | 2008-03-18 | 2014-03-28 | Genentech Inc | Combinations of an anti-her2 antibody-drug conjugate and chemotherapeutic agents, and methods of use |
| EP2276506A4 (en) | 2008-04-30 | 2014-05-07 | Immunogen Inc | EFFICIENT CONJUGATES AND HYDROPHILIC BINDER |
| CN102159248B (zh) * | 2008-07-15 | 2013-09-11 | 健泰科生物技术公司 | 蒽环类衍生物缀合物、它们的制备方法以及它们作为抗肿瘤化合物的用途 |
| EP2374481B1 (en) | 2008-07-21 | 2015-11-04 | Polytherics Limited | Novel reagents and method for conjugating biological molecules |
| US9005598B2 (en) | 2009-03-04 | 2015-04-14 | Polytherics Limited | Conjugated proteins and peptides |
| JO3182B1 (ar) | 2009-07-29 | 2018-03-08 | Regeneron Pharma | مضادات حيوية بشرية عالية الالفة مع تولد الاوعية البشرية - 2 |
| JP5954789B2 (ja) | 2009-08-10 | 2016-07-20 | ユーシーエル ビジネス パブリック リミテッド カンパニー | 機能的分子の可逆的共有結合 |
| AR078471A1 (es) | 2009-10-02 | 2011-11-09 | Sanofi Aventis | COMPUESTOS MAITANSINOIDES Y EL USO DE ESTOS PARA PREPARAR CONJUGADOS CON UN ANTICUERPO LOS CUALES SE UTILIZAN COMO AGENTES ANTICANCERIGENOS Y EL PROCEDIMIENTO DE PREPARACIoN DE ESTOS CONJUGADOS |
| EP2486023A4 (en) | 2009-10-06 | 2014-05-07 | Immunogen Inc | EFFICIENT CONJUGATES AND HYDROPHILIC BINDER |
| US8501692B2 (en) | 2009-12-14 | 2013-08-06 | The Regents Of The University Of Michigan | Compositions and methods for altering cocaine esterase activity |
| DK2528625T3 (da) | 2010-04-15 | 2013-10-14 | Spirogen Sarl | Pyrrolobenzodiazepiner og konjugater deraf |
| US20130244905A1 (en) | 2010-07-06 | 2013-09-19 | Ed Grabczyk | Reporter for RNA Polymerase II Termination |
| SG10201912639SA (en) | 2010-08-02 | 2020-02-27 | Regeneron Pharma | Mice that make binding proteins comprising vl domains |
| MY162780A (en) | 2010-09-01 | 2017-07-14 | Bayer Ip Gmbh | N-(Tetrazol-5-yl)- and N-(triazol-5-yl)arylcarboxamides and use thereof as herbicides |
| CN105399831A (zh) | 2010-10-29 | 2016-03-16 | 伊缪诺金公司 | 非拮抗性egfr结合分子及其免疫偶联物 |
| CN103269712B (zh) * | 2010-11-03 | 2016-09-21 | 伊缪诺金公司 | 包含新型安丝菌素衍生物的细胞毒性剂 |
| JP6215194B2 (ja) | 2011-05-16 | 2017-10-18 | コーニンクレッカ フィリップス エヌ ヴェＫｏｎｉｎｋｌｉｊｋｅ Ｐｈｉｌｉｐｓ Ｎ．Ｖ． | 生体直交型薬物活性化 |
| KR20140037105A (ko) | 2011-05-27 | 2014-03-26 | 암브룩스, 인코포레이티드 | 비-천연 아미노산 연결된 돌라스타틴 유도체를 함유하는 조성물, 이를 수반하는 방법, 및 용도 |
| US8815226B2 (en) | 2011-06-10 | 2014-08-26 | Mersana Therapeutics, Inc. | Protein-polymer-drug conjugates |
| CN103648532A (zh) * | 2011-06-21 | 2014-03-19 | 伊缪诺金公司 | 具有肽连接子的新型美登木素生物碱衍生物及其偶联物 |
| CA2850096C (en) | 2011-10-14 | 2018-07-03 | Spirogen Sarl | Synthesis method and intermediates useful in the preparation of pyrrolobenzodiazepines |
| ES2945932T3 (es) | 2011-10-14 | 2023-07-10 | Seagen Inc | Pirrolobenzodiazepinas y conjugados dirigidos |
| WO2013055993A1 (en) | 2011-10-14 | 2013-04-18 | Seattle Genetics, Inc. | Pyrrolobenzodiazepines and targeted conjugates |
| CA2850103C (en) | 2011-10-14 | 2019-09-10 | Spirogen Sarl | Pyrrolobenzodiazepines |
| WO2013068874A1 (en) | 2011-11-11 | 2013-05-16 | Pfizer Inc. | Antibody-drug conjugates |
| CN104244718A (zh) | 2011-12-05 | 2014-12-24 | 伊格尼卡生物治疗公司 | 抗体-药物缀合物以及相关化合物、组合物和方法 |
| GB201210770D0 (en) | 2012-06-18 | 2012-08-01 | Polytherics Ltd | Novel conjugation reagents |
| MX2014015682A (es) | 2012-06-19 | 2015-07-23 | Polytherics Ltd | Proceso novedoso para preparacion de conjugados de anticuerpo y conjugados de anticuerpo novedosos. |
| FI2911699T4 (fi) | 2012-10-23 | 2025-12-09 | Synaffix Bv | Muokattu vasta-aine, vasta-ainekonjugaatti ja menetelmä niiden valmistamiseksi |
| NO2789793T3 (https=) | 2012-10-24 | 2018-01-27 | ||
| US10131682B2 (en) | 2012-11-24 | 2018-11-20 | Hangzhou Dac Biotech Co., Ltd. | Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules |
| TW201425336A (zh) | 2012-12-07 | 2014-07-01 | Amgen Inc | Ｂｃｍａ抗原結合蛋白質 |
| CN104688740A (zh) * | 2012-12-21 | 2015-06-10 | 百奥泰生物科技(广州)有限公司 | 类美登素衍生物及其制备方法和用途 |
| CN103254213B (zh) | 2012-12-21 | 2015-02-25 | 百奥泰生物科技(广州)有限公司 | 类美登素酯的制备方法及用于所述方法的组合物 |
| EP2764866A1 (en) * | 2013-02-07 | 2014-08-13 | IP Gesellschaft für Management mbH | Inhibitors of nedd8-activating enzyme |
| MX379256B (es) | 2013-03-15 | 2025-03-10 | Regeneron Pharma | Moleculas biologicamente activas, conjugados de las mismas, y usos terapeuticos. |
| CN103254311B (zh) | 2013-05-09 | 2015-05-13 | 齐鲁制药有限公司 | 一种制备抗体-美登素类生物碱药物偶联物的方法 |
| WO2014194030A2 (en) | 2013-05-31 | 2014-12-04 | Immunogen, Inc. | Conjugates comprising cell-binding agents and cytotoxic agents |
| WO2014197871A2 (en) | 2013-06-06 | 2014-12-11 | Igenica Biotherapeutics, Inc. | Antibody-drug conjugates, compositions and methods of use |
| SG11201509982UA (https=) | 2013-06-06 | 2016-04-28 | Igenica Biotherapeutics Inc | |
| US11229711B2 (en) | 2013-06-06 | 2022-01-25 | Magenta Therapeutics, Inc. | Linkers for antibody-drug conjugates and related compounds, compositions, and methods of use |
| US10781259B2 (en) | 2013-06-06 | 2020-09-22 | Magenta Therapeutics, Inc. | Modified antibodies and related compounds, compositions, and methods of use |
| US9545451B2 (en) | 2013-08-21 | 2017-01-17 | Regeneron Pharmaceuticals, Inc. | Anti-PRLR antibodies and methods for killing PRLR-expressing cells |
| KR102252925B1 (ko) | 2013-08-26 | 2021-05-18 | 리제너론 파마슈티칼스 인코포레이티드 | 마크롤라이드 디아스테레오머를 포함하는 약제학적 조성물, 이의 합성 방법 및 치료학적 용도 |
| WO2015081282A1 (en) | 2013-11-27 | 2015-06-04 | Redwood Bioscience, Inc. | Hydrazinyl-pyrrolo compounds and methods for producing a conjugate |
| US9562059B2 (en) | 2013-12-02 | 2017-02-07 | Hong Kong Baptist University | Anticancer maytansinoids with two fused macrocyclic rings |
| CA2950155C (en) | 2014-06-02 | 2021-11-23 | Regeneron Pharmaceuticals, Inc. | Biologically active molecule conjugates, reagents and methods of manufacture, and therapeutic uses |
| EA034950B1 (ru) | 2015-03-27 | 2020-04-09 | Регенерон Фармасьютикалз, Инк. | Производные майтанзиноида, их конъюгаты и способы использования |
| WO2017132173A1 (en) | 2016-01-25 | 2017-08-03 | Regeneron Pharmaceuticals, Inc. | Maytansinoid derivatives, conjugates thereof, and methods of use |
| MX2019003325A (es) | 2016-09-23 | 2019-08-05 | Regeneron Pharma | Anticuerpos anti-steap2, conjugados anticuerpo-farmaco, y moleculas de fijacion al antigeno biespecificas que se fijan a steap2 y cd3, y usos de estos. |
| US11814428B2 (en) | 2019-09-19 | 2023-11-14 | Regeneron Pharmaceuticals, Inc. | Anti-PTCRA antibody-drug conjugates and uses thereof |
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2017
- 2017-01-24 WO PCT/US2017/014782 patent/WO2017132173A1/en not_active Ceased
- 2017-01-24 MY MYPI2018001339A patent/MY198605A/en unknown
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- 2017-01-24 EP EP17704134.0A patent/EP3408271B1/en active Active
- 2017-01-24 EA EA201800444A patent/EA039072B9/ru unknown
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- 2017-01-24 CN CN202210104739.1A patent/CN114478801A/zh active Pending
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