SG11201400770SA - Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates - Google Patents

Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates

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Publication number
SG11201400770SA
SG11201400770SA SG11201400770SA SG11201400770SA SG11201400770SA SG 11201400770S A SG11201400770S A SG 11201400770SA SG 11201400770S A SG11201400770S A SG 11201400770SA SG 11201400770S A SG11201400770S A SG 11201400770SA SG 11201400770S A SG11201400770S A SG 11201400770SA
Authority
SG
Singapore
Prior art keywords
pyrrolobenzodiazepines
inclusion
pbd compounds
targeted conjugates
dimeric pbd
Prior art date
Application number
SG11201400770SA
Other languages
English (en)
Inventor
Philip Wilson Howard
Original Assignee
Spirogen Sarl
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Spirogen Sarl filed Critical Spirogen Sarl
Publication of SG11201400770SA publication Critical patent/SG11201400770SA/en

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    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
    • C07D487/04—Ortho-condensed systems
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    • A61K47/50—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates
    • A61K47/51—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent
    • A61K47/54—Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient the non-active ingredient being chemically bound to the active ingredient, e.g. polymer-drug conjugates the non-active ingredient being a modifying agent the modifying agent being an organic compound
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SG11201400770SA 2011-09-20 2012-09-20 Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates SG11201400770SA (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201161536669P 2011-09-20 2011-09-20
PCT/EP2012/068506 WO2013041606A1 (en) 2011-09-20 2012-09-20 Pyrrolobenzodiazepines as unsymmetrical dimeric pbd compounds for inclusion in targeted conjugates

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SG11201400770SA true SG11201400770SA (en) 2014-04-28

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* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
CN103068405A (zh) 2010-04-15 2013-04-24 西雅图基因公司 靶向吡咯并苯并二氮杂卓结合物
MX368648B (es) 2010-04-15 2019-10-09 Seattle Genetics Inc Pirrolobenzodiazepinas usadas para tratar enfermedades proliferativas.
US9399641B2 (en) 2011-09-20 2016-07-26 Medimmune Limited Pyrrolobenzodiazepines as unsymmetrical dimeric PBD compounds for inclusion in targeted conjugates
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
CA2850375C (en) 2011-10-14 2019-07-02 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
AU2012322934B2 (en) 2011-10-14 2016-09-08 Medimmune Limited Pyrrolobenzodiazepines
CA2850264C (en) 2011-10-14 2019-11-05 Medimmune Limited Pyrrolobenzodiazepines
CN104520324A (zh) 2012-02-24 2015-04-15 施特姆森特Rx股份有限公司 Dll3调节剂及其使用方法
PT2906248T (pt) 2012-10-12 2019-03-04 Medimmune Ltd Pirrolobenzodiazepinas e conjugados das mesmas
KR101995620B1 (ko) 2012-10-12 2019-07-03 에이디씨 테라퓨틱스 에스에이 피롤로벤조디아제핀-항체 컨주게이트
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
DK2906298T3 (en) 2012-10-12 2018-12-17 Adc Therapeutics Sa Pyrrolobenzodiazepine-antibody conjugates
BR112015008238A2 (pt) 2012-10-12 2017-11-28 Adc Therapeutics Sarl conjugados de pirrolbenzodiazepina-anticorpo anti-cd22
DK2839860T3 (da) 2012-10-12 2019-06-17 Medimmune Ltd Pyrrolobenzodiazepiner og konjugater deraf
EP2906249B1 (en) 2012-10-12 2018-06-27 MedImmune Limited Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
WO2014057114A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sàrl Pyrrolobenzodiazepine-anti-psma antibody conjugates
PT2906253T (pt) 2012-10-12 2018-11-05 Medimmune Ltd Conjugados de anticorpo anti-psma de pirrolobenzodiazepina
AU2013366493B2 (en) 2012-12-21 2017-08-24 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
ES2731681T3 (es) 2013-02-22 2019-11-18 Abbvie Stemcentrx Llc Conjugados de anticuerpo anti-DLL3 y PBD y usos de los mismos
KR102066318B1 (ko) 2013-03-13 2020-01-14 메디뮨 리미티드 피롤로벤조디아제핀 및 그의 컨쥬게이트
MX363787B (es) 2013-03-13 2019-04-03 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de los mismos.
JP2016531915A (ja) 2013-08-28 2016-10-13 ステムセントリックス， インコーポレイテッド 部位特異的抗体コンジュゲーション方法および組成物
WO2015028850A1 (en) * 2013-09-02 2015-03-05 Hangzhou Dac Biotech Co., Ltd Novel cytotoxic agents for conjugation of drugs to cell binding molecule
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
GB201317981D0 (en) * 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052534A1 (en) * 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
US10010624B2 (en) 2013-10-11 2018-07-03 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
WO2015052535A1 (en) * 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
WO2015052533A1 (en) * 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
PT3057585T (pt) 2013-10-15 2020-10-21 Seagen Inc Fármaco-ligadores peguilados para farmacocinética melhorada de conjugados de fármaco-ligando
UA118113C2 (uk) * 2013-12-16 2018-11-26 Дженентек, Інк. Пептидоміметичні сполуки та їх кон'югати антитіла з лікарським засобом
BR112016014126B1 (pt) * 2013-12-16 2023-02-14 Medimmune Limited Composto não-peptídico, conjugados de anticorpo-fármaco do mesmo, uso dos ditos conjugados para o tratamento de câncer e composição farmacêutica que compreende os mesmos
SG11201605437YA (en) 2014-01-27 2016-08-30 Pfizer Bifunctional cytotoxic agents
EP3107576A4 (en) 2014-02-21 2017-09-06 Abbvie Stemcentrx LLC Anti-dll3 antibodies and drug conjugates for use in melanoma
SG11201607818WA (en) 2014-03-20 2016-10-28 Bristol Myers Squibb Co Stabilized fibronectin based scaffold molecules
EP3193940A1 (en) 2014-09-10 2017-07-26 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
SI3191135T1 (sl) 2014-09-12 2021-01-29 Genentech, Inc. Anti-HER2 protitelesa in imunokonjugati
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
ES2826566T3 (es) 2014-11-21 2021-05-18 Bristol Myers Squibb Co Anticuerpos que comprenden regiones constantes pesadas modificadas
JP6805142B2 (ja) 2014-11-21 2020-12-23 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ Ｃｄ７３に対する抗体およびその使用
CN107148285B (zh) 2014-11-25 2022-01-04 Adc治疗股份有限公司 吡咯并苯并二氮杂䓬-抗体缀合物
JP6622814B2 (ja) 2014-11-25 2019-12-18 ブリストル−マイヤーズ スクイブ カンパニーＢｒｉｓｔｏｌ−Ｍｙｅｒｓ Ｓｑｕｉｂｂ Ｃｏｍｐａｎｙ イメージングのための新規ｐｄ−ｌ１結合ポリペプチド
CN107231804B (zh) 2015-01-14 2019-11-26 百时美施贵宝公司 亚杂芳基桥连苯并二氮杂*二聚体、其缀合物及制备和使用方法
TW201632531A (zh) 2015-01-14 2016-09-16 必治妥美雅史谷比公司 苯二氮呯二聚物，其結合物及製造與使用方法
ES2736106T3 (es) 2015-03-10 2019-12-26 Bristol Myers Squibb Co Anticuerpos que se pueden conjugar mediante la transglutaminasa y conjugados producidos a partir de ellos
KR102046862B1 (ko) 2015-03-20 2019-11-20 화이자 인코포레이티드 Cti 약물작용발생단을 함유하는 이관능성 세포독성제
GB201506411D0 (en) 2015-04-15 2015-05-27 Bergenbio As Humanized anti-axl antibodies
GB201506389D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
AU2016271111B2 (en) 2015-05-29 2022-04-28 Bristol-Myers Squibb Company Antibodies against OX40 and uses thereof
US10017577B2 (en) 2015-06-15 2018-07-10 Genentech, Inc. Antibodies and immunoconjugates
AU2016284340A1 (en) 2015-06-23 2018-02-08 Bristol-Myers Squibb Company Macrocyclic benzodiazepine dimers, conjugates thereof, preparation and uses
EP3353198B1 (en) 2015-09-23 2020-06-17 Bristol-Myers Squibb Company Glypican-3binding fibronectin based scafflold molecules
CR20180243A (es) 2015-10-02 2018-07-31 Genentech Inc Conjugados de anticuerpo-fármaco de pirrolobenzodiazepina y métodos de uso
EP3394096A1 (en) 2015-12-21 2018-10-31 Bristol-Myers Squibb Company Variant antibodies for site-specific conjugation
GB201601431D0 (en) 2016-01-26 2016-03-09 Medimmune Ltd Pyrrolobenzodiazepines
GB201602359D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
GB201602356D0 (en) 2016-02-10 2016-03-23 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
AU2017228470A1 (en) 2016-03-04 2018-08-30 Bristol-Myers Squibb Company Combination therapy with anti-CD73 antibodies
EP3433278A4 (en) 2016-03-25 2019-11-06 Seattle Genetics, Inc. METHOD FOR THE PRODUCTION OF PEGYLATED ACTIVE LINKERS AND INTERMEDIATE PRODUCTS THEREOF
GB201607478D0 (en) 2016-04-29 2016-06-15 Medimmune Ltd Pyrrolobenzodiazepine Conjugates
WO2017201132A2 (en) 2016-05-18 2017-11-23 Mersana Therapeutics, Inc. Pyrrolobenzodiazepines and conjugates thereof
US10526294B2 (en) 2016-06-24 2020-01-07 Mersana Therapeutics, Inc. Pyrrolobenzodiazepines and conjugates thereof
US20190218294A1 (en) 2016-09-09 2019-07-18 Bristol-Myers Squibb Company Use of an anti-pd-1 antibody in combination with an anti-mesothelin antibody in cancer treatment
CN110049780A (zh) 2016-10-10 2019-07-23 塞勒兰特治疗公司 异喹啉并苯并二氮杂卓(iqb)-1(氯甲基)-2,3-二氢-1h-苯并[e]吲哚(cbi)二聚体
GB201617466D0 (en) 2016-10-14 2016-11-30 Medimmune Ltd Pyrrolobenzodiazepine conjugates
GB201702031D0 (en) 2017-02-08 2017-03-22 Medlmmune Ltd Pyrrolobenzodiazepine-antibody conjugates
RS61795B1 (sr) 2017-02-08 2021-06-30 Adc Therapeutics Sa Konjugati pirolobenzodiazepin antitela
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
SMT202200490T1 (it) 2017-04-18 2023-01-13 Medimmune Ltd Coniugati di pirrolobenzodiazepina
WO2018193102A1 (en) 2017-04-20 2018-10-25 Adc Therapeutics Sa Combination therapy with an anti-axl antibody-drug conjugate
MX2019013132A (es) 2017-05-25 2020-01-27 Bristol Myers Squibb Co Anticuerpos que comprenden regiones constantes pesadas modificadas.
KR102442736B1 (ko) 2017-06-14 2022-09-16 에이디씨 테라퓨틱스 에스에이 항-cd19 adc의 투여를 위한 투약량 체제
SI3668874T1 (sl) 2017-08-18 2022-04-29 Medimmune Limited Pirolobenzodiazepinski konjugati
CA3177215C (en) 2017-09-29 2026-06-09 Daiichi Sankyo Company, Limited Antibody-pyrrolobenzodiazepine derivative conjugate
ES2920123T3 (es) 2017-11-14 2022-08-01 Medimmune Ltd Conjugados de pirrolobenzodiazepina
US11638760B2 (en) 2017-11-27 2023-05-02 Mersana Therapeutics, Inc. Pyrrolobenzodiazepine antibody conjugates
CN111757757A (zh) 2017-12-21 2020-10-09 梅尔莎纳医疗公司 吡咯并苯并二氮呯抗体共轭物
GB201803342D0 (en) 2018-03-01 2018-04-18 Medimmune Ltd Methods
MX2020010110A (es) 2018-03-28 2020-11-06 Mitsubishi Tanabe Pharma Corp Conjugados de farmacos de agentes de union monoclonales de cmet, y usos de los mismos.
GB201806022D0 (en) * 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
JP2022513653A (ja) 2018-11-28 2022-02-09 ブリストル－マイヤーズ スクイブ カンパニー 修飾された重鎖定常領域を含む抗体
DK3886914T3 (da) 2018-11-30 2023-07-03 Bristol Myers Squibb Co Antistof omfattende en glutaminholdig letkæde-c-terminal forlængelse, konjugater deraf og fremgangsmåder samt anvendelser
WO2020123425A2 (en) 2018-12-12 2020-06-18 Bristol-Myers Squibb Company Antibodies modified for transglutaminase conjugation, conjugates thereof, and methods and uses
CN113631560B (zh) 2019-03-15 2025-02-18 麦迪穆有限责任公司 氮杂环丁烷并苯并二氮杂䓬二聚体和用于治疗癌症的包含它们的缀合物
US20240377413A1 (en) 2019-09-16 2024-11-14 Bristol-Myers Squibb Company Dual capture method for analysis of antibody-drug conjugates
WO2021080608A1 (en) 2019-10-25 2021-04-29 Medimmune, Llc Branched moiety for use in conjugates
AU2023298568A1 (en) 2022-06-30 2025-01-09 Toray Industries, Inc. Pharmaceutical composition for cancer treatment and/or prevention

Family Cites Families (119)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3361742A (en) 1964-12-07 1968-01-02 Hoffmann La Roche 5-oxo-1h-pyrrolo-[2, 1-c][1, 4]-benzodiazepin-2-crylamides
US3523941A (en) 1967-03-06 1970-08-11 Hoffmann La Roche Benzodiazepine compounds and process for their preparation
US3524849A (en) 1967-10-27 1970-08-18 Hoffmann La Roche Process for the preparation of pyrrolo-benzodiazepine acrylamides and intermediates useful therein
JPS4843755B1 (enExample) 1969-06-26 1973-12-20
IL33558A (en) 1968-12-30 1973-10-25 Fujisawa Pharmaceutical Co Antibiotic pyrrolo-benzodiazepine compound,its derivatives and processes for their production
DE1965304A1 (de) 1968-12-30 1970-07-23 Fujisawa Pharmaceutical Co Benzdiazepinon-Verbindungen und Verfahren zu ihrer Herstellung
JPS5382792U (enExample) 1976-12-10 1978-07-08
JPS585916B2 (ja) 1977-12-27 1983-02-02 株式会社ミドリ十字 新規ベンゾジアゼピン系化合物
JPS5615289A (en) 1979-07-17 1981-02-14 Green Cross Corp:The Novel benzodiazepinnbased compound 3
JPH0353356Y2 (enExample) 1981-02-06 1991-11-21
CA1184175A (en) 1981-02-27 1985-03-19 Walter Hunkeler Imidazodiazepines
CA1185602A (en) 1981-02-27 1985-04-16 Emilio Kyburz Imidazodiazepines
CA1173441A (en) 1981-02-27 1984-08-28 Hoffmann-La Roche Limited Imidazodiazepines
JPS58180487A (ja) 1982-04-16 1983-10-21 Kyowa Hakko Kogyo Co Ltd 抗生物質ｄｃ−８１およびその製造法
JPS58180487U (ja) 1982-05-28 1983-12-02 松下電工株式会社 光線式報知器の組立体
US4427588A (en) 1982-11-08 1984-01-24 Bristol-Myers Company Process for conversion of oxotomaymycin to tomaymycin
US4427587A (en) 1982-11-10 1984-01-24 Bristol-Myers Company Total synthesis of antitumor antibiotics BBM-2040A and BBM-2040B
JPS59152329A (ja) 1983-02-17 1984-08-31 Green Cross Corp:The 局所障害抑制剤
FR2586683B1 (fr) 1985-08-29 1988-07-01 Centre Nat Rech Scient Nouveaux derives de neothramycine, leur procede de preparation et leur application en tant que medicaments
JP2660201B2 (ja) 1988-08-05 1997-10-08 塩野義製薬株式会社 新規ピロロ［１，４］ベンゾジアゼピン誘導体および老人性痴呆薬
FR2676230B1 (fr) 1991-05-07 1993-08-27 Centre Nat Rech Scient Nouveaux derives de pyrrolo [1,4]-benzodiazepines, leur procede de preparation et medicaments les contenant.
GB9205051D0 (en) 1992-03-09 1992-04-22 Cancer Res Campaign Tech Pyrrolobenzodiazepine derivatives,their preparation,and compositions containing them
FR2696176B1 (fr) 1992-09-28 1994-11-10 Synthelabo Dérivés de pipéridine, leur préparation et leur application en thérapeutique.
US6214345B1 (en) 1993-05-14 2001-04-10 Bristol-Myers Squibb Co. Lysosomal enzyme-cleavable antitumor drug conjugates
GB9316162D0 (en) 1993-08-04 1993-09-22 Zeneca Ltd Fungicides
WO2000003291A1 (en) 1998-07-08 2000-01-20 E Ink Corporation Methods for achieving improved color in microencapsulated electrophoretic devices
ES2260570T3 (es) 1998-08-27 2006-11-01 Spirogen Limited Pirrolobenziodiazepinas dimericas.
GB9818731D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Compounds
GB9818732D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Collection of compounds
GB9818730D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Collections of compounds
US6909006B1 (en) 1999-08-27 2005-06-21 Spirogen Limited Cyclopropylindole derivatives
DE60115265T2 (de) 2000-09-19 2006-08-10 Lee, Moses, Holland Zusammensetzungen und verfahren zur verwendung achiraler analoge von cc-1065 und den duocarmycinen
US6362331B1 (en) 2001-03-30 2002-03-26 Council Of Scientific And Industrial Research Process for the preparation of antitumor agents
US6660856B2 (en) 2002-03-08 2003-12-09 Kaohsiung Medical University Synthesis of pyrrolo[2,1-c][1,4]benzodiazepine analogues
ES2369542T3 (es) 2002-07-31 2011-12-01 Seattle Genetics, Inc. Conjugados de auristatina y su uso para tratar cáncer, una enfermedad autoinmune o una enfermedad infecciosa.
US20040138269A1 (en) 2002-10-11 2004-07-15 Sugen, Inc. Substituted pyrroles as kinase inhibitors
GB0226593D0 (en) 2002-11-14 2002-12-24 Consultants Ltd Compounds
ATE421967T1 (de) 2003-03-31 2009-02-15 Council Scient Ind Res Nichtvernetzende pyrroloä2,1-cüä1, 4übenzodiazepine als potentielle antitumor- agentien und ihre herstellung
GB0321295D0 (en) 2003-09-11 2003-10-15 Spirogen Ltd Synthesis of protected pyrrolobenzodiazepines
GB0416511D0 (en) 2003-10-22 2004-08-25 Spirogen Ltd Pyrrolobenzodiazepines
AU2004284075A1 (en) 2003-10-22 2005-05-06 Government Of The United States Of America, Represented By The Secretary, Department Of Health And Human Services Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto
ES2605443T3 (es) 2003-11-06 2017-03-14 Seattle Genetics, Inc. Conjugados de auristatina con anticuerpos anti-HER2 o anti-CD22 y su uso en terapia
CA2556752C (en) 2004-02-23 2016-02-02 Genentech, Inc. Heterocyclic self-immolative linkers and conjugates
GB0404574D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Amino acids
ES2398975T3 (es) 2004-03-01 2013-03-25 Spirogen Sàrl Derivados de 11-hidroxi-5H-pirrolo[2,1-c][1,4]benzodiazepin-5-ona como intermedios clave para la preparación de pirrolobenzodiazepinas sustituidas en C2
GB0404577D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Pyrrolobenzodiazepines
GB0404578D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Pyrrolobenzodiazepines
DE102004010943A1 (de) 2004-03-03 2005-09-29 Degussa Ag Verfahren zur Herstellung von N-geschützten 4-Ketprolinderivaten
EP1723152B1 (en) 2004-03-09 2015-02-11 Spirogen Sàrl Pyrrolobenzodiazepines
FR2869231B1 (fr) 2004-04-27 2008-03-14 Sod Conseils Rech Applic Composition therapeutique contenant au moins un derive de la pyrrolobenzodiazepine et la fludarabine
GB0410725D0 (en) 2004-05-13 2004-06-16 Spirogen Ltd Pyrrolobenzodiazepine therapeutic agents
TR201808537T4 (tr) 2004-09-23 2018-07-23 Genentech Inc Sistein değiştirilmiş antikorlar ve konjugatlar.
WO2006068325A2 (en) 2004-12-24 2006-06-29 Showa Denko K. K. Production method of thermoelectric semiconductor alloy, thermoelectric conversion module and thermoelectric power generating device
US8067546B2 (en) 2005-04-19 2011-11-29 Seattle Genetics, Inc. Humanized anti-CD70 binding agents and uses thereof
ES2338696T3 (es) 2005-04-21 2010-05-11 Spirogen Limited Pirrolobenzodiazepinas.
DE602006006199D1 (de) 2005-10-05 2009-05-20 Spirogen Ltd 4-ä4-(5-oxo-2,3,5,11a-tetrahydro-5h-pyrrolo ä2, 1-cüä1,4übenzodiazepin-8-yloxy)-butyrylaminoü-1h-pyrrol-2-carbonsäurealkylesterderivate und verwandte verbindung zur behandlung einer proliferativen erkrankung
US20070154906A1 (en) 2005-10-05 2007-07-05 Spirogen Ltd. Methods to identify therapeutic candidates
DK1813614T3 (da) 2006-01-25 2012-01-23 Sanofi Sa Cytotoksiske midler, der omfatter nye tomaymycinderivater
ZA200900545B (en) 2006-07-18 2010-03-31 Sanofi Aventis Antagonist antibody against EPHA2 for the treatment of cancer
EP1914242A1 (en) 2006-10-19 2008-04-23 Sanofi-Aventis Novel anti-CD38 antibodies for the treatment of cancer
WO2008050140A2 (en) 2006-10-27 2008-05-02 Spirogen Limited Compounds for treatment of parasitic infection
PL2099823T5 (pl) 2006-12-01 2023-02-20 Seagen Inc. Wariant środków wiążących cel i jego zastosowania
US8465883B2 (en) 2007-07-11 2013-06-18 The Regents Of The University Of California Nanostructured polymer membranes for proton conduction
PT2019104E (pt) 2007-07-19 2013-12-03 Sanofi Sa Agentes citotóxicos compreendendo novos derivados de tomaimicina e sua utilização terapêutica
GB0722088D0 (en) 2007-11-09 2007-12-19 Spirogen Ltd Pyrrolobenzodiazepines
GB0722087D0 (en) 2007-11-09 2007-12-19 Spirogen Ltd Polyamides
WO2009117531A1 (en) * 2008-03-18 2009-09-24 Seattle Genetics, Inc. Auristatin drug linker conjugates
GB0813432D0 (en) 2008-07-22 2008-08-27 Spirogen Ltd Pyrrolobenzodiazepines
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
GB0819097D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
CA3014224C (en) 2009-02-05 2022-05-24 Immunogen, Inc. Condensed benzodiazepine-indoline derivatives and processes to prepare said derivatives
FR2949469A1 (fr) 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
CA2775350A1 (en) 2009-09-24 2011-03-31 Seattle Genetics, Inc. Dr5 ligand drug conjugates
US9040526B2 (en) 2010-02-09 2015-05-26 Bristol-Myers Squibb Company Benzylpyrrolidinone derivatives as modulators of chemokine receptor activity
MX368648B (es) 2010-04-15 2019-10-09 Seattle Genetics Inc Pirrolobenzodiazepinas usadas para tratar enfermedades proliferativas.
CN103068405A (zh) 2010-04-15 2013-04-24 西雅图基因公司 靶向吡咯并苯并二氮杂卓结合物
PT2528625E (pt) 2010-04-15 2013-10-17 Spirogen Sarl Pirrolobenzodiazepinas e conjugados das mesmas
GB201006340D0 (en) 2010-04-15 2010-06-02 Spirogen Ltd Synthesis method and intermediates
SI2675480T1 (sl) 2011-02-15 2019-05-31 Immunogen, Inc. Metode priprave konjugatov
DK2707031T3 (da) * 2011-05-08 2019-10-07 Legochem Biosciences Inc Protein-active agent conjugates and method for preparing the same
US9399641B2 (en) 2011-09-20 2016-07-26 Medimmune Limited Pyrrolobenzodiazepines as unsymmetrical dimeric PBD compounds for inclusion in targeted conjugates
KR101495215B1 (ko) * 2011-09-29 2015-02-25 다우 코닝 도레이 캄파니 리미티드 경화성 실리콘 조성물 및 이의 경화물
CA2850264C (en) 2011-10-14 2019-11-05 Medimmune Limited Pyrrolobenzodiazepines
AU2012322934B2 (en) 2011-10-14 2016-09-08 Medimmune Limited Pyrrolobenzodiazepines
JP6166728B2 (ja) 2011-10-14 2017-07-19 メドイミューン・リミテッドＭｅｄＩｍｍｕｎｅ Ｌｉｍｉｔｅｄ ピロロベンゾジアゼピンの製造に有用な合成方法及び中間体
CA2850373C (en) 2011-10-14 2019-07-16 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
JP6104257B2 (ja) 2011-10-14 2017-03-29 メドイミューン・リミテッドMedImmune Limited ピロロベンゾジアゼピンおよびそのコンジュゲート
CA2850375C (en) 2011-10-14 2019-07-02 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
IN2014MN02175A (enExample) 2012-04-30 2015-08-28 Ucl Business Plc
IN2014MN02092A (enExample) 2012-04-30 2015-09-04 Spirogen Sarl
BR112015000437A2 (pt) 2012-07-09 2017-06-27 Genentech Inc imunoconjugados, formulação farmacêutica, métodos de tratamento e de inbir a proliferação de uma célula
KR20150027829A (ko) 2012-07-09 2015-03-12 제넨테크, 인크. 항-cd22 항체를 포함하는 면역접합체
BR112015002193A2 (pt) 2012-08-02 2017-07-04 Genentech Inc anticorpos anti-etbr e imunoconjugados
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
DK2906298T3 (en) 2012-10-12 2018-12-17 Adc Therapeutics Sa Pyrrolobenzodiazepine-antibody conjugates
DK2839860T3 (da) 2012-10-12 2019-06-17 Medimmune Ltd Pyrrolobenzodiazepiner og konjugater deraf
PT2906252T (pt) 2012-10-12 2017-09-19 Medimmune Ltd Conjugados de anticorpo anti-her2 de pirrolobenzodiazepina
WO2014057114A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sàrl Pyrrolobenzodiazepine-anti-psma antibody conjugates
EP2906249B1 (en) 2012-10-12 2018-06-27 MedImmune Limited Synthesis and intermediates of pyrrolobenzodiazepine derivatives for conjugation
KR101995620B1 (ko) 2012-10-12 2019-07-03 에이디씨 테라퓨틱스 에스에이 피롤로벤조디아제핀-항체 컨주게이트
WO2014057118A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sarl Pyrrolobenzodiazepine-anti-cd22 antibody conjugates
BR112015008238A2 (pt) 2012-10-12 2017-11-28 Adc Therapeutics Sarl conjugados de pirrolbenzodiazepina-anticorpo anti-cd22
PT2906248T (pt) 2012-10-12 2019-03-04 Medimmune Ltd Pirrolobenzodiazepinas e conjugados das mesmas
PT2906253T (pt) 2012-10-12 2018-11-05 Medimmune Ltd Conjugados de anticorpo anti-psma de pirrolobenzodiazepina
AU2013366493B2 (en) 2012-12-21 2017-08-24 Medimmune Limited Pyrrolobenzodiazepines and conjugates thereof
US9567340B2 (en) 2012-12-21 2017-02-14 Medimmune Limited Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
ES2731681T3 (es) 2013-02-22 2019-11-18 Abbvie Stemcentrx Llc Conjugados de anticuerpo anti-DLL3 y PBD y usos de los mismos
ES2687439T3 (es) 2013-03-13 2018-10-25 Medimmune Limited Pirrolobenzodiazepinas y conjugados de las mismas
KR102066318B1 (ko) 2013-03-13 2020-01-14 메디뮨 리미티드 피롤로벤조디아제핀 및 그의 컨쥬게이트
MX363787B (es) 2013-03-13 2019-04-03 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de los mismos.
US20160106861A1 (en) 2013-04-26 2016-04-21 Spirogen Sarl Axl antibody-drug conjugate and its use for the treatment of cancer
GB201317981D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052533A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
WO2015052535A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
US10010624B2 (en) 2013-10-11 2018-07-03 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052534A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
BR112016014126B1 (pt) 2013-12-16 2023-02-14 Medimmune Limited Composto não-peptídico, conjugados de anticorpo-fármaco do mesmo, uso dos ditos conjugados para o tratamento de câncer e composição farmacêutica que compreende os mesmos
GB201406767D0 (en) 2014-04-15 2014-05-28 Cancer Rec Tech Ltd Humanized anti-Tn-MUC1 antibodies anf their conjugates

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CA2849039A1 (en) 2013-03-28
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CA2849039C (en) 2018-09-18
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KR20140064961A (ko) 2014-05-28
US20150158869A1 (en) 2015-06-11
EP2751120A1 (en) 2014-07-09
BR112014006703A8 (pt) 2018-01-09
KR101860174B1 (ko) 2018-05-21
CN103987718A (zh) 2014-08-13
MX341524B (es) 2016-08-24
EA027971B1 (ru) 2017-09-29
AU2012311505A1 (en) 2014-05-01
EP2751120B1 (en) 2018-08-22
JP2014527974A (ja) 2014-10-23
AU2012311505B2 (en) 2016-09-29
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BR112014006703A2 (pt) 2017-04-11
EA201490518A1 (ru) 2014-08-29

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