JP6170494B2 - ピロロベンゾジアゼピン - Google Patents

ピロロベンゾジアゼピン Download PDF

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Publication number
JP6170494B2
JP6170494B2 JP2014531224A JP2014531224A JP6170494B2 JP 6170494 B2 JP6170494 B2 JP 6170494B2 JP 2014531224 A JP2014531224 A JP 2014531224A JP 2014531224 A JP2014531224 A JP 2014531224A JP 6170494 B2 JP6170494 B2 JP 6170494B2
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JP2014527974A5 (enExample
JP2014527974A (ja
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フィリップ・ウィルソン・ハワード
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MedImmune Ltd
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MedImmune Ltd
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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D487/00Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
    • C07D487/02Heterocyclic 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
    • C07D487/04Ortho-condensed systems
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    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00Medicinal preparations characterised by the non-active ingredients used, e.g. carriers or inert additives; Targeting or modifying agents chemically bound to the active ingredient
    • A61K47/50Medicinal 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
    • A61K47/51Medicinal 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
    • A61K47/54Medicinal 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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  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
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  • General Chemical & Material Sciences (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Diabetes (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Pulmonology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Dermatology (AREA)
  • Hematology (AREA)
  • Endocrinology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Rheumatology (AREA)
  • Neurology (AREA)
  • Urology & Nephrology (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Vascular Medicine (AREA)
  • Neurosurgery (AREA)
  • Emergency Medicine (AREA)
  • Obesity (AREA)
JP2014531224A 2011-09-20 2012-09-20 ピロロベンゾジアゼピン Expired - Fee Related JP6170494B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201161536669P 2011-09-20 2011-09-20
US61/536,669 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

Publications (3)

Publication Number Publication Date
JP2014527974A JP2014527974A (ja) 2014-10-23
JP2014527974A5 JP2014527974A5 (enExample) 2015-11-12
JP6170494B2 true JP6170494B2 (ja) 2017-07-26

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US (1) US9399641B2 (enExample)
EP (1) EP2751120B1 (enExample)
JP (1) JP6170494B2 (enExample)
KR (1) KR101860174B1 (enExample)
CN (1) CN103987718A (enExample)
AU (1) AU2012311505B2 (enExample)
BR (1) BR112014006703A8 (enExample)
CA (1) CA2849039C (enExample)
EA (1) EA027971B1 (enExample)
MX (1) MX341524B (enExample)
SG (1) SG11201400770SA (enExample)
WO (1) WO2013041606A1 (enExample)

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Publication number Priority date Publication date Assignee Title
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
JP5875083B2 (ja) 2010-04-15 2016-03-02 メディミューン リミテッド 増殖性疾患治療用ピロロベンゾジアゼピン
EP2558127B1 (en) 2010-04-15 2022-01-19 Seagen Inc. Targeted pyrrolobenzodiazepine conjugates
KR101860174B1 (ko) 2011-09-20 2018-05-21 메디뮨 리미티드 표적 접합체 내의 내포를 위한 비대칭 이량체 pbd 화합물로서 피롤로벤조디아제핀
EA027386B1 (ru) 2011-10-14 2017-07-31 Медимьюн Лимитед Пирролобензодиазепины
ES2945932T3 (es) 2011-10-14 2023-07-10 Seagen Inc Pirrolobenzodiazepinas y conjugados dirigidos
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
US9387259B2 (en) 2011-10-14 2016-07-12 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
HUE037021T2 (hu) 2012-02-24 2018-08-28 Abbvie Stemcentrx Llc DLL3- modulátorok és eljárások alkalmazásukra
CA2887895C (en) 2012-10-12 2019-10-29 Adc Therapeutics Sarl Pyrrolobenzodiazepine-anti-cd19 antibody conjugates
CN105102004B (zh) 2012-10-12 2019-01-25 Adc疗法责任有限公司 吡咯并苯并二氮杂卓-抗cd22抗体结合物
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
WO2014057114A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sàrl Pyrrolobenzodiazepine-anti-psma antibody conjugates
HUE041274T2 (hu) 2012-10-12 2019-05-28 Adc Therapeutics Sa Pirrolobenzodiazepin-anti-PSMA-antitest konjugátumok
JP6367204B2 (ja) * 2012-10-12 2018-08-01 メドイミューン・リミテッドMedImmune Limited 結合用のピロロベンゾジアゼピン誘導体の合成および中間体
LT2906248T (lt) * 2012-10-12 2019-02-11 Medimmune Limited Pirolobenzodiazepinai ir jų konjugatai
TR201808051T4 (tr) 2012-10-12 2018-06-21 Adc Therapeutics Sa Pirrolobenzodiazepin antikor konjugatları.
SI2766048T1 (sl) 2012-10-12 2015-03-31 Spirogen Sarl Pirolobenzodiazepini in njihovi konjugati
CN110452242A (zh) 2012-12-21 2019-11-15 麦迪穆有限责任公司 吡咯并苯并二氮杂卓及其结合物
CA2894959C (en) * 2012-12-21 2022-01-11 Spirogen Sarl Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
ME03394B (me) * 2013-02-22 2020-01-20 Medimmune Ltd Antidllз-antitelo-pbd konjugati i nihovа upotreba
ES2731779T3 (es) 2013-03-13 2019-11-19 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de las mismas
MX363787B (es) 2013-03-13 2019-04-03 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de los mismos.
KR20160044042A (ko) 2013-08-28 2016-04-22 스템센트알엑스 인코포레이티드 부위-특이적 항체 접합 방법 및 조성물
AU2013399485B2 (en) * 2013-09-02 2019-07-25 Hangzhou Dac Biotech Co., Ltd Novel cytotoxic agents for conjugation of drugs to cell binding molecule
GB201317981D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
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
WO2015052533A1 (en) * 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
EP3054985B1 (en) 2013-10-11 2018-12-26 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
CA3187392A1 (en) 2013-10-15 2015-04-23 Seagen Inc. Pegylated drug-linkers for improved ligand-drug conjugate pharmacokinetics
CN105848685B (zh) * 2013-12-16 2020-09-22 健泰科生物技术公司 拟肽化合物及其抗体药物偶联物
EA201691023A1 (ru) 2013-12-16 2016-10-31 Дженентек, Инк. Пептидомиметические соединения и их конъюгаты антитела с лекарственным средством
JP6236540B2 (ja) 2014-01-27 2017-11-22 ファイザー・インク 二官能性細胞毒性剤
EA201691683A1 (ru) 2014-02-21 2017-04-28 ЭББВИ СТЕМСЕНТРКС ЭлЭлСи Антитела против dll3 и конъюгаты антитело-лекарственное средство для применения при меланоме
WO2015143156A1 (en) 2014-03-20 2015-09-24 Bristol-Myers Squibb Company Stabilized fibronectin based scaffold molecules
JP6531166B2 (ja) 2014-09-10 2019-06-12 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及びそのコンジュゲート
GB201416112D0 (en) 2014-09-12 2014-10-29 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
PT3191135T (pt) 2014-09-12 2020-11-12 Genentech Inc Anticorpos anti-her2 e imunoconjugados
HUE052526T2 (hu) 2014-11-21 2021-05-28 Bristol Myers Squibb Co Antitestek, amelyek tartalmaznak módosított nehéz konstans régiókat
HUE050596T2 (hu) 2014-11-21 2020-12-28 Bristol Myers Squibb Co Antitestek CD73 ellen és azok felhasználásai
CN114591420A (zh) 2014-11-25 2022-06-07 百时美施贵宝公司 用于成像的新型pd-l1结合多肽
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
AU2016206798A1 (en) 2015-01-14 2017-08-31 Bristol-Myers Squibb Company Benzodiazepine dimers, conjugates thereof, and methods of making and using
PE20171185A1 (es) 2015-01-14 2017-08-22 Bristol Myers Squibb Co Dimeros de benzodiazepina unidos con puentes de heteroarileno, conjugados de estos, y sus metodos de preparacion y uso
CN107406496A (zh) 2015-03-10 2017-11-28 百时美施贵宝公司 可通过转谷氨酰胺酶缀合的抗体和由其制备的缀合物
RU2682645C1 (ru) 2015-03-20 2019-03-20 Пфайзер Инк. Бифункциональные цитотоксические агенты, содержащие CTI фармакофор
GB201506402D0 (en) 2015-04-15 2015-05-27 Berkel Patricius H C Van And Howard Philip W Site-specific antibody-drug conjugates
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
CA2987410A1 (en) 2015-05-29 2016-12-08 Bristol-Myers Squibb Company Antibodies against ox40 and uses thereof
WO2016205176A1 (en) 2015-06-15 2016-12-22 Genentech, Inc. Antibodies and immunoconjugates
CN108391434A (zh) 2015-06-23 2018-08-10 百时美施贵宝公司 大环苯并二氮杂*二聚体、其缀合物、制备和用途
EP3733698A1 (en) 2015-09-23 2020-11-04 Bristol-Myers Squibb Company Glypican-3 binding fibronectin based scafflold molecules
MA43345A (fr) 2015-10-02 2018-08-08 Hoffmann La Roche Conjugués anticorps-médicaments de pyrrolobenzodiazépine et méthodes d'utilisation
AU2016377371A1 (en) 2015-12-21 2018-08-09 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
JP2019514844A (ja) 2016-03-04 2019-06-06 ブリストル−マイヤーズ スクイブ カンパニーBristol−Myers Squibb Company 抗cd73抗体を用いた併用療法
US11844839B2 (en) 2016-03-25 2023-12-19 Seagen Inc. Process for the preparation of pegylated drug-linkers and intermediates 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
EP3475284B1 (en) 2016-06-24 2022-11-02 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
EP3544636B1 (en) 2017-02-08 2021-03-31 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
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
JP2020517609A (ja) 2017-04-18 2020-06-18 メディミューン リミテッド ピロロベンゾジアゼピン複合体
ES2977788T3 (es) 2017-04-20 2024-08-30 Adc Therapeutics Sa Terapia combinada con un conjugado de anticuerpo anti-AXL y fármaco
SG10201913206RA (en) 2017-05-25 2020-02-27 Bristol Myers Squibb Co Antibodies comprising modified heavy constant regions
US11318211B2 (en) 2017-06-14 2022-05-03 Adc Therapeutics Sa Dosage regimes for the administration of an anti-CD19 ADC
EA039276B1 (ru) 2017-08-18 2021-12-27 Медимьюн Лимитед Пирролобензодиазепиновые конъюгаты
MX2020003125A (es) 2017-09-29 2020-10-01 Daiichi Sankyo Co Ltd Conjugado de anticuerpo-derivado de pirrolobenzodiazepina.
CN111417409B (zh) 2017-11-14 2022-07-08 麦迪穆有限责任公司 吡咯并苯并二氮杂䓬缀合物
EP3717021A1 (en) 2017-11-27 2020-10-07 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
JP7177848B2 (ja) 2018-03-28 2022-11-24 田辺三菱製薬株式会社 cMETモノクローナル結合剤の薬物複合体とその使用
GB201806022D0 (en) * 2018-04-12 2018-05-30 Medimmune Ltd Pyrrolobenzodiazepines and conjugates thereof
EP3887397A1 (en) 2018-11-28 2021-10-06 Bristol-Myers Squibb Company Antibodies comprising modified heavy constant regions
AU2019386945B9 (en) 2018-11-30 2025-10-23 Bristol-Myers Squibb Company Antibody comprising a glutamine-containing light chain C-terminal extension, conjugates thereof, and methods and uses
KR20210102334A (ko) 2018-12-12 2021-08-19 브리스톨-마이어스 스큅 컴퍼니 트랜스글루타미나제 접합을 위해 변형된 항체, 그의 접합체, 및 방법 및 용도
BR112021018260A2 (pt) 2019-03-15 2021-11-23 Medimmune Ltd Dímeros de azetidobenzodiazepina e conjugados compreendendo-os para uso no tratamento de câncer
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
WO2024005123A1 (ja) 2022-06-30 2024-01-04 東レ株式会社 癌の治療及び/又は予防用医薬組成物

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
IL33558A (en) 1968-12-30 1973-10-25 Fujisawa Pharmaceutical Co Antibiotic pyrrolo-benzodiazepine compound,its derivatives and processes for their production
JPS4843755B1 (enExample) 1969-06-26 1973-12-20
FR2027356A1 (en) 1968-12-30 1970-09-25 Fujisawa Pharmaceutical Co Benzodiazepinone antibiotics
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
CA1185602A (en) 1981-02-27 1985-04-16 Emilio Kyburz Imidazodiazepines
CA1184175A (en) 1981-02-27 1985-03-19 Walter Hunkeler 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
ATE349722T1 (de) 1998-07-08 2007-01-15 E Ink Corp Verbesserte farbige mikroverkapselte elektrophoretische anzeige
GB9818730D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Collections of compounds
NZ510493A (en) 1998-08-27 2003-11-28 Spirogen Ltd Pyrrolobenzodiazepin-5-one derivatives for treating viral, bacterial and protozoal infections
GB9818732D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Collection of compounds
GB9818731D0 (en) 1998-08-27 1998-10-21 Univ Portsmouth Compounds
US6909006B1 (en) 1999-08-27 2005-06-21 Spirogen Limited Cyclopropylindole derivatives
WO2002030894A2 (en) 2000-09-19 2002-04-18 Taiho Pharmaceutical Co., Ltd. Compositions and methods of the use thereof achiral analogues of cc-1065 and the duocarmycins
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
SI1545613T1 (sl) 2002-07-31 2011-11-30 Seattle Genetics Inc Avristatinski konjugati in njihova uporaba za zdravljenje raka avtoimunske bolezni ali infekcijskebolezni
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
US6884799B2 (en) 2003-03-31 2005-04-26 Council Of Scientific And Industrial Research Non-cross-linking pyrrolo[2,1-c][1,4]benzodiazepines and process thereof
GB0321295D0 (en) 2003-09-11 2003-10-15 Spirogen Ltd Synthesis of protected pyrrolobenzodiazepines
US7511032B2 (en) 2003-10-22 2009-03-31 The United States Of America As Represented By The Secretary, Department Of Health And Human Services Pyrrolobenzodiazepine derivatives, compositions comprising the same and methods related thereto
GB0416511D0 (en) 2003-10-22 2004-08-25 Spirogen Ltd Pyrrolobenzodiazepines
DK1725249T3 (en) 2003-11-06 2014-03-17 Seattle Genetics Inc Monomethylvaline compounds capable of conjugating to ligands.
JP5064037B2 (ja) 2004-02-23 2012-10-31 ジェネンテック, インコーポレイテッド 複素環式自壊的リンカーおよび結合体
SI2270010T1 (sl) 2004-03-01 2012-05-31 Spirogen Ltd hidroksi H pirolo c benzodiazepin onski derivati kot ključni intermediati za pripravo C substituiranih pirolobenzodiazepinov
GB0404578D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Pyrrolobenzodiazepines
GB0404577D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Pyrrolobenzodiazepines
GB0404574D0 (en) 2004-03-01 2004-04-07 Spirogen Ltd Amino acids
DE102004010943A1 (de) 2004-03-03 2005-09-29 Degussa Ag Verfahren zur Herstellung von N-geschützten 4-Ketprolinderivaten
WO2005085260A1 (en) 2004-03-09 2005-09-15 Spirogen Limited 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
ES2579805T3 (es) 2004-09-23 2016-08-16 Genentech, Inc. Anticuerpos y conjugados modificados por ingeniería genética con cisteína
EP1831418A2 (en) 2004-12-24 2007-09-12 Showa Denko Kabushiki Kaisha Production method of thermoelectric semiconductor alloy, thermoelectric conversion module and thermoelectric power generating device
AU2006236225C1 (en) 2005-04-19 2013-05-02 Seagen Inc. Humanized anti-CD70 binding agents and uses thereof
PL1879901T3 (pl) 2005-04-21 2010-06-30 Medimmune Ltd Pirolobenzodiazepiny
US20070154906A1 (en) 2005-10-05 2007-07-05 Spirogen Ltd. Methods to identify therapeutic candidates
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
SI1813614T1 (sl) 2006-01-25 2012-01-31 Sanofi 174 Citotoksična sredstva, ki obsegajo nove tomajmicinske derivate
NZ574215A (en) 2006-07-18 2012-07-27 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
ES2523915T5 (es) 2006-12-01 2022-05-26 Seagen Inc Agentes de unión a la diana variantes y usos de los mismos
WO2009011753A2 (en) 2007-07-11 2009-01-22 The Regents Of The University Of California Nanostructured polymer membranes for proton conduction
EP2019104B1 (en) 2007-07-19 2013-09-04 Sanofi Cytotoxic agents comprising new tomaymycin derivatives and their therapeutic use
GB0722087D0 (en) 2007-11-09 2007-12-19 Spirogen Ltd Polyamides
GB0722088D0 (en) 2007-11-09 2007-12-19 Spirogen Ltd Pyrrolobenzodiazepines
PL2265283T3 (pl) * 2008-03-18 2015-03-31 Seattle Genetics Inc Koniugaty aurystatyny lek łącznik
GB0813432D0 (en) 2008-07-22 2008-08-27 Spirogen Ltd Pyrrolobenzodiazepines
GB0819097D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
GB0819095D0 (en) 2008-10-17 2008-11-26 Spirogen Ltd Pyrrolobenzodiazepines
JP5977522B2 (ja) 2009-02-05 2016-08-24 イミュノジェン・インコーポレーテッド 新規ベンゾジアゼピン誘導体
FR2949469A1 (fr) 2009-08-25 2011-03-04 Sanofi Aventis Derives anticancereux, leur preparation et leur application en therapeutique
WO2011038159A2 (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
RS52983B (sr) 2010-04-15 2014-02-28 Spirogen Sárl Pirolobenzodiazepini i njihovi konjugati
GB201006340D0 (en) 2010-04-15 2010-06-02 Spirogen Ltd Synthesis method and intermediates
EP2558127B1 (en) 2010-04-15 2022-01-19 Seagen Inc. Targeted pyrrolobenzodiazepine conjugates
JP5875083B2 (ja) * 2010-04-15 2016-03-02 メディミューン リミテッド 増殖性疾患治療用ピロロベンゾジアゼピン
TWI617555B (zh) 2011-02-15 2018-03-11 免疫原公司 細胞毒性苯并二氮呯衍生物
BR112013028907A2 (pt) * 2011-05-08 2017-01-31 Legochem Biosciences Inc conjugados de proteína-agente ativo e método para preparar os mesmos
KR101860174B1 (ko) 2011-09-20 2018-05-21 메디뮨 리미티드 표적 접합체 내의 내포를 위한 비대칭 이량체 pbd 화합물로서 피롤로벤조디아제핀
WO2013047898A1 (en) * 2011-09-29 2013-04-04 Dow Corning Toray Co., Ltd. Curable silicone composition and cured product thereof
CN104011018B (zh) 2011-10-14 2016-12-14 麦迪穆有限责任公司 可用于制备吡咯并苯并二氮杂卓的合成方法和中间体
EP2751111B1 (en) 2011-10-14 2017-04-26 MedImmune Limited Asymmetrical bis-(5H-Pyrrolo[2,1-c][1,4]benzodiazepin-5-one) derivatives for the treatment of proliferative or autoimmune diseases
EA027386B1 (ru) 2011-10-14 2017-07-31 Медимьюн Лимитед Пирролобензодиазепины
ES2945932T3 (es) 2011-10-14 2023-07-10 Seagen Inc Pirrolobenzodiazepinas y conjugados dirigidos
HUE025661T2 (en) 2011-10-14 2016-04-28 Medimmune Ltd Pyrrolobenzodiazepines and their conjugates
US9387259B2 (en) 2011-10-14 2016-07-12 Seattle Genetics, Inc. Pyrrolobenzodiazepines and targeted conjugates
US9321774B2 (en) 2012-04-30 2016-04-26 Medimmune Limited Pyrrolobenzodiazepines
CN104684914B (zh) 2012-04-30 2017-12-15 麦迪穆有限责任公司 吡咯并苯并二氮杂卓
JP2015523380A (ja) 2012-07-09 2015-08-13 ジェネンテック, インコーポレイテッド 抗cd79b抗体を含む免疫複合体
EP2869849A1 (en) 2012-07-09 2015-05-13 Genentech, Inc. Immunoconjugates comprising anti-cd22 antibodies
EP2879708A4 (en) 2012-08-02 2016-03-16 Genentech Inc ANTIBODY AND ANTI-ETBR IMMUNOCONJUGATES
WO2014057118A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sarl Pyrrolobenzodiazepine-anti-cd22 antibody conjugates
HUE041274T2 (hu) 2012-10-12 2019-05-28 Adc Therapeutics Sa Pirrolobenzodiazepin-anti-PSMA-antitest konjugátumok
KR20150083856A (ko) 2012-10-12 2015-07-20 에이디씨 테라퓨틱스 에스에이알엘 피롤로벤조디아제핀-항-her2 항체 컨주게이트
JP6367204B2 (ja) 2012-10-12 2018-08-01 メドイミューン・リミテッドMedImmune Limited 結合用のピロロベンゾジアゼピン誘導体の合成および中間体
WO2014057114A1 (en) 2012-10-12 2014-04-17 Adc Therapeutics Sàrl Pyrrolobenzodiazepine-anti-psma antibody conjugates
CA2887895C (en) 2012-10-12 2019-10-29 Adc Therapeutics Sarl Pyrrolobenzodiazepine-anti-cd19 antibody conjugates
CN105102004B (zh) 2012-10-12 2019-01-25 Adc疗法责任有限公司 吡咯并苯并二氮杂卓-抗cd22抗体结合物
LT2906248T (lt) 2012-10-12 2019-02-11 Medimmune Limited Pirolobenzodiazepinai ir jų konjugatai
TR201808051T4 (tr) 2012-10-12 2018-06-21 Adc Therapeutics Sa Pirrolobenzodiazepin antikor konjugatları.
SI2766048T1 (sl) 2012-10-12 2015-03-31 Spirogen Sarl Pirolobenzodiazepini in njihovi konjugati
EP2906297B1 (en) 2012-10-12 2017-12-06 ADC Therapeutics SA Pyrrolobenzodiazepine-antibody conjugates
CN110452242A (zh) 2012-12-21 2019-11-15 麦迪穆有限责任公司 吡咯并苯并二氮杂卓及其结合物
CA2894959C (en) 2012-12-21 2022-01-11 Spirogen Sarl Unsymmetrical pyrrolobenzodiazepines-dimers for use in the treatment of proliferative and autoimmune diseases
ME03394B (me) 2013-02-22 2020-01-20 Medimmune Ltd Antidllз-antitelo-pbd konjugati i nihovа upotreba
MX363787B (es) 2013-03-13 2019-04-03 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de los mismos.
ES2731779T3 (es) 2013-03-13 2019-11-19 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de las mismas
MX362970B (es) 2013-03-13 2019-02-28 Medimmune Ltd Pirrolobenzodiazepinas y conjugados de las mismas.
JP2016518382A (ja) 2013-04-26 2016-06-23 ピエール、ファーブル、メディカマン Axl抗体薬物複合体および癌の治療のためのその使用
GB201317981D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
WO2015052535A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
GB201317982D0 (en) 2013-10-11 2013-11-27 Spirogen Sarl Pyrrolobenzodiazepines and conjugates thereof
US10010624B2 (en) 2013-10-11 2018-07-03 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
WO2015052533A1 (en) 2013-10-11 2015-04-16 Spirogen Sàrl Pyrrolobenzodiazepine-antibody conjugates
EP3054985B1 (en) 2013-10-11 2018-12-26 Medimmune Limited Pyrrolobenzodiazepine-antibody conjugates
CN105848685B (zh) 2013-12-16 2020-09-22 健泰科生物技术公司 拟肽化合物及其抗体药物偶联物
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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US9399641B2 (en) 2016-07-26
EA201490518A1 (ru) 2014-08-29
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EP2751120A1 (en) 2014-07-09
EP2751120B1 (en) 2018-08-22
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CA2849039C (en) 2018-09-18
US20150158869A1 (en) 2015-06-11
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