EA201692530A1 - Цитотоксические пептиды и их конъюгаты - Google Patents

Цитотоксические пептиды и их конъюгаты

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Publication number
EA201692530A1
EA201692530A1 EA201692530A EA201692530A EA201692530A1 EA 201692530 A1 EA201692530 A1 EA 201692530A1 EA 201692530 A EA201692530 A EA 201692530A EA 201692530 A EA201692530 A EA 201692530A EA 201692530 A1 EA201692530 A1 EA 201692530A1
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Eurasian Patent Office
Prior art keywords
immunoconjugates
conjugates
antibody
cell proliferative
proliferative disorders
Prior art date
Application number
EA201692530A
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English (en)
Inventor
Бернхард Гайерштангер
Ян Груневальд
Вэйцзя Оу
Шифенг Пан
Тецуо Уно
Юнцинь Ван
Син Ван
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Новартис Аг
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Publication date
Application filed by Новартис Аг filed Critical Новартис Аг
Publication of EA201692530A1 publication Critical patent/EA201692530A1/ru

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D207/00—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08—Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09—Radicals substituted by nitrogen atoms, not forming part of a nitro radical
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6801—Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6849—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a receptor, a cell surface antigen or a cell surface determinant
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K47/00—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
    • 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
    • A61K47/68—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment
    • A61K47/6835—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site
    • A61K47/6851—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell
    • A61K47/6855—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 antibody, an immunoglobulin or a fragment thereof, e.g. an Fc-fragment the modifying agent being an antibody or an immunoglobulin bearing at least one antigen-binding site the antibody targeting a determinant of a tumour cell the tumour determinant being from breast cancer cell
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A61P37/02—Immunomodulators
    • A61P37/04—Immunostimulants
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/14—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing three or more hetero rings
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K16/00—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies
    • C07K16/18—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32—Immunoglobulins [IGs], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link containing the structure -NH-(X)3-C(=0)-, e.g. statine or derivatives thereof

Abstract

В настоящей заявке раскрыты новые соединения формулы (I), как описано в данном документе:и применение таких пептидов в получении иммуноконъюгатов (т.е. конъюгатов антитело-лекарственное средство) Кроме того, в данном документе описаны иммуноконъюгаты (т.е. конъюгаты антитело-лекарственное средство), содержащие такое новое соединение, связанное с антигенсвязывающим фрагментом, таким как антитело, где такие иммуноконъюгаты пригодны для лечения клеточных пролиферативных нарушений. Кроме того, изобретение относится к фармацевтическим композициям, содержащим эти иммуноконъюгаты, композициям, содержащим иммуноконъюгаты с терапевтическим соагентом, и способам применения этих иммуноконъюгатов и композиций для лечения клеточных пролиферативных нарушений.
EA201692530A 2014-06-13 2015-06-11 Цитотоксические пептиды и их конъюгаты EA201692530A1 (ru)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462011961P 2014-06-13 2014-06-13
PCT/IB2015/054400 WO2015189791A1 (en) 2014-06-13 2015-06-11 Auristatin derivatives and conjugates thereof

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EA201692530A1 true EA201692530A1 (ru) 2017-07-31

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US (2) US9884817B2 (ru)
EP (1) EP3154997B9 (ru)
JP (1) JP6681346B2 (ru)
KR (1) KR20170016479A (ru)
CN (1) CN106573956A (ru)
AU (1) AU2015273098B2 (ru)
BR (1) BR112016028835A2 (ru)
CA (1) CA2951368A1 (ru)
EA (1) EA201692530A1 (ru)
IL (1) IL248961A0 (ru)
MX (1) MX2016016515A (ru)
SG (1) SG11201609462RA (ru)
WO (1) WO2015189791A1 (ru)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AU2014214751B2 (en) * 2013-02-08 2017-06-01 Novartis Ag Specific sites for modifying antibodies to make immunoconjugates
EP3122757B1 (en) * 2014-02-28 2023-09-06 Hangzhou Dac Biotech Co., Ltd Charged linkers and their uses for conjugation
JP6681346B2 (ja) * 2014-06-13 2020-04-15 ノバルティス アーゲー オーリスタチン誘導体およびその抱合体
US11566082B2 (en) 2014-11-17 2023-01-31 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
MA44334A (fr) 2015-10-29 2018-09-05 Novartis Ag Conjugués d'anticorps comprenant un agoniste du récepteur de type toll
US10654887B2 (en) 2016-05-11 2020-05-19 Ge Healthcare Bio-Process R&D Ab Separation matrix
US10730908B2 (en) 2016-05-11 2020-08-04 Ge Healthcare Bioprocess R&D Ab Separation method
JP6987424B2 (ja) 2016-05-11 2022-01-05 サイティバ・バイオプロセス・アールアンドディ・アクチボラグ 分離マトリックスを洗浄および／または消毒する方法
US10703774B2 (en) 2016-09-30 2020-07-07 Ge Healthcare Bioprocess R&D Ab Separation method
CN109071613A (zh) 2016-05-11 2018-12-21 通用电气医疗集团生物工艺研发股份公司 分离基质
JP7106187B2 (ja) 2016-05-11 2022-07-26 サイティバ・バイオプロセス・アールアンドディ・アクチボラグ 分離マトリックスを保存する方法
US10889615B2 (en) 2016-05-11 2021-01-12 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
JOP20190155A1 (ar) * 2016-12-21 2019-06-23 Novartis Ag مترافقات عقار جسم مضاد لإزالة خلايا جذعية مكونة للدم
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
KR20210095167A (ko) * 2019-09-29 2021-07-30 맙플렉스 인터내셔널 컴퍼니 리미티드 산 방법에 의한 항체-약물 접합체 중간체의 제조 방법 및 이의 적용
CN113321702B (zh) * 2020-02-28 2022-08-05 国家纳米科学中心 一种单甲基澳瑞他汀f甲酯前药及其制备方法和应用
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
CN111675694B (zh) * 2020-06-28 2021-11-26 山东大学 一种含肟基团的二芳基嘧啶类hiv-1逆转录酶抑制剂及其制备方法与应用
EP4319820A1 (en) 2021-04-10 2024-02-14 Profoundbio Us Co. Folr1 binding agents, conjugates thereof and methods of using the same
CA3216459A1 (en) 2021-04-23 2022-10-27 Profoundbio Us Co. Anti-cd70 antibodies, conjugates thereof and methods of using the same
TW202320857A (zh) 2021-07-06 2023-06-01 美商普方生物製藥美國公司 連接子、藥物連接子及其結合物及其使用方法
WO2023061405A1 (zh) * 2021-10-12 2023-04-20 成都科岭源医药技术有限公司 一种高稳定性的靶向接头-药物偶联物
WO2023122228A1 (en) * 2021-12-23 2023-06-29 Adcentrx Therapeutics Inc. Novel auristatin analogs and immunoconjugates thereof

Family Cites Families (33)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US4458066A (en) 1980-02-29 1984-07-03 University Patents, Inc. Process for preparing polynucleotides
KR0185440B1 (ko) 1991-08-09 1999-04-01 야마구찌 다까시 신규의 테트라 펩티트 유도체
DE69434136T2 (de) 1993-10-01 2005-12-01 Teikoku Hormone Mfg. Co., Ltd. Dolastatin-derivate
US5641870A (en) 1995-04-20 1997-06-24 Genentech, Inc. Low pH hydrophobic interaction chromatography for antibody purification
DK0831100T3 (da) 1995-04-21 2001-01-02 Teikoku Hormone Mfg Co Ltd Nye peptidderivater
JP3614866B2 (ja) 1997-06-12 2005-01-26 リサーチ コーポレイション テクノロジーズ，インコーポレイティド 人工抗体ポリペプチド
US6153655A (en) 1998-04-17 2000-11-28 Enzon, Inc. Terminally-branched polymeric linkers and polymeric conjugates containing the same
US7803915B2 (en) 2001-06-20 2010-09-28 Genentech, Inc. Antibody compositions for the diagnosis and treatment of tumor
US20090068178A1 (en) 2002-05-08 2009-03-12 Genentech, Inc. Compositions and Methods for the Treatment of Tumor of Hematopoietic Origin
CA2514733A1 (en) 2003-02-28 2004-09-16 Transform Pharmaceuticals, Inc. Pharmaceutical co-crystal compositions of drugs such as carbamazepine, celecoxib, olanzapine, itraconazole, topiramate, modafinil, 5-fluorouracil, hydrochlorothiazide, acetaminophen, aspirin, flurbiprofen, phenytoin and ibuprofen
SG149815A1 (en) 2003-11-06 2009-02-27 Seattle Genetics Inc Monomethylvaline compounds capable of conjugation to ligands
WO2006132670A2 (en) * 2004-11-12 2006-12-14 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the n terminus
JP2008521828A (ja) 2004-11-29 2008-06-26 シアトル ジェネティックス， インコーポレイテッド 操作された抗体およびイムノコンジュゲート
KR20140084242A (ko) 2005-06-20 2014-07-04 피에스엠에이 디벨롭먼트 캄파니, 엘엘씨 Ｐｓｍａ 항체-약물 접합체
US7750116B1 (en) 2006-02-18 2010-07-06 Seattle Genetics, Inc. Antibody drug conjugate metabolites
WO2007103288A2 (en) 2006-03-02 2007-09-13 Seattle Genetics, Inc. Engineered antibody drug conjugates
AR059900A1 (es) 2006-03-17 2008-05-07 Genentech Inc Anticuerpos anti-tat226 e inmunoconjugados
CA2702555A1 (en) 2007-10-19 2009-04-23 Seattle Genetics, Inc. Cd19 binding agents and uses thereof
NO2842575T3 (ru) 2008-03-18 2018-02-24
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
CN106563128B (zh) 2010-10-22 2020-05-22 西雅图遗传学公司 以奥里斯他汀为主的抗体药物结合物和结合mTOR的抑制剂在制备治疗癌症药物中的用途
ES2531471T3 (es) 2011-02-25 2015-03-16 Lonza Ltd Enlazador ramificado para conjugados de proteínas-fármacos
ES2543888T3 (es) 2011-03-16 2015-08-25 Seattle Genetics, Inc. N-carboxialquil-auristatinas y su utilización
CA2833477A1 (en) 2011-04-21 2012-10-26 Seattle Genetics, Inc. Novel binder-drug conjugates (adcs) and their use
EP2714684B1 (en) 2011-05-27 2018-09-05 Ambrx, Inc. Compositions containing, methods involving, and uses of non-natural amino acid linked dolastatin derivatives
JP2013100803A (ja) 2011-08-09 2013-05-23 Toru Shinohara 水力発電装置および水力発電システム
AR088694A1 (es) 2011-11-17 2014-06-25 Pfizer Peptidos citotoxicos y conjugados de anticuerpo-farmaco de los mismos
WO2013092998A1 (en) 2011-12-23 2013-06-27 Innate Pharma Enzymatic conjugation of antibodies
US9545449B2 (en) 2012-05-11 2017-01-17 Advanced Proteone Therapeutics Inc. Site-specific labeling and targeted delivery of proteins for the treatment of cancer
US9585970B2 (en) 2012-06-04 2017-03-07 Novartis Ag Site-specific labeling methods and molecules produced thereby
US20150314007A1 (en) 2012-12-21 2015-11-05 Glykos Finland Oy Linker-payload molecule conjugates
EP3082877B1 (en) * 2013-12-17 2019-08-28 Novartis AG Cytotoxic peptides and conjugates thereof
JP6681346B2 (ja) * 2014-06-13 2020-04-15 ノバルティス アーゲー オーリスタチン誘導体およびその抱合体

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US9884817B2 (en) 2018-02-06
SG11201609462RA (en) 2016-12-29
US10280139B2 (en) 2019-05-07
CA2951368A1 (en) 2015-12-17
WO2015189791A1 (en) 2015-12-17
EP3154997B1 (en) 2020-02-19
KR20170016479A (ko) 2017-02-13
EP3154997B9 (en) 2021-04-14
US20180155281A1 (en) 2018-06-07
AU2015273098A1 (en) 2016-12-01
JP2017523143A (ja) 2017-08-17
EP3154997A1 (en) 2017-04-19
CN106573956A (zh) 2017-04-19
JP6681346B2 (ja) 2020-04-15
MX2016016515A (es) 2017-04-27
US20170121282A1 (en) 2017-05-04
IL248961A0 (en) 2017-01-31
BR112016028835A2 (pt) 2017-10-24
AU2015273098B2 (en) 2018-05-10

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