CN106573956A - 澳瑞他汀衍生物及其缀合物 - Google Patents

澳瑞他汀衍生物及其缀合物 Download PDF

Info

Publication number
CN106573956A
CN106573956A CN201580043354.7A CN201580043354A CN106573956A CN 106573956 A CN106573956 A CN 106573956A CN 201580043354 A CN201580043354 A CN 201580043354A CN 106573956 A CN106573956 A CN 106573956A
Authority
CN
China
Prior art keywords
nhc
independently selected
alkyl
immunoconjugate
compound
Prior art date
Legal status (The legal status 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 status listed.)
Pending
Application number
CN201580043354.7A
Other languages
English (en)
Chinese (zh)
Inventor
B·盖尔斯唐格尔
J·格鲁内瓦尔德
W·欧
潘士峰
宇野哲郎
万咏勤
王兴
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Novartis AG
Original Assignee
Novartis AG
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 Novartis AG filed Critical Novartis AG
Publication of CN106573956A publication Critical patent/CN106573956A/zh
Pending legal-status Critical Current

Links

Classifications

    • 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
    • A61K47/6801—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
    • A61K47/68031—Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being an auristatin
    • 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

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Immunology (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Epidemiology (AREA)
  • Cell Biology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Biophysics (AREA)
  • Oncology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
  • Medicinal Preparation (AREA)
CN201580043354.7A 2014-06-13 2015-06-11 澳瑞他汀衍生物及其缀合物 Pending CN106573956A (zh)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201462011961P 2014-06-13 2014-06-13
US62/011,961 2014-06-13
PCT/IB2015/054400 WO2015189791A1 (en) 2014-06-13 2015-06-11 Auristatin derivatives and conjugates thereof

Publications (1)

Publication Number Publication Date
CN106573956A true CN106573956A (zh) 2017-04-19

Family

ID=53491655

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201580043354.7A Pending CN106573956A (zh) 2014-06-13 2015-06-11 澳瑞他汀衍生物及其缀合物

Country Status (13)

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

Cited By (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN111675694A (zh) * 2020-06-28 2020-09-18 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
CN113321702A (zh) * 2020-02-28 2021-08-31 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
WO2025152969A1 (zh) * 2024-01-15 2025-07-24 武汉人福创新药物研发中心有限公司 靶向化合物及其用途

Families Citing this family (27)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
SI2953976T1 (sl) * 2013-02-08 2021-08-31 Novartis Ag Specifična mesta z modificiranje protiteles za izdelavo imunokonjugatov
US10464955B2 (en) * 2014-02-28 2019-11-05 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
KR20170016479A (ko) * 2014-06-13 2017-02-13 노파르티스 아게 아우리스타틴 유도체 및 그의 접합체
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
JP7031934B2 (ja) 2016-05-11 2022-03-08 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
US10654887B2 (en) 2016-05-11 2020-05-19 Ge Healthcare Bio-Process R&D Ab Separation matrix
EP3455243B1 (en) 2016-05-11 2021-03-24 Cytiva BioProcess R&D AB Separation matrix
EP3455240B1 (en) 2016-05-11 2025-01-01 Cytiva BioProcess R&D AB Method of storing a separation matrix
US10889615B2 (en) 2016-05-11 2021-01-12 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
US10703774B2 (en) 2016-09-30 2020-07-07 Ge Healthcare Bioprocess R&D Ab Separation method
CN109311948B (zh) 2016-05-11 2022-09-16 思拓凡生物工艺研发有限公司 清洁和/或消毒分离基质的方法
US10730908B2 (en) 2016-05-11 2020-08-04 Ge Healthcare Bioprocess R&D Ab Separation method
US12448411B2 (en) 2016-09-30 2025-10-21 Cytiva Bioprocess R&D Ab Separation method
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
MX2020004530A (es) * 2017-11-18 2020-09-18 Magalhaes Nzola De Producto y proceso para emplear conjugados de union a antigeno basados en gc7 (n1-guanil-1,7-diaminoheptano) en terapia de cancer.
AU2019341067B2 (en) * 2019-09-29 2021-08-05 Mabplex International Co., Ltd. Method for producing antibody-drug conjugate intermediate by addition of acid and use thereof
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
AU2022253902A1 (en) 2021-04-10 2023-11-02 Genmab A/S Folr1 binding agents, conjugates thereof and methods of using the same
TW202308699A (zh) 2021-04-23 2023-03-01 美商普方生物製藥美國公司 Ｃｄ７０結合劑、其結合物及其使用方法
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
EP4420682A1 (en) * 2021-10-12 2024-08-28 Chengdu Scimount Pharmatech Co., Ltd. Highly-stable targeted linker-drug conjugate
KR20240152826A (ko) * 2021-12-23 2024-10-22 애드센트릭스 테라퓨틱스 잉크. 신규한 오리스타틴 유사체 및 이의 면역접합체
AR133955A1 (es) 2023-09-26 2025-11-19 Profoundbio Us Co Agentes de unión a ptk7, conjugados de éstos y métodos de uso de los mismos
US20250296992A1 (en) 2024-01-10 2025-09-25 Genmab A/S Slitrk6 binding agents, conjugates thereof and methods of using the same
WO2025181219A1 (en) 2024-02-29 2025-09-04 Genmab A/S Egfr and c-met bispecific binding agents, conjugates thereof and methods of using the same

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080300192A1 (en) * 2004-11-12 2008-12-04 Seattle Genetics, Inc. Auristatins Having an Aminobenzoic Acid Unit at the N Terminus
WO2013072813A2 (en) * 2011-11-17 2013-05-23 Pfizer Inc. Cytotoxic peptides and antibody drug conjugates thereof
WO2013184514A1 (en) * 2012-06-04 2013-12-12 Irm Llc Site-specific labeling methods and molecules produced thereby

Family Cites Families (30)

* 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
ES2233928T3 (es) 1993-10-01 2005-06-16 Teikoku Hormone Mfg. Co., Ltd. Derivados de dolastatina.
US5641870A (en) 1995-04-20 1997-06-24 Genentech, Inc. Low pH hydrophobic interaction chromatography for antibody purification
KR100408909B1 (ko) 1995-04-21 2004-04-29 데이꼬꾸 조끼 세이야꾸 가부시키가이샤 신규펩티드유도체
EP1958962A3 (en) 1997-06-12 2013-05-01 Novartis International Pharmaceutical Ltd. Artificial antibody polypeptides
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
JP2007524596A (ja) 2003-02-28 2007-08-30 トランスフォーム・ファーマシューティカルズ・インコーポレイテッド 共結晶医薬組成物
CN104998273A (zh) 2003-11-06 2015-10-28 西雅图基因公司 能够与配体偶联的单甲基缬氨酸化合物
CA2587589A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
PT1912677E (pt) 2005-06-20 2013-12-23 Psma Dev Company L L C Conjugados de anticorpos contra psma-fármaco
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
PT2211904T (pt) 2007-10-19 2016-11-02 Seattle Genetics Inc Agentes de ligação a cd19 e seus usos
EP2842575B1 (en) 2008-03-18 2017-09-27 Seattle Genetics, Inc. Auristatin drug linker conjugates
WO2012041805A1 (de) 2010-09-29 2012-04-05 Bayer Pharma Aktiengesellschaft N-carboxyalkyl-auristatine und ihre verwendung
US9272052B2 (en) 2010-10-22 2016-03-01 Seattle Genetics, Inc. Synergistic effects between auristatin-based antibody drug conjugates and inhibitors of the PI3K-AKT mTOR pathway
JP5559439B2 (ja) 2011-02-25 2014-07-23 ロンザ リミテッド タンパク質薬剤接合体のための分枝リンカー
CN103764667B (zh) 2011-03-16 2017-06-20 西雅图基因公司 N‑羧烷基耳他汀类及其应用
KR102023496B1 (ko) 2011-04-21 2019-09-20 시애틀 지네틱스, 인크. 신규 결합제-약물 콘주게이트 (adc) 및 그의 용도
US9796754B2 (en) 2011-05-27 2017-10-24 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
US9717803B2 (en) 2011-12-23 2017-08-01 Innate Pharma Enzymatic conjugation of polypeptides
JP6290187B2 (ja) 2012-05-11 2018-03-07 クランツ，アレクサンダー 癌の処置のためのタンパク質の部位特異的標識及び標的送達
US20150314007A1 (en) 2012-12-21 2015-11-05 Glykos Finland Oy Linker-payload molecule conjugates
PL3082877T3 (pl) * 2013-12-17 2020-02-28 Novartis Ag Cytotoksyczne peptydy i ich koniugaty
KR20170016479A (ko) * 2014-06-13 2017-02-13 노파르티스 아게 아우리스타틴 유도체 및 그의 접합체

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US20080300192A1 (en) * 2004-11-12 2008-12-04 Seattle Genetics, Inc. Auristatins Having an Aminobenzoic Acid Unit at the N Terminus
WO2013072813A2 (en) * 2011-11-17 2013-05-23 Pfizer Inc. Cytotoxic peptides and antibody drug conjugates thereof
WO2013184514A1 (en) * 2012-06-04 2013-12-12 Irm Llc Site-specific labeling methods and molecules produced thereby

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
KOICHI MIYAZAKI等: "Synthesis and antitumor activity of novel Dolastatin 10 analogs", 《CHEMICAL & PHARMACEUTICAL BULLETIN 》 *
朱贵东、傅阳心: "设计新一代抗体药物偶联物", 《药学学报》 *

Cited By (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CN113321702A (zh) * 2020-02-28 2021-08-31 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
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
CN111675694A (zh) * 2020-06-28 2020-09-18 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
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
WO2025152969A1 (zh) * 2024-01-15 2025-07-24 武汉人福创新药物研发中心有限公司 靶向化合物及其用途

Also Published As

Publication number Publication date
SG11201609462RA (en) 2016-12-29
KR20170016479A (ko) 2017-02-13
WO2015189791A1 (en) 2015-12-17
AU2015273098A1 (en) 2016-12-01
EP3154997B1 (en) 2020-02-19
US20170121282A1 (en) 2017-05-04
JP6681346B2 (ja) 2020-04-15
MX2016016515A (es) 2017-04-27
CA2951368A1 (en) 2015-12-17
US10280139B2 (en) 2019-05-07
AU2015273098B2 (en) 2018-05-10
BR112016028835A2 (pt) 2017-10-24
JP2017523143A (ja) 2017-08-17
US9884817B2 (en) 2018-02-06
EA201692530A1 (ru) 2017-07-31
EP3154997B9 (en) 2021-04-14
EP3154997A1 (en) 2017-04-19
US20180155281A1 (en) 2018-06-07
IL248961A0 (en) 2017-01-31

Similar Documents

Publication Publication Date Title
EP3154997B9 (en) Auristatin derivatives and conjugates thereof
US10787480B2 (en) Cytotoxic peptides and conjugates thereof
US9938323B2 (en) Amatoxin derivatives and conjugates thereof as inhibitors of RNA polymerase
US10464969B2 (en) Amatoxin derivatives and conjugates thereof as inhibitors of RNA polymerase
US9498540B2 (en) Cell proliferation inhibitors and conjugates thereof
EP2968591A1 (en) Cell proliferation inhibitors and conjugates thereof
JP2022502431A (ja) スルホマレイミドに基づくリンカーおよび対応する複合体
WO2025055920A1 (zh) 新型海鞘素衍生物、其制备方法及用途、抗体药物偶联物及其应用

Legal Events

Date Code Title Description
PB01 Publication
PB01 Publication
SE01 Entry into force of request for substantive examination
SE01 Entry into force of request for substantive examination
WD01 Invention patent application deemed withdrawn after publication

Application publication date: 20170419

WD01 Invention patent application deemed withdrawn after publication