KR20160098257A - 세포독성 펩티드 및 그의 접합체 - Google Patents

세포독성 펩티드 및 그의 접합체 Download PDF

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Publication number
KR20160098257A
KR20160098257A KR1020167015935A KR20167015935A KR20160098257A KR 20160098257 A KR20160098257 A KR 20160098257A KR 1020167015935 A KR1020167015935 A KR 1020167015935A KR 20167015935 A KR20167015935 A KR 20167015935A KR 20160098257 A KR20160098257 A KR 20160098257A
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South Korea
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alkyl
independently selected
nhc
mmol
rti
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KR1020167015935A
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English (en)
Korean (ko)
Inventor
베른하르드 가이어스탄거
얀 그뤼네발트
웨이지아 오우
테츠오 우노
용친 완
싱 왕
윤호 진
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노파르티스 아게
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Publication of KR20160098257A publication Critical patent/KR20160098257A/ko
Ceased legal-status Critical Current

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K5/00Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/02Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing at least one abnormal peptide link
    • C07K5/0205Peptides 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
    • A61K47/48438
    • A61K47/48569
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/68Medicinal 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
    • A61K47/6801Drug-antibody or immunoglobulin conjugates defined by the pharmacologically or therapeutically active agent
    • A61K47/6803Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates
    • A61K47/6811Drugs conjugated to an antibody or immunoglobulin, e.g. cisplatin-antibody conjugates the drug being a protein or peptide, e.g. transferrin or bleomycin
    • A61K47/6817Toxins
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • 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
    • A61K47/68Medicinal 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
    • A61K47/6835Medicinal 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
    • A61K47/6851Medicinal 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K16/00Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies
    • C07K16/18Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans
    • C07K16/32Immunoglobulins [IG], e.g. monoclonal or polyclonal antibodies against material from animals or humans against translation products of oncogenes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K19/00Hybrid peptides, i.e. peptides covalently bound to nucleic acids, or non-covalently bound protein-protein complexes
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07KPEPTIDES
    • C07K7/00Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02Linear peptides containing at least one abnormal peptide link
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00Medicinal preparations containing peptides

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Molecular Biology (AREA)
  • Biochemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Immunology (AREA)
  • Epidemiology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Toxicology (AREA)
  • Cell Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Peptides Or Proteins (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Medicinal Preparation (AREA)
  • Medicines Containing Antibodies Or Antigens For Use As Internal Diagnostic Agents (AREA)
KR1020167015935A 2013-12-17 2014-12-17 세포독성 펩티드 및 그의 접합체 Ceased KR20160098257A (ko)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US201361917293P 2013-12-17 2013-12-17
US61/917,293 2013-12-17
PCT/US2014/070800 WO2015095301A2 (en) 2013-12-17 2014-12-17 Cytotoxic peptides and conjugates thereof

Publications (1)

Publication Number Publication Date
KR20160098257A true KR20160098257A (ko) 2016-08-18

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KR1020167015935A Ceased KR20160098257A (ko) 2013-12-17 2014-12-17 세포독성 펩티드 및 그의 접합체

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Country Link
US (3) US9988420B2 (enExample)
EP (2) EP3082877B1 (enExample)
JP (2) JP6636925B2 (enExample)
KR (1) KR20160098257A (enExample)
CN (1) CN105899526A (enExample)
AU (1) AU2014364812B2 (enExample)
BR (1) BR112016012538A2 (enExample)
CA (1) CA2930614A1 (enExample)
EA (1) EA201691251A1 (enExample)
ES (1) ES2758506T3 (enExample)
IL (1) IL245558B (enExample)
MX (1) MX2016007865A (enExample)
PL (1) PL3082877T3 (enExample)
PT (1) PT3082877T (enExample)
SG (1) SG11201604877UA (enExample)
WO (1) WO2015095301A2 (enExample)

Families Citing this family (28)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
CA2900755C (en) * 2013-02-08 2021-07-20 Irm Llc Specific sites for modifying antibodies to make immunoconjugates
US9522876B2 (en) 2013-03-15 2016-12-20 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
ES2916722T3 (es) 2013-12-27 2022-07-05 Zymeworks Inc Sistemas de enlace que contienen sulfonamida para conjugados de fármacos
SG11201605260VA (en) 2013-12-27 2016-07-28 Zymeworks Inc Var2csa-drug conjugates
CN106659800A (zh) * 2014-03-12 2017-05-10 诺华股份有限公司 用于修饰抗体以制备免疫缀合物的特定位点
EA201692530A1 (ru) * 2014-06-13 2017-07-31 Новартис Аг Цитотоксические пептиды и их конъюгаты
EP3194421B1 (en) 2014-09-17 2021-11-03 Zymeworks Inc. Cytotoxic and anti-mitotic compounds, and methods of using the same
US11566082B2 (en) 2014-11-17 2023-01-31 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
US10730908B2 (en) 2016-05-11 2020-08-04 Ge Healthcare Bioprocess R&D Ab Separation method
US10889615B2 (en) 2016-05-11 2021-01-12 Cytiva Bioprocess R&D Ab Mutated immunoglobulin-binding polypeptides
ES2909833T3 (es) 2016-05-11 2022-05-10 Cytiva Bioprocess R & D Ab Método de limpieza y/o desinfección de una matriz de separación
ES2874974T3 (es) 2016-05-11 2021-11-05 Cytiva Bioprocess R & D Ab Matriz de separación
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
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
US10703774B2 (en) 2016-09-30 2020-07-07 Ge Healthcare Bioprocess R&D Ab Separation method
US10654887B2 (en) 2016-05-11 2020-05-19 Ge Healthcare Bio-Process R&D Ab Separation matrix
US12448411B2 (en) 2016-09-30 2025-10-21 Cytiva Bioprocess R&D Ab Separation method
US10517958B2 (en) 2016-10-04 2019-12-31 Zymeworks Inc. Compositions and methods for the treatment of platinum-drug resistant cancer
JOP20190187A1 (ar) 2017-02-03 2019-08-01 Novartis Ag مترافقات عقار جسم مضاد لـ ccr7
UY38265A (es) * 2018-06-20 2020-01-31 Novartis Ag Conjugados anticuerpo droga para ablación de células madre hematopoyéticas
US20220017462A1 (en) * 2018-11-23 2022-01-20 WuXi Biologics Ireland Limited Ortho-phthalaldehyde containing linkers and use for preparation of antibody-drug conjugate
IL296277A (en) * 2020-03-09 2022-11-01 Sigma Aldrich Co Llc Efficient preparation of dolstatin and oristatin analogs via a common intermediate
US20230181756A1 (en) 2020-04-30 2023-06-15 Novartis Ag Ccr7 antibody drug conjugates for treating cancer
KR20230133289A (ko) * 2021-01-18 2023-09-19 아지노모토 가부시키가이샤 화합물 또는 이의 염, 및 이들에 의해 얻어지는 항체
CN115957338B (zh) * 2021-10-12 2025-11-18 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
JP2025524986A (ja) * 2022-07-27 2025-08-01 メディボストン リミテッド オーリスタチン誘導体およびそのコンジュゲート
WO2024152000A1 (en) * 2023-01-13 2024-07-18 The Trustees Of The University Of Pennsylvania Disruptable linker compositions, switchable bispecific t cell nanoengager (switch-bite) compositions comprising the same, and methods of use thereof
DK4601703T3 (da) 2023-04-18 2026-05-11 Astrazeneca Ab Konjugater omfattende spaltelige linkere

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
SG87056A1 (en) 1991-08-09 2002-03-19 Teikoku Hormone Mfg Co Ltd Novel tetrapeptide derivative
JP3469580B2 (ja) 1993-10-01 2003-11-25 帝国臓器製薬株式会社 新規なペプチド誘導体
US5595756A (en) * 1993-12-22 1997-01-21 Inex Pharmaceuticals Corporation Liposomal compositions for enhanced retention of bioactive agents
US5641870A (en) 1995-04-20 1997-06-24 Genentech, Inc. Low pH hydrophobic interaction chromatography for antibody purification
CN1113066C (zh) 1995-04-21 2003-07-02 帝国脏器制药株式会社 新型肽衍生物
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
EP3434275A1 (en) 2003-11-06 2019-01-30 Seattle Genetics, Inc. Assay for cancer cells based on the use of auristatin conjugates with antibodies
JP2008519863A (ja) * 2004-11-12 2008-06-12 シアトル ジェネティクス インコーポレイティッド N末端にアミノ安息香酸単位を有するオーリスタチン
AU2005316844A1 (en) 2004-11-29 2006-06-22 Seattle Genetics, Inc. Engineered antibodies and immunoconjugates
CN103127523A (zh) 2005-06-20 2013-06-05 Psma开发有限公司 Psma抗体-药物缀合物
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
WO2009052431A2 (en) 2007-10-19 2009-04-23 Seattle Genetics, Inc. Cd19 binding agents and uses thereof
EP2265283B1 (en) 2008-03-18 2014-09-03 Seattle Genetics, Inc. Auristatin drug linker conjugates
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
ES3004351T3 (en) 2010-10-22 2025-03-12 Seagen Inc Synergistic effects between auristatin-based antibody drug conjugates and inhibitors of the pi3k-akt mtor pathway
ES2531471T3 (es) 2011-02-25 2015-03-16 Lonza Ltd Enlazador ramificado para conjugados de proteínas-fármacos
CA2829736C (en) 2011-03-16 2020-07-21 Seattle Genetics, Inc. N-carboxyalkylauristatins and use thereof
EP3501546A3 (de) 2011-04-21 2019-09-18 Seattle Genetics, Inc. Cystein-wirkstoff konjugate und ihre verwendung
CN103717595A (zh) 2011-05-27 2014-04-09 Ambrx公司 含有非天然氨基酸连接的海兔毒素衍生物的组合物、涉及该海兔毒素衍生物的方法及其用途
TWI589592B (zh) 2011-11-17 2017-07-01 輝瑞股份有限公司 胞毒性肽類以及其抗體藥物共軛體
EP3539982B1 (en) * 2011-12-23 2025-02-19 Pfizer Inc. Engineered antibody constant regions for site-specific conjugation and methods and uses therefor
SG11201407017WA (en) 2012-06-04 2014-12-30 Irm Llc Site-specific labeling methods and molecules produced thereby
CA2900755C (en) 2013-02-08 2021-07-20 Irm Llc Specific sites for modifying antibodies to make immunoconjugates

Also Published As

Publication number Publication date
WO2015095301A2 (en) 2015-06-25
AU2014364812B2 (en) 2017-05-25
EP3753578A1 (en) 2020-12-23
AU2014364812A1 (en) 2016-07-07
US10787480B2 (en) 2020-09-29
US20160311853A1 (en) 2016-10-27
MX2016007865A (es) 2017-01-11
CA2930614A1 (en) 2015-06-25
IL245558B (en) 2020-01-30
JP2017503777A (ja) 2017-02-02
US9988420B2 (en) 2018-06-05
BR112016012538A2 (pt) 2017-09-26
US10392421B2 (en) 2019-08-27
JP6636925B2 (ja) 2020-01-29
JP2020023514A (ja) 2020-02-13
ES2758506T3 (es) 2020-05-05
US20190382441A1 (en) 2019-12-19
EP3082877B1 (en) 2019-08-28
US20180244717A1 (en) 2018-08-30
SG11201604877UA (en) 2016-07-28
WO2015095301A3 (en) 2015-09-03
PL3082877T3 (pl) 2020-02-28
EA201691251A1 (ru) 2016-11-30
EP3082877A2 (en) 2016-10-26
IL245558A0 (en) 2016-06-30
PT3082877T (pt) 2019-12-03
CN105899526A (zh) 2016-08-24

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