JP6023097B2 - Ｎカルボキシアルキルオーリスタチンおよびその使用 - Google Patents

Ｎカルボキシアルキルオーリスタチンおよびその使用 Download PDF

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Publication number
JP6023097B2
JP6023097B2 JP2013558400A JP2013558400A JP6023097B2 JP 6023097 B2 JP6023097 B2 JP 6023097B2 JP 2013558400 A JP2013558400 A JP 2013558400A JP 2013558400 A JP2013558400 A JP 2013558400A JP 6023097 B2 JP6023097 B2 JP 6023097B2
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formula
methyl
compound
methoxy
phenyl
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Japanese (ja)
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JP2014515735A (ja
JP2014515735A5 (enExample
Inventor
ハンス−ゲオルク レルヒェン，
ハンス−ゲオルク レルヒェン，
シエイク， シェリフ エル
シエイク， シェリフ エル
ベアトリクス シュトルテ−ルートヴィヒ，
ベアトリクス シュトルテ−ルートヴィヒ，
ヨハヒム シューマッハー，
ヨハヒム シューマッハー，
マルク グノート，
マルク グノート，
Original Assignee
シアトル ジェネティックス， インコーポレイテッド
シアトル ジェネティックス， インコーポレイテッド
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/07—Tetrapeptides
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P9/00—Drugs for disorders of the cardiovascular system
    • 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
    • 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
    • A61K47/62—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 a protein, peptide or polyamino acid
    • A61K47/64—Drug-peptide, drug-protein or drug-polyamino acid conjugates, i.e. the modifying agent being a peptide, protein or polyamino acid which is covalently bonded or complexed to a therapeutically active agent
    • A61K47/6415—Toxins or lectins, e.g. clostridial toxins or Pseudomonas exotoxins

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Immunology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
JP2013558400A 2011-03-16 2012-03-12 Ｎカルボキシアルキルオーリスタチンおよびその使用 Active JP6023097B2 (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP11158481 2011-03-16
EP11158481.9 2011-03-16
PCT/EP2012/054294 WO2012123423A1 (de) 2011-03-16 2012-03-12 N-carboxyalkyl-auristatine und ihre verwendung

Related Child Applications (1)

Application Number Title Priority Date Filing Date
JP2016145282A Division JP2016185987A (ja) 2011-03-16 2016-07-25 Ｎカルボキシアルキルオーリスタチンおよびその使用

Publications (3)

Publication Number Publication Date
JP2014515735A JP2014515735A (ja) 2014-07-03
JP2014515735A5 JP2014515735A5 (enExample) 2015-07-02
JP6023097B2 true JP6023097B2 (ja) 2016-11-09

Family

ID=45812791

Family Applications (2)

Application Number Title Priority Date Filing Date
JP2013558400A Active JP6023097B2 (ja) 2011-03-16 2012-03-12 Ｎカルボキシアルキルオーリスタチンおよびその使用
JP2016145282A Withdrawn JP2016185987A (ja) 2011-03-16 2016-07-25 Ｎカルボキシアルキルオーリスタチンおよびその使用

Family Applications After (1)

Application Number Title Priority Date Filing Date
JP2016145282A Withdrawn JP2016185987A (ja) 2011-03-16 2016-07-25 Ｎカルボキシアルキルオーリスタチンおよびその使用

Country Status (7)

Country Link
US (1) US9029406B2 (enExample)
EP (1) EP2686336B1 (enExample)
JP (2) JP6023097B2 (enExample)
CN (1) CN103764667B (enExample)
CA (1) CA2829736C (enExample)
ES (1) ES2543888T3 (enExample)
WO (1) WO2012123423A1 (enExample)

Families Citing this family (14)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
TWI582112B (zh) * 2011-04-21 2017-05-11 西雅圖遺傳學公司 新穎結合劑－藥物接合物（ＡＤＣｓ）及其用途（二）
PT3327027T (pt) 2011-11-17 2021-02-15 Pfizer Péptidos citotóxicos e seus conjugados de anticorpos e fármacos
US10226535B2 (en) 2012-12-10 2019-03-12 Mersana Therapeutics, Inc. Auristatin compounds and conjugates thereof
FR3005051A1 (fr) * 2013-04-25 2014-10-31 Pf Medicament Derives de la dolastatine 10 et d'auristatines
US10208125B2 (en) 2013-07-15 2019-02-19 University of Pittsburgh—of the Commonwealth System of Higher Education Anti-mucin 1 binding agents and uses thereof
EP3753578A1 (en) 2013-12-17 2020-12-23 Novartis AG Cytotoxic peptides and conjugates thereof
CA2935077C (en) 2013-12-27 2022-03-15 Geoffrey C. Winters Sulfonamide-containing linkage systems for drug conjugates
UA120364C2 (uk) 2014-04-25 2019-11-25 Пьєр Фабр Медікамент Кон'югат антитіла до igf-1r з лікарським засобом
PL3134125T3 (pl) 2014-04-25 2020-04-30 Pierre Fabre Médicament Koniugat przeciwciało-lek i jego zastosowanie do leczenia raka
US9884817B2 (en) 2014-06-13 2018-02-06 Novartis Ag Auristatin derivatives and conjugates thereof
JP7350313B2 (ja) 2016-12-16 2023-09-26 ブルーフィン バイオメディシン， インコーポレイテッド 抗ｃｕｂドメイン含有タンパク質１（ｃｄｃｐ１）抗体、抗体薬物コンジュゲート、およびその使用方法
CN111393346B (zh) * 2020-06-02 2020-08-25 凯莱英生命科学技术(天津)有限公司 N-Boc-Dolaproine及Boc-Dap DCHA的合成方法
WO2023033129A1 (ja) 2021-09-03 2023-03-09 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 (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5663149A (en) 1994-12-13 1997-09-02 Arizona Board Of Regents Acting On Behalf Of Arizona State University Human cancer inhibitory pentapeptide heterocyclic and halophenyl amides
WO1999035164A1 (en) 1998-01-09 1999-07-15 Arizona Board Of Regents, A Body Corporate, Acting On Behalf Of Arizona State University Anti-cryptococcal peptides
JP2002544242A (ja) 1999-05-14 2002-12-24 ベーリンガー インゲルハイム ファーマシューティカルズ インコーポレイテッド 酵素活性化抗腫瘍プロドラッグ化合物
US6323315B1 (en) 1999-09-10 2001-11-27 Basf Aktiengesellschaft Dolastatin peptides
US6884869B2 (en) 2001-04-30 2005-04-26 Seattle Genetics, Inc. Pentapeptide compounds and uses related thereto
US6737409B2 (en) * 2001-07-19 2004-05-18 Hoffmann-La Roche Inc. Dolastatin 10 derivatives
WO2003026577A2 (en) 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
CA2802205C (en) 2002-07-31 2016-01-19 Seattle Genetics, Inc. Drug conjugates and their use for treating cancer, an autoimmune disease or an infectious disease
NZ583292A (en) 2003-11-06 2012-03-30 Seattle Genetics Inc Monomethylvaline compounds capable of conjugation to ligands
AU2005332660A1 (en) 2004-11-12 2006-12-14 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the N terminus
AU2006269422B2 (en) 2005-07-07 2012-12-06 Seagen Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the C-terminus
US8871720B2 (en) 2005-07-07 2014-10-28 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the C-terminus
MX2009003938A (es) 2006-10-27 2009-04-24 Genentech Inc Anticuerpos e inmunoconjugados y sus usos.
DK2842575T3 (da) 2008-03-18 2017-11-27 Seattle Genetics Inc Auristatin-lægemiddel-linker-konjugater
JP5791707B2 (ja) 2010-06-10 2015-10-07 シアトル ジェネティックス， インコーポレイテッド 新規アウリスタチン誘導体およびその使用
ES2553874T3 (es) 2010-09-29 2015-12-14 Seattle Genetics, Inc. N-Carboxialquil-auristatinas y su uso
TWI582112B (zh) 2011-04-21 2017-05-11 西雅圖遺傳學公司 新穎結合劑－藥物接合物（ＡＤＣｓ）及其用途（二）

Also Published As

Publication number Publication date
EP2686336A1 (de) 2014-01-22
CA2829736A1 (en) 2012-09-20
WO2012123423A1 (de) 2012-09-20
CA2829736C (en) 2020-07-21
HK1191034A1 (en) 2014-07-18
JP2014515735A (ja) 2014-07-03
CN103764667A (zh) 2014-04-30
US20140080763A1 (en) 2014-03-20
US9029406B2 (en) 2015-05-12
ES2543888T3 (es) 2015-08-25
JP2016185987A (ja) 2016-10-27
EP2686336B1 (de) 2015-05-06
CN103764667B (zh) 2017-06-20

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