CN103379912B - 正羧烷基耳他汀及其应用 - Google Patents

正羧烷基耳他汀及其应用 Download PDF

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Publication number
CN103379912B
CN103379912B CN201180057131.8A CN201180057131A CN103379912B CN 103379912 B CN103379912 B CN 103379912B CN 201180057131 A CN201180057131 A CN 201180057131A CN 103379912 B CN103379912 B CN 103379912B
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China
Prior art keywords
methyl
formula
methoxy
compound
benzyl
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Expired - Fee Related
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CN201180057131.8A
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English (en)
Chinese (zh)
Other versions
CN103379912A (zh
Inventor
H-G·莱尔臣
S·埃尔谢赫
B·斯泰尔特-路德维希
S·戈尔费亚
J·舒马赫
M·J·格诺特
U·科兰兹
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Seagen Inc
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Seattle Genetics Inc
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Expired - Fee Related legal-status Critical Current
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K5/00—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof
    • C07K5/04—Peptides containing up to four amino acids in a fully defined sequence; Derivatives thereof containing only normal peptide links
    • C07K5/10—Tetrapeptides
    • C07K5/1021—Tetrapeptides with the first amino acid being acidic
    • 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
    • A61K38/00—Medicinal preparations containing peptides
    • A61K38/04—Peptides having up to 20 amino acids in a fully defined sequence; Derivatives thereof
    • A61K38/08—Peptides having 5 to 11 amino acids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K1/00—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length
    • C07K1/107—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides
    • C07K1/1072—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups
    • C07K1/1077—General methods for the preparation of peptides, i.e. processes for the organic chemical preparation of peptides or proteins of any length by chemical modification of precursor peptides by covalent attachment of residues or functional groups by covalent attachment of residues other than amino acids or peptide residues, e.g. sugars, polyols, fatty acids
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07K—PEPTIDES
    • C07K7/00—Peptides having 5 to 20 amino acids in a fully defined sequence; Derivatives thereof
    • C07K7/02—Linear peptides containing at least one abnormal peptide link
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K38/00—Medicinal preparations containing peptides

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  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Epidemiology (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Engineering & Computer Science (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Analytical Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
  • Peptides Or Proteins (AREA)
CN201180057131.8A 2010-09-29 2011-09-26 正羧烷基耳他汀及其应用 Expired - Fee Related CN103379912B (zh)

Applications Claiming Priority (7)

Application Number Priority Date Filing Date Title
EP10181966 2010-09-29
EP10181966.2 2010-09-29
EP101819662 2010-09-29
EP11158466 2011-03-16
EP111584660 2011-03-16
EP11158466.0 2011-03-16
PCT/EP2011/066658 WO2012041805A1 (de) 2010-09-29 2011-09-26 N-carboxyalkyl-auristatine und ihre verwendung

Publications (2)

Publication Number Publication Date
CN103379912A CN103379912A (zh) 2013-10-30
CN103379912B true CN103379912B (zh) 2016-03-16

Family

ID=44674811

Family Applications (1)

Application Number Title Priority Date Filing Date
CN201180057131.8A Expired - Fee Related CN103379912B (zh) 2010-09-29 2011-09-26 正羧烷基耳他汀及其应用

Country Status (7)

Country Link
US (2) US8987209B2 (https=)
EP (1) EP2621508B1 (https=)
JP (1) JP5933562B2 (https=)
CN (1) CN103379912B (https=)
CA (1) CA2813056C (https=)
ES (1) ES2553874T3 (https=)
WO (1) WO2012041805A1 (https=)

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JP5933562B2 (ja) 2010-09-29 2016-06-15 シアトル ジェネティックス， インコーポレイテッド Ｎ−カルボキシアルキル−アウリスタチンおよびその使用
US9029406B2 (en) 2011-03-16 2015-05-12 Seattle Genetics, Inc N-carboxyalkylauristatins and use thereof
BR112013027119A8 (pt) * 2011-04-21 2018-03-06 Seattle Genetics Inc novos conjugados ligante-droga (adcs) e uso dos mesmos
CN104640572B (zh) * 2012-05-15 2018-04-27 索伦托医疗有限公司 药物偶联物，偶联方法，及其用途
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
AU2014337317A1 (en) 2013-10-15 2016-09-15 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
JP6636925B2 (ja) 2013-12-17 2020-01-29 ノバルティス アーゲー 細胞障害性ペプチドおよびその抱合体
HRP20190888T8 (hr) 2014-04-25 2019-10-04 Pierre Fabre Médicament Konjugat antitijela za igf-1r i lijeka i njegova upotreba u liječenju karcinoma
HUE047952T2 (hu) 2014-04-25 2020-05-28 Pf Medicament Ellenanyag-drog konjugátum és alkalmazása rák kezelésében történõ alkalmazásra
CA2951368A1 (en) 2014-06-13 2015-12-17 Novartis Ag Auristatin derivatives and conjugates thereof
EP3160513B1 (en) 2014-06-30 2020-02-12 Glykos Finland Oy Saccharide derivative of a toxic payload and antibody conjugates thereof
EP3250238B1 (en) 2015-01-28 2022-06-01 Sorrento Therapeutics, Inc. Antibody drug conjugates
CN106279352B (zh) 2015-05-29 2020-05-22 上海新理念生物医药科技有限公司 海兔毒素10的衍生物及其应用
EP3554544A4 (en) 2016-12-16 2020-07-29 Bluefin Biomedicine, Inc. ANTI-PROTEIN 1 ANTIBODY CONTAINING AN ANTI-CUB DOMAIN (CDCP1), ANTIBODY-DRUG CONJUGATES AND THEIR METHODS OF USE
CN119241554A (zh) * 2017-12-15 2025-01-03 四川科伦博泰生物医药股份有限公司 生物活性物偶联物及其制备方法和用途

Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2007008848A2 (en) * 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus
CN101573384A (zh) * 2006-10-27 2009-11-04 健泰科生物技术公司 抗体和免疫偶联物及其用途

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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
CA2370245A1 (en) 1999-05-14 2000-11-23 Boehringer Ingelheim Pharmaceuticals, Inc. Enzyme-activated anti-tumor prodrug compounds
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
US7091186B2 (en) 2001-09-24 2006-08-15 Seattle Genetics, Inc. p-Amidobenzylethers in drug delivery agents
WO2003026577A2 (en) 2001-09-24 2003-04-03 Seattle Genetics, Inc. P-amidobenzylethers in drug delivery agents
DK1545613T3 (da) 2002-07-31 2011-11-14 Seattle Genetics Inc Auristatinkonjugater og deres anvendelse til behandling af cancer, en autoimmun sygdom eller en infektiøs sygdom
EP2478912B1 (en) 2003-11-06 2016-08-31 Seattle Genetics, Inc. Auristatin conjugates with anti-HER2 or anti-CD22 antibodies and their use in therapy
US8288352B2 (en) 2004-11-12 2012-10-16 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the N terminus
ES2708763T3 (es) 2005-07-07 2019-04-11 Seattle Genetics Inc Compuestos de monometilvalina que tienen modificaciones de la cadena lateral de fenilalanina en el extremo C
BRPI0717638A2 (pt) 2006-10-27 2013-11-12 Genentech Inc Anticorpors e imunoconjugados e usos para os mesmos
JP5394246B2 (ja) * 2007-03-30 2014-01-22 ジェネンテック， インコーポレイテッド 抗体及びイムノコンジュゲートとこれらの使用方法
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JP5933562B2 (ja) 2010-09-29 2016-06-15 シアトル ジェネティックス， インコーポレイテッド Ｎ−カルボキシアルキル−アウリスタチンおよびその使用
US9029406B2 (en) 2011-03-16 2015-05-12 Seattle Genetics, Inc N-carboxyalkylauristatins and use thereof
BR112013027119A8 (pt) 2011-04-21 2018-03-06 Seattle Genetics Inc novos conjugados ligante-droga (adcs) e uso dos mesmos
SG11201403085PA (en) 2011-12-14 2014-10-30 Seattle Genetics Inc Fgfr antibody drug conjugates (adcs) and the use thereof

Patent Citations (2)

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Publication number Priority date Publication date Assignee Title
WO2007008848A2 (en) * 2005-07-07 2007-01-18 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine carboxy modifications at the c-terminus
CN101573384A (zh) * 2006-10-27 2009-11-04 健泰科生物技术公司 抗体和免疫偶联物及其用途

Non-Patent Citations (1)

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Title
Enhanced Activity of Monomethylauristatin F through Monoclonal Antibody Delivery: Effects of Linker Technology on Efficacy and Toxicity;Svetlana O. Doronina et al;《Bioconjugate Chem》;20061231;第17卷(第1期);114-124 *

Also Published As

Publication number Publication date
EP2621508A1 (de) 2013-08-07
US20130261064A1 (en) 2013-10-03
CN103379912A (zh) 2013-10-30
US20150148298A1 (en) 2015-05-28
ES2553874T3 (es) 2015-12-14
JP2013540114A (ja) 2013-10-31
WO2012041805A1 (de) 2012-04-05
CA2813056C (en) 2018-09-18
US8987209B2 (en) 2015-03-24
HK1187527A1 (en) 2014-04-11
EP2621508B1 (de) 2015-08-26
CA2813056A1 (en) 2012-04-05
JP5933562B2 (ja) 2016-06-15

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