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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    • 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)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Biochemistry (AREA)
  • Biophysics (AREA)
  • Genetics & Genomics (AREA)
  • Molecular Biology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Gastroenterology & Hepatology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Immunology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Crystallography & Structural Chemistry (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
EP101819662 2010-09-29
EP10181966.2 2010-09-29
EP111584660 2011-03-16
EP11158466.0 2011-03-16
EP11158466 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 (OSRAM)
EP (1) EP2621508B1 (OSRAM)
JP (1) JP5933562B2 (OSRAM)
CN (1) CN103379912B (OSRAM)
CA (1) CA2813056C (OSRAM)
ES (1) ES2553874T3 (OSRAM)
WO (1) WO2012041805A1 (OSRAM)

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WO2012041805A1 (de) 2010-09-29 2012-04-05 Bayer Pharma Aktiengesellschaft N-carboxyalkyl-auristatine und ihre verwendung
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
WO2013173391A1 (en) 2012-05-15 2013-11-21 Concortis Biosystems, Corp Drug-conjugates, conjugation methods, and uses 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
CN106132431A (zh) 2013-10-15 2016-11-16 索伦托治疗有限公司 具有靶向分子和两种不同药物的药物偶联物
PL3082877T3 (pl) 2013-12-17 2020-02-28 Novartis Ag Cytotoksyczne peptydy i ich koniugaty
KR101795984B1 (ko) 2014-04-25 2017-11-10 피에르 파브르 메디카먼트 Igf-1r 항체-약물-결합체 및 암의 치료를 위한 그의 용도
EP3134125B1 (en) 2014-04-25 2019-10-09 Pierre Fabre Medicament Antibody-drug-conjugate and its use for the treatment of cancer
KR20170016479A (ko) 2014-06-13 2017-02-13 노파르티스 아게 아우리스타틴 유도체 및 그의 접합체
WO2016001485A1 (en) 2014-06-30 2016-01-07 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
CN110234348B (zh) 2016-12-16 2024-06-25 蓝鳍生物医药公司 抗-含cub结构域蛋白1(cdcp1)抗体、抗体药物缀合物及其使用方法
CA3080236A1 (en) * 2017-12-15 2019-06-20 Sichuan Kelun-Biotech Biopharmaceutical Co., Ltd. Bioactive molecule conjugate, preparation method and use thereof

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
ATE284412T1 (de) 1998-01-09 2004-12-15 Univ Arizona State Anti-kryptokokkus peptide
MXPA01011502A (es) 1999-05-14 2003-08-20 Boehringer Ingelheim Pharma Compuestos de tipo profarmaco anti-tumorigenos, activados por enzimas.
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
JP4741838B2 (ja) 2002-07-31 2011-08-10 シアトル ジェネティクス，インコーポレーテッド 癌、自己免疫疾患または感染症を治療するための薬物結合体およびその使用
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
CA2586909A1 (en) 2004-11-12 2006-12-14 Seattle Genetics, Inc. Auristatins having an aminobenzoic acid unit at the n terminus
CA2614436C (en) 2005-07-07 2016-05-17 Seattle Genetics, Inc. Monomethylvaline compounds having phenylalanine side-chain modifications at the c-terminus
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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
EP2842575B1 (en) 2008-03-18 2017-09-27 Seattle Genetics, Inc. Auristatin drug linker conjugates
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WO2012041805A1 (de) 2010-09-29 2012-04-05 Bayer Pharma Aktiengesellschaft N-carboxyalkyl-auristatine und ihre verwendung
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
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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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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
ES2553874T3 (es) 2015-12-14
US20150148298A1 (en) 2015-05-28
EP2621508A1 (de) 2013-08-07
EP2621508B1 (de) 2015-08-26
CN103379912A (zh) 2013-10-30
JP5933562B2 (ja) 2016-06-15
CA2813056A1 (en) 2012-04-05
JP2013540114A (ja) 2013-10-31
WO2012041805A1 (de) 2012-04-05
CA2813056C (en) 2018-09-18
US8987209B2 (en) 2015-03-24
US20130261064A1 (en) 2013-10-03
HK1187527A1 (en) 2014-04-11

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