DE10254439A1 - Tubulysine, Herstellungsverfahren und Tubulysin-Mittel - Google Patents

Tubulysine, Herstellungsverfahren und Tubulysin-Mittel Download PDF

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Publication number
DE10254439A1
DE10254439A1 DE10254439A DE10254439A DE10254439A1 DE 10254439 A1 DE10254439 A1 DE 10254439A1 DE 10254439 A DE10254439 A DE 10254439A DE 10254439 A DE10254439 A DE 10254439A DE 10254439 A1 DE10254439 A1 DE 10254439A1
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DE
Germany
Prior art keywords
alkyl
compound
alkenyl
general formula
type
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.)
Withdrawn
Application number
DE10254439A
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German (de)
English (en)
Inventor
Gerhard Hoefle
Nicole Glaser
Heinrich Steinmetz
Thomas Leibold
Florenz Sasse
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.)
Helmholtz Zentrum Fuer Infektionsforschung De GmbH
Original Assignee
Helmholtz Zentrum fuer Infektionsforschung HZI GmbH
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 Helmholtz Zentrum fuer Infektionsforschung HZI GmbH filed Critical Helmholtz Zentrum fuer Infektionsforschung HZI GmbH
Priority to DE10254439A priority Critical patent/DE10254439A1/de
Priority to EP03775204A priority patent/EP1562979B1/de
Priority to AU2003283282A priority patent/AU2003283282A1/en
Priority to EP08018687A priority patent/EP2028185A1/de
Priority to DE50310721T priority patent/DE50310721D1/de
Priority to JP2004552485A priority patent/JP4620467B2/ja
Priority to AT03775204T priority patent/ATE412659T1/de
Priority to PCT/EP2003/011603 priority patent/WO2004046170A2/de
Priority to US10/535,630 priority patent/US7754885B2/en
Publication of DE10254439A1 publication Critical patent/DE10254439A1/de
Withdrawn legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
    • C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
    • C07D417/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing three or more hetero rings
    • 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
    • C07K5/021—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)n-C(=0)-, n being 5 or 6; for n > 6, classification in C07K5/06 - C07K5/10, according to the moiety having normal peptide bonds
    • 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)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Proteomics, Peptides & Aminoacids (AREA)
  • Crystallography & Structural Chemistry (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biophysics (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Polysaccharides And Polysaccharide Derivatives (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)
DE10254439A 2002-11-21 2002-11-21 Tubulysine, Herstellungsverfahren und Tubulysin-Mittel Withdrawn DE10254439A1 (de)

Priority Applications (9)

Application Number Priority Date Filing Date Title
DE10254439A DE10254439A1 (de) 2002-11-21 2002-11-21 Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
EP03775204A EP1562979B1 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin-mittel
AU2003283282A AU2003283282A1 (en) 2002-11-21 2003-10-20 Tubulysins, method for producing the same and tubulysin preparations
EP08018687A EP2028185A1 (de) 2002-11-21 2003-10-20 Tubulysine und Tubulysin-Mittel
DE50310721T DE50310721D1 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin-mittel
JP2004552485A JP4620467B2 (ja) 2002-11-21 2003-10-20 チューブライシン、その製造方法、及び、チューブライシン製剤
AT03775204T ATE412659T1 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin- mittel
PCT/EP2003/011603 WO2004046170A2 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin-mittel
US10/535,630 US7754885B2 (en) 2002-11-21 2003-10-20 Tubulysins, method for producing the same and tubulysin preparations

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
DE10254439A DE10254439A1 (de) 2002-11-21 2002-11-21 Tubulysine, Herstellungsverfahren und Tubulysin-Mittel

Publications (1)

Publication Number Publication Date
DE10254439A1 true DE10254439A1 (de) 2004-06-03

Family

ID=32240267

Family Applications (2)

Application Number Title Priority Date Filing Date
DE10254439A Withdrawn DE10254439A1 (de) 2002-11-21 2002-11-21 Tubulysine, Herstellungsverfahren und Tubulysin-Mittel
DE50310721T Expired - Lifetime DE50310721D1 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin-mittel

Family Applications After (1)

Application Number Title Priority Date Filing Date
DE50310721T Expired - Lifetime DE50310721D1 (de) 2002-11-21 2003-10-20 Tubulysine, herstellungsverfahren und tubulysin-mittel

Country Status (7)

Country Link
US (1) US7754885B2 (https=)
EP (2) EP1562979B1 (https=)
JP (1) JP4620467B2 (https=)
AT (1) ATE412659T1 (https=)
AU (1) AU2003283282A1 (https=)
DE (2) DE10254439A1 (https=)
WO (1) WO2004046170A2 (https=)

Cited By (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP2409983A1 (en) 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
WO2015127685A1 (en) 2014-02-28 2015-09-03 Hangzhou Dac Biotech Co., Ltd Charged linkers and their uses for conjugation
WO2015151081A2 (en) 2015-07-12 2015-10-08 Suzhou M-Conj Biotech Co., Ltd Bridge linkers for conjugation of a cell-binding molecule
EP3210627A1 (en) 2012-07-12 2017-08-30 Hangzhou Dac Biotech Co., Ltd Conjugates of cell binding molecules with cytotoxic agents
US10131682B2 (en) 2012-11-24 2018-11-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
US10232051B2 (en) 2015-07-15 2019-03-19 Hangzhou Dac Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
WO2021000067A1 (zh) 2019-06-29 2021-01-07 杭州多禧生物科技有限公司 一种细胞结合分子-Tubulysin衍生物偶联物及其制备方法
EP3888691A1 (en) 2016-11-14 2021-10-06 Hangzhou Dac Biotech Co., Ltd. Conjugation linkers, cell binding molecule-drug conjugates containing the likers, methods of making and uses such conjugates with the linkers
WO2023078273A1 (en) 2021-11-03 2023-05-11 Hangzhou Dac Biotech Co., Ltd. Specific conjugation for an antibody-drug conjugate

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EP1389209B1 (en) * 2001-04-24 2009-04-08 Purdue Research Foundation Folate mimetics and folate-receptor binding conjugates thereof
WO2003097647A1 (en) * 2002-05-15 2003-11-27 Endocyte, Inc. Vitamin-mitomycin conjugates
AU2003266233A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
DK1592457T3 (da) 2003-01-27 2012-10-22 Endocyte Inc Folat-vinblastin-konjugat som lægemiddel
JP5149620B2 (ja) 2004-07-23 2013-02-20 エンドサイト，インコーポレイテッド ２価リンカーおよびその結合体
EP1863816B1 (en) * 2005-03-16 2014-06-25 Endocyte, Inc. Synthesis and purification of pteroic acid and conjugates thereof
EP2382995A3 (en) * 2005-08-19 2013-09-25 Endocyte, Inc. Ligand conjugates of Vinca alkaloids, analogs and derivatives
AU2006279304A1 (en) * 2005-08-19 2007-02-22 Endocyte, Inc. Multi-drug ligand conjugates
WO2008101231A2 (en) 2007-02-16 2008-08-21 Endocyte, Inc. Methods and compositions for treating and diagnosing kidney disease
CN104127878A (zh) 2007-03-14 2014-11-05 恩多塞特公司 结合配体连接的微管溶素递药缀合物
US8980833B2 (en) * 2007-05-10 2015-03-17 R&D-Biopharmaceuticals Gmbh Tubulysine derivatives
BRPI0812970A2 (pt) 2007-06-25 2019-09-24 Endocyte Inc conjugados contendo espaçadores hidrofílicos
US9877965B2 (en) 2007-06-25 2018-01-30 Endocyte, Inc. Vitamin receptor drug delivery conjugates for treating inflammation
US8476451B2 (en) * 2007-07-20 2013-07-02 The Regents Of The University Of California Tubulysin D analogues
EP2181101A2 (en) * 2007-07-20 2010-05-05 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysin d analogues
US9187521B2 (en) 2007-10-25 2015-11-17 Endocyte, Inc. Tubulysins and processes for preparing
EP2174947A1 (en) * 2008-09-25 2010-04-14 Universität des Saarlandes Bioactive pre-tubulysins and use thereof
IT1394860B1 (it) 2009-07-22 2012-07-20 Kemotech S R L Composti farmaceutici
US8394922B2 (en) 2009-08-03 2013-03-12 Medarex, Inc. Antiproliferative compounds, conjugates thereof, methods therefor, and uses thereof
AU2011285532B2 (en) 2010-08-06 2015-09-10 Endocyte, Inc. Processes for preparing tubulysins
WO2012171020A1 (en) 2011-06-10 2012-12-13 Mersana Therapeutics, Inc. Protein-polymer-drug conjugates
CN104244718A (zh) * 2011-12-05 2014-12-24 伊格尼卡生物治疗公司 抗体-药物缀合物以及相关化合物、组合物和方法
US10080805B2 (en) 2012-02-24 2018-09-25 Purdue Research Foundation Cholecystokinin B receptor targeting for imaging and therapy
US20140080175A1 (en) 2012-03-29 2014-03-20 Endocyte, Inc. Processes for preparing tubulysin derivatives and conjugates thereof
US9981046B2 (en) 2012-05-15 2018-05-29 Concortis Biosystems, Corp., a wholly owned Subsidiary of Sorrento Therapeutics, Inc. Drug-conjugates, conjugation methods, and uses thereof
US11873281B2 (en) 2012-07-12 2024-01-16 Hangzhou Dac Biotech Co., Ltd. Conjugates of cell binding molecules with cytotoxic agents
EP2708243A1 (en) 2012-09-17 2014-03-19 OntoChem GmbH Receptor ligand linked cytotoxic molecules
EP2908818A4 (en) 2012-10-16 2016-07-13 Endocyte Inc CONJUGATES OF DRUG DELIVERY CONTAINING ARTIFICIAL AMINO ACIDS AND METHODS OF USE
BR112015011118B1 (pt) 2012-11-15 2022-12-13 Endocyte, Inc Conjugado; composição farmacêutica; e uso de um conjugado
CA2892863C (en) 2012-12-10 2022-03-15 Mersana Therapeutics, Inc. Polymeric scaffold based on phf for targeted drug delivery
WO2014093640A1 (en) 2012-12-12 2014-06-19 Mersana Therapeutics,Inc. Hydroxy-polmer-drug-protein conjugates
RS56169B1 (sr) 2013-02-14 2017-11-30 Bristol Myers Squibb Co Jedinjenja tubulisina, metode pripreme i primena
US20140249315A1 (en) 2013-03-01 2014-09-04 Endocyte, Inc. Processes for preparing tubulysins
US10781259B2 (en) 2013-06-06 2020-09-22 Magenta Therapeutics, Inc. Modified antibodies and related compounds, compositions, and methods of use
WO2015057876A1 (en) 2013-10-15 2015-04-23 Sorrento Therapeutics Inc. Drug-conjugates with a targeting molecule and two different drugs
ES2826398T3 (es) 2013-10-15 2021-05-18 Seagen Inc Enlazadores-fármacos pegilados para una mejor farmacocinética de los conjugados ligando-fármaco
WO2015113760A1 (en) * 2014-01-28 2015-08-06 Tube Pharmaceuticals Gmbh Cytotoxic tubulysin compounds for conjugation
MX2016012830A (es) 2014-04-11 2017-01-05 Medimmune Llc Anticuerpos contra el receptor 2 del factor de crecimiento epidermico humano (her2) biespecificos.
US10077287B2 (en) 2014-11-10 2018-09-18 Bristol-Myers Squibb Company Tubulysin analogs and methods of making and use
CN105641707B (zh) * 2014-11-11 2020-11-24 杭州多禧生物科技有限公司 细胞毒素分子同细胞结合受体分子的共轭体
EP3250238B1 (en) 2015-01-28 2022-06-01 Sorrento Therapeutics, Inc. Antibody drug conjugates
SMT202000285T1 (it) 2015-11-10 2020-07-08 Medimmune Llc Molecole di legame specifiche per asct2 e loro usi
CN108367043A (zh) 2015-12-04 2018-08-03 西雅图基因公司 季铵化的微管溶素化合物的缀合物
US11793880B2 (en) 2015-12-04 2023-10-24 Seagen Inc. Conjugates of quaternized tubulysin compounds
KR20180134351A (ko) 2016-03-25 2018-12-18 시애틀 지네틱스, 인크. 페길화된 약물-링커 및 그의 중간체의 제조를 위한 공정
AU2018237683A1 (en) 2017-03-24 2019-10-31 Seagen Inc. Process for the preparation of glucuronide drug-linkers and intermediates thereof
US10988546B2 (en) 2017-08-01 2021-04-27 Medimmune, Llc BCMA monoclonal antibody-drug conjugate
US20220241377A1 (en) 2019-07-24 2022-08-04 Molgenie GmbH Receptor-targeting peptide-drug conjugates
CR20230146A (es) 2020-09-11 2023-06-07 Medimmune Ltd Moléculas de unión a b7-h4 terapéuticas
GB202117928D0 (en) 2021-12-11 2022-01-26 Cancer Research Tech Ltd Immunotherapy for cancer
KR20240159839A (ko) 2022-03-09 2024-11-06 아스트라제네카 아베 FRα에 대한 결합 분자
TW202448517A (zh) 2023-02-16 2024-12-16 瑞典商阿斯特捷利康公司 用治療性結合分子治療癌症的組合療法

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Publication number Priority date Publication date Assignee Title
DE19638870B4 (de) 1996-09-23 2009-05-14 Helmholtz-Zentrum für Infektionsforschung GmbH Tubulysine, Verfahren zu ihrer Gewinnung und sie enthaltende Mittel
DE10008089A1 (de) 2000-02-22 2001-10-31 Biotechnolog Forschung Gmbh Syntheseverfahren zur Herstellung von Tubulysinen
AU2003266233A1 (en) * 2002-07-09 2004-01-23 Morphochem Aktiengesellschaft Fur Kombinatorische Chemie Novel tubulysin analogues
US20100047841A1 (en) * 2007-02-27 2010-02-25 University Of Pittsburgh-Of The Commonwealth System Of Higher Education Synthesis of desacetoxytubulysin h and analogs thereof

Cited By (19)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2012010287A1 (en) 2010-07-19 2012-01-26 Leibniz-Institut Für Pflanzenbiochemie Tubulysin analogues
EP2409983A1 (en) 2010-07-19 2012-01-25 Leibniz-Institut für Pflanzenbiochemie (IPB) Tubulysin analogues
US9371358B2 (en) 2010-07-19 2016-06-21 Leibniz-Institut fur Pflanzenbiochemie Tubulysin analogues
EP3348280A1 (en) 2012-07-12 2018-07-18 Hangzhou Dac Biotech Co., Ltd Conjugates of cell binding molecules with cytotoxic agents
EP3210627A1 (en) 2012-07-12 2017-08-30 Hangzhou Dac Biotech Co., Ltd Conjugates of cell binding molecules with cytotoxic agents
US10131682B2 (en) 2012-11-24 2018-11-20 Hangzhou Dac Biotech Co., Ltd. Hydrophilic linkers and their uses for conjugation of drugs to a cell binding molecules
US10683314B2 (en) 2014-02-28 2020-06-16 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
US10464955B2 (en) 2014-02-28 2019-11-05 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
WO2015127685A1 (en) 2014-02-28 2015-09-03 Hangzhou Dac Biotech Co., Ltd Charged linkers and their uses for conjugation
US10696699B2 (en) 2014-02-28 2020-06-30 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
US10696700B2 (en) 2014-02-28 2020-06-30 Hangzhou Dac Biotech Co., Ltd. Charged linkers and their uses for conjugation
WO2015151081A2 (en) 2015-07-12 2015-10-08 Suzhou M-Conj Biotech Co., Ltd Bridge linkers for conjugation of a cell-binding molecule
EP4678240A2 (en) 2015-07-12 2026-01-14 Hangzhou Dac Biotech Co., Ltd. Bridge linkers for conjugation of cell-binding molecules
US10232051B2 (en) 2015-07-15 2019-03-19 Hangzhou Dac Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
US10293055B2 (en) 2015-07-15 2019-05-21 Hangzhou Dac Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
US10328157B2 (en) 2015-07-15 2019-06-25 Hangzhou Dac Biotech Co., Ltd. Acetylenedicarboxyl linkers and their uses in specific conjugation of a cell-binding molecule
EP3888691A1 (en) 2016-11-14 2021-10-06 Hangzhou Dac Biotech Co., Ltd. Conjugation linkers, cell binding molecule-drug conjugates containing the likers, methods of making and uses such conjugates with the linkers
WO2021000067A1 (zh) 2019-06-29 2021-01-07 杭州多禧生物科技有限公司 一种细胞结合分子-Tubulysin衍生物偶联物及其制备方法
WO2023078273A1 (en) 2021-11-03 2023-05-11 Hangzhou Dac Biotech Co., Ltd. Specific conjugation for an antibody-drug conjugate

Also Published As

Publication number Publication date
JP4620467B2 (ja) 2011-01-26
DE50310721D1 (de) 2008-12-11
JP2006518704A (ja) 2006-08-17
EP1562979B1 (de) 2008-10-29
EP2028185A1 (de) 2009-02-25
US7754885B2 (en) 2010-07-13
US20060128754A1 (en) 2006-06-15
AU2003283282A1 (en) 2004-06-15
WO2004046170A2 (de) 2004-06-03
ATE412659T1 (de) 2008-11-15
AU2003283282A8 (en) 2004-06-15
EP1562979A2 (de) 2005-08-17
WO2004046170A3 (de) 2004-07-01

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Owner name: HELMHOLTZ-ZENTRUM FUER INFEKTIONSFORSCHUNG GMBH, DE

8141 Disposal/no request for examination