WO2000049020A3 - Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung - Google Patents

Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung Download PDF

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Publication number
WO2000049020A3
WO2000049020A3 PCT/EP2000/001332 EP0001332W WO0049020A3 WO 2000049020 A3 WO2000049020 A3 WO 2000049020A3 EP 0001332 W EP0001332 W EP 0001332W WO 0049020 A3 WO0049020 A3 WO 0049020A3
Authority
WO
WIPO (PCT)
Prior art keywords
cancer
novel
compounds
inventive compounds
suited
Prior art date
Application number
PCT/EP2000/001332
Other languages
English (en)
French (fr)
Other versions
WO2000049020A2 (de
Inventor
Ulrich Klar
Wolfgang Schwede
Bernd Buchmann
Werner Skuballa
Michael Schirner
Michael Grimm
Original Assignee
Schering Ag
Ulrich Klar
Wolfgang Schwede
Bernd Buchmann
Werner Skuballa
Michael Schirner
Michael Grimm
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 Schering Ag, Ulrich Klar, Wolfgang Schwede, Bernd Buchmann, Werner Skuballa, Michael Schirner, Michael Grimm filed Critical Schering Ag
Priority to AU31566/00A priority Critical patent/AU3156600A/en
Publication of WO2000049020A2 publication Critical patent/WO2000049020A2/de
Publication of WO2000049020A3 publication Critical patent/WO2000049020A3/de

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Classifications

    • 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
    • C07D417/06—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 carbon chain containing only aliphatic carbon atoms
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • Y—GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS; GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC; TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS
    • Y02—TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINST CLIMATE CHANGE
    • Y02P—CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION OR PROCESSING OF GOODS
    • Y02P20/00—Technologies relating to chemical industry
    • Y02P20/50—Improvements relating to the production of bulk chemicals
    • Y02P20/55—Design of synthesis routes, e.g. reducing the use of auxiliary or protecting groups

Abstract

Die vorliegende Erfindung betrifft die neuen Epothilon-Derivate der allgemeinen Formel (I), worin die Substituenten Y, Z, R?1a, R1b, R2a, R2b, R3a, R3b, E, R5, R6, R7, R8, R14¿ und X die in der Beschreibung näher angegebenen Bedeutungen haben. Die neuen Verbindungen interagieren mit Tubulin, indem sie gebildete Mikrotubuli stabilisieren. Sie sind in der Lage, die Zellteilung phasenspezifisch zu beeinflussen und sind zur Behandlung maligner Tumoren geeignet, beispielsweise Ovarial-, Magen-, Colon-, Adeno-, Brust-, Lungen-, Kopf- und Nacken-Karzinome, malignes Melanom, akute lymphozytäre und myelocytäre Leukämie. Ausserdem sind sie zur Anti-Angiogenese-Therapie sowie zur Behandlung chronischer entzündlicher Erkrankungen (Psoriasis, Arthritis) geeignet. Zur Vermeidung unkontrollierter Zellwucherungen an sowie der besseren Verträglichkeit von medizinischen Implantaten lassen sie sich in polymere Materialien auf- bzw. einbringen. Die erfindungsgemässen Verbindungen können alleine oder zur Erzielung additiver oder synergistischer Wirkungen in Kombination mit weiteren in der Tumortherapie anwendbaren Prinzipien und Substanzklassen verwendet werden.
PCT/EP2000/001332 1999-02-18 2000-02-18 Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung WO2000049020A2 (de)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU31566/00A AU3156600A (en) 1999-02-18 2000-02-18 Novel epothilon derivatives, method for the production thereof and their pharmaceutical application

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19908763A DE19908763A1 (de) 1999-02-18 1999-02-18 Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung
DE19908763.6 1999-02-18

Publications (2)

Publication Number Publication Date
WO2000049020A2 WO2000049020A2 (de) 2000-08-24
WO2000049020A3 true WO2000049020A3 (de) 2000-12-28

Family

ID=7899231

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/001332 WO2000049020A2 (de) 1999-02-18 2000-02-18 Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung

Country Status (3)

Country Link
AU (1) AU3156600A (de)
DE (1) DE19908763A1 (de)
WO (1) WO2000049020A2 (de)

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE41990E1 (en) 1996-12-03 2010-12-07 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof

Families Citing this family (17)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
ATE452896T1 (de) 2002-03-12 2010-01-15 Bristol Myers Squibb Co C3-cyanoepothilonderivate
JP4791183B2 (ja) 2002-08-23 2011-10-12 スローン−ケッタリング インスティトュート フォア キャンサー リサーチ エポチロン、その中間体、類似体の合成およびその使用
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
EP1674098A1 (de) 2004-12-23 2006-06-28 Schering Aktiengesellschaft Stabile, unbedenkliche parenterale Formulierungen von hochreaktiven organischen Arzneimitteln mit niedriger oder keiner wässrigen Löslichkeit
EP2065054A1 (de) 2007-11-29 2009-06-03 Bayer Schering Pharma Aktiengesellschaft Kombinationen mit einem Prostaglandin und Verwendungen davon
EP2070521A1 (de) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Nanopartikel mit modifizierter Oberfläche
DE102007059752A1 (de) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Funktionalisierte, feste Polymernanopartikel enthaltend Epothilone
EP2210584A1 (de) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Stabile Polymerzusammensetzung mit einem Epothilon und einem amphiphilischen Blockpolymer
US9717803B2 (en) 2011-12-23 2017-08-01 Innate Pharma Enzymatic conjugation of polypeptides
EP2872894B1 (de) 2012-07-13 2019-04-17 Innate Pharma Screening von konjugierten antikörpern
US10036010B2 (en) 2012-11-09 2018-07-31 Innate Pharma Recognition tags for TGase-mediated conjugation
WO2014140300A1 (en) 2013-03-15 2014-09-18 Innate Pharma Solid phase tgase-mediated conjugation of antibodies
US10071169B2 (en) 2013-06-20 2018-09-11 Innate Pharma Enzymatic conjugation of polypeptides
AU2014283185B2 (en) 2013-06-21 2019-05-02 Innate Pharma Enzymatic conjugation of polypeptides
CN107434780B (zh) * 2016-05-26 2020-08-07 上海韬勤生物医药科技有限公司 一种ar-13324的制备方法
WO2019092148A1 (en) 2017-11-10 2019-05-16 Innate Pharma Antibodies with functionalized glutamine residues
CN116940582A (zh) * 2020-11-11 2023-10-24 渤健马萨诸塞州股份有限公司 寡核苷酸、试剂及其制备

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025929A1 (en) * 1996-12-13 1998-06-18 Novartis Ag Epothilone analogs

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998025929A1 (en) * 1996-12-13 1998-06-18 Novartis Ag Epothilone analogs

Non-Patent Citations (4)

* Cited by examiner, † Cited by third party
Title
GLUNZ, PETER W. ET AL: "The synthesis and evaluation of 12,13-benzodesoxyepothilone B: a highly convergent route", TETRAHEDRON LETT. (1999), 40(38), 6895-6898, XP004175623 *
HARRIS, CHRISTINA R. ET AL: "New Chemical Synthesis of the Promising Cancer Chemotherapeutic Agent 12,13-Desoxyepothilone B: Discovery of a Surprising Long-Range Effect on the Diastereoselectivity of an Aldol Condensation", J. AM. CHEM. SOC. (1999), 121(30), 7050-7062, XP002150959 *
K C NICOLAOU ET AL: "Probing the ring size of epothilones: total synthesis of [14]-, [15]-, [17]-, and [18]Epothilones A", ANGEWANDTE CHEMIE. INTERNATIONAL EDITION,DE,VERLAG CHEMIE. WEINHEIM, vol. 37, no. 1/02, 1998, pages 81 - 84, XP002131226, ISSN: 0570-0833 *
NICOLAOU K C ET AL: "Chemical Biology of Epothilones", ANGEWANDTE CHEMIE. INTERNATIONAL EDITION,DE,VERLAG CHEMIE. WEINHEIM, vol. 37, no. 15, August 1998 (1998-08-01), pages 2014 - 2045, XP002131418, ISSN: 0570-0833 *

Cited By (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
USRE41990E1 (en) 1996-12-03 2010-12-07 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof

Also Published As

Publication number Publication date
WO2000049020A2 (de) 2000-08-24
DE19908763A1 (de) 2000-08-24
AU3156600A (en) 2000-09-04

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