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WO2000049019A3 - Nouveaux derives d'epothilon, leur procede de production et leur utilisation pharmaceutique - Google Patents

Nouveaux derives d'epothilon, leur procede de production et leur utilisation pharmaceutique Download PDF

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Publication number
WO2000049019A3
WO2000049019A3 PCT/EP2000/001331 EP0001331W WO0049019A3 WO 2000049019 A3 WO2000049019 A3 WO 2000049019A3 EP 0001331 W EP0001331 W EP 0001331W WO 0049019 A3 WO0049019 A3 WO 0049019A3
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WO
WIPO (PCT)
Prior art keywords
compounds
novel
epothilone derivatives
tumours
order
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.)
Ceased
Application number
PCT/EP2000/001331
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German (de)
English (en)
Other versions
WO2000049019A2 (fr
Inventor
Ulrich Klar
Wolfgang Schwede
Werner Skuballa
Bernd Buchmann
Michael Schirner
Andreas Menrad
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.)
Bayer Pharma AG
Original Assignee
Schering AG
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Filing date
Publication date
Application filed by Schering AG filed Critical Schering AG
Priority to AU38048/00A priority Critical patent/AU3804800A/en
Publication of WO2000049019A2 publication Critical patent/WO2000049019A2/fr
Publication of WO2000049019A3 publication Critical patent/WO2000049019A3/fr
Anticipated expiration legal-status Critical
Ceased legal-status Critical Current

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D405/00—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom
    • C07D405/02—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom containing two hetero rings
    • C07D405/06—Heterocyclic compounds containing both one or more hetero rings having oxygen atoms as the only ring hetero atoms, and one or more rings having nitrogen as the only ring hetero atom 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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/08—Bridged systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/10—Spiro-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D493/00—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/12—Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains three hetero rings
    • C07D493/14—Ortho-condensed systems
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
    • C07F7/02—Silicon compounds
    • C07F7/08—Compounds having one or more C—Si linkages
    • C07F7/18—Compounds having one or more C—Si linkages as well as one or more C—O—Si linkages
    • C07F7/1804—Compounds having Si-O-C linkages
    • 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

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

L'invention concerne de nouveaux dérivés d'épothilon correspondant à la formule générale (I), dans laquelle les substituants Y, Z, R?1a, R1b, R2a, R2b¿, G'-G-E-E', R?5, R6, R7, R8, R14¿ et X ont les significations données avec plus de précision dans la description. Ces nouveaux composés interagissent avec la tubuline par le fait qu'ils stabilisent des microtubules formés. Ils peuvent influer sur la division cellulaire de façon spécifique à une phase et ils conviennent pour le traitement de tumeurs malignes, par exemple des carcinomes ovarien, gastrique, du colon, du sein, du poumon, de la tête et du cou, de l'adénocarcinome, du mélanome malin, et de la leucémie lymphocytaire et myélocytaire. Ils peuvent en outre être utilisés pour la thérapie anti-angiogenèse ainsi que pour le traitement de maladies inflammatoires chroniques (psoriasis, arthrite). Pour éviter des proliférations cellulaires non contrôlées et pour améliorer la tolérance d'implants médicaux, ces composés peuvent être appliqués sur des matériaux polymères ou incorporés à ceux-ci. Les composés selon l'invention peuvent être utilisés seuls ou bien, pour l'obtention d'effets additifs ou synergiques, en combinaison avec d'autres principes actifs et classes de substances utilisables dans le traitement des tumeurs.
PCT/EP2000/001331 1999-02-18 2000-02-18 Nouveaux derives d'epothilon, leur procede de production et leur utilisation pharmaceutique Ceased WO2000049019A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU38048/00A AU3804800A (en) 1999-02-18 2000-02-18 Novel epothilone derivatives, method for producing them and their pharmaceuticaluse

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
DE19908760A DE19908760A1 (de) 1999-02-18 1999-02-18 Neue Epothilon-Derivate, Verfahren zu deren Herstellung und ihre pharmazeutische Verwendung
DE19908760.1 1999-02-18

Publications (2)

Publication Number Publication Date
WO2000049019A2 WO2000049019A2 (fr) 2000-08-24
WO2000049019A3 true WO2000049019A3 (fr) 2001-03-01

Family

ID=7899229

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP2000/001331 Ceased WO2000049019A2 (fr) 1999-02-18 2000-02-18 Nouveaux derives d'epothilon, leur procede de production et leur utilisation pharmaceutique

Country Status (3)

Country Link
AU (1) AU3804800A (fr)
DE (1) DE19908760A1 (fr)
WO (1) WO2000049019A2 (fr)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6849651B2 (en) 1996-12-03 2005-02-01 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6965034B2 (en) 1996-12-03 2005-11-15 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof

Families Citing this family (24)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ527764A (en) * 2001-02-27 2006-01-27 Novartis Ag Combination comprising a signal transduction inhibitor and an epothilone derivative
CZ305799B6 (cs) * 2001-03-14 2016-03-23 Bristol-Myers Squibb Company Kombinace analogů epothilonu a chemoterapeutických činidel pro léčení proliferačních nemocí
TWI315982B (en) * 2001-07-19 2009-10-21 Novartis Ag Combinations comprising epothilones and pharmaceutical uses thereof
AU2008203233B2 (en) * 2001-07-19 2010-04-29 Novartis Ag Combinations comprising epothilones and pharmaceutical uses thereof
US20030176368A1 (en) * 2001-09-06 2003-09-18 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
TWI287986B (en) * 2001-12-13 2007-10-11 Novartis Ag Use of Epothilones for the treatment of the carcinoid syndrome
ATE452896T1 (de) 2002-03-12 2010-01-15 Bristol Myers Squibb Co C3-cyanoepothilonderivate
CA2487147A1 (fr) * 2002-06-10 2003-12-18 Novartis Ag Combinaisons comprenant des epothilones, et utilisations pharmaceutiques de celles-ci
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
DK1767535T3 (da) 2002-08-23 2010-04-12 Sloan Kettering Inst Cancer Syntese af epothiloner, mellemprodukter deraf, analoge og deres anvendelse
EP1674098A1 (fr) 2004-12-23 2006-06-28 Schering Aktiengesellschaft Formulations parenterales stables et tolérables des substances de haut réactivité ayant une solubilité basse ou inexistante dans l'eau
CN101360494A (zh) * 2005-11-22 2009-02-04 斯克里普斯研究学院 高效埃博霉素的化学合成
EP2065054A1 (fr) 2007-11-29 2009-06-03 Bayer Schering Pharma Aktiengesellschaft Combinaisons comprenant une prostaglandine et leurs utilisations
EP2070521A1 (fr) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Nanoparticules à surface modifiée
DE102007059752A1 (de) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Funktionalisierte, feste Polymernanopartikel enthaltend Epothilone
EP2210584A1 (fr) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Composition polymère stable comprenant un copolymère séquencé d'épothilone et amphiphile
US9717803B2 (en) 2011-12-23 2017-08-01 Innate Pharma Enzymatic conjugation of polypeptides
US10132799B2 (en) 2012-07-13 2018-11-20 Innate Pharma Screening of conjugated antibodies
EP3564259A3 (fr) 2012-11-09 2020-02-12 Innate Pharma Étiquettes de reconnaissance pour la conjugaison à médiation par la tgase
WO2014140300A1 (fr) 2013-03-15 2014-09-18 Innate Pharma Conjugaison d'anticorps en phase solide médiée par la tgase
WO2014202773A1 (fr) 2013-06-20 2014-12-24 Innate Pharma Conjugaison enzymatique de polypeptides
CN105517577A (zh) 2013-06-21 2016-04-20 先天制药公司 多肽的酶促偶联
WO2019092148A1 (fr) 2017-11-10 2019-05-16 Innate Pharma Anticorps avec des résidus de glutamine fonctionnalisés

Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997019086A1 (fr) * 1995-11-17 1997-05-29 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Derives d'epothilone, leur preparation et leur utilisation
WO1999007692A2 (fr) * 1997-08-09 1999-02-18 Schering Aktiengesellschaft Nouveaux derives d'epothilone, leur procede de fabrication et leur utilisation pharmaceutique
WO1999065913A2 (fr) * 1998-06-18 1999-12-23 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Constituants secondaires d'epothilone

Patent Citations (3)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1997019086A1 (fr) * 1995-11-17 1997-05-29 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Derives d'epothilone, leur preparation et leur utilisation
WO1999007692A2 (fr) * 1997-08-09 1999-02-18 Schering Aktiengesellschaft Nouveaux derives d'epothilone, leur procede de fabrication et leur utilisation pharmaceutique
WO1999065913A2 (fr) * 1998-06-18 1999-12-23 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Constituants secondaires d'epothilone

Non-Patent Citations (7)

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Title
CHOU T C ET AL: "DESOXYEPOTHILONE B: AN EFFICACIOUS MICROTUBULE-TARGETED ANTITUMOR AGENT WITH A PROMISING IN VIVO PROFILE RELATIVE TO EPOTHILONE B", PROCEEDINGS OF THE NATIONAL ACADEMY OF SCIENCES OF USA,US,NATIONAL ACADEMY OF SCIENCE. WASHINGTON, vol. 95, no. 16, 1998, pages 9642 - 9647, XP000910107, ISSN: 0027-8424 *
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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 *
ZHEN YANG ET AL: "ANGEWANDTE CHEMIE,DE,VCH VERLAGSGESELLSCHAFT, WEINHEIM", ANGEWANDTE CHEMIE,DE,VCH VERLAGSGESELLSCHAFT, WEINHEIM, vol. 109, no. 1/02, 1997, pages 170 - 172, XP002095722, ISSN: 0044-8249 *

Cited By (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US6849651B2 (en) 1996-12-03 2005-02-01 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6965034B2 (en) 1996-12-03 2005-11-15 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6972335B2 (en) 1996-12-03 2005-12-06 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
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
AU3804800A (en) 2000-09-04
WO2000049019A2 (fr) 2000-08-24
DE19908760A1 (de) 2000-08-24

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