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WO1999067253A3 - Desmethyl epothilones - Google Patents

Desmethyl epothilones Download PDF

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Publication number
WO1999067253A3
WO1999067253A3 PCT/EP1999/004299 EP9904299W WO9967253A3 WO 1999067253 A3 WO1999067253 A3 WO 1999067253A3 EP 9904299 W EP9904299 W EP 9904299W WO 9967253 A3 WO9967253 A3 WO 9967253A3
Authority
WO
WIPO (PCT)
Prior art keywords
formula
compounds
desmethyl
epothilones
synthesis
Prior art date
Application number
PCT/EP1999/004299
Other languages
French (fr)
Other versions
WO1999067253A2 (en
Inventor
Kyriacos Costa Nicolaou
David Hepworth
Maurice Raymond Verscho Finlay
Nigel Paul King
Original Assignee
Novartis Ag
Novartis Erfind Verwalt Gmbh
Scripps Research Inst
Kyriacos Costa Nicolaou
David Hepworth
Maurice Raymond Verscho Finlay
Nigel Paul King
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
Priority claimed from US09/102,602 external-priority patent/US6380394B1/en
Application filed by Novartis Ag, Novartis Erfind Verwalt Gmbh, Scripps Research Inst, Kyriacos Costa Nicolaou, David Hepworth, Maurice Raymond Verscho Finlay, Nigel Paul King filed Critical Novartis Ag
Priority to AU47752/99A priority Critical patent/AU4775299A/en
Publication of WO1999067253A2 publication Critical patent/WO1999067253A2/en
Publication of WO1999067253A3 publication Critical patent/WO1999067253A3/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D417/00Heterocyclic 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
    • C07D417/02Heterocyclic 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
    • C07D417/06Heterocyclic 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
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D493/00Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system
    • C07D493/02Heterocyclic compounds containing oxygen atoms as the only ring hetero atoms in the condensed system in which the condensed system contains two hetero rings
    • C07D493/04Ortho-condensed systems

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Oxygen Or Sulfur (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

The invention relates to compounds of formula (I), wherein the group A-D represents a group of formula (Ia) or of formula (Ib) wherein Q is hydroxy, iodo or hydrogen, and in addition to methods of synthesis for these compounds, as well as for the synthesis of epothilone B, and intermediates. The compounds of formula (I) can be used e.g. in the treatment of proliferative diseases.
PCT/EP1999/004299 1998-06-22 1999-06-21 Desmethyl epothilones WO1999067253A2 (en)

Priority Applications (1)

Application Number Priority Date Filing Date Title
AU47752/99A AU4775299A (en) 1998-06-22 1999-06-21 Desmethyl epothilones

Applications Claiming Priority (6)

Application Number Priority Date Filing Date Title
US09/102,602 US6380394B1 (en) 1996-12-13 1998-06-22 Epothilone analogs
US09/102,602 1998-06-22
US12315599P 1999-03-06 1999-03-06
US60/123,155 1999-03-06
US12465399P 1999-03-16 1999-03-16
US60/124,653 1999-03-16

Publications (2)

Publication Number Publication Date
WO1999067253A2 WO1999067253A2 (en) 1999-12-29
WO1999067253A3 true WO1999067253A3 (en) 2000-04-20

Family

ID=27379376

Family Applications (1)

Application Number Title Priority Date Filing Date
PCT/EP1999/004299 WO1999067253A2 (en) 1998-06-22 1999-06-21 Desmethyl epothilones

Country Status (2)

Country Link
AU (1) AU4775299A (en)
WO (1) WO1999067253A2 (en)

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 (38)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
DK1005465T3 (en) 1997-08-09 2007-11-05 Bayer Schering Pharma Ag New epothilone derivatives, processes for their preparation and their pharmaceutical use
FR2775187B1 (en) 1998-02-25 2003-02-21 Novartis Ag USE OF EPOTHILONE B FOR THE MANUFACTURE OF AN ANTIPROLIFERATIVE PHARMACEUTICAL PREPARATION AND A COMPOSITION COMPRISING EPOTHILONE B AS AN IN VIVO ANTIPROLIFERATIVE AGENT
US6410301B1 (en) 1998-11-20 2002-06-25 Kosan Biosciences, Inc. Myxococcus host cells for the production of epothilones
JP4662635B2 (en) 1998-11-20 2011-03-30 コーサン バイオサイエンシーズ, インコーポレイテッド Recombinant methods and materials for producing epothilone and epothilone derivatives
CN1340053A (en) * 1999-02-11 2002-03-13 舍林股份公司 Epothilon derivatives, method for the production and the use as pharmaceuticals
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
TR200102969T2 (en) 1999-04-15 2002-08-21 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors.
US7125893B1 (en) 1999-04-30 2006-10-24 Schering Ag 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
WO2001092255A2 (en) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same
JP2005500974A (en) 2000-10-13 2005-01-13 ザ ユニバーシテイ オブ ミシシッピー Synthesis of epothilones and related analogues
EP1340498A1 (en) * 2002-03-01 2003-09-03 Schering Aktiengesellschaft Use of epothilones in the treatment of brain diseases associated with proliferative processes
AU2003218110A1 (en) 2002-03-12 2003-09-29 Bristol-Myers Squibb Company C3-cyano epothilone derivatives
US7405234B2 (en) 2002-05-17 2008-07-29 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
WO2004045518A2 (en) 2002-11-15 2004-06-03 Bristol-Myers Squibb Company Open chain prolyl urea-related modulators of androgen receptor function
US7820702B2 (en) 2004-02-04 2010-10-26 Bristol-Myers Squibb Company Sulfonylpyrrolidine modulators of androgen receptor function and method
US7378426B2 (en) 2004-03-01 2008-05-27 Bristol-Myers Squibb Company Fused heterotricyclic compounds as inhibitors of 17β-hydroxysteroid dehydrogenase 3
US7696241B2 (en) 2004-03-04 2010-04-13 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
US7625923B2 (en) 2004-03-04 2009-12-01 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
US10675326B2 (en) 2004-10-07 2020-06-09 The Board Of Trustees Of The University Of Illinois Compositions comprising cupredoxins for treating cancer
EP1674098A1 (en) 2004-12-23 2006-06-28 Schering Aktiengesellschaft Stable and tolerable parental formulations of highly reactive organic drug substances with low or no solubility in water
CA2671492A1 (en) 2006-12-04 2008-06-12 The Board Of Trustees Of The University Of Illinois Compositions and methods to treat cancer with cupredoxins and cpg rich dna
JP2010518123A (en) 2007-02-08 2010-05-27 ザ・ボード・オブ・トラスティーズ・オブ・ザ・ユニバーシティ・オブ・イリノイ Compositions and methods for preventing cancer with cupredoxins
EP2065054A1 (en) 2007-11-29 2009-06-03 Bayer Schering Pharma Aktiengesellschaft Combinations comprising a prostaglandin and uses thereof
DE102007059752A1 (en) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Functionalized solid polymer nanoparticles containing epothilones
EP2070521A1 (en) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Surface-modified nanoparticles
EP2210584A1 (en) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Stable polymeric composition comprising an epothilone and an amphiphilic block copolymer
US20110300150A1 (en) 2010-05-18 2011-12-08 Scott Eliasof Compositions and methods for treatment of autoimmune and other disease
EP2665493B1 (en) 2011-01-20 2018-03-21 Board Of Regents, The University Of Texas System Mri markers, delivery and extraction systems, and methods of manufacture and use thereof
CN102863474A (en) 2011-07-09 2013-01-09 陈小平 Platinum compounds for treating cell proliferative diseases and preparation method and application thereof
CN102993239A (en) 2011-09-19 2013-03-27 陈小平 Platinum compound of succinic acid derivative with leaving group containing amino or alkylamino
US9764038B2 (en) 2011-12-23 2017-09-19 Innate Pharma Enzymatic conjugation of antibodies
EP2872894B1 (en) 2012-07-13 2019-04-17 Innate Pharma Screening of conjugated antibodies
EP3564259A3 (en) 2012-11-09 2020-02-12 Innate Pharma Recognition tags for tgase-mediated conjugation
EP2924044B1 (en) 2012-11-17 2018-10-31 Beijing Shuobai Pharmaceutical Co., LTD Platinum compound of malonic acid derivative having leaving group containing amino or alkylamino
US10611824B2 (en) 2013-03-15 2020-04-07 Innate Pharma Solid phase TGase-mediated conjugation of antibodies
WO2014202773A1 (en) 2013-06-20 2014-12-24 Innate Pharma Enzymatic conjugation of polypeptides
WO2014202775A1 (en) 2013-06-21 2014-12-24 Innate Pharma Enzymatic conjugation of polypeptides
WO2019092148A1 (en) 2017-11-10 2019-05-16 Innate Pharma Antibodies with functionalized glutamine residues

Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998008849A1 (en) * 1996-08-30 1998-03-05 Novartis Aktiengesellschaft Method for producing epothilones, and intermediate products obtained during the production process
WO1998025929A1 (en) * 1996-12-13 1998-06-18 Novartis Ag Epothilone analogs

Patent Citations (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998008849A1 (en) * 1996-08-30 1998-03-05 Novartis Aktiengesellschaft Method for producing epothilones, and intermediate products obtained during the production process
WO1998025929A1 (en) * 1996-12-13 1998-06-18 Novartis Ag Epothilone analogs

Non-Patent Citations (2)

* Cited by examiner, † Cited by third party
Title
NICOLAOU K C ET AL.: "Chemical Biology of Epothilones", ANGEWANDTE CHEMIE INTERNATIONAL EDITION., vol. 37, no. 15, August 1998 (1998-08-01), WEINHEIM DE, pages 2014 - 2045, XP002131418 *
NICOLAOU K C ET AL: "Total Synthesis of 26-Hydroxy-Epothilone B and Related Analogs via a Macrolactonization Based Strategy", TETRAHEDRON,NL,ELSEVIER SCIENCE PUBLISHERS, AMSTERDAM, vol. 54, no. 25, 18 June 1998 (1998-06-18), pages 7127 - 7166, XP004128313, ISSN: 0040-4020 *

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
WO1999067253A2 (en) 1999-12-29
AU4775299A (en) 2000-01-10

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