+

WO1999067253A3 - Desmethyl epothilones - Google Patents

Desmethyl epothilones Download PDF

Info

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 1998-06-22
US09/102,602 US6380394B1 (en) 1996-12-13 1998-06-22 Epothilone analogs
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
EP1847540A1 (en) 1997-08-09 2007-10-24 Bayer Schering Pharma Aktiengesellschaft Nouveaux dérivés d'épothilone, leur procédé de production et leur utilisation pharmaceutique
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
KR100851418B1 (en) 1998-11-20 2008-08-08 코산 바이오사이언시즈, 인코포레이티드 Recombinant methods and materials for producing epothilone and epothilone derivatives
US6410301B1 (en) 1998-11-20 2002-06-25 Kosan Biosciences, Inc. Myxococcus host cells for the production of epothilones
CZ20012886A3 (en) 1999-02-11 2001-11-14 Schering Aktiengesellschaft Epothilone derivatives, process of their preparation and pharmaceutical use thereof
US7125875B2 (en) 1999-04-15 2006-10-24 Bristol-Myers Squibb Company Cyclic protein tyrosine kinase inhibitors
CN101481359A (en) 1999-04-15 2009-07-15 布里斯托尔-迈尔斯斯奎布公司 Cyclic protein tyrosine kinase inhibitors
AU772750C (en) 1999-04-30 2005-02-24 Schering Aktiengesellschaft 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations
US20020045609A1 (en) * 2000-05-26 2002-04-18 Gary Ashley Epothilone derivatives and methods for making and using the same
AU2002213248A1 (en) 2000-10-13 2002-04-22 The University Of Mississipi Synthesis of epothilones and relates analogs
EP1340498A1 (en) * 2002-03-01 2003-09-03 Schering Aktiengesellschaft Use of epothilones in the treatment of brain diseases associated with proliferative processes
DK1483251T3 (en) 2002-03-12 2010-04-12 Bristol Myers Squibb Co C3-cyano-epothilone derivatives
US7405234B2 (en) 2002-05-17 2008-07-29 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
AU2003302084A1 (en) 2002-11-15 2004-06-15 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
US7625923B2 (en) 2004-03-04 2009-12-01 Bristol-Myers Squibb Company Bicyclic modulators of androgen receptor function
US7696241B2 (en) 2004-03-04 2010-04-13 Bristol-Myers Squibb Company Bicyclic compounds as modulators of androgen receptor function and method
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
WO2008070672A2 (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
EP2114429A4 (en) 2007-02-08 2010-05-19 Univ Illinois 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
EP2070521A1 (en) 2007-12-10 2009-06-17 Bayer Schering Pharma Aktiengesellschaft Surface-modified nanoparticles
DE102007059752A1 (en) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Functionalized solid polymer nanoparticles containing epothilones
EP2210584A1 (en) 2009-01-27 2010-07-28 Bayer Schering Pharma Aktiengesellschaft Stable polymeric composition comprising an epothilone and an amphiphilic block copolymer
CA2927832C (en) 2010-05-18 2021-03-23 Cerulean Pharma Inc. Cyclodextrin-containing polymer-therapeutic agent conjugates and their use
AU2012207142B2 (en) 2011-01-20 2017-04-27 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
CA2858806A1 (en) 2011-12-23 2013-06-27 Innate Pharma Enzymatic conjugation of polypeptides
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
EP2968582B1 (en) 2013-03-15 2020-07-01 Innate Pharma Solid phase tgase-mediated conjugation of antibodies
WO2014202773A1 (en) 2013-06-20 2014-12-24 Innate Pharma Enzymatic conjugation of polypeptides
CN105517577A (en) 2013-06-21 2016-04-20 先天制药公司 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
AU4775299A (en) 2000-01-10
WO1999067253A2 (en) 1999-12-29

Similar Documents

Publication Publication Date Title
WO1999067253A3 (en) Desmethyl epothilones
IL151757A0 (en) Glucopyranosyloxy benzylbenzene derivatives, medicinal compounds containing the same and intermediates for the preparation of the derivatives
WO2003006425A3 (en) Novel compounds as anti-inflammatory, immunomodulatory and anti-proliferatory agents
EP1019389A4 (en) Epothilone derivatives
WO2003040076A3 (en) Novel difunctional photoinitiators
MXPA03012013A (en) Substituted 1-oxa-2,8-diaza-spiro[4,5]dec-2-ene derivatives as medicaments for the treatment of pain.
HK1155146A1 (en) Indene derivatives as pharmaceutical agents
EP0798288A4 (en) Triciclic compounds
WO2006047288A3 (en) Asymmetric synthesis of dihydrobenzofuran derivatives
EP1125907A3 (en) Intermediates for the production of citalopram
GR3036070T3 (en) New process for the production of cephalosporines and novel intermediates in this process.
HU9904634D0 (en) New thiaazolidine-derivatives
AU2002218337A1 (en) Method for inducing cognition enhancement by use of trimethyl-bicyclo(2.2.1)heptane derivatives
NO20040911L (en) Protected 3,5-dihydroxy-2,2-dimethylvaleronitriles for the synthesis of epothilones and derivatives, and processes for their preparation and use.
WO2002096855A3 (en) Anticholinergic compounds and methods of use
IL134788A0 (en) A process for preparing 2-alkyl-3-aminothiophene derivatives
BG107048A (en) Method for the preparation of citalopram
GB0019124D0 (en) Novel process
AU2001212914A1 (en) Friedel-craft process for the preparation of thioxanthones
MXPA04005788A (en) Process for the preparation of `1,4,5!-oxadiazepine derivatives.
AU6594900A (en) Tricyclic dihydrobenzofuran derivatives, process for the preparation thereof andagents
EP1388539A3 (en) Process for the preparation of 3-hydroxytetrahydrofuran
PL343546A1 (en) Processes for preparing intermediates
WO2000064902A3 (en) Process for the preparation of calanolide precursors
IL156768A0 (en) Process for preparing (+/-) trans-4-p-fluorophenyl-3-hydroxymethyl-1-methylpiperidine

Legal Events

Date Code Title Description
AK Designated states

Kind code of ref document: A2

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A2

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

121 Ep: the epo has been informed by wipo that ep was designated in this application
DFPE Request for preliminary examination filed prior to expiration of 19th month from priority date (pct application filed before 20040101)
AK Designated states

Kind code of ref document: A3

Designated state(s): AE AL AM AT AU AZ BA BB BG BR BY CA CH CN CU CZ DE DK EE ES FI GB GD GE GH GM HR HU ID IL IN IS JP KE KG KP KR KZ LC LK LR LS LT LU LV MD MG MK MN MW MX NO NZ PL PT RO RU SD SE SG SI SK SL TJ TM TR TT UA UG US UZ VN YU ZA ZW

AL Designated countries for regional patents

Kind code of ref document: A3

Designated state(s): GH GM KE LS MW SD SL SZ UG ZW AM AZ BY KG KZ MD RU TJ TM AT BE CH CY DE DK ES FI FR GB GR IE IT LU MC NL PT SE BF BJ CF CG CI CM GA GN GW ML MR NE SN TD TG

REG Reference to national code

Ref country code: DE

Ref legal event code: 8642

122 Ep: pct application non-entry in european phase
NENP Non-entry into the national phase

Ref country code: CA

点击 这是indexloc提供的php浏览器服务,不要输入任何密码和下载