BR0212107A - Análogos da ciclopropil e da ciclobutil epotilona - Google Patents

Análogos da ciclopropil e da ciclobutil epotilona

Info

Publication number
BR0212107A
BR0212107A BR0212107-7A BR0212107A BR0212107A BR 0212107 A BR0212107 A BR 0212107A BR 0212107 A BR0212107 A BR 0212107A BR 0212107 A BR0212107 A BR 0212107A
Authority
BR
Brazil
Prior art keywords
cyclopropyl
cyclobutyl
epothilone analogues
compounds
cyclobutyl epothilone
Prior art date
Application number
BR0212107-7A
Other languages
English (en)
Inventor
Kyriacos Costa Nicolaou
Kenji Namoto
Andreas Ritzen
Trond Ulven
Mutsuru Shoji
Karl-Heinz Altmann
Original Assignee
Novartis Ag
Scripps Research Inst
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 Novartis Ag, Scripps Research Inst filed Critical Novartis Ag
Publication of BR0212107A publication Critical patent/BR0212107A/pt

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D495/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms
    • C07D495/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having sulfur atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
    • C07D495/08—Bridged systems
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • A61P35/02—Antineoplastic agents specific for leukemia
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D313/00—Heterocyclic compounds containing rings of more than six members having one oxygen atom as the only ring hetero atom
    • 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
    • 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
    • C07D405/12—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 chain containing hetero atoms as chain links
    • 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
    • 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

Landscapes

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

Abstract

"ANáLOGOS DA CICLOPROPIL E DA CICLOBUTIL EPOTILONA". A presente invenção refere-se a cis- e trans-12,13-ciclopropil e 12,13-ciclobutil epotilonas da fórmula I até IV em que Ar é um radical representado pela estrutura a seguir: e os outros radicais e símbolos possuem os significados que são definidos aqui; à síntese química e à avaliação biológica dos mesmos; ao seu uso no tratamento de doenças neoplásticas e às preparações farmacêuticas contendo tais compostos. Os compostos descritos aqui são potentes promotores da polimerização da tubulina e agentes citotóxicos.
BR0212107-7A 2001-08-23 2002-08-22 Análogos da ciclopropil e da ciclobutil epotilona BR0212107A (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US31469801P 2001-08-23 2001-08-23
PCT/EP2002/009407 WO2003018002A2 (en) 2001-08-23 2002-08-22 Cyclopropyl and cyclobutyl epothilone analogs

Publications (1)

Publication Number Publication Date
BR0212107A true BR0212107A (pt) 2004-08-24

Family

ID=23221047

Family Applications (1)

Application Number Title Priority Date Filing Date
BR0212107-7A BR0212107A (pt) 2001-08-23 2002-08-22 Análogos da ciclopropil e da ciclobutil epotilona

Country Status (13)

Country Link
US (1) US7358266B2 (pt)
EP (2) EP1420780B1 (pt)
JP (2) JP4176015B2 (pt)
CN (1) CN100536841C (pt)
AT (1) ATE409473T1 (pt)
AU (1) AU2002331171A1 (pt)
BR (1) BR0212107A (pt)
CA (1) CA2456280A1 (pt)
DE (1) DE60229143D1 (pt)
ES (1) ES2315399T3 (pt)
HK (1) HK1066464A1 (pt)
PT (1) PT1420780E (pt)
WO (1) WO2003018002A2 (pt)

Families Citing this family (18)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999001124A1 (en) * 1996-12-03 1999-01-14 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6867305B2 (en) 1996-12-03 2005-03-15 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US20020058286A1 (en) * 1999-02-24 2002-05-16 Danishefsky Samuel J. Synthesis of epothilones, intermediates thereto and analogues thereof
ATE409473T1 (de) * 2001-08-23 2008-10-15 Novartis Pharma Gmbh Cyclopropyl und cyclobutyl epothilon analoge
AU2003266961A1 (en) * 2002-08-02 2004-02-25 Novartis Ag Epothilone derivatives
PT1767535E (pt) * 2002-08-23 2010-02-24 Sloan Kettering Inst Cancer Síntese de epotilonas, respectivos intermediários, análogos e suas utilizações
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US7384964B2 (en) * 2002-08-23 2008-06-10 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US20050171167A1 (en) 2003-11-04 2005-08-04 Haby Thomas A. Process and formulation containing epothilones and analogs thereof
GB0405898D0 (en) * 2004-03-16 2004-04-21 Novartis Ag Organic compounds
AU2006336468B2 (en) 2005-02-11 2012-04-12 University Of Southern California Method of expressing proteins with disulfide bridges
US8003801B2 (en) * 2005-11-22 2011-08-23 The Scripps Research Institute Chemical synthesis of a highly potent epothilone
US8008256B2 (en) * 2006-05-01 2011-08-30 University Of Southern California Combination therapy for treatment of cancer
JP5115729B2 (ja) * 2008-06-20 2013-01-09 信越化学工業株式会社 トリアルキルシリル基で保護されたアセト酢酸エステル基含有有機ケイ素化合物及びその製造方法
US8802394B2 (en) 2008-11-13 2014-08-12 Radu O. Minea Method of expressing proteins with disulfide bridges with enhanced yields and activity
CA2799202C (en) 2010-05-18 2016-07-05 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases
CN115850224A (zh) * 2022-07-22 2023-03-28 北京先通国际医药科技股份有限公司 一种修饰长链脂肪酸型pet试剂前体的合成方法及其用途
CN115141087B (zh) * 2022-09-06 2023-03-24 北京先通国际医药科技股份有限公司 Pet前体关键中间体的异构体的合成方法及其用途

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5969145A (en) * 1996-08-30 1999-10-19 Novartis Ag Process for the production of epothilones and intermediate products within the process
US6441186B1 (en) * 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US6380394B1 (en) * 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6399638B1 (en) * 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified epothilone derivatives
DE19848306A1 (de) * 1998-10-14 2000-04-20 Schering Ag Verfahren zur Herstellung von Epothilon B und Derivaten sowie Zwischenprodukte für dieses Verfahren
EA200100833A1 (ru) * 1999-02-11 2002-02-28 Шеринг Акциенгезельшафт Производные эпотилона, способ их получения и их применение в фармацевтике
ATE409473T1 (de) * 2001-08-23 2008-10-15 Novartis Pharma Gmbh Cyclopropyl und cyclobutyl epothilon analoge

Also Published As

Publication number Publication date
CA2456280A1 (en) 2003-03-06
DE60229143D1 (en) 2008-11-13
JP4176015B2 (ja) 2008-11-05
CN1545411A (zh) 2004-11-10
AU2002331171A1 (en) 2003-03-10
EP2070534A2 (en) 2009-06-17
EP2070534A3 (en) 2009-08-26
WO2003018002A2 (en) 2003-03-06
JP2009007367A (ja) 2009-01-15
EP1420780B1 (en) 2008-10-01
WO2003018002A3 (en) 2003-09-04
HK1066464A1 (en) 2005-03-24
JP2005501107A (ja) 2005-01-13
US20040039026A1 (en) 2004-02-26
PT1420780E (pt) 2008-12-29
ATE409473T1 (de) 2008-10-15
ES2315399T3 (es) 2009-04-01
EP1420780A2 (en) 2004-05-26
US7358266B2 (en) 2008-04-15
CN100536841C (zh) 2009-09-09

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Legal Events

Date Code Title Description
B06F Objections, documents and/or translations needed after an examination request according [chapter 6.6 patent gazette]
B08F Application dismissed because of non-payment of annual fees [chapter 8.6 patent gazette]

Free format text: REFERENTE A 8A E 9A A NUIDADES.

B08K Patent lapsed as no evidence of payment of the annual fee has been furnished to inpi [chapter 8.11 patent gazette]

Free format text: REFERENTE AO DESPACHO 8.6 PUBLICADO NA RPI 2108 DE 31/05/2011.