CN100522968C - 制备埃坡霉素衍生物的方法、埃坡霉素衍生物以及用于该方法的中间体及其制备方法 - Google Patents

制备埃坡霉素衍生物的方法、埃坡霉素衍生物以及用于该方法的中间体及其制备方法 Download PDF

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Publication number
CN100522968C
CN100522968C CNB038215837A CN03821583A CN100522968C CN 100522968 C CN100522968 C CN 100522968C CN B038215837 A CNB038215837 A CN B038215837A CN 03821583 A CN03821583 A CN 03821583A CN 100522968 C CN100522968 C CN 100522968C
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China
Prior art keywords
formula
compound
methyl
acid
reaction
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Expired - Fee Related
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CNB038215837A
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English (en)
Chinese (zh)
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CN1681824A (zh
Inventor
G·科克
O·卢瓦瑟勒尔
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Novartis AG
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Novartis AG
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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D275/00—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings
    • C07D275/04—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems
    • C07D275/06—Heterocyclic compounds containing 1,2-thiazole or hydrogenated 1,2-thiazole rings condensed with carbocyclic rings or ring systems with hetero atoms directly attached to the ring sulfur atom
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P17/00—Drugs for dermatological disorders
    • A61P17/06—Antipsoriatics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/04—Antibacterial agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P33/00—Antiparasitic agents
    • A61P33/02—Antiprotozoals, e.g. for leishmaniasis, trichomoniasis, toxoplasmosis
    • A61P33/06—Antimalarials
    • 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
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/16—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by esterified hydroxyl radicals
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D303/00—Compounds containing three-membered rings having one oxygen atom as the only ring hetero atom
    • C07D303/02—Compounds containing oxirane rings
    • C07D303/12—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms
    • C07D303/18—Compounds containing oxirane rings with hydrocarbon radicals, substituted by singly or doubly bound oxygen atoms by etherified hydroxyl radicals
    • 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
    • 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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  • Organic Chemistry (AREA)
  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Oncology (AREA)
  • Tropical Medicine & Parasitology (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Hematology (AREA)
  • Communicable Diseases (AREA)
  • Hospice & Palliative Care (AREA)
  • Psychiatry (AREA)
  • Dermatology (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)
CNB038215837A 2002-09-13 2003-09-12 制备埃坡霉素衍生物的方法、埃坡霉素衍生物以及用于该方法的中间体及其制备方法 Expired - Fee Related CN100522968C (zh)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB0221312.2A GB0221312D0 (en) 2002-09-13 2002-09-13 Organic compounds
GB0221312.2 2002-09-13

Publications (2)

Publication Number Publication Date
CN1681824A CN1681824A (zh) 2005-10-12
CN100522968C true CN100522968C (zh) 2009-08-05

Family

ID=9944042

Family Applications (1)

Application Number Title Priority Date Filing Date
CNB038215837A Expired - Fee Related CN100522968C (zh) 2002-09-13 2003-09-12 制备埃坡霉素衍生物的方法、埃坡霉素衍生物以及用于该方法的中间体及其制备方法

Country Status (29)

Country Link
US (1) US7470792B2 (enExample)
EP (1) EP1539768B1 (enExample)
JP (1) JP4628102B2 (enExample)
KR (1) KR20050042500A (enExample)
CN (1) CN100522968C (enExample)
AR (1) AR041231A1 (enExample)
AT (1) ATE373663T1 (enExample)
AU (2) AU2003267349B2 (enExample)
BR (1) BR0314263A (enExample)
CA (1) CA2497119C (enExample)
CY (1) CY1107794T1 (enExample)
DE (1) DE60316456T2 (enExample)
DK (1) DK1539768T3 (enExample)
EC (1) ECSP055652A (enExample)
ES (1) ES2290489T3 (enExample)
GB (1) GB0221312D0 (enExample)
IL (1) IL166829A (enExample)
MX (1) MXPA05002785A (enExample)
MY (1) MY140442A (enExample)
NO (1) NO20051794L (enExample)
NZ (1) NZ538612A (enExample)
PE (1) PE20050052A1 (enExample)
PL (1) PL375039A1 (enExample)
PT (1) PT1539768E (enExample)
RU (2) RU2404985C2 (enExample)
SG (1) SG155770A1 (enExample)
TW (1) TWI289563B (enExample)
WO (1) WO2004024735A2 (enExample)
ZA (1) ZA200501008B (enExample)

Families Citing this family (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP0977563B1 (en) 1996-12-03 2005-10-12 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US7649006B2 (en) 2002-08-23 2010-01-19 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
WO2004018478A2 (en) 2002-08-23 2004-03-04 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6921769B2 (en) 2002-08-23 2005-07-26 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
CA2799202C (en) 2010-05-18 2016-07-05 Cerulean Pharma Inc. Compositions and methods for treatment of autoimmune and other diseases

Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001007439A2 (en) * 1999-07-22 2001-02-01 Schering Aktiengesellschaft Process for the production of epothiolone b and derivatives as well as intermediate products for this process

Family Cites Families (10)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1998008849A1 (de) * 1996-08-30 1998-03-05 Novartis Aktiengesellschaft Verfahren zur herstellung von epothilonen und zwischenprodukte innerhalb des verfahrens
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
WO1998038192A1 (de) * 1997-02-25 1998-09-03 GESELLSCHAFT FüR BIOTECHNOLOGISCHE FORSCHUNG MBH (GBF) Seitenkettenmodifizierte epothilone
US6498257B1 (en) * 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
GB9810659D0 (en) * 1998-05-18 1998-07-15 Ciba Geigy Ag Organic compounds
AU2795000A (en) * 1998-12-22 2000-07-12 Novartis Ag Epothilone derivatives and their use as antitumor agents
US6593115B2 (en) * 2000-03-24 2003-07-15 Bristol-Myers Squibb Co. Preparation of epothilone intermediates
JP2005500974A (ja) 2000-10-13 2005-01-13 ザ ユニバーシテイ オブ ミシシッピー エポシロン類及び関連類似体の合成
PL374528A1 (en) * 2002-07-31 2005-10-31 Schering Aktiengesellschaft New effector conjugates, process for their production and their pharmaceutical use

Patent Citations (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2001007439A2 (en) * 1999-07-22 2001-02-01 Schering Aktiengesellschaft Process for the production of epothiolone b and derivatives as well as intermediate products for this process

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
Title
EPOTHILONE A-D ANDTHEIRTHIAZOLE-MODIFIEDANALOGS AS NOVELANTICANCERAGENTS. HOEFLE G 等人.PURE & APPLIEDCHEMISTRY,Vol.71 No.11. 1999 *

Also Published As

Publication number Publication date
EP1539768A2 (en) 2005-06-15
MXPA05002785A (es) 2005-06-03
AU2008203451A1 (en) 2008-08-21
CY1107794T1 (el) 2013-06-19
EP1539768B1 (en) 2007-09-19
RU2404985C2 (ru) 2010-11-27
DE60316456T2 (de) 2008-06-19
JP4628102B2 (ja) 2011-02-09
AR041231A1 (es) 2005-05-11
ECSP055652A (es) 2005-05-30
ATE373663T1 (de) 2007-10-15
CN1681824A (zh) 2005-10-12
RU2008129613A (ru) 2010-01-27
WO2004024735A2 (en) 2004-03-25
BR0314263A (pt) 2005-07-05
TW200413388A (en) 2004-08-01
KR20050042500A (ko) 2005-05-09
US7470792B2 (en) 2008-12-30
WO2004024735A3 (en) 2004-07-22
ZA200501008B (en) 2006-12-27
NZ538612A (en) 2008-01-31
AU2003267349A1 (en) 2004-04-30
NO20051794D0 (no) 2005-04-12
MY140442A (en) 2009-12-31
NO20051794L (no) 2005-04-12
RU2343155C2 (ru) 2009-01-10
DE60316456D1 (de) 2007-10-31
GB0221312D0 (en) 2002-10-23
PL375039A1 (en) 2005-11-14
ES2290489T3 (es) 2008-02-16
JP2006511469A (ja) 2006-04-06
CA2497119C (en) 2011-08-02
RU2005110925A (ru) 2006-01-20
CA2497119A1 (en) 2004-03-25
AU2003267349B2 (en) 2008-05-01
US20060106073A1 (en) 2006-05-18
IL166829A (en) 2011-01-31
PE20050052A1 (es) 2005-03-28
SG155770A1 (en) 2009-10-29
DK1539768T3 (da) 2008-01-07
HK1078853A1 (en) 2006-03-24
PT1539768E (pt) 2007-12-17
TWI289563B (en) 2007-11-11

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CF01 Termination of patent right due to non-payment of annual fee

Granted publication date: 20090805

Termination date: 20130912