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ZA200109859B - 6-Alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations. - Google Patents

6-Alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations.

Info

Publication number
ZA200109859B
ZA200109859B ZA200109859A ZA200109859A ZA200109859B ZA 200109859 B ZA200109859 B ZA 200109859B ZA 200109859 A ZA200109859 A ZA 200109859A ZA 200109859 A ZA200109859 A ZA 200109859A ZA 200109859 B ZA200109859 B ZA 200109859B
Authority
ZA
South Africa
Prior art keywords
alkinyl
alkenyl
epoxy
production
pharmaceutical preparations
Prior art date
Application number
ZA200109859A
Other languages
English (en)
Inventor
Ulrich Klar
Werner Skuballa
Jens Hoffmann
Wolfgang Schwede
Bernd Buchmann
Rosemarie Lichtner
Original Assignee
Schering Ag
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 DE19921086A external-priority patent/DE19921086A1/de
Priority claimed from DE19954228A external-priority patent/DE19954228A1/de
Priority claimed from DE10015836A external-priority patent/DE10015836A1/de
Application filed by Schering Ag filed Critical Schering Ag
Publication of ZA200109859B publication Critical patent/ZA200109859B/xx

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/06Heterocyclic 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • A61P35/02Antineoplastic agents specific for leukemia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/02Heterocyclic 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
    • C07D405/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D405/00Heterocyclic 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
    • C07D405/14Heterocyclic 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 three or more hetero rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/04Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings directly linked by a ring-member-to-ring-member bond
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/06Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a carbon chain containing only aliphatic carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/14Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
    • 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
    • C07D417/04Heterocyclic 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 directly linked by a ring-member-to-ring-member bond
    • 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
    • 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
    • C07D417/14Heterocyclic 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 three or more hetero rings
    • 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)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • General Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Public Health (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pain & Pain Management (AREA)
  • Rheumatology (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)
  • Heterocyclic Compounds That Contain Two Or More Ring Oxygen Atoms (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
ZA200109859A 1999-04-30 2001-11-29 6-Alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations. ZA200109859B (en)

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
DE19921086A DE19921086A1 (de) 1999-04-30 1999-04-30 6-Alkenyl- und 6-Alkinyl-Epothilon Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten
DE19954228A DE19954228A1 (de) 1999-11-04 1999-11-04 6-Alkenyl-und 6-Alkinyl-Epothilon-Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten
DE10015836A DE10015836A1 (de) 2000-03-27 2000-03-27 6-Alkenyl- und 6-Alkinyl-Epothilon-Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten
PCT/IB2000/000657 WO2000066589A1 (en) 1999-04-30 2000-05-01 6-alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations

Publications (1)

Publication Number Publication Date
ZA200109859B true ZA200109859B (en) 2003-02-28

Family

ID=27213767

Family Applications (1)

Application Number Title Priority Date Filing Date
ZA200109859A ZA200109859B (en) 1999-04-30 2001-11-29 6-Alkenyl-, 6-alkinyl- and 6-epoxy-epothilone derivatives, process for their production, and their use in pharmaceutical preparations.

Country Status (33)

Country Link
EP (1) EP1173441B1 (et)
JP (2) JP4024003B2 (et)
KR (1) KR100721488B1 (et)
CN (1) CN100368415C (et)
AR (1) AR023792A1 (et)
AT (1) ATE440847T1 (et)
BG (1) BG65601B1 (et)
BR (1) BR0010190A (et)
CA (2) CA2371226C (et)
CY (1) CY1109768T1 (et)
CZ (1) CZ299653B6 (et)
DE (1) DE60042821D1 (et)
DK (1) DK1173441T3 (et)
EA (1) EA011502B1 (et)
EE (1) EE05292B1 (et)
ES (1) ES2331506T3 (et)
HK (1) HK1046681B (et)
HR (1) HRP20010892A2 (et)
HU (1) HUP0201010A3 (et)
IL (1) IL145938A0 (et)
ME (1) MEP13908A (et)
MX (1) MXPA01011039A (et)
NO (1) NO328149B1 (et)
NZ (1) NZ514989A (et)
PE (1) PE20010116A1 (et)
PL (1) PL210762B1 (et)
PT (1) PT1173441E (et)
RS (1) RS51023B (et)
SI (1) SI1173441T1 (et)
SK (1) SK286858B6 (et)
TW (2) TWI294292B (et)
WO (1) WO2000066589A1 (et)
ZA (1) ZA200109859B (et)

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US6288237B1 (en) 1995-11-17 2001-09-11 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epothilons C and D, preparation and compositions
CN1196698C (zh) 1996-11-18 2005-04-13 生物技术研究有限公司(Gbf) Epothilone D、E和F,其制备方法,以及作为细胞抑制剂和植物保护剂的应用
US6242469B1 (en) 1996-12-03 2001-06-05 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto, analogues and uses thereof
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
US6365749B1 (en) 1997-12-04 2002-04-02 Bristol-Myers Squibb Company Process for the preparation of ring-opened epothilone intermediates which are useful for the preparation of epothilone analogs
US6399638B1 (en) 1998-04-21 2002-06-04 Bristol-Myers Squibb Company 12,13-modified epothilone derivatives
US6498257B1 (en) 1998-04-21 2002-12-24 Bristol-Myers Squibb Company 2,3-olefinic epothilone derivatives
US6518421B1 (en) 2000-03-20 2003-02-11 Bristol-Myers Squibb Company Process for the preparation of epothilone analogs
US6593115B2 (en) 2000-03-24 2003-07-15 Bristol-Myers Squibb Co. Preparation of epothilone intermediates
DE10020899A1 (de) * 2000-04-20 2001-10-25 Schering Ag 9-Oxa-Epothilon-Derivate, Verfahren zu deren Herstellung sowie ihre Verwendung in pharmazeutischen Präparaten
UA75365C2 (en) 2000-08-16 2006-04-17 Bristol Myers Squibb Co Epothilone analog polymorph modifications, a method for obtaining thereof (variants), a pharmaceutical composition based thereon
SK288098B6 (sk) 2001-01-25 2013-07-02 Bristol-Myers Squibb Company Methods of administering epothilone analogs for the treatment of cancer
WO2002058699A1 (en) * 2001-01-25 2002-08-01 Bristol-Myers Squibb Company Pharmaceutical forms of epothilones for oral administration
CZ20032022A3 (cs) 2001-01-25 2004-04-14 Bristol-Myers Squibb Company Parenterální prostředek obsahující epothilonová analoga
IL157128A0 (en) 2001-02-20 2004-02-08 Bristol Myers Squibb Co Pharmaceutical compositions containing epothilone derivatives
PL363362A1 (en) 2001-02-20 2004-11-15 Bristol-Myers Squibb Company Treatment of refractory tumors using epothilone derivatives
CN1496256A (zh) 2001-03-14 2004-05-12 ����˹�ж�-����˹˹������˾ 用于治疗增生性疾病的埃博霉素(epo thilone)类似物和化疗剂的组合
JP2004532888A (ja) 2001-06-01 2004-10-28 ブリストル−マイヤーズ スクイブ カンパニー エポチロン誘導体
EP1340498A1 (en) * 2002-03-01 2003-09-03 Schering Aktiengesellschaft Use of epothilones in the treatment of brain diseases associated with proliferative processes
WO2003078411A1 (en) 2002-03-12 2003-09-25 Bristol-Myers Squibb Company C3-cyano epothilone derivatives
WO2003077903A1 (en) 2002-03-12 2003-09-25 Bristol-Myers Squibb Company C12-cyano epothilone derivatives
TW200403994A (en) 2002-04-04 2004-03-16 Bristol Myers Squibb Co Oral administration of EPOTHILONES
TW200400191A (en) 2002-05-15 2004-01-01 Bristol Myers Squibb Co Pharmaceutical compositions and methods of using C-21 modified epothilone derivatives
US7008936B2 (en) 2002-06-14 2006-03-07 Bristol-Myers Squibb Company Combination of epothilone analogs and chemotherapeutic agents for the treatment of proliferative diseases
KR20050053681A (ko) 2002-09-23 2005-06-08 브리스톨-마이어스 스큅 컴퍼니 에포틸론 b의 제조, 분리 및 정제 방법, 및 에포틸론 b의x-선 결정 구조
DE10361794B3 (de) * 2003-12-31 2005-10-06 Schering Ag Optisch aktive heteroaromatische ß-Hydroxy-Ester und Verfahren zu deren Herstellung sowie deren Verwendung als Zwischenprodukte bei der Epothilon-Totalsynthese
EP1559447A1 (en) 2004-01-30 2005-08-03 Institut National De La Sante Et De La Recherche Medicale (Inserm) Use of epothilones in the treatment of neuronal connectivity defects such as schizophrenia and autism
EP1640004A1 (en) * 2004-09-24 2006-03-29 Schering Aktiengesellschaft Use of epothilones in the treatment of bone metastases and bone tumors or cancers
US20060121511A1 (en) 2004-11-30 2006-06-08 Hyerim Lee Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents
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
CN100384419C (zh) * 2005-12-02 2008-04-30 菏泽睿鹰制药集团有限公司 一种埃坡霉素缓释植入组合物及应用
DE102007016046A1 (de) 2007-03-30 2008-10-23 Bayer Schering Pharma Aktiengesellschaft Verfahren zur Herstellung von Epothilonderivaten durch selektive katalytische Epoxidierung
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 (de) 2007-12-10 2009-06-18 Bayer Schering Pharma Aktiengesellschaft Funktionalisierte, feste Polymernanopartikel enthaltend Epothilone
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
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
US10036010B2 (en) 2012-11-09 2018-07-31 Innate Pharma Recognition tags for TGase-mediated conjugation
EP2968582B1 (en) 2013-03-15 2020-07-01 Innate Pharma Solid phase tgase-mediated conjugation of antibodies
US10071169B2 (en) 2013-06-20 2018-09-11 Innate Pharma Enzymatic conjugation of polypeptides
AU2014283185B2 (en) 2013-06-21 2019-05-02 Araris Biotech Ltd. Enzymatic conjugation of polypeptides
WO2019092148A1 (en) 2017-11-10 2019-05-16 Innate Pharma Antibodies with functionalized glutamine residues

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JPS54115320A (en) * 1978-02-28 1979-09-07 Soda Aromatic Novel unsaturated keto acid and its manufacture
JP2653663B2 (ja) * 1988-02-15 1997-09-17 財団法人微生物化学研究会 1.3―ジヒドロキシ―8―デセン―5―オンを含む免疫賦活剤及び制癌剤
EP0469480A3 (en) * 1990-08-01 1993-03-10 Hoechst Aktiengesellschaft Process for stereoselective preparation of 5-substituted delta-lactones and their use
CA2281105A1 (en) * 1997-02-25 1998-09-03 Gesellschaft Fur Biotechnologische Forschung Mbh (Gbf) Epothilones with a modified side chain
ATE368036T1 (de) * 1997-08-09 2007-08-15 Bayer Schering Pharma Ag Neue epothilon-derivate, verfahren zu deren herstellung und ihre pharmazeutische verwendung

Also Published As

Publication number Publication date
PL210762B1 (pl) 2012-02-29
KR20020005737A (ko) 2002-01-17
CN100368415C (zh) 2008-02-13
EP1173441B1 (en) 2009-08-26
CA2651653C (en) 2012-02-14
WO2000066589A1 (en) 2000-11-09
MEP13908A (en) 2010-06-10
HK1046681A1 (en) 2003-01-24
PE20010116A1 (es) 2001-02-15
HUP0201010A2 (en) 2002-08-28
ES2331506T3 (es) 2010-01-07
HRP20010892A2 (en) 2008-06-30
JP2002543203A (ja) 2002-12-17
EP1173441A1 (en) 2002-01-23
HUP0201010A3 (en) 2005-02-28
EA011502B1 (ru) 2009-04-28
JP4024003B2 (ja) 2007-12-19
TW200711679A (en) 2007-04-01
NZ514989A (en) 2004-02-27
DE60042821D1 (de) 2009-10-08
CA2371226C (en) 2011-11-29
EE05292B1 (et) 2010-04-15
IL145938A0 (en) 2002-07-25
RS51023B (sr) 2010-10-31
EE200100568A (et) 2003-02-17
KR100721488B1 (ko) 2007-05-23
DK1173441T3 (da) 2009-12-07
CZ299653B6 (cs) 2008-10-08
BG65601B1 (bg) 2009-02-27
TWI294292B (en) 2008-03-11
HK1046681B (zh) 2008-08-29
CY1109768T1 (el) 2014-09-10
CZ20013885A3 (cs) 2002-04-17
CA2371226A1 (en) 2000-11-09
JP4886578B2 (ja) 2012-02-29
SI1173441T1 (sl) 2010-01-29
PT1173441E (pt) 2009-11-06
EA200101025A1 (ru) 2002-06-27
AR023792A1 (es) 2002-09-04
BG106053A (en) 2002-05-31
NO20015278D0 (no) 2001-10-29
MXPA01011039A (es) 2003-06-30
JP2007224038A (ja) 2007-09-06
ATE440847T1 (de) 2009-09-15
SK286858B6 (sk) 2009-06-05
TWI280962B (en) 2007-05-11
YU77601A (sh) 2005-07-19
CN1349534A (zh) 2002-05-15
NO20015278L (no) 2001-12-21
SK15512001A3 (sk) 2002-05-09
CA2651653A1 (en) 2000-11-09
PL351491A1 (en) 2003-04-22
BR0010190A (pt) 2002-01-08
NO328149B1 (no) 2009-12-21

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