JP2005513167A - エポシロン誘導体と代謝拮抗剤からなる組合せ - Google Patents

エポシロン誘導体と代謝拮抗剤からなる組合せ Download PDF

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Publication number
JP2005513167A
JP2005513167A JP2003557575A JP2003557575A JP2005513167A JP 2005513167 A JP2005513167 A JP 2005513167A JP 2003557575 A JP2003557575 A JP 2003557575A JP 2003557575 A JP2003557575 A JP 2003557575A JP 2005513167 A JP2005513167 A JP 2005513167A
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formula
combination
hydrogen
lower alkyl
methyl
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Japanese (ja)
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JP2005513167A5 (enExample
Inventor
ジョン・アーサー・ホーネカー
ポール・エム・ジェイ・マクシーヒー
ジョン・デイビッド・ロサーメル
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ノバルティス アクチエンゲゼルシャフト
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    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/425—Thiazoles
    • A61K31/427—Thiazoles not condensed and containing further heterocyclic rings
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/33—Heterocyclic compounds
    • A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
    • A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
    • A61K31/513—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim having oxo groups directly attached to the heterocyclic ring, e.g. cytosine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00—Medicinal preparations containing organic active ingredients
    • A61K31/70—Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042—Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom
    • A61K31/7064—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines
    • A61K31/7068—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing six-membered rings with nitrogen as a ring hetero atom containing condensed or non-condensed pyrimidines having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
    • A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00

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  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Chemical & Material Sciences (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Molecular Biology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Organic Chemistry (AREA)
  • Hematology (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
JP2003557575A 2002-01-14 2003-01-13 エポシロン誘導体と代謝拮抗剤からなる組合せ Ceased JP2005513167A (ja)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
US34862202P 2002-01-14 2002-01-14
US41617302P 2002-10-04 2002-10-04
PCT/EP2003/000232 WO2003057217A1 (en) 2002-01-14 2003-01-13 Combinations comprising epothilones and anti-metabolites

Publications (2)

Publication Number Publication Date
JP2005513167A true JP2005513167A (ja) 2005-05-12
JP2005513167A5 JP2005513167A5 (enExample) 2006-03-02

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JP2003557575A Ceased JP2005513167A (ja) 2002-01-14 2003-01-13 エポシロン誘導体と代謝拮抗剤からなる組合せ

Country Status (16)

Country Link
US (3) US20060089327A1 (enExample)
EP (2) EP1469847A1 (enExample)
JP (1) JP2005513167A (enExample)
KR (1) KR20040078123A (enExample)
CN (1) CN1615136A (enExample)
AU (1) AU2003235761A1 (enExample)
BR (1) BR0306861A (enExample)
CA (1) CA2471509A1 (enExample)
IL (1) IL162595A0 (enExample)
MX (1) MXPA04006822A (enExample)
NO (1) NO20043279L (enExample)
NZ (1) NZ533940A (enExample)
PL (1) PL369670A1 (enExample)
RU (1) RU2346686C2 (enExample)
TW (1) TWI341728B (enExample)
WO (1) WO2003057217A1 (enExample)

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006504745A (ja) * 2002-10-09 2006-02-09 コーザン バイオサイエンシス インコーポレイテッド エポd及び5−fu/ゲムシタビン
JP2009532497A (ja) * 2006-04-05 2009-09-10 ノバルティス アクチエンゲゼルシャフト 癌を処置するための治療剤の組合せ

Families Citing this family (9)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EP1386922B1 (en) 1996-12-03 2012-04-11 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereof, analogues and uses thereof
US6204388B1 (en) 1996-12-03 2001-03-20 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
ATE554756T1 (de) 2001-03-14 2012-05-15 Bristol Myers Squibb Co Kombination aus epothilon-analog und chemotherapeutika zur behandlung von proliferativen erkrankungen
EP1372650B1 (en) * 2001-03-19 2008-11-19 Novartis AG Combinations comprising an antidiarrheal agent and an epothilone or an epothilone derivative
CN1870995A (zh) * 2003-09-02 2006-11-29 诺瓦提斯公司 使用埃坡霉素的癌症治疗
US20050171167A1 (en) 2003-11-04 2005-08-04 Haby Thomas A. Process and formulation containing epothilones and analogs thereof
US20060121511A1 (en) 2004-11-30 2006-06-08 Hyerim Lee Biomarkers and methods for determining sensitivity to microtubule-stabilizing agents
CA2645633A1 (en) * 2006-04-05 2007-11-01 Novartis Ag Combinations of therapeutic agents for treating cancer
CA2927832C (en) 2010-05-18 2021-03-23 Cerulean Pharma Inc. Cyclodextrin-containing polymer-therapeutic agent conjugates and their use

Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999043320A1 (en) * 1998-02-25 1999-09-02 Novartis Ag Use of epothilones for the treatment of cancer
WO2000050423A1 (en) * 1999-02-22 2000-08-31 Gesellschaft Fuer Biotechnologische Forschung Mbh (Gbf) C-21 modified epothilones
WO2000061142A1 (en) * 1999-04-14 2000-10-19 Dana-Farber Cancer Institute, Inc. Method and composition for the treatment of cancer
WO2001010412A1 (en) * 1999-08-04 2001-02-15 Novartis Ag Epothilone compositions
WO2001092255A2 (en) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same

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US2802005A (en) 1957-08-06 S-eluorourace
US2705727A (en) 1952-07-10 1955-04-05 Du Pont Synthesis of ureas
US2933498A (en) 1954-12-28 1960-04-19 Burroughs Wellcome Co 7-aminothiazolo-(5,4-d) pyrimidine
US3116282A (en) 1960-04-27 1963-12-31 Upjohn Co Pyrimidine nucleosides and process
US4393064A (en) 1976-03-05 1983-07-12 Sri International Process and composition for treatment of leukemia and process for preparing the same
US4357324A (en) 1981-02-24 1982-11-02 The United States Of America As Represented By The Department Of Health And Human Services Prodrug derivatives of 9β-D-arabinofuranosyl-2-fluoroadenine
US4760135A (en) 1984-09-06 1988-07-26 University Of Kentucky Research Foundation Phloretin and phlorizin derivative containing compounds
DE3587500T2 (de) * 1984-12-04 1993-12-16 Lilly Co Eli Tumorbehandlung bei Säugetieren.
DE3773716D1 (de) 1986-03-24 1991-11-21 Nippon Kayaku Kk Verfahren zur herstellung von monosodiumsalz und dessen monohydrat von 1-beta-d-arabinofuranosylcytosin-5'stearylphosphat und diese enthaltende pharmazeutische zusammensetzung.
DE69003670T2 (de) 1989-01-05 1994-01-27 Otsuka Pharma Co Ltd Nicht einspritzbares karzinostatisches mittel zur vorbeugung der entzündung durch 5-fluoruracil und verfahren zur behandlung von krebs.
CA2087540C (en) * 1991-05-27 1999-01-19 Taiho Pharmaceutical Co., Ltd. Composition, method and kit for potentiating antitumor activity and for curing tumor
DE4138042C2 (de) 1991-11-19 1993-10-14 Biotechnolog Forschung Gmbh Epothilone, deren Herstellungsverfahren sowie diese Verbindungen enthaltende Mittel
AU671491B2 (en) * 1992-12-18 1996-08-29 F. Hoffmann-La Roche Ag N-oxycarbonyl substituted 5'-deoxy-5-fluorcytidines
AU716610B2 (en) 1996-08-30 2000-03-02 Novartis Ag Method for producing epothilones, and intermediate products obtained during the production process
ATE267197T1 (de) 1996-11-18 2004-06-15 Biotechnolog Forschung Gmbh Epothilon d, dessen herstellung und dessen verwendung als cytostatisches mittel bzw. als pflanzenschutzmittel
US6380394B1 (en) * 1996-12-13 2002-04-30 The Scripps Research Institute Epothilone analogs
US6441186B1 (en) 1996-12-13 2002-08-27 The Scripps Research Institute Epothilone analogs
US6605599B1 (en) 1997-07-08 2003-08-12 Bristol-Myers Squibb Company Epothilone derivatives
KR20080016756A (ko) 1998-02-05 2008-02-21 노파르티스 아게 유기화합물 함유 조성물
US6194181B1 (en) 1998-02-19 2001-02-27 Novartis Ag Fermentative preparation process for and crystal forms of cytostatics
CA2322157C (en) 1998-02-25 2012-05-29 Sloan-Kettering Institute For Cancer Research Synthesis of epothilones, intermediates thereto and analogues thereof
US6302838B1 (en) * 1998-02-25 2001-10-16 Novartis Ag Cancer treatment with epothilones
CN100381566C (zh) 1998-11-20 2008-04-16 科森生物科学公司 产生环氧噻酮及其衍生物的重组方法和材料
BR9916833A (pt) * 1998-12-22 2001-09-25 Novartis Ag Derivados de epotilona e seu uso como agentes antitumor
ATE554756T1 (de) * 2001-03-14 2012-05-15 Bristol Myers Squibb Co Kombination aus epothilon-analog und chemotherapeutika zur behandlung von proliferativen erkrankungen
TWI287986B (en) * 2001-12-13 2007-10-11 Novartis Ag Use of Epothilones for the treatment of the carcinoid syndrome

Patent Citations (5)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO1999043320A1 (en) * 1998-02-25 1999-09-02 Novartis Ag Use of epothilones for the treatment of cancer
WO2000050423A1 (en) * 1999-02-22 2000-08-31 Gesellschaft Fuer Biotechnologische Forschung Mbh (Gbf) C-21 modified epothilones
WO2000061142A1 (en) * 1999-04-14 2000-10-19 Dana-Farber Cancer Institute, Inc. Method and composition for the treatment of cancer
WO2001010412A1 (en) * 1999-08-04 2001-02-15 Novartis Ag Epothilone compositions
WO2001092255A2 (en) * 2000-05-26 2001-12-06 Kosan Biosciences, Inc. Epothilone derivatives and methods for making and using the same

Cited By (2)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
JP2006504745A (ja) * 2002-10-09 2006-02-09 コーザン バイオサイエンシス インコーポレイテッド エポd及び5−fu/ゲムシタビン
JP2009532497A (ja) * 2006-04-05 2009-09-10 ノバルティス アクチエンゲゼルシャフト 癌を処置するための治療剤の組合せ

Also Published As

Publication number Publication date
IL162595A0 (en) 2005-11-20
MXPA04006822A (es) 2004-12-08
US20110082101A1 (en) 2011-04-07
RU2004124943A (ru) 2005-08-10
AU2003235761A1 (en) 2003-07-24
CA2471509A1 (en) 2003-07-17
NO20043279L (no) 2004-08-05
EP2030618A2 (en) 2009-03-04
EP2030618A3 (en) 2009-03-11
US20090298791A1 (en) 2009-12-03
TWI341728B (en) 2011-05-11
EP1469847A1 (en) 2004-10-27
CN1615136A (zh) 2005-05-11
PL369670A1 (en) 2005-05-02
RU2346686C2 (ru) 2009-02-20
KR20040078123A (ko) 2004-09-08
BR0306861A (pt) 2004-11-03
NZ533940A (en) 2007-06-29
TW200306185A (en) 2003-11-16
US20060089327A1 (en) 2006-04-27
WO2003057217A1 (en) 2003-07-17

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