ATE137243T1 - 2'-deoxy-2',2'-difluor(4-substituierte pyrimidin)nukleoside mit antiviral und antikrebs- wirkung und zwischenverbindung - Google Patents

2'-deoxy-2',2'-difluor(4-substituierte pyrimidin)nukleoside mit antiviral und antikrebs- wirkung und zwischenverbindung

Info

Publication number
ATE137243T1
ATE137243T1 AT93304819T AT93304819T ATE137243T1 AT E137243 T1 ATE137243 T1 AT E137243T1 AT 93304819 T AT93304819 T AT 93304819T AT 93304819 T AT93304819 T AT 93304819T AT E137243 T1 ATE137243 T1 AT E137243T1
Authority
AT
Austria
Prior art keywords
deoxy
nucleosides
difluorine
antiviral
intermediate compound
Prior art date
Application number
AT93304819T
Other languages
English (en)
Inventor
Larry Wayne Hertel
Julian Stanley Kroin
Original Assignee
Lilly Co Eli
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 Lilly Co Eli filed Critical Lilly Co Eli
Application granted granted Critical
Publication of ATE137243T1 publication Critical patent/ATE137243T1/de

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06—Pyrimidine radicals
    • 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
    • A61K31/7056—Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides containing five-membered rings with nitrogen as a ring hetero atom
    • 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
    • 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
    • A61P31/12—Antivirals
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02—Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04—Heterocyclic radicals containing only nitrogen atoms as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Biotechnology (AREA)
  • Engineering & Computer Science (AREA)
  • Genetics & Genomics (AREA)
  • Biochemistry (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Animal Behavior & Ethology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Epidemiology (AREA)
  • Oncology (AREA)
  • Communicable Diseases (AREA)
  • Virology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
AT93304819T 1992-06-22 1993-06-21 2'-deoxy-2',2'-difluor(4-substituierte pyrimidin)nukleoside mit antiviral und antikrebs- wirkung und zwischenverbindung ATE137243T1 (de)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
US90231492A 1992-06-22 1992-06-22

Publications (1)

Publication Number Publication Date
ATE137243T1 true ATE137243T1 (de) 1996-05-15

Family

ID=25415673

Family Applications (1)

Application Number Title Priority Date Filing Date
AT93304819T ATE137243T1 (de) 1992-06-22 1993-06-21 2'-deoxy-2',2'-difluor(4-substituierte pyrimidin)nukleoside mit antiviral und antikrebs- wirkung und zwischenverbindung

Country Status (21)

Country Link
US (1) US5430026A (de)
EP (1) EP0576230B1 (de)
JP (1) JPH0656876A (de)
KR (1) KR940005657A (de)
CN (1) CN1084177A (de)
AT (1) ATE137243T1 (de)
AU (1) AU664096B2 (de)
BR (1) BR9302430A (de)
CA (1) CA2098875A1 (de)
CZ (1) CZ123193A3 (de)
DE (1) DE69302330T2 (de)
DK (1) DK0576230T3 (de)
ES (1) ES2087657T3 (de)
FI (1) FI932870A7 (de)
GR (1) GR3020064T3 (de)
HU (1) HUT64769A (de)
IL (1) IL106079A0 (de)
MX (1) MX9303711A (de)
NO (1) NO932289L (de)
PL (1) PL299414A1 (de)
YU (1) YU43193A (de)

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GB2321454A (en) * 1997-01-24 1998-07-29 Norsk Hydro As Gemcitabine esters and amides
GB9708611D0 (en) * 1997-04-28 1997-06-18 Univ Cardiff Chemical compounds
US6326507B1 (en) 1998-06-19 2001-12-04 Trustees Of Dartmouth College Therapeutic compounds and methods of use
JP4776843B2 (ja) 1999-10-01 2011-09-21 イムノゲン インコーポレーティッド 免疫複合体及び化学療法剤を用いる癌治療用組成物及び方法
GB0009486D0 (en) 2000-04-17 2000-06-07 Univ Cardiff Chemical compounds
US7435755B2 (en) 2000-11-28 2008-10-14 The Trustees Of Dartmouth College CDDO-compounds and combination therapies thereof
DK1465615T3 (da) 2002-01-15 2012-11-12 Dartmouth College Tricykliske bisenonderivater og fremgangsmåder til anvendelse heraf
EP1480982A4 (de) * 2002-02-14 2007-08-01 Pharmasset Inc Modifizierte fluorinierte nukleosidanaloga
WO2004041203A2 (en) 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
CA2508479A1 (en) * 2002-12-03 2004-06-17 Baylor University Compounds resistant to metabolic deactivation and methods of use
US7214791B2 (en) * 2004-07-01 2007-05-08 Shenzhen Hande Technology Co., Ltd. Method for preparation of 2′-deoxy-2′, 2′-difluoro-β-cytidine or pharmaceutically acceptable salts thereof by using 1,6-anhydro-β-d-glucose as raw material
ES2310860T3 (es) * 2004-12-17 2009-01-16 Eli Lilly And Company Profarmaco amida de gemcitabina, composiciones y uso del mismo.
DE602005019626D1 (de) * 2005-03-04 2010-04-08 Fresenius Kabi Oncology Ltd Zwischenprodukt und verfahren zur herstellung von an beta-anomeren angereicherten 2'-desoxy,2',2'-difluor-d-ribufuranosylnukleosiden
CN1693309A (zh) * 2005-04-18 2005-11-09 成都正开生物科技发展有限公司 N4－（取代的氧羰基）－2′，2′－二氟－2′－脱氧胞苷衍生物及其应用
AT502635A1 (de) * 2005-11-09 2007-05-15 Saischek Und Partner Meg Neue 1,3-dithioverbindungen, verfahren zu deren herstellung und ihre verwendung
GB0609178D0 (en) 2006-05-09 2006-06-21 Univ Cardiff Novel compounds
US8921340B2 (en) 2006-11-17 2014-12-30 Trustees Of Dartmouth College Methods for using synthetic triterpenoids in the treatment of bone or cartilage diseases or conditions
WO2008064132A2 (en) 2006-11-17 2008-05-29 Trustees Of Dartmouth College Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth
EP2094651A1 (de) 2006-11-17 2009-09-02 Trustees Of Dartmouth College Synthese und biologische wirkungen neuer tricyclischer bis-enone (tbes)
ME03529B (de) 2008-01-11 2020-04-20 Reata Pharmaceuticals Inc Synthetische triterpenoide und anwendungsverfahren bei der behandlung von erkrankungen
TW201006474A (en) 2008-04-18 2010-02-16 Reata Pharmaceuticals Inc Natural products including an anti-flammatory pharmacore and methods of use
RS58392B1 (sr) 2008-04-18 2019-04-30 Reata Pharmaceuticals Inc Antioksidantni modulatori inflamacije: derivati oleanoličke kiseline sa amino i drugim modifikacijama na c-17
HUE033288T2 (en) 2008-04-18 2017-11-28 Reata Pharmaceuticals Inc Antioxidant inflammation modulators: C-17 homologated oleic acid derivatives
EP2279197B1 (de) 2008-04-18 2014-11-05 Reata Pharmaceuticals, Inc. Antioxidationsmittel als entzündungsmodulierende substanz: im c-ring gesättigte oleanolsäurederivate
US8071632B2 (en) 2008-04-18 2011-12-06 Reata Pharmaceuticals, Inc. Antioxidant inflammation modulators: novel derivatives of oleanolic acid
DE102011077393A1 (de) 2011-06-10 2012-12-13 Johannes Reinmüller Antiinfektives Mittel
EP2833905B1 (de) 2012-04-04 2018-05-02 Halozyme, Inc. Kombinationbehnadlung von hyaluronidase und einem tumor-gerichteten taxane
US9809616B2 (en) 2012-10-29 2017-11-07 Emory University Pyrimidine nucleosides and their monophosphate prodrugs for the treatment of viral infections and cancer
US8921419B2 (en) 2012-05-08 2014-12-30 Trustees Of Dartmouth College Triterpenoids and compositions containing the same
WO2016078160A1 (zh) * 2014-11-17 2016-05-26 常州方圆制药有限公司 胞苷衍生物及其应用
WO2019222435A1 (en) 2018-05-16 2019-11-21 Halozyme, Inc. Methods of selecting subjects for combination cancer therapy with a polymer-conjugated soluble ph20
GR1009958B (el) * 2019-04-24 2021-03-18 ΕΝΟΡΑΣΙΣ ΑΝΩΝΥΜΗ ΕΜΠΟΡΙΚΗ ΕΤΑΙΡΕΙΑ ΦΑΡΜΑΚΕΥΤΙΚΩΝ ΚΑΙ ΙΑΤΡΙΚΩΝ ΥΛΙΚΩΝ ΚΑΙ ΜΗΧΑΝΗΜΑΤΩΝ με δ.τ. "ΕΝΟΡΑΣΙΣ Α.Ε." Παραγωγα γεμσιταβινης και μεθοδοι δημιουργιας παραγωγων γεμσιταβινης
CN116731097A (zh) * 2023-06-14 2023-09-12 河南省科学院高新技术研究中心 氨基酸甲酯取代的尿苷及其衍生物、其制备方法及应用

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* Cited by examiner, † Cited by third party
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US4526988A (en) * 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
DE3587500T2 (de) * 1984-12-04 1993-12-16 Lilly Co Eli Tumorbehandlung bei Säugetieren.
ZA859008B (en) * 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
CA1295998C (en) * 1985-07-29 1992-02-18 Sai P. Sunkara Nucleosides and their use as antineoplastic agents
US4965374A (en) * 1987-08-28 1990-10-23 Eli Lilly And Company Process for and intermediates of 2',2'-difluoronucleosides
DE3856158T2 (de) * 1987-08-28 1998-08-20 Lilly Co Eli Verfahren zur Herstellung von Zwischenverbindungen verwendbar in der Herstellung von 2',2'-Difluoronucleosiden
US4914028A (en) * 1988-02-10 1990-04-03 Eli Lilly And Company Method of preparing beta-2',2'-difluoronucleosides
CA1312599C (en) * 1988-02-16 1993-01-12 Larry Wayne Hertel 2',3'dideoxy-2',2'difluoronucleosides
EP0339161A1 (de) * 1988-04-01 1989-11-02 Merrell Dow Pharmaceuticals Inc. Derivate von Fluorphosphonat-Nukleotiden
JPH0232093A (ja) * 1988-06-08 1990-02-01 Merrell Dow Pharmaceut Inc 抗レトロウィルスジフルオロ化ヌクレオシド類
JPH05505815A (ja) * 1990-04-04 1993-08-26 ニユコメド・イメージング・アクシエセルカペト ヌクレオシド誘導体

Also Published As

Publication number Publication date
NO932289L (no) 1993-12-23
DE69302330D1 (de) 1996-05-30
AU4134893A (en) 1993-12-23
AU664096B2 (en) 1995-11-02
YU43193A (sh) 1997-01-08
EP0576230A1 (de) 1993-12-29
CZ123193A3 (en) 1994-04-13
GR3020064T3 (en) 1996-08-31
HU9301824D0 (en) 1993-09-28
EP0576230B1 (de) 1996-04-24
FI932870A0 (fi) 1993-06-21
ES2087657T3 (es) 1996-07-16
DK0576230T3 (da) 1996-05-20
IL106079A0 (en) 1993-10-20
FI932870L (fi) 1993-12-23
KR940005657A (ko) 1994-03-22
BR9302430A (pt) 1994-01-11
CN1084177A (zh) 1994-03-23
JPH0656876A (ja) 1994-03-01
PL299414A1 (en) 1993-12-27
US5430026A (en) 1995-07-04
FI932870A7 (fi) 1993-12-23
HUT64769A (en) 1994-02-28
NO932289D0 (no) 1993-06-21
CA2098875A1 (en) 1993-12-23
MX9303711A (es) 1994-05-31
DE69302330T2 (de) 1996-10-10

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Legal Events

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UEP Publication of translation of european patent specification
REN Ceased due to non-payment of the annual fee