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

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom
    • C07H19/06Pyrimidine radicals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/7056Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/70Carbohydrates; Sugars; Derivatives thereof
    • A61K31/7042Compounds having saccharide radicals and heterocyclic rings
    • A61K31/7052Compounds having saccharide radicals and heterocyclic rings having nitrogen as a ring hetero atom, e.g. nucleosides, nucleotides
    • A61K31/706Compounds 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
    • A61K31/7064Compounds 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P31/00Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12Antivirals
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07HSUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H19/00Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof
    • C07H19/02Compounds containing a hetero ring sharing one ring hetero atom with a saccharide radical; Nucleosides; Mononucleotides; Anhydro-derivatives thereof sharing nitrogen
    • C07H19/04Heterocyclic radicals containing only nitrogen atoms as ring hetero atom

Landscapes

  • Chemical & Material Sciences (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Engineering & Computer Science (AREA)
  • Biochemistry (AREA)
  • Biotechnology (AREA)
  • Genetics & Genomics (AREA)
  • Medicinal Chemistry (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Epidemiology (AREA)
  • Virology (AREA)
  • Communicable Diseases (AREA)
  • Oncology (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
EP2266607A3 (de) 1999-10-01 2011-04-20 Immunogen, Inc. Immunokonjugate für Krebsbehandlung
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
CA2476279A1 (en) * 2002-02-14 2003-08-21 Pharmasset, Inc. Modified fluorinated nucleoside analogues
WO2004041203A2 (en) 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
JP2006510633A (ja) * 2002-12-03 2006-03-30 ベイラー ユニバーシティー 代謝不活性化に耐性の化合物および使用方法
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
KR100874052B1 (ko) * 2004-12-17 2008-12-12 일라이 릴리 앤드 캄파니 젬시타빈의 아미드 전구약, 그의 조성물 및 그의 용도
MX2007010316A (es) * 2005-03-04 2008-02-19 Dabur Pharma Ltd Intermediario de 21-desoxi, 21,21-difluoro-d-ribofuranosil nucleosidos enriquecidos en (-anomero y proceso para prepararlo.
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
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
US7714012B2 (en) 2006-11-17 2010-05-11 Trustees Of Dartmouth University Synthesis and biological activities of new tricyclic-bis-enones (TBEs)
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
KR101880692B1 (ko) 2008-01-11 2018-07-20 리타 파마슈티컬스 잉크. 합성 트리테르페노이드 및 질병 치료시의 사용 방법
MX2010011437A (es) 2008-04-18 2010-12-20 Reata Pharmaceuticals Inc Moduladores antioxidantes de inflamacion: derivados del acido oleanolico con saturacion en el anillo c.
ES2613964T3 (es) 2008-04-18 2017-05-29 Reata Pharmaceuticals, Inc. Moduladores de inflamación antioxidantes: Derivados de ácido oleanólico homologado C-17
PT2276493T (pt) 2008-04-18 2019-01-10 Reata Pharmaceuticals Inc Moduladores de inflamação anti-oxidantes: derivados de ácidos oleonucleicos com uma modificação no grupo aminno e outras modificações em c-17
TW201004627A (en) 2008-04-18 2010-02-01 Reata Pharmaceuticals Inc Antioxidant inflammation modulators: novel derivatives of oleanolic acid
WO2009146218A2 (en) 2008-04-18 2009-12-03 Reata Pharmaceuticals, Inc. Compounds including an anti-inflammatory pharmacore and methods of use
DE102011077393A1 (de) * 2011-06-10 2012-12-13 Johannes Reinmüller Antiinfektives Mittel
BR112014024848A2 (pt) 2012-04-04 2017-07-11 Halozyme Inc terapia de combinação com um agente antihialuronano e um taxano direcionamento ao tumor
US8921419B2 (en) 2012-05-08 2014-12-30 Trustees Of Dartmouth College Triterpenoids and compositions containing the same
MX2015005500A (es) 2012-10-29 2016-02-09 Cocrystal Pharma Inc Nucleotidos de pirimidina y sus profarmacos de monofosfato para el tratamiento de infecciones virales y cancer.
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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US4526988A (en) * 1983-03-10 1985-07-02 Eli Lilly And Company Difluoro antivirals and intermediate therefor
ZA859008B (en) * 1984-12-04 1987-07-29 Lilly Co Eli The treatment of tumors in mammals
EP0184365B1 (de) * 1984-12-04 1993-08-04 Eli Lilly And Company Tumorbehandlung bei Säugetieren
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
ATE179713T1 (de) * 1987-08-28 1999-05-15 Lilly Co Eli Verfahren zur selektiven isolierung von beta-2'- desoxy-2'2'-difluorocytidin oder seiner salze
US4914028A (en) * 1988-02-10 1990-04-03 Eli Lilly And Company Method of preparing beta-2',2'-difluoronucleosides
DE68923387T2 (de) * 1988-02-16 1996-01-25 Lilly Co Eli 2',3'-Dideoxy-2',2'-difluornucleoside.
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
EP0523110A1 (de) * 1990-04-04 1993-01-20 Nycomed Imaging As Nukleosidderivate

Also Published As

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

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Legal Events

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