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)
  • Organic Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Genetics & Genomics (AREA)
  • Biotechnology (AREA)
  • Biochemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Public Health (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Families Citing this family (34)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5559222A (en) * 1995-02-03 1996-09-24 Eli Lilly And Company Preparation of 1-(2'-deoxy-2',2'-difluoro-D-ribo-pentofuranosyl)-cytosine from 2-deoxy-2,2-difluoro-β-D-ribo-pentopyranose
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
AU775373B2 (en) 1999-10-01 2004-07-29 Immunogen, Inc. Compositions and methods for treating cancer using immunoconjugates and chemotherapeutic agents
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
US7176237B2 (en) 2002-01-15 2007-02-13 The Trustees Of Dartmouth College Tricyclic-bis-enone derivatives and methods of use thereof
JP2005522443A (ja) * 2002-02-14 2005-07-28 フアーマセツト・リミテツド 改変フッ素化ヌクレオシド類似体
WO2004041203A2 (en) 2002-11-04 2004-05-21 Xenoport, Inc. Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
WO2004050678A2 (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
CA2589850C (en) * 2004-12-17 2012-05-01 Eli Lilly And Company Amide prodrug of gemcitabine, compositions and use thereof
KR20070112774A (ko) * 2005-03-04 2007-11-27 다브르 파마 리미티드 베타―아노머가 많은21데옥시,21,21-디플루오로-d-리보푸라노실뉴클레오시드의 제조를 위한 중간체 및 제조 방법
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
EP2094651A1 (de) 2006-11-17 2009-09-02 Trustees Of Dartmouth College Synthese und biologische wirkungen neuer tricyclischer bis-enone (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
US8299046B2 (en) 2006-11-17 2012-10-30 Trustees Of Dartmouth College Synthetic triterpenoids and tricyclic-bis-enones for use in stimulating bone and cartilage growth
BRPI0907423A2 (pt) 2008-01-11 2020-10-27 Reata Pharmaceuticals, Inc. composto triterpenoide sintético para uso em um método de melhoria da função renal em um indivíduo, e uso do referido composto
US8071632B2 (en) 2008-04-18 2011-12-06 Reata Pharmaceuticals, Inc. Antioxidant inflammation modulators: novel derivatives of oleanolic acid
JP5529851B2 (ja) 2008-04-18 2014-06-25 リアタ ファーマシューティカルズ インコーポレイテッド 抗酸化炎症モジュレーター:c−17においてアミノ改変およびその他の改変を加えたオレアノール酸誘導体
KR101713140B1 (ko) 2008-04-18 2017-03-08 리타 파마슈티컬스 잉크. C-환에서 포화된 산화방지성 염증 조절제 올레아놀산 유도체
WO2009146218A2 (en) 2008-04-18 2009-12-03 Reata Pharmaceuticals, Inc. Compounds including an anti-inflammatory pharmacore and methods of use
MX2010011439A (es) 2008-04-18 2011-01-25 Reata Pharmaceuticals Inc Moduladores de inflamacion antioxidantes: derivados del acido oleanolico homologacion c-17.
DE102011077393A1 (de) 2011-06-10 2012-12-13 Johannes Reinmüller Antiinfektives Mittel
CN108686203A (zh) 2012-04-04 2018-10-23 哈洛齐梅公司 使用抗透明质酸剂和肿瘤靶向紫杉烷的组合疗法
US8921419B2 (en) 2012-05-08 2014-12-30 Trustees Of Dartmouth College Triterpenoids and compositions containing the same
HK1214270A1 (zh) * 2012-10-29 2016-07-22 共晶制药股份有限公司 用於治療病毒感染和癌症的嘧啶核苷及其單磷酸酯前藥
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
US20190351031A1 (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

Family Cites Families (11)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
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
ES2157289T3 (es) * 1987-08-28 2001-08-16 Lilly Co Eli Procedimiento para la preparacion de 2'-desoxi-2',2'-difluoronucleosidos.
US4914028A (en) * 1988-02-10 1990-04-03 Eli Lilly And Company Method of preparing beta-2',2'-difluoronucleosides
EP0329348B1 (de) * 1988-02-16 1995-07-12 Eli Lilly And Company 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
WO1991015498A2 (en) * 1990-04-04 1991-10-17 Nycomed Imaging As Nucleoside derivatives

Also Published As

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

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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