ES8604943A1 - Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticals - Google Patents

Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticals

Info

Publication number
ES8604943A1
ES8604943A1 ES524997A ES524997A ES8604943A1 ES 8604943 A1 ES8604943 A1 ES 8604943A1 ES 524997 A ES524997 A ES 524997A ES 524997 A ES524997 A ES 524997A ES 8604943 A1 ES8604943 A1 ES 8604943A1
Authority
ES
Spain
Prior art keywords
acid addition
beta
desoxy
dione
imino
Prior art date
Legal status (The legal status 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 status listed.)
Expired
Application number
ES524997A
Other languages
Spanish (es)
Other versions
ES524997A0 (en
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Sandoz AG
Original Assignee
Sandoz 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
Application filed by Sandoz AG filed Critical Sandoz AG
Publication of ES8604943A1 publication Critical patent/ES8604943A1/en
Publication of ES524997A0 publication Critical patent/ES524997A0/en
Expired legal-status Critical Current

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
    • 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
    • A61P31/00—Antiinfectives, i.e. antibiotics, antiseptics, chemotherapeutics
    • A61P31/12—Antivirals
    • A61P31/20—Antivirals for DNA viruses
    • A61P31/22—Antivirals for DNA viruses for herpes viruses

Landscapes

  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Virology (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Communicable Diseases (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Molecular Biology (AREA)
  • Medicinal Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Biotechnology (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Oncology (AREA)
  • Engineering & Computer Science (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Biochemistry (AREA)
  • Genetics & Genomics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)

Abstract

1-(2-desoxy-D-erythropento or arabino-furanosyl and its 2-fluoro deriv.)-5-(R3-(CH2)n- CR1R2)-1H,3H-pyrimidin-2,4-dione and 2-one-4-imino derivs. of formula (I) and their acid addition salts are new (where R1, R2 independently are H or lower alkyl R3 is halo, difluoro-methyl or trifluoro-methyl R4 is H, hydroxy or fluoro X is O or -NH- and n is O or 1. The glucidic gp. may have alpha or beta configuration). - Antivirals effect against Herpes viruses, such as Herpes simplex I. They may be administered in daily doses of 200-1200 mg, as 2-4 unit doses of 50-600 mg. - 1-(2-desoxy-beta-D -erythro-pentofuranosyl) -5-(2-chloroethyl)-(1H,3H) pyrimidine-2,4-dione and its acid addition salts. (0/0) GBAB- GB2125401 B Compounds of formula (I) wherein R1 and R2 represent independently hydrogen or lower alkyl, R3 represents halogen, CHF2 or CF3, R4 represents hydrogen, hydroxy or fluorine, X represents oxygen or imino, and n is 0 or 1, whereby the sugar radical is alpha or beta-glycosically bound to the pyrimidine ring in free form or acid addition salt form.
ES524997A 1982-08-17 1983-08-17 Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticals Expired ES8604943A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH492282 1982-08-17

Publications (2)

Publication Number Publication Date
ES8604943A1 true ES8604943A1 (en) 1986-02-16
ES524997A0 ES524997A0 (en) 1986-02-16

Family

ID=4284858

Family Applications (1)

Application Number Title Priority Date Filing Date
ES524997A Expired ES8604943A1 (en) 1982-08-17 1983-08-17 Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticals

Country Status (16)

Country Link
JP (1) JPS5953499A (en)
AU (1) AU1800483A (en)
BE (1) BE897516A (en)
DE (1) DE3390162T1 (en)
DK (1) DK372283A (en)
ES (1) ES8604943A1 (en)
FI (1) FI832884A (en)
FR (1) FR2531962B1 (en)
GB (1) GB2125401B (en)
IL (1) IL69497A0 (en)
IT (1) IT1169765B (en)
NL (1) NL8302859A (en)
PT (1) PT77209B (en)
SE (1) SE8304408L (en)
WO (1) WO1984000759A1 (en)
ZA (1) ZA836072B (en)

Families Citing this family (16)

* 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
CA1295998C (en) * 1985-07-29 1992-02-18 Sai P. Sunkara Nucleosides and their use as antineoplastic agents
US5215971A (en) * 1986-12-19 1993-06-01 Medivir Ab Antiviral pharmaceutical composition comprising 5-substituted pyrimidine nucleosides
SE8605503D0 (en) * 1986-12-19 1986-12-19 Astra Laekemedel Ab NOVEL MEDICINAL USE
US5215970A (en) * 1987-04-16 1993-06-01 Medivir Ab Nucleosides and nucleotide analogues, pharmaceutical composition and processes for the preparation of the compounds
US4863927A (en) * 1987-05-11 1989-09-05 Merck & Co., Inc. 1-(2-hydroxymethyl)cycloalkylmethyl)-5-substituted uracils
US5606048A (en) * 1992-06-22 1997-02-25 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2', 2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5426183A (en) * 1992-06-22 1995-06-20 Eli Lilly And Company Catalytic stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5594124A (en) * 1992-06-22 1997-01-14 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-Deoxy-2',2'-difluoropyrimidine nucleosides and 2'-deoxy-2'-fluoropyrimidine nucleosides and intermediates thereof
US5371210A (en) * 1992-06-22 1994-12-06 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
US5821357A (en) * 1992-06-22 1998-10-13 Eli Lilly And Company Stereoselective glycosylation process for preparing 2'-deoxy-2',2'-difluoropurine and triazole nucleosides
US5401838A (en) * 1992-06-22 1995-03-28 Eli Lilly And Company Stereoselective fusion glycosylation process for preparing 2'-deoxy-2',2'-difluoronucleosides and 2'-deoxy-2'-fluoronucleosides
BR9302431A (en) * 1992-06-22 1994-01-11 Lilly Co Eli GLYCOSILATION PROCESS OF STEREOSELECTIVE ANION
US5424416A (en) * 1993-08-25 1995-06-13 Eli Lilly And Company Process for preparation of 2-deoxy-2,2-difluoro-D-ribofuranosyl-3,5-hydroxy protected-1-alkyl and aryl sulfonates and their use in preparation of 2',2'-difluoro-2'-deoxy nucleosides
SE9701219D0 (en) * 1997-04-04 1997-04-04 Astra Pharma Prod New compounds
AU2002326736B2 (en) * 2001-08-24 2007-08-02 Koronis Pharmaceuticals, Inc. Mutagenic nucleoside analogs for the treatment of viral disease

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3709874A (en) * 1970-03-19 1973-01-09 Syntex Corp 1-beta-d-arabinofuranosyl cytosine derivatives and methods of preparing
GB1601020A (en) * 1978-04-24 1981-10-21 Stichting Grega Vzw 2'-deoxy-5 (2-halogenovinyl)-uridines
GB2060604B (en) * 1979-10-03 1983-11-23 Univ Birmingham And Stichting E15-(2-halogenovinyl)-2'-deoxycytidines
DE3002197A1 (en) * 1980-01-22 1981-07-23 Robugen Gmbh Pharmazeutische Fabrik Esslingen A.N., 7300 Esslingen 5-Alkyl- and 5-alkenyl-uracil and -cytidine nucleoside derivs. - prepd. e.g. by reaction of 5'-chloro-5'-deoxy cpds. with ammonia
DE3010399A1 (en) * 1980-03-18 1981-09-24 Kailash Kumar Dr. 2359 Lentföhrden Gauri Cytostatic and antiviral pyrimidine nucleoside derivs. - which are 5-haloalkyl-pyrimidine nucleoside 5'-ester derivs.
HU183567B (en) * 1981-09-07 1984-05-28 Mta Koezponti Kemiai Kutato In Process for preparing /e/-5-/2-bromo-vinyl/-uridine and derivatives thereof

Also Published As

Publication number Publication date
GB8321880D0 (en) 1983-09-14
IT8322565A0 (en) 1983-08-16
PT77209B (en) 1986-03-18
FI832884A0 (en) 1983-08-10
ZA836072B (en) 1985-03-27
GB2125401B (en) 1985-10-16
DE3390162T1 (en) 1985-02-21
DK372283A (en) 1984-02-18
NL8302859A (en) 1984-03-16
IL69497A0 (en) 1983-11-30
GB2125401A (en) 1984-03-07
FR2531962A1 (en) 1984-02-24
PT77209A (en) 1983-09-01
IT1169765B (en) 1987-06-03
SE8304408D0 (en) 1983-08-15
SE8304408L (en) 1984-02-18
WO1984000759A1 (en) 1984-03-01
AU1800483A (en) 1984-02-23
DK372283D0 (en) 1983-08-15
JPS5953499A (en) 1984-03-28
ES524997A0 (en) 1986-02-16
FR2531962B1 (en) 1986-11-14
FI832884A (en) 1984-02-18
BE897516A (en) 1984-02-13

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