ES8604943A1 - Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticals - Google Patents
Desoxyuridine derivatives, processes for their preparation and their use as pharmaceuticalsInfo
- 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
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.
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)
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)
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 |
-
1983
- 1983-08-10 FR FR8313242A patent/FR2531962B1/en not_active Expired
- 1983-08-10 FI FI832884A patent/FI832884A/en not_active Application Discontinuation
- 1983-08-11 BE BE0/108521A patent/BE897516A/en not_active IP Right Cessation
- 1983-08-12 DE DE19833390162 patent/DE3390162T1/en not_active Withdrawn
- 1983-08-12 WO PCT/EP1983/000219 patent/WO1984000759A1/en active Application Filing
- 1983-08-15 DK DK372283A patent/DK372283A/en not_active Application Discontinuation
- 1983-08-15 AU AU18004/83A patent/AU1800483A/en not_active Abandoned
- 1983-08-15 GB GB08321880A patent/GB2125401B/en not_active Expired
- 1983-08-15 NL NL8302859A patent/NL8302859A/en not_active Application Discontinuation
- 1983-08-15 SE SE8304408A patent/SE8304408L/en not_active Application Discontinuation
- 1983-08-15 IL IL69497A patent/IL69497A0/en unknown
- 1983-08-16 PT PT77209A patent/PT77209B/en unknown
- 1983-08-16 IT IT22565/83A patent/IT1169765B/en active
- 1983-08-16 JP JP58150111A patent/JPS5953499A/en active Pending
- 1983-08-17 ZA ZA836072A patent/ZA836072B/en unknown
- 1983-08-17 ES ES524997A patent/ES8604943A1/en not_active Expired
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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