FI91763B - Förfarande för framställning av en terapeutiskt användbar 2',3'-dideoxi-3'-fluorpyrimidin- eller -purinnukleosid - Google Patents

Förfarande för framställning av en terapeutiskt användbar 2',3'-dideoxi-3'-fluorpyrimidin- eller -purinnukleosid Download PDF

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Publication number
FI91763B
FI91763B FI885094A FI885094A FI91763B FI 91763 B FI91763 B FI 91763B FI 885094 A FI885094 A FI 885094A FI 885094 A FI885094 A FI 885094A FI 91763 B FI91763 B FI 91763B
Authority
FI
Finland
Prior art keywords
formula
group
dideoxy
purine
active ingredient
Prior art date
Application number
FI885094A
Other languages
English (en)
Finnish (fi)
Other versions
FI885094A (sv
FI885094A0 (sv
FI91763C (sv
Inventor
Thomas Anthony Krenitsky
George Walter Koszalka
Charlene Louise Burns
Susan Mary Daluge
Tuttle Joel Van
Original Assignee
Wellcome Found
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 Wellcome Found filed Critical Wellcome Found
Publication of FI885094A0 publication Critical patent/FI885094A0/sv
Publication of FI885094A publication Critical patent/FI885094A/sv
Publication of FI91763B publication Critical patent/FI91763B/sv
Application granted granted Critical
Publication of FI91763C publication Critical patent/FI91763C/sv

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    • 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
    • A61K31/706—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
    • A61K31/7068—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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid
    • A61K31/7072—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 having oxo groups directly attached to the pyrimidine ring, e.g. cytidine, cytidylic acid having two oxo groups directly attached to the pyrimidine ring, e.g. uridine, uridylic acid, thymidine, zidovudine
    • 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
    • A61K31/7076—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 containing purines, e.g. adenosine, adenylic acid
    • 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
    • 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
    • C07H19/16—Purine radicals

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

Claims (5)

1. Förfarande för framställning av en terapeutiskt användbar 2',3'-dideoxi-3'-fluorpyrimidin- eller -purin-5 nukleosid med formeln (I) lp
10 F i vilken B är en grupp med formeln hV JVy 15 j | (A) eller j ^ (B) r2 i vilka R1 är en klor- eller jodatom, R2 är en väteatom 2 0 eller en aminogrupp och R3 är en C^-cykloalkylamino, rak eller förgrenad C,.6-alkoxi, C3.7-cykloalkoxi eller en hete-rocyklisk ring med 5 eller 6 medlemmar som anslutits tili puringruppen via en kväveatom i ringen, k ä n n e -.. t e c k n a t därav, att 25 (A) en förening med formeln (II) .·: 30 F i vilken B anger samma som ovan och R, är en prekursor-grupp tili hydroxigruppen, bringas att reagera med ett sädant medel eller under sädana förhällanden att nämnda 35 prekursorgrupp överförs i motsvarande önskad grupp; eller li 91763 29 (B) en purin- eller pyrimidinbas med formeln B - H (III) 5. vilken B anger samma som ovan, eller en funktionell ekvivalent tili denna, bringas att reagera med en fö-rening, som binder den önskade ribofuranosylgruppen tili 9-positionen i purinbasen eller tili 1-positionen i pyri-midinbasen med formeln (III). 10 2. Förfarande enligt patentkrav 1, känne- t e c k n a t därav, att R3 är en cyklopropylamino-, me-toxi-, cyklopentoxi- eller piperidinylgrupp.
3. Förfarande enligt patentkrav 1, känne- t e c k n a t därav, att man framställer 5-klor-l-(2,3-15 dideoxi-3-fluor-B-D-erytropentofuranosyl)uracil.
4. Förfarande enligt patentkrav 1, känne- t e c k n a t därav, att man framställer 5-jod-l-( 2,3-dideoxi-3-fluor-B-D-erytropentofuranosyl)uracil.
5. Förfarande enligt nägot av de föregäende pa- 20 tentkraven, kännetecknat därav, att en bas med formeln (III) i förfarande (B) bringas att reagera med 2',3'-deoxi-3’-fluortymidin i närvaro av ett pentosyl överförande enzym.
FI885094A 1987-11-07 1988-11-04 Förfarande för framställning av en terapeutiskt användbar 2',3'-dideoxi-3'-fluorpyrimidin- eller -purinnukleosid FI91763C (sv)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB878726136A GB8726136D0 (en) 1987-11-07 1987-11-07 Therapeutic nucleosides
GB8726136 1987-11-07

Publications (4)

Publication Number Publication Date
FI885094A0 FI885094A0 (sv) 1988-11-04
FI885094A FI885094A (sv) 1989-05-08
FI91763B true FI91763B (sv) 1994-04-29
FI91763C FI91763C (sv) 1994-08-10

Family

ID=10626612

Family Applications (1)

Application Number Title Priority Date Filing Date
FI885094A FI91763C (sv) 1987-11-07 1988-11-04 Förfarande för framställning av en terapeutiskt användbar 2',3'-dideoxi-3'-fluorpyrimidin- eller -purinnukleosid

Country Status (17)

Country Link
US (1) US5574149A (sv)
EP (3) EP0317128B1 (sv)
JP (1) JP2731551B2 (sv)
KR (1) KR890008160A (sv)
AT (1) ATE131826T1 (sv)
AU (1) AU616914B2 (sv)
CA (1) CA1333391C (sv)
DE (1) DE3854811T2 (sv)
DK (1) DK615788A (sv)
ES (1) ES2081286T3 (sv)
FI (1) FI91763C (sv)
GB (1) GB8726136D0 (sv)
GR (1) GR3019379T3 (sv)
HU (2) HU200931B (sv)
MX (1) MX9203217A (sv)
PT (1) PT88948B (sv)
ZA (1) ZA888289B (sv)

Families Citing this family (13)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5506215A (en) * 1987-11-03 1996-04-09 Medivir Ab 1-(3'-fluoro-2',3'-dideoxy-β-D-ribofuranosyl)-5-substituted pyrimidine nucleosides
US5157114A (en) * 1988-08-19 1992-10-20 Burroughs Wellcome Co. 2',3'-dideoxy-3'-fluoro-5-ethyngluridine
WO1990003978A1 (en) * 1988-10-03 1990-04-19 Stichting Rega Vzw 5-halogeno-3'-fluoro-2',3'-dideoxyuridine compounds and their therapeutic application
CA2073063A1 (en) * 1989-11-06 1991-05-07 Jo Klaveness Nucleoside derivatives
FR2668153B1 (fr) * 1990-10-22 1995-03-31 Pasteur Merieux Serums Vacc Nouveaux composes ribonucleosides, leur procede de preparation et les medicaments les contenant.
GB9200150D0 (en) * 1992-01-06 1992-02-26 Wellcome Found Therapeutic nucleosides
DE69324244T2 (de) * 1992-01-06 1999-09-30 Wellcome Found Therapeutische nukleoside der 2',3'-dideoxy-3'-fluor -purin reihe
EP0701564A1 (en) * 1993-03-31 1996-03-20 Sanofi Bifunctional nucleosides, oligomers thereof, and methods of making and using the same
US5717086A (en) * 1993-05-12 1998-02-10 Rhone-Poulenc Chemicals Limited Preparation of fluoro-nucleosides and intermediates for use therein
DE59804785D1 (de) * 1997-11-22 2002-08-22 Roche Diagnostics Gmbh Verbessertes Verfahren zur Stabilisierung von Proteinen
US6156349A (en) * 1998-12-14 2000-12-05 Steinbach, Pylant And Herman, L.L.C. Method of treating HIV infection with suppository containing mammalian liver extract
US6514979B1 (en) 1999-03-03 2003-02-04 University Of Maryland Biotechnology Institute Synergistic combinations of guanosine analog reverse transcriptase inhibitors and inosine monophosphate dehydrogenese inhibitors and uses therefor
US6949522B2 (en) * 2001-06-22 2005-09-27 Pharmasset, Inc. β-2′- or 3′-halonucleosides

Family Cites Families (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US3328388A (en) * 1964-09-02 1967-06-27 Merck & Co Inc Arabinofuranosyl pyrimidines and methods of preparing same
US3775397A (en) * 1969-11-12 1973-11-27 Akad Wissenschaften Ddr Novel cytostatic 2',3'-dideoxy-3'-fluoropyrimidine-nucleosides
SE8602981D0 (sv) * 1986-07-04 1986-07-04 Astra Laekemedel Ab Novel medicinal use
US5153180A (en) * 1986-07-24 1992-10-06 Eckart Matthes Fluorinated nucleosides and process for treating retrovirus infections therewith
DD279407A1 (de) * 1986-07-24 1990-06-06 Akad Wissenschaften Ddr Verfahren zur herstellung eines mittels gegen aids
GB8719877D0 (en) * 1987-08-22 1987-09-30 Wellcome Found Antiviral compounds
SE8704298D0 (sv) * 1987-11-03 1987-11-03 Astra Ab Compounds for use in therapy

Also Published As

Publication number Publication date
HU200931B (en) 1990-09-28
KR890008160A (ko) 1989-07-10
GR3019379T3 (en) 1996-06-30
DK615788D0 (da) 1988-11-04
EP0317128A3 (en) 1991-10-02
DK615788A (da) 1989-05-08
CA1333391C (en) 1994-12-06
DE3854811D1 (de) 1996-02-01
AU616914B2 (en) 1991-11-14
US5574149A (en) 1996-11-12
HUT48466A (en) 1989-06-28
EP0669341A1 (en) 1995-08-30
DE3854811T2 (de) 1996-08-01
ATE131826T1 (de) 1996-01-15
ES2081286T3 (es) 1996-03-01
EP0317128B1 (en) 1995-12-20
PT88948B (pt) 1993-02-26
FI885094A (sv) 1989-05-08
MX9203217A (es) 1992-07-01
JPH01153697A (ja) 1989-06-15
JP2731551B2 (ja) 1998-03-25
HU902123D0 (en) 1990-07-28
GB8726136D0 (en) 1987-12-09
FI885094A0 (sv) 1988-11-04
PT88948A (pt) 1988-12-01
HU204839B (en) 1992-02-28
FI91763C (sv) 1994-08-10
ZA888289B (en) 1990-07-25
EP0317128A2 (en) 1989-05-24
AU2476388A (en) 1989-05-25
EP0670328A1 (en) 1995-09-06

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Owner name: THE WELLCOME FOUNDATION LIMITED