HUP0000721A2 - Gemcitabinszármazékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények - Google Patents

Gemcitabinszármazékok, eljárás előállításukra és ilyen vegyületeket tartalmazó gyógyászati készítmények

Info

Publication number
HUP0000721A2
HUP0000721A2 HU0000721A HUP0000721A HUP0000721A2 HU P0000721 A2 HUP0000721 A2 HU P0000721A2 HU 0000721 A HU0000721 A HU 0000721A HU P0000721 A HUP0000721 A HU P0000721A HU P0000721 A2 HUP0000721 A2 HU P0000721A2
Authority
HU
Hungary
Prior art keywords
derivatives
effect
gemcitabine
hydrogen atom
anticancer
Prior art date
Application number
HU0000721A
Other languages
English (en)
Inventor
Bernt Borretzen
Are Dalen
Finn Myhren
Marit Liland Sandvold
Original Assignee
Norsk Hydro Asa.
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
Priority claimed from GB9701427A external-priority patent/GB2321454A/en
Application filed by Norsk Hydro Asa. filed Critical Norsk Hydro Asa.
Publication of HUP0000721A2 publication Critical patent/HUP0000721A2/hu
Publication of HUP0000721A3 publication Critical patent/HUP0000721A3/hu
Publication of HU224918B1 publication Critical patent/HU224918B1/hu

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
    • 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
    • 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
    • A61P35/00—Antineoplastic agents
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07H—SUGARS; DERIVATIVES THEREOF; NUCLEOSIDES; NUCLEOTIDES; NUCLEIC ACIDS
    • C07H1/00—Processes for the preparation of sugar derivatives

Abstract

A találmány rák elleni hatású gemcitabin (I) általános képletűszármazékaira, ahol az (I) képletben R1, R2 és R3 jelentése egymástólfüggetlenül hidrogénatom, vagy 18 szénatomos és 20 szénatomostelített, vagy egyszeresen telítetlen acilcsoport, azzal amegkötéssel, hogy Rl, R2 és R3 egyszerre nem jelenthet hidrogénatomot;valamint ezek előállítására vonatkozik. A találmány szerintivegyületek közül előnyösek az elaidinsav, és az eikozénsavgemcitabinnal alkotott észterei és amidjai. Az új származékok a rákelleni hatáson kívül antivirális hatást is mutattak. A származékokkedvezőbb hatásának oka valószínűleg abban áll, hogy a származékoknincsenek kitéve a foszforilezés hatásának, továbbá a származékokcitosztatikus aktivitása a nukleozid-transzportot gátló anyagokjelenlétében is megmarad. A találmány tárgyát képezik tehát a fentivegyületeket tartalmazó gyógyszerkészítmények is. Ó
HU0000721A 1997-01-24 1998-01-23 Gemcitabine derivatives, process for their preparation and pharmaceutical compositions containing them HU224918B1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GB9701427A GB2321454A (en) 1997-01-24 1997-01-24 Gemcitabine esters and amides
PCT/NO1998/000020 WO1998032762A1 (en) 1997-01-24 1998-01-23 Gemcitabine derivatives

Publications (3)

Publication Number Publication Date
HUP0000721A2 true HUP0000721A2 (hu) 2001-05-28
HUP0000721A3 HUP0000721A3 (en) 2002-12-28
HU224918B1 HU224918B1 (en) 2006-04-28

Family

ID=26310850

Family Applications (1)

Application Number Title Priority Date Filing Date
HU0000721A HU224918B1 (en) 1997-01-24 1998-01-23 Gemcitabine derivatives, process for their preparation and pharmaceutical compositions containing them

Country Status (15)

Country Link
US (1) US6384019B1 (hu)
EP (1) EP0986570B9 (hu)
JP (1) JP4352115B2 (hu)
KR (1) KR100483256B1 (hu)
AT (1) ATE236188T1 (hu)
AU (1) AU720451B2 (hu)
CA (1) CA2278056C (hu)
DE (1) DE69812934T2 (hu)
DK (1) DK0986570T3 (hu)
HU (1) HU224918B1 (hu)
NZ (1) NZ336676A (hu)
PL (1) PL186888B1 (hu)
SK (1) SK283879B6 (hu)
UA (1) UA67736C2 (hu)
WO (1) WO1998032762A1 (hu)

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Also Published As

Publication number Publication date
ATE236188T1 (de) 2003-04-15
CA2278056A1 (en) 1998-07-30
US6384019B1 (en) 2002-05-07
KR20000070351A (ko) 2000-11-25
AU5782798A (en) 1998-08-18
US20020042391A1 (en) 2002-04-11
JP2001509160A (ja) 2001-07-10
SK283879B6 (sk) 2004-04-06
EP0986570B1 (en) 2003-04-02
WO1998032762A1 (en) 1998-07-30
KR100483256B1 (ko) 2005-04-15
JP4352115B2 (ja) 2009-10-28
HU224918B1 (en) 2006-04-28
PL186888B1 (pl) 2004-03-31
HUP0000721A3 (en) 2002-12-28
UA67736C2 (uk) 2004-07-15
AU720451B2 (en) 2000-06-01
CA2278056C (en) 2006-12-12
PL334856A1 (en) 2000-03-27
SK102999A3 (en) 2000-05-16
EP0986570B9 (en) 2004-01-02
DK0986570T3 (da) 2003-07-28
NZ336676A (en) 2000-01-28
DE69812934D1 (de) 2003-05-08
EP0986570A1 (en) 2000-03-22
DE69812934T2 (de) 2004-01-29

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