HUP9901092A2 - Benzimidazolszármazékok és gyógyászati alkalmazásuk - Google Patents

Benzimidazolszármazékok és gyógyászati alkalmazásuk

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Publication number
HUP9901092A2
HUP9901092A2 HU9901092A HUP9901092A HUP9901092A2 HU P9901092 A2 HUP9901092 A2 HU P9901092A2 HU 9901092 A HU9901092 A HU 9901092A HU P9901092 A HUP9901092 A HU P9901092A HU P9901092 A2 HUP9901092 A2 HU P9901092A2
Authority
HU
Hungary
Prior art keywords
pyridine
benzyl
compounds
general formula
alkyl
Prior art date
Application number
HU9901092A
Other languages
English (en)
Inventor
Alan Hilary Calvert
Nicola Jane Curtin
Bernard Thomas Golding
Roger John Griffin
David Richard Newell
Original Assignee
Newcastle University Ventures Limited
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 GBGB9515843.2A external-priority patent/GB9515843D0/en
Priority claimed from GBGB9611245.3A external-priority patent/GB9611245D0/en
Application filed by Newcastle University Ventures Limited filed Critical Newcastle University Ventures Limited
Publication of HUP9901092A2 publication Critical patent/HUP9901092A2/hu
Publication of HUP9901092A3 publication Critical patent/HUP9901092A3/hu

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Classifications

    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/4151,2-Diazoles
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/41641,3-Diazoles
    • A61K31/41841,3-Diazoles condensed with carbocyclic rings, e.g. benzimidazoles
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/66Phosphorus compounds
    • A61K31/675Phosphorus compounds having nitrogen as a ring hetero atom, e.g. pyridoxal phosphate
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/08Radicals containing only hydrogen and carbon atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/10Radicals substituted by halogen atoms or nitro radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/12Radicals substituted by oxygen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/14Radicals substituted by nitrogen atoms
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/06Benzimidazoles; Hydrogenated benzimidazoles with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
    • C07D235/16Radicals substituted by carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D235/00Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
    • C07D235/02Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings condensed with carbocyclic rings or ring systems
    • C07D235/04Benzimidazoles; Hydrogenated benzimidazoles
    • C07D235/18Benzimidazoles; Hydrogenated benzimidazoles with aryl radicals directly attached in position 2

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  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Epidemiology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Saccharide Compounds (AREA)
  • Data Exchanges In Wide-Area Networks (AREA)

Abstract

A találmány tárgyát az (I) általánős képletű benzimidazől vegyületek,tővábbá ezek gyógyászatilag megfelelő sói és/vagy prő-gyógyszerszármazékai képezik, az (I) általánős képletben R jelentésehidrőgénatőm, alkil-, hidrőxi-alkil-csőpőrt, (mint CH2CH2OH),aceilcsőpőrt, (mint acetil- vagy benzőlilcsőpőrt), vagy adőtt esetbenszűbsztitűált arilcsőpőrt (mint fenilcsőpőrt), vagy aralkilcsőpőrt,mint benzil- vagy karbőxi-benzil-csőpőrt, és R' jelentésehidrőgénatőm, alkil-, hidrőxi-alkil-csőpőrt (mint CH2CH2OH),acilcsőpőrt (mint acetil- vagy benzilicsőpőrt), vagy adőtt esetbenszűbsztitűált arilcsőpőrt (mint fenilcsőpőrt) vagy aralkilcsőpőrt(mint benzil- vagy karbőxi-benzil-csőpőrt). E vegyületek hűmán- ésállatgyógyászati célra alkalmazhatók őlyan gyógyászati kezelés sőrán,ahől a pőli(ADP-ribóz) pőlimeráz vagy PARP enzim aktivitásánakinhibitálásra előnyös lehet, ezen kezelés daganatellenes gyógyászatikezelésénél alkalmazható. A találmány szerinti előnyös megőldásnál az(I) általánős képletű vegyületeket valamely DNS-t kárősító citőtőxikűsgyógyszerrel vagy sűgárterápiával együtt adják a daganatellenesgyógyászati kezelés sőrán. A találmány tárgyáhőz tartőzik az (I)általánős képletű vegyületek alkalmazása gyógyászati készítményekelőállítására, amelyek a fenti terápiás célra hasznősíthatók Atalálmány tárgyát képezik az (I) általánős képletű vegyületekettartalmazó gyógyászati készítmények is, amelyek az (I) általánősképletű hatóanyag mellett valamely gyógyászatilag megfelelő segéd- ésvivőanyagőt is tartalmaznak. A találmány tárgyát képezi az (I)általánős képletű vegyületek előállítására szőlgáló eljárás is,amelynek sőrán 2,3-diaminő-benzőesav-alkil-észtert egy arilsav-klőriddal reagáltatnak, majd a kapőtt vegyületet magasabbhőmérsékleten ecetsavval kezelik, majd a benzimidazől-gyűrűkialakűlása űtán a kapőtt vegyületet főlyékőny ammóniával reagáltatvaamidszármazékőt állítanak elő. ŕ
HU9901092A 1995-08-02 1996-07-30 Benzimidazole compounds and their pharmaceutical use HUP9901092A3 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
GBGB9515843.2A GB9515843D0 (en) 1995-08-02 1995-08-02 Benzimidazole compounds
GBGB9611245.3A GB9611245D0 (en) 1996-05-30 1996-05-30 Benzimidazole compounds

Publications (2)

Publication Number Publication Date
HUP9901092A2 true HUP9901092A2 (hu) 1999-07-28
HUP9901092A3 HUP9901092A3 (en) 2001-11-28

Family

ID=26307504

Family Applications (1)

Application Number Title Priority Date Filing Date
HU9901092A HUP9901092A3 (en) 1995-08-02 1996-07-30 Benzimidazole compounds and their pharmaceutical use

Country Status (26)

Country Link
US (2) US6100283A (hu)
EP (1) EP0841924B1 (hu)
JP (1) JPH11510154A (hu)
KR (1) KR100447539B1 (hu)
CN (1) CN1159007C (hu)
AP (1) AP866A (hu)
AT (1) ATE225173T1 (hu)
AU (1) AU714873B2 (hu)
BR (1) BR9610051A (hu)
CA (1) CA2225465A1 (hu)
CZ (1) CZ30398A3 (hu)
DE (1) DE69624115T2 (hu)
DK (1) DK0841924T3 (hu)
EA (1) EA000999B1 (hu)
ES (1) ES2183004T3 (hu)
HU (1) HUP9901092A3 (hu)
IL (1) IL123147A (hu)
MX (1) MX9800927A (hu)
NO (1) NO317033B1 (hu)
NZ (1) NZ313713A (hu)
OA (1) OA10661A (hu)
PL (1) PL324869A1 (hu)
PT (1) PT841924E (hu)
SK (1) SK13598A3 (hu)
TR (1) TR199800127T1 (hu)
WO (1) WO1997004771A1 (hu)

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