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1. WO2005121149 - FURANOPYRIMIDINE COMPOUNDS EFFECTIVE AS POTASSIUM CHANNEL INHIBITORS

Publication Number WO/2005/121149
Publication Date 22.12.2005
International Application No. PCT/GB2005/002318
International Filing Date 10.06.2005
IPC
C07D 491/04 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/-C07D459/290
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
A61K 31/44 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non-condensed pyridines; Hydrogenated derivatives thereof
A61P 9/04 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
CPC
A61K 31/44
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
435having six-membered rings with one nitrogen as the only ring hetero atom
44Non condensed pyridines; Hydrogenated derivatives thereof
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
A61P 9/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
04Inotropic agents, i.e. stimulants of cardiac contraction; Drugs for heart failure
A61P 9/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
06Antiarrhythmics
C07D 491/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
491Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • XENTION DISCOVERY LIMITED [GB]/[GB] (AllExceptUS)
  • FORD, John [GB]/[GB] (UsOnly)
  • PALMER, Nicholas, John [GB]/[GB] (UsOnly)
  • ATHERALL, John, Frederick [GB]/[GB] (UsOnly)
  • MADGE, David, John [GB]/[GB] (UsOnly)
Inventors
  • FORD, John
  • PALMER, Nicholas, John
  • ATHERALL, John, Frederick
  • MADGE, David, John
Agents
  • CHAPMAN, Paul, William
Priority Data
0412986.210.06.2004GB
60/578,35010.06.2004US
Publication Language English (en)
Filing Language English (EN)
Designated States
Title
(EN) FURANOPYRIMIDINE COMPOUNDS EFFECTIVE AS POTASSIUM CHANNEL INHIBITORS
(FR) COMPOSES DE FURANOPYRIMIDINE EFFICACES COMME INHIBITEURS DES CANAUX POTASSIQUES
Abstract
(EN) A compound of formula (I) wherein R1 is aryl, heteroaryl, cycloalkyl or alkyl; R2 is H, alkyl, nitro, -CO2R7, CONR4R5 or halo; R3 is H, NR4R5, NC(O)R8, halo, trifluoromethyl, alkyl, nitrile or alkoxy; R4 and R5 may be the same or different, and may be H, alkyl, aryl, heteroaryl or cycloalkyl; or R4 and R5 may together form a saturated, unsaturated or partially saturated 4 to 7 member ring, wherein said ring may optionally comprise one or more further heteroatoms selected from N, O or S; X is O, S or NR6; R6 is H or alkyl; R7 is hydrogen, methyl or ethyl; R8 is methyl or ethyl; Ll is (CH2)n, where n is 1,2 or 3; and Y is aryl, a heterocyclic group, alkyl, alkenyl or cycloalkyl; together with pharmaceutically acceptable salts thereof. The use of these compounds as potassium channel inhibitors is also described.
(FR) Cette invention concerne un composé représenté par la formule (I), dans laquelle R1 représente aryle, hétéroaryle, cycloalkyle ou alkyle ; R2 représente H, alkyle, nitro, -CO2R7, CONR4R5 ou halo ; R3 représente H, NR4R5, NC(O)R8, halo, trifluorométhyle, alkyle, nitrile ou alcoxy ; R4 et R5, qui peuvent être identiques ou différents, peuvent représenter H, alkyle, aryle, hétéroaryle ou cycloalkyle ; ou R4 et R5 peuvent former ensemble un cycle de 4 à 7 éléments saturé, insaturé ou partiellement saturé et pouvant éventuellement contenir un ou plusieurs autres hétéroatomes choisis parmi N, O ou S ; X représente O, S ou NR6 ; R6 représente H ou alkyle ; R7 représente hydrogène, méthyle ou éthyle ; R8 représente méthyle ou éthyle ; L représente (CH2)n, où n est égal à 1,2 ou 3 ; et Y représente aryle, un groupe hétérocyclique, alkyle, alcényle ou cycloalkyle ; ainsi que des sels de ces composés acceptables sur le plan pharmaceutique. L'utilisation de ces composés comme inhibiteurs des canaux potassiques est également décrite.
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