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1. WO1990012790 - PYRIMIDINE DERIVATIVES

Publication Number WO/1990/012790
Publication Date 01.11.1990
International Application No. PCT/GB1990/000595
International Filing Date 19.04.1990
IPC
C07D 239/48 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
48Two nitrogen atoms
C07D 239/95 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
C07D 401/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
C07D 401/12 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
401Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
02containing two hetero rings
12linked by a chain containing hetero atoms as chain links
C07D 403/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
403Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/167
02containing two hetero rings
04directly linked by a ring-member-to-ring- member bond
CPC
A61P 9/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
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
A61P 9/08
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
08Vasodilators for multiple indications
A61P 9/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
9Drugs for disorders of the cardiovascular system
10for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
C07D 239/48
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
46Two or more oxygen, sulfur or nitrogen atoms
48Two nitrogen atoms
C07D 239/95
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
70condensed with carbocyclic rings or ring systems
72Quinazolines; Hydrogenated quinazolines
95with hetero atoms directly attached in positions 2 and 4
Applicants
  • IMPERIAL CHEMICAL INDUSTRIES PLC [GB]/[GB]
Inventors
  • HARGREAVES, Rodney, Brian
  • MARSHALL, Paul, William
  • MCLOUGHLIN, Bernard, Joseph
  • MILLS, Stuart, Dennett
Agents
  • SMITH, Stephen, Collyer
Priority Data
8909054.221.04.1989GB
8910548.008.05.1989GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) PYRIMIDINE DERIVATIVES
(FR) DERIVES PYRIMIDINES
Abstract
(EN)
This invention concerns novel aminopyrimidinium salts of the formula (I), in which R1 is alkyl, alkenyl, cycloalkyl, phenyl, phenylalkyl or cycloalkyl-alkyl; one of R2 and R6 is a basic group selected from amino, alkylamino, dialkylamino of up to eight carbon atoms, pyrrolidino, piperridino and morpholino; and the other of R2 and R6 is hydrogen, alkyl, alkenyl, alkoxyalkyl, phenyl, phenylalkyl, cycloalkyl or cycloalkyl-alkyl; or both of R2 and R6 are basic groups as mentioned above; and R5 is hydrogen, (1-4C)alkyl or (3-6C)alkyl; or R2 is a basic group as mentioned above, and R5 and R6 together form alkylene or, together with the appendant carbon atoms of the pyrimidine ring, complete a benzene ring; R4 is hydrogen, alkyl, cycloalkyl-alkyl, alkenyl, alkynyl or phenylalkyl; or R4 is an optionally substituted alkylene or alkenylene linked to the nitrogen atom of the groupe Q.A.N-, either of which linking groups may thereby complete a ring including two adjacent carbon atoms of Q, the carbon atoms of A and the adjacent nitrogen atom of the group -A.N-; A is a direct bond to the group -N(R4)- or is alkylene or oxyalkylene; Q is a pyridyl, furyl, thienyl or phenyl moiety; and Y is a physiologically acceptable anion; but excluding a number of compounds specified hereinafter. The invention also includes certain closely related anhydro-base derivatives which, like the formula (I) compounds, possess beneficial effects on the cardiovascular system (and in particular beneficial effects modulated via the sino-atrial node). Also included are pharmaceutical compositions containing the formula (I) compound (or a related anhydro-base) as active ingredient, and processes for the manufacture of the various novel compounds.
(FR)
L'invention concerne de nouveaux sels d'aminopyrimidinium de formule (I) dans laquelle R1 est alcoyle, alkényle, cycloalcoyle, phényle, phénylalcoyle ou cycloalcoyle-alcoyle; l'un de R2 et R6 est un groupe de base choisi parmi amino, alcoyleamino, dialcoyleamino de jusqu'à huit atomes de carbone, pyrrolidino, piperidino, et morpholino; et l'autre de R2 et R6 est hydrogène, alcoyle, alkényle, alkoxyalcoyle, phényle, phénylalcoyle, cycloalcoyle ou cycloalcoyle-alcoyle; ou les R2 et R6 sont les groupes basiques mentionnés ci-dessus; et R5 est hydrogène, (1-AC)alcoyle ou (3-6C) alkényle; ou R2 est un groupe basique mentionné ci-dessus, et R5 et R6 ensemble constituent l'alkylène ou, avec les atomes de carbone pendants d'un cycle pyramidine, complètent un cycle benzène; R4 est hydrogène, alcoyle, cycloalcoyle-alcoyle, aldényle, alkynyle ou phénoalcoyle; ou R4 est un alkylène ou alkénylène, substitué ou non, lié à l'atome azote du groupe Q.A.N-, chacun des groupes de liaison pouvant compléter un noyau comprenant deux atomes adjacents de carbone de Q, les atomes de carbone d'A et l'atome d'azote adjacent du groupe -A.N-; A est une liaison direct avec le groupe -N(R4)- ou est alkylène ou oxyalkylène; Q est une unité pyridyle, furyle, thiényle, ou phényle; et Y est un anion physiologiquement acceptable, mais ne comprenant pas un certain nombre de composés. L'invention comprend aussi des dérivés anhydro-base affines qui, de même que les composés de formule (I), possèdent des effets bénéfiques pour le système cardiovasculaire (et en particulier, des effets bénéfiques modulés par le n÷ud sino-auriculaire). Sont également comprises des compositions pharmaceutiques contenant le composé de formule (I) (ou un anhydrobase affine) en tant qu'ingrédient actif, et procédés pour la fabrication des divers composés nouveaux.
Also published as
FI906307
NO19905519
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