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1. WO1991000280 - 6-(HYDRONAPHTYL-1-ETHYL)-4-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONES AND THE CORRESPONDING HYDROXY ACIDS

Publication Number WO/1991/000280
Publication Date 10.01.1991
International Application No. PCT/GB1990/001030
International Filing Date 04.07.1990
Chapter 2 Demand Filed 17.12.1990
IPC
C07C 69/732 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
732of unsaturated hydroxy carboxylic acids
C07C 69/738 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxyl groups bound to acyclic carbon atoms and having any of the groups OH, O-metal, -CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
738Esters of keto-carboxylic acids
C07D 309/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
309Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
16having one double bond between ring members or between a ring member and a non-ring member
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
30Oxygen atoms, e.g. delta-lactones
CPC
C07C 69/732
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
732of unsaturated hydroxy carboxylic acids
C07C 69/738
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
69Esters of carboxylic acids; Esters of carbonic or haloformic acids
66Esters of carboxylic acids having esterified carboxylic groups bound to acyclic carbon atoms and having any of the groups OH, O—metal, —CHO, keto, ether, acyloxy, groups, groups, or in the acid moiety
73of unsaturated acids
738Esters of keto-carboxylic acids ; or aldehydo-carboxylic acids
C07D 309/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
309Heterocyclic compounds containing six-membered rings having one oxygen atom as the only ring hetero atom, not condensed with other rings
16having one double bond between ring members or between a ring member and a non-ring member
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
30Oxygen atoms, e.g. delta-lactones
Applicants
  • BRITISH BIO-TECHNOLOGY LIMITED [GB/GB]; Watlington Road Cowley Oxford OX4 5LY, GB (AllExceptUS)
  • LEWIS, Christopher, Norman [GB/GB]; GB (UsOnly)
  • DAVIDSON, Alan, Hornsby [GB/GB]; GB (UsOnly)
  • FLOYD, Christopher, David [GB/GB]; GB (UsOnly)
  • DICKENS, Jonathan, Philip [GB/GB]; GB (UsOnly)
Inventors
  • LEWIS, Christopher, Norman; GB
  • DAVIDSON, Alan, Hornsby; GB
  • FLOYD, Christopher, David; GB
  • DICKENS, Jonathan, Philip; GB
Agents
  • SHEARD, Andrew, Gregory ; Kilburn & Strode 30 John Street London WC1N 2DD, GB
Priority Data
8915280.504.07.1989GB
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 6-(HYDRONAPHTYL-1-ETHYL)-4-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONES AND THE CORRESPONDING HYDROXY ACIDS
(FR) 6-(HYDRONAPHTYL-1-ETHYL)-4-HYDROXY-3,4,5,6-TETRAHYDRO-2H-PYRAN-2-ONES ET LES HYDROXY ACIDES CORRESPONDANTS
Abstract
(EN)
Compounds of either of general formulae (I) and (II), wherein: R1 represents a C1-8 alkyl, C3-8 cycloalkyl, C3-8 cycloalkyl(C1-8)alkyl, C2-8 alkenyl, or C1-6 alkyl substituted phenyl group; R2 represents a C1-8 alkyl, C2-8 alkenyl, C2-8 alkynyl group or a C1-5 alkyl, C2-5 alkenyl, or C2-5 alkynyl group substituted with a substituted phenyl group; R3 represents a hydrogen atom or a substituent R4 or M; R4 represents a C1-5 alkyl group, or a C1-5 alkyl group substituted with a group chosen from substituted phenyl, dimethylamino and acetylamino; R5 represents a hydrogen atom or a methyl or ethyl group, except that when R2 is methyl then R5 is not methyl; M represents a cation capable of forming a pharmaceutically acceptable salt; Q represents C=O or CHOH; and each of a, b, c, and d is independently a single or double bond except that when a and c are double bonds then b is a single bond; are inhibitors of the enzyme 3-hydroxy-3-methylglutaryl coenzyme A reductase (HMG-CoA reductase), the rate limiting enzyme in the biosynthesis of cholesterol in mammals including man, and as such are useful in the treatment of hypercholesterolaemia in general and arteriosclerosis, familiar hypercholesterolaemia or hyperlipidaemia in particular.
(FR)
Composés de l'une ou de l'autre des formules générales (I) et (II), dans lesquelles: R1 représente un groupe phényle C1-8 alkyle, C3-8 cycloakyle, C3-8 cycloalkyle(C1-8)alkyle, C2-8 alkényle, ou C1-6 alkyle phényle substitué; R2 représente un groupe C1-8 alkyle, C2-8 alkényle, C2-8 alkynyle ou un groupe C1-5 alkyle, C2-5 alkényle, ou C2-5 alkynyle substitué par un groupe phényle substitué; R3 représente un atome d'hydrogène ou un substituant R4 ou M; R4 représente un groupe C1-5 alkyle, ou un groupe C1-5 alkyle substitué par un groupe choisi d'entre phényle substitué, diméthylamino et acétylamino; R5 représente un atome d'hydrogène ou un groupe méthyle ou éthyle, à la condition que R5 ne soit pas méthyle lorsque R2 est méthyle; M répresente un cation capable de former un sel pharmaceutiquement acceptable; Q représente C=O ou CHOH; et chacune des liaisons a, b, c, et d, est indépendamment une liaison simple ou double, sauf si a et c sont des liaisons doubles, auquel cas b est une liaison simple; Ces composés sont des inhibiteurs de 3-hydroxy-3 méthylglutaryl-coenzyme A réductase (HMG-CoA Réductase), l'enzyme limitant la vitesse de biosynthèse du cholestérol chez les mammifères, y compris chez l'homme, et sont donc utiles dans le traitement de l'hypercholestérolémie en général et de l'artériosclérose, de l'hypercholestérolémie et de l'hyperlipidémie familiales en particulier.
Also published as
FI920036
NO19920057
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