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1. (WO1997021676) AZETIDINONE COMPOUNDS FOR THE TREATMENT OF ATHEROSCLEROSIS
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1997/021676 International Application No.: PCT/EP1996/005588
Publication Date: 19.06.1997 International Filing Date: 04.12.1996
Chapter 2 Demand Filed: 08.07.1997
IPC:
C07D 205/09 (2006.01) ,C07D 401/14 (2006.01) ,C07D 413/06 (2006.01) ,C07D 413/12 (2006.01) ,C07D 417/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
205
Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
02
not condensed with other rings
06
having one double bond between ring members or between a ring member and a non-ring member
08
with one oxygen atom directly attached in position 2, e.g. beta-lactams
09
with a sulfur atom directly attached in position 4
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
401
Heterocyclic 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
14
containing three or more hetero rings
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
06
linked by a carbon chain containing only aliphatic carbon atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
413
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
417
Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
02
containing two hetero rings
12
linked by a chain containing hetero atoms as chain links
Applicants:
SMITHKLINE BEECHAM PLC [GB/GB]; New Horizons Court Brentford Middlesex TW8 9EP, GB (AllExceptUS)
HICKEY, Deirdre, Mary, Bernadette [IE/GB]; GB (UsOnly)
DHANAK, Dashyant [GB/US]; US (UsOnly)
IFE, Robert, John [GB/GB]; GB (UsOnly)
LEACH, Colin, Andrew [GB/GB]; GB (UsOnly)
TEW, David, Graham [GB/GB]; GB (UsOnly)
Inventors:
HICKEY, Deirdre, Mary, Bernadette; GB
DHANAK, Dashyant; US
IFE, Robert, John; GB
LEACH, Colin, Andrew; GB
TEW, David, Graham; GB
Agent:
CONNELL, Anthony, Christopher; SmithKline Beecham Corporate Intellectual Property Two New Horizons Court Brentford Middlesex TW8 9EP, GB
THOMPSON, Clive; SmithKline Beecham Corporate Intellectual Property Two New Horizons Court Brentford, Middlesex TW8 9EP, GB
Priority Data:
9525148.408.12.1995GB
9525149.208.12.1995GB
9525150.008.12.1995GB
Title (EN) AZETIDINONE COMPOUNDS FOR THE TREATMENT OF ATHEROSCLEROSIS
(FR) COMPOSES AZETIDINONE DESTINES AU TRAITEMENT DE L'ATHEROSCLEROSE
Abstract:
(EN) Azetidinone compounds of formula (I) in which $i(inter alia): R0 is CR4R5-X1-Y1 or (CH2)pX2(CH2)qY2; R4 and R5 which may be the same or different is each selected from hydrogen and C(1-6)alkyl, or R4 and R5 may be linked together to form the residue of a C(3-7)cycloalkyl ring; X1 is a linker group and Y1 is optionally substituted C(1-12)alkyl C(2-12)alkynyl, C(2-12)alkynyl, C(3-7)-cycloalkylC(1-8) alkyl or an optionally substituted heteroaryl group; and X2 is a heteroaryl group and Y2 is an optionally substituted aryl group, p is an integer from 1 to 6, q is 0 or an integer from 1 to 6; are inhibitors of the phospholipase A2 enzyme Lp PLA2 and are of use in therapy, for instance in treating atherosclerosis.
(FR) On décrit des composés azétidinone de la formule (I) dans laquelle, entre autres, R0 représente CR4R5-X1-Y1 ou (CH2)pX2(CH2)qY2, R4 et R5 qui peuvent être semblables ou différents représentent chacun hydrogène ou alkyle C1-6, ou bien R4 et R5 peuvent être liés ensemble afin de former le reste d'un noyau cycloalkyle C3-7, X1 représente un groupe de liaison et Y1 représente alkyle C1-12-alcényle C2-12, alcynyle C2-12, cycloalkyle C3-7-alkyle C1-8, éventuellement substitués, ou un groupe hétéroaryle éventuellement substitué, X2 représente un groupe hétéroaryle, Y2 représente un groupe aryle éventuellement substitué, p est un nombre entier compris entre 1 et 6, et q vaut 0 ou est un nombre entier compris entre 1 et 6. Ces composés sont des inhibiteurs de la phospholipase A2 enzyme, ou Lp-PLA2, et ils sont utiles en thérapie, par exemple pour traiter l'athérosclérose.
Designated States: JP, US
European Patent Office (AT, BE, CH, DE, DK, ES, FI, FR, GB, GR, IE, IT, LU, MC, NL, PT, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
EP0865429JP2000505063