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1. (WO1991006538) SUBSTITUTED BENZOYLBENZENE-, BIPHENYL- AND 2-OXAZOLE- ALKANOIC ACID DERIVATIVES AS INHIBITORS OF PLA¿2? AND LIPOXYGENASE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/006538 International Application No.: PCT/US1990/006252
Publication Date: 16.05.1991 International Filing Date: 27.10.1990
Chapter 2 Demand Filed: 14.05.1991
IPC:
C07C 45/00 (2006.01) ,C07C 45/63 (2006.01) ,C07C 45/72 (2006.01) ,C07C 59/90 (2006.01) ,C07C 69/738 (2006.01) ,C07C 205/45 (2006.01) ,C07C 255/40 (2006.01) ,C07D 215/14 (2006.01) ,C07D 263/32 (2006.01) ,C07D 413/12 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
45
Preparation of compounds having CO groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
45
Preparation of compounds having CO groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61
by reactions not involving the formation of CO groups
63
by introduction of halogen; by substitution of halogen atoms by other halogen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
45
Preparation of compounds having CO groups bound only to carbon or hydrogen atoms; Preparation of chelates of such compounds
61
by reactions not involving the formation of CO groups
67
by isomerisation; by change of size of the carbon skeleton
68
by increase in the number of carbon atoms
72
by reaction of compounds containing CO groups with the same or other compounds containing CO groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
59
Compounds having carboxyl groups bound to acyclic carbon atoms and containing any of the groups OH, O-metal, -CHO, keto, ether, groups, groups, or groups
40
Unsaturated compounds
76
containing keto groups
90
containing singly bound oxygen-containing groups
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
69
Esters of carboxylic acids; Esters of carbonic or haloformic acids
66
Esters 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
73
of unsaturated acids
738
Esters of keto-carboxylic acids
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
205
Compounds containing nitro groups bound to a carbon skeleton
45
the carbon skeleton being further substituted by at least one doubly-bound oxygen atom, not being part of a -CHO group
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
255
Carboxylic acid nitriles
01
having cyano groups bound to acyclic carbon atoms
32
having cyano groups bound to acyclic carbon atoms of a carbon skeleton containing at least one six-membered aromatic ring
40
the carbon skeleton being further substituted by doubly-bound oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
215
Heterocyclic compounds containing quinoline or hydrogenated quinoline ring systems
02
having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen atoms or carbon atoms directly attached to the ring nitrogen atom
12
with substituted hydrocarbon radicals attached to ring carbon atoms
14
Radicals substituted by oxygen atoms
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
263
Heterocyclic compounds containing 1,3-oxazole or hydrogenated 1,3-oxazole rings
02
not condensed with other rings
30
having two or three double bonds between ring members or between ring members and non-ring members
32
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached to ring 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
Applicants:
AMERICAN HOME PRODUCTS CORPORATION [US/US]; 685 Third Avenue New York, NY 10017, US
Inventors:
FAILLI, Amedeo, Arturo; US
KREFT, Anthony, Frank, III; US
MUSSER, John, Henry; US
Agent:
ALICE, Ronald, W.; American Home Products Corporation 685 Third Avenue New York, NY 10017 , US
PORTER, Graham, Ronald ; Wyeth Laboratories Patents and Trademark Department Huntercombe Lane South Taplow/Nr Maidenhead Berks SL6 0PH, GB
Priority Data:
427,67727.10.1989US
Title (EN) SUBSTITUTED BENZOYLBENZENE-, BIPHENYL- AND 2-OXAZOLE- ALKANOIC ACID DERIVATIVES AS INHIBITORS OF PLA2 AND LIPOXYGENASE
(FR) DERIVES D'ACIDE ALCANOIQUES BENZOYLBENZENE, BIPHENYLE ET 2-OXAZOLE SUBSTITUES UTILISES COMME INHIBITEURS DE LA PHOSPHOLIPASE A2(PLA2) ET DE LA LIPOXYGENASE
Abstract:
(EN) There are disclosed compounds of the formula: A(CH2)nO-B, wherein A is phenoxyethyl, phenoxyphenyl or a group having formula (a), wherein X is -N- or (b); Z is (c), (d), (e), (f), -S- or -O-; R1 is hydrogen, lower alkyl or phenyl; R2 is hydrogen or lower alkyl; or R1 and R2 taken together form a benzene ring; R3 is hydrogen or lower alkyl; n is 1 -2; B is (g), (h), (i) or (j), wherein R4 and R5 are each, independently, hydrogen or lower alkyl; R6 is halo or nitro; R7 is (k) or (l); R8 is lower alkyl; m is 0-3; and the pharmacologically acceptable salts thereof, and their use in the treatment of inflammatory conditions, such as rheumatoid arthritis, ulcerative colitis, psoriasis and other immediate hypersensitivity reactions; in the treatment of leukotriene-mediated naso-bronchial obstructive air-passageway conditions, such as allergic rhinitis, allergic bronchial asthma and the like; and as gastric cytoprotective agents.
(FR) L'invention se rapporte à des composés représentés par la formule: A(CH2)nO-B, où: A représente un phénoxyéthyle, un phénoxyphényle ou un groupe ayant la formule (a), où X représente -N- ou (b), Z représente (c), (d), (e), (f), -S- ou -O-, R1 représene l'hydrogène, un alkyle inférieur ou un phényle, R2 représente l'hydrogène ou un alkyle inférieur, ou R1 et R2 forment ensemble une chaîne fermée de benzène, R3 représente l'hydrogène ou un alkyle inférieur; n est égal à 1 ou à 2; B représente un groupe ayant la formule (g), (h), (i) ou (j), où R4 et R5 représentent chacun séparément l'hydrogène ou un alkyle inférieur, R6 représente un halo ou un nitro, R7 représente (k) ou (l), R8 représente un alkyle inférieur, et m est égal à un nombre compris entre 0 et 3; ainsi qu'aux sels pharmacologiquement acceptables de tels composés, et à leur utilisation dans le traitement d'états inflammatoires, tels que l'arthrite rhumatoïde, la colite ulcérative, le psoriasis et d'autres réactions d'hypersensibilité immédiate, dans le traitement d'états obstructifs des voies bronchonasales se développant par l'intermédiaire de la leukotriène, tels que la rhinite allergique, l'asthme bronchique allergique et similaires et comme agents cytoprotecteurs gastriques.
Designated States: AU, BR, CA, FI, HU, JP, KR, SU
European Patent Office (AT, BE, CH, DE, DK, ES, FR, GB, GR, IT, LU, NL, SE)
Publication Language: English (EN)
Filing Language: English (EN)
Also published as:
FI921864EP0497888JPH05502021CA2067138PT95690KR1019927003552
AU1990067220ID002.671