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1. (WO1991006539) 2-ANILINO PHENYLACETIC ACID DERIVATIVES AS INHIBITORS OF PLA¿2? AND LIPOXYGENASE
Latest bibliographic data on file with the International Bureau

Pub. No.: WO/1991/006539 International Application No.: PCT/US1990/006253
Publication Date: 16.05.1991 International Filing Date: 27.10.1990
Chapter 2 Demand Filed: 26.04.1991
IPC:
C07C 229/42 (2006.01) ,C07D 215/14 (2006.01) ,C07D 215/18 (2006.01) ,C07D 235/12 (2006.01) ,C07D 401/04 (2006.01)
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
C
ACYCLIC OR CARBOCYCLIC COMPOUNDS
229
Compounds containing amino and carboxyl groups bound to the same carbon skeleton
40
having amino groups bound to carbon atoms of at least one six-membered aromatic ring and carboxyl groups bound to acyclic carbon atoms of the same carbon skeleton
42
with carboxyl groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by saturated carbon chains
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
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
16
with 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
18
Halogen atoms or nitro radicals
C CHEMISTRY; METALLURGY
07
ORGANIC CHEMISTRY
D
HETEROCYCLIC COMPOUNDS
235
Heterocyclic compounds containing 1,3-diazole or hydrogenated 1,3-diazole rings, condensed with other rings
02
condensed with carbocyclic rings or ring systems
04
Benzimidazoles; Hydrogenated benzimidazoles
06
with only hydrogen atoms, hydrocarbon or substituted hydrocarbon radicals, directly attached in position 2
12
Radicals substituted by oxygen atoms
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
02
containing two hetero rings
04
directly linked by a ring-member-to-ring- member bond
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 & Trademarks Department Huntercombe Lane South Taplow/Nr Maidenhead Berks SL6 OPH, GB
Priority Data:
428,09227.10.1989US
Title (EN) 2-ANILINO PHENYLACETIC ACID DERIVATIVES AS INHIBITORS OF PLA2 AND LIPOXYGENASE
(FR) DERIVES D'ACIDE PHENYLACETIQUE 2-ANILINO UTILISES COMME INHIBITEURS DE LA PHOSPHOLIPASE A2(PLA2) ET DE LA LIPOXYGENASE
Abstract:
(EN) The are disclosed compounds of formulae (I) or (II), wherein R is hydroxy, lower alkoxy or lower alkoxyamino; one of R1 and R2 is A(CH2)nO-, the other is hydrogen; n is 1 - 2; 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-; R3 is hydrogen, lower alkyl or phenyl; R4 is hydrogen or lower alkyl; or R3 and R4 taken together form a benzene ring optionally substituted by halogen; in which case the point of attachment of A to the rest of the molecule may be from this ring; R5 is hydrogen or lower alkyl and each may be the same or different; R6 is hydrogen, halo or lower alkyl and each may be the same or different; 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: (I) ou (II), où: R représente un hydroxy, un alkoxy inférieur ou un alkoxyamino inférieur; l'un des éléments R1 et R2 représente A(CH2)nO- et l'autre représente l'hydrogène; n est égal à 1 ou à 2; 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-, R3 représente l'hydrogène, un alkyle inférieur ou un phényle, R4 représente l'hydrogène ou un alkyle inférieur, ou R3 et R4 forment ensemble une chaîne fermée de benzène éventuellement substituée par un halogène, auquel cas le point d'attache de A au reste de la molécule peut former cette chaîne fermée, R5 représente l'hydrogène ou un alkyle inférieur, chacun pouvant être identique ou différent, R6 représente l'hydrogène, un halo ou un alkyle inférieur, chacun pouvant être identique ou différent; 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:
FI921863EP0523046CA2067135KR1019927003528AU1990067247