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1. (WO2001005749) AMINOBENZOPHENONES AS INHIBITORS OF IL-1β AND TNF-$g(a)

Pub. No.:    WO/2001/005749    International Application No.:    PCT/DK2000/000386
Publication Date: Fri Jan 26 00:59:59 CET 2001 International Filing Date: Wed Jul 12 01:59:59 CEST 2000
IPC: A61K 31/00
A61K 45/06
C07C 271/28
C07C 271/38
C07C 271/58
Applicants: LEO PHARMACEUTICAL PRODUCTS LTD. A/S (LØVENS KEMISKE FABRIK PRODUKTIONSAKTIESELSKAB)
OTTOSEN, Erik, Rytter
DANNACHER, Heinz, Wilhelm
Inventors: OTTOSEN, Erik, Rytter
DANNACHER, Heinz, Wilhelm
Title: AMINOBENZOPHENONES AS INHIBITORS OF IL-1β AND TNF-$g(a)
Abstract:
The present invention relates to compounds of formula (I) wherein R1, R2 and R3 independently represent one or more, same or different substituents selected from the group consisting of hydrogen, halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkyl, (C2-C3)olefinic group, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, carbamoyl, or phenyl; R1 and R2 further represented by nitro and R3 by carboxy; R4 represents hydrogen, (C1-C3)alkyl, or allyl; Q represents a bond, or -C(R6)(R7)(-O-C=O)-, in which formula R6 and R7 independently represent hydrogen, trifluoromethyl, or (C1-C4)alkyl; Y represents either (C5-C15)alkyl, (C2-C15)olefinic group, (C3-C10)monocyclic hydrocarbon, or phenyl, any of which may be optionally substituted with one or more, same or different substituents represented by the formula R5; or (C1-C4)alkyl substituted with at least one or more substituents with the formula R5; or Y represents a group of formula -CH2-(Z-O)n-Z where Z is a (C1-C3)alkyl, where n is a integer > 1 and no continuous linear sequence of atoms in the group Y > 15; R5 represents halogen, hydroxy, mercapto, trifluoromethyl, amino, (C1-C3)alkoxy, (C1-C3)alkylthio, (C1-C6)alkylamino, (C1-C3)alkoxycarbonyl, cyano, azido, nitro, -COOH, -CONH2, -CONHR', or -COONR'R' wherein R' stands for (C1-C3)alkyl; X represents oxygen or sulphur, or a pharmaceutically acceptable salt thereof, or a hydrate or solvate thereof. The compounds are valuable in the human and veterinary therapy.