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1. WO1996002541 - 8-ARYL-1,6-NAPHTHYRIDIN-5-ONES

Publication Number WO/1996/002541
Publication Date 01.02.1996
International Application No. PCT/IB1995/000529
International Filing Date 29.06.1995
Chapter 2 Demand Filed 23.01.1996
IPC
C07D 471/04 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/-C07D463/251
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
CPC
A61P 11/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
11Drugs for disorders of the respiratory system
06Antiasthmatics
C07D 471/04
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
471Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
02in which the condensed system contains two hetero rings
04Ortho-condensed systems
Applicants
  • F. HOFFMANN-LA ROCHE AG [CH/CH]; P.O. Box 3255 CH-4002 Basle, CH (AllExceptUS)
  • LOE, Bradley, Earl [US/US]; US (UsOnly)
  • WILHELM, Robert, Stephen [US/US]; US (UsOnly)
Inventors
  • LOE, Bradley, Earl; US
  • WILHELM, Robert, Stephen; US
Agents
  • POPPE, Regina; P.O. Box 3255 CH-4002 Basle, CH
Priority Data
08/274,61513.07.1994US
Publication Language English (EN)
Filing Language English (EN)
Designated States
Title
(EN) 8-ARYL-1,6-NAPHTHYRIDIN-5-ONES
(FR) 8-ARYLE-1,6-NAPHTHYRIDINE-5-ONES
Abstract
(EN)
The disclosed 8-aryl-1,6-naphthyridin-5-ones, compounds of Formula (I), wherein: R1 is hydrogen, alkyl, lower alkyl, cycloalkyl, heteroalkyl, heterocycloalkyl, aryl, heteroaryl, cycloalkyl lower alkyl, heterocycloalkyl lower alkyl, aralkyl or heteroaralkyl; and R2 is aryl; or a pharmaceutically acceptable salt or N-oxide thereof are useful as anti-inflammatory agents, immunosuppressive agents, anti-allograft rejection agents, anti-graft-vs-host disease agents, anti-allergic agents (e.g., asthma, rhinitis and atopic dermatitis), bronchodilation agents, anti-autoimmune agents or analgetic agents.
(FR)
La présente invention concerne des composés des 8-aryle-1,6-naphthyridine-5-ones représentés par la formule générale (I), dans laquelle 'R1' est hydrogène, alkyle, alkyle inférieur, cycloalkyle, hétéroalkyle, hétérocycloalkyle, aryle, hétéroaryle, alkyle inférieur de cycloalkyle, alkyle inférieur d'hétéroalkyle, aralkyle ou hétéroaralkyle, et 'R2' est aryle; ou l'un de leurs sels ou encore l'un de leurs N-oxydes pharmaceutiquement acceptables. Ces composés sont utiles comme anti-inflammatoires, immunodépresseurs, antirejets d'allogreffons, agents antiréaction du greffon contre l'hôte, antiallergiques (par exemple asthme, rhinite et eczéma atopique), bronchodilatateurs, anti-autoimmunitaires ou analgésiques.
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