HOFFMANN MATTHIAS,DAHMANN GEORG,FIEGEN DENNIS,HANDSCHUH SANDRA,KLICIC JASNA,LINZ GUENTER,SCHAENZLE GERHARD,SCHNAPP ANDREAS,EAST STEPHEN P.,MAZANETZ MICHAEL PHILIP,SCOTT ROBERT JOHN,WALKER EDWARD
申请号：
NZ60085711
公开号：
NZ600857A
申请日:
2011.01.21
申请国别(地区):
NZ
年份:
2014
代理人:
摘要：
Disclosed are 5-(heterocyclylalkoxy)-1,6-naphthyridine derivatives as represented by the general formula (I), wherein: R1 is selected from among -O-R3 or -NR3R4； wherein R3 is alkyl which is substituted by R5 and R6； wherein R5 is selected from hydrogen, branched or linear alkyl, alkenyl, alkylen-O-alkyl or haloalkyl； wherein R6 is a lactam ring moiety as defined in the specification； R2 is selected from hydrogen, optionally substituted aryl, optionally substituted heteroaryl, an optionally substituted saturated or partially unsaturated heterocycle and optionally substituted saturated or partially unsaturated cycloalkyl； and wherein the remaining substituents are as defined herein. Representative compounds include (R)-4-[(R)-1-[7-(3,4,5-trimethoxy-phenyl)-[1,6]naphthyridin-5-yloxy]-ethyl]pyrrolidin-2-one, (R)-4-[[7-(4-trifluoromethyl-phenyl)-[1,6]naphthyridin-5-yloxy]methyl]pyrrolidin-2-one, (R)-4-[[7-(5-methyl-1,2-oxazol-3-yl)-[1,6]naphthyridin-5-yloxy]methyl]pyrrolidin-2-one, 4-[[7-(3,4-dimethoxyphenyl)-[1,6]naphthyridin-5-yloxy]methyl]-2-oxo-1,3,4-oxadiazole. Further disclosed is a pharmaceutical formulation which contains one or more compounds of formula 1 as defined above, optionally in combination with an active substance selected from among anticholinergics, betamimetics, corticosteroids, PDE4-inhibitors, EGFR-inhibitors, LTD4-antagonists, CCR3-inhibitors, iNOS-inhibitors and HMG-CoA reductase inhibitors, for the treatment of diseases selected from among allergic rhinitis, asthma, COPD, adult respiratory distress syndrome, bronchitis, B-cell lymphoma, dermatitis and contact dermatitis, allergic dermatitis, allergic rhinoconjunctivitis, rheumatoid arthritis, anti-phospholipid syndrome, Berger&rsquo；s disease, Evans&rsquo；s syndrome, ulcerative colitis, allergic antibody-based glomerulonephritis, granulocytopenia, Goodpasture&rsquo；s syndrome, hepatitis, Henoch-Schönlein purpura, hypersensitivity vasculitis, immunohaemolytic anaemia, autoimmune haemolytic anemi
