Dimethyphosphinyl-alkyl anthranilate esters - water-sol. analgesics, anti-inflammatories and anti-rheumatics

Phosphinyl derivs. of formula (I): (X is CH or N; R1 = phenyl or quinolyl both opt. substd. by halo; CF3 or 1-3C alkyl gp. with together is not >4C; R2 = a dialkylphosphinyl gp. with its terminal gps. CH3, opt. substd. in the alkylene residue by an OH and having in total 3-7C). are prepd. e.g. by...

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Hauptverfasser: SOEDER,ALFONS,.DR, PERREY,KLAUS,.DR
Format: Patent
Sprache:eng ; ger
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Zusammenfassung:Phosphinyl derivs. of formula (I): (X is CH or N; R1 = phenyl or quinolyl both opt. substd. by halo; CF3 or 1-3C alkyl gp. with together is not >4C; R2 = a dialkylphosphinyl gp. with its terminal gps. CH3, opt. substd. in the alkylene residue by an OH and having in total 3-7C). are prepd. e.g. by reacting corresp. acids or their usual reactive derivs. with R2OH. (I) have analgesic anti-inflammatory and anti-rheumatic activities without side effects. They have adequate water solubility and for 8 cpds. quoted the LD50 (p.o mice) is from 596 to >3000 mg/kg.