6-Substd. 2-benzoxazolinone derivs. - useful as analgesics

Benzoxazolin-2-one derivs. of formula (I) and their salts are new. R is H or lower alkyl; X + Y is a bond and Z is OH, or X is H and Y and Z are H, 1-5C alkyl or arylmethyl). Specifically claimed are 5 cpds. (I), including 3-methyl-6 (1- hydroxyimino-2-phenylethyl)- 2-benzoxazolinone (Ia) and 3- met...

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1. Verfasser: DANIEL LESIEUR, CHARLES LESPAGNOL, DANIEL CAIGNARD, MICHELINE CASIN, NORBERT BUSCH ET MICHEL COMBOURIEU
Format: Patent
Sprache:eng ; fre
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Zusammenfassung:Benzoxazolin-2-one derivs. of formula (I) and their salts are new. R is H or lower alkyl; X + Y is a bond and Z is OH, or X is H and Y and Z are H, 1-5C alkyl or arylmethyl). Specifically claimed are 5 cpds. (I), including 3-methyl-6 (1- hydroxyimino-2-phenylethyl)- 2-benzoxazolinone (Ia) and 3- methyl-6 (1-amino-2-phenylethyl) 2-benzoxazolinone. (I) are analgesics which has low toxicity (LD50 generally 1-4g/kg., p.o. mouse) and are effective at daily doses of 0.1-2g. DERIVES D'(A-AMINO OU A-IMINO PHENETHYL)-6 BENZOXAZOLINONES.ILS ONT POUR FORMULE:(CF DESSIN DANS BOPI)DANS LAQUELLE R DESIGNE L'HYDROGENE OU UN RADICAL ALKYLE INFERIEUR; X ET Y REPRESENTENT ENSEMBLE UNE DOUBLE LIAISON, TANDIS QUE Z REPRESENTE LE RADICAL HYDROXY, OU BIEN X REPRESENTE L'HYDROGENE ET Y ET Z, IDENTIQUES OU DIFFERENTS, REPRESENTENT CHACUN L'HYDROGENE, UN RADICAL ALKYLE AYANT AU PLUS 5ATOMES DE CARBONE OU UN RADICAL ARALKYLE -CH-AR, TEL QUE LE RADICAL BENZYLE, AINSI QUE LEURS SELS PHARMACEUTIQUEMENT ACCEPTABLES.APPLICATION AU TRAITEMENT DES SYNDROMES DOULOUREUX.