Quinazoline:di:one derivs. - useful as analgesics, antiinflammatory agents and sedatives

摘要

Quinazolinedione derivs. of formula (I) and their acid-addn and quat. satls are new: In (I) R1 is (i) 1-6C alkyl, (ii) 1-4C alkyl substd. by COOH, 2-4C alkoxycarbonyl, OH, pyridyl, piperidino, morpholino or NMe2, (iii) benzyl opt. ring-substd. by one Me, Cl or Br substituent, or (iii) methoxyphenyl, ethoxyphenyl or 3,4-xylyl when R2 = H or R3 = halogen, or (v) H when R2 is benzyl or methyl-substd. phenyl. R2 is (i) benzyl, (ii) methyl or ethyl substd. by pyridyl or morpholino, or (iii) methyl-substd. phenyl; R2 can also be H when R3 is halogen and R1 is methoxyphenyl, ethoxyphenyl or 3,4-xylyl. R3 is H or halogen, but must be halogen when either (i) R1 is 1-6C alkyl, CH2CH2COOEt or morpholinoethyl and R2 is methyl-substd. phenyl, or (ii) R1 is methoxyphenyl, ethoxyphenyl or 3,4-xylyl and R2 is H. Cpds. (I) are analgesics and anti-inflammatory agents. Some also have sedative activity. A typical cpd. is 7-chloro-1-(2-methoxyphenyl)-1H, 3H-quinazoline-2,4-dione. In an example, this is prepd. from 4-chloro-N-(2-methoxyphenyl)-anthranilic acid and urea.