| 摘要 |
<p>Cpds. of formula (I) and their salts are esters are new. (R1-R3 are H, halogen, 1-10C alkyl or 1-4C alkoxy; R4 is OH, 1-3C alkoxy, 1-3C hydroxyalkoxy or NR5R6; R5 is H or 1-7C alkyl; and R6 is 1-7C alkyl or 5- to 7-membered cycloalkyl; or NR5R6 is a 5- to 7-membered heterocyclic ring. In the alkyl, alkoxy and hydroxyalkoxy gps. the no. of C atoms refers to those in the main chain of each gp.). - (I) have antiallergic, antiinflammatory and expectorant activities, and they have prolonged activity on oral admin. They have a strong antagonist and synthesis-inhibiting action against SRS-A. Typical LD50 values are 300 mg/kg orally in mice. Dose is 1-1000 mg 1-3 times daily. (0/0) EPAB- EP-100250 B 3-Methylflavone derivatives represented by the following general formula (I) in which R1, R2 and R3 are same or different and are hydrogen, halogen, alkyl with one to ten carbons, or alkoxy with one to four carbons; R4 is hydroxyl, alkoxy with one to three carbons, hydroxyalkyloxy with one to three carbons or (II) (wherein R5 is hydrogen or alkyl with one to seven carbons; R6 is alkyl with one to seven carbons or cycloalkyl with five to seven members; or R5 and R6 may be joined to form, together with the nitrogen atom to which they are joined, a five- to seven-membered ring, and salts thereof, except the compounds where R1, R2 and R3 are hydrogen and, at the same time, R4 is hydroxyl or ethoxy. (31pp) USAB- US4594345 A 3-Methylflavone-8-carboxylates of formula (I) are new. In (I), R1, R2 and R3 are each H, halo, 1-15C-alkyl, with 1-10C in longest chain or 1-6C alkoxy; R4 is OH, 1-6C alkoxy or hydroxy-1-6C alkoxy or NR5R6; R5 is H or 1-6C alkyl and R6, 1-6C alkyl or 5-7C cycloalkyl or R5 and R6 together with attached N are pyrrolidino, piperidino or morpholino; and salts. - (I) may be prepd. in various ways e.g. Fries rearrangement of 2-propionyloxybenzoic acid with AlCl3, followed by treatment with benzoic anhydride or alkali benzoate to (I).</p> |
