| 摘要 |
<p>Novel 1,4-benzodiazepines, muscle relaxants and bronchodilators. Have formula (where R1 is H, hal, lower alkyl, alkoxy, nitro, etc. and R2 = cycloalkylmethyl) and may be prepd. by treating 7-R1-1-(R2)-5-phenyl-1H-1,4-benzodiazepin-2(3H)-one with HAc and perHAc to obtain its corresponding N-oxide, treating this with acetic anhydride to obtain the corresponding 3-acetoxy deriv. which is treated with a base. They are useful muscle relaxants and bronchodilators, as demonstrated in histamine and serotonin induced lung constriction. Pref. R1=Cl, R2= -C Also claimed are the 3-acetoxy derivs. Typical doses are 5-25 mg., 3-4 times daily tranquilliser); and 1-20 mg/kg., pref. 10 mg/kg. (bronchodilators), given either orally, i.p. or rectally.</p> |
