| 摘要 |
<p>(A) Pharmaceutical compsns. in unit dose form for treatment of migraine contain 0.5-100 (pref. 3-30) mg per unit does of tropyl benzoate derivs. of formula (I) or their salts: (where R1 is 1-4C alkyl, 1-4C alkoxy or halogen; R2 is H, 1-4C alkyl, 1-4C alkoxy or halogen; R3 is H, 1-4C alkyl, 1-4C alkoxy or halogen, provided that R3 is H when R2 is H). (B) Cpds. (I) are new, except for those where: (a) R1=OMe, R2=R3=H; (b) R1=R2=R3=OMe; (c) R1=R2=OMe, R3=OBu; (d) R1=Cl, R2=R3=H; and (d) R1=R2= Cl, R3=H. Cpds. (I) are many times more potent than meto-clopramide as 5-hydroxytryptamine M-receptor antagonists and are highly selective in their action. GBAB- GB2100259 B (A) Pharmaceutical compsns. in unit dose form for treatment of migraine contain 0.5-100 (pref. 3-30) mg per unit does of tropyl benzoate derivs. of formula (I) or their salts: (where R1 is 1-4C alkyl, 1-4C alkoxy or halogen; R2 is H, 1-4C alkyl, 1-4C alkoxy or halogen; R3 is H, 1-4C alkyl, 1-4C alkoxy or halogen, provided that R3 is H when R2 is H). (B) Cpds. (I) are new, except for those where: (a) R1=OMe, R2=R3=H; (b) R1=R2=R3=OMe; (c) R1=R2=OMe, R3=OBu; (d) R1=Cl, R2=R3=H; and (d) R1=R2= Cl, R3=H. Cpds. (I) are many times more potent than meto-clopramide as 5-hydroxytryptamine M-receptor antagonists and are highly selective in their action. (15pp) USAB- US4563465 A Method of treating migraine comprises admin. of a substd. tropyl benzoate of formula (I) where R1 is 1-4C alkyl, 1-4C alkoxy, or halogen; R2 is H, 1-4C alkyl, 1-4C alkoxy or halogen; R3 is H, 1-4C alkyl or 1-4C alkoxy, but is H when R2 is H. Salts of cpds. (I) are also claimed. In pref. cpds., R1=Me, OMe or Cl, and R2=R3=H. Cpds.(I), some of which are known, can be prepd. by reaction of tropine with an acid halide of formula (II) (where X is halogen, esp. Cl) at 140-160 deg.C. 0.01-10 (0.03-3.0) mg cpd. (I) per kg body wt. is used. (7pp)</p> |
