A process for the preparation of novel derivatives of 4,9-dihydro-4,9-dioxo-naphtho (2,3-d) -u-triazole.

摘要

Cpds. of formula (I) and their salts are new (where R1, is H or 1-6C alkyl; R2-4 are each H, OH, halogen, 1-4C alkyl, 1-4C alkoxy or 1-4C alkanoyl, G is H or OH; and m and n are each 1,2 or 3; provided that when G is OH, m or n is 1). - 4 cpds. are specifically claimed e.g. 6-(3-(4-acetyl-3-hydroxy -2-n-propylphenoxy)propoxy) -4,9-dihydro-4,9-dioxo -1H-naphtho(2,3-d)-v-triazole. - (I) inhibit the release of mediators of the allergic response and also antagonise the effects of SRS-A released after anti-body antigen combination activation of certain cells. (I) are thus useful in prophylaxis and treatment of e.g. asthma, hay fever, rhinitis and allergic eczema. Admin. may be orally rectally topically, parenterally, etc. or pref. by inhalation. Doses are e.g. 0.001-100 mg/kg/day, e.g. in units of 1-500 mg p.o. or 0.01-10 mg by inhalation. EPAB- EP-112419 B A compound of formula (I): or a pharmaceutically acceptable salt thereof, wherein R1 is a hydrogen atom or a C1-6 alkyl group, R2, R3 and R4 are the same or different and are selected from hydrogen, hydroxyl, halogen, C1-4 alkyl, C1-4 alkoxy and C1-4 alkanoyl; G is a hydrogen atom or a hydroxyl group, and m and n are independently integers of from 1 to 3, with the proviso that when G is a hydroxyl group, m or n is 1. - (23pp) - EP-112419 B Cpds. of formula (I) and their salts are new (where R1, is H or 1-6C alkyl; R2-4 are each H, OH, halogen, 1-4C alkyl, 1-4C alkoxy or 1-4C alkanoyl, G is H or OH; and m and n are each 1,2 or 3; provided that when G is OH, m or n is 1). - 4 cpds. are specifically claimed e.g. 6-(3-(4-acetyl-3-hydroxy -2-n-propylphenoxy)propoxy) -4,9-dihydro-4,9-dioxo -1H-naphtho(2,3-d)-v-triazole. - (I) inhibit the release of mediators of the allergic response and also antagonise the effects of SRS-A released after anti-body antigen combination activation of certain cells. (I) are thus useful in prophylaxis and treatment of e.g. asthma, hay fever, rhinitis and allergic eczema. Admin. may be orally rectally topically, parenterally, etc. or pref. by inhalation. Doses are e.g. 0.001-100 mg/kg/day, e.g. in units of 1-500 mg p.o. or 0.01-10 mg by inhalation. (Dwg.0/0)