| 摘要 |
<p>1503032 Pyrido-pyridazines TAKEDA YAKUHIN KOYGO KK 25 March 1975 [25 March 1974] 12366/75 Heading C2C Novel compounds I in which R<SP>1</SP> is H or C 1-4 alkyl and R<SP>2</SP> is an optionally substituted cyclic amino group, and pharmaceutically acceptable salts thereof, are prepared by reacting a compound II in which X is halogen and R<SP>3</SP> is H, C 1-4 alkyl or aryl-C 1-4 alkyl, with a cyclic amine, and, when R<SP>3</SP> is alkyl or aralkyl, subjecting the resulting compound to a reaction leading to cleavage of the ether bond. Compounds II are prepared by halogenating an appropriate 7 - substituted - 1,2,3,4- tetrahydro - pyrido[3,4 - d]pyridazine - 1,4- dione. The following intermediates are prepared in the examples: 4-(4-hydroxyphenyl)oxazole, 2 - (4 - hydroxyphenyl) - N - phenylpyridine- 4,5 - dicarboximide, 7 - (4 - hydroxyphenyl- 1,2,3,4 - tetrahydropyrido[3,4 - d]pyridazine- 1,4 - dione, 6 - (4 - benzyloxyphenyl) - 3 - cyano- 4 - ethoxycarbonyl - 2(1H) - thiopyridone, 6 - (4- benzyloxyphenyl) - 3 - cyano - 4 - ethoxycarbonylpyridine, 6 - (4 - benzyloxyphenyl) - cinchomeronic acid and its anhydride, and 7 - (4- benzyloxyphenyl) - 1,4 - dioxo - 1,2,3,4 - tetrahydropyrido[3,4-d]pyridazine. Pharmaceutical compositions having diuretic activity, for oral or parenteral administration, comprise a compound of the invention together with a pharmaceutical carrier or diluent therefor.</p> |
