| abstract |
Isoquinolines having thromboxane synthetase inhibiting activity of the general formula:- <IMAGE> wherein X, which is attached to the 5-, 6-, 7- or 8-position, is a group of the formula -O-Y-Z or <IMAGE> Y is -(CH2)n- wherein n is 1, 2, 3 or 4, or a group of the formula;- <IMAGE> or -CH2-(Het)-; Het represents a 5 or 6 membered aromatic heterocyclic ring linked to Z by a ring carbon atom; Z is -CO2R<1>, -CONHR<2>, -CON(R<3>)2, -NHR<4>, -NHCONHR<5>, -CN, 5- tetrazolyl, 5-oxo-2-pyrazolin-1-yl or 3- methyl-5-oxo-2-pyrazolin-1-yl, with the proviso that when Y is -CH2-(Het)-, Z may also be C1-C4 alkyl, but may not be -NHR<4> or -NHCONHR<5>; R<1> is H or C1-C4 alkyl; R<2> is H, C1-C4 alkyl, C2-C4 alkanoyl, aroyl, C1-C4 alkyl-sulphonyl, arylsulphonyl, aryl, aralkyl, or a 5 or 6 membered aromatic heterocyclic ring optionally substituted by one or two C1-C4 alkyl, C1-C4 alkoxy, halogen or CF3 groups; each R<3> is C1-C4 alkyl or two groups R3 together with the nitrogen atom to which they are attached form a pyrrolidino or piperidino group; R<4> is H, C1-C4 alkyl, C2-C4 alkanoyl, C1-C4 alkylsulphonyl, or (C1-C4 alkoxy)carbonyl: and R<5> is C1-C4 alkyl or aryl: and the pharmaceutically acceptable acid addition salts thereof; pharmaceutical compositions containing them, and processes for their preparation. |