| abstract |
PCT No. PCT/EP92/00591 Sec. 371 Date Apr. 20, 1994 Sec. 102(e) Date Apr. 20, 1994 PCT Filed Mar. 17, 1992 PCT Pub. No. WO92/17451 PCT Pub. Date Oct. 15, 1992. <IMAGE> (I) Compounds of formula (I) or a biolabile ester thereof, or a pharmaceutically acceptable salt of either, wherein Rl, R2, R3 and R4 are each independently selected from H or C1-C4 alkyl; R5 is (CH2)mSO2R6, (CH2)mNHSO2R6 or (CH2)mNHCOR7; R6 and R7 are C1-C6 alkyl, C1-C3 perfluoroalkyl(CH2)n, C3-C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n; or R6 is NR8R9; R8 is H or C1-C4 alkyl; R9 is C1-C6 alkyl, C3-C6 cycloalkyl(CH2)n, aryl(CH2)n or heteroaryl(CH2)n; or R8 and R9 together with the nitrogen atom to which they are attached form a 5- to 7-membered heterocyclic ring which may optionally incorporate a carbon-carbon double bond or a further hetero atom linkage selected from O, S, NH, N(C1-C4 alkyl) and N(C1-C5 alkanoyl), and which may optionally be substituted with one to three substituents each independently selected from C1-C4 alkyl and C1-C4 alkoxy, and which may optionally be benzo-fused; X is CH2, CHCH3, C(OH)CH3, C=CH2 or O; m is 0 or 1; n is 0, 1, 2 or 3; and Het is 3- or 4-pyridyl or 1-imidazolyl; with the proviso that when Het is 1-imidazolyl then X is CH2 or CHCH3, are combined thromboxane A2 synthetase inhibitors and thromboxane A2/endoperoxide antagonists of utility in the treatment of disease conditions in which thromboxane A2 is a causative agent. |