GB9317764D0 — Therapeutic compound

USPTO Abstract

PCT No. PCT/EP94/02660 Sec. 371 Date Feb. 23, 1996 Sec. 102(e) Date Feb. 23, 1996 PCT Filed Aug. 9, 1994 PCT Pub. No. WO95/06046 PCT Pub. Date Mar. 2, 1995Compounds of formula (I): <IMAGE> (I) and pharmaceutically acceptable salt and biolabile esters thereof, wherein R1 is H, C1-C4 alkyl, phenyl optionally substituted by up to three substituents independently selected from C1-C4 alkyl, C1-C4 alkoxy, halogen and CF3, or is 1-imidazolyl, 3-pyridyl or 4-pyridyl; R2 is H or C1-C4 alkyl, R3 is SO2R4 or COR4where R4 is C1-C6 alkyl, C1-C3 perfluoroalkyl(CH2)p, C3-C6 cycloalkyl(CH2)p, aryl(CH2)p, or heteroaryl(CH2)p, p being 0, 1 or 2, or R4 may be NR5R6 where R5 is H or C1-C4 alkyl and R6 is C1-C6, alkyl, C3-C6 cycloalkyl or aryl, or R5 and R6 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 heteroatom linkage selected from O, S, NH, N(C1-C4 alkyl) and N(C1-C5 alkanoyl); X is CH2 or a direct link, with the proviso that when R1 is 1-imidazolyl then X is CH2; m is 2, or 3; n is 0, 1 or 2, and wherein the group (CH2)nNHR3 is attached at the 5-position when n is 0 or 1, or at the 5- or 4-position when n is 2. These compounds are selective TXA2 and PGH2 antagonists. Some also inhibit thromboxane synthetase.