C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 213/56 (2006.01) A61K 31/415 (2006.01) A61K 31/44 (2006.01) C07D 213/55 (2006.01) C07D 213/65 (2006.01) C07D 233/61 (2006.01) C07D 401/12 (2006.01) C07D 403/12 (2006.01) C07D 405/12 (2006.01) C07D 409/12 (2006.01) C07D 521/00 (2006.01)
Patent
CA 2104456
Compounds of formula (I) or a biolabile ester thereof, or a pharmaceutically acceptable salt of either, wherein R1, R2, R3 and R4 are each independently selected from H or C1-C4 alkyl, R5is (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 heteroa- ryl(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 heteroa- ryl(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 in- dependently 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.
Dack Kevin Neil
Dickinson Roger Peter
Steele John
Limited Pfizer
Smart & Biggar
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