Thiophene carboxamine derivatives and their use as...

C - Chemistry – Metallurgy – 07 – D

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167/208, 167/242

C07D 333/38 (2006.01) A61K 31/38 (2006.01) C07D 409/12 (2006.01)

Patent

CA 1338844

A pharmaceutical compound of the formula Image in which R1, R and R3 independently are hydrogen, hydroxy, halo, nitro, amino, C2-5 acylamino, C1-4 alkyl, -CHO, -CH2OH, -CH2OC1-4 alkyl, -COOH, -COC1-3 alkyl, -CH(OH)C1-3 alkyl, C1-4 alkoxy, C2-4, alkenyloxy, C1-4 alkylthio, C1-4 alkylsulphinyl, C1-4 alkylsulphonyl, N-substituted heterocyclyl, optionally substituted phenyl, optionally substituted phenylthio, option- ally substituted phenylsulphinyl, optionally substituted phenylsulphonyl or optionally substituted phenylsulphonamido, or R1 and R together form a C3-5 slkylene bridge; provided that at least one of R and R3 is C1-4 alkoxy or C2-4 alkenyl- oxy; and X is (i) -(CH2)nN(R4)2 where each R4 independently is C1-4 alkyl, C2-4 alkenyl or optionally substituted C6H5CH2-, and n is 1, 2 or 3, or (ii) a 5- to 8-membered alicyclic group containing one or two nitrogen atoms and directly attached to the amido nitrogen or attached by a C1-3 alkylene chain; and salts and esters thereof.

612910

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