4-acylaminobenzopyrans

C - Chemistry – Metallurgy – 07 – D

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260/356, 260/358

C07D 311/68 (2006.01) C07D 311/70 (2006.01)

Patent

CA 1250850

ABSTRACT Compounds of formula (I): (I) Image wherein: either one of R1 and R2 is hydrogen and the other is selected from the class of C1-6 alkylcarbonyl, C1-6 alkoxycarbonyl, C1-6 alkylcarbonyloxy, C1-6 alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, C1-6 alkylsulphinyl, C1-6 alkylsulphonyl, C1-6 alkoxysulphinyl, C1-6 aikoxysulphonyl, C1-6 alkylcarbonylamino, C1-6 alkoxycarbonylamino, C1-6 alkyl-thiocarbonyl, C1-6 alkoxy-thiocarbonyl, C1-6 alkyl-thiocarbonyloxy, C1-6 alkyl-thiolmethyl, formyl or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylamino C1-6 alkoxysulphinylamino or C1-6 alkoxysulphonylamino or ethylenyl terminally substituted by C1-6 alkylcarbonyl, nitro or cyano, or -C(C1-6 alkyl)NOH or -C(C1-6 alkyl)NNH2, or one of R1 and R2 is nitro, cyano or C1-3 alkylcarbonyl and the other is methoxy or amino optionally substituted by one or two C1-6 alkyl or by C2-7 alkanoyl; - 2 - one of R3 and R4 is hydrogen or C1-4 alkyl and the other is C1-4 alkyl or R3 and R4 together with the carbon atom to which they are attached are C2-5 polymethylene; either R5 is hydroxy, C1-6 alkoxy or C2-7 acyloxy and R6 is hydrogen or Rs and R6 together are a bond; R7 is hydrogen C1-6 alkyl optionally substituted by hydroxy, C1-6 alkoxy, C1-6 alkoxycarbonyl or carboxy, or C1-2 alkyl substituted by halogen, or C2-6 alkenyl; R8 is hydrogen or C1-6 alkyl; and X is oxygen or sulphur; the R8-N-CX-R7 group being trans to the R5 group when R5 and R6 together are not a bond; or, when one or the other of R1 and R2 is an amino or an amino-containing group, a pharmaceutically acceptable salt thereof having anti-hypertensive activity.

428501

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