C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/255, 260/300
C07D 405/04 (2006.01) C07D 405/14 (2006.01) C07D 413/04 (2006.01) C07D 417/04 (2006.01)
Patent
CA 1212946
Abstract Compounds o formula (I): Image (I) 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 alkoxysulphonyl, 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 beingoptionally substituted by one or two C1-6 alkyl groups, or C1-6 alkylsulphinylamino, C1-6 alkylsulphonylaminoC1-6 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 are C2-5 polymethylene; either R5 is hydrogen, hydroxy, C1-6 alkoxy or C1-8 acyloxy and R6 is hydrogen or R5 and R6 together are a bond; Q is O or S; m is an integer from 0 to 2 and n is an integer from 0 to 2 such that m+n is 1 or 2; X is O or S, or N-R7, R7 being hydrogen, C1-9 alkyl, C2-7 alkanoyl, phenylC1-4 alkyl, naphthylcarbonyl, phenylcarbonyl or benzylcarbonyl optionally substituted in the phenyl or naphthyl ring by one or two C1-6 alkyl, C1-6 alkoxy or halogen; mono- or bi-cyclicheteroarylcarbonyl; the lactam or thiolactam group being trans to the R5 group when R5 and R6 are not a bond; or, when one or the other of R1 and R2 is an amino or an amino-containing group, or when X is NR7 and R7 is hydrogen, a pharmaceutically acceptable salt or solvate thereof having anti-hypertensive activity, a process for their preparation and their use as pharmaceuticals.
439125
Ashwood Valerie A.
Evans John M.
Beecham Group P.l.c.
Borden Ladner Gervais Llp
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