C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
167/208, 260/279
C07D 405/04 (2006.01) A61K 31/40 (2006.01) A61K 31/445 (2006.01)
Patent
CA 1284150
Abstract The (3S,4R)-isomer of compounds of formula (I) optionally in admixture with up to 45% of the mixture by weight of the corresponding (3R,4S)-isomer: Image (I) wherein: one of R1 and R2 is hydrogen and the other is selected from the class of alkylcarbonyl, alkoxycarbonyl, alkylcarbonyloxy, alkylhydroxymethyl, nitro, cyano, chloro, trifluoromethyl, alkylsulphinyl, alkylsulphonyl, alkoxysulphinyl, alkoxysulphonyl, alkylcarbonylamino, alkoxycarbonylamino or aminosulphinyl, aminosulphonyl or aminocarbonyl, the amino moiety being optionally substituted by one or two alkyl groups, or alkylsulphinylamino, alkylsulphonyl- amino, alkoxysulphinylamino or alkoxysulphonylamino or ethylenyl terminally substituted by alkylcarbonyl, nitro or cyano, or -C(alkyl)NOH or -C(alkyl)NNH2, the alkyl groups or alkyl moieties of alkyl-containing groups having from 1 to 6 carbon atoms; one of R3 and R4 is hydrogen or alkyl having from 1 to 4 carbon atoms and the other is alkyl having from 1 to 4 carbon atoms, or R3 and R4 together are C2-5 polymethylene; R5 is hydrogen, alkyl having from 1 to 3 carbon atoms or acyl having from 1 to 8 carbon atoms; and n is 1 or 2, having pharmacological activity, in particular anti-hypertensive activity, a process for the preparation of such isomers, their pharmaceutical use and pharmaceutical compositions containing them.
450251
Faruk Erol
Beecham Group P.l.c.
Borden Ladner Gervais Llp
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