C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
260/314, 260/496
C07D 233/64 (2006.01) A61K 31/16 (2006.01) A61K 31/205 (2006.01) C07D 233/58 (2006.01)
Patent
CA 1167453
ABSTRACT "Carnitinamides of optically active aminoacids and process for preparing same" Amides of carnitine or acyl-carnitines having general formula Image wherein X- is a halogen anion, e.g. the chloride anion R is either hydrogen or an acyl radical, such as acetyl, propionyl or butyryl; and Y is the residue of an optically active esterified amino-acid (e.g. the residue of L-phenylglycine methyl ester, Image are prepared by either (a) directly condensing D,L-carnitine (or acyl-D,L-carnitine) with an ester of an optically active aminoacid, or (b) preparing the acid halogenide of D,L- carnitine or acyl-D,L-carnitine and subsequently condensing it with an ester of an optically active aminoacid. The mixture of the diastereoisomer amides thus obtained is resolved by fractional crystallization from organic solvents into the respective separated diastereoisomers. These optically active amides are useful therapeutic agents for treating cardiac disorders, hyperlipidaemias and hyperlipoproteinaemias and, furthermore, can be hydrolyzed with procedures known per se into L-carnitine and D-carnitine, respectively.
368952
de Witt Paolo
Tinti Maria O.
Gowling Lafleur Henderson Llp
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a
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