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US 2002/0119965 A1Published application
Nitriloxy derivatives of (R) and (S)-carnitine
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsOreste Piccolo, Roberto Castagnani, Paolo De Witt
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Abstract
Carnitine derivatives of formula (I) are described in racemic and/or optically active form, as well as the process for their preparation and their use as pharmaceutical anti-angina active ingredients for the treatment of ischaemic heart disease. 1 Also described is a process for producing the (R)-carnitine enantiomer from (S)-carnitine (or vice versa), using the derivatives of formula (I).
Claims36
Formula (I) compounds in optically active form with absolute configuration (R) or (S)
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- where
- Y is an OR or NR1R2 group with
- R equal to hydrogen, C1-C10 all or alkyl substituted with C6-C10 aryl, said aryl optionally carrying one or more C1-C4 alkyls;
- R1 and R2, equal or different from one another, are hydrogen, C1-C10 alkyl or alkyl substituted with C6-C10 aryl, said aryl optionally carrying one or more C1-C4 aryls;
- or, taken together, form a 5-7 atom heterocyclic ring with the nitrogen atom;
- or Y is the residue of an esterified polyalcohol with at least one nitric acid equivalent;
- X− is the anion of a pharmaceutically acceptable organic or inorganic acid,
- or, if Y is an OH group, the formula (I) product may exist in the form of an inner salt, i.e. with formula (II)
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- and their enantiomerically enriched mixtures.
8 more elements
Dependencies are inferred from the claim text.