Back to results
US 2001/0011074 A1Published application
Nitriloxy derivatives of (R) and (S)-carnitine
AssigneeSigma-Tau Industrie Farmaceutiche Riunite S.p.A.
InventorsOreste Piccolo, Roberto Castagnani, Paolo De Witt
Life of this patent
Estimating the term…
Abstract
New camitine derivatives of general 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 A further subject of the invention described herein is a process for producing the (R)-camitine enantiomer from (S)-carnitine (or vice versa), through the use of derivatives of general formula (I).
Claims36
Formula (I) compounds in optically active form with absolute configuration (R) or (S) 6
- where
- Y is an OR or NR1R2 group with
- R equal to hydrogen, C1-Clo alkyl 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) 7
- and their enantiomerically enriched mixtures.
7 more elements
Dependencies are inferred from the claim text.