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Method of treating memory disorders using R-enantiomers of N-propargyl-aminoindan compounds
| Details |
Inventors: Youdim, Moussa B. H.; Finberg, John P. M.; Levy, Ruth; Yellin, Haim;
Assignee: Teva Pharmaceutical Industries Ltd. (Jerusalem, IL); Technion Research and Development Foundation, Ltd. (Haifa, IL)
Primary Examiner: Burn; Brian M.
Assistant Examiner:
Attorney, Agent or Firm: White; John P.
R(+)-N-propargyl-1-aminoindan, its preparation and use and pharmaceutical compositions containing it. The novel compound was found to be useful for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type (DAT), depression and the hyperactive syndrome. |
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DETAILED DESCRIPTION OF THE INVENTION The present invention thus provides as a novel compound the R(+)-enantiomer of N-propargyl-1-aminoindan [R(+)PAI] of the formula (I): ##STR1## and pharmaceutically acceptable acid addition salts thereof.
The present invention also relates to the preparation of R(+)PAI, to pharmaceutical compositions comprising the compound R(+)PAI together with suitable carriers and to the use of R(+)PAI for the treatment of human patients for Parkinson's disease, memory disorders, dementia of the Alzheimer type and hyperactive syndrome.
The R(+)PAI may be obtained by optical resolution of racemic mixtures of R and S-enantiomer of PAI.
Such a resolution can be accomplished by any conventional resolution method, well known to a person skilled in the art, such as those described in "Enantiomers, Racemates and Resolutions" by J.
Jacques, A.
Collet and S.
Wilen, Pub.
John Wiley & Sons, N.
Y.
, 1981.
For example, the resolution may be carried out by preparative chomatography on a chiral column.
Another example of a suitable resolution method is the formation of diastereomeric salts with a chiral acid such as tartaric, malic, mandelic acid or N-acetyl derivatives of aminoacids, such as N-acetyl leucine, followed by recrystallisation to isolate the diastereomeric salt of the desired R enantiomer.
The racemic mixture of R and S enantiomers of PAI may be prepared, e.
g.
as described in GB 1,003,676 and GB 1,037,014.
The racemic mixture of PAI can also be prepared by reacting 1-chloroindan or 1-bromoindan with propargylamine.
Alternatively, this racemate may be prepared by reacting propargylamine with 1-indanone to form the corresponding imine, followed by reduction of the carbon-nitrogen double bond of the imine with a suitable agent, such as sodium borohydride.
In accordance with this invention, the R enantiomer of PAI, can also be prepared directly from the optically active R-enantiomer of 1-aminoindan by reaction with propargyl bromide or propargyl chloride, in the presence of an organic or inorganic base and optionally in the presence of a suitable solvent
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Gene Therapy 
