公开(公告)号：EP2364304A1

公开(公告)日：2011-09-14

申请号：EP09763890.2

申请日：2009-11-06

申请人： ISTITUTO BIOCHIMICO NAZIONALE SAVIO s.r.l.

发明人： BRUFANI, Mario ,  MEDICI, Ilaria ,  MARINI BETTOLO, Rinaldo ,  MIGNECO, Luisa Maria ,  MARZELLA, Rolando ,  FIGLIOLA, Rocco ,  LA BELLA, Angela

IPC分类号： C07D339/04 ,  A61K31/385 ,  A61K31/5377 ,  A61P3/00 ,  A61K31/4535 ,  A61K31/496 ,  A61P35/00

CPC分类号： C07D339/04 ,  A61K31/385 ,  A61K31/4535 ,  A61K31/496 ,  A61K31/5377

摘要： The present invention concerns an enantiomer R of a compound of Formula (I), wherein X is -NH-R
1 or of Formula (V) or (VI), R
1 is -(CH
2 )
n -R
2 , R
2 is a linear, branched or cyclic C
1 C
6 aliphatic group, -O-(CH
2 )
n -CH
3, -NH-CO- (CH
2 )
n -CH
3, a 5- or 6-membered aliphatic or aromatic ring optionally comprising a heteroatom, a 5- or 6-membered aromatic ring substituted by one or two substituents, said substituents being selected from the group consisting of -OH, - O(alkyl C
1 C
3 ) and -OCO(alkyl C
1 C
3 ), or of Formula (V), R
3 is H or a C
1 -C
3 aliphatic group and R
4 is a linear C
1 -C
3 or a branched C
3 -C
12 aliphatic group, or R
3 is a C
1 -C
3 aliphatic group and R
4 is a linear C
1 -C
12 aliphatic group, Y is O, CH-(CH
2 )
n -CH
3 or N(CO)(CH
2 )
n -CH
3, and n is an integer from O to 6. It has been found that the enantiomers of the invention are able to release (R)- alpha-lipoic acid, ensuring a longer permanence in the body for the pharmacologically active principle than that obtainable by its direct administration, or to simulate the pharmacological action of alpha-lipoic acid itself, while exhibiting a much more intense and lasting activity.