C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 401/04 (2006.01) A61K 31/445 (2006.01)
Patent
CA 2251060
The invention relates to thalidomide prodrugs of the formula (I), in which R is -CHR1-NHR2 or -(CH2)n COOH, R1 is H or C1-4-alkyl, R2 is H, C1-3-alkyl, C(O)-CH2-NHR3 or an amino protective group, R3 is H or an amino protective group, and n is an integer between 2 and 4, in the form of their bases or salts of physiological acids. It also relates to a process for the preparation of said prodrugs and the use thereof as an active drug substance.
L'invention concerne des promédicaments de la thalidomide, de la formule (I), dans laquelle R représente -CHR<1>-NHR<2> ou bien -(CH2)nCOOH, R<1> représente H ou alkyle C1-C4, R<2> représente H, alkyle C1-C3, C(O)-CH2-NHR<3> ou un groupe protecteur amino, R<3> représente H ou un groupe protecteur amino, et n représente un nombre entier compris entre 2 et 4, sous forme de leurs bases ou sels d'acides physiologiques. L'invention concerne également un procédé de production de ces promédicaments et leur utilisation comme substance active médicamenteuse.
Akermann Michaela
Eger Kurt
Schneider Johannes
Winter Werner
Wnendt Stephan
Fetherstonhaugh & Co.
Grunenthal Gmbh
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