C - Chemistry – Metallurgy – 07 – D
Patent
C - Chemistry, Metallurgy
07
D
C07D 273/02 (2006.01) A61K 31/16 (2006.01) A61K 31/395 (2006.01) A61P 35/00 (2006.01) C07D 273/01 (2006.01) C07D 498/04 (2006.01)
Patent
CA 2677874
The present invention relates to a compound of Formula (I), its geometrical isomers, in an optically active form as enantiomers, diastereomers, as well as in the form of racemate, as well as pharmaceutically acceptable salts thereof, wherein R is selected from CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 and CF3for the preparation of a medicament, in particular for for selectively inducing terminal differentiation of neoplastic cells and thereby inhibiting proliferation of such cells, for inducing differentiation of tumor cells in a tumor, for inhibiting the activity of histone deacetylase and for the treatment of primary cancer or secondary cancer.
La présente invention porte sur un composé de Formule (I), sur ses isomères géométriques, dans une forme optiquement active comme énantiomères, diastéréisomères ainsi que dans la forme de racémates, ainsi que sur leurs sels pharmaceutiquement acceptables. Dans la formule, R est choisi parmi CONHOH, CONHCH2SH, CONHCH2SCOCH3, SH, SCOCH3, SCH3, N(OH)COH, COCONHCH3 et CF3 pour la préparation d'un médicament, en particulier pour induire de façon sélective une différenciation terminale de cellules néoplasiques et, de ce fait, pour inhiber la prolifération de telles cellules, pour induire une différenciation de cellules tumorales dans une tumeur, pour inhiber l'activité de l'histone désacétylase et pour le traitement d'un cancer primaire ou d'un cancer secondaire.
Auzzas Luciana
Cabri Walter
Giannini Giuseppe
Hanessian Stephan
Pisano Claudio
Fetherstonhaugh & Co.
Sigma-Tau Industrie Farmaceutiche Riunite S.p.a.
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