The present invention relates to substituted cyclopropylamine derivs. of formula I and pharmaceutical compns. thereof, as KDM1 inhibitors useful in the prevention and/or treatment of cancer, infectious diseases, and aberrant cellular energy metab. disorders such as obesity. I [wherein R1 is heterocyclyl or heterocyclyl substituted by oxo, wherein the heterocyclyl is unsubstituted or substituted by one or more C1-C6 alkyl; R2 is hydrogen, halogen, C1-C6 alkyl, etc.] or stereoisomers or pharmaceutically salts thereof are claimed and exemplified. For example, 3-(benzyloxycarbonylamino)-4-(4-methylpiperazin-1-yl)benzoic acid underwent condensation with tert-Bu N-[trans-2-(4-aminophenyl)cyclopropyl]carbamate followed by BOC deprotection providing trans-II·2HCl. I were evaluated for inhibition for leukemia MV4-11 cell growth using a CellTiter-Flor® fluorescence assay from which II exhibited an IC50 value ≤ 5μM. Synthetic processes for the prepn. of I are also claimed. [on SciFinder(R)]
Preparation of cyclopropylamine derivatives as histone demethylase inhibitors / Vianello, Paola; Varasi, Mario; Mercurio, Ciro; Cappa, Anna; Meroni, Giuseppe; Villa, Manuela; Mai, Antonello; Valente, Sergio.. - (2014).
Preparation of cyclopropylamine derivatives as histone demethylase inhibitors
Mai, Antonello;Valente, Sergio.
2014
Abstract
The present invention relates to substituted cyclopropylamine derivs. of formula I and pharmaceutical compns. thereof, as KDM1 inhibitors useful in the prevention and/or treatment of cancer, infectious diseases, and aberrant cellular energy metab. disorders such as obesity. I [wherein R1 is heterocyclyl or heterocyclyl substituted by oxo, wherein the heterocyclyl is unsubstituted or substituted by one or more C1-C6 alkyl; R2 is hydrogen, halogen, C1-C6 alkyl, etc.] or stereoisomers or pharmaceutically salts thereof are claimed and exemplified. For example, 3-(benzyloxycarbonylamino)-4-(4-methylpiperazin-1-yl)benzoic acid underwent condensation with tert-Bu N-[trans-2-(4-aminophenyl)cyclopropyl]carbamate followed by BOC deprotection providing trans-II·2HCl. I were evaluated for inhibition for leukemia MV4-11 cell growth using a CellTiter-Flor® fluorescence assay from which II exhibited an IC50 value ≤ 5μM. Synthetic processes for the prepn. of I are also claimed. [on SciFinder(R)]I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
