NANOPARTICULATE COMPOSITIONS AND FORMULATIONS OF PIPERAZINE COMPOUNDS

摘要

The present invention relates to storage stable nanoparticulate compositions of piperazine compounds. The pharmaceutical compositions comprising the nanoparticulate compositions that are useful for the treatment and prevention of proliferative diseases including cancer are also described.

主权项

1. A stable composition comprising:
(a) nanoparticles of compound of formula (1), or pharmaceutically acceptable salts thereof, wherein
X and Y are independently N or C—R7;for the combination of variables R1 and R2:
R1 is hydrogen, C1-C3 alkoxy, C1-C3 alkyl or halogen and R2 is F; orR1 is F and R2 is hydrogen, C1-C3 alkoxy, C1-C3 alkyl or halogen;R3 is C1-C3 alkyl; andR4, R5, R6 and R7 are independently H, C1-C6 alkoxy, C1-C6 alkyl, C1-C6 haloalkyl, C1-C6 alkylcarbonyl, cyano, nitro or halogen; and (b) at least one surface stabilizer, wherein the nanoparticles have an effective median particle size (D50) of less than about 1,000 nm.