Patent ID: 6753442
Filing Date: 2004-06-22
Classification: A61P,C07C

Abstract:
A method for preparing a pharmaceutical formulation for oral administration comprising a compound of formula (I)Aâ€”X1â€”NO2â€ƒâ€ƒ(I) having a completely amorphous or partially amorphous form, said method comprising the following steps:admixing the compound of formula (I) with at least one excipient capable of at least partially amorphizing the compound; and at least partially amorphizing the obtained mixture; wherein in formula (I)A=R(COX) X=O, NH, NR1c, wherein R1c is a linear or branched C1-C10 alkyl, R is selected from the following radicals; wherein:R1 is a OCOR3 group; wherein R3 is methyl, ethyl or a linear or branched C3-C5 alkyl, or the residue of a saturated heterocyclic ring having 5 or 6 atoms, which can be aromatic or completely or partially saturated, said heterocyclic ring containing one or more heteroatoms independent selected from O and N and S; R2 is hydrogen, hydroxy, halogen, linear or branched C1-C4 alkyl, linear or branched C1-C4 alkoxyl; linear or branched C1-C4 perfluoroalkyl; mono- or di-(C1-C4) alkylamino; R1 and R2 together are the dioxymethylene group, with the proviso that when X=NH, then Y is ethylene and R2=H as defined hereunder; R1 cannot be OCOR3 in position 2 when R3 is methyl; nl is an integer and is 0 or 1; X1 is a bivalent linking bridge selected from the following YO: Y=linear or branched C1-C20 alkylene; or a substituted or unsubstituted C5-C7 cycloakylene; or X1 is selected from the following: wherein n3 is an integer from 0 to 3, n3â€² is an integer from 1 to 3; wherein n3 and n3â€² have the above mentioned meaning: wherein nfâ€² is an integer from 1 to 6; wherein R1f=H, CH3 and nfâ€² is as above defined.