ARYLCARBONYLPIPERAZINES AND HETEROARYLCARBONYLPIPERAZINES FOR TUMOUR TREATMENT (VERSIONS), MEDICATION (VERSIONS), METHOD OF OBTAINING AND METHOD OF TUMOUR TREATMENT Russian patent published in 2008 - IPC C07D241/06 C07D403/06 C07D405/06 C07D413/06 C07D417/06 A61K31/497 A61K31/495 A61P35/04 

Abstract RU 2335496 C2

FIELD: chemistry; medicine.

SUBSTANCE: invention concerns aryl- or heteroarylcarbonylpiperazine compound of the general formula (I) , where R1 is selected out of the group including fluorene-9-on, isoxazole, cinnoline, isothiazole, isoquinoline, 9H-fluorene, 9H-xanthene and 1H-pyrazole, where linkage is implemented by any desired and possible end atom of heteroaryl or aryl radical, so that they can optionally be unsubstituted or mono- or disubstituted by substitutes: halogen, SO2-alkyl, saturated alkyl, non-saturated alkyl with one double link, halogenalkyl where alkyl part contains 1 to 20 carbon atoms, phenyl optionally mono- or disubstituted by substitutes: NO2, -OH, -NH2, halogen; R2 is O; R3 is H; R4 is phenyl substituted by one or two substitutes selected out of group: OH, halogen, alkyl, alkoxy, where alkyl part contains 1 to 20 carbon atoms; or 5, 6 or 7-atom cyclic aromatic radical including N heteroatom and substituted by alkyl containing 1 to 20 carbon atoms; m and n are 1; or its physiologically acceptable salt. The invention also concerns method of obtaining compound of the formula (I), application of compounds of the formula (I) as therapeutically effective compounds for obtaining medication for human and animal tumour treatment, medical preparations based on compound of the formula (I), method of obtaining medications and method of benignant and malignant tumour treatment. The compounds inhibit tubulin polymerisation, thus enabling their application for indicated purpose.

EFFECT: improved efficiency.

15 cl, 2 tbl, 19 ex

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RU 2 335 496 C2

Authors

Baasner Sil'Ke

Gerlakh Matias

Gjunter Ehkkhard

Mjuller Gil'Bert

Polimeropulos Ehmmanuehl'

Shmidt Peter

Ehmig Peter

Dates

2008-10-10Published

2003-06-20Filed