RU97102152A - SULPHONAMIDE DERIVATIVES OF AZOLONES, ACTING AGAINST HELICOBACTER - Google Patents

Claims (1)

1. The compound of formula I

their pharmaceutically acceptable acid addition salts and stereochemically isomeric forms,
where Y is CH or N;
R ¹ , R ² and R ³ each independently represents hydrogen or C _1-4 alkyl;
R ⁴ and R ⁵ each independently represents hydrogen, halogen, C _1-4 alkyl, C _1-4 alkyloxy, hydroxy, trifluoromethyl, trifluoromethyloxy or difluoromethyloxy;
R ⁶ is C _1-4 alkyl or phenyl, optionally substituted with halogen, C _1-4 alkylcarbonylamino, C _1-4 alkyloxy, C _1-4 alkyl or nitro;
Z is C = O or CHOH; and

is a radical of the formula

2. The compound according to claim 1, wherein R ¹ , R ₃ and R ₅ are hydrogen; R ² is C _1-4 alkyl; R ⁴ is halogen; and Y represents N. 3. The compound according to claim 2, wherein R ² is ethyl; R ⁶ is C _1-4 alkyl; and

is a radical of formula (a-1) or (a-2).  4. The compound according to claim 1, characterized in that said compound is 1- [5- [2- [1 - [(4-chlorophenyl) hydroxymethyl] propyl] -2,3-dihydro-3-oxo-4H- 1 , 2,4-triazol-4-yl] -2-pyridinyl] -4- (methylsulfonyl) piperazine, its pharmaceutically acceptable acid addition salt and stereochemically isomeric form.  5. A pharmaceutical composition comprising a therapeutically effective amount of a compound according to any one of claims 1 to 4 and a pharmaceutically acceptable carrier.  6. A method of obtaining a pharmaceutical composition according to claim 5, characterized in that a therapeutically effective amount of the compound according to any one of paragraphs. 1-4 are homogeneously mixed with a pharmaceutically acceptable carrier.  7. The compound according to any one of claims 1 to 4 as a medicine.  8. Therapeutic combination, comprising the compound according to any one of paragraphs. 1-4, a pharmaceutically acceptable bismuth compound and / or a proton pump inhibitor. 9. The method of obtaining the compounds of formula I

where R ¹ , R ² , R ³ , R ⁴ , R ⁵ , R ⁶ , X, Y, Z and

characterized in that
a) conduct the interaction of the intermediate compounds of formula (II) with a reagent of formula (III) in a reaction-inert solvent, optionally in the presence of a base;

b) N-alkylation of the intermediate of formula (V) with a reagent of formula (VI) is carried out in a suitable solvent and in the presence of a suitable base;

and further, if this is desirable, by converting the compounds of formula (1) into each other, according to known methods for transforming functional groups; converting compounds of formula (1) to an acid addition salt by exposure to a pharmaceutically acceptable acid; or, conversely, the conversion of salt into the free base by exposure to alkali; and / or the manufacture of their stereochemically isomeric forms.