SUBSTITUTED DERIVATIVES OF PYRAZOLE CONDENSED WITH SIX-MEMBERED HETEROCYCLIC RINGS, MEDICINAL AGENT

FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention describes derivatives of pyrazole of the general formula (I): ^ ^ wherein R1 represents aromatic 6-membered heterocyclyl comprising up to 2 heteroatoms taken among nitrogen (N) representing pyrimidinyl that can be substituted up to...

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Hauptverfasser: DEMBOVSKI KLAUS, FOJRER AKHIM, SHTASH JOKHANES-PETER, PERTSBORN EHLIZABET, KHJUTTER JOAKHIM, SHTAL' EHL'KE, ALONSO-ALIJA KRISTINA, SHTRAUB ALEKSANDER
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Sprache:eng ; rus
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Zusammenfassung:FIELD: organic chemistry, medicine, pharmacy. ^ SUBSTANCE: invention describes derivatives of pyrazole of the general formula (I): ^ ^ wherein R1 represents aromatic 6-membered heterocyclyl comprising up to 2 heteroatoms taken among nitrogen (N) representing pyrimidinyl that can be substituted up to 2 times with similar or different residue taken among the group (i) involving amino-, hydroxy-group, alkoxycarbonyl comprising up to 6 carbon atoms, cyano-group, halogen atom, phenyl or linear alkyl comprising up to 6 carbon atoms that, in turn, can comprise linear acyl or acylamino-group as substituents and each of that comprises, respectively, up to 5 carbon atoms; and at least with one residue among the group (ii) involving imidazolyl, morpholinyl, piperidinyl, piperazinyl, pyrrolidinyl, triazolyl, pyrrolyl, thiomorpholinyl, S-oxothiomorpholinyl and S,S-dioxothiomorpholinyl and that can be substituted once with 1,4-dioxa-8-azaspiro[4.5]decane residue, and/or substituted with cyano-group, linear alkyl, acyl or alkoxycarbonyl each of that comprises, respectively, up to 6 carbon atoms and alkyl can be substituted with linear alkoxy-group comprising up to 3 carbon atoms; or R1 represents purine residue that can be substituted with halogen atom, methyl; R2 and R3 in the presence of double bond form 6-membered aromatic heterocyclyl comprising 1 heteroatom nitrogen taken among pyridine; A represents phenyl substituted with halogen atom. Invention describes medicinal agent eliciting properties of stimulating agent of soluble guanylate cyclase and containing compound of the formula (I). Invention provides preparing medicinal agents used for treatment of cardiovascular diseases. ^ EFFECT: valuable medicinal properties of compounds. ^ 6 cl, 5 tbl, 2 dwg, 109 ex