RU96112103A - NEW BENZOILGUANIDINES, THEIR RECEPTION AND APPLICATION IN MEDICINES - Google Patents

Claims (8)

1. The compounds of formula (I)

where A is one of the groups of formulas

R ₁ - group R'-SO ₂ - or R'-NH-SO ₂ -, where R 'means alkyl with 1-5 carbon atoms, unsubstituted or substituted by halogen or phenyl, unsubstituted or mono-, di- or trisubstituted by residues, selected from the group consisting of halogen, alkyl with 1-4 carbon atoms, alkoxy with 1-4 carbon atoms, fluorine, chlorine or trifluoromethyl;
R ₂ - radical of formulas

wherein

which may be the same or different, means hydrogen, alkyl with 1-4 carbon atoms, or

can also mean phenyl, benzyl and cycloalkyl with 3-7 carbon atoms;
R ₅ and R ₆ , which may be the same or different, are hydrogen, methyl, methoxy, hydroxyl or halogen;
R ₇ is hydrogen, alkyl with 1-4 carbon atoms, benzyl or benzyloxy;
R ₈ and R ₉ , which may be the same or different, are hydrogen, alkyl with 1-4 carbon atoms, phenyl or halogen;
R ₁₀ is hydrogen or alkyl with 1-6 carbon atoms, which may be substituted by phenyl, unsubstituted or substituted by methyl, methoxy or halogen;
R ₁₁ and R ₁₂ , which may be the same or different, mean hydrogen, methyl, methoxy, phenyl, benzyl, nitro, cyano, halogen, trifluoromethyl, amino, group NR ₁₀ R ₁₃ , 1-pyrrolidinyl, 1-pyrazolinyl, 1- imidazolidinyl, 1-piperidinyl, 1-piperazinyl or carbamoyl, while R ₁₁ may also mean a fused benzene ring that may have up to three substituents selected from the group comprising methyl, methoxy, halogen, trifluoromethyl and cyano;
R ₁₃ is hydrogen, alkyl with 1-4 carbon atoms, which may be substituted by phenyl, phenoxy or benzyloxy, or halogen;
E and G, which may be the same or different, denote nitrogen or a CH group;
m = 2, 3, 4, 5 or 6;
n = 0 or 1;
p - 2, 3 or 4,
moreover, the compounds of formula (I) may be present as bases or salts and, if necessary, in the form of individual stereoisomers or cis or trans isomers or mixtures thereof. 2. The compounds of formula (I), where the radical R ₂ means the residue of formula II '-

which may be the same or different, means hydrogen or alkyl with 1 to 3 carbon atoms. 3. The compounds of formula (I), where R ₂ means the residue of formula (XI), E or G means nitrogen. 4. The compounds of formula (Ia), where R ₂ and A have the above values.  5. Drug, different content of the compound in PP.1 - 4, along with the usual excipients and / or carriers.  6. The use of compounds according to PP.1 - 4 in the process of obtaining drugs.  7. The use of compounds on PP. 1 - 4 as antihypertensive, mucolytic, diuretic and carcinostatic substances for the treatment of diseases associated with ischemia, cerebral infarction, acute or chronic circulatory disorders of the brain, for cardioprotection and to prevent violations of the transplant. 8. The method of producing compounds in PP.1 - 4 conventional methods, characterized in that a) the compound of formula (XVI)

where R ₁ has the above meaning,
subjected to interaction with the amine of the formula (XVII)
R ₂ - A - H (XVII),
moreover, R ₂ and A have the above values,
or b) the compound of formula (XVIII)

where R ₁ has the above meaning, and A 'means a group A, which is linked to R ₂ through a nitrogen atom, as is the case in formulas (II'), (III ') and (IV')),
subjected to interaction with the compound of the formula (XIX)

or c) a compound of formula (XX)

where R ₁ and R ₂ have the above values, and R means a lower alkyl radical,
subjected to interaction with guanidine, and, if necessary, the resulting products are divided into sterically different forms and / or, if necessary, the resulting base is converted into salts with acids or the resulting salt is converted into free bases.