N-SUBSTITUTED HETEROCYCLIC DERIVATIVES OR THEIR SALTS, INTERMEDIATE DERIVATIVES OF PYRIMIDINE AND IMIDAZOLINE AND A PHARMACEUTICAL COMPOSITION BASED ON THE SUBSTITUTED HETEROCYCLIC DERIVATIVES Russian patent published in 1997 - IPC

Abstract RU 2099331 C1

FIELD: organic chemistry. SUBSTANCE: product: N-substituted heterocyclic derivatives of the formula (I) given in description where R1 and R2 are similar or different and each means independently hydrogen or group taken among C1-C4-alkyl, cyano, tetrazolyl, methyltetrazolyl, methylsulfonylamino, trifluoromethylsulfonylamino, trifluoromethylsulfonylaminomethyl, N-cyanoacetamide, N-hydroxyacetamide, N-[(4-carboxy)-1,3-thiazole-2-yl]-acetamide, ureido, 2-cyanoguanidinecarbonyl, 2-cyanoguanidinemethyl, 1-imidazolylcarbonyl, 3-cyano-2-methylisothioureidomethyl at condition that at least one of substituents R1 and R2 is distinct from hydrogen; R3 means hydrogen, (C1-C6)-alkyl that can be free or substituted with one or some halogen atoms, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl, phenyl, (C1-C3)-phenylalkyl; R4 and R5 each means independently (C1-C6)-alkyl, phenyl being alkyl and phenyl were not substituted or substituted with one or some halogen atoms or a single group of (C1-C4)-perfluoroalkyl; R4 and R5 together form group of the formula CR7R8 where R7 means hydrogen and R8 - phenyl; or R4R5 combined together mean group of the formula (CH2)n where n = 3-11; if this group is cyclohexane it can be substituted with (C1-C4)-alkyl or phenyl; or group (CH2)pY(CH2)q where p = q = 2; -y - HR6; R6 - acetyl, COF3,COC6H5, residue of Arg, Asp, Cys or Ile; or R4 and R5 combined together with carbon atom to which they bound form indan or adamantane; X means oxygen or sulfur atom; Z and t = 0 or one of their = 0 and another = 1; or their salts and intermediate compounds - derivatives of pyrimidine and imidazoline and pharmaceutical composition containing compound (I) as an active component at effective amount. The synthesized compounds show antagonistic effect with respect to angiotensin-II and can be used in medicine for treatment of cardiovascular illnesses. EFFECT: improved method of synthesis. 11 cl

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RU 2 099 331 C1

Authors

Klod Bernar[Fr]

Zhan-Klod Brel'Er[Fr]

Zhak Kleman[Fr]

Dino Nisato[It]

P'Er Perro[Fr]

Dates

1997-12-20Published

1991-11-19Filed