FIELD: chemistry.
SUBSTANCE: invention relates to new compounds with general formula I, 
in which R1 represents hydrogen or a group, which forms a biologically labile ester, R2 represents hydrogen, C1-C4-alkyl or C1-C4-hydroxyalkyl, and R3 represents C1-C4-alkyl; C1-C4-alkoxy-C1-C4-alkyl; C1-C4-hydroxyalkyl, which is optionally substituted with a second hydroxy group and all hydroxy groups of which are optionally esterified with C2-C4-alkanoyl or amino-acid residue; (C0-C4-alkyl)2amino-C1-C6-alkyl; C3-C7-cycloalkyl; C3-C7-cycloalkyl-C1-C4-alkyl; phenyl-C1-C4-alkyl, the phenyl group of which is optionally substituted 1-2 times with C1-C4-alkyl, C1-C4-alkoxy group and/or halogen; naphthyl-C1-C4-alkyl; C3-C6-oxoalkyl; phenylcarbonylmethyl, the phenyl group of which is optionally substituted 1-2 times with C1-C4-alkyl, C1-C4-alkoxy group and/or halogen, or 2-oxoazepanyl, or R2 and R3 together represent C4-C7-alkylene, methylene groups of which are optionally substituted 1-2 times with carbonyl, nitrogen, oxygen and/or sulphur and/or optionally substituted once with a hydroxy group, which is optionally esterified with C2-C4-alkanoyl or amino-acid residue; C1-C4-alkyl; C1-C4-hydroxyalkyl, the hydroxy group of which is optionally esterified with C2-C4-alkanoyl or amino-acid residue; phenyl or benzyl, and R4 represents hydrogen or a group, which forms a biologically labile ester, where R1 and R4 groups are independently chosen from C1-C4-alkyl; C1-C4-alkoxy-C1-C4-alkoxy-C1-C4-alkyl; C3-C7-cycloalkyl; C3-C7-cycloalkyl-C1-C4-alkyl; N,N-di-(C0-C4-alkyl)amino-C1-C6-alkyl; phenyl or phenyl-C1-C4-alkyl, optionally substituted 1 or 2 times in the phenyl ring with halogen, C1-C4-alkyl or C1-C4-alkoxy group or C1-C4-alkylene chain, bonded with two neighbouring carbon atoms; dioxolanylmethyl, optionally substituted in the dioxolane ring with C1-C4-alkyl; C1-C6-alkanoyloxy-C1-C4-alkyl, optionally substituted in the oxy-C1-C4-alkyl group with C1-C4-alkyl; 1-[[(C1-C4-alkyl)carbonyl]oxy]C1-C4-alkyl esters; 1-[[(C4-C7 cycloalkyloxy)carbonyl]oxy]C1-C4-alkyl esters, 2-oxo-1,3-dioxolan-4-yl-C1-C4-alkyl esters, which optionally contain a double bond in the dioxolane ring; 2-oxo-1,3-dioxolan-4-ylmethyl; and to physiologically compatible salts of acids with formula I and/or to physiologically compatible acid-additive salts of formula I compounds. The invention also relates to a pharmaceutical composition, to use of formula I compounds in paragraph 1, to a method of obtaining formula I compounds, as well as to compounds with general formula II.
EFFECT: obtaining new biologically active compounds, with inhibitory activity towards neutral endopeptidase, endothelin converting enzyme and soluble human endopeptidase.
20 cl, 80 ex, 9 tbl
| Title | Year | Author | Number |
|---|---|---|---|
| PHARMACEUTICAL COMPOSITIONS INCLUDING NEP (NEUTRAL ENDOPEPTIDASE) INHIBITORS, INHIBITORS OF ENDOGENOUS ENDOTHELIN-PRODUCING SYSTEM AND HMG (HYDROXYMETHYLGLUTARYL) CoA REDUCTASE INHIBITORS | 2005 |
|
RU2410118C2 |
| PHARMACEUTICAL COMPOSITIONS, INCLUDING NEP INHIBITORS, INHIBITORS OF SYSTEM PRODUCING ENDOGENIC ENDOTHELIUM AND DIURETICS | 2006 |
|
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| CONDENSED TRICYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY | 2014 |
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| TETRAHYDROBENZIMIDAZOLE DERIVATIVES AS TNF ACTIVITY MODULATORS | 2014 |
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| NEW CONDENSED PYRIMIDINE COMPOUND OR SALT THEREOF | 2017 |
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| IMIDAZOTRIAZINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY | 2014 |
|
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| PURINE DERIVATIVES AS TNF ACTIVITY MODULATORS | 2014 |
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RU2684644C1 |
| IMIDAZOPYRIDINE DERIVATIVES AS MODULATORS OF TNF ACTIVITY | 2014 |
|
RU2695664C1 |
| PHARMACEUTICAL COMPOSITIONS CONTAINING NEP-INHIBITORS, INHIBITORS OF ENDOGENOUS ENDOTHELIN-PRODUCING SYSTEM AND AT-RECEPTOR ANTAGONISTS | 2005 |
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RU2384346C2 |
| INHIBITORS OF NEUTRAL ENDOPEPTIDASE (NEP) HUMAN SOLUBLE ENDOPEPTIDASE (hSEP) FOR PREVENTION AND TREATMENT OF NEURODEGENERATIVE DISORDERS | 2005 |
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RU2362563C2 |
