ARYL AND HETEROARYLETHYLACTYLGUANIDINE, PREPARING AND USING THEM IN THERAPY Russian patent published in 2012 - IPC C07D295/14 C07D211/58 C07D401/12 C07D295/18 C07D239/26 C07D213/38 C07D279/22 C07D213/82 C07D231/12 C07D213/74 C07D307/14 C07D207/14 C07D211/46 C07D235/08 C07D241/08 A61K31/4427 A61K31/4523 A61K31/506 A61K31/5377 A61K31/496 A61K31/4709 A61P9/00 

FIELD: medicine, pharmaceutics.

SUBSTANCE: invention refers to a compound of formula (I)

wherein: A means a ring selected from phenyl group or heteroaryl group, Q means oxygen atom or a link -CH₂-, X, Y and Z mean carbon atoms; R1 and R2, identical or different are selected from the following atoms and groups: hydrogen, halogen, -CF₃, (C1-C6)alkyl, Alk, (C1-C6)alkoxy, (C1-C6)alkyl-O-(C1-C6)alkyl, -(CH₂)_m-SO₂-(C1-C6)alkyl with m equal to 0, 1 or 2, benzyl, pyrazolyl, -CH₂-triazolyl and -L-R12 wherein L represents a link or a bridge -CH₂- and/or -CO- and/or -SO₂-, and R12 means (C3-C8)cycloalkyl or group of formula ,

wherein: n=0 or 1, R13 means one-three groups, identical or different, selected from hydrogen atom and hydroxyl, (C1-C4)alkyl, oxo and phenyl, R14 means hydrogen atom or is selected from groups - NR18R19, -NR18-COOR19, -NR18-Alk-R20 and -R21, wherein R18, R19, R20, R21 and Alk have the values as specified below, R14' means -CO-(C1-C6)alkyl, R15 is selected from groups -Alk, -R20, -Alk-R20, -Alk-R21, -CO-Alk, -CO-R20, -CO-R21, -Alk-CO-NR18R19, (C3-C8)cycloalkyl and -CO-(C3-C8)cycloalkyl, wherein R18, R19, R20, R21 and Alk has the values as specified below, R16 means hydrogen atom or group Alk, wherein Alk has the values as specified below, R17 means group -Alk, -Alk-R20 or -Alk-R21, wherein Alk, R20 and R21 have the values as specified below, -CO-(C1-C6)alkyl, -CO-(C3-C8)cycloalkyl, R18 and R19, identical or different, mean hydrogen atom or (C1-C6)alkyl, R20 means phenyl or heteroaryl group (such as pyridinyl, pyrazolyl, pyrimidinyl or benzimidazolyl), which is optionally substituted by one (C1-C6)alkyl, R21 means heterocycloalkyl group optionally substituted by one or more halogen atoms or (C1-C6)alkyl, hydroxyl or (C1-C4)alkoxy groups, and Alk means (C1-C6)alkyl which is linear or branched and which is optionally substituted by one or two groups, identical or different, selected from hydroxyl, phenyl, (C1-C4)alkoxy and -NR18R19, wherein R18 and R19 have the values as specified above, R3 means linear (C1-C10)alkyl which is optionally substituted by one-three groups, identical or different, selected from halogen atoms and (C1-C4)alkoxy groups, R4 means hydrogen atom, R5 and R6 independently mean hydrogen atom or (C1-C5)alkyl, R7 and R8 independently mean hydrogen atom or (C1-C5)alkyl, R9 and R10 independently mean hydrogen atom, or R9 and R10 together form linear (C2-C3)alkylene chain, thereby forming 6-merous ring with nitrogen atom whereto attached with said alkylene chain optionally substituted by one-three groups selected from (C1-C4)alkyl, oxo, R11 means hydrogen atom or (C1-C8)alkyl which is optionally substituted by one-three groups selected from halogen atoms, hydroxyl, (C1-C6)alkoxy, -NR18R19, - or pyridinyl, wherein R18 and R19 have the values as specified above; wherein 'heterocyclic group' means saturated 5- or 6-member ring containing one or two heteroatoms selected from oxygen, nitrogen and sulphur atoms; 'heteroaryl group' means aromatic cyclic group containing 5-11 ring atoms selected from carbon, nitrogen and sulphur atoms with heteroaryl groups to be monocyclic or bicyclic, in this case at least one of two cyclic fragments are aromatic; in the form of a free base or an additive acid salt or base. Also, the invention refers to methods for preparing such compounds and to a based drug showing rennin inhibitory activity.

EFFECT: compounds can find application in medicine for preparing the drug for treating and preventing hypertension, cardiac damages, myocardial infraction, cardiac failure, cardiac and vascular hypertrophy, left ventricular dysfunction, restenosis, glaucoma, renal conditions, diabetic complications.

26 cl, 3 tbl, 18 ex