SUBSTITUTED CHROMAN-6-YLOXY-CYCLOALKANES AND USE THEREOF AS MEDICAMENTS Russian patent published in 2018 - IPC C07D311/60 C07D405/12 C07D407/12 C07D407/14 C07D409/12 C07D413/12 C07D417/12 C07D417/14 C07F9/09 A61K31/353 A61P9/00 

Abstract RU 2666350 C2

FIELD: medicine; pharmaceuticals.

SUBSTANCE: invention relates to a compound of formula I in any of its stereoisomeric forms or a mixture of stereoisomeric forms in any ratio, or pharmaceutically acceptable salts thereof, which have the property of inhibiting sodium-calcium exchange (NCX). In formula I, Ar is phenyl which is unsubstituted or contains one or more identical or different substituents R0; R0 is selected from a group comprising halogen, (C1-C6)-alkyl, (C1-C6)-alkyl-O-, (C3-C7)-cycloalkyl-O- and (C3-C7)-cycloalkyl-(C1-C4)-alkyl-O-; R1 is hydrogen or one or more identical or different substituents selected from a group comprising fluorine and (C1-C4)-alkyl; R2 is selected from a group comprising (C1-C6)-alkyl, HO-, (C1-C6)-alkyl-C(O)-O-, Het1-C(O)-O-, R5-N(R6)-, R7-C(O)-N(R8)-, R7-S(O)2-N(R8)-, R9-N(R10)-C(O)-N(R8)- and R5-N(R6)-C(O)-, where (C1-C6)-alkyl is unsubstituted or contains one or more identical or different substituents R20; R3 is selected from a group comprising hydrogen and (C1-C6)-alkyl, where (C1-C6)-alkyl is unsubstituted or contains one or more identical or different substituents selected from phenyl; or groups R2 and R3 together are an oxo group; R4 is hydrogen or one or more identical or different substituents selected from a group comprising halogen and (C1-C4)-alkyl; R5 and R6 are independently selected from a group comprising hydrogen, (C1-C6)-alkyl, (C2-C6)-alkenyl, (C3-C7)-cycloalkyl, Het1 and Het2, where (C1-C6)-alkyl is unsubstituted or contains one or more identical or different substituents R20, and (C3-C7) -cycloalkyl and Het2 are all unsubstituted or contain one or more identical or different substituents R21, and phenyl and Het1 are all unsubstituted or contain one or more identical or different substituents R22; R7 is selected from a group comprising (C1-C6)-alkyl, (C3-C7)-cycloalkyl, phenyl, Het1 and Het2; R8 is selected from hydrogen; R9 is selected from (C1-C6)-alkyl; R10 is selected from hydrogen and (C1-C6)-alkyl; R20 is selected from a group comprising R24, fluoro, HO-, (C1-C6)-alkyl-O-, (C3-C7)-cycloalkyl-O-, (HO)2P(O)-O-, (C1-C6)-alkyl-S(O)n-, (C3-C7)-cycloalkyl-S(O)n-, R31-N(R32)-, R33-C(O)-N(R32)-, (C1-C6)-alkyl-S(O)2-N(R32)-, R31-N(R32)-C(O)-, R34-O-C(O)- and R31-N(R32)-S(O)2-; R21 is selected from (C1-C4) -alkyl, fluorine, HO- and oxo groups; R22 is selected from halogen, (C1-C4)-alkyl, HO- and oxo groups; R24 is a 3–6 membered ring containing 0–4 identical or different heteroatoms selected from nitrogen, oxygen and sulphur; R33 is selected from (C1-C6)-alkyl; R31, R32, R34 are selected from hydrogen and (C1-C6)-alkyl; Het1 is a 5–6 membered aromatic heterocycle containing 1 to 3 heteroatoms selected from nitrogen, oxygen and sulphur; Het2 is a 4 to 6 membered heterocycle containing 1 or 2 heteroatoms selected from nitrogen, oxygen and sulphur; n is selected from 0, 1 and 2; p and q are selected from 0 and 1. Invention also relates to a pharmaceutical composition and the use of said compounds for the preparation of a medicament for inhibiting NCX. .

EFFECT: substituted chroman-6-yloxy-cycloalkanes and use thereof as medicaments are disclosed.

13 cl, 3 tbl, 306 ex

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RU 2 666 350 C2

Authors

Chekhtitskij Verngard

Ueston Dzhon

Rakelmann Nils

Kraft Folker

Arndt Petra

Virt Klaus

Gegelyajn Khajnts

Rittseler Olaf

Dates

2018-09-07Published

2014-03-07Filed