1-[M-CARBOXAMIDO(HETERO)ARYL-METHYL]-HETEROCYCLYL-CARBOXAMIDE DERIVATIVES

FIELD: chemistry.SUBSTANCE: invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocyclyl-carboxamide compounds of formula (I)(I), in which Arrepresents a phenylene group or a 5- or 6-member heteroarylene group, which is a 5-6 member monocyclic or bicyclic aromatic ring containing from one...

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Hauptverfasser: PFAJFER Tomas, LEEMBRE Fransua, GERRI Filipp, FRETTS Khajnts, KIMMERLEN Terri, VALDENER Anya, GUDE Markus
Format: Patent
Sprache:eng ; rus
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Zusammenfassung:FIELD: chemistry.SUBSTANCE: invention relates to 1-[m-carboxamido(hetero)aryl-methyl]-heterocyclyl-carboxamide compounds of formula (I)(I), in which Arrepresents a phenylene group or a 5- or 6-member heteroarylene group, which is a 5-6 member monocyclic or bicyclic aromatic ring containing from one to a maximum of four heteroatoms, each of which is independently selected from oxygen, nitrogen and sulfur; wherein -CHR- and -NH-CO-X-Rgroups in Formula (I) are joined in a meta-arrangement to ring carbon atoms Ar; wherein said phenylene or a 5- or 6-member heteroarylene is independently unsubstituted or monosubstituted, wherein the substituent is selected from a group consisting of (C)alkyl, (C)alkoxy, halogen, (C)fluoroalkyl and (C)fluoroalkoxy; X is * direct bond; * -(C)alkylene- which is optionally monosubstituted, wherein the substituent is hydroxy; * -(C)cycloalkylene-; * -CH-O-, whereby oxygen is bonded to R; or * -CH=CH-; Rrepresents * aryl or 5-10 member heteroaryl, which represents a 5-10 member monocyclic or bicyclic aromatic ring containing from one to a maximum of four heteroatoms, each of which is independently selected from oxygen, nitrogen and sulfur; wherein said aryl or 5-10 member heteroaryl is independently unsubstituted, mono-, di- or trisubstituted, wherein the substituents are independently selected from a group consisting of (C)alkyl; (C)alkoxy; (C)fluoroalkyl; (C)fluoroalkoxy; halogen; cyano; (C)cycloalkyl; -CO-(C)alkoxy; -SO-(C)alkyl; and -NRR, wherein Rand Rare independently hydrogen or (C)alkyl, or Rand Rtogether with the nitrogen atom, to which they are attached form a 5- or 6-member ring selected from pyrrolidinyl, morpholinyl, piperidinyl and piperazinyl, optionally substituted on the free nitrogen atom with (C)alkyl; where if the 5-10 member heteroaryl is pyridine, then such a pyridine may additionally be present in the form of a corresponding N-oxide; * or, if X is a direct bond or a methylene group, Rin addition, can be a > partially aromatic bicyclic ring system consisting of a phenyl ring, which is fused with a 4-6 member saturated carbocyclic ring optionally containing one or two heteroatoms independently selected from nitrogen and oxygen; wherein said ring system is optionally mono- or disubstituted with (C)alkyl or halogen; > (C)cycloalkyl, the cycloalkyl optionally having a ring oxygen atom, and wherein said cycloalkyl is optionally substituted with up to four methyl groups; * or, if X is a direct bond, Rin addition, can