Patent MY-119161-A (MY)
Title: Delta-amino-gamma-hydroxy-omega-aryl-alkanoic acid amides with enzyme especially renin inhibiting activities
Inventor: GOSCHKE RICHARD DR
IPC: C07D241/08
Filed: 1995-03-30
Abstract: ( )-AMINO-(GAMMA)-HYDROXY-( )-ARYL-ALKANOIC ACID AMIDES OF FORMULA I(FORMULA 1) WHEREIN R1 IS HYDROGEN, HYDROXY, LOWER ALKOXY, CYCYLOALKOXY, LOWER ALKOXY-LOWER ALKOXY OR FREE OR ESTERIFIED OR AMIDATED CARBOXY-LOWER ALKOXY, R2 IS HYDROGEN, LOWER ALKYL, CYCLOALKYL, LOWER ALKOXY-LOWER ALKYL, LOWER ALKOXY-LOWER ALKOXY-LOWER ALKYL, CYCLOALKOXY-LOWER ALKYL, HYDROXY, OPTIONALLY LOWER ALKANOYLATED, HALOGENATED OR SULFONYLATED HYDROXY-LOWER ALKOXY; AMINO-LOWER ALKYL THAT IS UNSUBSTITUTED OR SUBSTITUTED BY LOWER ALKYL, BY LOWER ALKANOYL AND/OR LOWER ALKOXYCARBONYL; OPTIONALLY HYDROGENATED HETEROARYL-LOWER ALKYL; AMINO-LOWER ALKOXY THAT IS SUBTITUTED BY LOWER ALKYL, BY LOWER ALKANOYL AND/OR BY LOWER ALKOXYCARBONYL; OXO-LOWER ALKOXY, LOWER ALKOXY, CYCYLOALKOXY, LOWER ALKENYLOXY, CYCLOALKOXY-LOWER ALKOXY, LOWER ALKOXY-LOWER ALKOXY, LOWER ALKOXY-LOWER ALKENYL, LOWER ALKENYLOXY-LOWER ALKOXY, LOWER ALKOXY-LOWER ALKENYLOXY, LOWER ALKENYLOXY-LOWER ALKYL, LOWER ALKANOYL-LOWER ALKOXY, OPTIONALLY S-OXIDISED LOWER ALKYL-THIO-LOWER ALKOXY, LOWER ALKYLTHIO-(HYDROXY)-LOWER ALKOXY, ARYL-LOWER ALKOXY, OPTIONALLY HYDROGENATED HETEROARYL-LOWER ALKOXY, CYANO-LOWER ALKOXY, FREE OR ESTERIFIED OR AMIDATED CARBOXY-LOWER ALKOXY OR FREE OR ESTERIFIED OR AMIDATED CARBOXY-LOWER ALKYL, R3 IS OPTIONALLY HALOGENATED LOWER ALKYL, LOWER ALKOXY-LOWER ALKYL, CYCLOALKYL-LOWER ALKYL, HYDROXY-LOWER ALKYL, OPTIONALLY S-OXIDISED LOWER ALKYLTHIO-LOWER ALKYL, OPTIONALLY HYDROGENATED HETEROARYLTHIO-LOWER ALKYL, OPTIONALLY HYDROGENATED HETEROARYL-LOWER ALKYL; AMINO-LOWER ALKYL THAT IS UNSUBSTITUTED OR N-MONO- OR N,N-DI-LOWER ALKYLATED, N-LOWER ALKANOYLATED OR N-LOWER ALKANESULFONYLATED OR N,N-SUBSTITUTED BY LOWER ALKYLENE, BY UNSUBSTITUTED OR N''''-LOWER ALKYLATED OR N''''-LOWER ALKANOYLATED AZA-LOWER ALKYLENE, BY OXA-LOWER ALKYLENE OR BY OPTIONALLY S-OXIDISED THIA-LOWER ALKYLENE; CYANO-LOWER ALKYL, FREE OR ESTERIFIED OR AMIDATED CARBOXY-LOWER ALKYL, CYCLOALKYL, ARYL, HYDROXY, LOWER ALKOXY, CYCLOALKYL, LOWER ALOKOXY-LOWERALKOXY, CYCYLOALKYL-LOWER ALKOXY, HYDROXY-LOWER ALKOXY, ARYL-LOWER ALKOXY, OPTIONALLY HALOGENATED LOWER ALKOXY, OPTIONALLY S-OXIDISED LOWER ALKYLTHIO-LOWER ALKOXY, OPTIONALLY HYDROGENATED HETEROARYL-LOWER ALKOXY,OPTIONALLYHYDROGENATED HETEROARYLTHIO-LOWER ALKOXY; AMINO-LOWER ALKOXY THAT IS UNSUBSTITUTED OR N-MONO- OR N,N-DI-LOWER ALKYLATED, N-LOWER ALKANOYLATED OR N-LOWER ALKANESULFONYLATED OR SUBSTITUTED BY LOWER ALKYLENE, BY UNSUBSTITUTED OR N''''-LOWER ALKYLATED OR N''''-LOWER ALKANOYLATED AZA-LOWER ALKYLENE, BY OXA-LOWER ALKYLENE OR BY OPTIONALLY S-OXIDISED THIA-LOWER ALKYLENE; CYANO-LOWER ALKOXY OR FREE OR ESTERIFIED OR AMIDATED CARBOXY-LOWER ALKOXY, OR TOGETHER WITH R4 IS LOWER ALKYLENEDIOXY OR A FUSED-ON BENZO OR CYCLOHEXENO RING, R4 TOGETHER WITH R3 IS LOWER ALKYLENEDIOXY OR A FUSED-ON BENZO OR CYCLOHEXENO RING, OR IS HYDROGEN, LOWER ALKYL, HYDROXY, LOWER ALKOXY OR CYCLOALKOXY, X IS METHYLENE OR HYDROXYMETHYLENE, R5 IS LOWER ALKYL OR CYCLOALKYL, R6 IS UNSUBTITUTED OR N-MONO- OR N,N-DI-LOWER ALKYLATED OR N-LOWER ALKANOYLATED AMINO, R7 ISLOWER ALKYL, LOWER ALKENYL, CYCLOALKYL OR ARYL-LOWER ALKYL, AND R8 IS LOWER ALKYL, CYCYLOALKYL, FREE OR ALIPHATICALLY ESTERIFIED OR ETHERIFIED HYDROXY-LOWER ALKYL; AMINO-LOWER ALKYL THAT IS UNSUBSTITUTED OR N-LOWER ALKONYLATED OR N-MONO- OR N,N-DI-LOWER ALKYL ALKYLATED OR N,N-DISUBSTITUTED BY LOWER ALKYLENE, BY HYDROXY-, LOWER ALKOXY- OR LOWER ALKONYLOXY-LOWER ALKYLENE, BY UNSUBSTITUTED OR N''''-LOWER ALKONYLATED OR N''''-LOWER ALKYLATED AZA-LOWER ALKYLENE, BY OXA-LOWER ALKYLENE OR BY OPTIONALLY S-OXIDISED THIA-LOWER ALKYLENE; FREE OR ESTERIFIED OR AMIDATED CARBOCY-LOWER ALKYL, FREE OR ESTERIFIED OR AMIDATED DICARBOXY-LOWER ALKYL, FREE OR ESTERIFIED OR AMIDATED CARBOXY-(HYDROXY)-LOWER ALKYL, FREE OR ESTERIFIED OR AMIDATED CARBOXYCYCLOALKYL-LOWER ALKYL, CYANO-LOWER ALKYL, LOWER ALKANESULFONYL-LOWER ALKYL, UNSUBSTITUTED OR N-MONO- OR N,N-DI-LOWER ALKYLATED THIOCARBAMOYL-LOWER ALKYL, UNSUBSTITUTED OR N-MONO- OR N,N-DI-LOWER ALKYLATED SULFAMOYL-LOWER ALKYL, OR A HETEROARYL RADICAL BONDED VIA A CARBON ATOM AND OPTIONALLY HYDROGENATED AND/OR OXOSUBSTITUTED, OR LOWER ALKYL SUBSTITUTED BY A HETEROARYL RADICAL BONDED VIA A CARBON ATOM AND OPTIONALLY HYDROGENATED AND/OR OXO-SUBSTITUTED, AND THE SALTS THEREOF, HAVE RENIN-INHIBITING PROPERTIES AND CAN BE USED AS ANTIHYPERTENSIVE MEDICINAL ACTIVE INGREDIENTS.