Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use

USRE43244E1 · kind E1 · reissue

Assignee

• H. LUNDBECK A/S · DK

Inventors

• Hakan V. Wikstrom · Mölndal, SE
• Durk Dijkstra · Bedum, NL
• Bastiaan Johan Venhuis · Groningen, NL

Key dates

• Filing date: Nov 12, 2010
• Grant date: Mar 13, 2012
• Expiry date: Nov 12, 2030

Classification

• Technology area (CPC —): General

Abstract

Compounds of the general formula Iwherein rings B, C, D and E may be present or not and, when present, are combined with A as A+C, A+E, A+B+C, A+B+D, A+B+E, A+C+E, A+B+C+D or A+B+C+D+E, rings B, C and E being aliphatic whereas ring D may be aliphatic or aromatic/heteroaromatic, and wherein X is —(CH2)m—, in which m is an integer 1-3, to form a ring E or, when E is absent, a group R1 bound to the nitrogen atom, wherein R1 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 3 carbon atoms, cycloalkyl(alkyl) groups of 3 to 5 carbon atoms (i.e. including cyclopropyl, cyclopropylmethyl, cyclobutyl and cyclobutylmethyl) and wherein Y is —(CH2)n—, in which n is an integer 1-3, to form a ring C or when C is absent, a group R2 bound to the nitrogen atom, wherein R2 is selected from the group consisting of a hydrogen atom, alkyl or haloalkyl groups of 1 to 7 carbon atoms, cycloalkyl(alkyl) groups of 3 to 7 carbon atoms, alkenyl or alkylnyl groups of 3 to 6 carbon atoms, arylalkyl, heteroarylalkyl having 1 to 3 carbon atoms in the alkyl moiety, whilst the aryl/heteroaryl nucleus may be substituted, provided that when rings B, C, D and E are absent NR1R2…