发明名称 Phenylethylamines and condensed rings variants as prodrugs of catecholamines, and their use
摘要 Compounds of the general formula I wherein 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 is different from dimethylamino, N-methyl-N-ethylamino, N-methyl-N-propynyl-amino, N-methyl-N-propylamino and N-hydroxipropyl-N-methylamino, and salts thereof with pharmaceutically acceptable acids or bases are disclosed as well as the use of such compounds for the manufacturing of pharmaceutical compositions for the treatment of Parkinson's disease, psychoses, Huntington's disease, impotence, renal failure, heart failure or hypertension, such pharmaceutical compositions and methods of treating Parkinson's disease and schizophrenia.
申请公布号 US2004138281(A1) 申请公布日期 2004.07.15
申请号 US20030737782 申请日期 2003.12.18
申请人 AXON BIOCHEMICALS B V 发明人 WIKSTROM HAKAN;DIJKSTRA DURK;VENHUIS BASTIAAN JOHAN
分类号 A61K31/13;A61K31/451;A61K31/473;A61P9/04;A61P9/12;A61P13/12;A61P15/10;A61P25/14;A61P25/16;A61P25/18;C07C225/14;C07C225/20;C07D211/32;C07D211/70;C07D221/08;C07D221/10;C07D221/14;C07D221/18;(IPC1-7):A61K31/13;A61K31/403 主分类号 A61K31/13
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