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Title:
カテコールアミンのプロドラッグとしてのフェニルエチルアミンおよび縮合環のヴァリアント(variant)、ならびにその使用
Document Type and Number:
Japanese Patent JP2004500426
Kind Code:
A
Abstract:
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.

Inventors:
Vixtrem, Hokan
Dijkstra, Durk
Fenheyes, Bastien, Johann
Application Number:
JP2001576014A
Publication Date:
January 08, 2004
Filing Date:
April 17, 2001
Export Citation:
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Assignee:
Axon Biochemicals B.F.
International Classes:
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): C07C225/14; A61K31/13; A61K31/451; A61K31/473; A61P9/04; A61P9/12; A61P13/12; A61P15/10; A61P25/14; A61P25/16; A61P25/18; C07D211/32; C07D221/08; C07D221/10; C07D221/18
Attorney, Agent or Firm:
Takashima Ichi