ISOXAZOLINE ALPHA 1a/1d ADRENORECEPTOR ANTAGONISTS

摘要

The present invention relates to isoxazolines (I) useful as selective aia/aid adrenoreceptor antagonists for the treatment of benign prostatic hypertrophy and/or lower urinary tract symptoms as well as to pharmaceutical compositions comprising said compounds, processes to prepare these compounds, and the use of these compounds as a?a/aid adrenoreceptor modulators in a method of treatment.(I) and a form thereof, wherein L is selected from the group consisting of-CH<SUB>2</SUB>-; -CO- and -CONH-; Het is heterocyclyl optionally substituted with one, two or three substituents selected from halo, nitro, oxo, C<SUB>1-6</SUB>alkyl, C<SUB>1-6</SUB>alkyloxy, C<SUB>1-6</SUB> alkyl-CO-, amino, amino mono-substituted with C<SUB>1-8</SUB>alkyl, amino di-substituted with C<SUB>1-6</SUB>alkyl, amino mono-substituted with ArC<SUB>1-6</SUB>alkyl, amino disubstituted with ArC<SUB>1-6</SUB>alkyl, Ar, Ar-CO, Ar-oxy, and Ar-SO2; Ar is selected from pyridinyl, phenyl and phenyl substituted with one or more substituents selected from halo, C<SUB>1-6</SUB>alkyl, and C<SUB>1-6</SUB>alkyloxy; with the proviso that 1-[[,5-dihydro-5-[[4-[2-(1- methylethoxy) phenyl]-1-piperazinyl]methyl]-3-isoxazolyl]methyl]-2-piperidone is not included