Synthesis of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives displaying combined alpha2-adrenoceptor antagonistic and 5-HT reuptake inhibiting activities |
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| Authors: | Andrés J Ignacio Alcázar Jesús Alonso José M De Lucas Ana I Iturrino Laura Biesmans Ilse Megens Anton A |
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| Affiliation: | Johnson & Johnson Pharmaceutical Research and Development, Division of Janssen-Cilag, Medicinal Chemistry Department, Toledo, Spain. iandres@prdes.jnj.com |
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| Abstract: | ![]()
Following a program searching for dual 5-HT reuptake inhibitors and alpha(2)-adrenoceptor antagonists started at Johnson & Johnson Pharmaceutical Research & Development, we now report on the synthesis of a series of 7-amino-3a,4-dihydro-3H-[1]benzopyrano[4,3-c]isoxazole derivatives, some of which proved to be the most potent alpha(2)-adrenoceptor blockers within this chemical class of tricyclic isoxazolines, while keeping potent 5-HT reuptake inhibiting activity. |
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