Patent · US Active

1-butyl-2-hydroxyaralkyl piperazine derivatives and the uses as anti-depression medicine thereof

US8252796B2 · kind B2 · utility

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2References
11Claims
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Key dates

Filing dateSep 29, 2009
Grant dateAug 28, 2012
Priority date
Expiry dateSep 29, 2029

Classification

  • Technology area (CPC C)Chemistry; Metallurgy
  • CPC primaryC07D295/092
  • WIPO fieldPharmaceuticals
  • WIPO sectorChemistry

Abstract

The invention discloses 1-butyl-2-hydroxyl aralkyl piperazine derivatives and their use as antidepressants. The derivatives of the present invention have triple inhibition effect on the reuptake of 5-HT, NA and DA, and can be administrated to the patients in need thereof in form of composition by route of oral administration, injection and the like. Compared with clinically currently used dual targets antidepressants (such as venlafaxine), said derivatives may have stronger antidepression effect, broader indications, faster onset and lower neurotoxicity and side reaction; and said derivatives have stronger antidepression activity, lower toxicity, higher bioavailability, longer half life and better druggablity, compared with aryl alkanol piperazine derivatives and optical isomers thereof disclosed in prior art. The 1-butyl-2-hydroxyl aralkyl piperazine derivative is the free alkali or its salt of a compound of formula below:

Source: USPTO / EPO open patent data. Objective bibliographic and citation counts.