Methanesulfonate salts of antipsychotic benzofuran derivatives

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Heterocyclic carbon compounds containing a hetero ring...

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514307, 514320, 514337, 514338, 514414, 544376, 546148, 546196, 5462541, 548454, C07D40506, A61K 31495

Patent

active

056818360

ABSTRACT:
The methanesulfonate salt of a class of antipsychotic compounds comprising antagonists of dopamine receptor subtypes within the brain, being extremely potent antagonists of the human dopamine D.sub.4 receptor subtype and having a selective affinity for the D.sub.4 subtype over other dopamine receptor subtypes, possess advantageous qualities in terms of their improved aqueous solubility relative to the corresponding free base and, as such, provide for greater ease of formulation and display enhanced pharmacokinetic properties, including oral absorption.

REFERENCES:
Zagurerskii, et al., Chemical Abstracts, vol. 120, No. 11, ABS. No. 124908t, (1994), "Derivatives of 2-aryl-3-(3-amioethylbenzofuran with neurotropic activity".
Chemical Abstracts, vol. 93, No. 7, ABS. No. 71429c, (1980), Prewysz-Kowinto A., et al., "Synthesis of 3-aminomethyl derivatives of 2-carbethoxy benzofuran".

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