Alpha-deuterated 2-alkylaminoacetamide derivatives having reduce

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Nitrogen containing other than solely as a nitrogen in an...

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5142375, 5142378, 5142388, 514255, 514313, 514330, 514331, 514423, 514426, 514428, 514594, 514616, 514620, 544164, 544168, 544382, 544390, 544400, 546224, 546226, 546232, 546244, A61K 3116, A61K 31165, A61K 3117, C07C23700

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active

050753371

ABSTRACT:
Deuterated 2-alkylaminoacetamide compounds are described having the alpha carbon of the alkyl side chain of the compounds substituted by one or two deuterium atoms. These compounds have pharmacokinetic properties which enable treatment of CNS diseases with lower toxic effects. These compounds are also useful in evaluating the metabolic fate of non-deuterated counterpart compounds. Of particular interest are compounds of Formula I: ##STR1## wherein X is deutero or hydrido; wherein R.sup.1 is selected from alkyl and aralkenyl; wherein each of R.sup.2 and R.sup.3 is independently selected from hydrido and alkyl; wherein each of R.sup.1, R.sup.2 and R.sup.3 having a substitutable position may be substituted with one or more halo radicals; or a pharmaceutically-acceptable salt thereof.

REFERENCES:
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M. I. Blake et al., J. Pharm. Sci., 64, 3, pp. 367-391 (1975).
A. B. Foster et al., Advances in Drug Research, vol. 14, pp. 2-36, Academic Press, London, (1985).
A. G. Goodman et al., Basis of Therapeutics, 7th Edn., p. 15, Mac Millan & Co., New York (1985).
P. L. Dostert et al., Med. Res. Rev., 9, 45-89 (1989).
L. E. Dyck et al., N. S. Arch. Pharm., 337, 279-283 (1988).

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