Hexa- and octahydro-pyrido[1,2-a]pyrazine derivatives with...

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

Reexamination Certificate

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Details

C544S333000, C544S335000, C544S349000

Reexamination Certificate

active

10946176

ABSTRACT:
The invention relates to hexahydro-pyrido[1,2-a]pyrazine derivatives having interesting neurokinin-NK1receptor antagonistic activity. The invention also relates to methods for the preparation of these compounds, to pharmaceutical compositions containing a pharmacologically active amount of at least one of these compounds as an active ingredient, as well as to the use of these compositions for the treatment of disorders in which neurokinin receptors are involved. The invention relates to compounds represented by the general formula (1)wherein the symbols have the meanings as given in the description.

REFERENCES:
patent: 6284757 (2001-09-01), Sanner
patent: 0 655 442 (1995-05-01), None
patent: 1125112 (1968-08-01), None
patent: WO 03/084955 (2003-10-01), None
Al-Dabbagh and Smith, “Species differences in oxidative drug metabolism: some basic considerations.” Archives of toxicology. Supplement. Archiv fur Toxikologie. supplement, vol. 7, pp. 219-231 (1984).
Hans Bundgaard, Design of Prodrugs, p. 1. © 1985 Elsevier Science Publishers.
Richard B. Silverman, The Organic Chemistry of Drug Design and Drug Action, pp. 352-400. © 1992 Academic Press, Inc.
Humphrey, J.M. “Medicinal Chemistry of Selective Neurokinin-1 Antagonists” Current Topics in Medicinal Chemistry, vol. 3(12), pp. 1423-1435 (2003).

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