VPA-analogous antiepileptics

Details VPA-analogous antiepileptics VPA-analogous antiepileptics

1994-11-23

1998-07-28

Shippen, Michael L.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Radical -xh acid, or anhydride, acid halide or salt thereof...

562506, 562598, 562606, 554 1, 554223, 514558, 514560, 514578, 514572, A61K 3119

Patent

active

057863806

ABSTRACT:
The invention provides compounds which are effective antiepileptics and at the same time display only a slight sedative and teratogenic effect and have the formula ##STR1## where the compounds of the formulae (I) and (II) can also be mono- or polyunsaturated, in which R.sup.1, R.sup.2, R.sup.3 and R.sup.4 are each, independently of one another, hydrogen or a C.sub.1 -C.sub.6 -alkyl group, R.sup.5 is hydrogen or a C.sub.1 -C.sub.2 -alkyl group, and at least one of the radicals R.sup.1 to R.sup.4 in the compounds of the formulae (I) and (II) is different from hydrogen, where the compounds of the formula (I), in the case where a center of asymmetry is present on the carbon atom in position 2, and the compounds of the formulae (II), (III) and (IV) are in the form of their racemate, their pure enantiomers or a mixture of their enantiomers which differs from the racemate, and pharmaceutically compatible salts thereof.

REFERENCES:
patent: 3325361 (1967-06-01), Meunier
Haj-Yehia, Abdulla and Bialer, Meir (1990) J. Pharm. Sci. 79:8, 719-724 (Exhibit C).
Hauck and Nau (1989) Toxicol. Lett. 49:41-48 (Exhibit D).
Hauck and Nau (1991) Naturwissenschaften 78:272-274 (Exhibit E).
Hauck, et al. (1992) Toxicol. Lett. 60:145-153 (Exhibit F).
Nau, et al., (1981) J. Pharmacol. Exp. Ther. 219:768-777 (Exhibit I).
Nau, et al., (1991) Pharmacol. and Toxicol. 69:310-321 (Exhibit J).
Okada, Katsuhide, et al., (1980) Agric. Biol. Chem., 44(11), 2595-2599 (Exhibit K).
Wilson, Stephen R., (1993) Proc. Workshop Vitam. D., 6th(Vitam. D), 749-754, New York University, NY, NY 10003 (Exhibit L).
Kurth, Mark J. and Brown, Edward G., (1987) J. Am. Chem. Soc., 109(22), 6844-5 (Exhibit G).
Kurth, Mark J., et al., (1988) Tetrahedron Lett., 29(13), 1517-1520 (Exhibit H).
Wilson, Stephen R., (1993) Proc. Workshop Vitam. D., 6th(Vitam. D), 749-754, New York University, NY, NY 10003 (Exhibit L).

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