Semicarbazones having CNS activity and pharmaceutical preparatio

Details Semicarbazones having CNS activity and pharmaceutical preparatio Semicarbazones having CNS activity and pharmaceutical preparatio

1995-06-07

1998-04-21

Lambkin, Deborah

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Nitrogen containing other than solely as a nitrogen in an...

564 36, A61K 31175, C07C28114

Patent

active

057418187

ABSTRACT:
A compound of general formula I below useful as an anticonvulsant for disorders of the central nervous system: ##STR1## wherein: R.sup.1, R.sup.2, R.sup.3 and R.sup.4 may be the same or different and each represents a hydrogen or halogen atom, or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl, cyano, C.sub.1-9 alkoxy or C.sub.6-10 aryloxy group; R.sup.5 represents a hydrogen atom or a C.sub.1-9 alkyl, C.sub.3-9 cycloalkyl or C.sub.6-10 aryl group; and X is oxygen or sulfur; or a pharmaceutically-acceptable salt thereof. The compound may be adimistered orally for treating convulsions in humans or animals.

REFERENCES:
patent: 3139458 (1964-06-01), Paquette
patent: 3300484 (1967-01-01), Pappo
patent: 3303214 (1967-02-01), Anderson et al.
patent: 3304323 (1967-02-01), Fonken et al.
patent: 3392171 (1968-07-01), Fonken et al.
patent: 3558654 (1971-01-01), Bamford et al.
patent: 3712914 (1973-01-01), Tilles
patent: 4015011 (1977-03-01), Schromm et al.
patent: 4394514 (1983-07-01), Kruse
patent: 4454337 (1984-06-01), Kruse
Chemical Abstract 50 4836 (1956).
Genzo Ito: Diesen Bulletin, 5 397 (1957)*.
Dimmock et al (I)., J. Med. Chem. 1993 36, pp. 2243-2252.
Krall et al "Antiepileptic drug development: II Anti-convulsant drug screening"-Epilepsia 1978, 19 409-428.
Yeager et al: Synthesis, 1991, pp. 63-68.
Racine: Electroencephalogr. Clin. Neurophysiol., 1972, 32, 281-294.
Skeen et al: Soc. Neurosci., 1990, 16(1) 307.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014745 see BRN 254223 & J. Org. Chem., vol. 26, 1961, pp. 2353-2355.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014746 see BRN 1890700, 3400167, 3400193, 3410343, 3419487, 341220, 3436628 & Bull. Soc. Chim. Fr., 1954. pp. 644, 646.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014747 see BRN 3396690 & Yakugaku Zasshi, vol. 72, 1952, p. 300.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014748 see BRN 3389800 & J. Chem. Soc., 1942, p. 347, 353.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014749 & J. Amer. Chem. Soc., vol. 65, 1943, p. 1736, 1738.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014750 see BRN 3422330, 3449771 & Yakugaku Zasshi, vol. 73, 1953, p. 243.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP 02014751 see BRN 3382967 & J. Amer. Chem. Soc., vol. 58, 1936, p. 1808, 1810.
Database Crossfire. Beilstein Informationsgesellschaft GmbH. XP002014752 see BRN 3347507 & Yakugaku Zasshi, vol. 57, 1937, p. 36, 37.
European Journal of Medicinal Chemistrychimica Therapeutica., vol. 26, No. 5, 1991, Paris Fr, pp. 529-534, XP002014742, J.R. Dimmock et al.: "Evaluation of the thiosemicarbazones of some aryl alkyl ketones and related compounds for anticonvulsant activities" cited in the application, see whole document; especially scheme 1, compound 1n; p. 531, table I. (II).
Pharmazie, vol. 46, No. 7, 1991, Berlin De, pp. 538-539, XP002014743 J.R. Dimmock et al.: "Evaluation of some mannich bases of 1-aryl-1-ethanones and related ketones for anticonvulsant activities" p. 539, copound 2f. (III).
Eur J. Med. Chem. (1995), 30(4), 287-301, XP002014744, Dimmock, J.R. et al: "Some aryl semicarbazones possessing anticonvulsant activities." IV.
Synthesis, No. 1, 1991, Stuttgart De, pp. 63-68, XP002014786 G.W. Yeager et al.: "A convient method for the preparation of 4-aryloxyphenols." p. 65, right-hand column, line 8 -line 24.

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