Spirocyclopropyl fluorenes as melatonergic agents

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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514530, 514534, 514538, 514595, 514624, 514625, 514627, 514629, 560 27, 560 28, 564 57, 564 60, 564189, 564190, 564204, 564219, 564220, 564222, A61K 3116, C07C23305

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06028112&

ABSTRACT:
There is provided novel spirocyclopropyl fluorene derivatives having the general Formula I ##STR1## wherein R, R.sup.1 and X are as defined herein which are useful as melatonergic agents.

REFERENCES:
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Arendt, J., et al., "Alleviation of Jet Lag by Melatonin: Preliminary Results of Controlled Double Blind Trial", Br. Med. J., 292, p. 1170 (May 1986).
Cassone, V. M., et al., "Dose-Dependent Entrainment of Rat Circadian Rhythms by Daily Injection of Melatonin", J. Biol. Rhythms, 1, (3), pp. 219-229 (1986).
Copinga, S., et al., "2-Amino-8-methoxytetralins: A Series of Nonindolic Melatonin-like-Agents", J. Med. Chem., 36, pp. 2891-2898 (1993).
Reppert, S. M., et al., "Cloning and Characterization of a Mammalian Melatonin Receptor That Mediates Reproductive and Circadian Responses", Neuron, 13, pp. 1177-1185(Nov., 1994).
Reppert, S. M., et al., "Molecular Characterization of a Second Melatonin Receptor Expressed in Human Retina and Brain: The Mel.sub.1b Melatonin Receptor ", Proc. Natl. Acad. Sci. USA, 92, pp. 8734-8738 (Sep. 1995).

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