Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...
Patent
1993-06-11
1995-11-07
Bernhardt, Emily
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Having -c-, wherein x is chalcogen, bonded directly to...
544376, 544377, 549 29, 549 50, 549 51, 549 68, 549 79, A61K 31495, C07D49504, C07D40714, C07D40510
Patent
active
054648343
ABSTRACT:
New N-substituted N'-heterobicyclic piperazines corresponding to the general formula I: ##STR1## wherein: R represents: ##STR2## D represents a single bond, except when R represents naphthyl, or a hydrocarbon chain having 1 to 8 carbon atoms inclusive which is straight-chain or branched by a gem-dimethyl; and
A-B represents: --(CH.sub.2).sub.2 --O--, --(CH.sub.2).sub.3 --O--, or --CO--CH.dbd.CH--,
as well as their possible stereoisomers, epimers, and pharmaceutically-acceptable acid addition salts thereof; and medicinal products containing the same, useful in the treatment of a disorder requiring a 5-HT.sub.1A receptor antagonist.
REFERENCES:
patent: 3808212 (1974-04-01), Renth et al.
patent: 4335126 (1982-06-01), Kleeman et al.
patent: 4782061 (1988-11-01), Kruse et al.
patent: 5242925 (1993-09-01), Boettcher et al.
Francis, Cortical Pyramidal Neurone Loss May Cause Glutamatergic Hypoactivity and Cognitive Impairment in Alzeheimer's Disease: Investigative and Therapeutic Perspectives, Journal of Neurochemistry vol. 60, No. 5, 1589-1604, 1589 (1993).
Dijk, NMDA-Induced Glutamate Release From Rat Cortical Pyramidal Neurones is Potentiated by a 5-HT.sub.1A Antagonist, Br. J. Pharmacol. 112, 10P (May 1994).
Carli, 8-Hydroxy-2-(di-n-Propylamino)Tetralin Impairs Spatial Learning in a Water Maze: Role of Postsynaptic 5-HT.sub.1A Receptors, Br. J. Pharmacol. 105, 720-726 (1992).
Bowen, Circumscribed Changes of the Cerebral Cortex in Neuropsychiatric Disorders of Later Life, Proc. Natl. Acad. Sci. USA 86, 9504-9508 (1989).
Rodgers, Anxiolytic-like Effect of (S)-Way 100135, a 5-HT.sub.1A Receptor Antagonist, in the Murine Elevated Plus-Maze Test, European Journal of Pharmacology 261, 321-325 (1994).
Millan, 5-Hydroxytryptamine (HT).sub.1A Receptors and the Tail-Flick Response. II. High Efficacy 5-HT.sub.1A Agonists Attenuate Morphine-Induced Antinociception in Mice in a Competitive-Like Manner, Journal of Pharmacology and Experimental Therapeutics vol. 256, No. 3, 983-992 (1991).
Kellar, Stimulation of Serotonin.sub.1A Receptors Increases Release of Prolactin in the Rat, Neuropharmacology vol. 31, No. 7, 643-647 (1992).
Chaouloff, 5-HT.sub.1A and Alpha-2 Adrenergic Receptors Mediate the Hyperglycemic and Hypoinsulinemic Effects of 8-Hydroxy-2-(di-n-Propylamino)Tetralin in the Conscious Rat, Journal of Pharmacology and Experimental Therapeutics vol. 243, No. 3, 1159-1166 (1987).
Millan, S 14671: A Naphtylpiperazine 5-Hydroxytryptamine.sub.1A Agonist of Exceptional Potency and High Efficacy Possessing Antagonist Activity at 5-Hydroxytryptamine.sub.1C/2 Receptors, Journal of Pharmacology and Experimental Therapeutics 262 No. 2, 451-463 (1992).
Tricklebank, The Involvement of Subtypes of the 5-HT.sub.1 Receptor and of Catecholaminergic Systems in the Behavioral Response to 8-Hydroxy-2-(Di-n-Propylamino-)Tetralin in the Rat, European Journal of Pharmacology 106, 271-282 (1984).
Aulakh, Food Intake, Neuroendocrine and Temperature Effects of 8-OH-DPAT in the Rat, European Journal of Pharmacology 146, 253-259 (1988).
Millan, Induction of Hypothermia as a Model of 5-Hydroxytryptamine.sub.1A Receptor-Mediated Activity in the Rat: A Pharmacological Characterization of the Actions of Novel Agonists and Antagonists, Journal of Pharmacology and Experimental Therapeutics 264 No. 3, 1364-1376 (1993).
Millan, 5-Hydroxytryptamine (5-HT).sub.1A Receptors and the Tail-Flick Response. I. 8-Hydroxy-2-(Di-n-Propylamino)Tetralin HBr-Induced Spontaneous Tail-Flicks in the Rat as an in vivo Model of 5-HT.sub.1A Receptor-Mediated Activity, Journal of Pharmacology and Experimental Therapeutics 256 No. 3, 973-982 (1991).
Tricklebank, Mediation of the Discriminative Stimulus Properties of 8-Hydroxy-2-(di-n-propylamino)tetralin (8-OH-DPAT) by the Putative 5-HT.sub.1A Receptor, European Journal of Pharmacology 133, 47-56 (1987).
Eiden et al, Arch. Pharm. 322, pp. 589-592 (1989).
Goument Bertrand
Millan Mark
Peglion Jean-Louis
Rivet Jean-Michel
Adir et Compagnie
Bernhardt Emily
Heuschen Gordon W.
LandOfFree
N-substituted N'-heterobicyclic piperazines having pharmaceutica does not yet have a rating. At this time, there are no reviews or comments for this patent.
If you have personal experience with N-substituted N'-heterobicyclic piperazines having pharmaceutica, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and N-substituted N'-heterobicyclic piperazines having pharmaceutica will most certainly appreciate the feedback.
Profile ID: LFUS-PAI-O-197399