Optically active 5H-pyrrolo[3,4-b]pyrazine derivative, its...

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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Reexamination Certificate

active

06864257

ABSTRACT:
Dextrorotatory isomer of 6-(5-chloro-2-pyridyl)-5-[(4-methyl-1-piperazinyl)carbonyloxy]-7-oxo-6,7-dihydro-5H-pyrrolo[3,4-b]pyrazine, its preparation and pharmaceutical compositions containing it which are usable as tranquillisers and hypnotics.

REFERENCES:
patent: 3862149 (1975-01-01), Cotrel et al.
patent: 4220646 (1980-09-01), Cotrel et al.
patent: 4868214 (1989-09-01), Sunshine et al.
patent: 4962124 (1990-10-01), Sunshine et al.
patent: 5102890 (1992-04-01), Bourzat et al.
patent: 5331000 (1994-07-01), Young et al.
patent: 5786357 (1998-07-01), Young et al.
patent: 6319926 (2001-11-01), Cotrel et al.
patent: 6436936 (2002-08-01), Young et al.
patent: 0 495 717 (1992-07-01), None
patent: WO 9310788 (1993-06-01), None
H. Tamura, et al, “Chronic Oral Toxicity Study of Zopiclone (27 267 RP) in Beagle dogs for 6 Months and Recovery Testing After Treatment,”Pharmacometrics, 26(6): 969-1003 (1983).*
Unpublished summary data sheet from IND Serial No. 000, (s)-zopiclone, owned by assignee Sepracor Inc., p. 8-108 (1 page total).*
Nair N.P.V., Schwartz G., Dimitri R. et al. A dose-range finding study of zopiclone in insomniac patients.Intl Clin Psychopharmacol1990; 5 (Suppl 2): 1-10.
Martindale. The Extra Pharmacopoeia. The Royal Pharmaceutical Society, London 1996; 31stedition: pp. 743-744.
Houghton G. W., Dennis M.J., Templeton R., Martin B.K. A repeated dose pharmacokinetic study of a new hypnotic agent, zopiclone (Imovane®).Intl J Clin Pharmacol Therap Toxicol1985, 23: 97-100.
Marc-Auréle J., Caille G., Bourgoin J. Comparison of zopiclone pharmacokinetics in patients with impaired renal function and normal subjects. Effects of hemodialysis.Sleep1987; 10(Suppl 1): 22-26.
Parker G., Roberts C.J.C.. Plasmas concentrations and central nervous system effects of the new hypnotic agent zopiclone in patients with chronic liver disease.Br J Clin Pharmacol1983; 16:259-265.
Viron B., De Meyer M., Le L'iboux A. et al., Steady-state pharmacokinetic of zopiclone during multiple oral dosing (7.5 mg nocte) in patients with severe chronic renal failure.Intl Clin Pysychopharmacol1990; 5 ( Suppl 2): 95-104.
Sikdar S., Ruben S.M., Zopiclone abuse among polydrug users.Addition1996; 91: 285-286.
Noble S., Langtry H.D., Lamb H.M., Zopiclone. An update of its pharmacology, clinical efficacy and tolerability in the treatment of Insomnia.Drugs198; 55:277-302.
Femandez C., Martin C., Gimenez F., Farinotti. Clinical pharmacokinets of zopiclone,Clin Pharmacokinet1995; 29: 431-441.
Le Liboux Z., Frydman A., Gaillot J., Simultaneous Determination of Zopicione and Its Two Major Metabolites (N-Oxide and N-Desmethyl) in Human Biological Fluids by Reversed-Phase High-Performance Liquid Chromatography,J. Chromatography, 417: (1987) 151-158.
Musch B. and Maillard F., Zopiclone, The Third Generation Hypnotic: a Clinical Overview,Intl. Clin. Psychopharmacol. 5:147-58 (1990).
Julou L., Blanchard J.C., and Dreyfus J.F., Pharmacological and Clinical Studies of Cyclopyrrolones: Copiclone and Suriclone,Pharmacol., Biochem.&Beh., 23: 653-659 (1985).
Broadhurst A. and Cushnaghan R.C., Residual effects of Zopiclone (Imovane),Sleep, 10 (Suppl. 1): 48-53 (1987).
Anderson A., Zopiclone and Nitrazepam: A Multicenter Placebo Controlled Comparative Study of Efficacy and Tolerance In Insomniac Patients in General Practice,Sleep, 10 (Suppl. 1): 54-62 (1987).
Tamminen T. and Hensen P.P., Chronic Administration of Zopiclone and Nitrazepam in the Treatment of Insomnia,Sleep, 10 (Suppl. 1): 63-72 (1987).
Inman W., Kubota K., Pearce G., Wilton W., PEM Report No. 10. Zopiclone,Pharmacoepidemiol Drug Safety1993; 2: 499-521.
Doble A., Canton T., Malgouris C., et al. The mechanism of action of zopiclone.Eur Psychiat1995; 10 (Suppl 3): 117s-128s.
Karle J. and Nielsen M., The Mechanism of Action and Pharmacology of Zopiclone, Rev. Contemp. Pharmacother., vol. 9, No. 2, pp. 77-87 (1998).
Richards G., Schoch P., Haefely W., Benzodiazepine receptors: new vistas.Sem Neurosci1991; 3: 191-203.
Doble A., Martin I.L.,The GABAA/benzodiazepine receptor as a target for psychoactive drugs, RG Landes Company, Austin 1996; pp. 229-264.
Langtry H.D., Benfield P., Zolpidem: A review of its pharmacodynamic and pharmacokinetic properties and therapeutic potential,Drugs, 1990; 40: 291-313.
Blanchard J.C., Boireau A., Garret C., Julou L. In vitro and in vivo Inhibition by zopiclone of benzodiazepine binding to rodent brain receptors.Life Sci1979; 24: 2417-2420.
Möhler H., Okada T. The benzodiazepine receptor in normal and pathological human brain.Brit J Psychiat1978; 133: 261-268.
Gaillot J., Le Roux Y., Houghton G.W., Dreyfus J.F.. Critical factors for pharmacokinetics of zopiclone ii the elderly and in patients with liver and renal Insufficiency.Sleep1987; 10 (Suppl 1): 7-21.
Doble et al., “The Pharmacology of Cyclopyrrolone Derivatives Acting at the GABAA/Benzodiazepine Receptor,”Adv. Biochem. Psychopharmacol., 47:407-418 (1992).
Gaillot et al., “Pharmacokinetics and Metabolism of Zopiclone,”Int. Pharmacophysiol. 17:suppl. 2, pp. 76-91 (1982)/Pharmacology 27:suppl. 2, pp. 76-91 (1983).
E.J. Ariens, “Stereoselectivity in Pharmacodynamics and Pharmacokinetics,”Schweiz. Med. Wschr. 120:131-134 (1990).
Dragstedt, C.A. and Lang, V.F., “Respiratory Stimulants In Acute Cocaine Poisoning In Rabbits,”J. Pharmacol. Ex. Ther. 32:215-222 (1928).
Utchfield, J.T., Jr., and Wilcoxon, F., “A Simplified Method of Evaluating Dose-Effect Experiments,”J. Pharmacol. and Exp. Therap. 96:99-113 (1949).
Casarett and Douil's Toxicology: The Basic Science of Poisons, 5th ed. (1996) pp. 21-23.
Prieur, David J. et al., “Procedures for Preclinical Toxicologic Evaluation of Cancer Chemotherapeutic Agents: Protocols of the Laboratory of Toxicology,”Cancer Chemotherapy Reports, Jan. 1973, part 3, vol. 4, No. 1:1-30.
Everett et al., “Comparative Anticonvulsive Action of 3,5,5-Trimethyloxazolidine-2,4-Dione (Tridone), Dilantin and Phenobarbital,”J. Pharmacol, 81:402 (1944).
Schwinn et al., “Functional Effects of Activation of Alpha-1 Adrenoceptors by Dexmedetomidine: In Vivo and In Vitro Studies,”J. Pharmacol.&Exp.. Therap., 259 (1991).
Marley et al., “Differential Response to Flurazepan In Long-Sleep and Short-Sleep Mice,”Pharmacol, Biochem.&Behav., 31:453-58 (1987).
G. Zbinden et al., “Pharmacology of Benzodiazepines: Laboratory and Clinical Correlations,”Advances in Pharmacology, 5:213-291 (1967).
W.H. DeCamp, “The FDA Perspective on the Development of Stereoisomers,”Chirality, 1:2-6 (1989).
D.J. Birkett, “Racemates or Enantiomers: Regulatory Approaches,”Clinical and Experimental Pharmacology&Physiology, 16:479-483 (1989).
R.F. Squires et al., “Benzodiazepine Receptors in Rat Brain,”Nature, 266:732-734 (1977).
R.E. Study et al., “Cellular Mechanisms of Benzodiazepine Action,”JAMA, 247:2137-2151 (1982).
D. Nutt, “Selective Ligands for Benzodiazepine Receptors: Recent Developments,”Curr. Aspects Neurosci., 2:259-293 (1990).
G. Richards et al., “Role of GABA in the mechanism of benzodiazepine action,”Seminars in Neurosciences, 3:191-203 (1991).
J.T. Litchfield, “A Method for Rapid Graphic Solution of Time-Percent Effect Curves,”J. Pharmacol. and Exp. Therap., 97:399-408 (1949).
G.W. Snedecor et al., Statistical Methods, 7th ed., 149.
Fiche Technique No. 6, J. Pharmacol. and Experim. Therap., 3:407-914 (1970).
E.J. Ariëns, “Racemic therapeutics—ethical and regulatory aspects,”Eur. J. Clin. Pharmacol. 41:89-93 (1991).
C. Fernandez et al., “Determination of zopiclone enantiomers in plasma by liquid chromatography using a chiral cellulose carbonate column,”J. Chromatog., 572:195-202 (1991).
P. Gauthier et al., “Influence of Zopiclone, a New Generation Hypnotic, on the Intermediate Stage and Paradoxical Sleep in the Rat,”Psychopharcacol., 130:139-143 (1997).
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