Combination of riluzole and of gabapentin and its use as a...

Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Having -c- – wherein x is chalcogen – bonded directly to...

Reexamination Certificate

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C514S561000

Reexamination Certificate

active

06350768

ABSTRACT:

BACKGROUND OF THE INVENTION
The present invention relates to the combination of riluzole and of gabapentin or one of their pharmaceutically acceptable salts and its use as a medicament which is useful in particular for the prevention and/or treatment of motoneuron diseases.
Motoneuron diseases include in particular amyotrophic lateral sclerosis, progressive spinal amyotrophy, infantile spinal amyotrophy and primary lateral sclerosis. They are caused by a progressive loss of motoneurons in the spinal cord.
Amyotrophic lateral sclerosis (ALS), also known by the name of CHARCOT's disease and LOU GEHRIG's disease, was described for the first time by CHARCOT in 1865. It is the most important motoneuron disease. ALS is a fatal disease resulting from degeneration of the motoneurons. The disease is accompanied by progressive paralysis, leading to the loss of motor and respiratory functions and then to death within a period of two to eight years after the appearance of the first symptoms.
To date, only riluzole (2-amino-6-trifluoromethoxybenzothiazole) is marketed under the name RILUTEK® for the treatment of amyotrophic lateral sclerosis. Riluzole makes it possible mainly to slow down the progression of the disease.
Gabapentin has also been recommended for the treatment of neurodegenerative diseases and in particular of amyotrophic lateral sclerosis U.S. Pat. No. 5,084,479). Gabapentin is currently marketed under the name NEURONTIN® for the treatment of epilepsy.


REFERENCES:
patent: 0446570 (1991-09-01), None
patent: 0558861 (1993-09-01), None
Louvel, E. et al: “Therapeutic Advances in Amyotrophic Lateral Sclerosis”; Trends in Pharmacological Sciences, GB, Elsevier Trends Journal, Cambridge, Jun. 1, 1997; vol. 18, No. 6; pp. 196-203.
Ross, M. A.: “Acquired Motor Neuron Disorders”; Neurologic Clinics, Aug., 1997; vol. 15, No. 3; pp. 481-500.
Mitsumoto, H. et al: “Druge Combination Treatment in Patients with ALS: Current Status and Future Directions”; Neurology, 1996; 47/4 Suppl. pp. S103-S107.
Lai, Eugene C.: “Therapeutic Developments in Amyotrophic Lateral Sclerosis”; Expert Opin. Invest. Drugs, 1999, pp. 347-361.
Lloyd-Williams, P. et al: “Convergent Solid-Phase Peptide Synthesis”; Tetrahedron, No. 347, 1993, p. 49.
Ciommer, M. et al: “Synthesis of Glyopeptides with Partial Structure of Human Glycophorin Using the Fluorenylmethoxycarbonyl Allyl Ester Protecting Group Combination”; SynLett, 1991, N8, pp. 593-595.
Lyttle, M. H. et al: “Peptides: Chemistry and Biology”; Proc. 12thAmerican Peptide Symposium, 1992; p. 583.
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