Drug – bio-affecting and body treating compositions – Designated organic active ingredient containing – Radical -xh acid – or anhydride – acid halide or salt thereof...
Reexamination Certificate
2001-01-09
2001-10-23
Spivack, Phyllis G. (Department: 1614)
Drug, bio-affecting and body treating compositions
Designated organic active ingredient containing
Radical -xh acid, or anhydride, acid halide or salt thereof...
C514S567000
Reexamination Certificate
active
06306910
ABSTRACT:
BACKGROUND OF THE INVENTION
1. Field of The Invention
The present invention relates to the use of analogs of glutamic acid and gamma-aminobutyric acid (GABA) for the treatment of insomnia.
2. Description of Related Art
GABA analogs are known agents useful in antiseizure therapy for central nervous system disorders such as epilepsy, Huntington's chorea, cerebral ischemia, Parkinson's disease, tardive dyskinesia, and spasticity. It has also been suggested that the compounds can be used as antidepressants, anxiolytics, and antipsychotics. See WO 92/09560 (U.S. Ser. No. 618,692 filed Nov. 27, 1990) and WP 93/23383 (U.S. Ser. No. 886,080 filed May 20, 1992).
WO 97/33858 teaches that compounds related to gabapentin are useful or treating epilespy, faintness attacks, hypokinesia, cranial disorders, neurodegenerative disorders, depression, anxiety, panic, pain, and neuropathological disorders. WO 97/33858 does not specify what forms of pain are treated.
Additionally, the compounds of the invention are known for treatment of neuropathic pain. For example, see Rosner H; Rubin L; Kestenbaum A., Gabapentin adjunctive therapy in neuropathic pain states. Clin J Pain, 1996 March, 12:1, 56-8; Segal A Z; Rordorf G., Gabapentin as a novel treatment for postherpetic neuralgia. Neurology, 1996 April, 46:4, 1175-6; Wetzel C H; Connelly J F., Use of gabapentin in pain management. Ann Pharmacother, 1997 September 31:9, 1082-3; Zapp J J., Postpoliomyelitis pain treated with gabapentin [letter]. Am Fam Physician, 1996 June, 53:8, 2442, 2445; Cheville A, et al., Neuropathic pain in radiation myelopathy: a case report. Program book, American Pain Society (14th Annual Scientific Meeting). Abstract #95823, p. A-115; Sist T; Filadora V; Miner M; Lema M., Gabapentin for idiopathic trigeminal neuralgia: report of two cases. Neurology, 1997 May 48:5, 1467; Waldman S D, Tutorial 28: Evaluation and Treatment of Trigeminal Neuralgia. Pain Digest (1997) 7:21-24; Mellick L B; Mellick G A., Successful treatment of reflex sympathetic dystrophy with gabapentin [letter]. Am J Emerg Med, 1995 January, 13:1, 96; Mellick G A; Seng M I., The use of gabapentin in the treatment of reflex sympathetic dystrophy and a phobic disorder. Am J Pain Manage 1995; 5:7-9; Mellick G A; Mellicy L B; Mellick L B., Gabapentin in the management of reflex sympathetic dystrophy [letter]. J Pain Symptom Manage, 1995 May, 10:4, 265-6; Mellick G A; Mellick L B., Reflex sympathetic dystrophy treated with gabapentin. Arch Phys Med Rehabil, 1997 January, 78:1, 98-105 and Mackin G A., Medical and pharmacologic management of upper extremity neuropathic pain syndromes. J Hand Ther, 1997 April-June, 10:2, 96-109.
Insomnia and sleeplessness are common problems. Often, the insomnia or sleeplessness is precipitated by stress, emotional and physical causes.
U.S. Pat. No. 5,510,381, directed to the use of gabapentin to treat mania, mentions one study in which gabapentin has also been found to enhance delta-wave (deep) sleep. This effect is beneficial in acute mania and also leads to reducing the risk for onset of a new episode of mania.
SUMMARY OF THE INVENTION
This invention provides a method for treating insomnia in a mammal comprising administering to a subject suffering from insomnia an effective amount of a GABA analog. A preferred embodiment utilizes a cyclic amino acid compound of Formula I
wherein R
1
is hydrogen or lower alkyl and n is an integer of from 4 to 6, and the pharmaceutically acceptable salts thereof. An especially preferred embodiment utilizes a compound of Formula I where R
1
is hydrogen and n is 4, which compound is 1-(aminomethyl)-cyclohexane acetic acid, known generically as gabapentin.
In another embodiment, the invention includes treating insomnia with a compound of Formula II.
wherein R
2
is a straight or branched alkyl of from 1 to 6 carbon atoms, phenyl, or cycloalkyl having from 3 to 6 carbon atoms; R
3
is hydrogen or methyl; and R4 is hydrogen, methyl, or carboxyl; or an individual enantiomeric isomer thereof; or a pharmaceutically acceptable salt thereof, in unit dosage form, to a mammal in need of said treatment.
Preferred compounds of the invention are those wherein R
4
and R
3
are hydrogen, and R
2
is —(CH
2
)
0-2
-i C
4
H
9
as an (R), (S), or (R,S) isomer.
The more preferred compounds of Formula II invention are (S)-3-(aminomethyl)-5-methylhexanoic acid and 3-aminomethyl-5-methyl-hexanoic acid, now known generically as pregabalin.
REFERENCES:
patent: 5510381 (1996-04-01), Pande
Rodenbeck et al., Somnologie, 2/1 (26-31) (abstract), 1998.*
Rao et al., “Gabapentin augments whole blood serotonin in healthy young men”, abstractJ. Neural Transmission, vol. 73, No. 2, 1988, pp. 129-134.
Placidi et al., “Effect of chronic treatment with Gabapentin on nocturnal sleep in epilepsy”, American Epilepsy Society, Annual Meeting, Boston, Dec. 4-7, 1997, abstract.
Karam-Hage and Brower, “Gabapentin is helpful for insomnia in alcohol-dependent patients during early recovery”,Alcoholism Clinical and Experimental Research, vol. 23, No. 5, Suppl., May 1999, p. 81A, abstract.
Field et al., “Gabapentin (neurontin) and S-(+)-3-isobutylgaba represent a novel class of selective antihyperalgesic agents”,British Journal of Pharmacology, vol. 121, No. 8, 1997, pp. 1513-1522.
Magnus Leslie
Segal Catherine A.
Ashbrook Charles W.
Spivack Phyllis G.
Warner-Lambert & Company
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