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1 441 702 B1 (19) TZZ__Z _T (11) EP 1 441 702 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/4045 (2006.01) A61P 25/20 (2006.01) 10.05.2017 Bulletin 2017/19 A61K 9/20 (2006.01) (21) Application number: 02760523.7 (86) International application number: PCT/IL2002/000662 (22) Date of filing: 12.08.2002 (87) International publication number: WO 2003/015690 (27.02.2003 Gazette 2003/09) (54) METHOD FOR TREATING PRIMARY INSOMNIA VERFAHREN ZUR BEHANDLUNG PRIMÄRER INSOMNIA METHODE DE TRAITEMENT DE L’INSOMNIE PRIMAIRE (84) Designated Contracting States: • ROTH T ET AL: "Consensus for the AT BE BG CH CY CZ DE DK EE ES FI FR GB GR pharmacological management of insomnia in th IE IT LI LU MC NL PT SE SK TR enew millennium", INTERNATIONAL JOURNAL Designated Extension States: OF CLINICAL PRACTICE, MEDICON LT LV RO SI INTERNATIONAL, ESHER, GB, vol. 55, no. 1, 1 January 2001 (2001-01-01), page 10PAGES, (30) Priority: 14.08.2001 IL 14490001 XP002990688, ISSN: 1368-5031 • PERLIS M L ET AL: "Psychophysiological (43) Date of publication of application: insomnia: the behavioural model and a 04.08.2004 Bulletin 2004/32 neurocognitive perspective", JOURNAL OF SLEEP RESEARCH, BLACKWELL SCIENTIFIC, (60) Divisional application: OXFORD, GB, vol. 6, 1 January 1997 (1997-01-01), 16172415.8 / 3 103 443 pages 179-188, XP002990686, ISSN: 0962-1105, DOI: DOI:10.1046/J.1365-2869.1997.00045.X (73) Proprietor: NEURIM PHARMACEUTICALS (1991) • SILVA J A C E ET AL: "Special report from a LIMITED symposium held by the WHO and the World Tel Aviv 69710 (IL) Federation of sleep research societies: an overview of insomnias and related disorders - (72) Inventor: ZISAPEL, Nava recognition, epidemiology and rational 69355 Tel Aviv (IL) management", SLEEP, ALLEN PRESS, LAWRENCE, KS,US, vol. 19, no. 5,1 January 1996 (74) Representative: ABG Patentes, S.L. (1996-01-01), pages412-416, XP002990669, ISSN: Avenida de Burgos, 16D 0161-8105 Edificio Euromor • UCHIKAWA O ET AL: "Synthesis of a novel series 28036 Madrid (ES) of tricyclic indan derivatives as melatonin receptor agonists", JOURNAL OF MEDICINAL (56) References cited: CHEMISTRY, AMERICAN CHEMICAL SOCIETY, EP-A- 0 565 296 EP-A- 0 724 878 WASHINGTON, US, vol. 45, 1 January 2002 EP-A2- 0 513 702 WO-A-01/49286 (2002-01-01), pages 4222-4239, XP002990691, US-A- 5 498 423 US-B1- 6 423 738 ISSN: 0022-2623, DOI: DOI:10.1021/JM0201159 • FAINSTEINET AL: "Effects of melatonin in elderly • DUBOCOVICH M L ET AL: "Melatonin receptors", patients with sleep disturbance: a pilot study", 19980101, vol. 1, 1 January 1998 (1998-01-01), CURRENT THERAPEUTIC RESEARCH, XX, XX, pages 187-193, XP002990671, vol. 58, no. 12, 1 December 1997 (1997-12-01), pages 990-1000, XP002990653, Note: Within nine months of the publication of the mention of the grant of the European patent in the European Patent Bulletin, any person may give notice to the European Patent Office of opposition to that patent, in accordance with the Implementing Regulations. Notice of opposition shall not be deemed to have been filed until the opposition fee has been paid. (Art. 99(1) European Patent Convention). EP 1 441 702 B1 Printed by Jouve, 75001 PARIS (FR) (Cont. next page) EP 1 441 702 B1 • BRUSCO ET AL: "Effect of melatonin in selected • Anonymous: "Assesment Report for Circadin", populations of sleep-disturbed patients", European Medicines Agency , 1 January 2007 BIOLOGICAL SIGNAL AND RECEPTORS, (2007-01-01), pages 1-52, London, UK Retrieved KARGER, BASEL, CH, vol. 8, 1 January 1999 from the Internet: (1999-01-01), pages126-131, XP002990655, ISSN: URL:http://www.ema.europa.eu/docs/en_GB/do 1422-4933 cument_library/EPAR_-_Scientific_Discussio • HAIMOV IET AL:"Melatonin replacement therapy n/human/000695/WC500026808.pdf [retrieved on elderly insomniacs", SLEEP, ALLEN PRESS, 2013-10-01] LAWRENCE, KS,US, vol. 18, no. 7,1 January 1995 • Anonymous: "Annex I Summary of Product (1995-01-01), pages598-603, XP002990657, ISSN: Characteristics", European Medicines Agency , 0161-8105 19 June 2012 (2012-06-19), pages 1-28, Retrieved • HAIMOV I ET AL: "Potential of melatonin from the Internet: replacement therapy in older patients with sleep URL:http://www.ema.europa.eu/docs/en_GB/do disorders", DRUGS & AGING, ADIS cument_library/EPAR_-_Product_Information/ INTERNATIONAL LTD, NZ, vol. 7, no. 2, 1 January human/000695/WC500026811.pdf [retrieved on 1995 (1995-01-01) , pages 75-78, XP002990660, 2013-10-01] ISSN: 1170-229X • LEMOINE PATRICK ET AL: "Prolonged-release • MONTI J M ET AL: "Polysomnographic study of melatonin improves sleep quality and morning theeffect of melatonin on sleepin elderly patients alertness in insomnia patients aged 55 years and with chronic primary insomnia", ARCHIVES OF older and has no withdrawal effects", JOURNAL GERONTOLOGY AND GERIATRICS, ELSEVIER, OF SLEEP RESEARCH, vol. 16, no. 4, December AMSTERDAM, NL, vol. 28, 1 January 1999 2007 (2007-12), pages 372-380, ISSN: 0962-1105 (1999-01-01), pages 85-98, XP002990661, ISSN: 0167-4943, DOI: Remarks: DOI:10.1016/S0167-4943(98)00129-0 Thefile contains technical information submitted after • HUGHES R J ET AL: "The role of melatonin and the application was filed and not included in this circadian phase in age-related specification sleep-maintenance insomnia: asessment in a clinical trial of melatonin replacement", SLEEP, ALLEN PRESS, LAWRENCE, KS, US, vol. 21, no. 1, 1 January 1998 (1998-01-01), pages 52-68, XP002990675, ISSN: 0161-8105 • BUYSSE D J ET AL: "Diagnostic concordance for DSM-IV sleep disorders: a report from the APA/NIMH DSM-IV field trial", AMERICAN JOURNAL OF PSYCHIATRY, AMERICAN PSYCHIATRIC PUBLISHING, INC, US, vol. 151, no. 9, 1 September 1994 (1994-09-01), pages 1351-1360, XP008152789, ISSN: 0002-953X 2 EP 1 441 702 B1 Description FIELD OF THE INVENTION 5 [0001] The present invention relates to a method for treating primary insomnia (as defined by DSM-IV or nonorganic insomnia as defined by ICD-10) when characterized by non-restorative sleep, and to the use of melatonin in the man- ufacture of a medicament for this purpose. BACKGROUND OF THE INVENTION 10 [0002] Sleep disorders, which are complex, are widespread, especially in Western industrial countries, in which it is estimated that about one third of the adult population reports at least occasional difficulties with sleeping, while at least half of the sleep-disordered population have had sleep complaints for years. In US 5,776,969 (James), which discloses a method of treating various sleep disorders, by therapy with a specified combination of chemical compounds, there is 15 discussed and defined inter alia, primary insomnia, which may or may not be characterized by non-restorative sleep. [0003] The definition of primary insomnia in the fourth revision of the Diagnostic and Statistical Manual of Mental Disorders (DSM-IV) (American Psychiatric Association, 1994) states: "The predominant complaint is difficulty initiating or maintaining sleep, or non-restorative sleep, for at least one month. The sleep disturbance (or associated daytime fatigue) causes clinically significant distress or impairment in social, occupational or other important areas of functioning." 20 Furthermore, according to the definition, non-restorative sleep alone is sufficient to establish the diagnosis of primary insomnia, providing it results in impaired daytime functioning. [0004] The tenth revision of the International Classification of Diseases (ICD-10) (World Health Organisation, 1991) describes nonorganic insomnia as "a condition of unsatisfactory quantity and/or quality of sleep." It goes on to state that "there are people who suffer immensely from the poor quality of their sleep, while sleep in quantity is judged subjectively 25 and/or objectively as within the normal limits." [0005] The diagnostic guidelines from ICD-10 state that the essential clinical features for a definitive diagnosis of primary insomnia are as follows: a) the complaint is either of difficulty falling asleep or maintaining sleep, or of poor quality sleep; b) the sleep disturbance has occurred at least three times per week for at least one month; c) there is preoccupation with the sleeplessness and excessive concern over its consequences at night and during the day; d) the 30 unsatisfactory quantity and/or quality of sleep either causes marked distress or interferes with social and occupational functioning. Thus, there is repeated emphasis in ICD-10 on the equal importance of quality of sleep and quantity of sleep in the diagnosis of insomnia. The invention thus relates to primary insomnia (DSM-IV) or nonorganic insomnia (ICD-10). [0006] Because, in normal humans, the natural hormone melatonin has an increased nocturnal concentration in the blood (according to a particular profile, see e.g. US 5,498,423 (Zisapel)), compared with its daytime concentration, and 35 because also a lack of nocturnal melatonin appears to correlate with the existence of sleep disorders, especially although not exclusively in the elderly, the possibility of administering exogenous melatonin to ameliorate sleep disorders has been investigated and is the subject of many scientific papers. [0007] Thus, for example, in James, S.P., et al. (Neuropsychopharmacology 1990, 3:19-23), melatonin (1 and 5 mg) and placebo were given at 10:45 pm for one night each to 10 polysomnographically pre-screened insomniacs with a 40 mean age of 33.4 years. These patients (who may not necessarily have had non-restorative sleep related insomnia) had quantitative sleep deficits that were demonstrable by PSG. Administration of melatonin did not alter sleep latency, sleep efficiency, total sleep time, or wake after sleep onset. The patients reported improved sleep quality, though they were not more rested in the morning and believed that their total sleep time had been shorter when on melatonin.
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