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Combination of Memantine and Donepezil for Treatment of CNS

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Combination of Memantine and Donepezil for Treatment of CNS (19) TZZ ¥_T (11) EP 2 243 475 B1 (12) EUROPEAN PATENT SPECIFICATION (45) Date of publication and mention (51) Int Cl.: of the grant of the patent: A61K 31/13 (2006.01) A61K 31/445 (2006.01) 13.01.2016 Bulletin 2016/02 A61P 25/00 (2006.01) A61K 9/16 (2006.01) A61K 9/48 (2006.01) A61K 9/70 (2006.01) (21) Application number: 10075323.5 (22) Date of filing: 06.04.2006 (54) Combination of memantine and donepezil for treatment of CNS disorders Kombination von Memantin und Donepezil zur Behandlung von Erkrankungen des ZNS Combinaison de mémantine et donépézil pour le traitement de conditions relatives au SNC (84) Designated Contracting States: (56) References cited: AT BE BG CH CY CZ DE DK EE ES FI FR GB GR EP-A1- 1 832 298 WO-A-2005/072705 HU IE IS IT LI LT LU LV MC NL PL PT RO SE SI WO-A1-2005/084655 WO-A2-2005/065645 SK TR US-A1- 2004 087 658 (30) Priority: 06.04.2005 US 669290 P • HARTMANN S ET AL: "Tolerability of memantine 22.11.2005 US 285905 in combination with cholinesterase inhibitors in dementia therapy" INTERNATIONAL CLINICAL (43) Date of publication of application: PSYCHOPHARMACOLOGY, vol. 18, no. 2, 2003, 27.10.2010 Bulletin 2010/43 pages 81-85, XP002967315 ISSN: 0268-1315 • PERICLOU A P ET AL: "Lack of pharmacokinetic (62) Document number(s) of the earlier application(s) in or pharmacodynamic interaction between accordance with Art. 76 EPC: memantine and donepezil." THE ANNALS OF 06749777.6 / 1 874 282 PHARMACOTHERAPY, vol. 38, no. 9, September 2004 (2004-09), pages 1389-1394, XP009075926 (73) Proprietor: Adamas Pharmaceuticals, Inc. ISSN: 1060-0280 Emeryville, CA 94608 (US) • TARIOT P N ET AL: "Memantine treatment in patients with moderate to severe Alzheimer (72) Inventors: disease already receiving donepezil: a • Went, Gregory T. randomized controlled trial." JAMA : THE Mill Valley, CA 94941-1204 (US) JOURNAL OF THE AMERICAN MEDICAL • Fultz, Timothy J. ASSOCIATION, vol. 291, no. 3, 21 January 2004 Pleasant Hill, CA 94523 (US) (2004-01-21), pages 317-324, XP009075923 ISSN: 1538-3598 (74) Representative: Warner, James Alexander Carpmaels & Ransford LLP One Southampton Row London WC1B 5HA (GB) 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 2 243 475 B1 Printed by Jouve, 75001 PARIS (FR) EP 2 243 475 B1 Description FIELD OF THE INVENTION 5 [0001] This invention relates to compositions for treating CNS-related conditions, such as Alzheimer’s disease. BACKGROUND OF THE INVENTION [0002] Acute and chronic neurological and neuropsychiatric diseases are among the leading causes of death, disability, 10 and economic expense in the world. Presently, Alzheimer’s disease is the fourth leading cause of death in the USA. Today there is no known cure for this chronic degenerative ailment, which directly affects millions of people throughout the world. Other diseases and disorders of the central nervous system also result in substantial suffering and cost for those afflicted by the ailments as well as their families and providers. [0003] Numerous drugs exist in the market today to treat the symptoms or manage the progression of these diseases, 15 but most have modest or limited efficacy. Frequently, polypharmacy is employed to optimize therapy to the specific needs of patients at different stages of the disease. One of the key challenges in treating these disorders is the high degree of interplay amongst the pathways that control both normal and abnormal neuronal functions. The therapeutic management of these functions is typically determined such that the therapeutic effects are maximized while minimizing the debilitating side effects of the therapies. This effort is usually more complex when multiple therapeutics are employed. 20 [0004] WO2005/065645 discloses donepezil formulations, including amorphous donepezil or pharmaceutically ac- ceptable salts thereof; sustained-release formulations; and donepezil sprinkle formulations. [0005] EP1832298 discloses a matrix type sustained-release preparation and a manufacturing method thereof. The matrix type sustained-release preparation contains a basic drug or a salt thereof and at least one enteric polymer. [0006] WO2005072705 discloses methods and compositions comprising a NMDA receptor antagonist and a monoam- 25 ine oxidase (MAO) inhibitor GADPH inhibitor for the treatment dementia-related conditions, such as Parkinson’s disease and Alzheimer’s disease. [0007] Int Clin Psychopharm 2003, 18, 81-85 - (Hartmann) discloses ACheIs and the NMDA receptor antagonist memantine for treatment of dementia, including Alzheimer’s disease. [0008] Ann Pharmacother 2004, 38, 1389-1394 discloses a study to determine whether an in vivo pharmacokinetic 30 interaction exists between memantine and the acetylcholinesterase inhibitor donepezil. The study indicated a lack of interaction between memantine and donepezil. [0009] JAMA 2004, 291, 317-324 discloses a study to compare the efficacy and safety of memantine vs placebo in patients with moderate to severe Alzheimer’s disease already receiving stable treatment with donepezil. It is suggested that memantine represents a new approach for the treatment of patients with moderate to severe Alzheimer disease. 35 [0010] Improved therapeutics for treatment of these diseases and disorders are needed. SUMMARY OF THE INVENTION [0011] In general, the present invention provides compositions for treating and preventing CNS-related conditions, 40 such as neurodegenerative conditions (e.g., Alzheimer’s disease and Parkinson’s disease) and pain, by administering to a subject in need thereof a combination that includes an N-Methyl-D-Aspartate receptor (NMDAr) antagonist selected from memantine and pharmaceutically acceptable salts thereof and a second agent as an acetylcholinesterase inhibitor (ACheI)selected from donepezil and pharmaceutically acceptable salts thereof. The administration of the combinations described herein results in the alleviation and prevention of symptoms associated with or arising from CNS-related 45 conditions such as Parkinson’s disease or Alzheimer’s disease including, for example, loss of memory, loss of balance, hallucinations, delusions, agitation,withdrawal, depression, communication problems, cognitive loss,personality change, confusion and insomnia. The combinations of the present invention may be used in the prevention or treatment of CNS- related conditions associated with Alzheimer’s disease and may also be helpful for the treatment and prevention of headaches, cerebrovascular diseases, motor neuron diseases, dementias, neurodegenerative diseases, strokes, move- 50 ment disorders, ataxic syndromes, disorders of the sympathetic nervous system, cranial nerve disorders, myelopathies, traumatic brain and spinal cord injuries, radiation brain injuries, multiple sclerosis, post-meningitis syndrome, prion diseases, myelitic disorders, radiculitis, neuropathies, pain syndromes, axonic brain damage, encephalopathies, chronic fatigue syndrome, psychiatric disorders, glucose dysregulation, and drug dependence. [0012] The NMDAr antagonist, the ACheI, or both agents may be administered in an amount similar to that typically 55 administered to subjects. Optionally, the amount of the NMDAr antagonist, the ACheI, or both agents may be administered in an amount greater than or less than the amount that is typically administered to subjects. If desired, the amount of the NMDAr antagonist in the pharmaceutical composition is less than the amount of NMDAr antagonist required in a unit dose to obtain the same therapeutic effect for treating or preventing a CNS-related condition when the NMDAr 2 EP 2 243 475 B1 antagonist is administered in the absence of the ACheI. Alternatively, the amount of the ACheI in the pharmaceutical composition is less than the amount of the ACheI required in a unit dose to obtain the same therapeutic effect for treating or preventing a CNS-related condition when the ACheI is administered in the absence of the NMDAr antagonist. Op- tionally, the NMDAr antagonist, the ACheI, or both are present at a higher dose than that typically administered to a 5 subject for a specific condition. For example, the amount of memantine required to positively affect the patient response (inclusive of adverse effects) may be 2.5-80 mg per day rather than the typical 10-20 mg per day administered for presently approved indications i.e. without the improved formulations described herein. A higher dose amount of the NMDAr antagonist in the present invention may be employed whereas a lower dose of the NMDAr antagonist may be sufficient when combined with the ACheI to achieve a therapeutic effect in the patient. Optionally, lower or reduced 10 amounts of both the NMDAr antagonist and the ACheI are used in a unit dose relative to the amount of each agent when administered as a monotherapy. In a preferred embodiment, the amount of the NMDAr antagonist in the pharmaceutical composition is equal to or greater than the amount typically administered to a subject for a specific condition as a monotherapy and the amount of the ACheI in the pharmaceutical composition is less than the amount typically admin- istered to a subject for a similar condition. 15 [0013] The invention relates to a pharmaceutical
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