AU6472799A - Therapy for improving cognition - Google Patents
Therapy for improving cognition Download PDFInfo
- Publication number
- AU6472799A AU6472799A AU64727/99A AU6472799A AU6472799A AU 6472799 A AU6472799 A AU 6472799A AU 64727/99 A AU64727/99 A AU 64727/99A AU 6472799 A AU6472799 A AU 6472799A AU 6472799 A AU6472799 A AU 6472799A
- Authority
- AU
- Australia
- Prior art keywords
- atypical antipsychotic
- acetylcholinesterase inhibitor
- patients suffering
- alzheimer
- disease
- Prior art date
- Legal status (The legal status is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the status listed.)
- Abandoned
Links
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
- A61K31/33—Heterocyclic compounds
- A61K31/395—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
- A61K31/55—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having seven-membered rings, e.g. azelastine, pentylenetetrazole
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K31/00—Medicinal preparations containing organic active ingredients
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P25/00—Drugs for disorders of the nervous system
- A61P25/28—Drugs for disorders of the nervous system for treating neurodegenerative disorders of the central nervous system, e.g. nootropic agents, cognition enhancers, drugs for treating Alzheimer's disease or other forms of dementia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Engineering & Computer Science (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Medicines Containing Plant Substances (AREA)
Description
WO 00/23057 PCT/EP99/07804 THERAPY FOR IMPROVING COGNITION The present invention is concerned with pharmaceutical compositions comprising a 5 carrier and as first active ingredient an atypical antipsychotic agent (I) and as second active ingredient an acetylcholinesterase inhibitor (II), each in an amount producing a therapeutically beneficial effect in patients suffering from psychosis, or Alzheimer's disease or related dementias. Said therapeutically beneficial effect can be a synergistic effect on the cognitive functioning of patients suffering from Alzheimer's disease or 10 related dementias, or the prevention of the further deterioration of cognition in said patients, or the reduction of adverse effects associated with the one of the active ingredients by the other of the active ingredients. Of particular interest is the use of an atypical antipsychotic agent (I) for the preparation 15 of a medicament for reducing adverse effects associated with acetylcholinesterase inhibitors (II) in patients suffering from Alzheimer's disease or related dementias, such as nausea, vomiting, sweating, restlessness and insomnia. Especially interesting is the use of an atypical antipsychotic agent (I) for the preparation of a medicament for improving sleep in patients suffering from Alzheimer's disease or related dementias 20 while being treated with acetylcholinesterase inhibitors (II). The present invention is concerned with a pharmaceutical composition comprising a carrier and as first active ingredient an atypical antipsychotic agent (I) and as second active ingredient an acetylcholinesterase inhibitor (II), each in an amount producing a 25 therapeutically beneficial effect in patients suffering from psychosis, or Alzheimer's disease or related dementias. Said therapeutically beneficial effect can be a synergistic effect on the cognitive functioning of patients suffering from Alzheimer's disease or related dementias, or the prevention of the further deterioration of cognition in said patients, or the reduction of adverse effects associated with the one of the active 30 ingredients by the other of the active ingredients. The atypical antipsychotic (I) is selected from risperidone, 9-hydroxyrisperidone or a
C
10
.
20 alkanoic acid ester thereof, olanzapine, quetiapine, iloperidone or ziprasidone, and the acetylcholinesterase inhibitor (II) is selected from galantamine, rivastigmine or 35 donepezil, or therapeutically active acid addition salt form of any of the foregoing. Said salts comprise salt forms which the active ingredients (I) and (II) are able to form with appropriate acids, such as, for example, inorganic acids such as hydrohalic acids, e.g. hydrochloric or hydrobromic acid; sulfuric; nitric; phosphoric and the like acids; or WO 00/23057 PCT/EP99/07804 -2 organic acids such as, for example, acetic, propanoic, hydroxyacetic, lactic, pyruvic, oxalic, malonic, succinic, maleic, fumaric, malic, tartaric, citric, methanesulfonic, ethanesulfonic, benzenesulfonic, p-toluenesulfonic, cyclamic, salicylic, p-amino salicylic, pamoic and the like acids. For example, galantamine may conveniently be 5 used as the (1:1) hydrobromide salt. C10-20alkanoic acids are selected from the group consisting of decanoic (capric), undecanoic, dodecanoic (lauric), tridecanoic, tetradecanoic (myristic), pentadecanoic, hexadecanoic (palmitic), heptadecanoic, octadecanoic (stearic), nonadecanoic and 10 eicosanoic acid. Due to their limited aqueous solubility, it was generally believed that the esters had to be suspended into oils. The ester having a C15 (pentadecyl) chain and the active ingredient corresponding thereto being the 9-hydroxyrisperidone palmitate ester was found to be the superior ester from a pharmacokinetic, as well as from a tolerance point of view. 15 Preferably, the amount of each of the active ingredients is equal to or less than that which is approved in monotherapy with said active ingredient. Most preferred are compositions wherein the atypical antipsychotic (I) is risperidone 20 and the acetylcholinesterase inhibitor (II) is galantamine, in particular as galantamine hydrobromide. In said compositions, the amount of risperidone is 0.5, 1, 2, 4, or 6 mg and that of galantamine (as base) is 8, 16, 24 or 32 mg per dosage form. The present invention also relates to products containing as first active ingredient an 25 atypical antipsychotic agent (I) and as second active ingredient an acetylcholinesterase inhibitor (II), as combined preparations for simultaneous, separate or sequential use in the treatment of patients suffering from psychosis, Alzheimer's disease or related dementias. 30 The present invention also concerns the use of an acetyicholinesterase inhibitor (II) for the preparation of a medicament for enhancing the effect of an atypical antipsychotic agent (I) on cognition in patients suffering from psychosis. Conversely, the present invention also concerns the use of an atypical antipsychotic 35 agent (I) for the preparation of a medicament for enhancing the effect of an acetylcholinesterase inhibitor (II) on cognition in patients suffering from Alzheimer's disease or related dementias.
- WO 00/23057 PCT/EP99/07804 -3 Additionally, the present invention concerns the use of an atypical antipsychotic agent (I) for the preparation of a medicament for reducing adverse effects associated with acetylcholinesterase inhibitors (II) in patients suffering from Alzheimer's disease or related dementias. Said adverse effect can be nausea, vomiting, sweating, restlessness 5 or insomnia. Especially interesting is the use of an atypical antipsychotic agent (I) for the preparation of a medicament for improving sleep in patients suffering from Alzheimer's disease or related dementias while being treated with acetylcholinesterase inhibitors (II). 10 Finally, the present invention also concerns the use of an acetylcholinesterase inhibitor (II) for the preparation of a medicament for reducing adverse effects associated with atypical antipsychotic agents (I) in patients suffering from psychoses. Said the adverse effect can be extrapyramidal syndrome or tardive dyskinesia. 15 In all the preceding uses the atypical antipsychotic (I) is preferably risperidone and the acetylcholinesterase inhibitor (II) is preferably galantamine, in particular the (1:1) hydrobromide.
Claims (14)
1. A pharmaceutical composition comprising a carrier and as first active ingredient an atypical antipsychotic agent (I) and as second active ingredient an 5 acetylcholinesterase inhibitor (II), each in an amount producing a therapeutically beneficial effect in patients suffering from psychosis, Alzheimer's disease or related dementias.
2. A composition according to claim 1 wherein said therapeutically beneficial effect is 10 a synergistic effect on the cognitive functioning of patients suffering from Alzheimer's disease or related dementias, or the prevention of the further deterioration of cognition in said patients, or the reduction of adverse effects associated with the one of the active ingredients by the other of the active ingredients. 15
3. A composition according to claim 1 wherein the atypical antipsychotic (I) is selected from risperidone, 9-hydroxyrisperidone or a C 10 - 20 alkanoic acid ester thereof, olanzapine, quetiapine, iloperidone or ziprasidone, and the acetylcholinesterase inhibitor (II) is selected from galantamine, rivastigmine or 20 donepezil.
4. A composition according to claim 3 wherein the amount of each of the active ingredients is equal to or less than that which is approved in monotherapy with said active ingredient. 25
5. A composition according to claim 3 wherein the atypical antipsychotic (I) is risperidone and the acetylcholinesterase inhibitor (II) is galantamine.
6. A composition according to claim 5 wherein the amount of risperidone is 0.5, 1, 2, 30 4, or 6 mg and that of galantamine (as base) is 8, 16, 24 or 32 mg per dosage form.
7. A product containing as first active ingredient an atypical antipsychotic agent (I) and as second active ingredient an acetylcholinesterase inhibitor (II), as a combined preparation for simultaneous, separate or sequential use in the treatment of patients 35 suffering from psychosis, Alzheimer's disease or related dementias. WO 00/23057 PCT/EP99/07804 -5
8. The use of an acetylcholinesterase inhibitor (II) for the preparation of a medicament for enhancing the effect of an atypical antipsychotic agent (I) on cognition in patients suffering from psychosis. 5
9. The use of an atypical antipsychotic agent (I) for the preparation of a medicament for enhancing the effect of an acetylcholinesterase inhibitor (II) on cognition in patients suffering from Alzheimer's disease or related dementias.
10. The use of an atypical antipsychotic agent (I) for the preparation of a medicament 10 for reducing adverse effects associated with acetyicholinesterase inhibitors (II) in patients suffering from Alzheimer's disease or related dementias.
11. Use according to claim 10 wherein the adverse effect is nausea, vomiting, sweating, restlessness or insomnia. 15
12. The use of an acetylcholinesterase inhibitor (II) for the preparation of a medicament for reducing adverse effects associated with atypical antipsychotic agents (I) in patients suffering from psychoses. 20
13. Use according to claim 12 wherein the adverse effect is extrapyramidal syndrome or tardive dyskinesia.
14. Use according to any one of claims 8 to 13 wherein the atypical antipsychotic (I) is risperidone and the acetylcholinesterase inhibitor (II) is galantamine.
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98203454 | 1998-10-16 | ||
| EP98203454 | 1998-10-16 | ||
| PCT/EP1999/007804 WO2000023057A2 (en) | 1998-10-16 | 1999-10-12 | Atypical antiphsychotic in combination with acetylcholinesterase inhibitor for improving cognition |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AU6472799A true AU6472799A (en) | 2000-05-08 |
Family
ID=8234219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| AU64727/99A Abandoned AU6472799A (en) | 1998-10-16 | 1999-10-12 | Therapy for improving cognition |
Country Status (20)
| Country | Link |
|---|---|
| EP (1) | EP1121131A2 (en) |
| JP (1) | JP2002527469A (en) |
| KR (1) | KR20010072878A (en) |
| CN (1) | CN1367697A (en) |
| AU (1) | AU6472799A (en) |
| BG (1) | BG105302A (en) |
| BR (1) | BR9914419A (en) |
| CA (1) | CA2345767A1 (en) |
| EE (1) | EE200100136A (en) |
| HK (1) | HK1039745A1 (en) |
| HR (1) | HRP20010262A2 (en) |
| HU (1) | HUP0103781A3 (en) |
| ID (1) | ID28441A (en) |
| IL (1) | IL142588A0 (en) |
| NO (1) | NO20011403D0 (en) |
| PL (1) | PL348107A1 (en) |
| SK (1) | SK4592001A3 (en) |
| TR (1) | TR200101082T2 (en) |
| WO (1) | WO2000023057A2 (en) |
| ZA (1) | ZA200103081B (en) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| GB0102841D0 (en) * | 2001-02-05 | 2001-03-21 | Novartis Ag | Organic compounds |
| AU2006201188B2 (en) * | 2001-02-05 | 2007-11-15 | Novartis Ag | New use of iloperidone |
| ES2358416T3 (en) | 2001-10-30 | 2011-05-10 | Novartis Ag | PROLONGED RELEASE FORMATIONS OF ILOPERIDONE AND POLYMER IN THE FORM OF A STAR. |
| GB0216416D0 (en) | 2002-07-15 | 2002-08-21 | Novartis Ag | Organic compounds |
| US20040192754A1 (en) * | 2003-03-24 | 2004-09-30 | Shapira Nathan Andrew | Methods for treating idiopathic hyperhidrosis and associated conditions |
| TW200501962A (en) * | 2003-04-01 | 2005-01-16 | Novartis Ag | Use of carbamazepine derivatives for the treatment of agitation in dementia patients |
| WO2005065645A2 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Donepezil formulations |
| JP2008523058A (en) * | 2004-12-10 | 2008-07-03 | アボット・ラボラトリーズ | Fused bicycloheterocyclic substituted quinuclidine derivatives |
| WO2008055945A1 (en) | 2006-11-09 | 2008-05-15 | Probiodrug Ag | 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcer, cancer and other diseases |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| CN101668525A (en) | 2007-03-01 | 2010-03-10 | 前体生物药物股份公司 | New use of glutaminyl cyclase inhibitors |
| EP2142514B1 (en) | 2007-04-18 | 2014-12-24 | Probiodrug AG | Thiourea derivatives as glutaminyl cyclase inhibitors |
| MX2007008642A (en) * | 2007-07-16 | 2009-02-25 | World Trade Imp Export Wtie Ag | Pharmaceutical composition comprising the combination of a benzisoxazolic derived agent and a reversible inhibiting agent of the cholinesterase enzyme prescribed for the control and treatment of psychotic disorders and dementias. |
| BR112012019923A2 (en) | 2010-02-09 | 2016-08-09 | Univ Johns Hopkins | methods and compositions for improving cognitive function |
| ES2586231T3 (en) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Glutaminyl cyclase inhibitors |
| DK2545047T3 (en) | 2010-03-10 | 2014-07-28 | Probiodrug Ag | Heterocyclic Inhibitors of Glutaminyl Cyclase (QC, EC 2.3.2.5) |
| WO2011131748A2 (en) | 2010-04-21 | 2011-10-27 | Probiodrug Ag | Novel inhibitors |
| ES2570167T3 (en) | 2011-03-16 | 2016-05-17 | Probiodrug Ag | Benzimidazole derivatives as glutaminyl cyclase inhibitors |
| CA2891122C (en) | 2012-11-14 | 2021-07-20 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| WO2014144663A1 (en) | 2013-03-15 | 2014-09-18 | The Johns Hopkins University | Methods and compositions for improving cognitive function |
| EP2968220B1 (en) | 2013-03-15 | 2021-05-05 | Agenebio, Inc. | Methods and compositions for improving cognitive function |
| CN107810002B (en) | 2015-05-22 | 2021-01-05 | 艾吉因生物股份有限公司 | Extended release pharmaceutical compositions of levetiracetam |
| PL3461819T3 (en) | 2017-09-29 | 2020-11-30 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
Family Cites Families (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US5336675A (en) * | 1991-05-14 | 1994-08-09 | Ernir Snorrason | Method of treating mania in humans |
| DK0584185T3 (en) * | 1991-05-14 | 2000-02-07 | Ernir Snorrason | Treatment of fatigue syndrome with cholinesterase inhibitors |
| CA2300148C (en) * | 1997-08-11 | 2009-06-23 | University Of South Florida | Nicotine antagonists for nicotine-responsive neuropsychiatric disorders |
| PT1073432E (en) * | 1998-04-14 | 2007-10-22 | Gen Hospital Corp | Use of d-serine or d-alanine for treating schizophrenia |
-
1999
- 1999-10-12 BR BR9914419-0A patent/BR9914419A/en not_active IP Right Cessation
- 1999-10-12 CN CN99812184A patent/CN1367697A/en active Pending
- 1999-10-12 AU AU64727/99A patent/AU6472799A/en not_active Abandoned
- 1999-10-12 EP EP99952580A patent/EP1121131A2/en not_active Withdrawn
- 1999-10-12 ID IDW20010828A patent/ID28441A/en unknown
- 1999-10-12 HU HU0103781A patent/HUP0103781A3/en unknown
- 1999-10-12 TR TR2001/01082T patent/TR200101082T2/en unknown
- 1999-10-12 PL PL99348107A patent/PL348107A1/en unknown
- 1999-10-12 EE EEP200100136A patent/EE200100136A/en unknown
- 1999-10-12 SK SK459-2001A patent/SK4592001A3/en unknown
- 1999-10-12 KR KR1020017002286A patent/KR20010072878A/en not_active Application Discontinuation
- 1999-10-12 WO PCT/EP1999/007804 patent/WO2000023057A2/en not_active Application Discontinuation
- 1999-10-12 JP JP2000576832A patent/JP2002527469A/en not_active Withdrawn
- 1999-10-12 CA CA002345767A patent/CA2345767A1/en not_active Abandoned
- 1999-10-12 IL IL14258899A patent/IL142588A0/en unknown
-
2001
- 2001-03-01 BG BG105302A patent/BG105302A/en unknown
- 2001-03-20 NO NO20011403A patent/NO20011403D0/en not_active Application Discontinuation
- 2001-04-10 HR HR20010262A patent/HRP20010262A2/en not_active Application Discontinuation
- 2001-04-12 ZA ZA200103081A patent/ZA200103081B/en unknown
-
2002
- 2002-01-10 HK HK02100158.6A patent/HK1039745A1/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CN1367697A (en) | 2002-09-04 |
| TR200101082T2 (en) | 2001-09-21 |
| SK4592001A3 (en) | 2001-12-03 |
| NO20011403L (en) | 2001-03-20 |
| ZA200103081B (en) | 2002-07-12 |
| NO20011403D0 (en) | 2001-03-20 |
| JP2002527469A (en) | 2002-08-27 |
| BR9914419A (en) | 2001-06-26 |
| HUP0103781A2 (en) | 2002-03-28 |
| WO2000023057A3 (en) | 2000-07-27 |
| IL142588A0 (en) | 2002-03-10 |
| EE200100136A (en) | 2002-06-17 |
| PL348107A1 (en) | 2002-05-06 |
| CA2345767A1 (en) | 2000-04-27 |
| WO2000023057A2 (en) | 2000-04-27 |
| HRP20010262A2 (en) | 2002-06-30 |
| EP1121131A2 (en) | 2001-08-08 |
| BG105302A (en) | 2001-11-30 |
| HUP0103781A3 (en) | 2003-09-29 |
| HK1039745A1 (en) | 2002-05-10 |
| ID28441A (en) | 2001-05-24 |
| KR20010072878A (en) | 2001-07-31 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| MK5 | Application lapsed section 142(2)(e) - patent request and compl. specification not accepted |