EP1121131A2 - Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition - Google Patents
Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognitionInfo
- Publication number
- EP1121131A2 EP1121131A2 EP99952580A EP99952580A EP1121131A2 EP 1121131 A2 EP1121131 A2 EP 1121131A2 EP 99952580 A EP99952580 A EP 99952580A EP 99952580 A EP99952580 A EP 99952580A EP 1121131 A2 EP1121131 A2 EP 1121131A2
- Authority
- EP
- European Patent Office
- 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.)
- Withdrawn
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
Definitions
- the present invention is concerned with pharmaceutical compositions comprising a carrier and as first active ingredient an atypical antipsychotic agent (I) and as second active ingredient an acetylcholinesterase inhibitor (H), 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 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.
- an atypical antipsychotic agent (I) for the preparation of a medicament for reducing adverse effects associated with acetylcholinesterase inhibitors (LI) in patients suffering from Alzheimer's disease or related dementias, such as nausea, vomiting, sweating, restlessness and insomnia.
- 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).
- the present invention is concerned with a pharmaceutical composition
- 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 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 ingredients by the other of the active ingredients.
- the atypical antipsychotic (I) is selected from risperidone, 9-hydroxyrisperidone or a o- 20 alkanoic acid ester thereof, olanzapine, quetiapine, iloperidone or ziprasidone, and the acetylcholinesterase inhibitor (II) is selected from galantamine, rivastigmine or donepezil, or therapeutically active acid addition salt form of any of the foregoing.
- Said salts comprise salt forms which the active ingredients (I) and (H) 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 organic acids such as, for example, acetic, propanoic, hydroxyacetic, lactic, pyruvic, oxalic, malonic, succinic, maleic, fumaric, malic, tartaric, citric, methanesulfonic, ethanesulfonic, benzenesulfonic, -toluenesulfonic, cyclamic, salicylic, p-amino- salicylic, pamoic and the like acids.
- galantamine may conveniently be used as the ( 1 : 1 ) hydrobromide salt.
- a lkanoic acids are selected from the group consisting of decanoic (capric), undecanoic, dodecanoic (lauric), tridecanoic, tetradecanoic (myristic), pentadecanoic, hexadecanoic (palmitic), heptadecanoic, octadecanoic (stearic), nonadecanoic and 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.
- the amount of each of the active ingredients is equal to or less than that which is approved in monotherapy with said active ingredient.
- compositions wherein the atypical antipsychotic (I) is risperidone and the acetylcholinesterase inhibitor (II) is galantamine, in particular as galantamine hydrobromide are particularly preferred.
- 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 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.
- an atypical antipsychotic agent I
- an acetylcholinesterase inhibitor II
- the present invention also concerns 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.
- II acetylcholinesterase inhibitor
- the present invention also concerns 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. Additionally, the present invention concerns the use of an atypical antipsychotic agent
- acetylcholinesterase inhibitors H
- Said adverse effect can be nausea, vomiting, sweating, restlessness or insomnia.
- 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).
- the present invention also concerns the use of an acetylcholinesterase inhibitor
- the atypical antipsychotic (I) is preferably risperidone and the acetylcholinesterase inhibitor (II) is preferably galantamine, in particular the (1:1) hydrobromide.
Landscapes
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Medicinal Chemistry (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Medicines Containing Plant Substances (AREA)
Abstract
Description
Claims
Priority Applications (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP99952580A EP1121131A2 (en) | 1998-10-16 | 1999-10-12 | Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition |
Applications Claiming Priority (4)
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 |
EP99952580A EP1121131A2 (en) | 1998-10-16 | 1999-10-12 | Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition |
Publications (1)
Publication Number | Publication Date |
---|---|
EP1121131A2 true EP1121131A2 (en) | 2001-08-08 |
Family
ID=8234219
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
EP99952580A Withdrawn EP1121131A2 (en) | 1998-10-16 | 1999-10-12 | Atypical antipsychotic in combination with acetylcholinesterase inhibitor 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) | NO20011403L (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 |
---|---|---|---|---|
AU2006201188B2 (en) * | 2001-02-05 | 2007-11-15 | Novartis Ag | New use of iloperidone |
GB0102841D0 (en) * | 2001-02-05 | 2001-03-21 | Novartis Ag | Organic compounds |
CN101912367A (en) | 2001-10-30 | 2010-12-15 | 诺瓦提斯公司 | The depot formulation of iloperidone and star-shape polymer |
GB0216416D0 (en) | 2002-07-15 | 2002-08-21 | Novartis Ag | Organic compounds |
WO2004084905A2 (en) * | 2003-03-24 | 2004-10-07 | University Of Florida | Use of 5-ht2c receptor activity affecting compounds 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 |
CA2552221A1 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Donepezil formulations |
AU2004325725A1 (en) * | 2004-12-10 | 2006-06-22 | Abbott Laboratories | Fused bicycloheterocycle 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 |
ATE554085T1 (en) | 2006-11-30 | 2012-05-15 | Probiodrug Ag | NEW INHIBITORS OF GLUTAMINYL CYCLASE |
EP2481408A3 (en) | 2007-03-01 | 2013-01-09 | Probiodrug AG | New use of glutaminyl cyclase inhibitors |
EP2865670B1 (en) | 2007-04-18 | 2017-01-11 | 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. |
US20110212928A1 (en) | 2010-02-09 | 2011-09-01 | The Johns Hopkins University | Methods and compositions for improving cognitive function |
ES2586231T3 (en) | 2010-03-03 | 2016-10-13 | Probiodrug Ag | Glutaminyl cyclase inhibitors |
CN102791704B (en) | 2010-03-10 | 2015-11-25 | 前体生物药物股份公司 | The heterocycle inhibitor of glutaminyl cyclase (QC, EC 2.3.2.5) |
EP2560953B1 (en) | 2010-04-21 | 2016-01-06 | Probiodrug AG | Inhibitors of glutaminyl cyclase |
US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | Methods and compositions for treating schizophrenia |
US11160785B2 (en) | 2013-03-15 | 2021-11-02 | Agenebio Inc. | Methods and compositions for improving cognitive function |
US10806717B2 (en) | 2013-03-15 | 2020-10-20 | The Johns Hopkins University | Methods and compositions for improving cognitive function |
JP6899043B2 (en) | 2015-05-22 | 2021-07-07 | エージンバイオ, インコーポレイテッド | Sustained release pharmaceutical composition 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 |
---|---|---|---|---|
DK0584185T3 (en) * | 1991-05-14 | 2000-02-07 | Ernir Snorrason | Treatment of fatigue syndrome with cholinesterase inhibitors |
US5336675A (en) * | 1991-05-14 | 1994-08-09 | Ernir Snorrason | Method of treating mania in humans |
ES2299214T3 (en) * | 1997-08-11 | 2008-05-16 | University Of South Florida | USE OF MECAMILAMINE FOR THE TREATMENT OF NEUROPSYCHIQUIATRIC DISORDERS NICOTINE. |
NZ508160A (en) * | 1998-04-14 | 2004-01-30 | Gen Hospital Corp | Methods for treating neuropsychiatric disorders |
-
1999
- 1999-10-12 CN CN99812184A patent/CN1367697A/en active Pending
- 1999-10-12 HU HU0103781A patent/HUP0103781A3/en unknown
- 1999-10-12 ID IDW20010828A patent/ID28441A/en unknown
- 1999-10-12 BR BR9914419-0A patent/BR9914419A/en not_active IP Right Cessation
- 1999-10-12 JP JP2000576832A patent/JP2002527469A/en not_active Withdrawn
- 1999-10-12 EP EP99952580A patent/EP1121131A2/en not_active Withdrawn
- 1999-10-12 IL IL14258899A patent/IL142588A0/en unknown
- 1999-10-12 CA CA002345767A patent/CA2345767A1/en not_active Abandoned
- 1999-10-12 EE EEP200100136A patent/EE200100136A/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 SK SK459-2001A patent/SK4592001A3/en unknown
- 1999-10-12 AU AU64727/99A patent/AU6472799A/en not_active Abandoned
- 1999-10-12 TR TR2001/01082T patent/TR200101082T2/en unknown
- 1999-10-12 PL PL99348107A patent/PL348107A1/en unknown
-
2001
- 2001-03-01 BG BG105302A patent/BG105302A/en unknown
- 2001-03-20 NO NO20011403A patent/NO20011403L/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
Non-Patent Citations (1)
Title |
---|
See references of WO0023057A2 * |
Also Published As
Publication number | Publication date |
---|---|
HUP0103781A2 (en) | 2002-03-28 |
ZA200103081B (en) | 2002-07-12 |
WO2000023057A2 (en) | 2000-04-27 |
ID28441A (en) | 2001-05-24 |
PL348107A1 (en) | 2002-05-06 |
KR20010072878A (en) | 2001-07-31 |
CN1367697A (en) | 2002-09-04 |
AU6472799A (en) | 2000-05-08 |
IL142588A0 (en) | 2002-03-10 |
NO20011403D0 (en) | 2001-03-20 |
SK4592001A3 (en) | 2001-12-03 |
JP2002527469A (en) | 2002-08-27 |
BR9914419A (en) | 2001-06-26 |
CA2345767A1 (en) | 2000-04-27 |
WO2000023057A3 (en) | 2000-07-27 |
NO20011403L (en) | 2001-03-20 |
HRP20010262A2 (en) | 2002-06-30 |
HK1039745A1 (en) | 2002-05-10 |
BG105302A (en) | 2001-11-30 |
TR200101082T2 (en) | 2001-09-21 |
HUP0103781A3 (en) | 2003-09-29 |
EE200100136A (en) | 2002-06-17 |
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