EP1121131A2 - Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition - Google Patents

Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition

Info

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Withdrawn
Application number
EP99952580A
Other languages
German (de)
English (en)
French (fr)
Inventor
Paul Leonce Irma De Nijs
Wim Louis Julien Parys
Current Assignee (The listed assignees may be inaccurate. Google has not performed a legal analysis and makes no representation or warranty as to the accuracy of the list.)
Janssen Pharmaceutica NV
Original Assignee
Janssen Pharmaceutica NV
Priority date (The priority date 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 date listed.)
Filing date
Publication date
Application filed by Janssen Pharmaceutica NV filed Critical Janssen Pharmaceutica NV
Priority to EP99952580A priority Critical patent/EP1121131A2/en
Publication of EP1121131A2 publication Critical patent/EP1121131A2/en
Withdrawn legal-status Critical Current

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)
  • Public Health (AREA)
  • Chemical & Material Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Neurology (AREA)
  • General Chemical & Material Sciences (AREA)
  • Biomedical Technology (AREA)
  • Organic Chemistry (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Epidemiology (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)
EP99952580A 1998-10-16 1999-10-12 Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition Withdrawn EP1121131A2 (en)

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
EP99952580A EP1121131A2 (en) 1998-10-16 1999-10-12 Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition
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
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 (id)
JP (1) JP2002527469A (id)
KR (1) KR20010072878A (id)
CN (1) CN1367697A (id)
AU (1) AU6472799A (id)
BG (1) BG105302A (id)
BR (1) BR9914419A (id)
CA (1) CA2345767A1 (id)
EE (1) EE200100136A (id)
HK (1) HK1039745A1 (id)
HR (1) HRP20010262A2 (id)
HU (1) HUP0103781A3 (id)
ID (1) ID28441A (id)
IL (1) IL142588A0 (id)
NO (1) NO20011403L (id)
PL (1) PL348107A1 (id)
SK (1) SK4592001A3 (id)
TR (1) TR200101082T2 (id)
WO (1) WO2000023057A2 (id)
ZA (1) ZA200103081B (id)

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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
ES2436439T3 (es) 2001-10-30 2014-01-02 Novartis Ag Formulaciones de medicamento de liberación lenta de iloperidona con un polímero
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
EP1824848A1 (en) * 2004-12-10 2007-08-29 Abbott Laboratories Fused bicycloheterocycle substituted quinuclidine derivatives
WO2005065645A2 (en) * 2003-12-31 2005-07-21 Actavis Group Hf Donepezil formulations
EP2089383B1 (en) 2006-11-09 2015-09-16 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
AU2008220785B2 (en) 2007-03-01 2013-02-21 Vivoryon Therapeutics N.V. New use of glutaminyl cyclase inhibitors
JP5667440B2 (ja) 2007-04-18 2015-02-12 プロビオドルグ エージー グルタミニルシクラーゼ阻害剤としてのチオ尿素誘導体
MX2007008642A (es) * 2007-07-16 2009-02-25 World Trade Imp Export Wtie Ag Composicion farmaceutica que comprende la combinacion de un agente derivado benzisoxazolico y un agente inhibidor reversible de la enzima colinesterasa, indicada para el control y tratamiento de trastornos psicoticos y demencias.
EA202092673A3 (ru) 2010-02-09 2021-05-31 Дзе Джонс Хопкинс Юниверсити Способы и композиции для улучшения когнитивной функции
WO2011107530A2 (en) 2010-03-03 2011-09-09 Probiodrug Ag Novel inhibitors
JP5688745B2 (ja) 2010-03-10 2015-03-25 プロビオドルグ エージー グルタミニルシクラーゼ（ｑｃ、ｅｃ２．３．２．５）の複素環阻害剤
WO2011131748A2 (en) 2010-04-21 2011-10-27 Probiodrug Ag Novel inhibitors
EP2686313B1 (en) 2011-03-16 2016-02-03 Probiodrug AG Benzimidazole derivatives as inhibitors of glutaminyl cyclase
US20140206667A1 (en) 2012-11-14 2014-07-24 Michela Gallagher Methods and compositions for treating schizophrenia
AU2014228512A1 (en) 2013-03-15 2015-10-01 Agenebio, Inc. Methods and compositions for improving cognitive function
WO2014144663A1 (en) 2013-03-15 2014-09-18 The Johns Hopkins University Methods and compositions for improving cognitive function
CA2986598C (en) 2015-05-22 2023-09-26 Agenebio, Inc. Extended release pharmaceutical compositions of levetiracetam
ES2812698T3 (es) 2017-09-29 2021-03-18 Probiodrug Ag Inhibidores de glutaminil ciclasa

Family Cites Families (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5336675A (en) * 1991-05-14 1994-08-09 Ernir Snorrason Method of treating mania in humans
EP0584185B1 (en) * 1991-05-14 1999-08-11 Ernir Snorrason Treatment of fatigue syndrome with cholinesterase inhibitors
AU8778498A (en) * 1997-08-11 1999-03-01 University Of South Florida Research Foundation, Inc. Nicotine antagonists for nicotine-responsive neuropsychiatric disorders
DE1073432T1 (de) * 1998-04-14 2002-02-07 The General Hospital Corp., Boston Verwendung von glycinrezeptoragonisten und glycinaufnahmeinhibitoren zur behandlung neuropsychiatrischer beschwerden

Non-Patent Citations (1)

* Cited by examiner, † Cited by third party
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See references of WO0023057A2 *

Also Published As

Publication number Publication date
NO20011403D0 (no) 2001-03-20
HUP0103781A2 (hu) 2002-03-28
HRP20010262A2 (en) 2002-06-30
AU6472799A (en) 2000-05-08
NO20011403L (no) 2001-03-20
KR20010072878A (ko) 2001-07-31
BG105302A (en) 2001-11-30
BR9914419A (pt) 2001-06-26
CN1367697A (zh) 2002-09-04
ZA200103081B (en) 2002-07-12
WO2000023057A2 (en) 2000-04-27
ID28441A (id) 2001-05-24
HK1039745A1 (zh) 2002-05-10
HUP0103781A3 (en) 2003-09-29
PL348107A1 (en) 2002-05-06
SK4592001A3 (en) 2001-12-03
JP2002527469A (ja) 2002-08-27
EE200100136A (et) 2002-06-17
WO2000023057A3 (en) 2000-07-27
TR200101082T2 (tr) 2001-09-21
CA2345767A1 (en) 2000-04-27
IL142588A0 (en) 2002-03-10

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