EP1121131A2 - Therapie visant a ameliorer la cognition - Google Patents

Therapie visant a ameliorer la 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Withdrawn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)
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/fr
Publication of EP1121131A2 publication Critical patent/EP1121131A2/fr
Withdrawn legal-status Critical Current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)
  • 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)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Organic Chemistry (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (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)

Abstract

Cette invention a trait à des compositions pharmaceutiques renfermant un excipient et, comme premier ingrédient actif, un agent antipsychotique atypique (I), ainsi que, comme second ingrédient actif, un inhibiteur de l'acétylcholinestérase (II), chacun sous des quantités produisant un effet thérapeutique bénéfique chez des patients atteints de psychose, de la maladie d'Alzheimer ou de démences connexes. Cet effet thérapeutique bénéfique peut être un effet de synergie sur le fonctionnement cognitif de patients atteints de la maladie d'Alzheimer ou de démences connexes, être prophylactique, évitant une dégradation ultérieure de la cognition chez ces patients, ou encore atténuant les réactions indésirables dues à l'action sur l'un des ingrédients actifs des autres ingrédients actifs.
EP99952580A 1998-10-16 1999-10-12 Therapie visant a ameliorer la cognition Withdrawn EP1121131A2 (fr)

Priority Applications (1)

Application Number Priority Date Filing Date Title
EP99952580A EP1121131A2 (fr) 1998-10-16 1999-10-12 Therapie visant a ameliorer la cognition

Applications Claiming Priority (4)

Application Number Priority Date Filing Date Title
EP98203454 1998-10-16
EP98203454 1998-10-16
EP99952580A EP1121131A2 (fr) 1998-10-16 1999-10-12 Therapie visant a ameliorer la cognition
PCT/EP1999/007804 WO2000023057A2 (fr) 1998-10-16 1999-10-12 Therapie visant a ameliorer la cognition

Publications (1)

Publication Number Publication Date
EP1121131A2 true EP1121131A2 (fr) 2001-08-08

Family

ID=8234219

Family Applications (1)

Application Number Title Priority Date Filing Date
EP99952580A Withdrawn EP1121131A2 (fr) 1998-10-16 1999-10-12 Therapie visant a ameliorer la cognition

Country Status (20)

Country Link
EP (1) EP1121131A2 (fr)
JP (1) JP2002527469A (fr)
KR (1) KR20010072878A (fr)
CN (1) CN1367697A (fr)
AU (1) AU6472799A (fr)
BG (1) BG105302A (fr)
BR (1) BR9914419A (fr)
CA (1) CA2345767A1 (fr)
EE (1) EE200100136A (fr)
HK (1) HK1039745A1 (fr)
HR (1) HRP20010262A2 (fr)
HU (1) HUP0103781A3 (fr)
ID (1) ID28441A (fr)
IL (1) IL142588A0 (fr)
NO (1) NO20011403L (fr)
PL (1) PL348107A1 (fr)
SK (1) SK4592001A3 (fr)
TR (1) TR200101082T2 (fr)
WO (1) WO2000023057A2 (fr)
ZA (1) ZA200103081B (fr)

Families Citing this family (23)

* Cited by examiner, † Cited by third party
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
DE60238780D1 (de) * 2001-10-30 2011-02-10 Novartis Ag Depot formulierungen von iloperidone und einem sternförmigen polymer
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 (fr) * 2004-12-10 2007-08-29 Abbott Laboratories Derives polycycliques de quinuclidine substitues par un bicycloheterocycle condense
US20050232990A1 (en) * 2003-12-31 2005-10-20 Garth Boehm Donepezil formulations
WO2008055945A1 (fr) 2006-11-09 2008-05-15 Probiodrug Ag Dérivés 3-hydr0xy-1,5-dihydr0-pyrr0l-2-one utiles en tant qu' inhibiteurs de la glutaminyl-cyclase dans le traitement des ulcères, du cancer et d'autres maladies
ATE554085T1 (de) 2006-11-30 2012-05-15 Probiodrug Ag Neue inhibitoren von glutaminylcyclase
EP2117540A1 (fr) 2007-03-01 2009-11-18 Probiodrug AG Nouvelle utilisation d'inhibiteurs de la glutaminyl cyclase
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.
EP2533645B1 (fr) 2010-02-09 2016-07-27 The Johns Hopkins University Procédés et compositions pour améliorer la fonction cognitive
US9181233B2 (en) 2010-03-03 2015-11-10 Probiodrug Ag Inhibitors of glutaminyl cyclase
AU2011226074B2 (en) 2010-03-10 2015-01-22 Vivoryon Therapeutics N.V. Heterocyclic inhibitors of glutaminyl cyclase (QC, EC 2.3.2.5)
US8541596B2 (en) 2010-04-21 2013-09-24 Probiodrug Ag Inhibitors
ES2570167T3 (es) 2011-03-16 2016-05-17 Probiodrug Ag Derivados de benzimidazol como inhibidores de glutaminil ciclasa
EP2919788A4 (fr) 2012-11-14 2016-05-25 Univ Johns Hopkins Méthodes et compositions pour le traitement de la schizophrénie
EP2968237A4 (fr) 2013-03-15 2016-08-31 Univ Johns Hopkins Procédés et compositions pour améliorer la fonction cognitive
DK2968220T3 (da) 2013-03-15 2021-06-14 Agenebio Inc Fremgangsmåder og sammensætninger til forbedring af kognitiv funktion
BR112017025031B1 (pt) 2015-05-22 2023-03-21 Agenebio, Inc Composições farmacêuticas de liberação prolongada de 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
DK0584185T3 (da) * 1991-05-14 2000-02-07 Ernir Snorrason Behandling af træthedssyndrom med cholinesteraseinhibitorer
US5336675A (en) * 1991-05-14 1994-08-09 Ernir Snorrason Method of treating mania in humans
DK1011678T3 (da) * 1997-08-11 2008-05-05 Univ South Florida Anvendelse af mecamylamin til behandling af nikotin-responsive neuropsykiatriske lidelser
IL139008A0 (en) * 1998-04-14 2001-11-25 Gen Hospital Corp Methods for treating neuropsychiatric disorders

Non-Patent Citations (1)

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

Also Published As

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

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