SK4592001A3 - Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition - Google Patents
Atypical antipsychotic in combination with acetylcholinesterase inhibitor for improving cognition Download PDFInfo
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- atypical antipsychotic
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- antipsychotic agent
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- 239000003693 atypical antipsychotic agent Substances 0.000 title claims abstract description 24
- 239000000544 cholinesterase inhibitor Substances 0.000 title claims abstract description 13
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 title claims abstract description 12
- 230000019771 cognition Effects 0.000 title abstract 2
- 229940127236 atypical antipsychotics Drugs 0.000 title 1
- 239000004480 active ingredient Substances 0.000 claims abstract description 26
- 239000003112 inhibitor Substances 0.000 claims abstract description 21
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 17
- 206010012289 Dementia Diseases 0.000 claims abstract description 16
- 230000000694 effects Effects 0.000 claims abstract description 16
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 10
- 230000002411 adverse Effects 0.000 claims abstract description 9
- 230000009286 beneficial effect Effects 0.000 claims abstract description 7
- 230000006866 deterioration Effects 0.000 claims abstract description 4
- 230000002195 synergetic effect Effects 0.000 claims abstract description 4
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 3
- ASUTZQLVASHGKV-JDFRZJQESA-N galanthamine Chemical compound O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 ASUTZQLVASHGKV-JDFRZJQESA-N 0.000 claims description 18
- 238000002360 preparation method Methods 0.000 claims description 15
- 230000003920 cognitive function Effects 0.000 claims description 11
- 239000003814 drug Substances 0.000 claims description 11
- 102000012440 Acetylcholinesterase Human genes 0.000 claims description 10
- 108010022752 Acetylcholinesterase Proteins 0.000 claims description 10
- 229940022698 acetylcholinesterase Drugs 0.000 claims description 10
- 229960003980 galantamine Drugs 0.000 claims description 9
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 claims description 9
- 239000002253 acid Substances 0.000 claims description 8
- 229960001534 risperidone Drugs 0.000 claims description 7
- RAPZEAPATHNIPO-UHFFFAOYSA-N risperidone Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCCC4=NC=3C)=NOC2=C1 RAPZEAPATHNIPO-UHFFFAOYSA-N 0.000 claims description 7
- 150000002148 esters Chemical class 0.000 claims description 6
- 208000008454 Hyperhidrosis Diseases 0.000 claims description 3
- 208000001431 Psychomotor Agitation Diseases 0.000 claims description 3
- 206010038743 Restlessness Diseases 0.000 claims description 3
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 3
- 206010047700 Vomiting Diseases 0.000 claims description 3
- 206010022437 insomnia Diseases 0.000 claims description 3
- 230000035900 sweating Effects 0.000 claims description 3
- 230000008673 vomiting Effects 0.000 claims description 3
- PMXMIIMHBWHSKN-UHFFFAOYSA-N 3-{2-[4-(6-fluoro-1,2-benzoxazol-3-yl)piperidin-1-yl]ethyl}-9-hydroxy-2-methyl-6,7,8,9-tetrahydropyrido[1,2-a]pyrimidin-4-one Chemical compound FC1=CC=C2C(C3CCN(CC3)CCC=3C(=O)N4CCCC(O)C4=NC=3C)=NOC2=C1 PMXMIIMHBWHSKN-UHFFFAOYSA-N 0.000 claims description 2
- 208000012661 Dyskinesia Diseases 0.000 claims description 2
- 208000027776 Extrapyramidal disease Diseases 0.000 claims description 2
- 206010028813 Nausea Diseases 0.000 claims description 2
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical compound CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 claims description 2
- 239000002552 dosage form Substances 0.000 claims description 2
- 229960003162 iloperidone Drugs 0.000 claims description 2
- XMXHEBAFVSFQEX-UHFFFAOYSA-N iloperidone Chemical compound COC1=CC(C(C)=O)=CC=C1OCCCN1CCC(C=2C3=CC=C(F)C=C3ON=2)CC1 XMXHEBAFVSFQEX-UHFFFAOYSA-N 0.000 claims description 2
- 230000008693 nausea Effects 0.000 claims description 2
- 229960005017 olanzapine Drugs 0.000 claims description 2
- KVWDHTXUZHCGIO-UHFFFAOYSA-N olanzapine Chemical compound C1CN(C)CCN1C1=NC2=CC=CC=C2NC2=C1C=C(C)S2 KVWDHTXUZHCGIO-UHFFFAOYSA-N 0.000 claims description 2
- 229960004431 quetiapine Drugs 0.000 claims description 2
- URKOMYMAXPYINW-UHFFFAOYSA-N quetiapine Chemical compound C1CN(CCOCCO)CCN1C1=NC2=CC=CC=C2SC2=CC=CC=C12 URKOMYMAXPYINW-UHFFFAOYSA-N 0.000 claims description 2
- 229960004136 rivastigmine Drugs 0.000 claims description 2
- 238000009097 single-agent therapy Methods 0.000 claims description 2
- 229960000607 ziprasidone Drugs 0.000 claims description 2
- MVWVFYHBGMAFLY-UHFFFAOYSA-N ziprasidone Chemical compound C1=CC=C2C(N3CCN(CC3)CCC3=CC=4CC(=O)NC=4C=C3Cl)=NSC2=C1 MVWVFYHBGMAFLY-UHFFFAOYSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 5
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical compound O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims 2
- 206010067484 Adverse reaction Diseases 0.000 claims 1
- 230000006838 adverse reaction Effects 0.000 claims 1
- 229960003530 donepezil Drugs 0.000 claims 1
- 230000001225 therapeutic effect Effects 0.000 claims 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 150000007513 acids Chemical class 0.000 description 5
- 150000003839 salts Chemical class 0.000 description 3
- CPELXLSAUQHCOX-UHFFFAOYSA-N Hydrogen bromide Chemical class Br CPELXLSAUQHCOX-UHFFFAOYSA-N 0.000 description 2
- -1 hydrohalic acids Chemical class 0.000 description 2
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- COVZYZSDYWQREU-UHFFFAOYSA-N Busulfan Chemical compound CS(=O)(=O)OCCCCOS(C)(=O)=O COVZYZSDYWQREU-UHFFFAOYSA-N 0.000 description 1
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 1
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 1
- 229960004373 acetylcholine Drugs 0.000 description 1
- 229960002024 galantamine hydrobromide Drugs 0.000 description 1
- QORVDGQLPPAFRS-XPSHAMGMSA-N galantamine hydrobromide Chemical compound Br.O1C(=C23)C(OC)=CC=C2CN(C)CC[C@]23[C@@H]1C[C@@H](O)C=C2 QORVDGQLPPAFRS-XPSHAMGMSA-N 0.000 description 1
- 150000007522 mineralic acids Chemical class 0.000 description 1
- 239000003921 oil Substances 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000005985 organic acids Nutrition 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-N palmitic acid group Chemical group C(CCCCCCCCCCCCCCC)(=O)O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 1
- 125000002958 pentadecyl group Chemical group [H]C([*])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])C([H])([H])[H] 0.000 description 1
- 239000000825 pharmaceutical preparation Substances 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
Classifications
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- 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
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- 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)
- Organic Chemistry (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurosurgery (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)
Abstract
Description
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Liečba zlepšujúca kognitívne funkcieTreatment improving cognitive function
Oblasť technikyTechnical field
Predkladaný vynález sa týka farmaceutických preparátov obsahujúcich nosič a atypickú antipsychotickú látku (I) ako prvú aktívnu zložku, a inhibítor acetylcholinesterázy (II) ako druhú aktívnu zložku, každú obsiahnutú v množstve vytvárajúcom terapeuticky prospešný efekt pacientov trpiacich psychózou, Alzheimerovou chorobou, alebo príbuznými demenciami. Spomínaný terapeuticky prospešný efekt môže byť synergistickým efektom na kognitívne funkcie pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami, alebo prevenciou ďalšieho zhoršovania kognitívnych funkcií spomínaných pacientov, alebo môže znižovať nežiadúce účinky spojené s jednou z aktívnych zložiek pomocou inej aktívnej zložky.The present invention relates to pharmaceutical compositions comprising a carrier and an atypical antipsychotic agent (I) as the first active ingredient, and an acetylcholinesterase inhibitor (II) as the second active ingredient, each contained in an amount producing a therapeutically beneficial effect for patients suffering from psychosis, Alzheimer's disease or related dementia. Said therapeutically beneficial effect may be a synergistic effect on the cognitive functions of patients suffering from Alzheimer's disease or related dementias, or preventing further deterioration of the cognitive functions of said patients, or it may reduce the adverse effects associated with one of the active ingredients with another active ingredient.
Doterajší stav technikyBACKGROUND OF THE INVENTION
Špecifickým záujmom je použitie atypickej antipsychotickej látky (I) na prípravu lieku znižujúceho nežiadúce účinky spojené s inhibítormi acetylcholinesterázy (II), ako sú napríklad neusea, zvracanie, potenie, neklud a nespavosť, pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami. Obzvlášť zaujímavým je použitie atypickej antipsychotickej látky (I) na prípravu lieku zlepšujúceho spánok pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami, ktorí sú liečení inhibítormi acetylcholinesterázy (II).Of particular interest is the use of an atypical antipsychotic agent (I) for the preparation of a medicament for reducing the adverse effects associated with acetylcholinesterase (II) inhibitors such as neusea, vomiting, sweating, restlessness and insomnia in patients suffering from Alzheimer's disease or related dementias. Of particular interest is the use of an atypical antipsychotic agent (I) for the preparation of a medicament for improving sleep sleep in patients suffering from Alzheimer's disease or related dementias who are treated with acetylcholinesterase (II) inhibitors.
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Opis vynálezuDescription of the invention
Predkladaný vynález sa týka farmaceutických preparátov obsahujúcich nosič a atypickú antipsychotickú látku (I) ako prvú aktívnu zložku, a inhibítor acetylcholinesterázy (II) ako druhú aktívnu zložku, každú obsiahnutú v množstve vytvárajúcom terapeuticky prospešný efekt pacientom trpiacich psychózou, Alzheimerovou chorobou, alebo príbuznými demenciami.The present invention relates to pharmaceutical preparations comprising a carrier and an atypical antipsychotic agent (I) as the first active ingredient, and an acetylcholinesterase inhibitor (II) as the second active ingredient, each contained in an amount producing a therapeutically beneficial effect for patients suffering from psychosis, Alzheimer's disease or related.
Spomínaný terapeuticky prospešný efekt môže byť synergistickým efektom na kognitívne funkcie pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami, alebo prevenciou ďalšieho zhoršovania kognitívnych funkcií spomínaných pacientov, alebo môže znižovať nežiadúce účinky spojené s jednou z aktívnych zložiek pomocou inej aktívnej zložky.Said therapeutically beneficial effect may be a synergistic effect on the cognitive functions of patients suffering from Alzheimer's disease or related dementias, or preventing further deterioration of the cognitive functions of said patients, or it may reduce the adverse effects associated with one of the active ingredients with another active ingredient.
Atypická antipsychotická látka (I) je vybraná z risperidónu, 9-hydroxyrisperidónu, alebo jeho esteru C10-20 alkánovej kyseliny, olanzapínu, quetiapínu,iloperidónu alebo ziprasidónu, a inhibítor acetylcholinesterázy (II) je vybraný z galantamínu, rivastigmínu alebo donepezilu, alebo terapeuticky aktívnej kyslej adičnej soli akejkoľvek z predchádzajúcich látok. Spomínané soli zahŕňajú formy solí, ktoré sú aktívne zložky (I) a (II) schopné vytvárať s príslušnými kyselinami, ako sú napríklad anorganické kyseliny, ako napríklad kyseliny hydrohalové, napríklad kyselina chlorovodíková a bromovodíková; sírová, dusičná, fosforečná a podobné kyseliny, alebo organické kyseliny, ako sú napríklad kyselina octová, propánová, hydroxyoctová, mliečna, pyrohroznová, šťavelová, malónová, jantárová, pyrogalólová, fumárová, jablčná, vinná, citrónová, metansulfonová, etansulfonová, benzensulfonová,p-toluénsulfonová, cyklamová, β· *·· ·· ·· ·· s ··· · · · · a a *!The atypical antipsychotic agent (I) is selected from risperidone, 9-hydroxyrisperidone, or a C10-20 alkanoic acid ester, olanzapine, quetiapine, iloperidone or ziprasidone, and the acetylcholinesterase (II) inhibitor is selected from galantamine, rivastigmine or donepeziline an acid addition salt of any of the foregoing. Said salts include the salt forms which the active ingredients (I) and (II) are able to form with the corresponding acids, such as inorganic acids such as hydrohalic acids, for example hydrochloric and hydrobromic acid; sulfuric, nitric, phosphoric and the like acids, or organic acids such as acetic, propanoic, hydroxyacetic, lactic, pyruvic, oxalic, malonic, succinic, pyrogallic, fumaric, malic, tartaric, methanesulfonic, ethanesulfonic, benzenesulfonic, benzenesulfonic toluenesulfonic, cyclamic, β * · · · · · · · · · · · · · to · a *!
J · · · · · ··· a · a a ··· ·· ·· ·· ·· aaa salicylová, p-amínosalicylová, pamoová a podobné kyseliny. Napríklad galantamín môže byť pohodlne použitý ako (1:1) hydrobromidová sol.J and a and a and salicylic, β-aminosalicylic, pamoic and the like acids. For example, galantamine can conveniently be used as the (1: 1) hydrobromide salt.
Cio-20 alkánové kyseliny sú vybrané zo skupiny obsahujúcej kyselinu dekanoovú (kaprxnová), undekanoová, dodekanoová (laurová), tridekanoová, tetradekanoová (myristová), pentadekanoová, hexadekanoová (palmitová), heptadekanoová, oktadekanoová (stearová), nonadekanoová a eikosanoová. V dôsledku ich obmedzenej rozpustnosti vo vode sa všeobecne domnievalo, že estery musia byť rozpustené v olejoch. Ester majúci C15 (pentadecylový) reťazec a aktívnu zložku zodpovedajúcu esteru 9-hydroxysperidón palminátu bol zistený ako najlepší ester z pohladu farmakokinetiky, rovnako tak, ako z pohladu tolerancie.The C 10-20 alkanoic acids are selected from the group consisting of decanoic (caproic), undecanoic, dodecanoic (lauric), tridecanoic, tetradecanoic (myristic), pentadecanoic, hexadecanoic (palmitic), heptadecanoic, octadecanoic (stearic), eosadanoic. Due to their limited solubility in water, it was generally believed that esters had to be dissolved in oils. The ester having the C15 (pentadecyl) chain and the active ingredient corresponding to the 9-hydroxysperidone palminate ester was found to be the best ester in terms of pharmacokinetics as well as in terms of tolerance.
Množstvo každej z aktívnych látok je prednostne rovnaké, alebo nižšie ako ktoré je schválené na monoterapiu spomínanou aktívnou zložkou.The amount of each of the active ingredients is preferably equal to or less than that which is approved for monotherapy with said active ingredient.
Najprednostnejšie sú preparáty, kde atypickou antipsychotickou látkou (I) je risperidón a inhibítorom acetylcholinesterázy (II) je galantamín, predovšetkým ako galantamín hydrobromid. V spomínaných preparátoch je množstvo resperidónu 0,5, 1, 2, 4, alebo 6 mg a množstvo galantamínu (vo forme bázi) je 8, 16, 24, alebo 32 na dávkovú formu.Most preferred are preparations wherein the atypical antipsychotic agent (I) is risperidone and the acetylcholinesterase (II) inhibitor is galantamine, especially as galantamine hydrobromide. In said preparations, the amount of resperidone is 0.5, 1, 2, 4, or 6 mg, and the amount of galantamine (as base) is 8, 16, 24, or 32 per dosage form.
Predkladaný vynález sa týka tiež produktov obsahujúcich atypickú antipsychotickú látku (I) ako prvú aktívnu zložku, a inhibitor acetylcholinesterázy (II) ako druhú aktívnu zložku, ako kombinované preparáty na súčasné, oddelené alebo postupné použitie v liečbe pacientov trpiacich psychózou, Alzheimerovou chorobou alebo príbuznými demenciami.The present invention also relates to products comprising an atypical antipsychotic agent (I) as the first active ingredient, and an acetylcholinesterase inhibitor (II) as the second active ingredient, as a combination preparation for simultaneous, separate or sequential use in the treatment of patients suffering from psychosis, Alzheimer's disease or related dementias .
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Predkladný vynález sa tiež týka použitia inhibítora acetylcholinesterázy (II) na prípravu lieku zvyšujúceho účinok atypickej antipsychotickej látky (I) na kognitívne funkcie pacientov trpiacich psychózou.The present invention also relates to the use of an acetylcholinesterase inhibitor (II) for the preparation of a medicament for increasing the effect of an atypical antipsychotic agent (I) on the cognitive functions of patients suffering from psychosis.
Na druhú stranu sa vynález tiež týka použitia atypickej antipsychotickej látky (I) na prípravu lieku zvyšujúceho účinok inhibítora acetylcholinesterázy (II) na kognitívne funkcie pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami.On the other hand, the invention also relates to the use of an atypical antipsychotic agent (I) for the preparation of a medicament for increasing the effect of an acetylcholinesterase (II) inhibitor on the cognitive functions of patients suffering from Alzheimer's disease or related dementias.
Naviac sa predkladaný vynález týka použitia atypickej antipsychotickej látky (I) na prípravu lieku znižujúceho nežiadúce účinky spojené s inhibítormi acetylcholinesterázy (II) pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami. Spomínaným nežiadúcim účinkom môže byť nausea,zvracanie, potenie, neklud alebo nespavosť. Obzvlášť zaujímavé je použitie atypickej antipsychotickej látky (I) na prípravu lieku zlepšujúceho spánok pacientov trpiacich Alzheimerovou chorobou alebo príbuznými demenciami, ktorí sú liečení inhibítormi acetylcholinesterázy (II) .In addition, the present invention relates to the use of an atypical antipsychotic agent (I) for the preparation of a medicament for reducing the adverse effects associated with acetylcholinesterase (II) inhibitors in patients suffering from Alzheimer's disease or related dementias. Said side effect may be nausea, vomiting, sweating, restlessness or insomnia. Of particular interest is the use of an atypical antipsychotic agent (I) for the preparation of a medicament for improving sleep sleep in patients suffering from Alzheimer's disease or related dementias who are treated with acetylcholinesterase (II) inhibitors.
Predkladaný vynález sa nakoniec týka použitia inhibítora acetylcholinestrázy (II) na prípravu lieku znižujúceho nežiadúce účinky spojené s atypickými antipsychotickými látkami (I) pacientov trpiacich psychózami. Spomínaný nežiadúci účinok môže byť extrapyramídovým syndrómom alebo pozvoľne sa vyvíjajúcou dyskinéziou.Finally, the present invention relates to the use of an acetylcholine estrase inhibitor (II) for the preparation of a medicament for reducing adverse effects associated with atypical antipsychotic agents (I) in patients suffering from psychoses. Said side effect may be extrapyramidal syndrome or slowly developing dyskinesia.
Vo všetkých predchádzajúcich použitiach je atypickou antipsychotickou látkou (I) prednostne risperidón a inhibítorom acetylcholinesterázy (II) je prednostne galantamín, obzvlášť hydrobromid (1:1).In all previous uses, the atypical antipsychotic agent (I) is preferably risperidone and the acetylcholinesterase (II) inhibitor is preferably galantamine, especially hydrobromide (1: 1).
Claims (14)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| 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 |
|---|---|
| SK4592001A3 true SK4592001A3 (en) | 2001-12-03 |
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| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SK459-2001A SK4592001A3 (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) | 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 |
|---|---|---|---|---|
| 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 |
| CA2463158C (en) | 2001-10-30 | 2013-07-30 | Novartis Ag | Depot formulations of iloperidone and a star 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 |
| 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 |
| JP5379692B2 (en) | 2006-11-09 | 2013-12-25 | プロビオドルグ エージー | 3-Hydroxy-1,5-dihydro-pyrrol-2-one derivatives as inhibitors of glutaminyl cyclase for the treatment of ulcers, cancer and other diseases |
| DK2091948T3 (en) | 2006-11-30 | 2012-07-23 | Probiodrug Ag | Novel inhibitors of glutaminyl cyclase |
| AU2008220785B2 (en) | 2007-03-01 | 2013-02-21 | Vivoryon Therapeutics N.V. | New use of glutaminyl cyclase inhibitors |
| US9656991B2 (en) | 2007-04-18 | 2017-05-23 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| 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. |
| CA2789014C (en) | 2010-02-09 | 2019-01-15 | Michela Gallagher | Methods and compositions for improving cognitive function |
| JP6026284B2 (en) | 2010-03-03 | 2016-11-16 | プロビオドルグ エージー | Inhibitors of glutaminyl cyclase |
| EA022420B1 (en) | 2010-03-10 | 2015-12-30 | Пробиодруг Аг | 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 |
| US20140206667A1 (en) | 2012-11-14 | 2014-07-24 | Michela Gallagher | 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 |
| CN105142623A (en) | 2013-03-15 | 2015-12-09 | 艾吉因生物股份有限公司 | 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 |
| ES2812698T3 (en) | 2017-09-29 | 2021-03-18 | Probiodrug Ag | Glutaminyl cyclase inhibitors |
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 |
| JP4640888B2 (en) * | 1997-08-11 | 2011-03-02 | ザ ユニヴァーシティー オブ サウス フロリダ | Nicotine antagonists for neuropsychiatric disorders |
| WO1999052519A2 (en) * | 1998-04-14 | 1999-10-21 | The General Hospital Corporation | Methods for treating neuropsychiatric disorders |
-
1999
- 1999-10-12 CA CA002345767A patent/CA2345767A1/en not_active Abandoned
- 1999-10-12 EE EEP200100136A patent/EE200100136A/en unknown
- 1999-10-12 PL PL99348107A patent/PL348107A1/en unknown
- 1999-10-12 AU AU64727/99A patent/AU6472799A/en not_active Abandoned
- 1999-10-12 ID IDW20010828A patent/ID28441A/en unknown
- 1999-10-12 HU HU0103781A patent/HUP0103781A3/en unknown
- 1999-10-12 SK SK459-2001A patent/SK4592001A3/en unknown
- 1999-10-12 TR TR2001/01082T patent/TR200101082T2/en unknown
- 1999-10-12 KR KR1020017002286A patent/KR20010072878A/en not_active Withdrawn
- 1999-10-12 WO PCT/EP1999/007804 patent/WO2000023057A2/en not_active Ceased
- 1999-10-12 HR HR20010262A patent/HRP20010262A2/en not_active Application Discontinuation
- 1999-10-12 CN CN99812184A patent/CN1367697A/en active Pending
- 1999-10-12 HK HK02100158.6A patent/HK1039745A1/en unknown
- 1999-10-12 IL IL14258899A patent/IL142588A0/en unknown
- 1999-10-12 JP JP2000576832A patent/JP2002527469A/en not_active Withdrawn
- 1999-10-12 BR BR9914419-0A patent/BR9914419A/en not_active IP Right Cessation
- 1999-10-12 EP EP99952580A patent/EP1121131A2/en not_active Withdrawn
-
2001
- 2001-03-01 BG BG105302A patent/BG105302A/en unknown
- 2001-03-20 NO NO20011403A patent/NO20011403D0/en not_active Application Discontinuation
- 2001-04-12 ZA ZA200103081A patent/ZA200103081B/en unknown
Also Published As
| Publication number | Publication date |
|---|---|
| HRP20010262A2 (en) | 2002-06-30 |
| JP2002527469A (en) | 2002-08-27 |
| WO2000023057A3 (en) | 2000-07-27 |
| NO20011403L (en) | 2001-03-20 |
| PL348107A1 (en) | 2002-05-06 |
| ID28441A (en) | 2001-05-24 |
| CN1367697A (en) | 2002-09-04 |
| CA2345767A1 (en) | 2000-04-27 |
| BG105302A (en) | 2001-11-30 |
| EE200100136A (en) | 2002-06-17 |
| AU6472799A (en) | 2000-05-08 |
| EP1121131A2 (en) | 2001-08-08 |
| BR9914419A (en) | 2001-06-26 |
| HUP0103781A3 (en) | 2003-09-29 |
| KR20010072878A (en) | 2001-07-31 |
| TR200101082T2 (en) | 2001-09-21 |
| IL142588A0 (en) | 2002-03-10 |
| NO20011403D0 (en) | 2001-03-20 |
| HK1039745A1 (en) | 2002-05-10 |
| HUP0103781A2 (en) | 2002-03-28 |
| WO2000023057A2 (en) | 2000-04-27 |
| ZA200103081B (en) | 2002-07-12 |
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