CN1367697A - Therapeutical method for improving cognition - Google Patents
Therapeutical method for improving cognition Download PDFInfo
- Publication number
- CN1367697A CN1367697A CN99812184A CN99812184A CN1367697A CN 1367697 A CN1367697 A CN 1367697A CN 99812184 A CN99812184 A CN 99812184A CN 99812184 A CN99812184 A CN 99812184A CN 1367697 A CN1367697 A CN 1367697A
- Authority
- CN
- China
- Prior art keywords
- effective ingredient
- atypical antipsychotic
- relevant
- acetylcholinesteraseinhibitors inhibitors
- application
- 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.)
- Pending
Links
- 230000019771 cognition Effects 0.000 title abstract 2
- 230000001225 therapeutic effect Effects 0.000 title description 2
- 239000003112 inhibitor Substances 0.000 claims abstract description 32
- 239000003693 atypical antipsychotic agent Substances 0.000 claims abstract description 23
- 239000000544 cholinesterase inhibitor Substances 0.000 claims abstract description 23
- 208000024827 Alzheimer disease Diseases 0.000 claims abstract description 17
- 230000000694 effects Effects 0.000 claims abstract description 11
- 208000028017 Psychotic disease Diseases 0.000 claims abstract description 10
- 206010012289 Dementia Diseases 0.000 claims abstract description 7
- 239000008194 pharmaceutical composition Substances 0.000 claims abstract description 6
- 239000004615 ingredient Substances 0.000 claims description 25
- 229940127236 atypical antipsychotics Drugs 0.000 claims description 22
- 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 19
- 206010036631 Presenile dementia Diseases 0.000 claims description 15
- 239000003814 drug Substances 0.000 claims description 14
- 239000000203 mixture Substances 0.000 claims description 11
- 229960001534 risperidone Drugs 0.000 claims description 11
- 229960003980 galantamine Drugs 0.000 claims description 10
- 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
- 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 9
- 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 description 4
- 238000009472 formulation Methods 0.000 claims description 4
- 208000013738 Sleep Initiation and Maintenance disease Diseases 0.000 claims description 3
- 230000003920 cognitive function Effects 0.000 claims description 3
- 206010022437 insomnia Diseases 0.000 claims description 3
- 210000004916 vomit Anatomy 0.000 claims description 3
- 230000008673 vomiting Effects 0.000 claims description 3
- 208000027776 Extrapyramidal disease 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
- 206010043118 Tardive Dyskinesia Diseases 0.000 claims description 2
- 239000003795 chemical substances by application Substances 0.000 claims description 2
- 229960003530 donepezil Drugs 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
- 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
- 239000004480 active ingredient Substances 0.000 abstract 4
- 230000009286 beneficial effect Effects 0.000 abstract 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 abstract 1
- 230000002411 adverse Effects 0.000 abstract 1
- 230000001149 cognitive effect Effects 0.000 abstract 1
- 230000006866 deterioration Effects 0.000 abstract 1
- 230000002265 prevention Effects 0.000 abstract 1
- 230000002195 synergetic effect Effects 0.000 abstract 1
- 239000002253 acid Substances 0.000 description 10
- QTBSBXVTEAMEQO-UHFFFAOYSA-N Acetic acid Chemical compound CC(O)=O QTBSBXVTEAMEQO-UHFFFAOYSA-N 0.000 description 3
- CSCPPACGZOOCGX-UHFFFAOYSA-N Acetone Chemical compound CC(C)=O CSCPPACGZOOCGX-UHFFFAOYSA-N 0.000 description 3
- OFOBLEOULBTSOW-UHFFFAOYSA-N Malonic acid Chemical compound OC(=O)CC(O)=O OFOBLEOULBTSOW-UHFFFAOYSA-N 0.000 description 3
- MUBZPKHOEPUJKR-UHFFFAOYSA-N Oxalic acid Chemical compound OC(=O)C(O)=O MUBZPKHOEPUJKR-UHFFFAOYSA-N 0.000 description 3
- KRKNYBCHXYNGOX-UHFFFAOYSA-N citric acid Chemical compound OC(=O)CC(O)(C(O)=O)CC(O)=O KRKNYBCHXYNGOX-UHFFFAOYSA-N 0.000 description 3
- POULHZVOKOAJMA-UHFFFAOYSA-N dodecanoic acid Chemical compound CCCCCCCCCCCC(O)=O POULHZVOKOAJMA-UHFFFAOYSA-N 0.000 description 3
- 150000002148 esters Chemical class 0.000 description 3
- IPCSVZSSVZVIGE-UHFFFAOYSA-N hexadecanoic acid Chemical compound CCCCCCCCCCCCCCCC(O)=O IPCSVZSSVZVIGE-UHFFFAOYSA-N 0.000 description 3
- 150000003839 salts Chemical group 0.000 description 3
- VZCYOOQTPOCHFL-OWOJBTEDSA-N Fumaric acid Chemical compound OC(=O)\C=C\C(O)=O VZCYOOQTPOCHFL-OWOJBTEDSA-N 0.000 description 2
- AEMRFAOFKBGASW-UHFFFAOYSA-N Glycolic acid Chemical compound OCC(O)=O AEMRFAOFKBGASW-UHFFFAOYSA-N 0.000 description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 description 2
- AFVFQIVMOAPDHO-UHFFFAOYSA-N Methanesulfonic acid Chemical compound CS(O)(=O)=O AFVFQIVMOAPDHO-UHFFFAOYSA-N 0.000 description 2
- NBIIXXVUZAFLBC-UHFFFAOYSA-N Phosphoric acid Chemical compound OP(O)(O)=O NBIIXXVUZAFLBC-UHFFFAOYSA-N 0.000 description 2
- GHVNFZFCNZKVNT-UHFFFAOYSA-N decanoic acid Chemical compound CCCCCCCCCC(O)=O GHVNFZFCNZKVNT-UHFFFAOYSA-N 0.000 description 2
- KEMQGTRYUADPNZ-UHFFFAOYSA-N heptadecanoic acid Chemical compound CCCCCCCCCCCCCCCCC(O)=O KEMQGTRYUADPNZ-UHFFFAOYSA-N 0.000 description 2
- JVTAAEKCZFNVCJ-UHFFFAOYSA-N lactic acid Chemical compound CC(O)C(O)=O JVTAAEKCZFNVCJ-UHFFFAOYSA-N 0.000 description 2
- ISYWECDDZWTKFF-UHFFFAOYSA-N nonadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCCC(O)=O ISYWECDDZWTKFF-UHFFFAOYSA-N 0.000 description 2
- YGSDEFSMJLZEOE-UHFFFAOYSA-N salicylic acid Chemical compound OC(=O)C1=CC=CC=C1O YGSDEFSMJLZEOE-UHFFFAOYSA-N 0.000 description 2
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 2
- SZHOJFHSIKHZHA-UHFFFAOYSA-N tridecanoic acid Chemical compound CCCCCCCCCCCCC(O)=O SZHOJFHSIKHZHA-UHFFFAOYSA-N 0.000 description 2
- BJEPYKJPYRNKOW-REOHCLBHSA-N (S)-malic acid Chemical compound OC(=O)[C@@H](O)CC(O)=O BJEPYKJPYRNKOW-REOHCLBHSA-N 0.000 description 1
- BMYNFMYTOJXKLE-UHFFFAOYSA-N 3-azaniumyl-2-hydroxypropanoate Chemical compound NCC(O)C(O)=O BMYNFMYTOJXKLE-UHFFFAOYSA-N 0.000 description 1
- WUBBRNOQWQTFEX-UHFFFAOYSA-N 4-aminosalicylic acid Chemical compound NC1=CC=C(C(O)=O)C(O)=C1 WUBBRNOQWQTFEX-UHFFFAOYSA-N 0.000 description 1
- 239000005632 Capric acid (CAS 334-48-5) Substances 0.000 description 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 1
- 239000005639 Lauric acid Substances 0.000 description 1
- GRYLNZFGIOXLOG-UHFFFAOYSA-N Nitric acid Chemical compound O[N+]([O-])=O GRYLNZFGIOXLOG-UHFFFAOYSA-N 0.000 description 1
- 235000021314 Palmitic acid Nutrition 0.000 description 1
- 235000021355 Stearic acid Nutrition 0.000 description 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 description 1
- QAOWNCQODCNURD-UHFFFAOYSA-N Sulfuric acid Chemical compound OS(O)(=O)=O QAOWNCQODCNURD-UHFFFAOYSA-N 0.000 description 1
- FEWJPZIEWOKRBE-UHFFFAOYSA-N Tartaric acid Natural products [H+].[H+].[O-]C(=O)C(O)C(O)C([O-])=O FEWJPZIEWOKRBE-UHFFFAOYSA-N 0.000 description 1
- BJEPYKJPYRNKOW-UHFFFAOYSA-N alpha-hydroxysuccinic acid Natural products OC(=O)C(O)CC(O)=O BJEPYKJPYRNKOW-UHFFFAOYSA-N 0.000 description 1
- 229910000147 aluminium phosphate Inorganic materials 0.000 description 1
- 229960004909 aminosalicylic acid Drugs 0.000 description 1
- SRSXLGNVWSONIS-UHFFFAOYSA-N benzenesulfonic acid Chemical compound OS(=O)(=O)C1=CC=CC=C1 SRSXLGNVWSONIS-UHFFFAOYSA-N 0.000 description 1
- 229940092714 benzenesulfonic acid Drugs 0.000 description 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 description 1
- 235000015165 citric acid Nutrition 0.000 description 1
- 239000000625 cyclamic acid and its Na and Ca salt Substances 0.000 description 1
- HCAJEUSONLESMK-UHFFFAOYSA-N cyclohexylsulfamic acid Chemical compound OS(=O)(=O)NC1CCCCC1 HCAJEUSONLESMK-UHFFFAOYSA-N 0.000 description 1
- XBDQKXXYIPTUBI-UHFFFAOYSA-N dimethylselenoniopropionate Natural products CCC(O)=O XBDQKXXYIPTUBI-UHFFFAOYSA-N 0.000 description 1
- CCIVGXIOQKPBKL-UHFFFAOYSA-N ethanesulfonic acid Chemical compound CCS(O)(=O)=O CCIVGXIOQKPBKL-UHFFFAOYSA-N 0.000 description 1
- 239000001530 fumaric acid Substances 0.000 description 1
- 235000011087 fumaric acid Nutrition 0.000 description 1
- 229960004275 glycolic acid Drugs 0.000 description 1
- 229910052736 halogen Inorganic materials 0.000 description 1
- -1 halogen acids Chemical class 0.000 description 1
- IPCSVZSSVZVIGE-UHFFFAOYSA-M hexadecanoate Chemical compound CCCCCCCCCCCCCCCC([O-])=O IPCSVZSSVZVIGE-UHFFFAOYSA-M 0.000 description 1
- VKOBVWXKNCXXDE-UHFFFAOYSA-N icosanoic acid Chemical compound CCCCCCCCCCCCCCCCCCCC(O)=O VKOBVWXKNCXXDE-UHFFFAOYSA-N 0.000 description 1
- 229910052500 inorganic mineral Inorganic materials 0.000 description 1
- YAQXGBBDJYBXKL-UHFFFAOYSA-N iron(2+);1,10-phenanthroline;dicyanide Chemical compound [Fe+2].N#[C-].N#[C-].C1=CN=C2C3=NC=CC=C3C=CC2=C1.C1=CN=C2C3=NC=CC=C3C=CC2=C1 YAQXGBBDJYBXKL-UHFFFAOYSA-N 0.000 description 1
- 239000004310 lactic acid Substances 0.000 description 1
- 235000014655 lactic acid Nutrition 0.000 description 1
- VZCYOOQTPOCHFL-UPHRSURJSA-N maleic acid Chemical compound OC(=O)\C=C/C(O)=O VZCYOOQTPOCHFL-UPHRSURJSA-N 0.000 description 1
- 239000011976 maleic acid Substances 0.000 description 1
- 239000001630 malic acid Substances 0.000 description 1
- 235000011090 malic acid Nutrition 0.000 description 1
- 229940098779 methanesulfonic acid Drugs 0.000 description 1
- 239000011707 mineral Substances 0.000 description 1
- DUWWHGPELOTTOE-UHFFFAOYSA-N n-(5-chloro-2,4-dimethoxyphenyl)-3-oxobutanamide Chemical compound COC1=CC(OC)=C(NC(=O)CC(C)=O)C=C1Cl DUWWHGPELOTTOE-UHFFFAOYSA-N 0.000 description 1
- WQEPLUUGTLDZJY-UHFFFAOYSA-N n-Pentadecanoic acid Natural products CCCCCCCCCCCCCCC(O)=O WQEPLUUGTLDZJY-UHFFFAOYSA-N 0.000 description 1
- 229910017604 nitric acid Inorganic materials 0.000 description 1
- QIQXTHQIDYTFRH-UHFFFAOYSA-N octadecanoic acid Chemical compound CCCCCCCCCCCCCCCCCC(O)=O QIQXTHQIDYTFRH-UHFFFAOYSA-N 0.000 description 1
- OQCDKBAXFALNLD-UHFFFAOYSA-N octadecanoic acid Natural products CCCCCCCC(C)CCCCCCCCC(O)=O OQCDKBAXFALNLD-UHFFFAOYSA-N 0.000 description 1
- 150000002885 octadecanoids Chemical class 0.000 description 1
- 150000007524 organic acids Chemical class 0.000 description 1
- 235000006408 oxalic acid Nutrition 0.000 description 1
- FJKROLUGYXJWQN-UHFFFAOYSA-N papa-hydroxy-benzoic acid Natural products OC(=O)C1=CC=C(O)C=C1 FJKROLUGYXJWQN-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
- RLLPVAHGXHCWKJ-UHFFFAOYSA-N permethrin Chemical compound CC1(C)C(C=C(Cl)Cl)C1C(=O)OCC1=CC=CC(OC=2C=CC=CC=2)=C1 RLLPVAHGXHCWKJ-UHFFFAOYSA-N 0.000 description 1
- 235000019260 propionic acid Nutrition 0.000 description 1
- 229960004889 salicylic acid Drugs 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000001117 sulphuric acid Substances 0.000 description 1
- 235000011149 sulphuric acid Nutrition 0.000 description 1
- 239000011975 tartaric acid Substances 0.000 description 1
- 235000002906 tartaric acid Nutrition 0.000 description 1
- ZTUXEFFFLOVXQE-UHFFFAOYSA-N tetradecanoic acid Chemical compound CCCCCCCCCCCCCC(O)=O.CCCCCCCCCCCCCC(O)=O ZTUXEFFFLOVXQE-UHFFFAOYSA-N 0.000 description 1
- 238000002560 therapeutic procedure Methods 0.000 description 1
- JOXIMZWYDAKGHI-UHFFFAOYSA-N toluene-4-sulfonic acid Chemical compound CC1=CC=C(S(O)(=O)=O)C=C1 JOXIMZWYDAKGHI-UHFFFAOYSA-N 0.000 description 1
- ZDPHROOEEOARMN-UHFFFAOYSA-N undecanoic acid Chemical compound CCCCCCCCCCC(O)=O ZDPHROOEEOARMN-UHFFFAOYSA-N 0.000 description 1
- XLYOFNOQVPJJNP-UHFFFAOYSA-N water Substances O XLYOFNOQVPJJNP-UHFFFAOYSA-N 0.000 description 1
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
Abstract
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 (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.
Description
The present invention relates to Pharmaceutical composition, described Pharmaceutical composition comprises a kind of carrier and as the atypical antipsychotic (I) of first effective ingredient with as the acetylcholinesteraseinhibitors inhibitors (II) of second effective ingredient, the amount of every kind of effective ingredient produces useful treatment effect in suffering from psychosis or presenile dementia or relevant dull-witted patient.Described useful treatment effect can be the synergism to the cognitive function of presenile dementia or relevant dementia patients, or prevent the further infringement of described patient understanding, or reduce because of the described effective ingredient of another kind with illeffects that wherein a kind of described effective ingredient is relevant.
Special concern be to use atypical antipsychotic (I) to prepare medicine, described medicine is used for reducing presenile dementia or relevant dementia patients and the relevant illeffects of acetylcholinesteraseinhibitors inhibitors (II), for example feels sick, vomits, perspires, is on tenterhooks and insomnia.Especially pay close attention to use atypical antipsychotic (I) and prepare medicine, described medicine be used for improving suffer from presenile dementia or relevant dull-witted, use the patient's of acetylcholinesteraseinhibitors inhibitors (II) treatment sleep simultaneously.
The present invention relates to Pharmaceutical composition, described Pharmaceutical composition comprises a kind of carrier and as the atypical antipsychotic (I) of first effective ingredient with as the acetylcholinesteraseinhibitors inhibitors (II) of second effective ingredient, the amount of every kind of effective ingredient produces useful treatment effect in suffering from psychosis or presenile dementia or relevant dull-witted patient.Described useful treatment effect can be the synergism to the patient's of presenile dementia or relevant dementia cognitive function, or prevent the further infringement of described patient understanding, or reduce because of the described effective ingredient of another kind with illeffects that wherein a kind of described effective ingredient is relevant.
Described atypical antipsychotic (I) is selected from risperidone, 9-hydroxyl risperidone or its C
10-20Alkanoate, olanzapine, quetiapine, iloperidone or ziprasidone, and described acetylcholinesteraseinhibitors inhibitors (II) is selected from galantamine, rivastigmine or donepezil; Or the acid-addition salts form that therapeutic activity is arranged of arbitrary said medicine.Described salt comprises effective ingredient (I) and the salt form that (II) can form with appropriate acid, and described appropriate acid is mineral acid for example, such as halogen acids, and for example hydrochloric acid or hydrobromic acid; Sulphuric acid; Nitric acid; Acid such as phosphoric acid; Or organic acid for example acetic acid, propanoic acid, hydroxyacetic acid, lactic acid, acetone acid, oxalic acid, malonic acid, succinic acid, maleic acid, fumaric acid, malic acid, tartaric acid, citric acid, methanesulfonic acid, ethyl sulfonic acid, benzenesulfonic acid, p-methyl benzenesulfonic acid, cyclamic acid, salicylic acid, para-aminosalicylic acid, pounce on acid such as acid.For example, can use galantamine with (1: 1) hydrobromate form easily.
C
10-20Alkanoic acid is selected from capric acid, hendecanoic acid, dodecylic acid (lauric acid), tridecanoic acid, tetradecanoic acid (myristic acid), pentadecanoic acid, hexadecanoic acid (Palmic acid), heptadecanoic acid, octadecanoid acid (stearic acid), nonadecylic acid and arachic acid.Because their water solublity is limited, therefore generally believes and described ester must be suspended in the oil.From the viewpoint of pharmacokinetics and toleration, the ester that to find to have C15 (pentadecyl) chain and corresponding therewith effective ingredient be 9-hydroxyl risperidone cetylate is superior ester.
The amount of every kind of described effective ingredient preferably is equal to or less than the permission amount in the monotherapy that adopts described effective ingredient.
Most preferably such compositions, wherein said atypical antipsychotic (I) is a risperidone, and described acetylcholinesteraseinhibitors inhibitors (II) is a galantamine, particularly with the form of galanthamine hydrobromide.In described compositions, the amount of the risperidone of every kind of dosage form is 0.5,1,2,4 or 6mg, and the amount of galantamine (as principal agent) is 8,16,24 or 32mg.
The present invention also relates to contain as the atypical antipsychotic (I) of first effective ingredient with as the acetylcholinesteraseinhibitors inhibitors (II) of second effective ingredient goods as combination formulations, described combination formulations is used for simultaneously, separately or sequentially be used for the treatment of suffer from psychosis, presenile dementia or relevant dull-witted patient.
The present invention also relates to use acetylcholinesteraseinhibitors inhibitors (II) prepares strengthen the medicine of atypical antipsychotic (I) to the understanding effect in the psychotic.
On the contrary, the present invention also relates to use atypical antipsychotic (I) prepares in suffering from presenile dementia or relevant dull-witted patient and strengthens the medicine of acetylcholinesteraseinhibitors inhibitors (II) to the understanding effect.
In addition, the present invention relates to use atypical antipsychotic (I) and prepare the medicine that in the patient who suffers from presenile dementia or relevant dementia, reduces the illeffects relevant with acetylcholinesteraseinhibitors inhibitors (II).Described illeffects can be to feel sick, vomit, perspire, be on tenterhooks or insomnia.What especially pay close attention to is to use atypical antipsychotic (I) to prepare the medicine that improves sleep in patient's presenile dementia or relevant patient dull-witted, that use acetylcholinesteraseinhibitors inhibitors (II) to treat simultaneously.
At last, the present invention relates to use acetylcholinesteraseinhibitors inhibitors (II) and prepare the medicine that in the psychotic, reduces the illeffects relevant with atypical antipsychotic (I).Described illeffects can be extrapyramidal symptom or tardive dyskinesia.
In all aforementioned applications, described atypical antipsychotic (I) is risperidone preferably, and described acetylcholinesteraseinhibitors inhibitors (II) preferably galantamine, particularly its (1: 1) hydrobromate.
Claims (14)
1. Pharmaceutical composition, it comprises a kind of carrier and as the atypical antipsychotic (I) of first effective ingredient with as the acetylcholinesteraseinhibitors inhibitors (II) of second effective ingredient, the amount of every kind of effective ingredient produces useful treatment effect in suffering from psychosis or presenile dementia or relevant dull-witted patient.
2. according to the compositions of claim 1, wherein said useful treatment effect is the synergism to the cognitive function of presenile dementia or relevant dementia patients, or prevent the further infringement of described patient understanding, or reduce because of the described effective ingredient of another kind with illeffects that wherein a kind of described effective ingredient is relevant.
3. according to the compositions of claim 1, wherein said atypical antipsychotic (I) is selected from risperidone, 9-hydroxyl risperidone or its C
10-20Alkanoate, olanzapine, quetiapine, iloperidone or ziprasidone, and described acetylcholinesteraseinhibitors inhibitors (II) is selected from galantamine, rivastigmine or donepezil.
4. according to the compositions of claim 3, wherein the amount of every kind of described effective ingredient is equal to or less than the permission amount in the monotherapy that adopts described effective ingredient.
5. according to the compositions of claim 3, wherein said atypical antipsychotic (I) is a risperidone, and described acetylcholinesteraseinhibitors inhibitors (II) is a galantamine.
6. according to the compositions of claim 5, wherein the amount of the risperidone of every kind of dosage form is 0.5,1,2,4 or 6mg, and the amount of galantamine (as principal agent) is 8,16,24 or 32mg.
7. contain as the atypical antipsychotic (I) of first effective ingredient with as the acetylcholinesteraseinhibitors inhibitors (II) of second effective ingredient goods as combination formulations, described combination formulations is used for simultaneously, separately or sequentially be used for the treatment of suffer from psychosis, presenile dementia or relevant dull-witted patient.
8. the application of acetylcholinesteraseinhibitors inhibitors (II) is used for preparation and strengthens the medicine of atypical antipsychotic (I) to the understanding effect the psychotic.
9. the application of atypical antipsychotic (I) is used for preparing and is suffering from presenile dementia or relevant dull-witted patient strengthens the medicine of acetylcholinesteraseinhibitors inhibitors (II) to the understanding effect.
10. the application of atypical antipsychotic (I) is used for preparing and is suffering from the medicine that presenile dementia or relevant dull-witted patient reduce the illeffects relevant with acetylcholinesteraseinhibitors inhibitors (II).
11. according to the application of claim 10, wherein said illeffects can be to feel sick, vomit, perspire, be on tenterhooks or insomnia.
12. the application of acetylcholinesteraseinhibitors inhibitors (II) is used for preparation reduces the illeffects relevant with atypical antipsychotic (I) the psychotic medicine.
13. according to the application of claim 12, wherein said illeffects is extrapyramidal symptom or tardive dyskinesia.
14. each application according to Claim 8-13, wherein said atypical antipsychotic (I) is a risperidone, and described acetylcholinesteraseinhibitors inhibitors (II) is a galantamine.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP98203454.8 | 1998-10-16 | ||
| EP98203454 | 1998-10-16 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CN1367697A true CN1367697A (en) | 2002-09-04 |
Family
ID=8234219
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN99812184A Pending CN1367697A (en) | 1998-10-16 | 1999-10-12 | Therapeutical method 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 |
| WO2003037337A1 (en) | 2001-10-30 | 2003-05-08 | 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 |
| WO2006065233A1 (en) * | 2004-12-10 | 2006-06-22 | Abbott Laboratories | Fused bicycloheterocycle substituted quinuclidine derivatives |
| WO2005065645A2 (en) * | 2003-12-31 | 2005-07-21 | Actavis Group Hf | Donepezil formulations |
| 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 |
| US9126987B2 (en) | 2006-11-30 | 2015-09-08 | Probiodrug Ag | Inhibitors of glutaminyl cyclase |
| JP5930573B2 (en) | 2007-03-01 | 2016-06-15 | プロビオドルグ エージー | New use of glutaminyl cyclase inhibitors |
| DK2142514T3 (en) | 2007-04-18 | 2015-03-23 | 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. |
| WO2011100373A1 (en) | 2010-02-09 | 2011-08-18 | The Johns Hopkins University | Methods and compositions for improving cognitive function |
| EP2542549B1 (en) | 2010-03-03 | 2016-05-11 | Probiodrug AG | 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) |
| JP5945532B2 (en) | 2010-04-21 | 2016-07-05 | プロビオドルグ エージー | Benzimidazole derivatives as inhibitors of glutaminyl cyclase |
| US8530670B2 (en) | 2011-03-16 | 2013-09-10 | Probiodrug Ag | Inhibitors |
| WO2014078568A1 (en) | 2012-11-14 | 2014-05-22 | The Johns Hopkins University | Methods and compositions for treating schizophrenia |
| EP3827820A1 (en) | 2013-03-15 | 2021-06-02 | The Johns Hopkins University | Brivaracetam 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 |
| EA034167B8 (en) | 2015-05-22 | 2021-04-27 | Эйджинбайо, Инк. | Extended release pharmaceutical compositions 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 |
| ATE183084T1 (en) * | 1991-05-14 | 1999-08-15 | 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 |
| RU2219924C2 (en) * | 1998-04-14 | 2003-12-27 | Дзе Дженерал Хоспитал Корпорейшн | Method for treatment of neuropsychiatric disorders |
-
1999
- 1999-10-12 WO PCT/EP1999/007804 patent/WO2000023057A2/en not_active Application Discontinuation
- 1999-10-12 CA CA002345767A patent/CA2345767A1/en not_active Abandoned
- 1999-10-12 PL PL99348107A patent/PL348107A1/en unknown
- 1999-10-12 TR TR2001/01082T patent/TR200101082T2/en unknown
- 1999-10-12 AU AU64727/99A patent/AU6472799A/en not_active Abandoned
- 1999-10-12 KR KR1020017002286A patent/KR20010072878A/en not_active Application Discontinuation
- 1999-10-12 BR BR9914419-0A patent/BR9914419A/en not_active IP Right Cessation
- 1999-10-12 SK SK459-2001A patent/SK4592001A3/en unknown
- 1999-10-12 EP EP99952580A patent/EP1121131A2/en not_active Withdrawn
- 1999-10-12 EE EEP200100136A patent/EE200100136A/en unknown
- 1999-10-12 HU HU0103781A patent/HUP0103781A3/en unknown
- 1999-10-12 ID IDW20010828A patent/ID28441A/en unknown
- 1999-10-12 CN CN99812184A patent/CN1367697A/en active Pending
- 1999-10-12 IL IL14258899A patent/IL142588A0/en unknown
- 1999-10-12 JP JP2000576832A patent/JP2002527469A/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
- 2001-04-10 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 |
|---|---|
| ZA200103081B (en) | 2002-07-12 |
| JP2002527469A (en) | 2002-08-27 |
| BG105302A (en) | 2001-11-30 |
| ID28441A (en) | 2001-05-24 |
| WO2000023057A3 (en) | 2000-07-27 |
| EP1121131A2 (en) | 2001-08-08 |
| AU6472799A (en) | 2000-05-08 |
| NO20011403L (en) | 2001-03-20 |
| HRP20010262A2 (en) | 2002-06-30 |
| NO20011403D0 (en) | 2001-03-20 |
| HUP0103781A3 (en) | 2003-09-29 |
| PL348107A1 (en) | 2002-05-06 |
| WO2000023057A2 (en) | 2000-04-27 |
| SK4592001A3 (en) | 2001-12-03 |
| EE200100136A (en) | 2002-06-17 |
| TR200101082T2 (en) | 2001-09-21 |
| KR20010072878A (en) | 2001-07-31 |
| HUP0103781A2 (en) | 2002-03-28 |
| CA2345767A1 (en) | 2000-04-27 |
| IL142588A0 (en) | 2002-03-10 |
| BR9914419A (en) | 2001-06-26 |
| HK1039745A1 (en) | 2002-05-10 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| CN1367697A (en) | Therapeutical method for improving cognition | |
| US6444665B1 (en) | Method for treating pain | |
| DE60009697T2 (en) | USE OF 1- [4- (5-CYANOINDOL-3YL) BUTYL] -4- (2-CARBAMOYLBENZOFURAN-5-YL) PIPERAZINE AND ITS PHYSIOLOGICAL ACCEPTABLE SALTS FOR THE TREATMENT OF BIPOLAR DISEASES AND MANIA | |
| KR101125462B1 (en) | Pharmaceutical formulations of modafinil | |
| DE19167974T1 (en) | PHARMACEUTICAL FORM WITH OXYCODONE AND NALOXONE | |
| RU2008116931A (en) | APPLICATION OF N-DESMETHYLCLOSAPINE FOR TREATMENT OF NEUROPSYCHIATRIC DISEASES IN PEOPLE | |
| Kraus | Treatment of kleptomania with paroxetine. | |
| EP3454848B1 (en) | 5ht6 receptor antagonists for use in the treatment of alzheimer's disease with apathy as comorbidity | |
| CA2480275C (en) | Statin therapy for enhancing cognitive maintenance | |
| HU214629B (en) | Process for producing pharmaceutical composition for the treatment of post-operative nausea and vomiting | |
| US20090124606A1 (en) | Composition for Treatment of Psychosis | |
| JP2008106028A (en) | Use of flibanserin for treatment of chronic pain | |
| PL371264A1 (en) | Method for the treatment of bone disorders | |
| JP2012500248A (en) | Treatment of anxiety disorder | |
| KR20150132888A (en) | Method of treating thermoregulatory disfunction with paroxetine | |
| CA2469702A1 (en) | Darifenacin for use in the treatment of urgency induced by overactive bladder | |
| EP0868181B1 (en) | Use of alpha,alpha-diphenylacetic acid-4-(n-methyl-piperidyl)ester as anti-spasmodic | |
| US20050222122A1 (en) | Statin therapy for enhancing cognitive maintenance | |
| WO2008019070A2 (en) | Pharmaceutical compositions of trospium for treating smooth muscle hyperactivity disorders | |
| Works et al. | SAFETY AND TOLERABILITY | |
| Jones et al. | 58. 5-HT2A receptor blockade by quetiapine is related to its side effect profile | |
| Douglass | Introduction to Palliative Care | |
| Walbert | Palliative care in end-stage neurological | |
| JP2008523015A (en) | Drug 4- (S)-(4-acetyl-piperazin-1-yl) -2- (R)-(4-fluoro-2-methyl-phenyl) -piperazine-1-carboxylic acid, [1- (R) Use of-(3,5-bis-trifluoromethyl-phenyl) -ethyl] -methylamide | |
| CN1207037A (en) | Use of the L-enantiomer of centchroman for the manufacture of a pharmaceutical composition for the treatment or prophylaxis of breast cancer |
Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| C10 | Entry into substantive examination | ||
| SE01 | Entry into force of request for substantive examination | ||
| C06 | Publication | ||
| PB01 | Publication | ||
| C02 | Deemed withdrawal of patent application after publication (patent law 2001) | ||
| WD01 | Invention patent application deemed withdrawn after publication |