WO2004039321A2 - Therapie associee agoniste nicotinique/agoniste d1 pour le traitement de la maladie d'alzheimer - Google Patents
Therapie associee agoniste nicotinique/agoniste d1 pour le traitement de la maladie d'alzheimer Download PDFInfo
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- WO2004039321A2 WO2004039321A2 PCT/US2003/033729 US0333729W WO2004039321A2 WO 2004039321 A2 WO2004039321 A2 WO 2004039321A2 US 0333729 W US0333729 W US 0333729W WO 2004039321 A2 WO2004039321 A2 WO 2004039321A2
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- Prior art keywords
- alpha
- nicotinic
- agonist
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- 229940052760 dopamine agonists Drugs 0.000 description 1
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- BEFDCLMNVWHSGT-UHFFFAOYSA-N ethenylcyclopentane Chemical compound C=CC1CCCC1 BEFDCLMNVWHSGT-UHFFFAOYSA-N 0.000 description 1
- RTZKZFJDLAIYFH-UHFFFAOYSA-N ether Substances CCOCC RTZKZFJDLAIYFH-UHFFFAOYSA-N 0.000 description 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 1
- 229950002163 etisulergine Drugs 0.000 description 1
- 230000029142 excretion Effects 0.000 description 1
- 229960003980 galantamine Drugs 0.000 description 1
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 description 1
- 210000001035 gastrointestinal tract Anatomy 0.000 description 1
- 229920000159 gelatin Polymers 0.000 description 1
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- 235000019322 gelatine Nutrition 0.000 description 1
- 235000011852 gelatine desserts Nutrition 0.000 description 1
- 239000008103 glucose Substances 0.000 description 1
- 229940074045 glyceryl distearate Drugs 0.000 description 1
- 125000003976 glyceryl group Chemical group [H]C([*])([H])C(O[H])([H])C(O[H])([H])[H] 0.000 description 1
- 239000002748 glycoprotein P inhibitor Substances 0.000 description 1
- 239000007902 hard capsule Substances 0.000 description 1
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- 239000003701 inert diluent Substances 0.000 description 1
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- 229940102223 injectable solution Drugs 0.000 description 1
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- QXJSBBXBKPUZAA-UHFFFAOYSA-N isooleic acid Natural products CCCCCCCC=CCCCCCCCCC(O)=O QXJSBBXBKPUZAA-UHFFFAOYSA-N 0.000 description 1
- NLYAJNPCOHFWQQ-UHFFFAOYSA-N kaolin Chemical compound O.O.O=[Al]O[Si](=O)O[Si](=O)O[Al]=O NLYAJNPCOHFWQQ-UHFFFAOYSA-N 0.000 description 1
- 239000008101 lactose Substances 0.000 description 1
- 150000002611 lead compounds Chemical class 0.000 description 1
- 235000020778 linoleic acid Nutrition 0.000 description 1
- OYHQOLUKZRVURQ-IXWMQOLASA-N linoleic acid Natural products CCCCC\C=C/C\C=C\CCCCCCCC(O)=O OYHQOLUKZRVURQ-IXWMQOLASA-N 0.000 description 1
- 239000007788 liquid Substances 0.000 description 1
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- XXPANQJNYNUNES-UHFFFAOYSA-N nomifensine Chemical class C12=CC=CC(N)=C2CN(C)CC1C1=CC=CC=C1 XXPANQJNYNUNES-UHFFFAOYSA-N 0.000 description 1
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- 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
- ZQPPMHVWECSIRJ-KTKRTIGZSA-N oleic acid Chemical compound CCCCCCCC\C=C/CCCCCCCC(O)=O ZQPPMHVWECSIRJ-KTKRTIGZSA-N 0.000 description 1
- 210000000056 organ Anatomy 0.000 description 1
- 239000012188 paraffin wax Substances 0.000 description 1
- 239000000312 peanut oil Substances 0.000 description 1
- 229960001511 pergolide mesylate Drugs 0.000 description 1
- UWCVGPLTGZWHGS-ZORIOUSZSA-N pergolide mesylate Chemical compound CS(O)(=O)=O.C1=CC([C@H]2C[C@@H](CSC)CN([C@@H]2C2)CCC)=C3C2=CNC3=C1 UWCVGPLTGZWHGS-ZORIOUSZSA-N 0.000 description 1
- 239000008196 pharmacological composition Substances 0.000 description 1
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- 229920001223 polyethylene glycol Polymers 0.000 description 1
- 239000000244 polyoxyethylene sorbitan monooleate Substances 0.000 description 1
- 235000010482 polyoxyethylene sorbitan monooleate Nutrition 0.000 description 1
- 229920000053 polysorbate 80 Polymers 0.000 description 1
- 239000001267 polyvinylpyrrolidone Substances 0.000 description 1
- 235000013855 polyvinylpyrrolidone Nutrition 0.000 description 1
- 229920000036 polyvinylpyrrolidone Polymers 0.000 description 1
- YRVIKLBSVVNSHF-JTQLQIEISA-N pozanicline Chemical compound CC1=NC=CC=C1OC[C@H]1NCCC1 YRVIKLBSVVNSHF-JTQLQIEISA-N 0.000 description 1
- 230000002335 preservative effect Effects 0.000 description 1
- 230000002265 prevention Effects 0.000 description 1
- 230000007425 progressive decline Effects 0.000 description 1
- 208000037821 progressive disease Diseases 0.000 description 1
- 210000004129 prosencephalon Anatomy 0.000 description 1
- 210000000664 rectum Anatomy 0.000 description 1
- 230000009467 reduction Effects 0.000 description 1
- 230000002829 reductive effect Effects 0.000 description 1
- CVHZOJJKTDOEJC-UHFFFAOYSA-N saccharin Chemical compound C1=CC=C2C(=O)NS(=O)(=O)C2=C1 CVHZOJJKTDOEJC-UHFFFAOYSA-N 0.000 description 1
- 229940081974 saccharin Drugs 0.000 description 1
- 235000019204 saccharin Nutrition 0.000 description 1
- 239000000901 saccharin and its Na,K and Ca salt Substances 0.000 description 1
- 239000008159 sesame oil Substances 0.000 description 1
- 235000011803 sesame oil Nutrition 0.000 description 1
- 230000011664 signaling Effects 0.000 description 1
- 235000010413 sodium alginate Nutrition 0.000 description 1
- 239000000661 sodium alginate Substances 0.000 description 1
- 229940005550 sodium alginate Drugs 0.000 description 1
- WXMKPNITSTVMEF-UHFFFAOYSA-M sodium benzoate Chemical compound [Na+].[O-]C(=O)C1=CC=CC=C1 WXMKPNITSTVMEF-UHFFFAOYSA-M 0.000 description 1
- 235000010234 sodium benzoate Nutrition 0.000 description 1
- 239000004299 sodium benzoate Substances 0.000 description 1
- 229910001467 sodium calcium phosphate Inorganic materials 0.000 description 1
- 229910000029 sodium carbonate Inorganic materials 0.000 description 1
- 235000019812 sodium carboxymethyl cellulose Nutrition 0.000 description 1
- 229920001027 sodium carboxymethylcellulose Polymers 0.000 description 1
- 239000001488 sodium phosphate Substances 0.000 description 1
- 239000007901 soft capsule Substances 0.000 description 1
- 235000010199 sorbic acid Nutrition 0.000 description 1
- 239000004334 sorbic acid Substances 0.000 description 1
- 229940075582 sorbic acid Drugs 0.000 description 1
- 239000000600 sorbitol Substances 0.000 description 1
- 239000007921 spray Substances 0.000 description 1
- 239000008107 starch Substances 0.000 description 1
- 235000019698 starch Nutrition 0.000 description 1
- 239000008117 stearic acid Substances 0.000 description 1
- 239000008174 sterile solution Substances 0.000 description 1
- 238000003860 storage Methods 0.000 description 1
- 208000011117 substance-related disease Diseases 0.000 description 1
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- 239000012730 sustained-release form Substances 0.000 description 1
- 239000000454 talc Substances 0.000 description 1
- 235000012222 talc Nutrition 0.000 description 1
- 229910052623 talc Inorganic materials 0.000 description 1
- 230000001225 therapeutic effect Effects 0.000 description 1
- 239000002562 thickening agent Substances 0.000 description 1
- 231100000419 toxicity Toxicity 0.000 description 1
- 230000001988 toxicity Effects 0.000 description 1
- VZCYOOQTPOCHFL-UHFFFAOYSA-N trans-butenedioic acid Natural products OC(=O)C=CC(O)=O VZCYOOQTPOCHFL-UHFFFAOYSA-N 0.000 description 1
- RYFMWSXOAZQYPI-UHFFFAOYSA-K trisodium phosphate Chemical compound [Na+].[Na+].[Na+].[O-]P([O-])([O-])=O RYFMWSXOAZQYPI-UHFFFAOYSA-K 0.000 description 1
Classifications
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K45/00—Medicinal preparations containing active ingredients not provided for in groups A61K31/00 - A61K41/00
- A61K45/06—Mixtures of active ingredients without chemical characterisation, e.g. antiphlogistics and cardiaca
-
- 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
Definitions
- Another embodiment of the invention provides a method of treating Alzheimer's disease in a subject comprising administration to the subject a combination comprising an alpha-7-nicotinic agonist and a Dl receptor agonist, wherein the alpha-7-nicotinic agonist and the Dl receptor agonist together comprise a therapeutically effective amount of the alpha-7-nicotinic agonist and the Dl receptor agonist.
- the administration of each of the alpha-7-nicotinic agonist and the Dl receptor agonist can occur sequentially within about 24 hours, about 12 hours, about 6 hours, about 3 hours, and about 1 hour.
- the administration of each of the alpha-7-nicotinic agonist and the Dl receptor agonist can occur substantially concomitantly.
- compositions of the invention can be delivered to a subject by systemic administration.
- Systemic administration is in vivo systemic absorption or accumulation of drugs in the blood stream followed by distribution throughout the entire body. Administration routes that can lead to systemic absorption include, without limitation: intravenous, subcutaneous, intraperitoneal, inhalation, transdermal, oral, intrapulmonary and intramuscular.
- Formulations for oral use can also be presented as hard gelatin capsules wherein the active ingredient is mixed with an inert solid diluent, for example, calcium carbonate, calcium phosphate or kaolin, or as soft gelatin capsules wherein the active ingredient is mixed with water or an oil medium, for example peanut oil, liquid paraffin or olive oil.
- an inert solid diluent for example, calcium carbonate, calcium phosphate or kaolin
- water or an oil medium for example peanut oil, liquid paraffin or olive oil.
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Abstract
Cette invention concerne des thérapies associées pour le traitement de la maladie d'Alzheimer. Selon un de ses aspects, l'invention concerne une thérapie combinatoire pour des sujets chez lesquelles la maladie d'Alzheimer a été diagnostiquée, qui consiste en une combinaison optimale d'un de plusieurs agonistes nicotiniques alpha-7 et d'un ou de plusieurs agonistes du récepteur D1.
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| AU2003284898A AU2003284898A1 (en) | 2002-10-29 | 2003-10-24 | Combinative nicotinic/d1 agonism therapy for the treatment of alzheimer's disease |
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US42204702P | 2002-10-29 | 2002-10-29 | |
| US60/422,047 | 2002-10-29 |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| WO2004039321A2 true WO2004039321A2 (fr) | 2004-05-13 |
| WO2004039321A8 WO2004039321A8 (fr) | 2005-05-26 |
Family
ID=32230314
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PCT/US2003/033729 WO2004039321A2 (fr) | 2002-10-29 | 2003-10-24 | Therapie associee agoniste nicotinique/agoniste d1 pour le traitement de la maladie d'alzheimer |
Country Status (2)
| Country | Link |
|---|---|
| AU (1) | AU2003284898A1 (fr) |
| WO (1) | WO2004039321A2 (fr) |
Cited By (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2006048294A1 (fr) * | 2004-11-05 | 2006-05-11 | Novartis Ag | Combinaisons d'agonistes du recepteur nicotinique alpha 7 de l'acetylcholine |
| US7713977B2 (en) | 2005-12-16 | 2010-05-11 | Novartis Ag | (1-aza-bicyclo[3.3.1]non-4-yl)-[5-(1H-indol-5-yl)-heteroaryl]-amines as cholinergic ligands of the n-achr for the treatment of psychotic and neurodegenerative disorders |
| US7713976B2 (en) | 2005-12-16 | 2010-05-11 | Novartis Ag | [(1H-indol-5-yl)-heteroaryloxy]-1-aza-bicylco[3.3.1]nonanes as cholinergic ligands of the n-AChR for the treatment of psychotic and neurodegenerative disorders |
| US8173667B2 (en) | 2005-10-21 | 2012-05-08 | Novartis Ag | 1-aza-bicycloalkyl derivatives |
| US8236803B2 (en) | 2002-09-04 | 2012-08-07 | Novartis Ag | Aza-bicycloalkyl ethers and their use as alpha7-nAChR agonists |
| US8609662B2 (en) | 2004-07-14 | 2013-12-17 | Novartis Ag | 3-(heteroaryl-oxy)-2-alkyl-1-aza-bicycloalkyl derivatives as alpha. 7-nachr ligands for the treatment of CNS diseases |
| US8884017B2 (en) | 2001-12-27 | 2014-11-11 | Bayer Intellectual Property Gmbh | 2-heteroarylcarboxylic acid amides |
| US8933090B2 (en) | 2004-06-18 | 2015-01-13 | Novartis Ag | 1-aza-bicyclo[3.3.1]nonanes |
Families Citing this family (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| PT3029039T (pt) | 2010-05-17 | 2017-11-28 | Forum Pharmaceuticals Inc | Formulações farmacêuticas que compreendem formas cristalinas de cloridrato de (r)-7-cloro-n-(quinuclidin-3-il)benzo(b)tiofeno-2-carboxamida mono-hidratado |
| MX358512B (es) | 2012-05-08 | 2018-08-24 | Forum Pharmaceuticals Inc | Uso de (r)-7cloro-n-(quinuclidin-3-il) benzo[b] tiofeno-2-carboxamida o una sal farmacéuticamente aceptable de la misma para preparar una composición farmacéutica en el tratamiento de una disfunción cognitiva. |
-
2003
- 2003-10-24 AU AU2003284898A patent/AU2003284898A1/en not_active Abandoned
- 2003-10-24 WO PCT/US2003/033729 patent/WO2004039321A2/fr not_active Application Discontinuation
Cited By (20)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8884017B2 (en) | 2001-12-27 | 2014-11-11 | Bayer Intellectual Property Gmbh | 2-heteroarylcarboxylic acid amides |
| US9567343B2 (en) | 2002-09-04 | 2017-02-14 | Novartis Ag | Aza-bicyloalkyl ethers and their use as alpha7-nachr agonists |
| US9849117B2 (en) | 2002-09-04 | 2017-12-26 | Novartis Ag | Aza-bicycloalkyl ethers and their use as alpha7-nachr agonists |
| US9012451B2 (en) | 2002-09-04 | 2015-04-21 | Novartis Ag | Aza-bicycloalkyl ethers and their use as ALPHA7-nachr agonists |
| US8236803B2 (en) | 2002-09-04 | 2012-08-07 | Novartis Ag | Aza-bicycloalkyl ethers and their use as alpha7-nAChR agonists |
| US9475811B2 (en) | 2004-06-18 | 2016-10-25 | Novartis Ag | 1-aza-bicyclo[3.3.1]nonanes |
| US8933090B2 (en) | 2004-06-18 | 2015-01-13 | Novartis Ag | 1-aza-bicyclo[3.3.1]nonanes |
| US9657010B2 (en) | 2004-07-14 | 2017-05-23 | Novartis Ag | Substituted quinuclidines as alpha 7-nicotinic acetylcholine receptor activity modulators |
| US8609662B2 (en) | 2004-07-14 | 2013-12-17 | Novartis Ag | 3-(heteroaryl-oxy)-2-alkyl-1-aza-bicycloalkyl derivatives as alpha. 7-nachr ligands for the treatment of CNS diseases |
| EP2135609A1 (fr) * | 2004-11-05 | 2009-12-23 | Novartis AG | Combinaisons d'agonistes du recepteur nicotine-acetylcholine-alpha-7 |
| EP2332537A1 (fr) * | 2004-11-05 | 2011-06-15 | Novartis AG | Combinaisons d'agonistes du recepteur nicotine-acetylcholine-alpha-7 |
| WO2006048294A1 (fr) * | 2004-11-05 | 2006-05-11 | Novartis Ag | Combinaisons d'agonistes du recepteur nicotinique alpha 7 de l'acetylcholine |
| JP2008518896A (ja) * | 2004-11-05 | 2008-06-05 | ノバルティス アクチエンゲゼルシャフト | ニコチン性アセチルコリンα７受容体アンタゴニストの組合せ剤 |
| US8173667B2 (en) | 2005-10-21 | 2012-05-08 | Novartis Ag | 1-aza-bicycloalkyl derivatives |
| US8637517B2 (en) | 2005-12-16 | 2014-01-28 | Novartis Ag | Organic compounds |
| US9206181B2 (en) | 2005-12-16 | 2015-12-08 | Novartis Ag | 1-aza-bicyclo[3.3.1] non-4-yl)-[5-(1H-indol-5-yl)-heteroaryl]-amines as cholinergic ligands of the n-AChR for the treatment of psychotic and neurodegenerative disorders |
| US8759346B2 (en) | 2005-12-16 | 2014-06-24 | Novartis Ag | Organic compounds |
| US8048885B2 (en) | 2005-12-16 | 2011-11-01 | Novartis Ag | Organic compounds |
| US7713976B2 (en) | 2005-12-16 | 2010-05-11 | Novartis Ag | [(1H-indol-5-yl)-heteroaryloxy]-1-aza-bicylco[3.3.1]nonanes as cholinergic ligands of the n-AChR for the treatment of psychotic and neurodegenerative disorders |
| US7713977B2 (en) | 2005-12-16 | 2010-05-11 | Novartis Ag | (1-aza-bicyclo[3.3.1]non-4-yl)-[5-(1H-indol-5-yl)-heteroaryl]-amines as cholinergic ligands of the n-achr for the treatment of psychotic and neurodegenerative disorders |
Also Published As
| Publication number | Publication date |
|---|---|
| WO2004039321A8 (fr) | 2005-05-26 |
| AU2003284898A1 (en) | 2004-05-25 |
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