CA2310990A1 - Utilisation de la galantamine pour le traitement de la maladie d'alzheimer; ciblage de la cause sous-jacente de la maladie - Google Patents
Utilisation de la galantamine pour le traitement de la maladie d'alzheimer; ciblage de la cause sous-jacente de la maladie Download PDFInfo
- Publication number
- CA2310990A1 CA2310990A1 CA002310990A CA2310990A CA2310990A1 CA 2310990 A1 CA2310990 A1 CA 2310990A1 CA 002310990 A CA002310990 A CA 002310990A CA 2310990 A CA2310990 A CA 2310990A CA 2310990 A1 CA2310990 A1 CA 2310990A1
- Authority
- CA
- Canada
- Prior art keywords
- galantamine
- day
- disease
- dose
- adas
- 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.)
- Abandoned
Links
- 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 title claims abstract description 117
- 229960003980 galantamine Drugs 0.000 title claims abstract description 58
- ASUTZQLVASHGKV-UHFFFAOYSA-N galanthamine hydrochloride Natural products O1C(=C23)C(OC)=CC=C2CN(C)CCC23C1CC(O)C=C2 ASUTZQLVASHGKV-UHFFFAOYSA-N 0.000 title claims abstract description 58
- 201000010099 disease Diseases 0.000 title claims abstract description 14
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 title claims abstract description 14
- 230000008685 targeting Effects 0.000 title claims description 8
- 238000011282 treatment Methods 0.000 title abstract description 48
- 208000024827 Alzheimer disease Diseases 0.000 title abstract description 11
- 238000000034 method Methods 0.000 claims description 17
- 239000003814 drug Substances 0.000 claims description 14
- 230000002401 inhibitory effect Effects 0.000 claims description 9
- 208000031124 Dementia Alzheimer type Diseases 0.000 claims description 7
- 150000003839 salts Chemical class 0.000 claims description 5
- 238000004519 manufacturing process Methods 0.000 claims description 2
- 238000004448 titration Methods 0.000 claims 7
- 229940126585 therapeutic drug Drugs 0.000 abstract description 3
- 208000017667 Chronic Disease Diseases 0.000 abstract description 2
- 230000008859 change Effects 0.000 description 23
- 239000000902 placebo Substances 0.000 description 21
- 229940068196 placebo Drugs 0.000 description 21
- 229940079593 drug Drugs 0.000 description 13
- 238000012360 testing method Methods 0.000 description 12
- 230000003920 cognitive function Effects 0.000 description 10
- 230000006872 improvement Effects 0.000 description 10
- 230000001149 cognitive effect Effects 0.000 description 9
- 238000004458 analytical method Methods 0.000 description 8
- 230000002411 adverse Effects 0.000 description 7
- 102000019315 Nicotinic acetylcholine receptors Human genes 0.000 description 6
- 108050006807 Nicotinic acetylcholine receptors Proteins 0.000 description 6
- 230000000694 effects Effects 0.000 description 6
- 238000012423 maintenance Methods 0.000 description 6
- 150000001875 compounds Chemical class 0.000 description 5
- 230000001276 controlling effect Effects 0.000 description 5
- 108010022752 Acetylcholinesterase Proteins 0.000 description 4
- 102100033639 Acetylcholinesterase Human genes 0.000 description 4
- OIPILFWXSMYKGL-UHFFFAOYSA-N acetylcholine Chemical compound CC(=O)OCC[N+](C)(C)C OIPILFWXSMYKGL-UHFFFAOYSA-N 0.000 description 4
- 229960004373 acetylcholine Drugs 0.000 description 4
- 229940022698 acetylcholinesterase Drugs 0.000 description 4
- 239000000544 cholinesterase inhibitor Substances 0.000 description 4
- 229960002024 galantamine hydrobromide Drugs 0.000 description 4
- 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 4
- 230000003518 presynaptic effect Effects 0.000 description 4
- 230000004044 response Effects 0.000 description 4
- 229940122041 Cholinesterase inhibitor Drugs 0.000 description 3
- 102000004190 Enzymes Human genes 0.000 description 3
- 108090000790 Enzymes Proteins 0.000 description 3
- 229930013930 alkaloid Natural products 0.000 description 3
- 230000003111 delayed effect Effects 0.000 description 3
- 238000003745 diagnosis Methods 0.000 description 3
- 229960003135 donepezil hydrochloride Drugs 0.000 description 3
- XWAIAVWHZJNZQQ-UHFFFAOYSA-N donepezil hydrochloride Chemical compound [H+].[Cl-].O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 XWAIAVWHZJNZQQ-UHFFFAOYSA-N 0.000 description 3
- 229940088598 enzyme Drugs 0.000 description 3
- 230000015654 memory Effects 0.000 description 3
- 238000000959 Cochran–Mantel–Haenszel (CMH) test Methods 0.000 description 2
- 150000003797 alkaloid derivatives Chemical group 0.000 description 2
- 238000000540 analysis of variance Methods 0.000 description 2
- 201000007201 aphasia Diseases 0.000 description 2
- 230000003542 behavioural effect Effects 0.000 description 2
- 230000008901 benefit Effects 0.000 description 2
- 231100000870 cognitive problem Toxicity 0.000 description 2
- 230000007423 decrease Effects 0.000 description 2
- 238000011156 evaluation Methods 0.000 description 2
- 238000009472 formulation Methods 0.000 description 2
- 230000006870 function Effects 0.000 description 2
- 230000003993 interaction Effects 0.000 description 2
- 239000000203 mixture Substances 0.000 description 2
- 230000009467 reduction Effects 0.000 description 2
- 230000002441 reversible effect Effects 0.000 description 2
- 230000002459 sustained effect Effects 0.000 description 2
- GXFZCDMWGMFGFL-KKXMJGKMSA-N (+)-Tubocurarine chloride hydrochloride Chemical compound [Cl-].[Cl-].C([C@H]1[N+](C)(C)CCC=2C=C(C(=C(OC3=CC=C(C=C3)C[C@H]3C=4C=C(C(=CC=4CC[NH+]3C)OC)O3)C=21)O)OC)C1=CC=C(O)C3=C1 GXFZCDMWGMFGFL-KKXMJGKMSA-N 0.000 description 1
- FTOAOBMCPZCFFF-UHFFFAOYSA-N 5,5-diethylbarbituric acid Chemical compound CCC1(CC)C(=O)NC(=O)NC1=O FTOAOBMCPZCFFF-UHFFFAOYSA-N 0.000 description 1
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 description 1
- 208000037259 Amyloid Plaque Diseases 0.000 description 1
- 108010053652 Butyrylcholinesterase Proteins 0.000 description 1
- 102100032404 Cholinesterase Human genes 0.000 description 1
- 241001111317 Chondrodendron tomentosum Species 0.000 description 1
- 208000028698 Cognitive impairment Diseases 0.000 description 1
- 239000008709 Curare Substances 0.000 description 1
- 241000196324 Embryophyta Species 0.000 description 1
- 208000001375 Facial Neuralgia Diseases 0.000 description 1
- 241000234271 Galanthus Species 0.000 description 1
- 241001502107 Galanthus alpinus Species 0.000 description 1
- 241000234283 Galanthus nivalis Species 0.000 description 1
- 108090000862 Ion Channels Proteins 0.000 description 1
- 102000004310 Ion Channels Human genes 0.000 description 1
- WHUUTDBJXJRKMK-VKHMYHEASA-N L-glutamic acid Chemical compound OC(=O)[C@@H](N)CCC(O)=O WHUUTDBJXJRKMK-VKHMYHEASA-N 0.000 description 1
- 102000014415 Muscarinic acetylcholine receptor Human genes 0.000 description 1
- 108050003473 Muscarinic acetylcholine receptor Proteins 0.000 description 1
- 241000234479 Narcissus Species 0.000 description 1
- 208000009668 Neurobehavioral Manifestations Diseases 0.000 description 1
- 206010067482 No adverse event Diseases 0.000 description 1
- 208000034530 PLAA-associated neurodevelopmental disease Diseases 0.000 description 1
- 101150107341 RERE gene Proteins 0.000 description 1
- 101100532451 Rattus norvegicus Slc22a17 gene Proteins 0.000 description 1
- 208000007271 Substance Withdrawal Syndrome Diseases 0.000 description 1
- 238000001793 Wilcoxon signed-rank test Methods 0.000 description 1
- 230000005856 abnormality Effects 0.000 description 1
- 125000000218 acetic acid group Chemical group C(C)(=O)* 0.000 description 1
- 230000003281 allosteric effect Effects 0.000 description 1
- 230000003444 anaesthetic effect Effects 0.000 description 1
- 238000010876 biochemical test Methods 0.000 description 1
- 230000008499 blood brain barrier function Effects 0.000 description 1
- 210000001218 blood-brain barrier Anatomy 0.000 description 1
- 239000002775 capsule Substances 0.000 description 1
- 230000015556 catabolic process Effects 0.000 description 1
- 230000001713 cholinergic effect Effects 0.000 description 1
- 210000002932 cholinergic neuron Anatomy 0.000 description 1
- 230000000718 cholinopositive effect Effects 0.000 description 1
- 230000002060 circadian Effects 0.000 description 1
- 239000004927 clay Substances 0.000 description 1
- 208000010877 cognitive disease Diseases 0.000 description 1
- 238000010276 construction Methods 0.000 description 1
- 208000012790 cranial neuralgia Diseases 0.000 description 1
- 239000006071 cream Substances 0.000 description 1
- 230000007850 degeneration Effects 0.000 description 1
- 230000006866 deterioration Effects 0.000 description 1
- 239000003085 diluting agent Substances 0.000 description 1
- 230000003292 diminished effect Effects 0.000 description 1
- 239000003937 drug carrier Substances 0.000 description 1
- 230000008030 elimination Effects 0.000 description 1
- 238000003379 elimination reaction Methods 0.000 description 1
- 229930195712 glutamate Natural products 0.000 description 1
- 150000004820 halides Chemical class 0.000 description 1
- JGPMMRGNQUBGND-UHFFFAOYSA-N idebenone Chemical compound COC1=C(OC)C(=O)C(CCCCCCCCCCO)=C(C)C1=O JGPMMRGNQUBGND-UHFFFAOYSA-N 0.000 description 1
- 229960004135 idebenone Drugs 0.000 description 1
- 239000003112 inhibitor Substances 0.000 description 1
- 238000011221 initial treatment Methods 0.000 description 1
- 238000002955 isolation Methods 0.000 description 1
- 238000009533 lab test Methods 0.000 description 1
- 230000000670 limiting effect Effects 0.000 description 1
- 238000010234 longitudinal analysis Methods 0.000 description 1
- 239000007937 lozenge Substances 0.000 description 1
- 230000007246 mechanism Effects 0.000 description 1
- 239000012528 membrane Substances 0.000 description 1
- 230000003340 mental effect Effects 0.000 description 1
- 238000013460 mixed model approach Methods 0.000 description 1
- 238000012986 modification Methods 0.000 description 1
- 230000004048 modification Effects 0.000 description 1
- 230000016273 neuron death Effects 0.000 description 1
- 230000002981 neuropathic effect Effects 0.000 description 1
- 239000002858 neurotransmitter agent Substances 0.000 description 1
- 238000001543 one-way ANOVA Methods 0.000 description 1
- 238000007427 paired t-test Methods 0.000 description 1
- 230000000737 periodic effect Effects 0.000 description 1
- 230000002093 peripheral effect Effects 0.000 description 1
- -1 pessaries Substances 0.000 description 1
- 239000008194 pharmaceutical composition Substances 0.000 description 1
- 239000000546 pharmaceutical excipient Substances 0.000 description 1
- 229940001470 psychoactive drug Drugs 0.000 description 1
- 102000005962 receptors Human genes 0.000 description 1
- 108020003175 receptors Proteins 0.000 description 1
- 230000001105 regulatory effect Effects 0.000 description 1
- 239000012313 reversal agent Substances 0.000 description 1
- 238000012552 review Methods 0.000 description 1
- 238000012216 screening Methods 0.000 description 1
- 230000006403 short-term memory Effects 0.000 description 1
- 239000000243 solution Substances 0.000 description 1
- 230000000638 stimulation Effects 0.000 description 1
- 239000000829 suppository Substances 0.000 description 1
- 238000012353 t test Methods 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 238000007492 two-way ANOVA Methods 0.000 description 1
- 210000002700 urine Anatomy 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Neurosurgery (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Chemical & Material Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Pharmacology & Pharmacy (AREA)
- Hospice & Palliative Care (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Psychiatry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US19426200P | 2000-04-03 | 2000-04-03 | |
| US60/194,262 | 2000-04-03 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CA2310990A1 true CA2310990A1 (fr) | 2000-10-09 |
Family
ID=22716910
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CA002310990A Abandoned CA2310990A1 (fr) | 2000-04-03 | 2000-06-27 | Utilisation de la galantamine pour le traitement de la maladie d'alzheimer; ciblage de la cause sous-jacente de la maladie |
Country Status (4)
| Country | Link |
|---|---|
| EP (1) | EP1272190A2 (fr) |
| AU (1) | AU2001246518A1 (fr) |
| CA (1) | CA2310990A1 (fr) |
| WO (1) | WO2001074364A2 (fr) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2310926C (fr) * | 2000-04-03 | 2002-10-15 | Janssen Pharmaceutica N.V. | Utilisation de la galantamine pour le traitement du comportement neuropsychiatrique associe a la maladie d'alzheimer |
| GB0329498D0 (en) * | 2003-12-19 | 2004-01-28 | Novartis Ag | Organic compounds |
| CA2986431C (fr) * | 2015-05-18 | 2020-04-14 | Synaptec Development Llc | Clairance de galantamine d'amyloide.beta. |
Family Cites Families (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US4663318A (en) | 1986-01-15 | 1987-05-05 | Bonnie Davis | Method of treating Alzheimer's disease |
| AU1738800A (en) | 1998-11-23 | 2000-06-13 | Bonnie Davis | Dosage formulations for acetylcholinesterase inhibitors |
-
2000
- 2000-06-27 CA CA002310990A patent/CA2310990A1/fr not_active Abandoned
-
2001
- 2001-03-28 WO PCT/EP2001/003551 patent/WO2001074364A2/fr not_active Application Discontinuation
- 2001-03-28 EP EP01919406A patent/EP1272190A2/fr not_active Withdrawn
- 2001-03-28 AU AU2001246518A patent/AU2001246518A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| WO2001074364A3 (fr) | 2002-05-16 |
| WO2001074364A2 (fr) | 2001-10-11 |
| EP1272190A2 (fr) | 2003-01-08 |
| AU2001246518A1 (en) | 2001-10-15 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| EEER | Examination request | ||
| FZDE | Dead |