JP2011518776A5 - - Google Patents
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- Publication number
- JP2011518776A5 JP2011518776A5 JP2011501792A JP2011501792A JP2011518776A5 JP 2011518776 A5 JP2011518776 A5 JP 2011518776A5 JP 2011501792 A JP2011501792 A JP 2011501792A JP 2011501792 A JP2011501792 A JP 2011501792A JP 2011518776 A5 JP2011518776 A5 JP 2011518776A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutically acceptable
- composition
- nspaccha
- acceptable salts
- unit form
- 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.)
- Granted
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- 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 14
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 claims description 11
- 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 11
- 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 7
- 229960003530 donepezil Drugs 0.000 claims description 7
- 229960004136 rivastigmine Drugs 0.000 claims description 7
- 102000012440 Acetylcholinesterase Human genes 0.000 claims description 6
- 108010022752 Acetylcholinesterase Proteins 0.000 claims description 6
- 229960003980 galantamine Drugs 0.000 claims description 6
- 229940022698 acetylcholinesterase Drugs 0.000 claims description 5
- 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 5
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 230000005764 inhibitory process Effects 0.000 claims description 3
- 229960001685 tacrine Drugs 0.000 claims description 2
- YLJREFDVOIBQDA-UHFFFAOYSA-N tacrine Chemical compound C1=CC=C2C(N)=C(CCCC3)C3=NC2=C1 YLJREFDVOIBQDA-UHFFFAOYSA-N 0.000 claims description 2
- 239000000203 mixture Substances 0.000 claims 15
- 150000003839 salts Chemical class 0.000 claims 14
- 239000000544 cholinesterase inhibitor Substances 0.000 claims 8
- 229960003855 solifenacin Drugs 0.000 claims 4
- FBOUYBDGKBSUES-VXKWHMMOSA-N solifenacin Chemical compound C1([C@H]2C3=CC=CC=C3CCN2C(O[C@@H]2C3CCN(CC3)C2)=O)=CC=CC=C1 FBOUYBDGKBSUES-VXKWHMMOSA-N 0.000 claims 4
- QPCVHQBVMYCJOM-UHFFFAOYSA-N Propiverine Chemical compound C=1C=CC=CC=1C(C=1C=CC=CC=1)(OCCC)C(=O)OC1CCN(C)CC1 QPCVHQBVMYCJOM-UHFFFAOYSA-N 0.000 claims 3
- 230000001078 anti-cholinergic effect Effects 0.000 claims 3
- 239000008194 pharmaceutical composition Substances 0.000 claims 3
- 229960003510 propiverine Drugs 0.000 claims 3
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical compound Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims 2
- DUDKAZCAISNGQN-UHFFFAOYSA-N Oxyphencyclimine Chemical compound CN1CCCN=C1COC(=O)C(O)(C=1C=CC=CC=1)C1CCCCC1 DUDKAZCAISNGQN-UHFFFAOYSA-N 0.000 claims 2
- 229960002369 oxyphencyclimine Drugs 0.000 claims 2
- 230000001225 therapeutic effect Effects 0.000 claims 2
- OOGJQPCLVADCPB-HXUWFJFHSA-N tolterodine Chemical compound C1([C@@H](CCN(C(C)C)C(C)C)C=2C(=CC=C(C)C=2)O)=CC=CC=C1 OOGJQPCLVADCPB-HXUWFJFHSA-N 0.000 claims 2
- 229960001491 trospium Drugs 0.000 claims 2
- OYYDSUSKLWTMMQ-JKHIJQBDSA-N trospium Chemical compound [N+]12([C@@H]3CC[C@H]2C[C@H](C3)OC(=O)C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CCCC1 OYYDSUSKLWTMMQ-JKHIJQBDSA-N 0.000 claims 2
- FBOUYBDGKBSUES-KEKNWZKVSA-N 1-azabicyclo[2.2.2]octan-3-yl (1s)-1-phenyl-3,4-dihydro-1h-isoquinoline-2-carboxylate Chemical compound C1([C@H]2C3=CC=CC=C3CCN2C(OC2C3CCN(CC3)C2)=O)=CC=CC=C1 FBOUYBDGKBSUES-KEKNWZKVSA-N 0.000 claims 1
- GQDSJYDRNIZSNY-UHFFFAOYSA-N 1-phenyl-3,4-dihydro-1h-isoquinoline-2-carboxylic acid Chemical compound OC(=O)N1CCC2=CC=CC=C2C1C1=CC=CC=C1 GQDSJYDRNIZSNY-UHFFFAOYSA-N 0.000 claims 1
- RSWGJHLUYNHPMX-UHFFFAOYSA-N Abietic-Saeure Natural products C12CCC(C(C)C)=CC2=CCC2C1(C)CCCC2(C)C(O)=O RSWGJHLUYNHPMX-UHFFFAOYSA-N 0.000 claims 1
- FEWJPZIEWOKRBE-JCYAYHJZSA-M L-tartrate(1-) Chemical compound OC(=O)[C@H](O)[C@@H](O)C([O-])=O FEWJPZIEWOKRBE-JCYAYHJZSA-M 0.000 claims 1
- 229940121948 Muscarinic receptor antagonist Drugs 0.000 claims 1
- KHPCPRHQVVSZAH-HUOMCSJISA-N Rosin Natural products O(C/C=C/c1ccccc1)[C@H]1[C@H](O)[C@@H](O)[C@@H](O)[C@@H](CO)O1 KHPCPRHQVVSZAH-HUOMCSJISA-N 0.000 claims 1
- KDYFGRWQOYBRFD-UHFFFAOYSA-N Succinic acid Natural products OC(=O)CCC(O)=O KDYFGRWQOYBRFD-UHFFFAOYSA-N 0.000 claims 1
- 230000001668 ameliorated effect Effects 0.000 claims 1
- KDYFGRWQOYBRFD-NUQCWPJISA-N butanedioic acid Chemical compound O[14C](=O)CC[14C](O)=O KDYFGRWQOYBRFD-NUQCWPJISA-N 0.000 claims 1
- 239000000812 cholinergic antagonist Substances 0.000 claims 1
- 150000001875 compounds Chemical class 0.000 claims 1
- 229960003135 donepezil hydrochloride Drugs 0.000 claims 1
- 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 claims 1
- 239000003937 drug carrier Substances 0.000 claims 1
- 230000003551 muscarinic effect Effects 0.000 claims 1
- -1 oct- 3-yl Chemical group 0.000 claims 1
- 230000002093 peripheral effect Effects 0.000 claims 1
- 125000001453 quaternary ammonium group Chemical group 0.000 claims 1
- 229960001368 solifenacin succinate Drugs 0.000 claims 1
- RWSOTUBLDIXVET-UHFFFAOYSA-O sulfonium Chemical compound [SH3+] RWSOTUBLDIXVET-UHFFFAOYSA-O 0.000 claims 1
- 208000024891 symptom Diseases 0.000 claims 1
- RWRDLPDLKQPQOW-UHFFFAOYSA-N tetrahydropyrrole Substances C1CCNC1 RWRDLPDLKQPQOW-UHFFFAOYSA-N 0.000 claims 1
- 238000011287 therapeutic dose Methods 0.000 claims 1
- 229960004045 tolterodine Drugs 0.000 claims 1
- KHPCPRHQVVSZAH-UHFFFAOYSA-N trans-cinnamyl beta-D-glucopyranoside Natural products OC1C(O)C(O)C(CO)OC1OCC=CC1=CC=CC=C1 KHPCPRHQVVSZAH-UHFFFAOYSA-N 0.000 claims 1
- BDIAUFOIMFAIPU-UHFFFAOYSA-N valepotriate Natural products CC(C)CC(=O)OC1C=C(C(=COC2OC(=O)CC(C)C)COC(C)=O)C2C11CO1 BDIAUFOIMFAIPU-UHFFFAOYSA-N 0.000 claims 1
- 239000002775 capsule Substances 0.000 description 4
- 230000000694 effects Effects 0.000 description 4
- 210000003169 central nervous system Anatomy 0.000 description 3
- FEWJPZIEWOKRBE-JCYAYHJZSA-N Dextrotartaric acid Chemical compound OC(=O)[C@H](O)[C@@H](O)C(O)=O FEWJPZIEWOKRBE-JCYAYHJZSA-N 0.000 description 2
- 102000004190 Enzymes Human genes 0.000 description 2
- 108090000790 Enzymes Proteins 0.000 description 2
- 229940088598 enzyme Drugs 0.000 description 2
- 230000001537 neural effect Effects 0.000 description 2
- 229940100688 oral solution Drugs 0.000 description 2
- 229940095064 tartrate Drugs 0.000 description 2
- QCQCHGYLTSGIGX-GHXANHINSA-N 4-[[(3ar,5ar,5br,7ar,9s,11ar,11br,13as)-5a,5b,8,8,11a-pentamethyl-3a-[(5-methylpyridine-3-carbonyl)amino]-2-oxo-1-propan-2-yl-4,5,6,7,7a,9,10,11,11b,12,13,13a-dodecahydro-3h-cyclopenta[a]chrysen-9-yl]oxy]-2,2-dimethyl-4-oxobutanoic acid Chemical compound N([C@@]12CC[C@@]3(C)[C@]4(C)CC[C@H]5C(C)(C)[C@@H](OC(=O)CC(C)(C)C(O)=O)CC[C@]5(C)[C@H]4CC[C@@H]3C1=C(C(C2)=O)C(C)C)C(=O)C1=CN=CC(C)=C1 QCQCHGYLTSGIGX-GHXANHINSA-N 0.000 description 1
- RVCSYOQWLPPAOA-CVPHZBIISA-M [(5s)-spiro[8-azoniabicyclo[3.2.1]octane-8,1'-azolidin-1-ium]-3-yl] 2-hydroxy-2,2-diphenylacetate;chloride Chemical compound [Cl-].[N+]12([C@H]3CCC2CC(C3)OC(=O)C(O)(C=2C=CC=CC=2)C=2C=CC=CC=2)CCCC1 RVCSYOQWLPPAOA-CVPHZBIISA-M 0.000 description 1
- 230000032683 aging Effects 0.000 description 1
- 239000003795 chemical substances by application Substances 0.000 description 1
- 230000000973 chemotherapeutic effect Effects 0.000 description 1
- 230000007370 cognitive improvement Effects 0.000 description 1
- 230000002596 correlated effect Effects 0.000 description 1
- 230000000875 corresponding effect Effects 0.000 description 1
- 229940079593 drug Drugs 0.000 description 1
- 239000003814 drug Substances 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
- 239000012728 immediate-release (IR) tablet Substances 0.000 description 1
- 239000006191 orally-disintegrating tablet Substances 0.000 description 1
- 230000003285 pharmacodynamic effect Effects 0.000 description 1
- 102000004169 proteins and genes Human genes 0.000 description 1
- 108090000623 proteins and genes Proteins 0.000 description 1
- 239000003826 tablet Substances 0.000 description 1
- 229960001530 trospium chloride Drugs 0.000 description 1
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP08005750.8 | 2008-03-27 | ||
| EP08005750 | 2008-03-27 | ||
| PCT/US2009/001662 WO2009120277A1 (en) | 2008-03-27 | 2009-03-17 | Use and composition for treating dementia |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014004320A Division JP2014114295A (ja) | 2008-03-27 | 2014-01-14 | 認知症を治療するための使用及び組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2011518776A JP2011518776A (ja) | 2011-06-30 |
| JP2011518776A5 true JP2011518776A5 (https=) | 2013-04-25 |
| JP5647099B2 JP5647099B2 (ja) | 2014-12-24 |
Family
ID=39535697
Family Applications (3)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2011501792A Expired - Fee Related JP5647099B2 (ja) | 2008-03-27 | 2009-03-17 | 認知症を治療するための使用及び組成物 |
| JP2014004320A Pending JP2014114295A (ja) | 2008-03-27 | 2014-01-14 | 認知症を治療するための使用及び組成物 |
| JP2016078787A Expired - Fee Related JP6427522B2 (ja) | 2008-03-27 | 2016-04-11 | 認知症を治療するための使用及び組成物 |
Family Applications After (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2014004320A Pending JP2014114295A (ja) | 2008-03-27 | 2014-01-14 | 認知症を治療するための使用及び組成物 |
| JP2016078787A Expired - Fee Related JP6427522B2 (ja) | 2008-03-27 | 2016-04-11 | 認知症を治療するための使用及び組成物 |
Country Status (10)
| Country | Link |
|---|---|
| US (5) | US8404701B2 (https=) |
| EP (3) | EP4088717A1 (https=) |
| JP (3) | JP5647099B2 (https=) |
| AU (1) | AU2009229372C1 (https=) |
| CA (1) | CA2718411C (https=) |
| DK (1) | DK2271218T3 (https=) |
| ES (1) | ES2634421T3 (https=) |
| MX (3) | MX344177B (https=) |
| PL (1) | PL2271218T3 (https=) |
| WO (1) | WO2009120277A1 (https=) |
Families Citing this family (23)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8969402B2 (en) | 2006-11-15 | 2015-03-03 | Steven A. Rich | Combined acetylcholinesterase inhibitor and quaternary ammonium antimuscarinic therapy to alter progression of cognitive diseases |
| US20110201597A1 (en) | 2008-03-27 | 2011-08-18 | Chase Thomas N | Method and composition for treating alzheimer-type dementia |
| WO2011034568A1 (en) | 2009-09-18 | 2011-03-24 | Chase Pharmaceuticals Corporation | Method and composition for treating alzheimer-type dementia |
| AU2009229372C1 (en) | 2008-03-27 | 2017-02-02 | Chase Pharmaceuticals Corporation | Use and composition for treating dementia |
| PT3061821T (pt) | 2009-07-22 | 2019-09-05 | PureTech Health LLC | Composições para tratamento de distúrbios melhorados por ativação de recetores muscarínicos |
| JP2011213606A (ja) * | 2010-03-31 | 2011-10-27 | Sawai Pharmaceutical Co Ltd | ドネペジルを含有する固形製剤の製造方法 |
| JP2011213695A (ja) * | 2010-04-02 | 2011-10-27 | Taisho Pharm Ind Ltd | ドネペジル塩酸塩含有口腔内速崩壊錠 |
| BR112015004902A2 (pt) * | 2012-09-05 | 2017-07-04 | Chase Pharmaceuticals Corp | métodos e composição neutroprotetores anticolinérgicos |
| EP3242659A4 (en) | 2015-01-09 | 2018-09-12 | Chase Pharmaceuticals Corporation | Oxybutynin transdermal therapeutic system combination |
| US10596139B2 (en) | 2015-03-06 | 2020-03-24 | Chase Pharmaceuticals Corporation | Oxybutynin transdermal therapeutic system muscarinic agonist combination |
| CA2978214A1 (en) * | 2015-03-06 | 2016-09-15 | Chase Pharmaceuticals Corporation | Peripheral-anticholinergic muscarinic agonist combination |
| US10307409B2 (en) * | 2015-03-06 | 2019-06-04 | Chase Pharmaceuticals Corporation | Muscarinic combinations and their use for combating hypocholinergic disorders of the central nervous system |
| CN108024967B (zh) | 2015-06-15 | 2021-12-21 | 库姆制药有限责任公司 | 格隆铵脂肪酸盐及其制备方法 |
| US20180360845A1 (en) * | 2015-07-20 | 2018-12-20 | Chase Pharmaceuticals Corporation | Muscarinic combination of a selective m2-antagonist and a peripheral non-selective antagonist for treating hypocholinergic disorders |
| CA2996717A1 (en) | 2015-09-11 | 2017-03-16 | Chase Pharmaceuticals Corporation | Muscarinic combination and its use for combating hypocholinergic disorders of the central nervous system |
| WO2017147104A1 (en) * | 2016-02-24 | 2017-08-31 | Chase Pharmaceuticals Corporation | Muscarinic m2-antagonist combinations |
| US10479706B2 (en) * | 2016-06-03 | 2019-11-19 | Katz Water Tech, Llc | Apparatus, method and system for desalinating water |
| WO2018081508A1 (en) * | 2016-10-28 | 2018-05-03 | Chase Pharmaceutical Corporation | Memantine combinations and use |
| BR112020021173A2 (pt) * | 2018-04-17 | 2021-01-19 | Lts Lohmann Therapie-Systeme Ag | Sistema terapêutico transdérmico para a administração transdérmica de solifenacina |
| KR102408292B1 (ko) | 2018-09-28 | 2022-06-10 | 카루나 세러퓨틱스 인코포레이티드 | 무스카린성 수용체 활성화에 의해 개선된 장애의 치료를 위한 조성물 및 방법 |
| WO2022058940A1 (ko) * | 2020-09-21 | 2022-03-24 | 닥터레이몬드 랩(주) | 인지 능력 개선 또는 기억력 증진용 의약 조성물 |
| WO2022111500A1 (en) * | 2020-11-26 | 2022-06-02 | Rezubio Pharmaceuticals Co., Ltd | Anticholinergic agents |
| US12109202B2 (en) | 2021-01-29 | 2024-10-08 | Qaam Pharmaceuticals, Llc | Fixed dose combination of cholinesterase inhibitor and a quaternary ammonium antimuscarinic agent to treat neurodegenerative cognitive disorders |
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| US8097633B2 (en) * | 2006-11-15 | 2012-01-17 | Rich Steven A | Uses for quaternary ammonium anticholinergic muscarinic receptor antagonists in patients being treated for cognitive impairment or acute delirium |
| WO2011034568A1 (en) * | 2009-09-18 | 2011-03-24 | Chase Pharmaceuticals Corporation | Method and composition for treating alzheimer-type dementia |
| AU2009229372C1 (en) | 2008-03-27 | 2017-02-02 | Chase Pharmaceuticals Corporation | Use and composition for treating dementia |
-
2009
- 2009-03-17 AU AU2009229372A patent/AU2009229372C1/en not_active Ceased
- 2009-03-17 EP EP22177194.2A patent/EP4088717A1/en not_active Withdrawn
- 2009-03-17 DK DK09726036.8T patent/DK2271218T3/en active
- 2009-03-17 MX MX2013009019A patent/MX344177B/es unknown
- 2009-03-17 MX MX2014004035A patent/MX347901B/es unknown
- 2009-03-17 PL PL09726036T patent/PL2271218T3/pl unknown
- 2009-03-17 CA CA2718411A patent/CA2718411C/en active Active
- 2009-03-17 EP EP17150365.9A patent/EP3178477A1/en not_active Withdrawn
- 2009-03-17 EP EP09726036.8A patent/EP2271218B1/en not_active Revoked
- 2009-03-17 US US12/934,140 patent/US8404701B2/en active Active
- 2009-03-17 ES ES09726036.8T patent/ES2634421T3/es active Active
- 2009-03-17 JP JP2011501792A patent/JP5647099B2/ja not_active Expired - Fee Related
- 2009-03-17 WO PCT/US2009/001662 patent/WO2009120277A1/en not_active Ceased
- 2009-03-17 MX MX2010010460A patent/MX2010010460A/es active IP Right Grant
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2013
- 2013-02-12 US US13/765,240 patent/US20130158012A1/en not_active Abandoned
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2014
- 2014-01-14 JP JP2014004320A patent/JP2014114295A/ja active Pending
- 2014-05-29 US US14/290,123 patent/US9044472B2/en active Active
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2015
- 2015-04-27 US US14/696,861 patent/US20150224096A1/en not_active Abandoned
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2016
- 2016-04-11 JP JP2016078787A patent/JP6427522B2/ja not_active Expired - Fee Related
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2018
- 2018-11-21 US US16/198,517 patent/US20190091214A1/en not_active Abandoned
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