CN109069466B - 5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病 - Google Patents
5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病 Download PDFInfo
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- CN109069466B CN109069466B CN201780028711.1A CN201780028711A CN109069466B CN 109069466 B CN109069466 B CN 109069466B CN 201780028711 A CN201780028711 A CN 201780028711A CN 109069466 B CN109069466 B CN 109069466B
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- China
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- pharmaceutically acceptable
- apathy
- disease
- alzheimer
- treatment
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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
- A61K31/40—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil
- A61K31/403—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with one nitrogen as the only ring hetero atom, e.g. sulpiride, succinimide, tolmetin, buflomedil condensed with carbocyclic rings, e.g. carbazole
- A61K31/404—Indoles, e.g. pindolol
- A61K31/4045—Indole-alkylamines; Amides thereof, e.g. serotonin, melatonin
-
- 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
- A61K31/21—Esters, e.g. nitroglycerine, selenocyanates
- A61K31/27—Esters, e.g. nitroglycerine, selenocyanates of carbamic or thiocarbamic acids, meprobamate, carbachol, neostigmine
-
- 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
- A61K31/325—Carbamic acids; Thiocarbamic acids; Anhydrides or salts thereof
-
- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/44—Non condensed pyridines; Hydrogenated derivatives thereof
- A61K31/445—Non condensed piperidines, e.g. piperocaine
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/496—Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene or sparfloxacin
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/505—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
- A61K31/519—Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim ortho- or peri-condensed with heterocyclic rings
-
- 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
- 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
- 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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Epidemiology (AREA)
- Emergency Medicine (AREA)
- Biomedical Technology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- Hospice & Palliative Care (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201600286 | 2016-05-11 | ||
| DKPA201600286 | 2016-05-11 | ||
| PCT/EP2017/060979 WO2017194496A1 (en) | 2016-05-11 | 2017-05-09 | 5ht6 receptor antagonists for use in the treatment of alzheimer's disease with apathy as comorbidity |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| CN109069466A CN109069466A (zh) | 2018-12-21 |
| CN109069466B true CN109069466B (zh) | 2021-06-15 |
Family
ID=58707519
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CN201780028711.1A Active CN109069466B (zh) | 2016-05-11 | 2017-05-09 | 5-ht6受体拮抗剂用于治疗阿尔茨海默病伴情感淡漠共病 |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10864191B2 (https=) |
| EP (1) | EP3454848B1 (https=) |
| JP (2) | JP6961622B2 (https=) |
| CN (1) | CN109069466B (https=) |
| BR (1) | BR112018000568A2 (https=) |
| ES (1) | ES2826386T3 (https=) |
| WO (1) | WO2017194496A1 (https=) |
Families Citing this family (4)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10864191B2 (en) * | 2016-05-11 | 2020-12-15 | H. Lundbeck A/S | 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity |
| BR112019001145A2 (pt) * | 2017-05-24 | 2019-04-30 | H. Lundbeck A/S | combinação de um antagonista do receptor 5-ht6 e de um inibidor de acetilcolinesterase para uso no tratamento da doença de alzheimer em uma subpopulação de pacientes portadores de alelos de apoe4 |
| CA3104811C (en) * | 2017-06-30 | 2024-05-28 | Chase Therapeutics Corporation | Composition comprising pramipexole and nk1-antagonists for treating depression |
| JP2023510082A (ja) | 2019-12-02 | 2023-03-13 | スヴェン・ライフ・サイエンシーズ・リミテッド | 認知症患者における行動・心理症状を治療するための方法 |
Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009093206A2 (ru) * | 2008-01-24 | 2009-07-30 | Alla Chem, Llc | 3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| CN104619344A (zh) * | 2012-09-09 | 2015-05-13 | H.隆德贝克有限公司 | 治疗阿尔茨海默病的方法及其药物组合物 |
Family Cites Families (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US2006641A (en) * | 1932-09-26 | 1935-07-02 | Charles E Johnson | Hydraulic tappet |
| DK1859798T3 (en) | 2001-03-29 | 2016-03-21 | Lilly Co Eli | N- (2-arylethyl) -BENZYLAMINER as antagonists of 5-HT6 receptor |
| PE20071143A1 (es) * | 2006-01-13 | 2008-01-20 | Wyeth Corp | Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6 |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| EP2508177A1 (en) | 2007-12-12 | 2012-10-10 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| US8629154B2 (en) | 2008-01-24 | 2014-01-14 | Andrey Alexandrovich Ivashchenko | Substituted cycloalcano[e and d] pyrazolo [1,5-a]pyrimidines/antagonists of serotonin 5-HT6 receptors and methods for production and the use thereof |
| KR20100119776A (ko) | 2008-01-24 | 2010-11-10 | 알라 캠, 엘엘씨 | 2-알킬아미노-3-아릴설포닐-사이클로알카노[e 또는 d]피라졸로[1,5-A]피리미딘/세로토닌 5-HT6 수용체의 길항제, 이의 제조방법 및 이의 용도 |
| US8309559B2 (en) | 2008-01-24 | 2012-11-13 | Nikolay Filippovich Savchuk | (EN) substituted 2-amino-3-sulfonyl-pyrazolo[1,5-A] pyrimidines/antagonists of serotonin 5-HT6 receptors, methods for the production and the use thereof |
| US10864191B2 (en) | 2016-05-11 | 2020-12-15 | H. Lundbeck A/S | 5-HT6 receptor antagonists for use in the treatment of Alzheimer's disease with apathy as comorbidity |
-
2017
- 2017-05-05 US US15/587,935 patent/US10864191B2/en active Active
- 2017-05-09 WO PCT/EP2017/060979 patent/WO2017194496A1/en not_active Ceased
- 2017-05-09 EP EP17723326.9A patent/EP3454848B1/en active Active
- 2017-05-09 JP JP2018559275A patent/JP6961622B2/ja active Active
- 2017-05-09 ES ES17723326T patent/ES2826386T3/es active Active
- 2017-05-09 BR BR112018000568A patent/BR112018000568A2/pt not_active Application Discontinuation
- 2017-05-09 CN CN201780028711.1A patent/CN109069466B/zh active Active
-
2021
- 2021-10-13 JP JP2021168436A patent/JP7217789B2/ja active Active
Patent Citations (2)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2009093206A2 (ru) * | 2008-01-24 | 2009-07-30 | Alla Chem, Llc | 3-CУЛЬФOHИЛ-ПИPAЗOЛO[1,5-a]ПИPИMИДИHЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-HT6РЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| CN104619344A (zh) * | 2012-09-09 | 2015-05-13 | H.隆德贝克有限公司 | 治疗阿尔茨海默病的方法及其药物组合物 |
Non-Patent Citations (5)
| Title |
|---|
| A prospective longitudinal study of apathy in Alzheimer’s disease;S E Starkstein;《J Neurol Neurosurg Psychiatry》;20051216;第77卷(第1期);第8-11页 * |
| Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands;Kevin G. Liu;《Bioorganic & Medicinal Chemistry Letters》;20090503;第3214-3216页 * |
| Kevin G. Liu.Identification of a novel series of 3-piperidinyl-5-sulfonylindazoles as potent 5-HT6 ligands.《Bioorganic & Medicinal Chemistry Letters》.2009,第3214-3216页. * |
| Safety and effi cacy of idalopirdine, a 5-HT6 receptor antagonist, in patients with moderate Alzheimer’s disease (LADDER): a randomised, double-blind, placebo-controlled phase 2 trial;David Wilkinson;《Lancet Neurol》;20141006;第13卷(第11期);第1092-1099页 * |
| The 5-HT6 receptor antagonist idalopirdine potentiates the effects of acetylcholinesterase inhibition on neuronal network oscillations and extracellular acetylcholine levels in the rat dorsal hippocampus;Kjartan F. Herrik;《Neuro pharmacology》;20160331(第107期);第351-363页 * |
Also Published As
| Publication number | Publication date |
|---|---|
| EP3454848B1 (en) | 2020-09-09 |
| US10864191B2 (en) | 2020-12-15 |
| JP6961622B2 (ja) | 2021-11-05 |
| US20170326107A1 (en) | 2017-11-16 |
| JP2019518736A (ja) | 2019-07-04 |
| WO2017194496A1 (en) | 2017-11-16 |
| ES2826386T3 (es) | 2021-05-18 |
| JP2022009121A (ja) | 2022-01-14 |
| EP3454848A1 (en) | 2019-03-20 |
| BR112018000568A2 (pt) | 2018-09-11 |
| CN109069466A (zh) | 2018-12-21 |
| JP7217789B2 (ja) | 2023-02-03 |
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| PB01 | Publication | ||
| SE01 | Entry into force of request for substantive examination | ||
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| GR01 | Patent grant | ||
| GR01 | Patent grant |