JP2019518736A5 - - Google Patents
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- Publication number
- JP2019518736A5 JP2019518736A5 JP2018559275A JP2018559275A JP2019518736A5 JP 2019518736 A5 JP2019518736 A5 JP 2019518736A5 JP 2018559275 A JP2018559275 A JP 2018559275A JP 2018559275 A JP2018559275 A JP 2018559275A JP 2019518736 A5 JP2019518736 A5 JP 2019518736A5
- Authority
- JP
- Japan
- Prior art keywords
- pharmaceutical composition
- pharmaceutically acceptable
- receptor antagonist
- acceptable salt
- composition according
- 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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- 150000003839 salts Chemical class 0.000 claims description 20
- 239000003751 serotonin 6 antagonist Substances 0.000 claims description 19
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 claims description 17
- 239000000544 cholinesterase inhibitor Substances 0.000 claims description 17
- ADEBPBSSDYVVLD-UHFFFAOYSA-N donepezil Chemical group O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 ADEBPBSSDYVVLD-UHFFFAOYSA-N 0.000 claims description 14
- 239000008194 pharmaceutical composition Substances 0.000 claims description 14
- YBAWYTYNMZWMMJ-UHFFFAOYSA-N 2-(6-fluoro-1h-indol-3-yl)-n-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine Chemical group FC(F)C(F)(F)COC1=CC=CC(CNCCC=2C3=CC=C(F)C=C3NC=2)=C1 YBAWYTYNMZWMMJ-UHFFFAOYSA-N 0.000 claims description 11
- 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 claims description 8
- 229960003530 donepezil Drugs 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 4
- 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 4
- 229960003135 donepezil hydrochloride Drugs 0.000 claims description 3
- XWAIAVWHZJNZQQ-UHFFFAOYSA-N donepezil hydrochloride Chemical group [H+].[Cl-].O=C1C=2C=C(OC)C(OC)=CC=2CC1CC(CC1)CCN1CC1=CC=CC=C1 XWAIAVWHZJNZQQ-UHFFFAOYSA-N 0.000 claims description 3
- KSAUCBGUWGWPDL-UHFFFAOYSA-N 3-(benzenesulfonyl)-5,7-dimethyl-2-methylsulfanylpyrazolo[1,5-a]pyrimidine Chemical compound CSC1=NN2C(C)=CC(C)=NC2=C1S(=O)(=O)C1=CC=CC=C1 KSAUCBGUWGWPDL-UHFFFAOYSA-N 0.000 claims description 2
- JJZFWROHYSMCMU-UHFFFAOYSA-N 3-(benzenesulfonyl)-8-piperazin-1-ylquinoline Chemical compound C=1N=C2C(N3CCNCC3)=CC=CC2=CC=1S(=O)(=O)C1=CC=CC=C1 JJZFWROHYSMCMU-UHFFFAOYSA-N 0.000 claims description 2
- 206010002942 Apathy 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
- 230000000694 effects Effects 0.000 claims description 2
- 229960003980 galantamine Drugs 0.000 claims description 2
- 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 2
- 239000002464 receptor antagonist Substances 0.000 claims description 2
- 229940044551 receptor antagonist Drugs 0.000 claims description 2
- 229960004136 rivastigmine Drugs 0.000 claims description 2
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
- 230000002708 enhancing effect Effects 0.000 description 1
Priority Applications (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| JP2021168436A JP7217789B2 (ja) | 2016-05-11 | 2021-10-13 | 併存疾患としてアパシーを伴うアルツハイマー病の治療における使用のための５－ｈｔ６受容体アンタゴニスト |
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 |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021168436A Division JP7217789B2 (ja) | 2016-05-11 | 2021-10-13 | 併存疾患としてアパシーを伴うアルツハイマー病の治療における使用のための５－ｈｔ６受容体アンタゴニスト |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2019518736A JP2019518736A (ja) | 2019-07-04 |
| JP2019518736A5 true JP2019518736A5 (enExample) | 2020-06-18 |
| JP6961622B2 JP6961622B2 (ja) | 2021-11-05 |
Family
ID=58707519
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018559275A Active JP6961622B2 (ja) | 2016-05-11 | 2017-05-09 | 併存疾患としてアパシーを伴うアルツハイマー病の治療における使用のための５−ｈｔ６受容体アンタゴニスト |
| JP2021168436A Active JP7217789B2 (ja) | 2016-05-11 | 2021-10-13 | 併存疾患としてアパシーを伴うアルツハイマー病の治療における使用のための５－ｈｔ６受容体アンタゴニスト |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2021168436A Active JP7217789B2 (ja) | 2016-05-11 | 2021-10-13 | 併存疾患としてアパシーを伴うアルツハイマー病の治療における使用のための５－ｈｔ６受容体アンタゴニスト |
Country Status (7)
| Country | Link |
|---|---|
| US (1) | US10864191B2 (enExample) |
| EP (1) | EP3454848B1 (enExample) |
| JP (2) | JP6961622B2 (enExample) |
| CN (1) | CN109069466B (enExample) |
| BR (1) | BR112018000568A2 (enExample) |
| ES (1) | ES2826386T3 (enExample) |
| WO (1) | WO2017194496A1 (enExample) |
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 |
| PT3630098T (pt) | 2017-05-24 | 2021-04-21 | H Lundbeck As | Combinação de um antagonista do receptor 5-ht6 e de um inibidor de acetilcolinesterase para utilização no tratamento da doença de alzheimer numa subpopulação de pacientes portadores de alelos apoe4 |
| BR112019028034A2 (pt) * | 2017-06-30 | 2020-07-07 | Chase Therapeutics Corporation | composições de antagonista de nk-1 e métodos para uso no tratamento da depressão |
| CN114761008B (zh) | 2019-12-02 | 2024-07-19 | 苏文生命科学有限公司 | 用于在患有痴呆的患者中治疗行为和心理症状的方法 |
Family Cites Families (11)
| 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 |
| EP2254564A1 (en) | 2007-12-12 | 2010-12-01 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| RU2369600C1 (ru) | 2008-01-24 | 2009-10-10 | Андрей Александрович Иващенко | ЗАМЕЩЕННЫЕ 4-СУЛЬФОНИЛ-ПИРАЗОЛЫ И 3-СУЛЬФОНИЛ-ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ5-HT6 РЕЦЕПТОРОВ, АКТИВНЫЙ КОМПОНЕНТ, ФАРМАЦЕВТИЧЕСКАЯ КОМПОЗИЦИЯ, ЛЕКАРСТВЕННОЕ СРЕДСТВО И СПОСОБЫ ИХ ПОЛУЧЕНИЯ |
| EA017818B1 (ru) | 2008-01-24 | 2013-03-29 | Андрей Александрович ИВАЩЕНКО | ЗАМЕЩЕННЫЕ ЦИКЛОАЛКАНО[e ИЛИ d]ПИРАЗОЛО[1,5-a]ПИРИМИДИНЫ - АНТАГОНИСТЫ СЕРОТОНИНОВЫХ 5-НТРЕЦЕПТОРОВ, СПОСОБЫ ИХ ПОЛУЧЕНИЯ И ПРИМЕНЕНИЯ |
| EP2248817B1 (en) | 2008-01-24 | 2015-01-07 | Alla Chem, LLC. | Substituted 2-amino-3-sulfonyl-pyrazolo[1,5-a] pyrimidines/antagonists of serotonin 5-ht6 receptors, methods for the production and the use thereof |
| JP5584626B2 (ja) | 2008-01-24 | 2014-09-03 | アンドレイ・アレクサンドロビッチ・イワシェンコ | ２−アルキルアミノ−３−（アリールスルホニル）−シクロアルキル［ｅ又はｄ］ピラゾロ［１，５−ａ］ピリミジン−セロトニン５−ＨＴ６受容体アンタゴニスト、その調製の方法及び使用 |
| JO3459B1 (ar) * | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
| 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 CN CN201780028711.1A patent/CN109069466B/zh active Active
- 2017-05-09 ES ES17723326T patent/ES2826386T3/es active Active
- 2017-05-09 JP JP2018559275A patent/JP6961622B2/ja active Active
- 2017-05-09 BR BR112018000568A patent/BR112018000568A2/pt not_active Application Discontinuation
- 2017-05-09 EP EP17723326.9A patent/EP3454848B1/en active Active
-
2021
- 2021-10-13 JP JP2021168436A patent/JP7217789B2/ja active Active
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