JP2015528471A5 - - Google Patents
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- JP2015528471A5 JP2015528471A5 JP2015530420A JP2015530420A JP2015528471A5 JP 2015528471 A5 JP2015528471 A5 JP 2015528471A5 JP 2015530420 A JP2015530420 A JP 2015530420A JP 2015530420 A JP2015530420 A JP 2015530420A JP 2015528471 A5 JP2015528471 A5 JP 2015528471A5
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- 239000008194 pharmaceutical composition Substances 0.000 claims description 22
- 150000001875 compounds Chemical class 0.000 claims description 15
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 claims description 14
- -1 2- (6-fluoro-1H-indol-3-yl) ethyl Chemical group 0.000 claims description 13
- 150000003839 salts Chemical class 0.000 claims description 9
- 239000000544 cholinesterase inhibitor Substances 0.000 claims description 8
- 239000000203 mixture Substances 0.000 claims description 8
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 claims description 7
- 208000024827 Alzheimer disease Diseases 0.000 claims description 5
- 230000036470 plasma concentration Effects 0.000 claims description 5
- 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 4
- 108091005435 5-HT6 receptors Proteins 0.000 claims description 2
- 102000012440 Acetylcholinesterase Human genes 0.000 claims description 2
- 108010022752 Acetylcholinesterase Proteins 0.000 claims description 2
- VEXZGXHMUGYJMC-UHFFFAOYSA-N Hydrochloric acid Chemical group Cl VEXZGXHMUGYJMC-UHFFFAOYSA-N 0.000 claims description 2
- XSVMFMHYUFZWBK-NSHDSACASA-N Rivastigmine Chemical group CCN(C)C(=O)OC1=CC=CC([C@H](C)N(C)C)=C1 XSVMFMHYUFZWBK-NSHDSACASA-N 0.000 claims description 2
- 229940022698 acetylcholinesterase Drugs 0.000 claims description 2
- 229960003530 donepezil Drugs 0.000 claims description 2
- 230000000694 effects Effects 0.000 claims description 2
- 230000002708 enhancing effect Effects 0.000 claims description 2
- 239000012729 immediate-release (IR) formulation Substances 0.000 claims description 2
- 108020003175 receptors Proteins 0.000 claims description 2
- 229960004136 rivastigmine Drugs 0.000 claims description 2
- 238000002560 therapeutic procedure Methods 0.000 claims description 2
- YBAWYTYNMZWMMJ-UHFFFAOYSA-N 2-(6-fluoro-1h-indol-3-yl)-n-[[3-(2,2,3,3-tetrafluoropropoxy)phenyl]methyl]ethanamine Chemical compound FC(F)C(F)(F)COC1=CC=CC(CNCCC=2C3=CC=C(F)C=C3NC=2)=C1 YBAWYTYNMZWMMJ-UHFFFAOYSA-N 0.000 description 7
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 description 6
- 125000004377 trifluoropropoxy group Chemical group FC(CCO*)(F)F 0.000 description 2
- XRQGMTXHIBWGAJ-UHFFFAOYSA-N 1-phenyl-n-(2,2,3,3-tetrafluoropropoxy)methanamine Chemical compound FC(F)C(F)(F)CONCC1=CC=CC=C1 XRQGMTXHIBWGAJ-UHFFFAOYSA-N 0.000 description 1
- VZAUDURHBQEVDH-UHFFFAOYSA-N [3-(2,2,3,3-tetrafluoropropoxy)phenyl]methanamine Chemical compound FC(COC=1C=C(CN)C=CC=1)(C(F)F)F VZAUDURHBQEVDH-UHFFFAOYSA-N 0.000 description 1
- 201000010099 disease Diseases 0.000 description 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 description 1
Applications Claiming Priority (5)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698664P | 2012-09-09 | 2012-09-09 | |
| US61/698,664 | 2012-09-09 | ||
| US201361782084P | 2013-03-14 | 2013-03-14 | |
| US61/782,084 | 2013-03-14 | ||
| PCT/EP2013/068516 WO2014037532A1 (en) | 2012-09-09 | 2013-09-06 | Methods of treating alzheimer's disease and pharmaceutical compositions thereof |
Related Child Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018228631A Division JP2019059760A (ja) | 2012-09-09 | 2018-12-06 | アルツハイマー病の治療方法およびその医薬組成物 |
Publications (3)
| Publication Number | Publication Date |
|---|---|
| JP2015528471A JP2015528471A (ja) | 2015-09-28 |
| JP2015528471A5 true JP2015528471A5 (enExample) | 2016-10-20 |
| JP6693744B2 JP6693744B2 (ja) | 2020-05-13 |
Family
ID=49118521
Family Applications (2)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2015530420A Active JP6693744B2 (ja) | 2012-09-09 | 2013-09-06 | アルツハイマー病の治療方法およびその医薬組成物 |
| JP2018228631A Pending JP2019059760A (ja) | 2012-09-09 | 2018-12-06 | アルツハイマー病の治療方法およびその医薬組成物 |
Family Applications After (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JP2018228631A Pending JP2019059760A (ja) | 2012-09-09 | 2018-12-06 | アルツハイマー病の治療方法およびその医薬組成物 |
Country Status (33)
Families Citing this family (31)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| NZ544331A (en) | 2003-07-22 | 2010-03-26 | Arena Pharm Inc | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto |
| EP2254564A1 (en) | 2007-12-12 | 2010-12-01 | Glaxo Group Limited | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-quinoline |
| WO2009123714A2 (en) | 2008-04-02 | 2009-10-08 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| US9126946B2 (en) | 2008-10-28 | 2015-09-08 | Arena Pharmaceuticals, Inc. | Processes useful for the preparation of 1-[3-(4-bromo-2-methyl-2H-pyrazol-3-yl)-4-methoxy-phenyl]-3-(2,4-difluoro-phenyl)urea and crystalline forms related thereto |
| JO3459B1 (ar) | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
| JO3509B1 (ar) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| JP6294953B2 (ja) | 2013-03-14 | 2018-03-14 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐ２ｘ７調節物質 |
| ES2689526T3 (es) | 2013-03-14 | 2018-11-14 | Janssen Pharmaceutica Nv | Moduladores de P2X7 |
| TWI599567B (zh) | 2013-03-14 | 2017-09-21 | 健生藥品公司 | Ｐ２ｘ７調節劑 |
| EA029052B1 (ru) | 2013-03-14 | 2018-02-28 | Бёрингер Ингельхайм Интернациональ Гмбх | Замещенные (бензилцианометил)амиды 2-азабицикло[2.2.1]гептан-3-карбоновых кислот в качестве ингибиторов катепсина с |
| JO3639B1 (ar) | 2014-07-04 | 2020-08-27 | H Lundbeck As | صورة متعددة الشكل جديدة لـ n-[2-(6-فلورو-1h-إندول-3-يل)إيثيل]-3-(2،2،3،3-تترا فلورو بروبوكسي)بنزيل أمين هيدروكلوريد |
| AU2015315693B2 (en) | 2014-09-12 | 2020-01-16 | Janssen Pharmaceutica Nv | P2X7 modulating n-acyl-triazolopyrazines |
| WO2016039977A1 (en) | 2014-09-12 | 2016-03-17 | Janssen Pharmaceutica Nv | P2x7 modulators |
| HUE047208T2 (hu) | 2014-09-12 | 2020-04-28 | Boehringer Ingelheim Int | A katepszin-C spirociklikus inhibitorai |
| CN105175307A (zh) * | 2014-11-18 | 2015-12-23 | 苏州晶云药物科技有限公司 | Lu AE58054的盐酸盐晶型A及其制备方法和用途 |
| WO2016179569A1 (en) * | 2015-05-07 | 2016-11-10 | Axovant Sciences Ltd. | Compositions and methods of treating a neurodegenerative disease |
| JP2018516992A (ja) | 2015-06-12 | 2018-06-28 | アクソファント サイエンシーズ ゲーエムベーハーＡｘｏｖａｎｔ Ｓｃｉｅｎｃｅｓ Ｇｍｂｈ | レム睡眠行動障害の予防および処置のために有用なジアリールおよびアリールヘテロアリール尿素誘導体 |
| CN108472285A (zh) | 2015-07-15 | 2018-08-31 | 阿速万科学有限责任公司 | 用于预防和治疗与神经退行性疾病相关联的幻觉的二芳基和芳基杂芳基脲衍生物 |
| KR102473545B1 (ko) * | 2016-04-26 | 2022-12-01 | 하. 룬드벡 아크티에셀스카브 | 파킨슨병 환자에서 낙상을 감소시키기 위한 아세틸콜린에스테라아제 억제제 및 아이달로피르딘의 용도 |
| 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 |
| KR102015484B1 (ko) | 2016-05-18 | 2019-08-28 | 수벤 라이프 사이언시스 리미티드 | 순수한 5-ht6 수용체 길항제와 아세틸콜린에스테라제 저해제의 조합물 |
| CN106309436A (zh) * | 2016-07-25 | 2017-01-11 | 宁波大学 | 可用作乙酰胆碱酯酶抑制剂的色胺衍生物及其用途 |
| CN107118146B (zh) * | 2017-04-13 | 2019-09-03 | 宁波大学 | 一种6-溴色胺衍生物及其制备方法和用途 |
| RS61704B1 (sr) * | 2017-05-24 | 2021-05-31 | H Lundbeck As | Kombinacija antagonista 5-ht6 receptora i inhibitora acetilholinesteraze za upotrebu u lečenju alchajmerove bolesti kod subpopulacije pacijenata koji nose apoe4 alele |
| JP7413368B2 (ja) | 2018-09-28 | 2024-01-15 | ヤンセン ファーマシューティカ エヌ．ベー． | モノアシルグリセロールリパーゼ調節因子 |
| MA53721A (fr) | 2018-09-28 | 2021-09-15 | Janssen Pharmaceutica Nv | Modulateurs de la monoacylglycérol lipase |
| CA3156100A1 (en) | 2019-09-30 | 2021-04-08 | Janssen Pharmaceutica Nv | Radiolabelled mgl pet ligands |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
| CA3176946A1 (en) | 2020-03-26 | 2021-09-30 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| EP3960174B1 (en) | 2020-08-28 | 2024-10-30 | Westfälische Wilhelms-Universität Münster | Parasympathetic active phenyl-glycosid-substituted hydroxy-methyl-piperidine and -pyrrolidine alkaloids for medicinal use |
| JP2026514626A (ja) * | 2024-03-22 | 2026-05-13 | クイーン アーリック | マグネシウム・リドカイン組成物 |
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| US3597149A (en) | 1969-04-29 | 1971-08-03 | Showa Denko Kk | Inhibition of gas-fume fading of dyed cellulose acetate material |
| FR2181559A1 (en) | 1972-04-28 | 1973-12-07 | Aec Chimie Organique Bio | N-Phenylalkyl-N-3-indolylalkyl-alkylamines - with sedative, neuroleptic, analgesic, hypotensive, antiserotonin, adrenolytic activity |
| JPS5764632A (en) | 1980-10-09 | 1982-04-19 | Mitsui Toatsu Chem Inc | Novel 2-arylethyl ether derivative and thioether derivative, their production and insecticide and acaricide |
| US5202336A (en) | 1986-09-24 | 1993-04-13 | Bayer Aktiengesellschaft | Antiflammatory quinolin methoxy phenylsulphonamides |
| DE3632329A1 (de) | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| SE9103745D0 (sv) | 1991-12-18 | 1991-12-18 | Wikstroem Haakan | Aryl-triflates and related compounds |
| WO1995006638A1 (en) | 1993-09-01 | 1995-03-09 | Allelix Biopharmaceuticals Inc. | Tryptamine analogs with 5-ht1d selectivity |
| US5504101A (en) | 1994-05-06 | 1996-04-02 | Allelix Biopharmaceuticals, Inc. | 5-HT-1D receptor ligands |
| KR20010040254A (ko) | 1997-09-29 | 2001-05-15 | 스티븐 엘. 네스빗 | 아미노알킬페놀 유도체 및 관련 화합물 |
| GB9820113D0 (en) | 1998-09-15 | 1998-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| AU767009B2 (en) | 1998-12-11 | 2003-10-30 | Virginia Commonwealth University | Selective 5-HT6 receptor ligands |
| HK1044539A1 (zh) | 1999-01-13 | 2002-10-25 | 千年药品公司 | 作为趋化因子受体调节剂的官能化杂环 |
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| ES2566056T3 (es) | 2001-03-29 | 2016-04-08 | Eli Lilly And Company | N-(2-ariletil)bencilaminas como antagonistas del receptor 5-HT6 |
| RU2252936C2 (ru) | 2002-12-05 | 2005-05-27 | Институт физиологически активных веществ РАН | S-замещенные n-1-[(гетеро)арил]алкил-n`-[(гетеро)арил]алкилизотиомочевины, способ их получения, фармацевтическая композиция, способ изучения глутаматэргической системы, способы лечения (варианты) |
| PE20071143A1 (es) | 2006-01-13 | 2008-01-20 | Wyeth Corp | Composicion farmaceutica que comprende un inhibidor de acetilcolinesterasa y un antagonista 5-hidroxitriptamina-6 |
| JP2009541423A (ja) | 2006-06-23 | 2009-11-26 | ラボラトリオス・デル・ドクトル・エステベ・ソシエダッド・アノニマ | コリンエステラーゼ阻害剤と５‐ｈｔ６レセプター親和性の化合物との組合せ |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| US20120184532A1 (en) * | 2009-07-23 | 2012-07-19 | Shire Llc | Galantamine amino acid and peptide prodrugs and uses thereof |
| TW201139370A (en) | 2009-12-23 | 2011-11-16 | Lundbeck & Co As H | Processes for the manufacture of a pharmaceutically active agent |
| JO3459B1 (ar) * | 2012-09-09 | 2020-07-05 | H Lundbeck As | تركيبات صيدلانية لعلاج مرض الزهايمر |
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2013
- 2013-08-21 JO JOP/2013/0248A patent/JO3459B1/ar active
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 SM SM20180678T patent/SMT201800678T1/it unknown
- 2013-09-06 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt unknown
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active Ceased
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2013-09-06 EA EA201590353A patent/EA030448B1/ru not_active IP Right Cessation
- 2013-09-06 BR BR112015005117-0A patent/BR112015005117B1/pt active IP Right Grant
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active Active
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en not_active Ceased
- 2013-09-09 US US14/021,033 patent/US9375418B2/en active Active
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2015
- 2015-02-23 IL IL237369A patent/IL237369B/en active IP Right Grant
- 2015-03-02 TN TNP2015000076A patent/TN2015000076A1/fr unknown
- 2015-03-06 CL CL2015000578A patent/CL2015000578A1/es unknown
- 2015-03-06 NI NI201500031A patent/NI201500031A/es unknown
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2016
- 2016-03-30 US US15/084,712 patent/US9687473B2/en active Active
- 2016-06-28 US US15/194,947 patent/US9789085B2/en active Active
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2017
- 2017-09-06 US US15/696,880 patent/US10660878B2/en active Active
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2018
- 2018-12-06 JP JP2018228631A patent/JP2019059760A/ja active Pending
- 2018-12-21 CY CY181101390T patent/CY1121062T1/el unknown