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 |
|---|---|---|---|---|
| US8754238B2 (en) | 2003-07-22 | 2014-06-17 | Arena Pharmaceuticals, Inc. | Diaryl and arylheteroaryl urea derivatives as modulators of the 5-HT2A serotonin receptor useful for the prophylaxis and treatment of disorders related thereto |
| US9084742B2 (en) | 2007-12-12 | 2015-07-21 | Axovant Sciences Ltd. | Combinations comprising 3-phenylsulfonyl-8-piperazinyl-1yl-Quinoline |
| US20110021538A1 (en) | 2008-04-02 | 2011-01-27 | Arena Pharmaceuticals, Inc. | Processes for the preparation of pyrazole derivatives useful as modulators of the 5-ht2a serotonin receptor |
| WO2010062321A1 (en) | 2008-10-28 | 2010-06-03 | 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 |
| 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 |
| GEP201706780B (en) | 2013-03-14 | 2017-11-27 | Boehringer Ingelheim Int | Substituted 2-aza-bicyclo [2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c |
| TWI627174B (zh) | 2013-03-14 | 2018-06-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調控劑 |
| TWI644671B (zh) | 2013-03-14 | 2018-12-21 | 比利時商健生藥品公司 | Ｐ２ｘ７調節劑 |
| WO2014152537A1 (en) | 2013-03-14 | 2014-09-25 | Janssen Pharmaceutica Nv | P2x7 modulators |
| 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 |
| EA201790600A1 (ru) | 2014-09-12 | 2017-07-31 | Янссен Фармацевтика Нв | Модулирующие p2x7 n-ацил-триазолопиразины |
| JP6592510B2 (ja) | 2014-09-12 | 2019-10-16 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐ２ｘ７調節因子 |
| UA118610C2 (uk) | 2014-09-12 | 2019-02-11 | Бьорінгер Інгельхайм Інтернаціональ Гмбх | Спіроциклічні інгібітори катепсину c |
| 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 |
| WO2016179566A1 (en) * | 2015-05-07 | 2016-11-10 | Axovant Sciences Ltd. | Methods of treating a neurodegenerative disease |
| RU2017145976A (ru) | 2015-06-12 | 2019-07-15 | Аксовант Сайенсиз Гмбх | Производные диарил- и арилгетероарилмочевины, применимые для профилактики и лечения нарушения поведения во время REM-фазы сна |
| TW201720439A (zh) | 2015-07-15 | 2017-06-16 | Axovant Sciences Gmbh | 用於預防及治療與神經退化性疾病相關的幻覺之作為５－ｈｔ２ａ血清素受體的二芳基及芳基雜芳基脲衍生物 |
| ES2949288T3 (es) * | 2016-04-26 | 2023-09-27 | H Lundbeck As | Uso de un inhibidor de acetilcolinesterasa e idalopirdina para reducir las caídas en pacientes con enfermedad de Parkinson |
| 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 |
| HUE050819T2 (hu) | 2016-05-18 | 2021-01-28 | Suven Life Sciences Ltd | Tiszta 5-HT6 receptor antagonisták kombinációja acetilkolinészteráz inhibitorokkal |
| 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 |
| SG11201909895UA (en) * | 2017-05-24 | 2019-11-28 | H Lundbeck As | Combination of a 5-ht6 receptor antagonist and an acetylcholinesterase inhibitor for use in the treatment of alzheimer's disease in a patient subpopulation carrying apoe4 alleles |
| WO2020065614A1 (en) | 2018-09-28 | 2020-04-02 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| CN113164459B (zh) | 2018-09-28 | 2024-09-03 | 詹森药业有限公司 | 单酰基甘油脂肪酶调节剂 |
| ES3037365T3 (en) | 2019-09-30 | 2025-10-01 | Janssen Pharmaceutica Nv | Radiolabelled mgl pet ligands |
| NL2024431B1 (en) | 2019-12-11 | 2021-09-07 | Sulfateq Bv | Compounds for treatment of alzheimer’s disease |
| BR112022019077A2 (pt) | 2020-03-26 | 2022-12-27 | Janssen Pharmaceutica Nv | Moduladores da monoacilglicerol lipase |
| 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 |
| CN121013715A (zh) * | 2024-03-22 | 2025-11-25 | 艾瑞克·奎因 | 镁和利多卡因组合物 |
Family Cites Families (21)
| Publication number | Priority date | Publication date | Assignee | Title |
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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 |
| DE3632329A1 (de) | 1986-09-24 | 1988-03-31 | Bayer Ag | Substituierte phenylsulfonamide |
| US5202336A (en) | 1986-09-24 | 1993-04-13 | Bayer Aktiengesellschaft | Antiflammatory quinolin methoxy phenylsulphonamides |
| SE9103745D0 (sv) | 1991-12-18 | 1991-12-18 | Wikstroem Haakan | Aryl-triflates and related compounds |
| AU685837B2 (en) | 1993-09-01 | 1998-01-29 | 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 |
| WO1999016746A1 (en) | 1997-09-29 | 1999-04-08 | Aventis Pharmaceuticals Inc. | Aminoalkylphenol derivatives and related compounds |
| GB9820113D0 (en) | 1998-09-15 | 1998-11-11 | Merck Sharp & Dohme | Therapeutic agents |
| DE69930308T2 (de) | 1998-12-11 | 2006-11-30 | Virginia Commonwealth University | Selektive 5-ht 6-rezeptor-liganden |
| AP2001002228A0 (en) | 1999-01-13 | 2001-09-30 | Millenium Pharmaceuticals Inc | Functionalized heterocycles as chemokine receptor modulators. |
| US6750348B1 (en) | 1999-03-24 | 2004-06-15 | Anormed, Inc. | Chemokine receptor binding heterocyclic compounds |
| CZ305838B6 (cs) | 2001-03-29 | 2016-04-06 | Eli Lilly And Company | N-(2-arylethyl)benzylaminy jako antagonisté receptoru 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 |
| ATE509636T1 (de) | 2006-06-23 | 2011-06-15 | Esteve Labor Dr | Kombination aus einem cholinesterase-hemmer und einer verbindung mit 5-ht6-rezeptor-affinität |
| AR061637A1 (es) | 2006-06-26 | 2008-09-10 | Epix Delaware Inc | Composiciones y metodos de tratamiento de trastornos del snc |
| JP2013500268A (ja) * | 2009-07-23 | 2013-01-07 | シャイア エルエルシー | ガランタミンアミノ酸およびペプチドプロドラッグならびにその使用 |
| 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 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 SM SM20180678T patent/SMT201800678T1/it unknown
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en not_active Ceased
- 2013-09-06 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active Ceased
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt unknown
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active Active
- 2013-09-06 BR BR112015005117-0A patent/BR112015005117B1/pt active IP Right Grant
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 EA EA201590353A patent/EA030448B1/ru not_active IP Right Cessation
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 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 NI NI201500031A patent/NI201500031A/es unknown
- 2015-03-06 CL CL2015000578A patent/CL2015000578A1/es unknown
-
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
-
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
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