IL237369B - N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease - Google Patents
N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's diseaseInfo
- Publication number
- IL237369B IL237369B IL237369A IL23736915A IL237369B IL 237369 B IL237369 B IL 237369B IL 237369 A IL237369 A IL 237369A IL 23736915 A IL23736915 A IL 23736915A IL 237369 B IL237369 B IL 237369B
- Authority
- IL
- Israel
- Prior art keywords
- tetrafluoropropoxy
- benzylamine
- indol
- fluoro
- disease
- Prior art date
Links
- WGQKYBSKWIADBV-UHFFFAOYSA-N benzylamine Chemical compound NCC1=CC=CC=C1 WGQKYBSKWIADBV-UHFFFAOYSA-N 0.000 title 2
- 229940100578 Acetylcholinesterase inhibitor Drugs 0.000 title 1
- 208000024827 Alzheimer disease Diseases 0.000 title 1
- 239000000544 cholinesterase inhibitor Substances 0.000 title 1
- 125000001495 ethyl group Chemical group [H]C([H])([H])C([H])([H])* 0.000 title 1
Classifications
-
- 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
- A61K31/33—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
- A61K31/55—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
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- 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
-
- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
Landscapes
- Health & Medical Sciences (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Chemical & Material Sciences (AREA)
- Epidemiology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Organic Chemistry (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Emergency Medicine (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
- Medicines That Contain Protein Lipid Enzymes And Other Medicines (AREA)
Applications Claiming Priority (3)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201261698664P | 2012-09-09 | 2012-09-09 | |
| US201361782084P | 2013-03-14 | 2013-03-14 | |
| PCT/EP2013/068516 WO2014037532A1 (en) | 2012-09-09 | 2013-09-06 | Methods of treating alzheimer's disease and pharmaceutical compositions thereof |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| IL237369A0 IL237369A0 (en) | 2015-04-30 |
| IL237369B true IL237369B (en) | 2018-11-29 |
Family
ID=49118521
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| IL237369A IL237369B (en) | 2012-09-09 | 2015-02-23 | N-]2-(6-fluoro-h1-indol-3-yl)ethyl]-3-(2, 2, 3, 3- tetrafluoropropoxy) benzylamine in combination with an acetylcholinesterase inhibitor for the treatment of Alzheimer's disease |
Country Status (33)
Families Citing this family (31)
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| DE602004000260T2 (de) | 2003-07-22 | 2006-08-24 | Arena Pharmaceuticals, Inc., San Diego | Diaryl- und arylheteroarylharnstoffderivate als modulatoren des 5-ht2a-serotoninrezeptors, die sich zur prophylaxe und behandlung von damit im zusammenhang stehenden erkrankungen eignen |
| 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 |
| JO3773B1 (ar) | 2013-03-14 | 2021-01-31 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| JO3509B1 (ar) | 2013-03-14 | 2020-07-05 | Janssen Pharmaceutica Nv | معدلات p2x7 |
| EP3112366B1 (en) | 2013-03-14 | 2018-02-28 | Janssen Pharmaceutica NV | P2x7 modulators |
| WO2014140075A1 (en) | 2013-03-14 | 2014-09-18 | Boehringer Ingelheim International Gmbh | Substituted 2-aza-bicyclo[2.2.1]heptane-3-carboxylic acid (benzyl-cyano-methyl)-amides inhibitors of cathepsin c |
| JP6467404B2 (ja) | 2013-03-14 | 2019-02-13 | ヤンセン ファーマシューティカ エヌ．ベー． | Ｐ２ｘ７モジュレーター |
| 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 |
| JP2017526716A (ja) | 2014-09-12 | 2017-09-14 | ベーリンガー インゲルハイム インターナショナル ゲゼルシャフト ミット ベシュレンクテル ハフツング | カテプシンｃのスピロ環状阻害剤 |
| CA2960972C (en) | 2014-09-12 | 2023-10-03 | Janssen Pharmaceutica Nv | P2x7 modulating n-acyl-triazolopyrazines |
| 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 |
| 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 |
| MX2017014192A (es) * | 2015-05-07 | 2018-08-01 | Axovant Sciences Gmbh | Composiciones y metodos de tratamiento de una enfermedad neurodegenerativa. |
| 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 |
| MX387444B (es) * | 2016-04-26 | 2025-03-18 | H Lundbeck As | Uso de un inhibidor de la acetilcolinesterasa e idalopirdina para reducir las caidas en pacientes con la 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 |
| EP3484467B1 (en) | 2016-05-18 | 2020-04-29 | Suven Life Sciences Limited | Combination of pure 5-ht6 receptor antagonists with acetylcholinesterase inhibitors |
| 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 |
| JP7167065B2 (ja) * | 2017-05-24 | 2022-11-08 | ハー・ルンドベック・アクチエゼルスカベット | Ａｐｏｅ４アレルを有する患者亜集団におけるアルツハイマー病の治療での使用のための５－ｈｔ６受容体アンタゴニストとアセチルコリンエステラーゼ阻害剤の組み合わせ |
| 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 |
| MY205440A (en) | 2018-09-28 | 2024-10-21 | Janssen Pharmaceutica Nv | Monoacylglycerol lipase modulators |
| 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 |
| MX2022011902A (es) | 2020-03-26 | 2023-01-04 | Janssen Pharmaceutica Nv | Moduladores de la monoacilglicerol lipasa. |
| 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 |
| WO2025198622A1 (en) * | 2024-03-22 | 2025-09-25 | Queen Aaric | Magnesium and lidocaine composition |
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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 |
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| 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 |
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| 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 |
| US20110098278A1 (en) * | 2009-07-23 | 2011-04-28 | 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 DK DK13759195.4T patent/DK2892563T3/en active
- 2013-09-06 TW TW102132182A patent/TWI632909B/zh active
- 2013-09-06 GE GEAP201313752A patent/GEP201706776B/en unknown
- 2013-09-06 SI SI201331303T patent/SI2892563T1/sl unknown
- 2013-09-06 KR KR1020207034028A patent/KR102342127B1/ko active Active
- 2013-09-06 NZ NZ630589A patent/NZ630589A/en unknown
- 2013-09-06 PL PL13759195T patent/PL2892563T3/pl unknown
- 2013-09-06 RU RU2015107877A patent/RU2675786C2/ru active
- 2013-09-06 LT LTEP13759195.4T patent/LT2892563T/lt unknown
- 2013-09-06 MY MYPI2015000575A patent/MY182539A/en unknown
- 2013-09-06 CA CA2883751A patent/CA2883751C/en active Active
- 2013-09-06 KR KR1020157007345A patent/KR20150065680A/ko not_active Ceased
- 2013-09-06 AU AU2013311573A patent/AU2013311573B2/en active Active
- 2013-09-06 JP JP2015530420A patent/JP6693744B2/ja active Active
- 2013-09-06 CN CN201380046768.6A patent/CN104619344A/zh active Pending
- 2013-09-06 WO PCT/EP2013/068516 patent/WO2014037532A1/en not_active Ceased
- 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 MX MX2015002879A patent/MX368305B/es active IP Right Grant
- 2013-09-06 SM SM20180678T patent/SMT201800678T1/it unknown
- 2013-09-06 SG SG11201501774QA patent/SG11201501774QA/en unknown
- 2013-09-06 ES ES13759195T patent/ES2703630T3/es active Active
- 2013-09-06 EP EP13759195.4A patent/EP2892563B1/en active Active
- 2013-09-06 RS RS20181571A patent/RS58104B1/sr unknown
- 2013-09-06 AP AP2015008306A patent/AP2015008306A0/xx unknown
- 2013-09-06 HR HRP20182069TT patent/HRP20182069T1/hr unknown
- 2013-09-06 PT PT13759195T patent/PT2892563T/pt 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
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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
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