JO3458B1 - 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 - Google Patents
2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1Info
- Publication number
- JO3458B1 JO3458B1 JOP/2015/0260A JOP20150260A JO3458B1 JO 3458 B1 JO3458 B1 JO 3458B1 JO P20150260 A JOP20150260 A JO P20150260A JO 3458 B1 JO3458 B1 JO 3458B1
- Authority
- JO
- Jordan
- Prior art keywords
- span
- tetrahydropyridine
- difluoromethyl
- difluoro
- phenyl
- Prior art date
Links
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
- C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
- C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links
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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
- A61K31/435—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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/4439—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. omeprazole
-
- 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
- A61K31/4427—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems
- A61K31/444—Non condensed pyridines; Hydrogenated derivatives thereof containing further heterocyclic ring systems containing a six-membered ring with nitrogen as a ring heteroatom, e.g. amrinone
-
- 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
- A61K31/4965—Non-condensed pyrazines
- A61K31/497—Non-condensed pyrazines containing further heterocyclic rings
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D417/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
- C07D417/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings
- C07D417/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Biomedical Technology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Pyridine Compounds (AREA)
Abstract
يتم توجيه الاختراع الحالي إلى مثبطات جديدة لإنزيم <span dir="LTR"> BACE 1</span>. يتم توجيه السمات المنفصلة من الاختراع إلى تركيبات صيدلانية تشمل المركبات المذكورة و استخدامات المركبات لعلاج اضطربات يكون من المفيد لها خفص رواسب <span dir="LTR">A</span><span dir="LTR">β</span> مثل مرض الزهايمر.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400648 | 2014-11-10 | ||
| DKPA201500447 | 2015-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| JO3458B1 true JO3458B1 (ar) | 2020-07-05 |
Family
ID=54783558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| JOP/2015/0260A JO3458B1 (ar) | 2014-11-10 | 2015-10-25 | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
Country Status (44)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3627B1 (ar) | 2015-04-30 | 2020-08-27 | H Lundbeck As | إيميدازو بيرازينونات على هيئة مثبطات pde1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| US20180244645A1 (en) * | 2015-08-12 | 2018-08-30 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| JOP20190081A1 (ar) * | 2016-10-13 | 2019-04-11 | Novartis Ag | مشتق أوكسازين للاستخدام في علاج أو الوقاية من اعتلال وعائي دماغي نشواني |
| BR112018013084A2 (pt) | 2016-10-28 | 2018-12-11 | H Lundbeck As | tratamentos de combinação compreendendo a administração de imidazopirazinonas |
| SG11201903770UA (en) | 2016-10-28 | 2019-05-30 | H Lundbeck As | Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders |
| WO2018114910A1 (en) | 2016-12-21 | 2018-06-28 | H. Lundbeck A/S | 6-amino-5-fluoro-5-(fluoromethyl)-2,3,4,5-tetrahydropyridin-2-yl-phenyl-5-(methoxy-d3)-pyrazine-2-carboxamides and fluorinated derivatives thereof as bace1 inhibitors |
| LT3723807T (lt) | 2017-12-14 | 2021-12-10 | H. Lundbeck A/S | Kombinuoti gydymai, apimantys 1h-pirazolo[4,3-b]piridinų vartojimą |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| US11535611B2 (en) | 2017-12-20 | 2022-12-27 | H. Lundbeck A/S | Pyrazolo[3,4-B]pyridines and imidazo[1,5-B]pyridazines as PDE1 inhibitors |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2002100399A1 (en) | 2001-06-12 | 2002-12-19 | Elan Pharmaceuticals, Inc. | Macrocycles useful in the treatment of alzheimer's disease |
| GB0124928D0 (en) | 2001-10-17 | 2001-12-05 | Glaxo Group Ltd | Chemical compounds |
| BRPI0307351B8 (pt) | 2002-02-12 | 2021-05-25 | Smithkline Beecham Corp | composto, composição farmacêutica, uso de um composto, e, processo para preparar um composto |
| AR077277A1 (es) | 2009-07-09 | 2011-08-17 | Lilly Co Eli | Compuestos de biciclo (1,3)tiazin-2-amina formulacion farmaceutica que lo comprende y su uso para la manufactura de un medicamento util para el tratamiento de la enfermedad de alzheimer |
| AU2011263797B2 (en) * | 2010-06-09 | 2014-06-05 | Janssen Pharmaceutica Nv | 5,6-dihydro-2H-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (BACE) |
| EA201391029A1 (ru) | 2011-01-12 | 2014-01-30 | Новартис Аг | Производные оксазина и их применение при лечении неврологических нарушений |
| CA2824220C (en) | 2011-01-13 | 2020-09-01 | Novartis Ag | Novel heterocyclic derivatives and their use in the treatment of neurological disorders |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| WO2012147763A1 (ja) | 2011-04-26 | 2012-11-01 | 塩野義製薬株式会社 | オキサジン誘導体およびそれを含有するｂａｃｅ１阻害剤 |
| US8987255B2 (en) * | 2011-06-07 | 2015-03-24 | Hoffmann-La Roche Inc. | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| UY34278A (es) | 2011-08-25 | 2013-04-05 | Novartis Ag | Derivados novedosos de oxazina y su uso en el tratamiento de enfermedades |
| US8338413B1 (en) | 2012-03-07 | 2012-12-25 | Novartis Ag | Oxazine derivatives and their use in the treatment of neurological disorders |
| HK1206597A1 (en) | 2012-03-20 | 2016-01-15 | 艾朗制药股份有限公司 | Spirocyclic dihydro-thiazine and dihydro-oxazine bace inhibitors, and compositions and uses thereof |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Ｂａｃｅ抑制劑 |
| TW201609700A (zh) | 2014-02-19 | 2016-03-16 | Ｈ 朗德貝克公司 | ２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶作爲ｂａｃｅ１抑制劑用於治療阿茲海默症 |
| TW201623295A (zh) | 2014-04-11 | 2016-07-01 | 塩野義製藥股份有限公司 | 具有ｂａｃｅ１抑制活性之二氫噻及二氫衍生物 |
| MA40941A (fr) | 2014-11-10 | 2017-09-19 | H Lundbeck As | 2-amino-5,5-difluoro-6-(fluorométhyl)-6-phényl-3,4,5,6-tétrahydropyridines comme inhibiteurs de bace1 |
| CR20170187A (es) | 2014-11-10 | 2018-02-01 | H Lundbeck As | 2-Amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de BACE1 para el tratamiento de la enfermedad de Alzheimer |
| JO3458B1 (ar) | 2014-11-10 | 2020-07-05 | H Lundbeck As | 2- أمينو-6- (دايفلوروميثيل) – 5، 5- ديفلورو-6-فينيل-3،4، 5، 6-تيتراهيدروبيريدين كمثبطات bace1 |
| TW201717948A (zh) | 2015-08-10 | 2017-06-01 | Ｈ 朗德貝克公司 | 包括給予２－胺基－３，５，５－三氟－３，４，５，６－四氫吡啶的聯合治療 |
| US20180244645A1 (en) | 2015-08-12 | 2018-08-30 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as bace1 inhibitors |
| WO2018114910A1 (en) | 2016-12-21 | 2018-06-28 | H. Lundbeck A/S | 6-amino-5-fluoro-5-(fluoromethyl)-2,3,4,5-tetrahydropyridin-2-yl-phenyl-5-(methoxy-d3)-pyrazine-2-carboxamides and fluorinated derivatives thereof as bace1 inhibitors |
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2015
- 2015-10-25 JO JOP/2015/0260A patent/JO3458B1/ar active
- 2015-11-05 US US14/933,301 patent/US9346797B1/en not_active Expired - Fee Related
- 2015-11-09 PL PL15805109T patent/PL3218365T3/pl unknown
- 2015-11-09 MA MA40955A patent/MA40955B1/fr unknown
- 2015-11-09 UA UAA201704639A patent/UA119576C2/uk unknown
- 2015-11-09 EP EP15805109.4A patent/EP3218365B1/en active Active
- 2015-11-09 TN TN2017000144A patent/TN2017000144A1/en unknown
- 2015-11-09 TW TW104136839A patent/TWI690318B/zh not_active IP Right Cessation
- 2015-11-09 US US15/524,546 patent/US10045974B2/en not_active Expired - Fee Related
- 2015-11-09 GE GEAP201814485A patent/GEAP201814485A/en unknown
- 2015-11-09 CR CR20170186A patent/CR20170186A/es unknown
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- 2015-11-09 JP JP2017525010A patent/JP6629320B2/ja not_active Expired - Fee Related
- 2015-11-09 HR HRP20181698TT patent/HRP20181698T1/hr unknown
- 2015-11-09 SM SM20180570T patent/SMT201800570T1/it unknown
- 2015-11-09 DK DK15805109.4T patent/DK3218365T3/en active
- 2015-11-09 ME MEP-2018-267A patent/ME03723B/me unknown
- 2015-11-09 MX MX2017006049A patent/MX2017006049A/es unknown
- 2015-11-09 GE GEAP201514485A patent/GEP20196949B/en unknown
- 2015-11-09 AU AU2015345258A patent/AU2015345258B2/en not_active Expired - Fee Related
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- 2015-11-09 HU HUE15805109A patent/HUE040304T2/hu unknown
- 2015-11-09 WO PCT/EP2015/076015 patent/WO2016075063A1/en not_active Ceased
- 2015-11-09 KR KR1020177012442A patent/KR20170081184A/ko not_active Withdrawn
- 2015-11-09 SG SG11201703547XA patent/SG11201703547XA/en unknown
- 2015-11-09 CN CN201580060803.9A patent/CN107074836B/zh not_active Expired - Fee Related
- 2015-11-09 EP EP18198764.5A patent/EP3461483A1/en not_active Withdrawn
- 2015-11-09 BR BR112017009583A patent/BR112017009583A2/pt not_active Application Discontinuation
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- 2015-11-09 PE PE2017000825A patent/PE20170946A1/es unknown
- 2015-11-09 CA CA2965563A patent/CA2965563A1/en not_active Abandoned
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- 2015-11-09 RU RU2017116196A patent/RU2017116196A/ru not_active Application Discontinuation
- 2015-11-09 LT LTEP15805109.4T patent/LT3218365T/lt unknown
- 2015-11-09 EA EA201790818A patent/EA032339B1/ru not_active IP Right Cessation
- 2015-11-09 RS RS20181321A patent/RS57946B1/sr unknown
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2017
- 2017-04-20 ZA ZA2017/02797A patent/ZA201702797B/en unknown
- 2017-05-03 CO CONC2017/0004465A patent/CO2017004465A2/es unknown
- 2017-05-03 IL IL252089A patent/IL252089B/en not_active IP Right Cessation
- 2017-05-04 CL CL2017001112A patent/CL2017001112A1/es unknown
- 2017-05-05 PH PH12017500841A patent/PH12017500841B1/en unknown
- 2017-05-09 EC ECIEPI201728459A patent/ECSP17028459A/es unknown
- 2017-05-09 DO DO2017000117A patent/DOP2017000117A/es unknown
- 2017-05-09 SV SV2017005435A patent/SV2017005435A/es unknown
- 2017-05-09 NI NI201700055A patent/NI201700055A/es unknown
- 2017-05-10 GT GT201700099A patent/GT201700099A/es unknown
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2018
- 2018-08-09 US US16/059,715 patent/US10603310B2/en not_active Expired - Fee Related
- 2018-11-13 CY CY20181101200T patent/CY1120846T1/el unknown
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