SV2017005434A - 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 - Google Patents
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 alzheimerInfo
- Publication number
- SV2017005434A SV2017005434A SV2017005434A SV2017005434A SV2017005434A SV 2017005434 A SV2017005434 A SV 2017005434A SV 2017005434 A SV2017005434 A SV 2017005434A SV 2017005434 A SV2017005434 A SV 2017005434A SV 2017005434 A SV2017005434 A SV 2017005434A
- Authority
- SV
- El Salvador
- Prior art keywords
- alzheimer
- disease
- tetrahydropiridins
- difluoro
- phenyl
- Prior art date
Links
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 229940125759 BACE1 protease inhibitor Drugs 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 239000003112 inhibitor Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B59/00—Introduction of isotopes of elements into organic compounds ; Labelled organic compounds per se
- C07B59/002—Heterocyclic compounds
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D211/00—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings
- C07D211/04—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
- C07D211/68—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member
- C07D211/72—Heterocyclic compounds containing hydrogenated pyridine rings, not condensed with other rings with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having one double bond between ring members or between a ring member and a non-ring member with hetero atoms or with carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, directly attached to ring carbon atoms
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07B—GENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
- C07B2200/00—Indexing scheme relating to specific properties of organic compounds
- C07B2200/05—Isotopically modified compounds, e.g. labelled
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Hydrogenated Pyridines (AREA)
- Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
Abstract
LA PRESENTE INVENCIÓN SE DIRIGE A COMPUESTOS DE ACUERDO CON LA FÓRMULA I: (VER FORMULA); COMPUESTOS QUE SON INHIBIDORES DE LA ENZIMA BACE1. ASPECTOS SEPARADOS DE LA INVENCIÓN SE DIRIGEN A COMPOSICIONES FARMACÉUTICAS QUE COMPRENDEN DICHOS COMPUESTOS Y A USOS DE LOS COMPUESTOS PARA TRATAR TRASTORNOS PARA LOS CUALES LA REDUCCIÓN DE DEPÓSITOS DE ABETA ES BENEFICIOSA TAL COMO LA ENFERMEDAD DE ALZHEIMER
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| DKPA201400649 | 2014-11-10 | ||
| DKPA201500450 | 2015-08-07 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| SV2017005434A true SV2017005434A (es) | 2017-07-19 |
Family
ID=54476983
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| SV2017005434A SV2017005434A (es) | 2014-11-10 | 2017-05-09 | 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 |
Country Status (26)
| Country | Link |
|---|---|
| US (1) | US10059669B2 (es) |
| EP (1) | EP3218362B1 (es) |
| JP (1) | JP2017533253A (es) |
| KR (1) | KR20170082529A (es) |
| CN (1) | CN107074809A (es) |
| AU (1) | AU2015345257A1 (es) |
| BR (1) | BR112017009647A2 (es) |
| CA (1) | CA2964305A1 (es) |
| CL (1) | CL2017001113A1 (es) |
| CO (1) | CO2017004530A2 (es) |
| CR (1) | CR20170187A (es) |
| DO (1) | DOP2017000118A (es) |
| EA (1) | EA201790817A1 (es) |
| EC (1) | ECSP17028463A (es) |
| ES (1) | ES2710602T3 (es) |
| IL (1) | IL252091A0 (es) |
| MX (1) | MX2017006048A (es) |
| NI (1) | NI201700056A (es) |
| PE (1) | PE20170947A1 (es) |
| PH (1) | PH12017500829A1 (es) |
| RU (1) | RU2017116197A (es) |
| SG (1) | SG11201703177WA (es) |
| SV (1) | SV2017005434A (es) |
| TN (1) | TN2017000134A1 (es) |
| WO (1) | WO2016075062A1 (es) |
| ZA (1) | ZA201702799B (es) |
Families Citing this family (17)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| 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 |
| 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 |
| EP3334720A1 (en) | 2015-08-12 | 2018-06-20 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors |
| US10034861B2 (en) | 2016-07-04 | 2018-07-31 | H. Lundbeck A/S | 1H-pyrazolo[4,3-b]pyridines as PDE1 inhibitors |
| CN106366073B (zh) * | 2016-10-24 | 2018-11-30 | 扬子江药业集团南京海陵药业有限公司 | 一种盐酸替吡嘧啶的制备方法 |
| SG11201903770UA (en) | 2016-10-28 | 2019-05-30 | H Lundbeck As | Combination treatments comprising imidazopyrazinones for the treatment of psychiatric and/or cognitive disorders |
| KR20190077349A (ko) | 2016-10-28 | 2019-07-03 | 하. 룬드벡 아크티에셀스카브 | 이미다조피라지논의 투여를 포함하는 병용 치료 |
| BR112018017058A2 (pt) * | 2016-12-21 | 2019-07-02 | H Lundbeck As | 6-amino-5-fluoro-5-(fluorometil)-2,3,4,5-tetra-hidropiridin-2-il-fenil-5-(metóxi-d3)-pirazina-2-carboxamidas e derivados fluorados do mesmo como inibidores de bace1 |
| AR113926A1 (es) | 2017-12-14 | 2020-07-01 | H Lundbeck As | Derivados de 1h-pirazolo[4,3-b]piridinas |
| RS62551B1 (sr) | 2017-12-14 | 2021-12-31 | H Lundbeck As | Kombinovane terapije koje obuhvataju primenu 1h-pirazolo[4,3-b]piridina |
| CN117447475A (zh) | 2017-12-20 | 2024-01-26 | H.隆德贝克有限公司 | 作为PDE1抑制剂的吡唑并[4,3-b]吡啶和咪唑并[1,5-a]嘧啶 |
| CN109970681A (zh) * | 2019-04-19 | 2019-07-05 | 安徽海康药业有限责任公司 | 一种瑞格列奈的合成方法 |
| CN113720930A (zh) * | 2021-07-26 | 2021-11-30 | 南京一诺医药科技有限公司 | 一种hplc-ms/ms联用检测人血浆中奥美拉唑的方法 |
| CN114235985A (zh) * | 2021-11-25 | 2022-03-25 | 南京海纳医药科技股份有限公司 | 一种hplc-ms/ms联用检测人血浆中胍法辛的方法 |
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 |
| PT1474395E (pt) | 2002-02-12 | 2008-01-02 | Smithkline Beecham Corp | Derivados de nicotinamida úteis como inibidores de p38 |
| 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 |
| SG185651A1 (en) * | 2010-06-09 | 2012-12-28 | Janssen Pharmaceutica Nv | 5,6-dihydro-2h-[1,4]oxazin-3-yl-amine derivatives useful as inhibitors of beta-secretase (bace) |
| JP2014505688A (ja) | 2011-01-12 | 2014-03-06 | ノバルティス アーゲー | オキサジン誘導体および神経障害の処置におけるその使用 |
| AU2012206561B2 (en) | 2011-01-13 | 2015-12-17 | 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 |
| CN103608345A (zh) | 2011-04-26 | 2014-02-26 | 盐野义制药株式会社 | 噁嗪衍生物和含有该噁嗪衍生物的bace1抑制剂 |
| KR20140041687A (ko) | 2011-06-07 | 2014-04-04 | 에프. 호프만-라 로슈 아게 | Bace1 및/또는 bace2 억제제로서의 할로겐-알킬-1,3-옥사진 |
| 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 |
| JP2015514073A (ja) | 2012-03-20 | 2015-05-18 | エラン ファーマシューティカルズ， リミテッド・ライアビリティ・カンパニー | スピロ環式ジヒドロ−チアジンおよびジヒドロ−オキサジンｂａｃｅ阻害剤、ならびにその組成物および使用 |
| WO2014056816A1 (en) | 2012-10-10 | 2014-04-17 | F. Hoffmann-La Roche Ag | COMBINATION OF AN Aβ ANTIBODY AND A BACE INHIBITOR |
| US9556135B2 (en) * | 2012-10-12 | 2017-01-31 | Amgen, Inc. | Amino-dihydrothiazine and amino-dioxido dihydrothiazine compounds as beta-secretase antagonists and methods of use |
| EP2912035A4 (en) | 2012-10-24 | 2016-06-15 | Shionogi & Co | DERIVATIVES OF DIHYDROOXAZINE OR OXAZEPINE HAVING BACE1 INHIBITING ACTIVITY |
| MX366855B (es) | 2013-03-01 | 2019-07-26 | Amgen Inc | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. |
| TWI639607B (zh) | 2013-06-18 | 2018-11-01 | 美國禮來大藥廠 | Ｂａｃｅ抑制劑 |
| CR20160352A (es) * | 2014-02-19 | 2016-10-20 | H Lundbeck As | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer |
| 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 |
| 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 |
| 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 |
| EP3334720A1 (en) | 2015-08-12 | 2018-06-20 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridins as bace1 inhibitors |
-
2014
- 2014-11-09 CR CR20170187A patent/CR20170187A/es unknown
-
2015
- 2015-11-09 WO PCT/EP2015/076014 patent/WO2016075062A1/en not_active Ceased
- 2015-11-09 US US15/524,479 patent/US10059669B2/en not_active Expired - Fee Related
- 2015-11-09 CN CN201580060814.7A patent/CN107074809A/zh active Pending
- 2015-11-09 EP EP15790975.5A patent/EP3218362B1/en active Active
- 2015-11-09 ES ES15790975T patent/ES2710602T3/es active Active
- 2015-11-09 EA EA201790817A patent/EA201790817A1/ru unknown
- 2015-11-09 TN TN2017000134A patent/TN2017000134A1/en unknown
- 2015-11-09 JP JP2017525124A patent/JP2017533253A/ja active Pending
- 2015-11-09 BR BR112017009647A patent/BR112017009647A2/pt not_active Application Discontinuation
- 2015-11-09 MX MX2017006048A patent/MX2017006048A/es unknown
- 2015-11-09 KR KR1020177012461A patent/KR20170082529A/ko not_active Withdrawn
- 2015-11-09 CA CA2964305A patent/CA2964305A1/en not_active Abandoned
- 2015-11-09 AU AU2015345257A patent/AU2015345257A1/en not_active Abandoned
- 2015-11-09 PE PE2017000827A patent/PE20170947A1/es unknown
- 2015-11-09 RU RU2017116197A patent/RU2017116197A/ru unknown
- 2015-11-09 SG SG11201703177WA patent/SG11201703177WA/en unknown
-
2017
- 2017-04-20 ZA ZA2017/02799A patent/ZA201702799B/en unknown
- 2017-05-03 IL IL252091A patent/IL252091A0/en unknown
- 2017-05-04 CL CL2017001113A patent/CL2017001113A1/es unknown
- 2017-05-04 PH PH12017500829A patent/PH12017500829A1/en unknown
- 2017-05-05 CO CONC2017/0004530A patent/CO2017004530A2/es unknown
- 2017-05-09 DO DO2017000118A patent/DOP2017000118A/es unknown
- 2017-05-09 SV SV2017005434A patent/SV2017005434A/es unknown
- 2017-05-09 EC ECIEPI201728463A patent/ECSP17028463A/es unknown
- 2017-05-10 NI NI201700056A patent/NI201700056A/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| IL252091A0 (en) | 2017-07-31 |
| ZA201702799B (en) | 2018-08-29 |
| CR20170187A (es) | 2018-02-01 |
| JP2017533253A (ja) | 2017-11-09 |
| DOP2017000118A (es) | 2017-07-15 |
| KR20170082529A (ko) | 2017-07-14 |
| EP3218362B1 (en) | 2019-01-09 |
| WO2016075062A1 (en) | 2016-05-19 |
| US20170313658A1 (en) | 2017-11-02 |
| US10059669B2 (en) | 2018-08-28 |
| ES2710602T3 (es) | 2019-04-26 |
| MX2017006048A (es) | 2017-06-19 |
| NI201700056A (es) | 2017-09-22 |
| CA2964305A1 (en) | 2016-05-19 |
| PH12017500829A1 (en) | 2017-10-09 |
| CO2017004530A2 (es) | 2017-07-28 |
| RU2017116197A (ru) | 2018-12-13 |
| ECSP17028463A (es) | 2017-08-31 |
| CN107074809A (zh) | 2017-08-18 |
| BR112017009647A2 (pt) | 2017-12-19 |
| SG11201703177WA (en) | 2017-05-30 |
| AU2015345257A1 (en) | 2017-05-04 |
| TN2017000134A1 (en) | 2018-10-19 |
| PE20170947A1 (es) | 2017-07-13 |
| CL2017001113A1 (es) | 2017-12-01 |
| EP3218362A1 (en) | 2017-09-20 |
| EA201790817A1 (ru) | 2017-09-29 |
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