PE20170946A1 - 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 - Google Patents
2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1Info
- Publication number
- PE20170946A1 PE20170946A1 PE2017000825A PE2017000825A PE20170946A1 PE 20170946 A1 PE20170946 A1 PE 20170946A1 PE 2017000825 A PE2017000825 A PE 2017000825A PE 2017000825 A PE2017000825 A PE 2017000825A PE 20170946 A1 PE20170946 A1 PE 20170946A1
- Authority
- PE
- Peru
- Prior art keywords
- difluoro
- phenyl
- amino
- tetrahydropyridines
- difluorometil
- Prior art date
Links
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
- A61K31/435—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
- 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
-
- 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
Abstract
Se refiere a compuestos derivados de 2-amino-6-(difluorometil)-5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas de formula (I) donde Ar es fenilo, piridilo, entre otros opcionalmente sustituido; R1 es H, halogeno, entre otros. Es un compuesto seleccionado (S)-N-(3-(6-amino-2-(difluorometil)-3,3-difluoro-2,3,4,5-tetrahidropiridin-2-il)-4-fluorofenil)-5-cloropicolinamida; entre otros. Tambien se refiere a una composicion farmaceutica que la contiene. Dichos compuestos son inhibidores de la enzima beta-secretasa 1 (BACE1) siendo utiles para tratar trastornos para los cuales la reduccion de depositos de beta-amiloides es beneficioso, tal como la enfermedad de Alzheimer
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 |
|---|---|
| PE20170946A1 true PE20170946A1 (es) | 2017-07-13 |
Family
ID=54783558
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2017000825A PE20170946A1 (es) | 2014-11-10 | 2015-11-09 | 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 |
Country Status (43)
Families Citing this family (14)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| 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 |
| US10011596B2 (en) * | 2015-08-12 | 2018-07-03 | 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 |
| MX2019004763A (es) | 2016-10-28 | 2019-07-01 | H Lundbeck As | Tratamientos de combinacion que comprenden imidazopirazinonas para el tratamiento de trastornos psiquiatricos y/o cognitivos. |
| SG11201903061YA (en) | 2016-10-28 | 2019-05-30 | H Lundbeck As | Combination treatments comprising administration of imidazopyrazinones |
| 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 |
| US11634416B2 (en) | 2017-12-14 | 2023-04-25 | H. Lundbeck A/S | Combination treatments comprising administration of 1H-pyrazolo[4,3-b]pyridines |
| EP3728250A1 (en) | 2017-12-20 | 2020-10-28 | H. Lundbeck A/S | PYRAZOLO[3,4-beta]PYRIDINES AND IMIDAZO[1,5-beta]PYRIDAZINES AS PDE1 INHIBITORS |
Family Cites Families (25)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2450167A1 (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 |
| DE60316913T2 (de) | 2002-02-12 | 2008-11-20 | Smithkline Beecham Corp. | Nicotinamide und deren verwendung als p38 inhibitoren |
| 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 |
| EP2580200B1 (en) * | 2010-06-09 | 2016-09-14 | Janssen Pharmaceutica, N.V. | 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 |
| SI2663561T1 (sl) | 2011-01-13 | 2016-07-29 | Novartis Ag | Novi heterociklični derivati in njihova uporaba v zdravljenju nevroloških obolenj |
| US8754075B2 (en) * | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| EP2703399A4 (en) | 2011-04-26 | 2014-10-15 | Shionogi & Co | OXAZINE DERIVATIVE AND BACE-1 HEMMER THEREOF |
| 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 |
| CA2867851A1 (en) | 2012-03-20 | 2013-09-26 | Elan Pharmaceuticals, Inc. | 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 |
| AU2014223334C1 (en) | 2013-03-01 | 2018-10-18 | Amgen Inc. | Perfluorinated 5,6-dihydro-4H-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| JO3318B1 (ar) | 2013-06-18 | 2019-03-13 | Lilly Co Eli | مثبطات bace |
| EA031132B1 (ru) | 2014-02-19 | 2018-11-30 | Х. Лундбекк А/С | 2-амино-3,5,5-трифтор-3,4,5,6-тетрагидропиридины в качестве ингибиторов bace1 для лечения болезни альцгеймера |
| 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 |
| 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 |
| 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 |
| US10011596B2 (en) | 2015-08-12 | 2018-07-03 | H. Lundbeck A/S | 2-amino-3-fluoro-3-(fluoromethyl)-6-methyl-6-phenyl-3,4,5,6-tetrahydropyridines as BACE1 inhibitors |
| 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 |
-
2015
- 2015-10-25 JO JOP/2015/0260A patent/JO3458B1/ar active
- 2015-11-05 US US14/933,301 patent/US9346797B1/en active Active
- 2015-11-09 SG SG11201703547XA patent/SG11201703547XA/en unknown
- 2015-11-09 RS RS20181321A patent/RS57946B1/sr unknown
- 2015-11-09 EA EA201790818A patent/EA032339B1/ru not_active IP Right Cessation
- 2015-11-09 KR KR1020177012442A patent/KR20170081184A/ko unknown
- 2015-11-09 UA UAA201704639A patent/UA119576C2/uk unknown
- 2015-11-09 TR TR2018/16427T patent/TR201816427T4/tr unknown
- 2015-11-09 MX MX2017006049A patent/MX2017006049A/es unknown
- 2015-11-09 CN CN201580060803.9A patent/CN107074836B/zh not_active Expired - Fee Related
- 2015-11-09 MA MA40955A patent/MA40955B1/fr unknown
- 2015-11-09 TW TW104136839A patent/TWI690318B/zh not_active IP Right Cessation
- 2015-11-09 ES ES15805109.4T patent/ES2694860T3/es active Active
- 2015-11-09 PT PT15805109T patent/PT3218365T/pt unknown
- 2015-11-09 BR BR112017009583A patent/BR112017009583A2/pt not_active Application Discontinuation
- 2015-11-09 EP EP15805109.4A patent/EP3218365B1/en active Active
- 2015-11-09 TN TN2017000144A patent/TN2017000144A1/en unknown
- 2015-11-09 PL PL15805109T patent/PL3218365T3/pl unknown
- 2015-11-09 DK DK15805109.4T patent/DK3218365T3/en active
- 2015-11-09 GE GEAP201514485A patent/GEP20196949B/en unknown
- 2015-11-09 EP EP18198764.5A patent/EP3461483A1/en not_active Withdrawn
- 2015-11-09 WO PCT/EP2015/076015 patent/WO2016075063A1/en active Application Filing
- 2015-11-09 ME MEP-2018-267A patent/ME03723B/me unknown
- 2015-11-09 CA CA2965563A patent/CA2965563A1/en not_active Abandoned
- 2015-11-09 RU RU2017116196A patent/RU2017116196A/ru not_active Application Discontinuation
- 2015-11-09 US US15/524,546 patent/US10045974B2/en not_active Expired - Fee Related
- 2015-11-09 SI SI201530464T patent/SI3218365T1/sl unknown
- 2015-11-09 PE PE2017000825A patent/PE20170946A1/es unknown
- 2015-11-09 CR CR20170186A patent/CR20170186A/es unknown
- 2015-11-09 JP JP2017525010A patent/JP6629320B2/ja not_active Expired - Fee Related
- 2015-11-09 LT LTEP15805109.4T patent/LT3218365T/lt unknown
- 2015-11-09 HU HUE15805109A patent/HUE040304T2/hu unknown
- 2015-11-09 AU AU2015345258A patent/AU2015345258B2/en not_active Expired - Fee Related
-
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/PH12017500841A1/en unknown
- 2017-05-09 EC ECIEPI201728459A patent/ECSP17028459A/es unknown
- 2017-05-09 SV SV2017005435A patent/SV2017005435A/es unknown
- 2017-05-09 NI NI201700055A patent/NI201700055A/es unknown
- 2017-05-09 DO DO2017000117A patent/DOP2017000117A/es unknown
- 2017-05-10 GT GT201700099A patent/GT201700099A/es unknown
-
2018
- 2018-08-09 US US16/059,715 patent/US10603310B2/en active Active
- 2018-10-17 HR HRP20181698TT patent/HRP20181698T1/hr unknown
- 2018-11-13 CY CY20181101200T patent/CY1120846T1/el unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20170946A1 (es) | 2-amino-6-(difluorometil)- 5,5-difluoro-6-fenil-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 | |
| PE20170947A1 (es) | 2-amino-3,5-difluoro-6-metil-6-fenil-3,4,5,6-tetrahidropiridinas en calidad de inhibidores de bace1 | |
| CL2020001576A1 (es) | Componentes heterocíclicos bicíclicos sustituidos como inhibidores de prmt5. | |
| GEP20207105B (en) | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2yl carbamate derivatives as magl inhibitors | |
| EA201691302A1 (ru) | Новые гетероциклические соединения | |
| PH12018502102A1 (en) | Pyrrolotriazine compounds as tam inhibitors | |
| PH12016502382A1 (en) | Substituted indazole compounds as irak4 inhibitors | |
| MX2023001876A (es) | Derivados de rapamicina. | |
| EA201891494A1 (ru) | Гетероциклические соединения в качестве иммуномодуляторов | |
| EA201890086A1 (ru) | 1,4-замещенные производные пиперидина | |
| ECSP16072941A (es) | 2-amino-3,5,5-trifluoro-3,4,5,6-tetrahidropiridinas como inhibidores de bace1 para el tratamiento de la enfermedad de alzheimer | |
| EA201691428A1 (ru) | Бициклические гетероциклические производные в качестве ингибиторов irak4 | |
| MX2016016516A (es) | Inhibidores de fosfatidilinositol 3-cinasa. | |
| EA201890152A1 (ru) | Производные 2,3-дигидро-4h-1,3-бензоксазин-4-онов в качестве модуляторов холинергического мускаринового m1 рецептора | |
| MX2016016530A (es) | Inhibidores de fosfatidilinositol 3-quinasa. | |
| UY34480A (es) | Compuestos de 2-(fenilo sustituido)-ciclopentan-1,3-diona y derivados de los mismos, composiciones y métodos para controlar malezas. | |
| EA201691997A1 (ru) | Производные 2,4-тиазолинидона в лечении расстройств центральной нервной системы | |
| EA201791259A1 (ru) | Производные пиперидина в качестве ингибиторов hdac1/2 | |
| EA201791030A1 (ru) | 2-амино-5,5-дифтор-6-(фторметил)-6-фенил-3,4,5,6-тетрагидпропиридины в качестве ингибиторов bace1 | |
| UY36263A (es) | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso | |
| EA201791021A1 (ru) | 1-[2-(АМИНОМЕТИЛ)БЕНЗИЛ]-2-ТИОКСО-1,2,3,5-ТЕТРАГИДРО-4H-ПИРРОЛО[3,2-d]ПИРИМИДИН-4-ОНЫ КАК ИНГИБИТОРЫ МИЕЛОПЕРОКСИДАЗЫ | |
| MX2019013979A (es) | Metodos para la preparacion de compuestos heterociclicos de 1,3-benzodioxol. | |
| EA201790315A1 (ru) | Модуляторы x-рецепторов печени | |
| EA201892188A1 (ru) | Соединения пирролотриазина в качестве ингибиторов tam | |
| EA201790231A1 (ru) | Профилактическое или терапевтическое средство для лечения болезней заднего сегмента глаза |