CR20170426A - Inhibidores de bace 1 - Google Patents
Inhibidores de bace 1Info
- Publication number
- CR20170426A CR20170426A CR20170426A CR20170426A CR20170426A CR 20170426 A CR20170426 A CR 20170426A CR 20170426 A CR20170426 A CR 20170426A CR 20170426 A CR20170426 A CR 20170426A CR 20170426 A CR20170426 A CR 20170426A
- Authority
- CR
- Costa Rica
- Prior art keywords
- bace inhibitors
- present
- bace1
- alzheimer
- therapeutic
- Prior art date
Links
- 102100021257 Beta-secretase 1 Human genes 0.000 title abstract 2
- 101000894895 Homo sapiens Beta-secretase 1 Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 239000013543 active substance Substances 0.000 abstract 1
- 230000002401 inhibitory effect Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 230000001225 therapeutic effect Effects 0.000 abstract 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
- A61K31/54—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with at least one nitrogen and one sulfur as the ring hetero atoms, e.g. sulthiame
- A61K31/541—Non-condensed thiazines 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
-
- 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
- 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
- C07D417/14—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 three or more hetero rings
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)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
Abstract
La presente invención proporciona un compuesto de fórmula I, que presenta una actividad inhibidora de BACE1, su preparación, composiciones farmacéuticas que los contienen y su utilización como sustancias terapéuticamente activas. Los compuestos activos de la presente invención resultan útiles en el tratamiento terapéutico y/o profiláctico de, por ejemplo, la enfermedad de Alzheimer.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP15160101 | 2015-03-20 | ||
| PCT/EP2016/055649 WO2016150785A1 (en) | 2015-03-20 | 2016-03-16 | Bace1 inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20170426A true CR20170426A (es) | 2017-10-23 |
Family
ID=52780400
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20170426A CR20170426A (es) | 2015-03-20 | 2016-03-16 | Inhibidores de bace 1 |
Country Status (18)
| Country | Link |
|---|---|
| US (4) | US10047081B2 (es) |
| EP (1) | EP3271355B1 (es) |
| JP (1) | JP6674960B2 (es) |
| KR (1) | KR20170129745A (es) |
| CN (1) | CN107406440B (es) |
| AU (1) | AU2016236402B2 (es) |
| BR (1) | BR112017015474A2 (es) |
| CA (1) | CA2979113A1 (es) |
| CL (1) | CL2017002229A1 (es) |
| CO (1) | CO2017007691A2 (es) |
| CR (1) | CR20170426A (es) |
| IL (1) | IL253322A0 (es) |
| MX (1) | MX2017012188A (es) |
| PE (1) | PE20171349A1 (es) |
| PH (1) | PH12017501668A1 (es) |
| RU (1) | RU2712272C2 (es) |
| SG (1) | SG11201707050VA (es) |
| WO (1) | WO2016150785A1 (es) |
Families Citing this family (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| CA2979113A1 (en) | 2015-03-20 | 2016-09-29 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
| CN110467611B (zh) * | 2018-05-11 | 2022-09-27 | 广东东阳光药业有限公司 | 亚氨基噻二嗪二氧化物衍生物及其用途 |
| PY1943991A (es) | 2018-06-06 | 2020-03-09 | Syngenta Crop Protection Ag | Derivados heterocíclicos con sustituyentes que contienen azufre activos como plaguicidas |
Family Cites Families (35)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| DE19962924A1 (de) | 1999-12-24 | 2001-07-05 | Bayer Ag | Substituierte Oxazolidinone und ihre Verwendung |
| CN101952260B (zh) | 2008-02-18 | 2013-02-13 | 弗·哈夫曼-拉罗切有限公司 | 4,5-二氢-*唑-2-基胺衍生物 |
| US8461160B2 (en) | 2009-05-08 | 2013-06-11 | Hoffmann-La Roche, Inc. | Dihydropyrimidinones |
| US8188079B2 (en) | 2009-08-19 | 2012-05-29 | Hoffman-La Roche Inc. | 3-amino-5-phenyl-5,6-dihydro-2H-[1,4]oxazines |
| US20110065695A1 (en) | 2009-09-11 | 2011-03-17 | Jeremy Beauchamp | Use of aminodihydrothiazines for the treatment or prevention of diabetes |
| US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
| UA103272C2 (uk) | 2009-12-11 | 2013-09-25 | Ф. Хоффманн-Ля Рош Аг | 2-аміно-5,5-дифтор-5,6-дигідро-4h-оксазини як інгібітори bace1 і/або bace2 |
| US8673894B2 (en) | 2010-05-07 | 2014-03-18 | Hoffmann-La Roche Inc. | 2,5,6,7-tetrahydro-[1,4]oxazepin-3-ylamine or 2,3,6,7-tetrahydro-[1,4]oxazepin-5-ylamine compounds |
| US8815881B2 (en) | 2010-08-09 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4,5,6-tetrahydro-pyrimidin-2-ylamine compounds |
| US20120053200A1 (en) | 2010-09-01 | 2012-03-01 | Harald Mauser | Bace 2 inhibitors |
| US9242943B2 (en) | 2011-01-18 | 2016-01-26 | Siena Biotech S.P.A. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US8399459B2 (en) | 2011-02-02 | 2013-03-19 | Hoffmann-La Roche Inc. | 1,4 oxazines as BACE1 and/or BACE2 inhibitors |
| US8404680B2 (en) | 2011-02-08 | 2013-03-26 | Hoffmann-La Roche Inc. | N-[3-(5-amino-3,3a,7,7a-tetrahydro-1H-2,4-dioxa-6-aza-inden-7-yl)-phenyl]-amides as BACE1 and/or BACE2 inhibitors |
| US8815841B2 (en) | 2011-02-18 | 2014-08-26 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| US9067924B2 (en) | 2011-03-04 | 2015-06-30 | Hoffmann-La Roche Inc. | 1,4 thiazepines/sulfones as BACE1 and/or BACE2 inhibitors |
| US8748418B2 (en) | 2011-03-18 | 2014-06-10 | Hoffmann-La Roche Inc. | 1,4-oxazepines as BACE1 and/or BACE2 inhibitors |
| US8877744B2 (en) | 2011-04-04 | 2014-11-04 | Hoffmann-La Roche Inc. | 1,4-Oxazepines as BACE1 and/or BACE2 inhibitors |
| US8754075B2 (en) | 2011-04-11 | 2014-06-17 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE1 and/or BACE2 inhibitors |
| BR112013026341A2 (pt) | 2011-04-13 | 2019-09-24 | Merck Sharp & Dohe Corp. | composto, composição farmacêutica, e, método para tratar, prevenir e/ou atrasar o início de uma doença ou patologia |
| US8785436B2 (en) | 2011-05-16 | 2014-07-22 | Hoffmann-La Roche Inc. | 1,3-oxazines as BACE 1 and/or BACE2 inhibitors |
| US9079919B2 (en) | 2011-05-27 | 2015-07-14 | Hoffmann-La Roche Inc. | Spiro-[1,3]-oxazines and spiro-[1,4]-oxazepines as BACE1 and/or BACE2 inhibitors |
| EP2718287A1 (en) | 2011-06-07 | 2014-04-16 | F.Hoffmann-La Roche Ag | [1,3]oxazines |
| AU2012266544A1 (en) | 2011-06-07 | 2013-11-21 | F. Hoffmann-La Roche Ag | Halogen-alkyl-1,3 oxazines as BACE1 and/or BACE2 inhibitors |
| US8927535B2 (en) | 2011-07-06 | 2015-01-06 | Hoffman-La Roche Inc. | Cyclopropyl-fused-1,3-thiazepines as BACE1 and/or BACE2 inhibitors |
| RU2014111055A (ru) * | 2011-08-22 | 2015-09-27 | Мерк Шарп И Доум Корп. | 2-спирозамещенные иминотиазины и их моно- и диоксиды в качестве ингибиторов bace, композиции и их применение |
| US20130073953A1 (en) | 2011-09-21 | 2013-03-21 | Timothy Onyenobi | News headline screenshot viewing system |
| KR101669349B1 (ko) | 2012-01-26 | 2016-10-25 | 에프. 호프만-라 로슈 아게 | 플루오로메틸-5,6-다이하이드로-4h-[1,3]옥사진 |
| JP6251249B2 (ja) * | 2012-05-24 | 2017-12-20 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害薬としての5−アミノ[1,4]チアジン類 |
| JP6251257B2 (ja) | 2012-06-26 | 2017-12-20 | エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft | Bace1阻害薬としてのジフルオロ−ヘキサヒドロ−シクロペンタオキサジニル類及びジフルオロ−ヘキサヒドロ−ベンゾオキサジニル類 |
| EP2908825B1 (en) * | 2012-10-17 | 2018-04-18 | Merck Sharp & Dohme Corp. | Tricyclic substituted thiadiazine dioxide compounds as bace inhibitors, compositions, and their use |
| CN104968660A (zh) | 2013-01-22 | 2015-10-07 | 霍夫曼-拉罗奇有限公司 | 作为bace1抑制剂的氟-[1,3]噁嗪类化合物 |
| US9422255B2 (en) * | 2013-03-15 | 2016-08-23 | Merck Sharp & Dohme Corp. | S-imino-S-oxo-iminothiazine compounds as BACE inhibitors, compositions, and their use |
| WO2014150340A1 (en) | 2013-03-15 | 2014-09-25 | Merck Sharp & Dohme Corp. | S-imino-s-oxo iminothiadiazine compounds as bace inhibitors, compositions, and their use |
| US9453034B2 (en) | 2013-03-15 | 2016-09-27 | Merck Sharp & Dohme Corp. | C2-azaspiro iminothiazine dioxides as BACE inhibitors, compositions, and their use |
| CA2979113A1 (en) | 2015-03-20 | 2016-09-29 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
-
2016
- 2016-03-16 CA CA2979113A patent/CA2979113A1/en not_active Abandoned
- 2016-03-16 SG SG11201707050VA patent/SG11201707050VA/en unknown
- 2016-03-16 BR BR112017015474-9A patent/BR112017015474A2/pt not_active Application Discontinuation
- 2016-03-16 MX MX2017012188A patent/MX2017012188A/es unknown
- 2016-03-16 RU RU2017134884A patent/RU2712272C2/ru not_active IP Right Cessation
- 2016-03-16 CN CN201680016799.0A patent/CN107406440B/zh not_active Expired - Fee Related
- 2016-03-16 EP EP16710170.8A patent/EP3271355B1/en not_active Not-in-force
- 2016-03-16 AU AU2016236402A patent/AU2016236402B2/en not_active Ceased
- 2016-03-16 KR KR1020177026060A patent/KR20170129745A/ko not_active Withdrawn
- 2016-03-16 JP JP2017546991A patent/JP6674960B2/ja not_active Expired - Fee Related
- 2016-03-16 PE PE2017001451A patent/PE20171349A1/es unknown
- 2016-03-16 US US15/558,273 patent/US10047081B2/en active Active
- 2016-03-16 WO PCT/EP2016/055649 patent/WO2016150785A1/en not_active Ceased
- 2016-03-16 CR CR20170426A patent/CR20170426A/es unknown
-
2017
- 2017-07-05 IL IL253322A patent/IL253322A0/en unknown
- 2017-07-28 CO CONC2017/0007691A patent/CO2017007691A2/es unknown
- 2017-09-04 CL CL2017002229A patent/CL2017002229A1/es unknown
- 2017-09-13 PH PH12017501668A patent/PH12017501668A1/en unknown
-
2018
- 2018-07-12 US US16/033,785 patent/US10399969B2/en not_active Expired - Fee Related
-
2019
- 2019-07-16 US US16/512,905 patent/US10723729B2/en not_active Expired - Fee Related
-
2020
- 2020-06-17 US US16/903,616 patent/US11034687B2/en not_active Expired - Fee Related
Also Published As
| Publication number | Publication date |
|---|---|
| US20200308166A1 (en) | 2020-10-01 |
| JP2018507879A (ja) | 2018-03-22 |
| AU2016236402A1 (en) | 2017-07-27 |
| JP6674960B2 (ja) | 2020-04-01 |
| PE20171349A1 (es) | 2017-09-13 |
| WO2016150785A1 (en) | 2016-09-29 |
| US10723729B2 (en) | 2020-07-28 |
| US20190337936A1 (en) | 2019-11-07 |
| AU2016236402B2 (en) | 2019-08-01 |
| EP3271355A1 (en) | 2018-01-24 |
| US20180057485A1 (en) | 2018-03-01 |
| MX2017012188A (es) | 2017-12-15 |
| SG11201707050VA (en) | 2017-10-30 |
| US11034687B2 (en) | 2021-06-15 |
| CL2017002229A1 (es) | 2018-04-13 |
| BR112017015474A2 (pt) | 2018-01-30 |
| KR20170129745A (ko) | 2017-11-27 |
| EP3271355B1 (en) | 2020-07-29 |
| CO2017007691A2 (es) | 2017-10-20 |
| RU2712272C2 (ru) | 2020-01-28 |
| CN107406440B (zh) | 2021-05-07 |
| US10047081B2 (en) | 2018-08-14 |
| PH12017501668A1 (en) | 2018-03-19 |
| HK1244790A1 (zh) | 2018-08-17 |
| IL253322A0 (en) | 2017-09-28 |
| RU2017134884A (ru) | 2019-04-22 |
| US20180319787A1 (en) | 2018-11-08 |
| RU2017134884A3 (es) | 2019-07-17 |
| CA2979113A1 (en) | 2016-09-29 |
| CN107406440A (zh) | 2017-11-28 |
| US10399969B2 (en) | 2019-09-03 |
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