MX2015011313A - Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. - Google Patents
Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso.Info
- Publication number
- MX2015011313A MX2015011313A MX2015011313A MX2015011313A MX2015011313A MX 2015011313 A MX2015011313 A MX 2015011313A MX 2015011313 A MX2015011313 A MX 2015011313A MX 2015011313 A MX2015011313 A MX 2015011313A MX 2015011313 A MX2015011313 A MX 2015011313A
- Authority
- MX
- Mexico
- Prior art keywords
- compounds
- beta
- bace
- methods
- oxazin
- Prior art date
Links
- 238000000034 method Methods 0.000 title abstract 3
- VPVZSRIIAONGMU-UHFFFAOYSA-N 5,6-dihydro-4h-1,3-oxazin-2-amine Chemical class N=C1NCCCO1 VPVZSRIIAONGMU-UHFFFAOYSA-N 0.000 title 1
- 239000002439 beta secretase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 6
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 2
- 208000035475 disorder Diseases 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 230000007351 Aβ plaque formation Effects 0.000 abstract 1
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 230000006933 amyloid-beta aggregation Effects 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 210000003169 central nervous system Anatomy 0.000 abstract 1
- 230000007278 cognition impairment Effects 0.000 abstract 1
- 208000010877 cognitive disease Diseases 0.000 abstract 1
- 230000000694 effects Effects 0.000 abstract 1
- 239000000543 intermediate Substances 0.000 abstract 1
- 230000001404 mediated effect Effects 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 201000000980 schizophrenia Diseases 0.000 abstract 1
Classifications
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- 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
- C07D413/14—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing three or more hetero rings
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- 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
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P7/00—Drugs for disorders of the blood or the extracellular fluid
- A61P7/04—Antihaemorrhagics; Procoagulants; Haemostatic agents; Antifibrinolytic agents
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P9/00—Drugs for disorders of the cardiovascular system
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/04—1,3-Oxazines; Hydrogenated 1,3-oxazines
- C07D265/06—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings
- C07D265/08—1,3-Oxazines; Hydrogenated 1,3-oxazines not condensed with other rings having one double bond between ring members or between a ring member and a non-ring member
-
- 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
- C07D413/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- C07D413/10—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 carbon chain containing aromatic rings
-
- 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
- C07D471/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00
- C07D471/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, at least one ring being a six-membered ring with one nitrogen atom, not provided for by groups C07D451/00 - C07D463/00 in which the condensed system contains two hetero rings
- C07D471/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D498/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms in which the condensed system contains two hetero rings
- C07D498/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
- C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
- C07D513/04—Ortho-condensed systems
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07F—ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
- C07F7/00—Compounds containing elements of Groups 4 or 14 of the Periodic Table
- C07F7/02—Silicon compounds
- C07F7/08—Compounds having one or more C—Si linkages
- C07F7/0803—Compounds with Si-C or Si-Si linkages
- C07F7/081—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te
- C07F7/0812—Compounds with Si-C or Si-Si linkages comprising at least one atom selected from the elements N, O, halogen, S, Se or Te comprising a heterocyclic ring
Landscapes
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Neurology (AREA)
- Heart & Thoracic Surgery (AREA)
- Diabetes (AREA)
- Hospice & Palliative Care (AREA)
- Cardiology (AREA)
- Hematology (AREA)
- Psychiatry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
Abstract
La presente invención da a conocer una nueva clase de compuestos útiles para la modulación de la actividad de la enzima beta-secretasa (BACE). Los compuestos poseen una Fórmula general I: (ver Fórmula) donde las variables A4, A5, A6, A8, cada uno de R1 y R2, R3 y R7 de la Fórmula I, en forma independiente, se definen en la presente descripción. La invención también da a conocer composiciones farmacéuticas que comprenden los compuestos, y los correspondientes usos de los compuestos y composiciones para el tratamiento de trastornos y/o condiciones asociadas con la formación y deposición de placa A-beta que resulta de la actividad biológica de BACE. Dichos trastornos mediados por BACE incluyen, por ejemplo, la enfermedad de Alzheimer, déficits cognitivos, deterioro cognitivo, esquizofrenia y otras condiciones del sistema nervioso central. La invención asimismo da a conocer compuestos de Fórmulas II y III, y sub-Fórmulas de los mismos, y compuestos intermediarios, así como procesos y métodos útiles para la preparación de los compuestos de Fórmulas I-III.
Applications Claiming Priority (4)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
US201361771615P | 2013-03-01 | 2013-03-01 | |
US201361826431P | 2013-05-22 | 2013-05-22 | |
US201461928898P | 2014-01-17 | 2014-01-17 | |
PCT/US2014/019100 WO2014134341A1 (en) | 2013-03-01 | 2014-02-27 | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (2)
Publication Number | Publication Date |
---|---|
MX2015011313A true MX2015011313A (es) | 2015-12-03 |
MX366855B MX366855B (es) | 2019-07-26 |
Family
ID=50349866
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2015011313A MX366855B (es) | 2013-03-01 | 2014-02-27 | Compuestos perfluorados de 5,6-dihidro-4h-1,3-oxazin-2-amina como inhibidores de beta-secretasa y metodos de uso. |
Country Status (9)
Country | Link |
---|---|
US (1) | US9296734B2 (es) |
EP (1) | EP2961749B1 (es) |
JP (1) | JP6389830B2 (es) |
AU (2) | AU2014223334C1 (es) |
CA (1) | CA2902212C (es) |
MX (1) | MX366855B (es) |
TW (1) | TW201446758A (es) |
UY (1) | UY35361A (es) |
WO (1) | WO2014134341A1 (es) |
Families Citing this family (26)
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NZ589590A (en) | 2008-06-13 | 2012-05-25 | Shionogi & Co | Sulfur-containing heterocyclic derivative having beta-secretase-inhibiting activity |
MX2012006491A (es) | 2009-12-11 | 2012-07-03 | Shionogi & Co | Derivados de oxazina. |
WO2014065434A1 (en) | 2012-10-24 | 2014-05-01 | Shionogi & Co., Ltd. | Dihydrooxazine or oxazepine derivatives having bace1 inhibitory 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 |
EP2964644B1 (en) | 2013-03-08 | 2018-12-26 | Amgen, Inc. | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
CA2900433C (en) | 2013-04-11 | 2021-06-22 | F. Hoffmann-La Roche Ag | Bace1 inhibitors |
KR20160115936A (ko) | 2014-02-19 | 2016-10-06 | 하. 룬드벡 아크티에셀스카브 | 알츠하이머병의 치료를 위한 bace1 저해제로서의 2-아미노-3,5,5-트리플루오로-3,4,5,6-테트라하이드로피리딘 |
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 |
AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
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 |
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US10889581B2 (en) * | 2016-12-15 | 2021-01-12 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
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2014
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JP6389830B2 (ja) | 2018-09-12 |
UY35361A (es) | 2014-09-30 |
US20140249104A1 (en) | 2014-09-04 |
TW201446758A (zh) | 2014-12-16 |
MX366855B (es) | 2019-07-26 |
JP2016511258A (ja) | 2016-04-14 |
AU2014223334C1 (en) | 2018-10-18 |
CA2902212C (en) | 2020-10-13 |
AU2018204589A1 (en) | 2018-07-12 |
WO2014134341A1 (en) | 2014-09-04 |
CA2902212A1 (en) | 2014-09-04 |
EP2961749B1 (en) | 2019-10-09 |
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