MX2020011382A - Derivados de tetrahidropiranoxazina que tienen actividad inhibidora de beta-secretasa 1 (bace1) selectiva. - Google Patents
Derivados de tetrahidropiranoxazina que tienen actividad inhibidora de beta-secretasa 1 (bace1) selectiva.Info
- Publication number
- MX2020011382A MX2020011382A MX2020011382A MX2020011382A MX2020011382A MX 2020011382 A MX2020011382 A MX 2020011382A MX 2020011382 A MX2020011382 A MX 2020011382A MX 2020011382 A MX2020011382 A MX 2020011382A MX 2020011382 A MX2020011382 A MX 2020011382A
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- halogen
- tetrahydropyranooxazine
- derivatives
- inhibitory activity
- Prior art date
Links
Classifications
-
- 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
-
- 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
- A61K31/535—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines
- A61K31/5365—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 oxygen as the ring hetero atoms, e.g. 1,2-oxazines ortho- or peri-condensed with heterocyclic ring systems
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0019—Injectable compositions; Intramuscular, intravenous, arterial, subcutaneous administration; Compositions to be administered through the skin in an invasive manner
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/0012—Galenical forms characterised by the site of application
- A61K9/0053—Mouth and digestive tract, i.e. intraoral and peroral administration
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2013—Organic compounds, e.g. phospholipids, fats
- A61K9/2018—Sugars, or sugar alcohols, e.g. lactose, mannitol; Derivatives thereof, e.g. polysorbates
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61K—PREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/48—Preparations in capsules, e.g. of gelatin, of chocolate
- A61K9/4841—Filling excipients; Inactive ingredients
- A61K9/4858—Organic compounds
-
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Engineering & Computer Science (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Molecular Biology (AREA)
- Biophysics (AREA)
- Nutrition Science (AREA)
- Physiology (AREA)
- Dermatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención proporciona un compuesto que tiene el efecto de inhibir la producción del ß amiloide, especialmente un efecto de inhibición de BACE1, y que es útil como agente terapéutico o profiláctico para enfermedades inducidas por la producción, secreción y/o deposición de proteínas ß amiloides. Un compuesto de la fórmula (I) en la que R3 es cada uno independientemente alquilo opcionalmente sustituido con halógeno, ciano, alquiloxi, haloalquiloxi o carbociclilo no aromático, o similares; t es un número entero de 0 a 3; R5 es un átomo de hidrógeno o halógeno; R6 se selecciona del grupo que consiste de un átomo de hidrógeno, halógeno y alquilo sustituido o no sustituido, el anillo B es una pirazina sustituida o no sustituida o similar, o una sal farmacéuticamente aceptable del mismo.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
JP2018086206 | 2018-04-27 | ||
PCT/JP2019/017619 WO2019208693A1 (en) | 2018-04-27 | 2019-04-25 | Tetrahydropyranooxazine derivatives having selective bace1 inhibitory activity |
Publications (1)
Publication Number | Publication Date |
---|---|
MX2020011382A true MX2020011382A (es) | 2020-11-24 |
Family
ID=66589826
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
MX2020011382A MX2020011382A (es) | 2018-04-27 | 2019-04-25 | Derivados de tetrahidropiranoxazina que tienen actividad inhibidora de beta-secretasa 1 (bace1) selectiva. |
Country Status (11)
Country | Link |
---|---|
US (1) | US11629154B2 (es) |
EP (1) | EP3784674B1 (es) |
JP (1) | JP7353708B2 (es) |
KR (1) | KR20210003872A (es) |
CN (1) | CN112313238A (es) |
AU (1) | AU2019258575A1 (es) |
BR (1) | BR112020021728A2 (es) |
CA (1) | CA3098430A1 (es) |
MX (1) | MX2020011382A (es) |
TW (1) | TW202014191A (es) |
WO (1) | WO2019208693A1 (es) |
Family Cites Families (69)
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BRPI0617852A2 (pt) | 2005-10-25 | 2011-08-09 | Shionogi & Co | compostos derivados de aminodi-hidrotiazina assim como composições contendo os mesmos |
AU2008245082B8 (en) | 2007-04-24 | 2012-09-13 | Shionogi & Co., Ltd. | Aminodihydrothiazine derivatives substituted with a cyclic group |
WO2008133273A1 (ja) | 2007-04-24 | 2008-11-06 | Shionogi & Co., Ltd. | アルツハイマー症治療用医薬組成物 |
TWI431004B (zh) | 2008-05-02 | 2014-03-21 | Lilly Co Eli | Bace抑制劑 |
WO2009151098A1 (ja) | 2008-06-13 | 2009-12-17 | 塩野義製薬株式会社 | βセクレターゼ阻害作用を有する含硫黄複素環誘導体 |
EP2360155A4 (en) | 2008-10-22 | 2012-06-20 | Shionogi & Co | 2-AMINOPYRIDIN-4-ON AND 2-AMINOPYRIDINE DERIVATIVE WITH BACE1-HEMDERING EFFECT |
US20120015961A1 (en) | 2009-03-31 | 2012-01-19 | Shionogi & Co., Ltd. | Isothiourea derivatives or isourea derivatives having bace1 inhibitory activity |
UA108363C2 (uk) | 2009-10-08 | 2015-04-27 | Похідні імінотіадіазиндіоксиду як інгібітори bace, композиція на їх основі і їх застосування | |
US20120238557A1 (en) | 2009-11-13 | 2012-09-20 | Shionogi & Co., Ltd. | Aminothiazine or aminooxazine derivative having amino linker |
JP5554346B2 (ja) | 2009-12-09 | 2014-07-23 | 塩野義製薬株式会社 | 含硫黄複素環誘導体を含有するアルツハイマー症の治療用または予防用医薬組成物 |
EP2514747A4 (en) | 2009-12-09 | 2013-05-08 | Shionogi & Co | SUBSTITUTED AMINOTHIAZINE DERIVATIVE |
US7964594B1 (en) | 2009-12-10 | 2011-06-21 | Hoffmann-La Roche Inc. | Amino oxazine derivatives |
JPWO2011071109A1 (ja) | 2009-12-11 | 2013-04-22 | 塩野義製薬株式会社 | アミノ基を有する縮合ヘテロ環化合物 |
RU2012129168A (ru) | 2009-12-11 | 2014-01-20 | Сионоги Энд Ко. Лтд. | Производные оксазина |
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 |
JPWO2011077726A1 (ja) | 2009-12-24 | 2013-05-02 | 塩野義製薬株式会社 | 4−アミノ−1,3−チアジンまたはオキサジン誘導体 |
US9910049B2 (en) | 2014-09-11 | 2018-03-06 | Amprion, Inc. | Detection of misfolded amyloid beta protein |
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US9018219B2 (en) | 2010-10-29 | 2015-04-28 | Shionogi & Co., Ltd. | Fused aminodihydropyrimidine derivative |
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JP2014514302A (ja) | 2011-04-13 | 2014-06-19 | メルク・シャープ・アンド・ドーム・コーポレーション | Bace阻害薬としての5−置換されたイミノチアジン類およびそれのモノおよびジオキシド、組成物およびそれらの使用 |
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US20160213645A1 (en) | 2015-04-04 | 2016-07-28 | James Wallace | Combination of levetiracetam and a beta-secretase (bace) inhibitor |
TW201726651A (zh) | 2015-09-23 | 2017-08-01 | 健生藥品公司 | 2,3,4,5-四氫吡啶-6-胺衍生物 |
WO2017061534A1 (en) | 2015-10-08 | 2017-04-13 | Shionogi & Co., Ltd. | Dihydrothiazine derivatives |
JP2017071603A (ja) | 2015-10-09 | 2017-04-13 | 塩野義製薬株式会社 | ジヒドロチアジンまたはジヒドロオキサジン誘導体を含有する医薬組成物 |
EP3414322A4 (en) | 2015-12-23 | 2020-03-04 | Memorial Sloan-Kettering Cancer Center | CELL THERAPY AND DRUG DISCOVERY BASED ON CELL LINES DERIVED FROM HUMAN ENTERAL NEURAL CREST DERIVED FROM PLURIPOTENT STEM CELLS |
CN108699051B (zh) | 2016-03-01 | 2021-12-24 | 豪夫迈·罗氏有限公司 | Bace1抑制剂 |
JP7177773B2 (ja) | 2016-12-15 | 2022-11-24 | アムジエン・インコーポレーテツド | β-セクレターゼ阻害剤としてのオキサジン誘導体および使用方法 |
JP2022511167A (ja) | 2018-04-23 | 2022-01-31 | 塩野義製薬株式会社 | 選択的bace1阻害活性を有する二環式複素環誘導体 |
JP2022532810A (ja) | 2018-07-06 | 2022-07-20 | 塩野義製薬株式会社 | 選択的bace1阻害活性を有する縮合複素環誘導体 |
JP2021075519A (ja) | 2019-10-24 | 2021-05-20 | 塩野義製薬株式会社 | 選択的bace1阻害活性を有するテトラヒドロピラノオキサジン誘導体を含有する医薬組成物 |
-
2019
- 2019-04-25 KR KR1020207033925A patent/KR20210003872A/ko unknown
- 2019-04-25 TW TW108114505A patent/TW202014191A/zh unknown
- 2019-04-25 EP EP19724946.9A patent/EP3784674B1/en active Active
- 2019-04-25 MX MX2020011382A patent/MX2020011382A/es unknown
- 2019-04-25 WO PCT/JP2019/017619 patent/WO2019208693A1/en unknown
- 2019-04-25 BR BR112020021728-0A patent/BR112020021728A2/pt not_active Application Discontinuation
- 2019-04-25 AU AU2019258575A patent/AU2019258575A1/en not_active Abandoned
- 2019-04-25 JP JP2020557347A patent/JP7353708B2/ja active Active
- 2019-04-25 US US17/050,663 patent/US11629154B2/en active Active
- 2019-04-25 CA CA3098430A patent/CA3098430A1/en active Pending
- 2019-04-25 CN CN201980042653.7A patent/CN112313238A/zh active Pending
Also Published As
Publication number | Publication date |
---|---|
EP3784674A1 (en) | 2021-03-03 |
EP3784674B1 (en) | 2023-02-22 |
JP2021522194A (ja) | 2021-08-30 |
US11629154B2 (en) | 2023-04-18 |
TW202014191A (zh) | 2020-04-16 |
AU2019258575A1 (en) | 2020-10-29 |
JP7353708B2 (ja) | 2023-10-02 |
WO2019208693A1 (en) | 2019-10-31 |
CA3098430A1 (en) | 2019-10-31 |
US20210238194A1 (en) | 2021-08-05 |
CN112313238A (zh) | 2021-02-02 |
BR112020021728A2 (pt) | 2021-01-26 |
KR20210003872A (ko) | 2021-01-12 |
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