MX2019007104A - Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso. - Google Patents
Derivados de dioxido de 1,4-tiazina y dioxido de 1,2,4-tiadiazina como inhibidores de beta-secretasa y metodos de uso.Info
- Publication number
- MX2019007104A MX2019007104A MX2019007104A MX2019007104A MX2019007104A MX 2019007104 A MX2019007104 A MX 2019007104A MX 2019007104 A MX2019007104 A MX 2019007104A MX 2019007104 A MX2019007104 A MX 2019007104A MX 2019007104 A MX2019007104 A MX 2019007104A
- Authority
- MX
- Mexico
- Prior art keywords
- dioxide
- beta
- compounds
- bace
- tiadiazine
- Prior art date
Links
- LCKXJCKRKBQVJZ-UHFFFAOYSA-N 2h-1,4-thiazine 1,1-dioxide Chemical class O=S1(=O)CC=NC=C1 LCKXJCKRKBQVJZ-UHFFFAOYSA-N 0.000 title 1
- 239000002439 beta secretase inhibitor Substances 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 4
- 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
- 208000028698 Cognitive impairment Diseases 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process 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
- 230000008021 deposition Effects 0.000 abstract 1
- 230000000694 effects Effects 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
Classifications
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- 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
- C07D513/08—Bridged systems
-
- 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
- C07D417/10—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 carbon chain containing aromatic 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
- 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
-
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/04—Ortho-condensed systems
- C07D491/056—Ortho-condensed systems with two or more oxygen atoms as ring hetero atoms in the oxygen-containing ring
-
- 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
- C07D498/08—Bridged 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
Landscapes
- Organic Chemistry (AREA)
- Chemical & Material Sciences (AREA)
- Health & Medical Sciences (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Medicinal Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Hospice & Palliative Care (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Psychiatry (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen- Or Sulfur-Containing Heterocyclic Ring Compounds With Rings Of Six Or More Members (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente divulgación proporciona una clase de compuestos útiles para la modulación de la actividad de la enzima beta-secretasa (BACE). Los compuestos tienen una Fórmula general I: (ver fórmula). En donde las variables A, X, R2, R2', R3, R4, R5, R6 Y R7 de Fórmula I se definen en el presente documento. La presente divulgación también proporciona composiciones farmacéuticas que comprenden los compuestos, y usos de los compuestos y composiciones para el tratamiento de trastornos y/o afecciones relacionadas con la formación y deposición de placas Aß, como resultado de la actividad biológica de BACE. Tales trastornos mediados por BACE incluyen, por ejemplo, enfermedad de Alzheimer, déficits cognitivos, deterioros cognitivos y otras afecciones del sistema nervioso central.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201662434715P | 2016-12-15 | 2016-12-15 | |
| PCT/US2017/066197 WO2018112094A1 (en) | 2016-12-15 | 2017-12-13 | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2019007104A true MX2019007104A (es) | 2019-11-05 |
| MX387729B MX387729B (es) | 2025-03-18 |
Family
ID=60888749
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2019007104A MX387729B (es) | 2016-12-15 | 2017-12-13 | Derivados de dióxido de 1,4-tiazina y dióxido 1,2,4-tiadiazina como inhibidores de beta-secretasa y métodos de uso. |
Country Status (8)
| Country | Link |
|---|---|
| US (1) | US11021493B2 (es) |
| EP (1) | EP3555086B1 (es) |
| JP (1) | JP7149271B2 (es) |
| AU (1) | AU2017376446B2 (es) |
| CA (1) | CA3047290A1 (es) |
| MA (1) | MA50007A (es) |
| MX (1) | MX387729B (es) |
| WO (1) | WO2018112094A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| MX386618B (es) | 2016-12-15 | 2025-03-19 | Amgen Inc | Derivados de tiazina condensados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso. |
| JP7149271B2 (ja) | 2016-12-15 | 2022-10-06 | 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1,4-チアジンジオキシドおよび1,2,4-チアジアジンジオキシド誘導体ならびに使用方法 |
| JP7148518B2 (ja) | 2016-12-15 | 2022-10-05 | 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二環式チアジンおよびオキサジン誘導体ならびに使用方法 |
| CN108997328B (zh) * | 2018-09-06 | 2021-06-08 | 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 |
| CN109180672A (zh) * | 2018-09-29 | 2019-01-11 | 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 |
| CN110078613B (zh) * | 2019-05-31 | 2022-04-22 | 杭州科耀医药科技有限公司 | 一种2-卤-5-碘苯甲酸的合成方法 |
| BR112022017563A2 (pt) | 2020-03-04 | 2022-10-18 | Basf Se | Uso de compostos, composição agroquímica e método para combater fungos fitopatogênicos nocivos |
| WO2022074631A1 (en) * | 2020-10-11 | 2022-04-14 | Dynarx Technology (India) Ltd | A process for preparing sglt2 inhibitor intermediate 2-chloro-5-iodobenzoic acid |
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| EP3555084B1 (en) | 2016-12-15 | 2022-03-16 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| JP7148518B2 (ja) | 2016-12-15 | 2022-10-05 | 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二環式チアジンおよびオキサジン誘導体ならびに使用方法 |
| US10947223B2 (en) | 2016-12-15 | 2021-03-16 | Amgen Inc. | Substituted oxazines as beta-secretase inhibitors |
| JP7149271B2 (ja) | 2016-12-15 | 2022-10-06 | 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1,4-チアジンジオキシドおよび1,2,4-チアジアジンジオキシド誘導体ならびに使用方法 |
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2017
- 2017-12-13 JP JP2019531721A patent/JP7149271B2/ja active Active
- 2017-12-13 WO PCT/US2017/066197 patent/WO2018112094A1/en not_active Ceased
- 2017-12-13 AU AU2017376446A patent/AU2017376446B2/en active Active
- 2017-12-13 CA CA3047290A patent/CA3047290A1/en active Pending
- 2017-12-13 EP EP17822989.4A patent/EP3555086B1/en active Active
- 2017-12-13 US US16/466,207 patent/US11021493B2/en active Active
- 2017-12-13 MA MA050007A patent/MA50007A/fr unknown
- 2017-12-13 MX MX2019007104A patent/MX387729B/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3047290A1 (en) | 2018-06-21 |
| AU2017376446B2 (en) | 2021-10-14 |
| EP3555086A1 (en) | 2019-10-23 |
| US20200231601A1 (en) | 2020-07-23 |
| JP7149271B2 (ja) | 2022-10-06 |
| JP2020503291A (ja) | 2020-01-30 |
| MX387729B (es) | 2025-03-18 |
| MA50007A (fr) | 2021-04-07 |
| US11021493B2 (en) | 2021-06-01 |
| AU2017376446A1 (en) | 2019-07-04 |
| WO2018112094A1 (en) | 2018-06-21 |
| EP3555086B1 (en) | 2021-09-01 |
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