UY36263A - Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso - Google Patents
Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y métodos de usoInfo
- Publication number
- UY36263A UY36263A UY0001036263A UY36263A UY36263A UY 36263 A UY36263 A UY 36263A UY 0001036263 A UY0001036263 A UY 0001036263A UY 36263 A UY36263 A UY 36263A UY 36263 A UY36263 A UY 36263A
- Authority
- UY
- Uruguay
- Prior art keywords
- beta
- compounds
- tiazin
- amina
- cyclopropyl
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 5
- XIPUIGPNIDKXJU-UHFFFAOYSA-N [CH]1CC1 Chemical class [CH]1CC1 XIPUIGPNIDKXJU-UHFFFAOYSA-N 0.000 title 1
- 239000002439 beta secretase inhibitor Substances 0.000 title 1
- 102000002659 Amyloid Precursor Protein Secretases Human genes 0.000 abstract 1
- 108010043324 Amyloid Precursor Protein Secretases Proteins 0.000 abstract 1
- 101800001718 Amyloid-beta protein Proteins 0.000 abstract 1
- 230000004071 biological effect Effects 0.000 abstract 1
- 230000015572 biosynthetic process Effects 0.000 abstract 1
- 230000008021 deposition Effects 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 230000000694 effects 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
- 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
-
- 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
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D279/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one sulfur atom as the only ring hetero atoms
- C07D279/04—1,3-Thiazines; Hydrogenated 1,3-thiazines
- C07D279/08—1,3-Thiazines; Hydrogenated 1,3-thiazines condensed with carbocyclic rings or ring 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
- C07D417/04—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 directly linked by a ring-member-to-ring-member bond
-
- 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
- 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
- C07D513/10—Spiro-condensed systems
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)
- Plural Heterocyclic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La presente invención proporciona una clase nueva de compuestos útiles para la modulación de la actividad de la enzima beta-secretase (BACE). Los compuestos tienen una Fórmula general I: en donde las variables A4, A5, A6, A8, y cada uno de Ra, Rb, R1, R2, R3 y R7 de la Fórmula I, independientemente, se definen en la presente. La invención 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 placa A-beta, que resulta de la actividad biológica de BACE.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462035269P | 2014-08-08 | 2014-08-08 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| UY36263A true UY36263A (es) | 2016-02-29 |
Family
ID=54150645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| UY0001036263A UY36263A (es) | 2014-08-08 | 2015-08-07 | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y métodos de uso |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US9550762B2 (es) |
| EP (1) | EP3177618A1 (es) |
| JP (1) | JP6576433B2 (es) |
| CN (1) | CN106795147B (es) |
| AR (1) | AR101483A1 (es) |
| AU (1) | AU2015301028B2 (es) |
| CA (1) | CA2957544C (es) |
| JO (1) | JO3569B1 (es) |
| MX (1) | MX381482B (es) |
| TW (1) | TWI614250B (es) |
| UY (1) | UY36263A (es) |
| WO (1) | WO2016022724A1 (es) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| KR20150124985A (ko) | 2013-03-08 | 2015-11-06 | 암젠 인크 | 베타-세크레타제 억제제로서 퍼플루오르화된 사이클로프로필 융합된 1,3-옥사진-2-아민 화합물 및 그의 사용 방법 |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US10246429B2 (en) | 2015-08-06 | 2019-04-02 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| MX394391B (es) | 2016-12-15 | 2025-03-24 | Amgen Inc | Derivados de tiazina y oxazina biciclicos como inhibidores de beta-secretasa y metodos de uso. |
| AU2017376444B2 (en) | 2016-12-15 | 2021-09-30 | Amgen Inc. | Thiazine derivatives as beta-secretase inhibitors and methods of use |
| WO2018112086A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Cyclopropyl fused thiazine derivatives as beta-secretase inhibitors and methods of use |
| US11021493B2 (en) | 2016-12-15 | 2021-06-01 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| AU2017376441B2 (en) | 2016-12-15 | 2021-10-14 | Amgen Inc. | Oxazine derivatives as beta-secretase inhibitors and methods of use |
| WO2018224455A1 (en) | 2017-06-07 | 2018-12-13 | Basf Se | Substituted cyclopropyl derivatives |
| CN113087669B (zh) * | 2019-12-23 | 2023-11-17 | 南京药石科技股份有限公司 | 一种4-氰基-5-溴嘧啶的制备方法 |
| CN115684413A (zh) * | 2022-11-01 | 2023-02-03 | 重庆市涪陵食品药品检验所 | 一种硫酸羟氯喹中硫酸二甲酯和硫酸二乙酯的检测方法 |
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| EP2931284B1 (en) | 2012-12-14 | 2017-08-23 | Merck Sharp & Dohme Corp. | Bace inhibitors of iminothiadiazine dioxides |
| EP2935282A1 (en) | 2012-12-19 | 2015-10-28 | Pfizer Inc. | CARBOCYCLIC- AND HETEROCYCLIC-SUBSTITUTED HEXAHYDROPYRANO[3,4-d][1,3]THIAZIN-2-AMINE COMPOUNDS |
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| EP2934539B1 (en) | 2012-12-20 | 2019-03-27 | Merck Sharp & Dohme Corp. | C5, c6 oxacyclic-fused iminothiazine dioxide compounds as bace inhibitors |
| WO2014099788A1 (en) | 2012-12-21 | 2014-06-26 | Merck Sharp & Dohme Corp. | C5-spiro iminothiadiazine dioxides as bace inhibitors |
| 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 |
| CA2902212C (en) | 2013-03-01 | 2020-10-13 | Amgen Inc. | Perfluorinated 5,6-dihydro-4h-1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| KR20150124985A (ko) * | 2013-03-08 | 2015-11-06 | 암젠 인크 | 베타-세크레타제 억제제로서 퍼플루오르화된 사이클로프로필 융합된 1,3-옥사진-2-아민 화합물 및 그의 사용 방법 |
| AU2014253275B2 (en) | 2013-04-11 | 2018-10-18 | F. Hoffmann-La Roche Ag | BACE1 inhibitors |
| HK1213562A1 (zh) | 2013-04-26 | 2016-07-08 | 豪夫迈‧罗氏有限公司 | Bace抑制剂的合成 |
| 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 |
| WO2016001266A1 (en) | 2014-07-04 | 2016-01-07 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
| AU2015301028B2 (en) | 2014-08-08 | 2019-09-26 | Amgen Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
-
2015
- 2015-08-05 AU AU2015301028A patent/AU2015301028B2/en active Active
- 2015-08-05 CA CA2957544A patent/CA2957544C/en active Active
- 2015-08-05 US US14/819,256 patent/US9550762B2/en active Active
- 2015-08-05 EP EP15766951.6A patent/EP3177618A1/en not_active Withdrawn
- 2015-08-05 MX MX2017001794A patent/MX381482B/es unknown
- 2015-08-05 WO PCT/US2015/043868 patent/WO2016022724A1/en not_active Ceased
- 2015-08-05 CN CN201580054674.2A patent/CN106795147B/zh active Active
- 2015-08-05 JP JP2017506879A patent/JP6576433B2/ja active Active
- 2015-08-07 AR ARP150102557A patent/AR101483A1/es unknown
- 2015-08-07 TW TW104125848A patent/TWI614250B/zh active
- 2015-08-07 UY UY0001036263A patent/UY36263A/es not_active Application Discontinuation
- 2015-08-09 JO JOP/2015/0190A patent/JO3569B1/ar active
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2016
- 2016-11-17 US US15/354,877 patent/US20170267673A1/en not_active Abandoned
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|---|---|
| CA2957544A1 (en) | 2016-02-11 |
| US20170267673A1 (en) | 2017-09-21 |
| CN106795147A (zh) | 2017-05-31 |
| US9550762B2 (en) | 2017-01-24 |
| CN106795147B (zh) | 2020-09-22 |
| US20160046618A1 (en) | 2016-02-18 |
| EP3177618A1 (en) | 2017-06-14 |
| TW201619154A (zh) | 2016-06-01 |
| JP2017523223A (ja) | 2017-08-17 |
| JP6576433B2 (ja) | 2019-09-18 |
| AR101483A1 (es) | 2016-12-21 |
| WO2016022724A1 (en) | 2016-02-11 |
| TWI614250B (zh) | 2018-02-11 |
| MX2017001794A (es) | 2017-06-29 |
| AU2015301028B2 (en) | 2019-09-26 |
| CA2957544C (en) | 2023-01-24 |
| AU2015301028A1 (en) | 2017-03-09 |
| MX381482B (es) | 2025-03-12 |
| JO3569B1 (ar) | 2020-07-05 |
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