MX381482B - Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. - Google Patents
Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso.Info
- Publication number
- MX381482B MX381482B MX2017001794A MX2017001794A MX381482B MX 381482 B MX381482 B MX 381482B MX 2017001794 A MX2017001794 A MX 2017001794A MX 2017001794 A MX2017001794 A MX 2017001794A MX 381482 B MX381482 B MX 381482B
- Authority
- MX
- Mexico
- Prior art keywords
- sup
- compounds
- beta
- methods
- bace
- Prior art date
Links
- 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
- WADGHWKXQZVKFK-UHFFFAOYSA-N thiazin-2-amine Chemical class NN1SC=CC=C1 WADGHWKXQZVKFK-UHFFFAOYSA-N 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
- 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
- 230000008021 deposition Effects 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
-
- 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)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Medicinal Chemistry (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Veterinary Medicine (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Public Health (AREA)
- Neurology (AREA)
- Biomedical Technology (AREA)
- Neurosurgery (AREA)
- Diabetes (AREA)
- Hematology (AREA)
- Cardiology (AREA)
- Heart & Thoracic Surgery (AREA)
- Hospice & Palliative Care (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)
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| US201462035269P | 2014-08-08 | 2014-08-08 | |
| PCT/US2015/043868 WO2016022724A1 (en) | 2014-08-08 | 2015-08-05 | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
Publications (2)
| Publication Number | Publication Date |
|---|---|
| MX2017001794A MX2017001794A (es) | 2017-06-29 |
| MX381482B true MX381482B (es) | 2025-03-12 |
Family
ID=54150645
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| MX2017001794A MX381482B (es) | 2014-08-08 | 2015-08-05 | Compuestos de tiazin-2-amina fusionados con ciclopropilo como inhibidores de beta-secretasa y metodos de uso. |
Country Status (12)
| Country | Link |
|---|---|
| US (2) | US9550762B2 (enExample) |
| EP (1) | EP3177618A1 (enExample) |
| JP (1) | JP6576433B2 (enExample) |
| CN (1) | CN106795147B (enExample) |
| AR (1) | AR101483A1 (enExample) |
| AU (1) | AU2015301028B2 (enExample) |
| CA (1) | CA2957544C (enExample) |
| JO (1) | JO3569B1 (enExample) |
| MX (1) | MX381482B (enExample) |
| TW (1) | TWI614250B (enExample) |
| UY (1) | UY36263A (enExample) |
| WO (1) | WO2016022724A1 (enExample) |
Families Citing this family (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AP2015008716A0 (en) | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| WO2017024180A1 (en) | 2015-08-06 | 2017-02-09 | Amgen Inc. | Vinyl fluoride cyclopropyl fused thiazin-2-amine compounds 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 |
| MX388697B (es) | 2016-12-15 | 2025-03-20 | Amgen Inc | Derivados de tiazina como inhibidores de beta-secretasa y metodos de uso. |
| WO2018112084A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | Bicyclic thiazine and oxazine derivatives as beta-secretase inhibitors and methods of use |
| CA3047290A1 (en) | 2016-12-15 | 2018-06-21 | Amgen Inc. | 1,4-thiazine dioxide and 1,2,4-thiadiazine dioxide derivatives as beta-secretase inhibitors and methods of use |
| WO2018112081A1 (en) | 2016-12-15 | 2018-06-21 | 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 |
| US9403846B2 (en) | 2012-12-19 | 2016-08-02 | Pfizer Inc. | Carbocyclic- and heterocyclic-substituted hexahydropyrano[3,4-d][1,3]thiazin-2-amine compounds |
| WO2014098831A1 (en) | 2012-12-19 | 2014-06-26 | Bristol-Myers Squibb Company | 4,6-diarylaminothiazines as bace1 inhibitors and their use for the reduction of beta-amyloid production |
| JP2016504998A (ja) | 2012-12-20 | 2016-02-18 | メルク・シャープ・アンド・ドーム・コーポレーションＭｅｒｃｋ Ｓｈａｒｐ ＆ Ｄｏｈｍｅ Ｃｏｒｐ． | Ｂａｃｅ阻害剤としてのｃ５，ｃ６オキサ環縮合イミノチアジンジオキシド化合物、組成物およびそれらの使用 |
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| WO2014114532A1 (en) | 2013-01-22 | 2014-07-31 | F. Hoffmann-La Roche Ag | Fluoro-[1,3]oxazines as bace1 inhibitors |
| 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 |
| AP2015008716A0 (en) * | 2013-03-08 | 2015-09-30 | Amgen Inc | Perfluorinated cyclopropyl fused 1,3-oxazin-2-amine compounds as beta-secretase inhibitors and methods of use |
| MX2015014083A (es) | 2013-04-11 | 2016-07-26 | Hoffmann La Roche | Inhibidores de enzima de escision de proteina precursora beta-amiloide (app) en el sitio beta 1 (bace1). |
| EP2989081A1 (en) | 2013-04-26 | 2016-03-02 | F. Hoffmann-La Roche AG | Synthesis of bace inhibitors |
| 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 |
| US9550762B2 (en) | 2014-08-08 | 2017-01-24 | Amgen, Inc. | Cyclopropyl fused thiazin-2-amine compounds as beta-secretase inhibitors and methods of use |
-
2015
- 2015-08-05 US US14/819,256 patent/US9550762B2/en active Active
- 2015-08-05 MX MX2017001794A patent/MX381482B/es unknown
- 2015-08-05 CN CN201580054674.2A patent/CN106795147B/zh active Active
- 2015-08-05 JP JP2017506879A patent/JP6576433B2/ja active Active
- 2015-08-05 AU AU2015301028A patent/AU2015301028B2/en active Active
- 2015-08-05 EP EP15766951.6A patent/EP3177618A1/en not_active Withdrawn
- 2015-08-05 CA CA2957544A patent/CA2957544C/en active Active
- 2015-08-05 WO PCT/US2015/043868 patent/WO2016022724A1/en not_active Ceased
- 2015-08-07 UY UY0001036263A patent/UY36263A/es not_active Application Discontinuation
- 2015-08-07 TW TW104125848A patent/TWI614250B/zh active
- 2015-08-07 AR ARP150102557A patent/AR101483A1/es unknown
- 2015-08-09 JO JOP/2015/0190A patent/JO3569B1/ar active
-
2016
- 2016-11-17 US US15/354,877 patent/US20170267673A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN106795147A (zh) | 2017-05-31 |
| CN106795147B (zh) | 2020-09-22 |
| JP2017523223A (ja) | 2017-08-17 |
| AU2015301028A1 (en) | 2017-03-09 |
| JO3569B1 (ar) | 2020-07-05 |
| JP6576433B2 (ja) | 2019-09-18 |
| CA2957544A1 (en) | 2016-02-11 |
| AR101483A1 (es) | 2016-12-21 |
| UY36263A (es) | 2016-02-29 |
| WO2016022724A1 (en) | 2016-02-11 |
| US20160046618A1 (en) | 2016-02-18 |
| EP3177618A1 (en) | 2017-06-14 |
| US20170267673A1 (en) | 2017-09-21 |
| US9550762B2 (en) | 2017-01-24 |
| CA2957544C (en) | 2023-01-24 |
| MX2017001794A (es) | 2017-06-29 |
| AU2015301028B2 (en) | 2019-09-26 |
| TWI614250B (zh) | 2018-02-11 |
| TW201619154A (zh) | 2016-06-01 |
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