PE20211776A1 - Derivados de 7-fenoxi-n-(3-azabiciclo[3.2.1]octan-8-il)-6,7-dihidro-5h-pirrolo[1,2-b][1,2,4]triazol-2-amina y compuestos relacionados como moduladores de gamma-secretasa para el tratamiento de la enfermedad de alzheimer - Google Patents
Derivados de 7-fenoxi-n-(3-azabiciclo[3.2.1]octan-8-il)-6,7-dihidro-5h-pirrolo[1,2-b][1,2,4]triazol-2-amina y compuestos relacionados como moduladores de gamma-secretasa para el tratamiento de la enfermedad de alzheimerInfo
- Publication number
- PE20211776A1 PE20211776A1 PE2021000726A PE2021000726A PE20211776A1 PE 20211776 A1 PE20211776 A1 PE 20211776A1 PE 2021000726 A PE2021000726 A PE 2021000726A PE 2021000726 A PE2021000726 A PE 2021000726A PE 20211776 A1 PE20211776 A1 PE 20211776A1
- Authority
- PE
- Peru
- Prior art keywords
- octan
- triazol
- alzheimer
- dihydro
- gamma
- Prior art date
Links
- 150000001875 compounds Chemical class 0.000 title abstract 4
- VHNYOQKVZQVBLC-RTCGXNAVSA-N (4r,7e,9as)-7-[[3-methoxy-4-(4-methylimidazol-1-yl)phenyl]methylidene]-4-(3,4,5-trifluorophenyl)-1,3,4,8,9,9a-hexahydropyrido[2,1-c][1,4]oxazin-6-one Chemical compound C1([C@@H]2COC[C@@H]3CC\C(C(N32)=O)=C/C=2C=C(C(=CC=2)N2C=C(C)N=C2)OC)=CC(F)=C(F)C(F)=C1 VHNYOQKVZQVBLC-RTCGXNAVSA-N 0.000 title abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 title abstract 2
- 229940124648 γ-Secretase Modulator Drugs 0.000 title abstract 2
- NHAZGSRLKBTDBF-UHFFFAOYSA-N 1,2,4-triazol-1-amine Chemical compound NN1C=NC=N1 NHAZGSRLKBTDBF-UHFFFAOYSA-N 0.000 title 1
- -1 3,5-difluorophenoxy Chemical group 0.000 abstract 1
- 206010011878 Deafness Diseases 0.000 abstract 1
- 206010012289 Dementia Diseases 0.000 abstract 1
- 201000010374 Down Syndrome Diseases 0.000 abstract 1
- 208000005314 Multi-Infarct Dementia Diseases 0.000 abstract 1
- 206010044688 Trisomy 21 Diseases 0.000 abstract 1
- 201000004810 Vascular dementia Diseases 0.000 abstract 1
- 230000006933 amyloid-beta aggregation Effects 0.000 abstract 1
- 210000004556 brain Anatomy 0.000 abstract 1
- 201000010099 disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 230000010370 hearing loss Effects 0.000 abstract 1
- 231100000888 hearing loss Toxicity 0.000 abstract 1
- 208000016354 hearing loss disease Diseases 0.000 abstract 1
- 125000001072 heteroaryl group Chemical group 0.000 abstract 1
Classifications
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- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D487/00—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00
- C07D487/02—Heterocyclic compounds containing nitrogen atoms as the only ring hetero atoms in the condensed system, not provided for by groups C07D451/00 - C07D477/00 in which the condensed system contains two hetero rings
- C07D487/04—Ortho-condensed systems
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- 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
- A61K31/435—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
- A61K31/46—8-Azabicyclo [3.2.1] octane; Derivatives thereof, e.g. atropine, cocaine
-
- 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
- A61P27/00—Drugs for disorders of the senses
- A61P27/16—Otologicals
-
- 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
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)
- Medicinal Chemistry (AREA)
- Public Health (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Chemical & Material Sciences (AREA)
- Neurosurgery (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Biomedical Technology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Neurology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Emergency Medicine (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Medicinal Preparation (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Un compuesto de formula (I) donde R 1 es halogeno; m es 1,2 o 3; n es 1, 2, 3; Ar es un grupo heteroarilo de seis miembros. Los presentes compuestos son como moduladores de gamma-secretasa para el tratamiento de enfermedades asociadas al deposito de beta-amiloide en el cerebro, tales como enfermedad de Alzheimer, hipoacusia, demencia multiinfarto, demencia pugilistica y sindrome de Down. Un compuesto de ejemplo es (R)-7-(3,5-difluorofenoxi)-N- ((1R,5S,8s)-3-(6-metoxipiridazin-4-il)-3-azabiciclo[3.2.1]octan-8-il)-6,7-dihidro-5Hpirrolo[1,2-b][1,2,4]triazol-2-amina.
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18212199 | 2018-12-13 | ||
| PCT/EP2019/084538 WO2020120521A1 (en) | 2018-12-13 | 2019-12-11 | 7-phenoxy-n-(3-azabicyclo[3.2.1]octan-8-yl)-6,7-dihydro-5h-pyrrolo[1,2-b][1,2,4]triazol-2-amine derivatives and related compounds as gamma-secretase modulators for the treatment of alzheimer's disease |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| PE20211776A1 true PE20211776A1 (es) | 2021-09-08 |
Family
ID=64665266
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021000726A PE20211776A1 (es) | 2018-12-13 | 2019-12-11 | Derivados de 7-fenoxi-n-(3-azabiciclo[3.2.1]octan-8-il)-6,7-dihidro-5h-pirrolo[1,2-b][1,2,4]triazol-2-amina y compuestos relacionados como moduladores de gamma-secretasa para el tratamiento de la enfermedad de alzheimer |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20220056036A1 (es) |
| EP (1) | EP3894411A1 (es) |
| JP (1) | JP2022513466A (es) |
| KR (1) | KR20210102900A (es) |
| CN (2) | CN117946116A (es) |
| AR (1) | AR116906A1 (es) |
| AU (1) | AU2019395774A1 (es) |
| BR (1) | BR112021009443A2 (es) |
| CA (1) | CA3117870A1 (es) |
| CL (1) | CL2021001547A1 (es) |
| CO (1) | CO2021006837A2 (es) |
| CR (1) | CR20210305A (es) |
| IL (2) | IL310081A (es) |
| MA (1) | MA54447A (es) |
| MX (1) | MX2021006761A (es) |
| PE (1) | PE20211776A1 (es) |
| SG (1) | SG11202103340PA (es) |
| TW (1) | TWI831892B (es) |
| WO (1) | WO2020120521A1 (es) |
Family Cites Families (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US8703763B2 (en) * | 2011-03-02 | 2014-04-22 | Hoffmann-La Roche Inc. | Bridged piperidine derivatives |
| EP3347363B1 (en) * | 2015-09-09 | 2020-01-01 | H. Hoffnabb-La Roche Ag | N-(3-azabicyclo[3.2.1]octan-8-yl)-8-(4-phenyl)-5,6,7,8-tetrahydro-[1,2,4]triazolo[l,5-a]pyridin-2-amine derivatives as gamma-secretase modulators for treating alzheimer's disease |
| CN108137579B (zh) * | 2015-12-10 | 2022-01-07 | 豪夫迈·罗氏有限公司 | 桥连哌啶衍生物 |
| EP3475279B1 (en) * | 2016-06-27 | 2021-07-14 | F. Hoffmann-La Roche AG | Triazolopyridines as gamma-secretase modulators |
| CN109641912B (zh) * | 2016-11-01 | 2021-10-29 | 豪夫迈·罗氏有限公司 | 二环杂芳基衍生物 |
| US11319314B2 (en) * | 2016-11-08 | 2022-05-03 | Hoffmann-La Roche Inc. | Phenoxytriazoles |
| AU2017376109A1 (en) | 2016-12-16 | 2019-07-11 | Pipeline Therapeutics, Inc. | Methods of treating cochlear synaptopathy |
-
2019
- 2019-12-11 MA MA054447A patent/MA54447A/fr unknown
- 2019-12-11 JP JP2021533563A patent/JP2022513466A/ja active Pending
- 2019-12-11 SG SG11202103340PA patent/SG11202103340PA/en unknown
- 2019-12-11 CN CN202311792520.6A patent/CN117946116A/zh active Pending
- 2019-12-11 EP EP19824250.5A patent/EP3894411A1/en active Pending
- 2019-12-11 CN CN201980076253.8A patent/CN113179641B/zh active Active
- 2019-12-11 IL IL310081A patent/IL310081A/en unknown
- 2019-12-11 KR KR1020217017774A patent/KR20210102900A/ko unknown
- 2019-12-11 BR BR112021009443-1A patent/BR112021009443A2/pt unknown
- 2019-12-11 CA CA3117870A patent/CA3117870A1/en active Pending
- 2019-12-11 AU AU2019395774A patent/AU2019395774A1/en active Pending
- 2019-12-11 MX MX2021006761A patent/MX2021006761A/es unknown
- 2019-12-11 PE PE2021000726A patent/PE20211776A1/es unknown
- 2019-12-11 IL IL283823A patent/IL283823B1/en unknown
- 2019-12-11 CR CR20210305A patent/CR20210305A/es unknown
- 2019-12-11 US US17/413,413 patent/US20220056036A1/en active Pending
- 2019-12-11 WO PCT/EP2019/084538 patent/WO2020120521A1/en unknown
- 2019-12-12 AR ARP190103631A patent/AR116906A1/es unknown
- 2019-12-12 TW TW108145480A patent/TWI831892B/zh active
-
2021
- 2021-05-24 CO CONC2021/0006837A patent/CO2021006837A2/es unknown
- 2021-06-11 CL CL2021001547A patent/CL2021001547A1/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| EP3894411A1 (en) | 2021-10-20 |
| AR116906A1 (es) | 2021-06-23 |
| CR20210305A (es) | 2021-07-20 |
| MA54447A (fr) | 2022-03-23 |
| CL2021001547A1 (es) | 2021-12-24 |
| IL283823B1 (en) | 2024-03-01 |
| JP2022513466A (ja) | 2022-02-08 |
| SG11202103340PA (en) | 2021-04-29 |
| CA3117870A1 (en) | 2020-06-18 |
| IL283823A (en) | 2021-07-29 |
| KR20210102900A (ko) | 2021-08-20 |
| WO2020120521A1 (en) | 2020-06-18 |
| CN113179641A (zh) | 2021-07-27 |
| CO2021006837A2 (es) | 2021-06-10 |
| IL310081A (en) | 2024-03-01 |
| MX2021006761A (es) | 2021-07-15 |
| BR112021009443A2 (pt) | 2021-08-17 |
| AU2019395774A1 (en) | 2021-04-08 |
| TWI831892B (zh) | 2024-02-11 |
| US20220056036A1 (en) | 2022-02-24 |
| CN117946116A (zh) | 2024-04-30 |
| TW202039499A (zh) | 2020-11-01 |
| CN113179641B (zh) | 2024-01-02 |
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