PE20220565A1 - Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl - Google Patents
Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de maglInfo
- Publication number
- PE20220565A1 PE20220565A1 PE2022000245A PE2022000245A PE20220565A1 PE 20220565 A1 PE20220565 A1 PE 20220565A1 PE 2022000245 A PE2022000245 A PE 2022000245A PE 2022000245 A PE2022000245 A PE 2022000245A PE 20220565 A1 PE20220565 A1 PE 20220565A1
- Authority
- PE
- Peru
- Prior art keywords
- oxazin
- compounds
- hexapirido
- azetidine
- heteroaryl
- Prior art date
Links
Classifications
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- 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
- A61K9/00—Medicinal preparations characterised by special physical form
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2009—Inorganic compounds
-
- 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
- A61K31/5375—1,4-Oxazines, e.g. morpholine
- A61K31/5383—1,4-Oxazines, e.g. morpholine 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
- A61K9/20—Pills, tablets, discs, rods
- A61K9/2004—Excipients; Inactive ingredients
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2054—Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
-
- 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
- A61K9/2022—Organic macromolecular compounds
- A61K9/205—Polysaccharides, e.g. alginate, gums; Cyclodextrin
- A61K9/2059—Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
-
- 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
- A61K9/485—Inorganic compounds
-
- 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
- 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
- A61K9/4866—Organic macromolecular compounds
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P1/00—Drugs for disorders of the alimentary tract or the digestive 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
-
- 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
- A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P29/00—Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
-
- A—HUMAN NECESSITIES
- A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
- A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
- A61P35/00—Antineoplastic agents
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D265/00—Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
- C07D265/28—1,4-Oxazines; Hydrogenated 1,4-oxazines
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
- C07D413/02—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
- C07D413/12—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Epidemiology (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Esta referido a un compuesto de Formula I, en donde: R1, R2 y R3 son H, alquilo; R4, R5, R6, R7 son H, halogeno, ciano, hidroxi, alcoxi, entre otros; Anillo A es arilo, heteroarilo heterociclilo; Anillo B es arilo y L1 es O; o B es heteroarilo y L1 es un enlace u O; m es 0, n es 0 o 1 y X es CR8; o m es 1, n es 1 o 2 y X es CR8 o N. Entre los compuestos preferidos tenemos los siguientes: (4aR,8aS)-6-(3-(4-fenoxifenil)azetidin-1-carbonil)hexahidro-2H-pirido[4,3- b][1,4]oxazin-3(4H)-ona; (4aR,8aS)-6-[3-[4-(2-clorofenoxi)fenil]azetidin-1-carbonil]-4,4a,5,7,8,8ahexahidropirido[4,3-b][1,4]oxazin-3-ona; entre otros. Estos compuestos son inhibidores de monoacilglicerol lipasa (MAGL) y se emplean en el tratamiento de neuroinflamacion, enfermedades neurodegenerativas, dolor, cancer, trastornos mentales, esclerosis multiple, enfermedad de Alzheimer, enfermedad de Parkinson, esclerosis lateral amiotrofica, lesion cerebral traumatica, entre otras.
Applications Claiming Priority (2)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP19196879 | 2019-09-12 | ||
PCT/EP2020/075260 WO2021048242A1 (en) | 2019-09-12 | 2020-09-10 | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
Publications (1)
Publication Number | Publication Date |
---|---|
PE20220565A1 true PE20220565A1 (es) | 2022-04-13 |
Family
ID=67953598
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
PE2022000245A PE20220565A1 (es) | 2019-09-12 | 2020-09-10 | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl |
Country Status (17)
Country | Link |
---|---|
US (1) | US11814375B2 (es) |
EP (1) | EP4028403B1 (es) |
JP (1) | JP2022548028A (es) |
KR (1) | KR20220062515A (es) |
CN (1) | CN114269755A (es) |
AR (1) | AR119943A1 (es) |
AU (1) | AU2020346350A1 (es) |
BR (1) | BR112022002375A2 (es) |
CA (1) | CA3151516A1 (es) |
CL (1) | CL2022000556A1 (es) |
CO (1) | CO2022001879A2 (es) |
CR (1) | CR20220104A (es) |
IL (1) | IL289186A (es) |
MX (1) | MX2022002311A (es) |
PE (1) | PE20220565A1 (es) |
TW (1) | TW202128706A (es) |
WO (1) | WO2021048242A1 (es) |
Families Citing this family (7)
Publication number | Priority date | Publication date | Assignee | Title |
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WO2018165520A1 (en) | 2017-03-10 | 2018-09-13 | Vps-3, Inc. | Metalloenzyme inhibitor compounds |
AR114136A1 (es) | 2017-10-10 | 2020-07-29 | Hoffmann La Roche | Compuestos heterocíclicos |
EP3717477B1 (en) | 2017-11-28 | 2022-07-20 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
EP3837263A1 (en) | 2018-08-13 | 2021-06-23 | F. Hoffmann-La Roche AG | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
EP4028403B1 (en) | 2019-09-12 | 2023-11-22 | F. Hoffmann-La Roche AG | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
CR20220325A (es) | 2019-12-20 | 2022-08-19 | Tenaya Therapeutics Inc | Fluoroalquil-oxadiazoles y sus usos |
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EP3837263A1 (en) | 2018-08-13 | 2021-06-23 | F. Hoffmann-La Roche AG | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
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EP4028403B1 (en) | 2019-09-12 | 2023-11-22 | F. Hoffmann-La Roche AG | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
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EP4034239A1 (en) | 2019-09-23 | 2022-08-03 | F. Hoffmann-La Roche AG | Heterocyclic compounds |
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AU2020354414A1 (en) | 2019-09-24 | 2022-02-17 | F. Hoffmann-La Roche Ag | New heterocyclic monoacylglycerol lipase (MAGL) inhibitors |
AR120029A1 (es) | 2019-09-24 | 2022-01-26 | Hoffmann La Roche | Compuestos heterocíclicos |
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2020
- 2020-09-10 EP EP20774901.1A patent/EP4028403B1/en active Active
- 2020-09-10 MX MX2022002311A patent/MX2022002311A/es unknown
- 2020-09-10 BR BR112022002375A patent/BR112022002375A2/pt unknown
- 2020-09-10 PE PE2022000245A patent/PE20220565A1/es unknown
- 2020-09-10 CR CR20220104A patent/CR20220104A/es unknown
- 2020-09-10 CA CA3151516A patent/CA3151516A1/en active Pending
- 2020-09-10 KR KR1020227007925A patent/KR20220062515A/ko unknown
- 2020-09-10 JP JP2022516054A patent/JP2022548028A/ja active Pending
- 2020-09-10 US US17/017,200 patent/US11814375B2/en active Active
- 2020-09-10 WO PCT/EP2020/075260 patent/WO2021048242A1/en unknown
- 2020-09-10 CN CN202080059190.8A patent/CN114269755A/zh active Pending
- 2020-09-10 AU AU2020346350A patent/AU2020346350A1/en active Pending
- 2020-09-11 TW TW109131236A patent/TW202128706A/zh unknown
- 2020-09-11 AR ARP200102527A patent/AR119943A1/es unknown
-
2021
- 2021-12-20 IL IL289186A patent/IL289186A/en unknown
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2022
- 2022-02-22 CO CONC2022/0001879A patent/CO2022001879A2/es unknown
- 2022-03-07 CL CL2022000556A patent/CL2022000556A1/es unknown
Also Published As
Publication number | Publication date |
---|---|
MX2022002311A (es) | 2022-03-25 |
CR20220104A (es) | 2022-04-20 |
EP4028403C0 (en) | 2023-11-22 |
CA3151516A1 (en) | 2021-03-18 |
KR20220062515A (ko) | 2022-05-17 |
CO2022001879A2 (es) | 2022-03-29 |
WO2021048242A1 (en) | 2021-03-18 |
TW202128706A (zh) | 2021-08-01 |
EP4028403B1 (en) | 2023-11-22 |
US20210094943A1 (en) | 2021-04-01 |
AR119943A1 (es) | 2022-01-19 |
CL2022000556A1 (es) | 2022-10-21 |
US11814375B2 (en) | 2023-11-14 |
IL289186A (en) | 2022-02-01 |
AU2020346350A1 (en) | 2022-02-17 |
CN114269755A (zh) | 2022-04-01 |
JP2022548028A (ja) | 2022-11-16 |
EP4028403A1 (en) | 2022-07-20 |
BR112022002375A2 (pt) | 2022-07-19 |
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