CR20220104A - 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
- CR20220104A CR20220104A CR20220104A CR20220104A CR20220104A CR 20220104 A CR20220104 A CR 20220104A CR 20220104 A CR20220104 A CR 20220104A CR 20220104 A CR20220104 A CR 20220104A CR 20220104 A CR20220104 A CR 20220104A
- Authority
- CR
- Costa Rica
- Prior art keywords
- compounds
- hexapirido
- oxazin
- magl inhibitors
- magl
- Prior art date
Links
- 239000003112 inhibitor Substances 0.000 title abstract 2
- XEKAWZARUWARND-UHFFFAOYSA-N 6h-oxazin-3-one Chemical class O=C1NOCC=C1 XEKAWZARUWARND-UHFFFAOYSA-N 0.000 title 1
- 102100029814 Monoglyceride lipase Human genes 0.000 title 1
- 101710116393 Monoglyceride lipase Proteins 0.000 title 1
- 150000001875 compounds Chemical class 0.000 abstract 3
- 102000005398 Monoacylglycerol Lipase Human genes 0.000 abstract 2
- 108020002334 Monoacylglycerol lipase Proteins 0.000 abstract 2
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 239000000203 mixture Substances 0.000 abstract 1
Classifications
-
- 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)
- Public Health (AREA)
- Veterinary Medicine (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- General Health & Medical Sciences (AREA)
- Epidemiology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Inorganic Chemistry (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Rheumatology (AREA)
- Psychiatry (AREA)
- Pain & Pain Management (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La invención proporciona nuevos compuestos heterocíclicos que tienen la Fórmula general (I), en donde A, B, L1 , X, m, n, y R1 a R7 son como se describen en la presente, composiciones que incluyen los compuestos, procesos de elaboración de los compuestos y métodos de uso de los compuestos como inhibidores de monoacilglicerol lipasa (MAGL)
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 |
|---|---|
| CR20220104A true CR20220104A (es) | 2022-04-20 |
Family
ID=67953598
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20220104A CR20220104A (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 (18)
| Country | Link |
|---|---|
| US (1) | US11814375B2 (es) |
| EP (1) | EP4028403B1 (es) |
| JP (1) | JP7609854B2 (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) |
| PH (1) | PH12022550339A1 (es) |
| TW (1) | TW202128706A (es) |
| WO (1) | WO2021048242A1 (es) |
Families Citing this family (15)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| 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 |
| WO2019105915A1 (en) | 2017-11-28 | 2019-06-06 | 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 |
| PE20211089A1 (es) | 2018-08-13 | 2021-06-14 | Hoffmann La Roche | Nuevos compuestos heterociclicos como inhibidores de la monoacilglicerol lipasa |
| WO2020104494A1 (en) | 2018-11-22 | 2020-05-28 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| AU2020321955A1 (en) | 2019-07-30 | 2022-03-17 | Eikonizo Therapapeutics, Inc. | HDAC6 inhibitors and uses thereof |
| CN114269755A (zh) | 2019-09-12 | 2022-04-01 | 豪夫迈·罗氏有限公司 | 作为magl抑制剂的4,4a,5,7,8,8a-六吡啶并[4,3-b][1,4]噁嗪-3-酮化合物 |
| MX2022007376A (es) | 2019-12-20 | 2022-09-02 | Tenaya Therapeutics Inc | Fluoroalqull-oxadiazoles y sus usos. |
| CA3190277A1 (en) | 2020-09-03 | 2022-03-10 | Joerg Benz | Heterocyclic compounds |
| US20240252502A1 (en) | 2021-05-04 | 2024-08-01 | Tenaya Therapeutics, Inc. | Hdac6 inhibitors for treatment of metabolic disease and hfpef |
| CA3242372A1 (en) | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Inhibiting monoacylglycerol lipase (magl) |
| TW202345813A (zh) | 2022-04-08 | 2023-12-01 | 美商艾科尼佐療法股份有限公司 | 㗁二唑hdac6抑制劑及其用途 |
| CN116410483A (zh) * | 2023-04-14 | 2023-07-11 | 沈阳工业大学 | 一种羰基联氮杂环超分子鎓盐及其制备方法与应用 |
| CN120040415A (zh) * | 2023-11-24 | 2025-05-27 | 中国药科大学 | 一种含喹啉酮骨架的化合物及其应用 |
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| US7160888B2 (en) | 2003-08-22 | 2007-01-09 | Warner Lambert Company Llc | [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia |
| US7579495B2 (en) | 2003-12-19 | 2009-08-25 | Momentive Performance Materials Inc. | Active-releasing cyclic siloxanes |
| ATE450525T1 (de) | 2005-06-20 | 2009-12-15 | Schering Corp | Kohlenstoffgebundene substituierte piperidine und derivate daraus als histamin-h3-antagonisten |
| JP5116687B2 (ja) | 2005-11-02 | 2013-01-09 | バイエル・ファルマ・アクチェンゲゼルシャフト | がんおよび他の過剰増殖性疾患の処置のためのピロロ[2,1−f][1,2,4]トリアジン−4−イルアミンIGF−1Rキナーゼ阻害剤 |
| EP1984351A1 (en) | 2006-02-17 | 2008-10-29 | Memory Pharmaceuticals Corporation | Compounds having 5-ht6 receptor affinity |
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| KR20150143720A (ko) | 2013-04-16 | 2015-12-23 | 액테리온 파마슈티칼 리미티드 | 항균성 이방향족 유도체 |
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| KR20180005250A (ko) | 2015-05-21 | 2018-01-15 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | Pad4 억제제로서의 벤조이미다졸 유도체 |
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| AU2018285131B2 (en) | 2017-06-12 | 2021-11-11 | Boehringer Ingelheim International Gmbh | Heteroaromatic compounds as Vanin inhibitors |
| MX2020007318A (es) | 2017-09-29 | 2020-08-24 | Takeda Pharmaceuticals Co | Compuesto heterociclico. |
| AR114136A1 (es) | 2017-10-10 | 2020-07-29 | Hoffmann La Roche | Compuestos heterocíclicos |
| WO2019105915A1 (en) * | 2017-11-28 | 2019-06-06 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| TW201930300A (zh) | 2017-12-15 | 2019-08-01 | 瑞士商赫孚孟拉羅股份公司 | 新雜環化合物 |
| WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| ES2942319T3 (es) | 2018-03-22 | 2023-05-31 | Hoffmann La Roche | Inhibidores de oxacina monoacilglicerol lipasa (MAGL) |
| PE20211089A1 (es) | 2018-08-13 | 2021-06-14 | Hoffmann La Roche | Nuevos compuestos heterociclicos como inhibidores de la monoacilglicerol lipasa |
| AU2019322161A1 (en) | 2018-08-13 | 2020-11-12 | F. Hoffmann-La Roche Ag | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| MA54555A (fr) | 2018-11-22 | 2021-09-29 | Qilu Regor Therapeutics Inc | Agonistes de glp-1r et leurs utilisations |
| WO2020104494A1 (en) * | 2018-11-22 | 2020-05-28 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| EP3953360B1 (en) | 2019-04-09 | 2024-02-28 | F. Hoffmann-La Roche AG | Heterocyclic compounds as inhibitors of monoacylglycerol lipase (magl) |
| MX2022000083A (es) | 2019-07-03 | 2022-02-03 | Hoffmann La Roche | Inhibidores de monoacilglicerol lipasa (magl) heterociclicos. |
| CN114096545A (zh) | 2019-07-09 | 2022-02-25 | 豪夫迈·罗氏有限公司 | 新杂环化合物 |
| US20210094971A1 (en) | 2019-09-09 | 2021-04-01 | Hoffmann-La Roche Inc. | Heterocyclic compounds |
| CN114269755A (zh) | 2019-09-12 | 2022-04-01 | 豪夫迈·罗氏有限公司 | 作为magl抑制剂的4,4a,5,7,8,8a-六吡啶并[4,3-b][1,4]噁嗪-3-酮化合物 |
| WO2021048241A1 (en) | 2019-09-12 | 2021-03-18 | F. Hoffmann-La Roche Ag | Radiolabeled compounds |
| PH12022550433A1 (en) | 2019-09-23 | 2024-01-29 | Hoffmann La Roche | Heterocyclic compounds |
| WO2021058443A1 (en) | 2019-09-24 | 2021-04-01 | F. Hoffmann-La Roche Ag | Fluorescent probes for monoacylglycerol lipase (magl) |
| WO2021058445A1 (en) | 2019-09-24 | 2021-04-01 | F. Hoffmann-La Roche Ag | New heterocyclic monoacylglycerol lipase (magl) inhibitors |
| CR20220117A (es) | 2019-09-24 | 2022-04-20 | F Horrmann La Roche Ag | Compuestos heterocíclicos |
| CA3190277A1 (en) | 2020-09-03 | 2022-03-10 | Joerg Benz | Heterocyclic compounds |
-
2020
- 2020-09-10 CN CN202080059190.8A patent/CN114269755A/zh active Pending
- 2020-09-10 MX MX2022002311A patent/MX2022002311A/es unknown
- 2020-09-10 PE PE2022000245A patent/PE20220565A1/es unknown
- 2020-09-10 US US17/017,200 patent/US11814375B2/en active Active
- 2020-09-10 EP EP20774901.1A patent/EP4028403B1/en active Active
- 2020-09-10 PH PH1/2022/550339A patent/PH12022550339A1/en unknown
- 2020-09-10 CA CA3151516A patent/CA3151516A1/en active Pending
- 2020-09-10 AU AU2020346350A patent/AU2020346350A1/en not_active Abandoned
- 2020-09-10 WO PCT/EP2020/075260 patent/WO2021048242A1/en not_active Ceased
- 2020-09-10 JP JP2022516054A patent/JP7609854B2/ja active Active
- 2020-09-10 BR BR112022002375A patent/BR112022002375A2/pt not_active Application Discontinuation
- 2020-09-10 KR KR1020227007925A patent/KR20220062515A/ko not_active Ceased
- 2020-09-10 CR CR20220104A patent/CR20220104A/es unknown
- 2020-09-11 AR ARP200102527A patent/AR119943A1/es not_active Application Discontinuation
- 2020-09-11 TW TW109131236A patent/TW202128706A/zh unknown
-
2021
- 2021-12-20 IL IL289186A patent/IL289186A/en unknown
-
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 |
|---|---|
| PE20220565A1 (es) | 2022-04-13 |
| US20210094943A1 (en) | 2021-04-01 |
| EP4028403B1 (en) | 2023-11-22 |
| CN114269755A (zh) | 2022-04-01 |
| CA3151516A1 (en) | 2021-03-18 |
| CL2022000556A1 (es) | 2022-10-21 |
| JP2022548028A (ja) | 2022-11-16 |
| EP4028403C0 (en) | 2023-11-22 |
| PH12022550339A1 (en) | 2023-03-13 |
| KR20220062515A (ko) | 2022-05-17 |
| AR119943A1 (es) | 2022-01-19 |
| CO2022001879A2 (es) | 2022-03-29 |
| JP7609854B2 (ja) | 2025-01-07 |
| US11814375B2 (en) | 2023-11-14 |
| EP4028403A1 (en) | 2022-07-20 |
| IL289186A (en) | 2022-02-01 |
| TW202128706A (zh) | 2021-08-01 |
| MX2022002311A (es) | 2022-03-25 |
| WO2021048242A1 (en) | 2021-03-18 |
| AU2020346350A1 (en) | 2022-02-17 |
| BR112022002375A2 (pt) | 2022-07-19 |
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