CR20210630A - Inhibidores de monoacilglicerol lipasa (magl) heterocíclicos - Google Patents
Inhibidores de monoacilglicerol lipasa (magl) heterocíclicosInfo
- Publication number
- CR20210630A CR20210630A CR20210630A CR20210630A CR20210630A CR 20210630 A CR20210630 A CR 20210630A CR 20210630 A CR20210630 A CR 20210630A CR 20210630 A CR20210630 A CR 20210630A CR 20210630 A CR20210630 A CR 20210630A
- Authority
- CR
- Costa Rica
- Prior art keywords
- inhibitors
- magl
- heterocyclic
- monoacylglycerol lipase
- monoacylglycerol
- Prior art date
Links
- 102000005398 Monoacylglycerol Lipase Human genes 0.000 title abstract 4
- 108020002334 Monoacylglycerol lipase Proteins 0.000 title abstract 4
- 239000003112 inhibitor Substances 0.000 title abstract 3
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 150000001875 compounds Chemical class 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 230000004770 neurodegeneration Effects 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 230000003959 neuroinflammation Effects 0.000 abstract 1
- 230000036407 pain Effects 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 238000011282 treatment Methods 0.000 abstract 1
Classifications
-
- 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
-
- 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
-
- 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
- A61K31/495—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with two or more nitrogen atoms as the only ring heteroatoms, e.g. piperazine or tetrazines
- A61K31/4985—Pyrazines or piperazines 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
- 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
- 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
- C07D491/00—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00
- C07D491/02—Heterocyclic compounds containing in the condensed ring system both one or more rings having oxygen atoms as the only ring hetero atoms and one or more rings having nitrogen atoms as the only ring hetero atoms, not provided for by groups C07D451/00 - C07D459/00, C07D463/00, C07D477/00 or C07D489/00 in which the condensed system contains two hetero rings
- C07D491/10—Spiro-condensed systems
- C07D491/107—Spiro-condensed systems with only one oxygen atom as ring hetero atom in the oxygen-containing ring
-
- C—CHEMISTRY; METALLURGY
- C07—ORGANIC CHEMISTRY
- C07D—HETEROCYCLIC COMPOUNDS
- C07D519/00—Heterocyclic compounds containing more than one system of two or more relevant hetero rings condensed among themselves or condensed with a common carbocyclic ring system not provided for in groups C07D453/00 or C07D455/00
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Life Sciences & Earth Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- General Health & Medical Sciences (AREA)
- Medicinal Chemistry (AREA)
- Animal Behavior & Ethology (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Epidemiology (AREA)
- Hospice & Palliative Care (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Psychiatry (AREA)
- Inorganic Chemistry (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
La solicitud se refiere a compuestos heterocíclicos de la fórmula general (I), (I) un proceso para su preparación, composiciones farmacéuticas que los contienen y su uso médico. Los compuestos actúan como inhibidores de inhibidores de la monoacilglicerol lipasa (MAGL) y son útiles para el tratamiento o la profilaxis de neuroinflamación, enfermedades neurodegenerativas, dolor, cáncer o trastornos mentales
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19184218 | 2019-07-03 | ||
| PCT/EP2020/068320 WO2021001330A1 (en) | 2019-07-03 | 2020-06-30 | Heterocyclic monoacylglycerol lipase (magl) inhibitors |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| CR20210630A true CR20210630A (es) | 2022-02-11 |
Family
ID=67180549
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| CR20210630A CR20210630A (es) | 2019-07-03 | 2020-06-30 | Inhibidores de monoacilglicerol lipasa (magl) heterocíclicos |
Country Status (19)
| Country | Link |
|---|---|
| US (1) | US20220213093A1 (es) |
| EP (1) | EP3994137A1 (es) |
| JP (1) | JP7669299B2 (es) |
| KR (1) | KR20220027991A (es) |
| CN (1) | CN114072405A (es) |
| AR (1) | AR119322A1 (es) |
| AU (1) | AU2020299965A1 (es) |
| BR (1) | BR112021026820A2 (es) |
| CA (1) | CA3143280A1 (es) |
| CL (1) | CL2022000005A1 (es) |
| CO (1) | CO2022000749A2 (es) |
| CR (1) | CR20210630A (es) |
| IL (1) | IL288936A (es) |
| MA (1) | MA56443A (es) |
| MX (1) | MX2022000083A (es) |
| PE (1) | PE20220514A1 (es) |
| PH (1) | PH12021553248A1 (es) |
| TW (1) | TW202116768A (es) |
| WO (1) | WO2021001330A1 (es) |
Families Citing this family (9)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| AU2019322538B2 (en) | 2018-08-13 | 2021-09-30 | F. Hoffmann-La Roche Ag | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| PL3883936T3 (pl) | 2018-11-22 | 2023-11-20 | F. Hoffmann-La Roche Ag | Nowe związki heterocykliczne |
| WO2021000297A1 (en) | 2019-07-03 | 2021-01-07 | Merck Sharp & Dohme Corp. | Compounds and methods of use thereof as antibacterial agents |
| JP7649283B2 (ja) * | 2019-07-09 | 2025-03-19 | エフ. ホフマン-ラ ロシュ アーゲー | 新規複素環化合物 |
| MX2022002311A (es) | 2019-09-12 | 2022-03-25 | Hoffmann La Roche | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de monoacilglicerol lipasa (magl). |
| CR20230115A (es) | 2020-09-03 | 2023-04-11 | Hoffmann La Roche | Compuestos heterocíclicos |
| CA3217423A1 (en) | 2021-06-16 | 2022-12-22 | Jeffrey M. Schkeryantz | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
| IL313987A (en) | 2021-12-29 | 2024-08-01 | Psy Therapeutics Inc | Inhibiting monoacylglycerol lipase (magl) |
Family Cites Families (3)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US6673908B1 (en) * | 1999-02-22 | 2004-01-06 | Nuvelo, Inc. | Tumor necrosis factor receptor 2 |
| CN101668746A (zh) | 2007-03-01 | 2010-03-10 | 詹森药业有限公司 | 作为组胺h3受体调节剂的四氢异喹啉化合物 |
| WO2019134985A1 (en) * | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
-
2020
- 2020-06-30 JP JP2021577946A patent/JP7669299B2/ja active Active
- 2020-06-30 EP EP20734956.4A patent/EP3994137A1/en active Pending
- 2020-06-30 BR BR112021026820A patent/BR112021026820A2/pt not_active Application Discontinuation
- 2020-06-30 CA CA3143280A patent/CA3143280A1/en active Pending
- 2020-06-30 WO PCT/EP2020/068320 patent/WO2021001330A1/en not_active Ceased
- 2020-06-30 CN CN202080048854.0A patent/CN114072405A/zh active Pending
- 2020-06-30 PE PE2021002264A patent/PE20220514A1/es unknown
- 2020-06-30 AU AU2020299965A patent/AU2020299965A1/en not_active Abandoned
- 2020-06-30 PH PH1/2021/553248A patent/PH12021553248A1/en unknown
- 2020-06-30 MX MX2022000083A patent/MX2022000083A/es unknown
- 2020-06-30 KR KR1020227002453A patent/KR20220027991A/ko not_active Withdrawn
- 2020-06-30 MA MA056443A patent/MA56443A/fr unknown
- 2020-06-30 CR CR20210630A patent/CR20210630A/es unknown
- 2020-07-01 AR ARP200101858A patent/AR119322A1/es not_active Application Discontinuation
- 2020-07-02 TW TW109122385A patent/TW202116768A/zh unknown
-
2021
- 2021-12-12 IL IL288936A patent/IL288936A/en unknown
- 2021-12-16 US US17/552,792 patent/US20220213093A1/en active Pending
-
2022
- 2022-01-03 CL CL2022000005A patent/CL2022000005A1/es unknown
- 2022-01-27 CO CONC2022/0000749A patent/CO2022000749A2/es unknown
Also Published As
| Publication number | Publication date |
|---|---|
| CA3143280A1 (en) | 2021-01-07 |
| JP7669299B2 (ja) | 2025-04-28 |
| AR119322A1 (es) | 2021-12-09 |
| US20220213093A1 (en) | 2022-07-07 |
| TW202116768A (zh) | 2021-05-01 |
| BR112021026820A2 (pt) | 2022-02-22 |
| MX2022000083A (es) | 2022-02-03 |
| KR20220027991A (ko) | 2022-03-08 |
| CN114072405A (zh) | 2022-02-18 |
| IL288936A (en) | 2022-02-01 |
| WO2021001330A1 (en) | 2021-01-07 |
| JP2022540367A (ja) | 2022-09-15 |
| PH12021553248A1 (en) | 2023-02-27 |
| PE20220514A1 (es) | 2022-04-07 |
| CL2022000005A1 (es) | 2022-10-21 |
| AU2020299965A1 (en) | 2022-02-03 |
| CO2022000749A2 (es) | 2022-02-07 |
| MA56443A (fr) | 2022-05-11 |
| EP3994137A1 (en) | 2022-05-11 |
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