PE20220514A1 - Inhibidores de monoacilglicerol lipasa (magl) heterociclicos - Google Patents
Inhibidores de monoacilglicerol lipasa (magl) heterociclicosInfo
- Publication number
- PE20220514A1 PE20220514A1 PE2021002264A PE2021002264A PE20220514A1 PE 20220514 A1 PE20220514 A1 PE 20220514A1 PE 2021002264 A PE2021002264 A PE 2021002264A PE 2021002264 A PE2021002264 A PE 2021002264A PE 20220514 A1 PE20220514 A1 PE 20220514A1
- Authority
- PE
- Peru
- Prior art keywords
- chloro
- magl
- inhibitors
- heterocyclic
- methanone
- 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 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000001072 heteroaryl group Chemical group 0.000 abstract 2
- 208000024827 Alzheimer disease Diseases 0.000 abstract 1
- 208000019901 Anxiety disease Diseases 0.000 abstract 1
- UQGWUTGDHPNEIA-IVZQSRNASA-N ClC=1C=C(C=CC=1F)[C@]1(CC[C@H]2N(CCN(C2)C(=O)C2=C(C(=CC=C2)OC)Cl)C1)O Chemical compound ClC=1C=C(C=CC=1F)[C@]1(CC[C@H]2N(CCN(C2)C(=O)C2=C(C(=CC=C2)OC)Cl)C1)O UQGWUTGDHPNEIA-IVZQSRNASA-N 0.000 abstract 1
- 208000019695 Migraine disease Diseases 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000036110 Neuroinflammatory disease Diseases 0.000 abstract 1
- 206010029350 Neurotoxicity Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 208000018737 Parkinson disease Diseases 0.000 abstract 1
- 208000006011 Stroke Diseases 0.000 abstract 1
- 206010044221 Toxic encephalopathy Diseases 0.000 abstract 1
- 208000030886 Traumatic Brain injury Diseases 0.000 abstract 1
- IEDDDPZMBFHSTM-MZNJEOGPSA-N [(7S,9aR)-7-(4-chlorophenyl)-7-hydroxy-3,4,6,8,9,9a-hexahydro-1H-pyrido[1,2-a]pyrazin-2-yl]-[2-chloro-3-(5-fluoro-1H-pyrazol-4-yl)phenyl]methanone Chemical compound C1C[C@@](CN2[C@H]1CN(CC2)C(=O)C3=CC=CC(=C3Cl)C4=C(NN=C4)F)(C5=CC=C(C=C5)Cl)O IEDDDPZMBFHSTM-MZNJEOGPSA-N 0.000 abstract 1
- 125000003545 alkoxy group Chemical group 0.000 abstract 1
- 125000000217 alkyl group Chemical group 0.000 abstract 1
- 206010002026 amyotrophic lateral sclerosis Diseases 0.000 abstract 1
- 230000036506 anxiety Effects 0.000 abstract 1
- 125000003118 aryl group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 125000000000 cycloalkoxy group Chemical group 0.000 abstract 1
- 125000000753 cycloalkyl group Chemical group 0.000 abstract 1
- 206010015037 epilepsy Diseases 0.000 abstract 1
- 229910052736 halogen Inorganic materials 0.000 abstract 1
- 150000002367 halogens Chemical class 0.000 abstract 1
- 150000002391 heterocyclic compounds Chemical class 0.000 abstract 1
- 125000000623 heterocyclic group Chemical group 0.000 abstract 1
- 206010027599 migraine Diseases 0.000 abstract 1
- 201000006417 multiple sclerosis Diseases 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
- 230000007135 neurotoxicity Effects 0.000 abstract 1
- 231100000228 neurotoxicity Toxicity 0.000 abstract 1
- 230000036407 pain Effects 0.000 abstract 1
- 238000011321 prophylaxis Methods 0.000 abstract 1
- 208000020016 psychiatric disease Diseases 0.000 abstract 1
- 230000009529 traumatic brain injury Effects 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
Esta referido a compuestos heterociclicos de formula general (I), en donde: R1 es arilo, heteroarilo, heterociclilo; R2 es alquilo, cicloalquilo, heteroarilo; R3 es H, halogeno, alcoxi, cicloalquiloxi, OH. Entre los compuestos preferidos tenemos los siguientes: [(7S,9aR)-7-(3-cloro-4-fluorofenil)-7-hidroxi-3,4,6,8,9,9a-hexahidro-1Hpirido[1,2-a]pirazin-2-il]-(2-cloro-3-metoxifenil)metanona; [(7S,9aR)-7-(4-clorofenil)-7-hidroxi-3,4,6,8,9,9a-hexahidro-1H-pirido[1,2- a]pirazin-2-il]-[2-cloro-3-(3-fluoro-1H-pirazol-4-il)fenil]metanona; entre otros. Estos compuestos son inhibidores de monoacilglicerol lipasa (MAGL) destinados al tratamiento o la profilaxis de neuroinflamacion, enfermedades neurodegenerativas, dolor, cancer, trastornos mentales, esclerosis multiple, enfermedad de Alzheimer, enfermedad de Parkinson, esclerosis lateral amiotrofica, traumatismo craneoencefalico, neurotoxicidad, apoplejia, epilepsia, ansiedad, jaqueca y/o depresion.
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 |
|---|---|
| PE20220514A1 true PE20220514A1 (es) | 2022-04-07 |
Family
ID=67180549
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2021002264A PE20220514A1 (es) | 2019-07-03 | 2020-06-30 | Inhibidores de monoacilglicerol lipasa (magl) heterociclicos |
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 (8)
| 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 |
| JP7637049B2 (ja) | 2018-08-13 | 2025-02-27 | エフ． ホフマン－ラ ロシュ アーゲー | モノアシルグリセロールリパーゼ阻害剤としての新規の複素環化合物 |
| WO2021000297A1 (en) | 2019-07-03 | 2021-01-07 | Merck Sharp & Dohme Corp. | Compounds and methods of use thereof as antibacterial agents |
| AU2020311584A1 (en) * | 2019-07-09 | 2022-01-20 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| CA3151516A1 (en) | 2019-09-12 | 2021-03-18 | F. Hoffmann-La Roche Ag | 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors |
| AU2021338497A1 (en) | 2020-09-03 | 2023-02-09 | F. Hoffmann-La Roche Ag | Heterocyclic compounds |
| WO2022266162A1 (en) | 2021-06-16 | 2022-12-22 | Celgene Corporation | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
| CA3242372A1 (en) | 2021-12-29 | 2023-07-06 | 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 |
| RU2009136330A (ru) | 2007-03-01 | 2011-04-10 | Янссен Фармацевтика Н.В. (Be) | Тетрагидроизохинолиновые соединения в качестве модуляторов гистаминового н3 рецептора |
| 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 MX MX2022000083A patent/MX2022000083A/es unknown
- 2020-06-30 CN CN202080048854.0A patent/CN114072405A/zh active Pending
- 2020-06-30 MA MA056443A patent/MA56443A/fr unknown
- 2020-06-30 WO PCT/EP2020/068320 patent/WO2021001330A1/en not_active Ceased
- 2020-06-30 KR KR1020227002453A patent/KR20220027991A/ko not_active Withdrawn
- 2020-06-30 JP JP2021577946A patent/JP7669299B2/ja active Active
- 2020-06-30 AU AU2020299965A patent/AU2020299965A1/en not_active Abandoned
- 2020-06-30 CA CA3143280A patent/CA3143280A1/en active Pending
- 2020-06-30 PE PE2021002264A patent/PE20220514A1/es unknown
- 2020-06-30 BR BR112021026820A patent/BR112021026820A2/pt not_active Application Discontinuation
- 2020-06-30 EP EP20734956.4A patent/EP3994137A1/en active Pending
- 2020-06-30 CR CR20210630A patent/CR20210630A/es unknown
- 2020-06-30 PH PH1/2021/553248A patent/PH12021553248A1/en 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 |
|---|---|
| AR119322A1 (es) | 2021-12-09 |
| JP7669299B2 (ja) | 2025-04-28 |
| AU2020299965A1 (en) | 2022-02-03 |
| CR20210630A (es) | 2022-02-11 |
| CL2022000005A1 (es) | 2022-10-21 |
| BR112021026820A2 (pt) | 2022-02-22 |
| TW202116768A (zh) | 2021-05-01 |
| EP3994137A1 (en) | 2022-05-11 |
| CN114072405A (zh) | 2022-02-18 |
| MX2022000083A (es) | 2022-02-03 |
| CO2022000749A2 (es) | 2022-02-07 |
| JP2022540367A (ja) | 2022-09-15 |
| US20220213093A1 (en) | 2022-07-07 |
| WO2021001330A1 (en) | 2021-01-07 |
| PH12021553248A1 (en) | 2023-02-27 |
| IL288936A (en) | 2022-02-01 |
| KR20220027991A (ko) | 2022-03-08 |
| MA56443A (fr) | 2022-05-11 |
| CA3143280A1 (en) | 2021-01-07 |
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