AR119910A1 - DERIVADOS DE 4,4a,5,7,8,8a-HEXAHIDROPIRIDO[4,3-b][1,4]OXAZIN-3-ONA COMO INHIBIDORES DE MAGL - Google Patents
DERIVADOS DE 4,4a,5,7,8,8a-HEXAHIDROPIRIDO[4,3-b][1,4]OXAZIN-3-ONA COMO INHIBIDORES DE MAGLInfo
- Publication number
- AR119910A1 AR119910A1 ARP200102489A ARP200102489A AR119910A1 AR 119910 A1 AR119910 A1 AR 119910A1 AR P200102489 A ARP200102489 A AR P200102489A AR P200102489 A ARP200102489 A AR P200102489A AR 119910 A1 AR119910 A1 AR 119910A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- hydrogen
- halogen
- alkoxy
- Prior art date
Links
- 102100029814 Monoglyceride lipase Human genes 0.000 title abstract 2
- 101710116393 Monoglyceride lipase Proteins 0.000 title abstract 2
- 239000003112 inhibitor Substances 0.000 title abstract 2
- CPDAYCDBCSPKNF-UHFFFAOYSA-N 4a,5,6,7,8,8a-hexahydro-4h-pyrido[4,3-b][1,4]oxazin-3-one Chemical class C1CNCC2NC(=O)COC21 CPDAYCDBCSPKNF-UHFFFAOYSA-N 0.000 title 1
- 125000004169 (C1-C6) alkyl group Chemical group 0.000 abstract 11
- 229910052739 hydrogen Inorganic materials 0.000 abstract 6
- 239000001257 hydrogen Substances 0.000 abstract 6
- 125000004435 hydrogen atom Chemical group [H]* 0.000 abstract 6
- 229910052736 halogen Inorganic materials 0.000 abstract 5
- 150000002367 halogens Chemical class 0.000 abstract 5
- 125000006708 (C5-C14) heteroaryl group Chemical group 0.000 abstract 3
- 125000005915 C6-C14 aryl group Chemical group 0.000 abstract 3
- 125000002887 hydroxy group Chemical group [H]O* 0.000 abstract 3
- 125000004191 (C1-C6) alkoxy group Chemical group 0.000 abstract 2
- 125000006376 (C3-C10) cycloalkyl group Chemical group 0.000 abstract 2
- 150000001875 compounds Chemical class 0.000 abstract 2
- 125000004093 cyano group Chemical group *C#N 0.000 abstract 2
- HCMJWOGOISXSDL-UHFFFAOYSA-N (2-isothiocyanato-1-phenylethyl)benzene Chemical compound C=1C=CC=CC=1C(CN=C=S)C1=CC=CC=C1 HCMJWOGOISXSDL-UHFFFAOYSA-N 0.000 abstract 1
- 125000004739 (C1-C6) alkylsulfonyl group Chemical group 0.000 abstract 1
- 206010028980 Neoplasm Diseases 0.000 abstract 1
- 208000002193 Pain Diseases 0.000 abstract 1
- 125000002618 bicyclic heterocycle group Chemical group 0.000 abstract 1
- 201000011510 cancer Diseases 0.000 abstract 1
- 208000015114 central nervous system disease Diseases 0.000 abstract 1
- 208000037265 diseases, disorders, signs and symptoms Diseases 0.000 abstract 1
- 208000035475 disorder Diseases 0.000 abstract 1
- 238000004519 manufacturing process Methods 0.000 abstract 1
- 238000000034 method Methods 0.000 abstract 1
- 208000015122 neurodegenerative disease Diseases 0.000 abstract 1
- 239000008194 pharmaceutical composition Substances 0.000 abstract 1
- -1 pyridin-[1,4]oxazin-3-one Chemical compound 0.000 abstract 1
- 150000003839 salts Chemical class 0.000 abstract 1
- 125000001424 substituent group Chemical group 0.000 abstract 1
Classifications
-
- 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
-
- 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
- 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
- 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
- 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
- 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
Landscapes
- Health & Medical Sciences (AREA)
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- General Health & Medical Sciences (AREA)
- Veterinary Medicine (AREA)
- Public Health (AREA)
- Medicinal Chemistry (AREA)
- Pharmacology & Pharmacy (AREA)
- Life Sciences & Earth Sciences (AREA)
- Animal Behavior & Ethology (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- General Chemical & Material Sciences (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Biomedical Technology (AREA)
- Rheumatology (AREA)
- Pain & Pain Management (AREA)
- Hospice & Palliative Care (AREA)
- Psychiatry (AREA)
- Epidemiology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
Abstract
Compuestos derivados de piridin-[1,4]oxazin-3-ona como inhibidores de MAGL, composición farmacéutica que los comprende, un proceso para su fabricación y su uso para el tratamiento de enfermedades del SNC, enfermedades degenerativas, dolor y cáncer entre otros tipos de trastornos. Reivindicación 1: Un compuesto de la fórmula (1) o una sal de este aceptable desde el punto de vista farmacéutico, en donde: X es N o C-R⁵; L se selecciona de una unión covalente, -(CH₂)ₙ-O-, -O-(CH₂)ₚ-, y -SO₂-; n es un entero seleccionado de 0, 1, 2 y 3; p es un entero seleccionado de 1, 2 y 3; A es: (i) C₆₋₁₄-arilo sustituido con R⁶, R⁷ y R⁸; o (ii) heteroarilo de 5 - 14 miembros sustituido con R⁹, R¹⁰ y R¹¹; o B es un heterociclo bicíclico en puente; R¹ es hidrógeno o C₁₋₆-alquilo; R² es hidrógeno o C₁₋₆-alquilo; R³ es hidrógeno, C₁₋₆-alquilo, halo-C₁₋₆-alquilo, halógeno o hidroxi; R⁴ es hidrógeno, C₁₋₆-alquilo, halo-C₁₋₆-alquilo, halógeno o hidroxi; R⁵ es hidrógeno, C₁₋₆-alquilo, halo-C₁₋₆-alquilo, halógeno o hidroxi; y R⁶, R⁷, R⁸, R⁹, R¹⁰ y R¹¹ se seleccionan independientemente de hidrógeno, C₁₋₆-alquilo, halo-C₁₋₆-alquilo, halógeno, C₁₋₆-alcoxi, halo-C₁₋₆-alcoxi, SF₅, C₁₋₆-alquilsulfonilo, ciano, C₃₋₁₀-cicloalquilo, C₆₋₁₄-arilo y heteroarilo de 5 - 14 miembros, en donde dicho C₃₋₁₀-cicloalquilo, C₆₋₁₄-arilo y heteroarilo de 5 - 14 miembros se sustituyen opcionalmente con 1 - 2 sustituyentes seleccionados de halógeno, ciano, SF₅ C₁₋₆-alquilo, C₁₋₆- alcoxi, halo-C₁₋₆-alquilo y halo-C₁₋₆-alcoxi.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19196089 | 2019-09-09 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR119910A1 true AR119910A1 (es) | 2022-01-19 |
Family
ID=67902336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP200102489A AR119910A1 (es) | 2019-09-09 | 2020-09-07 | DERIVADOS DE 4,4a,5,7,8,8a-HEXAHIDROPIRIDO[4,3-b][1,4]OXAZIN-3-ONA COMO INHIBIDORES DE MAGL |
Country Status (18)
| Country | Link |
|---|---|
| US (2) | US20210094971A1 (es) |
| EP (1) | EP4028401B1 (es) |
| JP (1) | JP2022546853A (es) |
| KR (1) | KR20220061119A (es) |
| CN (1) | CN114364682A (es) |
| AR (1) | AR119910A1 (es) |
| AU (1) | AU2020344921A1 (es) |
| BR (1) | BR112022003704A2 (es) |
| CA (1) | CA3151218A1 (es) |
| CL (1) | CL2022000551A1 (es) |
| CO (1) | CO2022002339A2 (es) |
| CR (1) | CR20220091A (es) |
| IL (1) | IL289233A (es) |
| MX (1) | MX2022002554A (es) |
| PE (1) | PE20220904A1 (es) |
| PH (1) | PH12022550321A1 (es) |
| TW (1) | TW202124392A (es) |
| WO (1) | WO2021048036A1 (es) |
Families Citing this family (7)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| AR114136A1 (es) | 2017-10-10 | 2020-07-29 | Hoffmann La Roche | Compuestos heterocíclicos |
| CN111386269A (zh) | 2017-11-28 | 2020-07-07 | 豪夫迈·罗氏有限公司 | 新型杂环化合物 |
| WO2019134985A1 (en) | 2018-01-08 | 2019-07-11 | F. Hoffmann-La Roche Ag | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| PT3837263T (pt) | 2018-08-13 | 2024-08-30 | Hoffmann La Roche | Novos compostos heterocíclicos enquanto inibidores da monoacilglicerol lípase |
| KR20220062515A (ko) | 2019-09-12 | 2022-05-17 | 에프. 호프만-라 로슈 아게 | Magl 억제제로서 4,4a,5,7,8,8a-헥사피리도[4,3-b][1,4]옥사진-3-온 화합물 |
| EP4208456A1 (en) | 2020-09-03 | 2023-07-12 | F. Hoffmann-La Roche AG | Heterocyclic compounds |
| TW202421635A (zh) * | 2022-09-30 | 2024-06-01 | 日商小野藥品工業股份有限公司 | Abhd6拮抗劑 |
Family Cites Families (11)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7579495B2 (en) | 2003-12-19 | 2009-08-25 | Momentive Performance Materials Inc. | Active-releasing cyclic siloxanes |
| WO2011059118A1 (ko) | 2009-11-10 | 2011-05-19 | Kim Hyun Jeen | 후각인지능력 검사 시스템 |
| KR20180005250A (ko) | 2015-05-21 | 2018-01-15 | 글락소스미스클라인 인털렉츄얼 프로퍼티 디벨로프먼트 리미티드 | Pad4 억제제로서의 벤조이미다졸 유도체 |
| WO2017087863A1 (en) * | 2015-11-20 | 2017-05-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| US10385057B2 (en) * | 2015-11-20 | 2019-08-20 | Lundbeck La Jolla Research Center, Inc. | Pyrazole compounds and methods of making and using same |
| 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 |
| HUE061584T2 (hu) * | 2018-03-22 | 2023-07-28 | Hoffmann La Roche | Oxazin-monoacil-glicerol-lipáz (MAGL) gátlók |
| MX2020013719A (es) * | 2018-08-13 | 2021-03-02 | Hoffmann La Roche | Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa. |
| PT3837263T (pt) * | 2018-08-13 | 2024-08-30 | Hoffmann La Roche | Novos compostos heterocíclicos enquanto inibidores da monoacilglicerol lípase |
| SI3883936T1 (sl) * | 2018-11-22 | 2023-10-30 | F. Hoffmann - La Roche Ag | Nove heterociklične spojine |
-
2020
- 2020-09-04 US US17/012,589 patent/US20210094971A1/en not_active Abandoned
- 2020-09-07 WO PCT/EP2020/074897 patent/WO2021048036A1/en active Application Filing
- 2020-09-07 CN CN202080062559.0A patent/CN114364682A/zh active Pending
- 2020-09-07 KR KR1020227007722A patent/KR20220061119A/ko unknown
- 2020-09-07 AR ARP200102489A patent/AR119910A1/es not_active Application Discontinuation
- 2020-09-07 AU AU2020344921A patent/AU2020344921A1/en not_active Abandoned
- 2020-09-07 MX MX2022002554A patent/MX2022002554A/es unknown
- 2020-09-07 JP JP2022515504A patent/JP2022546853A/ja active Pending
- 2020-09-07 CR CR20220091A patent/CR20220091A/es unknown
- 2020-09-07 PH PH1/2022/550321A patent/PH12022550321A1/en unknown
- 2020-09-07 BR BR112022003704A patent/BR112022003704A2/pt unknown
- 2020-09-07 EP EP20772007.9A patent/EP4028401B1/en active Active
- 2020-09-07 CA CA3151218A patent/CA3151218A1/en active Pending
- 2020-09-07 PE PE2022000300A patent/PE20220904A1/es unknown
- 2020-09-08 TW TW109130703A patent/TW202124392A/zh unknown
-
2021
- 2021-12-21 IL IL289233A patent/IL289233A/en unknown
-
2022
- 2022-02-28 CO CONC2022/0002339A patent/CO2022002339A2/es unknown
- 2022-03-04 CL CL2022000551A patent/CL2022000551A1/es unknown
- 2022-05-05 US US17/737,656 patent/US20220275005A1/en not_active Abandoned
Also Published As
| Publication number | Publication date |
|---|---|
| CN114364682A (zh) | 2022-04-15 |
| EP4028401B1 (en) | 2023-11-22 |
| CR20220091A (es) | 2022-04-01 |
| IL289233A (en) | 2022-02-01 |
| CL2022000551A1 (es) | 2022-11-18 |
| KR20220061119A (ko) | 2022-05-12 |
| MX2022002554A (es) | 2022-03-22 |
| US20220275005A1 (en) | 2022-09-01 |
| JP2022546853A (ja) | 2022-11-09 |
| WO2021048036A1 (en) | 2021-03-18 |
| AU2020344921A1 (en) | 2022-02-17 |
| CO2022002339A2 (es) | 2022-03-08 |
| BR112022003704A2 (pt) | 2022-05-24 |
| TW202124392A (zh) | 2021-07-01 |
| CA3151218A1 (en) | 2021-03-18 |
| PE20220904A1 (es) | 2022-05-30 |
| EP4028401A1 (en) | 2022-07-20 |
| US20210094971A1 (en) | 2021-04-01 |
| PH12022550321A1 (en) | 2023-02-13 |
| EP4028401C0 (en) | 2023-11-22 |
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Legal Events
| Date | Code | Title | Description |
|---|---|---|---|
| FA | Abandonment or withdrawal |