PE20220904A1 - 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
- PE20220904A1 PE20220904A1 PE2022000300A PE2022000300A PE20220904A1 PE 20220904 A1 PE20220904 A1 PE 20220904A1 PE 2022000300 A PE2022000300 A PE 2022000300A PE 2022000300 A PE2022000300 A PE 2022000300A PE 20220904 A1 PE20220904 A1 PE 20220904A1
- Authority
- PE
- Peru
- Prior art keywords
- alkyl
- halo
- hydrogen
- compounds
- halogen
- Prior art date
Links
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)
- Animal Behavior & Ethology (AREA)
- Life Sciences & Earth Sciences (AREA)
- Pharmacology & Pharmacy (AREA)
- General Chemical & Material Sciences (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (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
La invencion proporciona nuevos compuestos heterociclicos que tienen la Formula general (I) donde; X es N o C-R5; L se selecciona de una union 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 biciclico en puente; R1 es hidrogeno o C1-6-alquilo; R2 es hidrogeno o C1-6-alquilo; R3 es hidrogeno, C1-6-alquilo, halo-C1-6-alquilo, halogeno o hidroxi; R4 es hidrogeno, C1-6-alquilo, halo-C1-6-alquilo, halogeno o hidroxi; R5 es hidrogeno, C1-6-alquilo, halo-C1-6-alquilo, halogeno o hidroxi; y R6, R7, R8, R9, R10 y R11 se seleccionan independientemente de hidrogeno, C1-6-alquilo, halo-C1-6-alquilo, halogeno, 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 halogeno, ciano, SF5 C1-6-alquilo, C1-6-alcoxi, halo-C1-6-alquilo y halo-C1- 6-alcoxi. La presente invencion define composiciones que incluyen los compuestos, procesos para fabricar los compuestos y metodos para usar los compuestos como inhibidores de monoacilglicerol lipasa (MAGL).
Applications Claiming Priority (2)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP19196089 | 2019-09-09 | ||
| PCT/EP2020/074897 WO2021048036A1 (en) | 2019-09-09 | 2020-09-07 | 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 |
|---|---|
| PE20220904A1 true PE20220904A1 (es) | 2022-05-30 |
Family
ID=67902336
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| PE2022000300A PE20220904A1 (es) | 2019-09-09 | 2020-09-07 | 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 (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) |
| 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 |
| EP3717477B1 (en) | 2017-11-28 | 2022-07-20 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
| CN111566105A (zh) | 2018-01-08 | 2020-08-21 | 豪夫迈·罗氏有限公司 | 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物 |
| CA3104928A1 (en) | 2018-08-13 | 2020-02-20 | F. Hoffmann-La Roche Ag | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| CR20220104A (es) | 2019-09-12 | 2022-04-20 | Hoffmann La Roche | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl |
| JP2023539690A (ja) | 2020-09-03 | 2023-09-15 | エフ． ホフマン－ラ ロシュ アーゲー | 複素環式化合物 |
| WO2024071398A1 (ja) * | 2022-09-30 | 2024-04-04 | 小野薬品工業株式会社 | Ａｂｈｄ６アンタゴニスト |
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 |
| WO2016185279A1 (en) | 2015-05-21 | 2016-11-24 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as pad4 inhibitors |
| US10323038B2 (en) * | 2015-11-20 | 2019-06-18 | 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 |
| CN111566105A (zh) * | 2018-01-08 | 2020-08-21 | 豪夫迈·罗氏有限公司 | 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物 |
| DK3768684T3 (da) * | 2018-03-22 | 2023-04-24 | Hoffmann La Roche | Oxazin-monoacylglycerol-lipase (MAGL)-hæmmere |
| CA3104928A1 (en) * | 2018-08-13 | 2020-02-20 | F. Hoffmann-La Roche Ag | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| SG11202012222TA (en) * | 2018-08-13 | 2021-01-28 | Hoffmann La Roche | New heterocyclic compounds as monoacylglycerol lipase inhibitors |
| PL3883936T3 (pl) * | 2018-11-22 | 2023-11-20 | F. Hoffmann-La Roche Ag | Nowe związki heterocykliczne |
-
2020
- 2020-09-04 US US17/012,589 patent/US20210094971A1/en not_active Abandoned
- 2020-09-07 CN CN202080062559.0A patent/CN114364682A/zh active Pending
- 2020-09-07 CR CR20220091A patent/CR20220091A/es unknown
- 2020-09-07 PE PE2022000300A patent/PE20220904A1/es unknown
- 2020-09-07 AU AU2020344921A patent/AU2020344921A1/en active Pending
- 2020-09-07 AR ARP200102489A patent/AR119910A1/es unknown
- 2020-09-07 EP EP20772007.9A patent/EP4028401B1/en active Active
- 2020-09-07 WO PCT/EP2020/074897 patent/WO2021048036A1/en active Application Filing
- 2020-09-07 MX MX2022002554A patent/MX2022002554A/es unknown
- 2020-09-07 JP JP2022515504A patent/JP2022546853A/ja active Pending
- 2020-09-07 KR KR1020227007722A patent/KR20220061119A/ko unknown
- 2020-09-07 CA CA3151218A patent/CA3151218A1/en active Pending
- 2020-09-07 BR BR112022003704A patent/BR112022003704A2/pt 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 |
|---|---|
| WO2021048036A1 (en) | 2021-03-18 |
| EP4028401C0 (en) | 2023-11-22 |
| MX2022002554A (es) | 2022-03-22 |
| CO2022002339A2 (es) | 2022-03-08 |
| AU2020344921A1 (en) | 2022-02-17 |
| KR20220061119A (ko) | 2022-05-12 |
| JP2022546853A (ja) | 2022-11-09 |
| TW202124392A (zh) | 2021-07-01 |
| CL2022000551A1 (es) | 2022-11-18 |
| EP4028401A1 (en) | 2022-07-20 |
| BR112022003704A2 (pt) | 2022-05-24 |
| AR119910A1 (es) | 2022-01-19 |
| CA3151218A1 (en) | 2021-03-18 |
| CR20220091A (es) | 2022-04-01 |
| US20220275005A1 (en) | 2022-09-01 |
| IL289233A (en) | 2022-02-01 |
| US20210094971A1 (en) | 2021-04-01 |
| EP4028401B1 (en) | 2023-11-22 |
| CN114364682A (zh) | 2022-04-15 |
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| PE20220904A1 (es) | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl | |
| CO2021002382A2 (es) | Nuevos compuestos heterocíclicos como inhibidores de la monoacilglicerol lipasa | |
| CO2020009567A2 (es) | Inhibidores de monoacilglicerol lipasa (magl) de oxazina | |
| PE20211779A1 (es) | COMPUESTOS DE PIRAZOLO[3,4-b]PIRIDINA COMO INHIBIDORES DE CINASAS TAM Y MET | |
| CL2021001330A1 (es) | Nuevos compuestos heterocíclicos | |
| AR113748A1 (es) | Proceso estereoselectivo para preparar derivados de piridona policíclicos sustituidos | |
| PE20030808A1 (es) | Derivados triciclicos heterociclicos como antagonistas receptores de trombina | |
| NO20065619L (no) | Pyrrolidin-2-on- og piperidin-2-onderivat som 11-beta-hydroksysteroid-dehydrogenaseinhibitorer | |
| CL2022000556A1 (es) | Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl | |
| PE20140961A1 (es) | Inhibidores macrociclicos de serina proteasas de hepatitis c | |
| CO2017003132A2 (es) | Inhibidores de la aldosterona sintasa derivados de la 2,6-diazaspiro[3.3]heptán-6-il]-3-piridil]isoindolín-1-ona o 2,7-diazaspiro[3.5]nonán-2-il]-3-piridil]isoindolín-1-ona | |
| ECSP099781A (es) | Novedosos compuestos que son inhibidores de erk | |
| ES2308299T3 (es) | Tiadiazoles como ligandos de receptores de cxc-y cc-quimioquinas. | |
| PE20040373A1 (es) | Composiciones herbicidas que comprenden derivados de isoxazolina | |
| ES2248114T3 (es) | Derivados de sulfonamida farmaceuticamente activos. | |
| PE20151781A1 (es) | Piridonamidas como moduladores de canales de sodio | |
| ECSP088550A (es) | Nuevos compuestos que son inhibidores de erk | |
| AR072726A1 (es) | Derivados de indol macrociclicos utiles como inhibidores del virus de la hepatitis c | |
| AR049443A1 (es) | Derivados de pirrolpiridinas | |
| AR058124A1 (es) | Derivados de ftalazinona como inhibidores de parp-1 | |
| CO6150144A2 (es) | Inhibidores de proteina tirosina fosfatasa humana y metodos de uso | |
| PE20170323A1 (es) | Derivados de indano e indolina y el uso de los mismos como activadores de la guanilato ciclasa soluble | |
| CO6160326A2 (es) | Derivados de pirrolidin-2-ona como moduladores del receptor de androgeno | |
| CO6220935A2 (es) | Derivados de 1,2,4-triazol como moduladores de mglur5 | |
| CO5690598A2 (es) | 6-[(sustituido)fenil]triazolopirimidinas como agentes anticancer |