AR117139A1 - Derivados de piridooxazinona como inhibidores de monoacilglicerol ligasa (magl) - Google Patents
Derivados de piridooxazinona como inhibidores de monoacilglicerol ligasa (magl)Info
- Publication number
- AR117139A1 AR117139A1 ARP190103417A ARP190103417A AR117139A1 AR 117139 A1 AR117139 A1 AR 117139A1 AR P190103417 A ARP190103417 A AR P190103417A AR P190103417 A ARP190103417 A AR P190103417A AR 117139 A1 AR117139 A1 AR 117139A1
- Authority
- AR
- Argentina
- Prior art keywords
- alkyl
- halo
- alkoxy
- membered
- compounds
- Prior art date
Links
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
- 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
- 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
- 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
- Chemical & Material Sciences (AREA)
- Organic Chemistry (AREA)
- Health & Medical Sciences (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)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Neurosurgery (AREA)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Epidemiology (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (AREA)
- Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
- Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
- Nitrogen Condensed Heterocyclic Rings (AREA)
- Plural Heterocyclic Compounds (AREA)
Abstract
La presente proporciona compuestos heterocíclicos que tienen la fórmula general (1) en donde A, B, L, X, R¹, R², R³ y R⁴ son como se describen en el presente documento, composiciones que incluyen los compuestos, procesos para fabricar los compuestos y métodos de uso de los compuestos. Reivindicación 1: Un compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en donde: (i) X es C-R⁵; L es un enlace covalente, -(CH₂)ₙ-N(alquilo C₁₋₆)-, -(CH₂)ₙ-NH-, -N(alquil C₁₋₆)-(CH₂)ₚ-, -NH-(CH₂)ₚ-, -(CH₂)ₙ-O-, -O-(CH₂)ₚ-, -SO₂-N(alquilo C₁₋₆)-, -SO₂-NH-, -N(alquil C₁₋₆)-SO₂-, -NH-SO₂-, carbonilo, -(CH₂)ₙ-, -CHR⁶-, -CF₂-(CH₂)ₙ-, -(CH₂)ₚ-CF₂-, -(CH₂)ₙ-S-, -S-(CH₂)ₚ-, -SO₂-, -C(O)-NH-, -C(O)-N(alquilo C₁₋₆)-, -NH-C(O)- o -N(alquil C₁₋₆)-C(O)-; y A es: (i) arilo C₆₋₁₄ sustituido con R⁷, R⁸ y R⁹; o (ii) heteroarilo de 5 - 14 miembros sustituido con R¹⁰, R¹¹ y R¹²; o (ii) X es N; L es un enlace covalente, -(CH₂)ₙ-, -CHR⁶ -, -SO₂-, carbonilo, -N(alquil C₁₋₆)-(CH₂)ₚ-, -NH-(CH₂)ₚ-, -O-(CH₂)ₚ-, -CF₂-CH₂-, -N(alquil C₁₋₆)-SO₂-, -NH-SO₂-, -NH-C(O)- o -N(alquil C₁₋₆)-C(O)-; y A es: (i) arilo C₆₋₁₄ sustituido con R⁷, R⁸ y R⁹; o (ii) heteroarilo de 5 - 14 miembros sustituido con R¹⁰, R¹¹ y R¹²; o (iii) X es N; L es alcoxi C₁₋₆-carbonilo, ariloxicarbonilo C₆₋₁₄ o heteroariloxicarbonilo de 5 - 14 miembros; y A está ausente; B es un espirociclo bicíclico; R¹, R², R³, R⁴ y R⁵ son independientemente hidrógeno, halógeno, hidroxi, alquilo C₁₋₆ o halo-alquilo C₁₋₆; R⁶ es arilo C₆₋₁₄ o heteroarilo de 5 - 14 miembros; R⁷, R⁸, R⁹, R¹⁰, R¹¹ y R¹² son en cada aparición independientemente hidrógeno, hidroxi, alquilo C₁₋₆, halo-alquilo C₁₋₆, halógeno, alcoxi C₁₋₆, halo-alcoxi C₁₋₆, SF₅, alquil C₁₋₆sulfonilo, ciano o un grupo de fórmula (2); C es heteroarilo de 5 - 14 miembros, heterociclilo de 3 - 14 miembros o cicloalquilo C₃₋₁₀; RC¹, RC² y RC³ son cada uno independientemente hidrógeno, alquilo C₁₋₆, halo-alquilo C₁₋₆, oxo, halógeno, hidroxi, alcoxi C₁₋₆ o halo-alcoxi C₁₋₆; cada aparición de n es independientemente 0, 1, 2 ó 3; cada aparición de p es independientemente 1, 2 ó 3; y q es 0, 1 ó 2.
Applications Claiming Priority (1)
| Application Number | Priority Date | Filing Date | Title |
|---|---|---|---|
| EP18207725 | 2018-11-22 |
Publications (1)
| Publication Number | Publication Date |
|---|---|
| AR117139A1 true AR117139A1 (es) | 2021-07-14 |
Family
ID=64453331
Family Applications (1)
| Application Number | Title | Priority Date | Filing Date |
|---|---|---|---|
| ARP190103417A AR117139A1 (es) | 2018-11-22 | 2019-11-21 | Derivados de piridooxazinona como inhibidores de monoacilglicerol ligasa (magl) |
Country Status (30)
| Country | Link |
|---|---|
| US (1) | US20210387999A1 (es) |
| EP (1) | EP3883936B1 (es) |
| JP (1) | JP7444882B2 (es) |
| CN (1) | CN113166170A (es) |
| AR (1) | AR117139A1 (es) |
| AU (1) | AU2019383500B2 (es) |
| BR (1) | BR112021009348A2 (es) |
| CA (1) | CA3119506A1 (es) |
| CL (1) | CL2021001330A1 (es) |
| CO (1) | CO2021007056A2 (es) |
| CR (1) | CR20210247A (es) |
| DK (1) | DK3883936T3 (es) |
| ES (1) | ES2955037T3 (es) |
| FI (1) | FI3883936T3 (es) |
| HR (1) | HRP20231083T1 (es) |
| HU (1) | HUE062913T2 (es) |
| IL (1) | IL283333B2 (es) |
| LT (1) | LT3883936T (es) |
| MA (1) | MA55131B1 (es) |
| MX (1) | MX2021005714A (es) |
| PE (1) | PE20211870A1 (es) |
| PH (1) | PH12021551167A1 (es) |
| PL (1) | PL3883936T3 (es) |
| PT (1) | PT3883936T (es) |
| RS (1) | RS64579B1 (es) |
| SG (1) | SG11202104206SA (es) |
| SI (1) | SI3883936T1 (es) |
| TW (1) | TWI825227B (es) |
| UA (1) | UA128505C2 (es) |
| WO (1) | WO2020104494A1 (es) |
Families Citing this family (22)
| 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 |
| EP3737680A1 (en) | 2018-01-08 | 2020-11-18 | F. Hoffmann-La Roche AG | Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors |
| RS65912B1 (sr) | 2018-08-13 | 2024-10-31 | Hoffmann La Roche | Nova heterociklična jedinjenja kao inhibitori monoacilglicerol lipaze |
| US20210094971A1 (en) * | 2019-09-09 | 2021-04-01 | Hoffmann-La Roche Inc. | Heterocyclic compounds |
| JP7609854B2 (ja) | 2019-09-12 | 2025-01-07 | エフ． ホフマン－ラ ロシュ アーゲー | Ｍａｇｌ阻害剤としての４，４ａ，５，７，８，８ａ－ヘキサピリド［４，３－ｂ］［１，４］オキサジン－３－オン化合物 |
| CN115989228A (zh) | 2020-09-03 | 2023-04-18 | 豪夫迈·罗氏有限公司 | 杂环化合物 |
| US20240101552A1 (en) * | 2020-09-18 | 2024-03-28 | Shanghai Pharmaceuticals Holding Co., Ltd. | Carbonyl heterocyclic compound and application thereof |
| PE20240050A1 (es) | 2021-01-29 | 2024-01-09 | Cedilla Therapeutics Inc | Inhibidores de cdk2 y metodos de uso de los mismos |
| EP4358954A4 (en) | 2021-06-26 | 2025-09-03 | Cedilla Therapeutics Inc | CDK2 INHIBITORS AND METHODS OF USE THEREOF |
| US20250170100A1 (en) * | 2021-12-29 | 2025-05-29 | Psy Therapeutics, Inc. | Monoacylglycerol lipase inhibitors and use thereof for the treatment of anxiety and related conditions |
| WO2023130023A1 (en) | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Inhibiting monoacylglycerol lipase (magl) |
| WO2023130050A1 (en) * | 2021-12-29 | 2023-07-06 | Psy Therapeutics, Inc. | Monoacylglycerol lipase inhibitors and use thereof for the treatment and management of pain |
| JP2025504522A (ja) * | 2022-01-25 | 2025-02-12 | エフ． ホフマン－ラ ロシュ アーゲー | 新規の複素環式化合物 |
| WO2023247670A1 (en) * | 2022-06-24 | 2023-12-28 | F. Hoffmann-La Roche Ag | New heterocyclic-carbonyl-cyclic compounds as magl inhibitors |
| EP4568972A1 (en) | 2022-08-08 | 2025-06-18 | F. Hoffmann-La Roche AG | New heterocyclic compounds |
| CA3261797A1 (en) * | 2022-08-11 | 2024-02-15 | Remynd N.V. | (AZA)SPIROHEPTANE DERIVATIVES FOR THE TREATMENT OF NEURODEGENERATIVE DISORDERS |
| CN119894887A (zh) * | 2022-09-20 | 2025-04-25 | 豪夫迈·罗氏有限公司 | 用于magl的荧光探针 |
| AR130836A1 (es) * | 2022-10-24 | 2025-01-22 | Hoffmann La Roche | Nuevos compuestos heterocíclicos |
| EP4665718A1 (en) | 2023-02-13 | 2025-12-24 | Apogee Pharmaceuticals, Inc. | Small molecules as monoacylglycerol lipase (magl) inhibitors, compositions and use thereof |
| WO2025068347A1 (en) | 2023-09-28 | 2025-04-03 | F. Hoffmann-La Roche Ag | New heterocyclic compounds |
| WO2025153656A1 (en) | 2024-01-19 | 2025-07-24 | F. Hoffmann-La Roche Ag | Heterocyclic inhibitors of monoacylglycerol lipase (magl) |
Family Cites Families (8)
| Publication number | Priority date | Publication date | Assignee | Title |
|---|---|---|---|---|
| US7579495B2 (en) | 2003-12-19 | 2009-08-25 | Momentive Performance Materials Inc. | Active-releasing cyclic siloxanes |
| CN102596962A (zh) | 2009-09-10 | 2012-07-18 | 弗·哈夫曼-拉罗切有限公司 | Jak抑制剂 |
| WO2011059118A1 (ko) | 2009-11-10 | 2011-05-19 | Kim Hyun Jeen | 후각인지능력 검사 시스템 |
| WO2016158956A1 (ja) * | 2015-03-30 | 2016-10-06 | 武田薬品工業株式会社 | 複素環化合物 |
| CA2986199C (en) | 2015-05-21 | 2023-07-18 | Glaxosmithkline Intellectual Property Development Limited | Benzoimidazole derivatives as pad4 inhibitors |
| TN2017000544A1 (en) | 2015-07-31 | 2019-04-12 | Pfizer | 1,1,1-trifluoro-3-hydroxypropan-2-yl carbamate derivatives and 1,1,1-trifluoro-4-hydroxybutan-2-yl carbamate derivatives as magl inhibitors |
| WO2017087858A1 (en) * | 2015-11-20 | 2017-05-26 | Abide Therapeutics, Inc. | Pyrazole compounds and methods of making and using same |
| WO2021048241A1 (en) * | 2019-09-12 | 2021-03-18 | F. Hoffmann-La Roche Ag | Radiolabeled compounds |
-
2019
- 2019-11-20 PL PL19809026.8T patent/PL3883936T3/pl unknown
- 2019-11-20 BR BR112021009348-6A patent/BR112021009348A2/pt unknown
- 2019-11-20 PT PT198090268T patent/PT3883936T/pt unknown
- 2019-11-20 CN CN201980077284.5A patent/CN113166170A/zh active Pending
- 2019-11-20 AU AU2019383500A patent/AU2019383500B2/en active Active
- 2019-11-20 RS RS20230788A patent/RS64579B1/sr unknown
- 2019-11-20 HR HRP20231083TT patent/HRP20231083T1/hr unknown
- 2019-11-20 SI SI201930619T patent/SI3883936T1/sl unknown
- 2019-11-20 MA MA55131A patent/MA55131B1/fr unknown
- 2019-11-20 HU HUE19809026A patent/HUE062913T2/hu unknown
- 2019-11-20 DK DK19809026.8T patent/DK3883936T3/da active
- 2019-11-20 LT LTEPPCT/EP2019/081870T patent/LT3883936T/lt unknown
- 2019-11-20 ES ES19809026T patent/ES2955037T3/es active Active
- 2019-11-20 PE PE2021000714A patent/PE20211870A1/es unknown
- 2019-11-20 MX MX2021005714A patent/MX2021005714A/es unknown
- 2019-11-20 IL IL283333A patent/IL283333B2/en unknown
- 2019-11-20 FI FIEP19809026.8T patent/FI3883936T3/fi active
- 2019-11-20 EP EP19809026.8A patent/EP3883936B1/en active Active
- 2019-11-20 CA CA3119506A patent/CA3119506A1/en active Pending
- 2019-11-20 WO PCT/EP2019/081870 patent/WO2020104494A1/en not_active Ceased
- 2019-11-20 CR CR20210247A patent/CR20210247A/es unknown
- 2019-11-20 SG SG11202104206SA patent/SG11202104206SA/en unknown
- 2019-11-20 JP JP2021528972A patent/JP7444882B2/ja active Active
- 2019-11-20 UA UAA202103201A patent/UA128505C2/uk unknown
- 2019-11-21 TW TW108142267A patent/TWI825227B/zh active
- 2019-11-21 AR ARP190103417A patent/AR117139A1/es unknown
-
2021
- 2021-05-20 US US17/325,934 patent/US20210387999A1/en active Pending
- 2021-05-20 CL CL2021001330A patent/CL2021001330A1/es unknown
- 2021-05-21 PH PH12021551167A patent/PH12021551167A1/en unknown
- 2021-05-28 CO CONC2021/0007056A patent/CO2021007056A2/es unknown
Also Published As
Similar Documents
| Publication | Publication Date | Title |
|---|---|---|
| AR117139A1 (es) | Derivados de piridooxazinona como inhibidores de monoacilglicerol ligasa (magl) | |
| AR120338A1 (es) | Piridazinonas como inhibidores de parp7 | |
| AR099228A1 (es) | Inhibidores macrocíclicos de fxia que tienen grupos heterocíclicos | |
| AR091981A1 (es) | Dihidropiridona p1 como inhibidores del factor xia | |
| AR119943A1 (es) | Compuestos heterocíclicos | |
| AR127309A2 (es) | Derivados de piridazinona | |
| AR107714A1 (es) | Derivados de pirazolo[1,5-a]pirazin-4-ilo | |
| AR113299A1 (es) | Compuestos de isoindolina | |
| AR099367A1 (es) | Inhibidores de la tirosina quinasa de bruton | |
| AR088423A1 (es) | Ligadores p1 ciclicos como inhibidores del factor xia | |
| AR098872A1 (es) | Moduladores de tetrahidropiridopirazinas de gpr6 | |
| AR110405A1 (es) | Compuestos | |
| AR106945A2 (es) | Compuestos de isoindolina y composiciones farmacéuticas de los mismos | |
| AR113929A1 (es) | Compuestos heterocíclicos | |
| AR100807A1 (es) | Inhibidores de fosfatidilinositol 3-quinasa | |
| AR088828A1 (es) | DERIVADOS DE CICLOHEXILAMINA QUE TIENEN ACTIVIDAD COMO AGONISTAS ADRENERGICOS b2 Y COMO ANTAGONISTAS MUSCARINICOS M3 | |
| AR107321A1 (es) | Compuestos antiproliferativos, y sus composiciones farmacéuticas y usos | |
| AR106865A1 (es) | Piridinas sustituidas y métodos de uso | |
| AR088810A1 (es) | Moduladores del receptor mas acoplado a la proteina g utiles en el tratamiento de trastornos cardiovasculares y composiciones farmaceuticas que los contienen | |
| AR094496A1 (es) | Compuestos tetracíclicos sustituidos con heterociclo y métodos de uso de los mismos para el tratamiento de enfermedades víricas | |
| AR100418A1 (es) | Compuestos y composiciones para inducir condrogénesis | |
| AR110498A1 (es) | DERIVADOS DE ISOXAZOLIL ÉTER COMO MODULADORES ALOSTÉRICOS POSITIVOS (PAM) DE RECEPTORES DE GABAA a5 | |
| AR059621A1 (es) | Acidos 4- fenil- tiazol-5- carboxilicos y amidas de acidos 4- fenil- tiazol5 carboxilicos como inhibidores de la plk1 | |
| AR108610A1 (es) | Derivados de imidazolona inhibidores de la elastasa de neutrófilos humana | |
| AR120649A1 (es) | Antagonistas del receptor de crf y métodos de uso |