AR119322A1 - Compuestos derivados de 1h-pirido[1,2-a]pirazina como inhibidores de magl - Google Patents
Compuestos derivados de 1h-pirido[1,2-a]pirazina como inhibidores de maglInfo
- Publication number
- AR119322A1 AR119322A1 ARP200101858A ARP200101858A AR119322A1 AR 119322 A1 AR119322 A1 AR 119322A1 AR P200101858 A ARP200101858 A AR P200101858A AR P200101858 A ARP200101858 A AR P200101858A AR 119322 A1 AR119322 A1 AR 119322A1
- Authority
- AR
- Argentina
- Prior art keywords
- halogen
- group
- alkyl
- optionally substituted
- substituents independently
- Prior art date
Links
Classifications
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- 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
- A61K9/48—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
-
- 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
-
- 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
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)
- General Chemical & Material Sciences (AREA)
- Chemical Kinetics & Catalysis (AREA)
- Engineering & Computer Science (AREA)
- Bioinformatics & Cheminformatics (AREA)
- Biomedical Technology (AREA)
- Neurology (AREA)
- Neurosurgery (AREA)
- Epidemiology (AREA)
- Psychiatry (AREA)
- Hospice & Palliative Care (AREA)
- Pain & Pain Management (AREA)
- Rheumatology (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
Derivados de pirido-pirazina como inhibidores de monoacilglicerol lipasa (MAGL), composiciones farmacéuticas que los comprenden y la utilización de los mismos para el tratamiento o profilaxis de neuroinflamación, enfermedades neurodegenerativas, dolor, cáncer y trastornos mentales. Reivindicación 1: Compuesto de fórmula (1) o una sal farmacéuticamente aceptable del mismo, en el que: R¹ se selecciona del grupo que consiste en: (i) arilo C₆₋₁₄ sustituido opcionalmente con 1 a 2 sustituyentes seleccionados independientemente del grupo que consiste en alcoxi C₁₋₆, halógeno y un grupo de fórmula (2), (ii) heteroarilo de 5 a 6 elementos sustituido opcionalmente con 1 a 2 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, hidroxi, alcoxi C₁₋₆, -B(OH)₂, heteroarilo de 5 a 6 elementos, alquilo C₁₋₆, y amino, y (iii) heterociclilo de 5 a 14 elementos sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente del grupo que consiste en halógeno, alquilo C₁₋₆ y oxo, R² se selecciona del grupo que consiste en: (i) alquilo C₁₋₆ sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente de halógeno, (ii) cicloalquilo C₃₋₁₄, (iii) arilo C₆₋₁₄ sustituido opcionalmente con 1 a 2 sustituyentes seleccionados independientemente de halógeno, (iv) heteroarilo de 5 a 14 elementos sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente de halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆ y oxo, y (v) heteroariloxi de 5 a 14 elementos sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente de halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆ y oxo, y (vi) heterociclilo de 5 a 14 elementos sustituido opcionalmente con 1 a 3 sustituyentes seleccionados independientemente de halógeno, alquilo C₁₋₆, haloalquilo C₁₋₆ y oxo, R³ se selecciona del grupo que consiste en hidrógeno, halógeno, alcoxi C₁₋₆, cicloalquiloxi C₃₋₁₄ e hidroxi, R⁴ se selecciona del grupo que consiste en hidrógeno, halógeno, alquilo C₁₋₆, hidroxi-alquilo C₁₋₆, alcoxiC₁₋₆-carbonilo, alcoxi C₁₋₆-carbonil-NH-, hidroxi, amino, carboxi, alquil C₁₋₆-C(O)-NH-, alquenil C₂₋₆-C(O)-NH-, carboxi-NH-, oxo, cicloalquilo C₃₋₁₄ e hidroxi-cicloalquilo C₃₋₁₄, L se selecciona del grupo que consiste en un enlace covalente y -CH=CH-, A se selecciona del grupo que consiste en arilo C₆₋₁₄, heteroarilo de 5 a 14 elementos y heterociclilo de 5 a 14 elementos, y n es 1, 2, 3 ó 4.
Applications Claiming Priority (1)
Application Number | Priority Date | Filing Date | Title |
---|---|---|---|
EP19184218 | 2019-07-03 |
Publications (1)
Publication Number | Publication Date |
---|---|
AR119322A1 true AR119322A1 (es) | 2021-12-09 |
Family
ID=67180549
Family Applications (1)
Application Number | Title | Priority Date | Filing Date |
---|---|---|---|
ARP200101858A AR119322A1 (es) | 2019-07-03 | 2020-07-01 | Compuestos derivados de 1h-pirido[1,2-a]pirazina como inhibidores de magl |
Country Status (18)
Country | Link |
---|---|
US (1) | US20220213093A1 (es) |
EP (1) | EP3994137A1 (es) |
JP (1) | JP2022540367A (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) |
TW (1) | TW202116768A (es) |
WO (1) | WO2021001330A1 (es) |
Families Citing this family (5)
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 |
MA53219A (fr) | 2018-08-13 | 2021-11-17 | Hoffmann La Roche | Nouveaux composés hétérocycliques en tant qu'inhibiteurs de monoacylglycérol lipase |
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). |
CN115989228A (zh) | 2020-09-03 | 2023-04-18 | 豪夫迈·罗氏有限公司 | 杂环化合物 |
WO2022266162A1 (en) | 2021-06-16 | 2022-12-22 | Celgene Corporation | Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases |
Family Cites Families (1)
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 |
-
2020
- 2020-06-30 CR CR20210630A patent/CR20210630A/es unknown
- 2020-06-30 KR KR1020227002453A patent/KR20220027991A/ko unknown
- 2020-06-30 EP EP20734956.4A patent/EP3994137A1/en active Pending
- 2020-06-30 CA CA3143280A patent/CA3143280A1/en active Pending
- 2020-06-30 BR BR112021026820A patent/BR112021026820A2/pt not_active Application Discontinuation
- 2020-06-30 MA MA056443A patent/MA56443A/fr unknown
- 2020-06-30 WO PCT/EP2020/068320 patent/WO2021001330A1/en unknown
- 2020-06-30 JP JP2021577946A patent/JP2022540367A/ja active Pending
- 2020-06-30 AU AU2020299965A patent/AU2020299965A1/en not_active Abandoned
- 2020-06-30 CN CN202080048854.0A patent/CN114072405A/zh active Pending
- 2020-06-30 PE PE2021002264A patent/PE20220514A1/es unknown
- 2020-06-30 MX MX2022000083A patent/MX2022000083A/es unknown
- 2020-07-01 AR ARP200101858A patent/AR119322A1/es unknown
- 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 |
---|---|
IL288936A (en) | 2022-02-01 |
WO2021001330A1 (en) | 2021-01-07 |
MA56443A (fr) | 2022-05-11 |
CR20210630A (es) | 2022-02-11 |
BR112021026820A2 (pt) | 2022-02-22 |
AU2020299965A1 (en) | 2022-02-03 |
MX2022000083A (es) | 2022-02-03 |
JP2022540367A (ja) | 2022-09-15 |
CA3143280A1 (en) | 2021-01-07 |
KR20220027991A (ko) | 2022-03-08 |
EP3994137A1 (en) | 2022-05-11 |
TW202116768A (zh) | 2021-05-01 |
CO2022000749A2 (es) | 2022-02-07 |
CL2022000005A1 (es) | 2022-10-21 |
PE20220514A1 (es) | 2022-04-07 |
US20220213093A1 (en) | 2022-07-07 |
CN114072405A (zh) | 2022-02-18 |
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