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 magl

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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
Application number
ARP200101858A
Other languages
English (en)
Inventor
Hans Richter
Fionn Ohara
Bernd Kuhn
Carsten Kroll
Benoit Hornsperger
Uwe Grether
Joerg Benz
Original Assignee
Hoffmann La Roche
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Hoffmann La Roche filed Critical Hoffmann La Roche
Publication of AR119322A1 publication Critical patent/AR119322A1/es

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Classifications

    • 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

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.
ARP200101858A 2019-07-03 2020-07-01 Compuestos derivados de 1h-pirido[1,2-a]pirazina como inhibidores de magl AR119322A1 (es)

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 (4)

* Cited by examiner, † Cited by third party
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
EP3837263A1 (en) 2018-08-13 2021-06-23 F. Hoffmann-La Roche AG New heterocyclic compounds as monoacylglycerol lipase inhibitors
EP4028403B1 (en) 2019-09-12 2023-11-22 F. Hoffmann-La Roche AG 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors
CA3217423A1 (en) 2021-06-16 2022-12-22 Jeffrey M. Schkeryantz Azetidinyl compounds comprising a carboxylic acid group for the treatment of neurodegenerative diseases

Family Cites Families (1)

* Cited by examiner, † Cited by third party
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

Also Published As

Publication number Publication date
MA56443A (fr) 2022-05-11
CL2022000005A1 (es) 2022-10-21
PE20220514A1 (es) 2022-04-07
WO2021001330A1 (en) 2021-01-07
BR112021026820A2 (pt) 2022-02-22
CR20210630A (es) 2022-02-11
IL288936A (en) 2022-02-01
US20220213093A1 (en) 2022-07-07
AU2020299965A1 (en) 2022-02-03
KR20220027991A (ko) 2022-03-08
TW202116768A (zh) 2021-05-01
MX2022000083A (es) 2022-02-03
CO2022000749A2 (es) 2022-02-07
EP3994137A1 (en) 2022-05-11
CA3143280A1 (en) 2021-01-07
JP2022540367A (ja) 2022-09-15
CN114072405A (zh) 2022-02-18

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