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PE20220514A1 - Inhibidores de monoacilglicerol lipasa (magl) heterociclicos - Google Patents

Inhibidores de monoacilglicerol lipasa (magl) heterociclicos

Info

Publication number
PE20220514A1
PE20220514A1 PE2021002264A PE2021002264A PE20220514A1 PE 20220514 A1 PE20220514 A1 PE 20220514A1 PE 2021002264 A PE2021002264 A PE 2021002264A PE 2021002264 A PE2021002264 A PE 2021002264A PE 20220514 A1 PE20220514 A1 PE 20220514A1
Authority
PE
Peru
Prior art keywords
chloro
magl
inhibitors
heterocyclic
methanone
Prior art date
Application number
PE2021002264A
Other languages
English (en)
Inventor
Joerg Benz
Uwe Grether
Benoit Hornsperger
Carsten Kroll
Bernd Kuhn
Fionn O`Hara
Hans Richter
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 PE20220514A1 publication Critical patent/PE20220514A1/es

Links

Classifications

    • 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
    • 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
    • A61K9/20—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
    • 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

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

Esta referido a compuestos heterociclicos de formula general (I), en donde: R1 es arilo, heteroarilo, heterociclilo; R2 es alquilo, cicloalquilo, heteroarilo; R3 es H, halogeno, alcoxi, cicloalquiloxi, OH. Entre los compuestos preferidos tenemos los siguientes: [(7S,9aR)-7-(3-cloro-4-fluorofenil)-7-hidroxi-3,4,6,8,9,9a-hexahidro-1Hpirido[1,2-a]pirazin-2-il]-(2-cloro-3-metoxifenil)metanona; [(7S,9aR)-7-(4-clorofenil)-7-hidroxi-3,4,6,8,9,9a-hexahidro-1H-pirido[1,2- a]pirazin-2-il]-[2-cloro-3-(3-fluoro-1H-pirazol-4-il)fenil]metanona; entre otros. Estos compuestos son inhibidores de monoacilglicerol lipasa (MAGL) destinados al tratamiento o la profilaxis de neuroinflamacion, enfermedades neurodegenerativas, dolor, cancer, trastornos mentales, esclerosis multiple, enfermedad de Alzheimer, enfermedad de Parkinson, esclerosis lateral amiotrofica, traumatismo craneoencefalico, neurotoxicidad, apoplejia, epilepsia, ansiedad, jaqueca y/o depresion.
PE2021002264A 2019-07-03 2020-06-30 Inhibidores de monoacilglicerol lipasa (magl) heterociclicos PE20220514A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19184218 2019-07-03
PCT/EP2020/068320 WO2021001330A1 (en) 2019-07-03 2020-06-30 Heterocyclic monoacylglycerol lipase (magl) inhibitors

Publications (1)

Publication Number Publication Date
PE20220514A1 true PE20220514A1 (es) 2022-04-07

Family

ID=67180549

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2021002264A PE20220514A1 (es) 2019-07-03 2020-06-30 Inhibidores de monoacilglicerol lipasa (magl) heterociclicos

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)

* 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
BR112021002298A2 (pt) 2018-08-13 2021-05-04 F. Hoffmann-La Roche Ag compostos heterocíclicos como inibidores da monoacilglicerol lipase
AU2020346350A1 (en) 2019-09-12 2022-02-17 F. Hoffmann-La Roche Ag 4,4A,5,7,8,8A-hexapyrido(4,3-b)(1,4)oxazin-3-one compounds as magl inhibitors
EP4208456A1 (en) 2020-09-03 2023-07-12 F. Hoffmann-La Roche AG Heterocyclic compounds
IL308122A (en) 2021-06-16 2023-12-01 Celgene Corp Azetidinyl compounds consisting of 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
EP3994137A1 (en) 2022-05-11
WO2021001330A1 (en) 2021-01-07
JP2022540367A (ja) 2022-09-15
CN114072405A (zh) 2022-02-18
CO2022000749A2 (es) 2022-02-07
CL2022000005A1 (es) 2022-10-21
KR20220027991A (ko) 2022-03-08
CA3143280A1 (en) 2021-01-07
TW202116768A (zh) 2021-05-01
US20220213093A1 (en) 2022-07-07
BR112021026820A2 (pt) 2022-02-22
CR20210630A (es) 2022-02-11
MX2022000083A (es) 2022-02-03
MA56443A (fr) 2022-05-11
AU2020299965A1 (en) 2022-02-03
AR119322A1 (es) 2021-12-09
IL288936A (en) 2022-02-01

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