CO2022002000A2 - Nuevos inhibidores heterocíclicos de monoacilglicerol lipasa (magl) - Google Patents

Nuevos inhibidores heterocíclicos de monoacilglicerol lipasa (magl)

Info

Publication number
CO2022002000A2
CO2022002000A2 CONC2022/0002000A CO2022002000A CO2022002000A2 CO 2022002000 A2 CO2022002000 A2 CO 2022002000A2 CO 2022002000 A CO2022002000 A CO 2022002000A CO 2022002000 A2 CO2022002000 A2 CO 2022002000A2
Authority
CO
Colombia
Prior art keywords
magl
monoacylglycerol lipase
new heterocyclic
compounds
heterocyclic inhibitors
Prior art date
Application number
CONC2022/0002000A
Other languages
English (en)
Inventor
Luca Gobbi
Uwe Grether
Hans Richter
Zbinden Katrin Groebke
Benoit Hornsperger
Carsten Kroll
Fionn O`Hara
Martin Ritter
Marius Daniel Rinaldo Lutz
Bernd Kuhn
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 CO2022002000A2 publication Critical patent/CO2022002000A2/es

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    • 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
    • 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
    • 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
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    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/04—Centrally acting analgesics, e.g. opioids
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    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/06—Antimigraine agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
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    • A61P25/08—Antiepileptics; Anticonvulsants
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    • A61P35/00—Antineoplastic agents
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    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
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    • A61P9/00—Drugs for disorders of the cardiovascular system
    • A61P9/10—Drugs for disorders of the cardiovascular system for treating ischaemic or atherosclerotic diseases, e.g. antianginal drugs, coronary vasodilators, drugs for myocardial infarction, retinopathy, cerebrovascula insufficiency, renal arteriosclerosis
    • 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
    • C07D491/04—Ortho-condensed systems

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Neurosurgery (AREA)
  • Epidemiology (AREA)
  • Pain & Pain Management (AREA)
  • Inorganic Chemistry (AREA)
  • Psychiatry (AREA)
  • Rheumatology (AREA)
  • Immunology (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Psychology (AREA)
  • Cardiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Vascular Medicine (AREA)
  • Urology & Nephrology (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Preparation Of Compounds By Using Micro-Organisms (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La invención proporciona nuevos compuestos heterocíclicos, que son inhibidores de monoacilglicerol lipasa (MAGL) que tienen la Fórmula general (I) en donde A, L1, X, m, n y R1 a R4 son como se describen en la presente, composiciones que incluyen los compuestos, procesos de elaboración de los compuestos y métodos de uso de los compuestos.
CONC2022/0002000A 2019-09-24 2022-02-24 Nuevos inhibidores heterocíclicos de monoacilglicerol lipasa (magl) CO2022002000A2 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19199108 2019-09-24
PCT/EP2020/076347 WO2021058445A1 (en) 2019-09-24 2020-09-22 New heterocyclic monoacylglycerol lipase (magl) inhibitors

Publications (1)

Publication Number Publication Date
CO2022002000A2 true CO2022002000A2 (es) 2022-04-08

Family

ID=68066569

Family Applications (1)

Application Number Title Priority Date Filing Date
CONC2022/0002000A CO2022002000A2 (es) 2019-09-24 2022-02-24 Nuevos inhibidores heterocíclicos de monoacilglicerol lipasa (magl)

Country Status (16)

Country Link
US (1) US20210094973A1 (es)
EP (1) EP4034538A1 (es)
JP (1) JP2022549446A (es)
KR (1) KR20220069003A (es)
CN (1) CN114401968A (es)
AR (1) AR120030A1 (es)
AU (1) AU2020354414A1 (es)
BR (1) BR112022005472A2 (es)
CA (1) CA3152213A1 (es)
CO (1) CO2022002000A2 (es)
CR (1) CR20220118A (es)
IL (1) IL289594A (es)
MX (1) MX2022002711A (es)
PE (1) PE20220710A1 (es)
TW (1) TW202126663A (es)
WO (1) WO2021058445A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
AR114136A1 (es) 2017-10-10 2020-07-29 Hoffmann La Roche Compuestos heterocíclicos
WO2019105915A1 (en) 2017-11-28 2019-06-06 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
DK3837263T3 (da) 2018-08-13 2024-09-09 Hoffmann La Roche Nye heterocykliske forbindelser som monoacylglycerollipasehæmmere
BR112022002375A2 (pt) 2019-09-12 2022-07-19 Hoffmann La Roche Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl
WO2022049134A1 (en) 2020-09-03 2022-03-10 F. Hoffmann-La Roche Ag Heterocyclic compounds
AR128333A1 (es) * 2022-01-25 2024-04-17 Hoffmann La Roche Nuevos compuestos heterociclicos
TW202428574A (zh) * 2022-10-24 2024-07-16 瑞士商赫孚孟拉羅股份公司 新穎雜環化合物

Family Cites Families (7)

* Cited by examiner, † Cited by third party
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
KR101653473B1 (ko) * 2012-01-06 2016-09-01 어바이드 테라퓨틱스, 인크. 카르바메이트 화합물 및 그의 제조 및 이용 방법
CN107849015B (zh) 2015-05-21 2021-03-19 葛兰素知识产权发展有限公司 作为pad4抑制剂的苯并咪唑衍生物
HUE061584T2 (hu) * 2018-03-22 2023-07-28 Hoffmann La Roche Oxazin-monoacil-glicerol-lipáz (MAGL) gátlók
DK3837263T3 (da) * 2018-08-13 2024-09-09 Hoffmann La Roche Nye heterocykliske forbindelser som monoacylglycerollipasehæmmere
SG11202012222TA (en) * 2018-08-13 2021-01-28 Hoffmann La Roche New heterocyclic compounds as monoacylglycerol lipase inhibitors

Also Published As

Publication number Publication date
WO2021058445A1 (en) 2021-04-01
AR120030A1 (es) 2022-01-26
CN114401968A (zh) 2022-04-26
US20210094973A1 (en) 2021-04-01
CA3152213A1 (en) 2021-04-01
MX2022002711A (es) 2022-03-22
EP4034538A1 (en) 2022-08-03
IL289594A (en) 2022-03-01
TW202126663A (zh) 2021-07-16
PE20220710A1 (es) 2022-05-04
JP2022549446A (ja) 2022-11-25
CR20220118A (es) 2022-04-20
BR112022005472A2 (pt) 2022-06-14
AU2020354414A1 (en) 2022-02-17
KR20220069003A (ko) 2022-05-26

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