BR112022005472A2 - Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica - Google Patents

Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica

Info

Publication number
BR112022005472A2
BR112022005472A2 BR112022005472A BR112022005472A BR112022005472A2 BR 112022005472 A2 BR112022005472 A2 BR 112022005472A2 BR 112022005472 A BR112022005472 A BR 112022005472A BR 112022005472 A BR112022005472 A BR 112022005472A BR 112022005472 A2 BR112022005472 A2 BR 112022005472A2
Authority
BR
Brazil
Prior art keywords
magl
inhibitors
heterocyclic
pharmaceutical composition
manufacturing process
Prior art date
Application number
BR112022005472A
Other languages
English (en)
Inventor
Benoit Hornsperger
Bernd Kuhn
Carsten Kroll
Fionn O'hara
Hans Richter
Groebke Zbinden Katrin
Luca Gobbi
Daniel Rinaldo Lutz Marius
Martin Ritter
Uwe Grether
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 BR112022005472A2 publication Critical patent/BR112022005472A2/pt

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
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P21/00—Drugs for disorders of the muscular or neuromuscular 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/08—Antiepileptics; Anticonvulsants
    • 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
    • A61P25/14—Drugs for disorders of the nervous system for treating abnormal movements, e.g. chorea, dyskinesia
    • A61P25/16—Anti-Parkinson drugs
    • 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
    • A61P25/18—Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • 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
    • A61P25/22—Anxiolytics
    • 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
    • A61P25/24—Antidepressants
    • 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
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P37/00—Drugs for immunological or allergic disorders
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • 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

Landscapes

  • 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

nibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica. a presente invenção refere-se a compostos heterocíclicos que são inibidores de monoacilclicerol lipase (magl) tendo a fórmula geral (i) em que a, l1, x, m, n e r1 a r4 são como descritos no presente documento, composições incluindo os compostos, processos de fabricação dos compostos e métodos de uso dos compostos.
BR112022005472A 2019-09-24 2020-09-22 Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica BR112022005472A2 (pt)

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
BR112022005472A2 true BR112022005472A2 (pt) 2022-06-14

Family

ID=68066569

Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022005472A BR112022005472A2 (pt) 2019-09-24 2020-09-22 Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica

Country Status (16)

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

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
EP3717477B1 (en) 2017-11-28 2022-07-20 F. Hoffmann-La Roche AG New heterocyclic compounds
CN111566105A (zh) 2018-01-08 2020-08-21 豪夫迈·罗氏有限公司 作为MAGL抑制剂的八氢吡啶并[1,2-α]吡嗪类化合物
CA3104928A1 (en) 2018-08-13 2020-02-20 F. Hoffmann-La Roche Ag New heterocyclic compounds as monoacylglycerol lipase inhibitors
CR20220104A (es) 2019-09-12 2022-04-20 Hoffmann La Roche Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl
JP2023539690A (ja) 2020-09-03 2023-09-15 エフ． ホフマン－ラ ロシュ アーゲー 複素環式化合物
WO2023144160A1 (en) * 2022-01-25 2023-08-03 F. Hoffmann-La Roche Ag New heterocyclic compounds
WO2024088922A1 (en) * 2022-10-24 2024-05-02 F. Hoffmann-La Roche Ag Heterocyclic compounds as inhibitors of monoacylglycerol lipase (magl)

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
WO2016185279A1 (en) 2015-05-21 2016-11-24 Glaxosmithkline Intellectual Property Development Limited Benzoimidazole derivatives as pad4 inhibitors
DK3768684T3 (da) * 2018-03-22 2023-04-24 Hoffmann La Roche Oxazin-monoacylglycerol-lipase (MAGL)-hæmmere
CA3104928A1 (en) * 2018-08-13 2020-02-20 F. Hoffmann-La Roche Ag New heterocyclic compounds as monoacylglycerol lipase inhibitors
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
CO2022002000A2 (es) 2022-04-08
AU2020354414A1 (en) 2022-02-17
EP4034538A1 (en) 2022-08-03
AR120030A1 (es) 2022-01-26
CA3152213A1 (en) 2021-04-01
TW202126663A (zh) 2021-07-16
WO2021058445A1 (en) 2021-04-01
US20210094973A1 (en) 2021-04-01
CR20220118A (es) 2022-04-20
JP2022549446A (ja) 2022-11-25
KR20220069003A (ko) 2022-05-26
IL289594A (en) 2022-03-01
MX2022002711A (es) 2022-03-22
PE20220710A1 (es) 2022-05-04
CN114401968A (zh) 2022-04-26

Similar Documents

Publication Publication Date Title
BR112022005472A2 (pt) Inibidores heterocíclicos de monoacilglicerol lipase (magl), seus usos, processo de fabricação e composição farmacêutica
BR112022003704A2 (pt) Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl
CO2021002382A2 (es) Nuevos compuestos heterocíclicos como inhibidores de la monoacilglicerol lipasa
BR112022002375A2 (pt) Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl
BR112021012635A2 (pt) Compostos de 3-carbonilamino-5-ciclopentil-1 fi-pirazol tendo atividade inibitória sobre cdk2
BR112019003519A2 (pt) compostos de sulfonimidoilpurinona 7-substituídos para o tratamento e profilaxia de infecção por vírus
CL2021000361A1 (es) Nuevos compuestos heterocíclicos como inhibidores de monoacilglicerol lipasa
MX2020008894A (es) Inhibidores de oxazin monoacilglicerol lipasa (magl).
BR112022003982A2 (pt) Compostos heterocíclicos
BR112018003595A2 (pt) análogos de nucleosídeos substituídos no anel aromático 6-6 bicíclico para uso como inibidores de prmt5
BR112015004113A2 (pt) 6-aminoácido heteroarila diidropirimidinas para o tratamento e profilaxia da infecção pelo vírus da hepatite b
BR112021022758A2 (pt) Compostos de 1-oxo-isoindolina-5-carboxamida substituídos, suas composições e métodos de tratamento com os mesmos
BR112012027062B8 (pt) composto, processo para a preparação de um composto e usos do mesmo
BR112018013251A2 (pt) compostos heterocílicos tricíclicos fundidos como inibidores da hiv integrase
BR112014010576B8 (pt) compostos inibidores de neprilisina (nep), seus usos, processo de preparação dos compostos e composição farmacêutica compreendendo os compostos
BR112015023397A2 (pt) benzoxazois substituídos e métodos de uso dos mesmos
BR112017017349A2 (pt) composto, composição, método para tratar um distúrbio
BRPI0507830A (pt) derivados azabicìclicos, o respectivo processo de preparo e as composições farmacêuticas que os contêm
BR112021026899A2 (pt) Compostos heterocíclicos
BRPI0408353A (pt) composto, composição farmacêutica, métodos para o tratamento de neoplasias suscetìveis e para o tratamento de infecções virais, e, uso de um composto
BR112022022608A2 (pt) Compostos como inibidores de bcl-2
BR112023003580A2 (pt) Compostos heterocíclicos
BR112022018828A2 (pt) Derivados de benzodiazepina como gaba a gamma1 pams
BR112019006414A2 (pt) análogos de carbanucleosídeos de sistema de anel monocíclico e bicíclico substituídos para uso como inibidores de prmt5
BR112015024109A2 (pt) derivados de ureia e seu uso como inibidores de proteína de ligação de ácidos graxos (fabp)

Legal Events

Date Code Title Description
B11A Dismissal acc. art.33 of ipl - examination not requested within 36 months of filing
B11Y Definitive dismissal - extension of time limit for request of examination expired [chapter 11.1.1 patent gazette]