BR112022002375A2 - Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl - Google Patents

Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl

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Publication number
BR112022002375A2
BR112022002375A2 BR112022002375A BR112022002375A BR112022002375A2 BR 112022002375 A2 BR112022002375 A2 BR 112022002375A2 BR 112022002375 A BR112022002375 A BR 112022002375A BR 112022002375 A BR112022002375 A BR 112022002375A BR 112022002375 A2 BR112022002375 A2 BR 112022002375A2
Authority
BR
Brazil
Prior art keywords
compounds
hexapyrido
oxazin
ona
magl
Prior art date
Application number
BR112022002375A
Other languages
English (en)
Inventor
Benz Joerg
Gobbi Luca
Grether Uwe
Groebke Zbinden Katrin
Hornsperger Benoit
KROLL Carsten
Kuhn Bernd
E Martin Rainer
O'hara Fionn
Puellmann Bernd
Richter Hans
Ritter Martin
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 BR112022002375A2 publication Critical patent/BR112022002375A2/pt

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    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D413/00Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings
    • C07D413/12Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms containing two hetero rings linked by a chain containing hetero atoms as chain links
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2009Inorganic compounds
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D498/00Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02Heterocyclic 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
    • C07D498/04Ortho-condensed systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K31/00Medicinal preparations containing organic active ingredients
    • A61K31/33Heterocyclic compounds
    • A61K31/395Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
    • A61K31/535Heterocyclic 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
    • A61K31/53751,4-Oxazines, e.g. morpholine
    • A61K31/53831,4-Oxazines, e.g. morpholine ortho- or peri-condensed with heterocyclic ring systems
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2054Cellulose; Cellulose derivatives, e.g. hydroxypropyl methylcellulose
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/20Pills, tablets, discs, rods
    • A61K9/2004Excipients; Inactive ingredients
    • A61K9/2022Organic macromolecular compounds
    • A61K9/205Polysaccharides, e.g. alginate, gums; Cyclodextrin
    • A61K9/2059Starch, including chemically or physically modified derivatives; Amylose; Amylopectin; Dextrin
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/485Inorganic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4858Organic compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61KPREPARATIONS FOR MEDICAL, DENTAL OR TOILETRY PURPOSES
    • A61K9/00Medicinal preparations characterised by special physical form
    • A61K9/48Preparations in capsules, e.g. of gelatin, of chocolate
    • A61K9/4841Filling excipients; Inactive ingredients
    • A61K9/4866Organic macromolecular compounds
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P1/00Drugs for disorders of the alimentary tract or the digestive system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/18Antipsychotics, i.e. neuroleptics; Drugs for mania or schizophrenia
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P29/00Non-central analgesic, antipyretic or antiinflammatory agents, e.g. antirheumatic agents; Non-steroidal antiinflammatory drugs [NSAID]
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P35/00Antineoplastic agents
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D265/00Heterocyclic compounds containing six-membered rings having one nitrogen atom and one oxygen atom as the only ring hetero atoms
    • C07D265/281,4-Oxazines; Hydrogenated 1,4-oxazines

Abstract

COMPOSTOS DE 4,4A,5,7,8,8A-HEXAPIRIDO[4,3- B][1,4]OXAZIN-3-ONA COMO INIBIDORES DE MAGL. A presente invenção refere-se a compostos heterocíclicos tendo a fórmula geral (I) em que A, B, L1, X, m, n, R1 a R7 são conforme descritos no presente documento, composições incluindo os compostos, processos para fabricar os compostos, métodos para usar os compostos como inibidores de monoacilglicerol lipase (MAGL).
BR112022002375A 2019-09-12 2020-09-10 Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl BR112022002375A2 (pt)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP19196879 2019-09-12
PCT/EP2020/075260 WO2021048242A1 (en) 2019-09-12 2020-09-10 4,4a,5,7,8,8a-hexapyrido[4,3-b][1,4]oxazin-3-one compounds as magl inhibitors

Publications (1)

Publication Number Publication Date
BR112022002375A2 true BR112022002375A2 (pt) 2022-07-19

Family

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Family Applications (1)

Application Number Title Priority Date Filing Date
BR112022002375A BR112022002375A2 (pt) 2019-09-12 2020-09-10 Compostos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inibidores de magl

Country Status (17)

Country Link
US (1) US11814375B2 (pt)
EP (1) EP4028403B1 (pt)
JP (1) JP2022548028A (pt)
KR (1) KR20220062515A (pt)
CN (1) CN114269755A (pt)
AR (1) AR119943A1 (pt)
AU (1) AU2020346350A1 (pt)
BR (1) BR112022002375A2 (pt)
CA (1) CA3151516A1 (pt)
CL (1) CL2022000556A1 (pt)
CO (1) CO2022001879A2 (pt)
CR (1) CR20220104A (pt)
IL (1) IL289186A (pt)
MX (1) MX2022002311A (pt)
PE (1) PE20220565A1 (pt)
TW (1) TW202128706A (pt)
WO (1) WO2021048242A1 (pt)

Families Citing this family (7)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
WO2018165520A1 (en) 2017-03-10 2018-09-13 Vps-3, Inc. Metalloenzyme inhibitor compounds
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
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
CR20220325A (es) 2019-12-20 2022-08-19 Tenaya Therapeutics Inc Fluoroalquil-oxadiazoles y sus usos

Family Cites Families (50)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
US5214038A (en) 1991-04-15 1993-05-25 Hoechst-Roussel Pharmaceuticals Inc. 1-(pyrido[3,4-b]-1,4-oxazinyl-4-yl)-1H-indoles and intermediates for the preparation thereof
US7160888B2 (en) 2003-08-22 2007-01-09 Warner Lambert Company Llc [1,8]naphthyridin-2-ones and related compounds for the treatment of schizophrenia
US7579495B2 (en) 2003-12-19 2009-08-25 Momentive Performance Materials Inc. Active-releasing cyclic siloxanes
MX2007016523A (es) 2005-06-20 2008-03-06 Schering Corp Piperidinas sustituidas ligadas a carbono y derivados de las mismas utiles como antagonistas de hsitamina h3.
US8431695B2 (en) 2005-11-02 2013-04-30 Bayer Intellectual Property Gmbh Pyrrolo[2,1-f][1,2,4]triazin-4-ylamines IGF-1R kinase inhibitors for the treatment of cancer and other hyperproliferative diseases
US7696229B2 (en) 2006-02-17 2010-04-13 Memory Pharmaceuticals Corporation Compounds having 5-HT6 receptor affinity
US7872028B2 (en) 2006-04-05 2011-01-18 Vitae Pharmaceuticals, Inc. Diaminopropanol renin inhibitors
TW200942537A (en) 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
US8309734B2 (en) 2008-10-29 2012-11-13 Hoffmann-La Roche Inc. Substituted pyridines as GPBAR1 agonists
WO2011059118A1 (ko) 2009-11-10 2011-05-19 Kim Hyun Jeen 후각인지능력 검사 시스템
WO2011058766A1 (en) 2009-11-16 2011-05-19 Raqualia Pharma Inc. Aryl carboxamide derivatives as ttx-s blockers
US8420661B2 (en) 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
JP6254075B2 (ja) 2011-05-16 2017-12-27 バイオノミックス リミテッド カリウムチャネル遮断剤としてのアミン誘導体
WO2013059118A1 (en) 2011-10-19 2013-04-25 The Trustees Of Columbia University In The City Of New York Cyclopropenimine catalyst compositions and processes
JP2014533747A (ja) 2011-11-30 2014-12-15 アクテリオン ファーマシューティカルズ リミテッドActelion Pharmaceuticals Ltd 3,7−二置換オクタヒドロ−2H−ピリド[4,3−e][1,3]オキサジン−2−オン抗生物質
LT2794600T (lt) 2011-12-22 2018-02-26 Novartis Ag 2,3-dihidro-benzo[1,4]oksazino dariniai ir giminingi junginiai kaip fosfoinozitido-3 kinazės (pi3k) inhibitoriai, skirti gydymui, pavyzdžiui, reumatoidinio artrito
EP3698782B1 (en) 2012-01-06 2024-05-15 H. Lundbeck A/S Carbamate compounds for use in therapy
GB201209587D0 (en) 2012-05-30 2012-07-11 Takeda Pharmaceutical Therapeutic compounds
TW201422625A (zh) 2012-11-26 2014-06-16 Novartis Ag 二氫-吡啶并-□衍生物之固體形式
PL2986607T3 (pl) 2013-04-16 2017-11-30 Idorsia Pharmaceuticals Ltd Przeciwbakteryjne pochodne biaromatyczne
WO2016109501A1 (en) 2014-12-30 2016-07-07 Karos Pharmaceuticals, Inc. Amide compounds as tryptophan hydroxylase inhibitors
WO2016158956A1 (ja) 2015-03-30 2016-10-06 武田薬品工業株式会社 複素環化合物
AU2016261031A1 (en) 2015-05-13 2017-10-05 Selvita S.A. Substituted quinoxaline derivatives
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
CA3014432A1 (en) 2015-06-18 2016-12-22 Cephalon, Inc. Substituted 4-benzyl and 4-benzoyl piperidine derivatives
US10323038B2 (en) 2015-11-20 2019-06-18 Abide Therapeutics, Inc. Pyrazole compounds and methods of making and using same
US10385057B2 (en) * 2015-11-20 2019-08-20 Lundbeck La Jolla Research Center, Inc. Pyrazole compounds and methods of making and using same
BR112018068538B1 (pt) 2016-03-31 2023-12-12 Takeda Pharmaceutical Company Limited Composto, medicamento, e, uso de um composto
WO2017170830A1 (ja) 2016-03-31 2017-10-05 武田薬品工業株式会社 複素環化合物
ES2927021T3 (es) 2017-06-12 2022-11-02 Boehringer Ingelheim Int Compuestos heteroaromáticos como inhibidores de vanina
MX2020007318A (es) 2017-09-29 2020-08-24 Takeda Pharmaceuticals Co Compuesto heterociclico.
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
TW201930300A (zh) * 2017-12-15 2019-08-01 瑞士商赫孚孟拉羅股份公司 新雜環化合物
WO2019134985A1 (en) 2018-01-08 2019-07-11 F. Hoffmann-La Roche Ag Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors
HRP20230388T1 (hr) * 2018-03-22 2023-06-23 F. Hoffmann - La Roche Ag Inhibitori oksazin monoacilglicerol lipaze (magl)
MA53220A (fr) * 2018-08-13 2021-11-17 Hoffmann La Roche Nouveaux composés hétérocycliques utilisés en tant qu'inhibiteurs de monoacylglycérol lipase
EP3837263A1 (en) 2018-08-13 2021-06-23 F. Hoffmann-La Roche AG New heterocyclic compounds as monoacylglycerol lipase inhibitors
EP3883936B1 (en) 2018-11-22 2023-07-12 F. Hoffmann-La Roche AG New heterocyclic compounds
EP3883928A4 (en) 2018-11-22 2022-06-29 Qilu Regor Therapeutics Inc. Glp-1r agonists and uses thereof
JP2022527590A (ja) 2019-04-09 2022-06-02 エフ.ホフマン-ラ ロシュ アーゲー モノアシルグリセロールリパーゼ(magl)の阻害剤としての複素環式化合物
KR20220027991A (ko) 2019-07-03 2022-03-08 에프. 호프만-라 로슈 아게 헤테로시클릭 모노아실글리세롤 리파아제(magl) 억제제
CA3145338A1 (en) 2019-07-09 2021-01-14 F. Hoffmann-La Roche Ag New heterocyclic compounds
US20210094971A1 (en) 2019-09-09 2021-04-01 Hoffmann-La Roche Inc. Heterocyclic compounds
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
CN114650994A (zh) 2019-09-12 2022-06-21 豪夫迈·罗氏有限公司 放射性标记的化合物
EP4034239A1 (en) 2019-09-23 2022-08-03 F. Hoffmann-La Roche AG Heterocyclic compounds
CN114514233A (zh) 2019-09-24 2022-05-17 豪夫迈·罗氏有限公司 用于单酰基甘油脂肪酶(magl)的荧光探针
AU2020354414A1 (en) 2019-09-24 2022-02-17 F. Hoffmann-La Roche Ag New heterocyclic monoacylglycerol lipase (MAGL) inhibitors
AR120029A1 (es) 2019-09-24 2022-01-26 Hoffmann La Roche Compuestos heterocíclicos

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MX2022002311A (es) 2022-03-25
CR20220104A (es) 2022-04-20
EP4028403C0 (en) 2023-11-22
CA3151516A1 (en) 2021-03-18
KR20220062515A (ko) 2022-05-17
CO2022001879A2 (es) 2022-03-29
WO2021048242A1 (en) 2021-03-18
TW202128706A (zh) 2021-08-01
PE20220565A1 (es) 2022-04-13
EP4028403B1 (en) 2023-11-22
US20210094943A1 (en) 2021-04-01
AR119943A1 (es) 2022-01-19
CL2022000556A1 (es) 2022-10-21
US11814375B2 (en) 2023-11-14
IL289186A (en) 2022-02-01
AU2020346350A1 (en) 2022-02-17
CN114269755A (zh) 2022-04-01
JP2022548028A (ja) 2022-11-16
EP4028403A1 (en) 2022-07-20

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