PE20211380A1 - Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa - Google Patents

Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa

Info

Publication number
PE20211380A1
PE20211380A1 PE2020002021A PE2020002021A PE20211380A1 PE 20211380 A1 PE20211380 A1 PE 20211380A1 PE 2020002021 A PE2020002021 A PE 2020002021A PE 2020002021 A PE2020002021 A PE 2020002021A PE 20211380 A1 PE20211380 A1 PE 20211380A1
Authority
PE
Peru
Prior art keywords
monoacylglicerol
compounds
chr4
oxazin
trifluoromethyl
Prior art date
Application number
PE2020002021A
Other languages
English (en)
Inventor
Lilli Anselm
Joerg Benz
Uwe Grether
Zbinden Katrin Groebke
Dominik Heer
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 PE20211380A1 publication Critical patent/PE20211380A1/es

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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
    • 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
    • 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

Abstract

Esta referido a compuestos organicos de Formula I, en donde: A es arilo C6-C14, heteroarilo de 5 a14 miembros, entre otras opciones; X es C-R3, m es 0 o 1, n es 0, 1 o 2 y L es C?C, S(O), SO2, SCH2, entre otras opciones; o X es N, m es 1, n es 1 o 2 y L es NR5-CH2-CHR4, NR5-CHR4-CH2 o NR8C(O)-(CR6R7)p; R1 es H, alquilo C1-C6; R2 es H, alquilo C1-C6, hidroxialquilo C1-C6. Entre los compuestos preferidos tenemos los siguientes: (+)- o (-)-(4aR,8aS)-6-[3-[[[2,2,2-trifluoro-1-[4-(trifluorometil)fenil]etil]amino]metil]azetidin-1-carbonil]hexahidro-2Hpirido[4,3-b][1,4]oxazin-3(4H)-ona; (4aR,8aS)-6-[4-[N-metil-4-(trifluorometil)anilino]piperidin-1-carbonil]-4,4a,5,7,8,8a-hexahidropirido[4,3-b][1,4]oxazin-3-ona; entre otros. Estos compuestos son inhibidores de monoacilglicerol lipasa (MAGL) y se emplean en el tratamiento o profilaxis de la neuroinflamacion, enfermedades neurodegenerativas, dolor, cancer, trastornos mentales, esclerosis multiple, enfermedad de Alzheimer, enfermedad de Parkinson, esclerosis lateral amiotrofica, lesion cerebral traumatica, neurotoxicidad, apoplejia, epilepsia, ansiedad, migrana y/o depresion en un mamifero.
PE2020002021A 2018-08-13 2019-08-12 Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa PE20211380A1 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP18188679 2018-08-13
PCT/EP2019/071522 WO2020035425A1 (en) 2018-08-13 2019-08-12 New heterocyclic compounds as monoacylglycerol lipase inhibitors

Publications (1)

Publication Number Publication Date
PE20211380A1 true PE20211380A1 (es) 2021-07-27

Family

ID=63244466

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2020002021A PE20211380A1 (es) 2018-08-13 2019-08-12 Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa

Country Status (19)

Country Link
US (1) US20210277020A1 (es)
EP (1) EP3837264A1 (es)
JP (1) JP2021533093A (es)
KR (1) KR20210044217A (es)
CN (1) CN112469724A (es)
AR (1) AR115949A1 (es)
AU (1) AU2019322161A1 (es)
BR (1) BR112020025642A2 (es)
CA (1) CA3098272A1 (es)
CL (1) CL2021000361A1 (es)
CR (1) CR20210056A (es)
IL (1) IL280762A (es)
MA (1) MA53220A (es)
MX (1) MX2020013719A (es)
PE (1) PE20211380A1 (es)
PH (1) PH12021500015A1 (es)
SG (1) SG11202012222TA (es)
TW (1) TWI814882B (es)
WO (1) WO2020035425A1 (es)

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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
JP7269943B2 (ja) 2018-01-08 2023-05-09 エフ． ホフマン－ラ ロシュ アーゲー Ｍａｇｌ阻害剤としてのオクタヒドロピリド［１，２－アルファ］ピラジン
US20190292188A1 (en) 2018-02-27 2019-09-26 Incyte Corporation Imidazopyrimidines and triazolopyrimidines as a2a / a2b inhibitors
US11168089B2 (en) 2018-05-18 2021-11-09 Incyte Corporation Fused pyrimidine derivatives as A2A / A2B inhibitors
MX2021001433A (es) 2018-08-13 2021-04-12 Hoffmann La Roche Nuevos compuestos heterociclicos como inhibidores de la monoacilglicerol lipasa.
TWI829857B (zh) 2019-01-29 2024-01-21 美商英塞特公司 作為a2a / a2b抑制劑之吡唑并吡啶及三唑并吡啶
US20210094971A1 (en) * 2019-09-09 2021-04-01 Hoffmann-La Roche Inc. Heterocyclic compounds
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
CN114269755A (zh) 2019-09-12 2022-04-01 豪夫迈·罗氏有限公司 作为magl抑制剂的4,4a,5,7,8,8a-六吡啶并[4,3-b][1,4]噁嗪-3-酮化合物
KR20220066894A (ko) * 2019-09-23 2022-05-24 에프. 호프만-라 로슈 아게 헤테로사이클릭 화합물
AR120030A1 (es) * 2019-09-24 2022-01-26 Hoffmann La Roche Compuestos heterocíclicos
AR120029A1 (es) * 2019-09-24 2022-01-26 Hoffmann La Roche Compuestos heterocíclicos

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US7579495B2 (en) 2003-12-19 2009-08-25 Momentive Performance Materials Inc. Active-releasing cyclic siloxanes
TW200942537A (en) * 2008-02-01 2009-10-16 Irm Llc Compounds and compositions as kinase inhibitors
WO2011029804A1 (en) 2009-09-10 2011-03-17 F. Hoffmann-La Roche Ag Inhibitors of jak
WO2011059118A1 (ko) 2009-11-10 2011-05-19 Kim Hyun Jeen 후각인지능력 검사 시스템
US8420661B2 (en) * 2010-04-13 2013-04-16 Hoffmann-La Roche Inc. Arylethynyl derivatives
WO2013080156A1 (en) * 2011-11-30 2013-06-06 Actelion Pharmaceuticals Ltd 3,7-disubstituted octahydro-2h-pyrido[4,3-e][1,3]oxazin-2-one antibiotics
US10106556B2 (en) * 2015-03-30 2018-10-23 Takeda Pharmaceutical Company Limited Heterocyclic compound
JP6703553B2 (ja) 2015-05-21 2020-06-03 グラクソスミスクライン、インテレクチュアル、プロパティー、ディベロップメント、リミテッドＧｌａｘｏｓｍｉｔｈｋｌｉｎｅ Ｉｎｔｅｌｌｅｃｔｕａｌ Ｐｒｏｐｅｒｔｙ Ｄｅｖｅｌｏｐｍｅｎｔ Ｌｉｍｉｔｅｄ Ｐａｄ４阻害剤としてのベンゾイミダゾール誘導体
PE20190409A1 (es) * 2016-03-31 2019-03-14 Takeda Pharmaceuticals Co Compuesto heterociclico

Also Published As

Publication number Publication date
CR20210056A (es) 2021-03-02
PH12021500015A1 (en) 2021-09-13
EP3837264A1 (en) 2021-06-23
AU2019322161A1 (en) 2020-11-12
BR112020025642A2 (pt) 2021-03-23
IL280762A (en) 2021-04-29
MX2020013719A (es) 2021-03-02
CA3098272A1 (en) 2020-02-20
KR20210044217A (ko) 2021-04-22
SG11202012222TA (en) 2021-01-28
MA53220A (fr) 2021-11-17
WO2020035425A1 (en) 2020-02-20
TWI814882B (zh) 2023-09-11
JP2021533093A (ja) 2021-12-02
AR115949A1 (es) 2021-03-17
CL2021000361A1 (es) 2021-07-09
CN112469724A (zh) 2021-03-09
US20210277020A1 (en) 2021-09-09
TW202035421A (zh) 2020-10-01

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