PE20221450A1 - Compuestos heterociclicos - Google Patents

Compuestos heterociclicos

Info

Publication number
PE20221450A1
PE20221450A1 PE2022000376A PE2022000376A PE20221450A1 PE 20221450 A1 PE20221450 A1 PE 20221450A1 PE 2022000376 A PE2022000376 A PE 2022000376A PE 2022000376 A PE2022000376 A PE 2022000376A PE 20221450 A1 PE20221450 A1 PE 20221450A1
Authority
PE
Peru
Prior art keywords
halogen
alkyl
cycloalkyl
disease
hydrogen
Prior art date
Application number
PE2022000376A
Other languages
English (en)
Inventor
Joerg Benz
Luca Gobbi
Uwe Grether
Steven Paul Hanlon
Benoit Hornsperger
Carsten Kroll
Bernd Kuhn
Martin Kuratli
Guofu Liu
Fionn O'hara
Hans Richter
Martin Ritter
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 PE20221450A1 publication Critical patent/PE20221450A1/es

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
    • 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
    • A61P1/00—Drugs for disorders of the alimentary tract or the digestive system
    • A61P1/06—Anti-spasmodics, e.g. drugs for colics, esophagic dyskinesia
    • 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
    • A61P25/06—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
    • A61P25/22—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
    • 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
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D513/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00
    • C07D513/02—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for in groups C07D463/00, C07D477/00 or C07D499/00 - C07D507/00 in which the condensed system contains two hetero rings
    • C07D513/04—Ortho-condensed systems

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Medicinal Chemistry (AREA)
  • Public Health (AREA)
  • Veterinary Medicine (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (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)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Hospice & Palliative Care (AREA)
  • Rheumatology (AREA)
  • Epidemiology (AREA)
  • Urology & Nephrology (AREA)
  • Psychology (AREA)
  • Vascular Medicine (AREA)
  • Cardiology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Orthopedic Medicine & Surgery (AREA)
  • Physical Education & Sports Medicine (AREA)
  • Immunology (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Nitrogen And Oxygen Or Sulfur-Condensed Heterocyclic Ring Systems (AREA)
  • Nitrogen Condensed Heterocyclic Rings (AREA)

Abstract

La invencion proporciona compuestos heterociclicos de formula general (I); en donde i) U es CH2; V es O; W y X son ambos CH; R1 se selecciona de halogeno y alquilo C1-6; y R2 se selecciona de hidrogeno, halogeno y alquilo C1-6; o R1 y R2, junto con el atomo de carbono al que se encuentran unidos, forman un cicloalquilo C3-C10; o ii) U es CH2; V es O; W es CRw; X es CH; Rw se selecciona de halogeno y alquilo C1-6; R1 y R2 se seleccionan independientemente de hidrogeno, halogeno y alquilo C1-6; o R1 y R2, junto con el atomo de carbono al que se encuentran unidos, forman un cicloalquilo C3-C10; entre otras combinaciones, Z es CH o N; Q es CRq o N; L se selecciona de un enlace covalente, -CHR5-, -O-, -OCH2-, entre otros; A se selecciona de arilo C6-C14, heteroarilo de 5 a 14 miembros y heterociclilo de 3 a 14 miembros. Un compuesto seleccionado es rel-(4aR,8S,8aS)-6-[3-[[2-fluoro-4-(trifluorometil)fenil]metoxi]azetidina1-carbonil]-8-metil-4,4a,5,7,8,8a-hexahidropirido[4,3-b][1,4]oxazin-3-ona. Dichos compuestos son inhibidores de monoacilglicerol-lipasa (MAGL). Tambien revela una composicion farmaceutica que comprende dicho compuesto y un procedimiento de preparacion de los mismos; siendo utiles en el tratamiento o profilaxis de neuroinflamacion, enfermedades neurodegenerativas, dolor, cancer, trastornos mentales, esclerosis multiple, enfermedad de Alzheimer, enfermedad de Parkinson, entre otros.
PE2022000376A 2019-09-23 2020-09-21 Compuestos heterociclicos PE20221450A1 (es)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
EP19198974 2019-09-23
CN2020109184 2020-08-14
PCT/EP2020/076228 WO2021058416A1 (en) 2019-09-23 2020-09-21 Heterocyclic compounds

Publications (1)

Publication Number Publication Date
PE20221450A1 true PE20221450A1 (es) 2022-09-21

Family

ID=72659185

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2022000376A PE20221450A1 (es) 2019-09-23 2020-09-21 Compuestos heterociclicos

Country Status (15)

Country Link
US (2) US20210107921A1 (es)
EP (1) EP4034239A1 (es)
JP (1) JP2022549810A (es)
KR (1) KR20220066894A (es)
CN (1) CN114401969A (es)
AU (1) AU2020355507A1 (es)
BR (1) BR112022003982A2 (es)
CA (1) CA3155161A1 (es)
CO (1) CO2022003062A2 (es)
CR (1) CR20220116A (es)
IL (1) IL289617A (es)
MX (1) MX2022003023A (es)
PE (1) PE20221450A1 (es)
TW (1) TW202120502A (es)
WO (1) WO2021058416A1 (es)

Families Citing this family (6)

* 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
CN111386269A (zh) 2017-11-28 2020-07-07 豪夫迈·罗氏有限公司 新型杂环化合物
WO2019134985A1 (en) 2018-01-08 2019-07-11 F. Hoffmann-La Roche Ag Octahydropyrido[1,2-alpha]pyrazines as magl inhibitors
MA53219A (fr) 2018-08-13 2021-11-17 Hoffmann La Roche Nouveaux composés hétérocycliques en tant qu'inhibiteurs de monoacylglycérol lipase
MX2022002311A (es) 2019-09-12 2022-03-25 Hoffmann La Roche Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de monoacilglicerol lipasa (magl).
CN115989228A (zh) 2020-09-03 2023-04-18 豪夫迈·罗氏有限公司 杂环化合物

Family Cites Families (11)

* 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
US7872028B2 (en) 2006-04-05 2011-01-18 Vitae Pharmaceuticals, Inc. Diaminopropanol renin inhibitors
WO2012155199A1 (en) 2011-05-16 2012-11-22 Bionomics Limited Amine derivatives as potassium channel blockers
US10106556B2 (en) * 2015-03-30 2018-10-23 Takeda Pharmaceutical Company Limited Heterocyclic compound
US20180148429A1 (en) 2015-05-13 2018-05-31 Selvita S.A. Substituted quinoxaline derivatives
CN111386269A (zh) * 2017-11-28 2020-07-07 豪夫迈·罗氏有限公司 新型杂环化合物
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
BR112020014992A2 (pt) * 2018-03-22 2020-12-29 F. Hoffmann-La Roche Ag Inibidores de oxazina monoacilglicerol lipase (magl)
MA53219A (fr) * 2018-08-13 2021-11-17 Hoffmann La Roche Nouveaux composés hétérocycliques en tant qu'inhibiteurs de monoacylglycérol lipase
JP2021533093A (ja) * 2018-08-13 2021-12-02 エフ.ホフマン−ラ ロシュ アーゲーF. Hoffmann−La Roche Aktiengesellschaft モノアシルグリセロールリパーゼ阻害剤としての新規複素環化合物

Also Published As

Publication number Publication date
BR112022003982A2 (pt) 2022-05-24
CA3155161A1 (en) 2021-04-01
WO2021058416A1 (en) 2021-04-01
JP2022549810A (ja) 2022-11-29
US20210107921A1 (en) 2021-04-15
MX2022003023A (es) 2022-04-07
CN114401969A (zh) 2022-04-26
KR20220066894A (ko) 2022-05-24
CR20220116A (es) 2022-04-20
EP4034239A1 (en) 2022-08-03
AU2020355507A1 (en) 2022-02-17
CO2022003062A2 (es) 2022-04-19
US20220267349A1 (en) 2022-08-25
TW202120502A (zh) 2021-06-01
IL289617A (en) 2022-03-01

Similar Documents

Publication Publication Date Title
PE20221450A1 (es) Compuestos heterociclicos
PE20211870A1 (es) Nuevos compuestos heterociclicos
PE20211089A1 (es) Nuevos compuestos heterociclicos como inhibidores de la monoacilglicerol lipasa
PE20211380A1 (es) Nuevos compuestos heterociclicos como inhibidores de monoacilglicerol lipasa
PE20212247A1 (es) Compuestos de 3-((3-aminofenil)amino)piperidina-2,6-diona sustituida, composiciones de estos y metodos de tratamiento con estos
PE20211795A1 (es) Compuestos heteroaril tetraciclicos
PE20220565A1 (es) Compuestos de 4,4a,5,7,8,8a-hexapirido[4,3-b][1,4]oxazin-3-ona como inhibidores de magl
PE20211411A1 (es) Compuestos de anillo fusionado
PE20180500A1 (es) Derivados de 2,3-dihidro-4h-1,3-benzoxazin-4-ona como moduladores del receptor muscarinico colinergico m1
PE20220710A1 (es) Nuevos inhibidores heterociclicos de monoacilglicerol lipasa (magl)
MX2015017343A (es) Derivados de pirrolopiridina o pirazolopiridina.
AR048789A1 (es) Derivados de oxazol y sus composiciones como moduladores de receptor activado de proliferador de peroxisoma (ppar)
PE20171177A1 (es) Compuestos aminopirimidinilo inhibidores de jak
PE20141010A1 (es) Derivados de piridin-2(1h)-ona utiles como medicamentos para el tratamiento de transtornos mieloproliferativos, rechazo de transplantes, enfermedades mediadas por el sistema inmune y enfermedades inflamatorias
AR029717A1 (es) Derivados del pro-farmaco de 4-fenil-piridina
AR049521A1 (es) Derivados de pirrazol - pirimidina
DE602006019221D1 (de) Von dopamin-d3-rezeptoren
PE20090493A1 (es) DERIVADOS DE LA 6-CICLOAMINO-3-(PIRIDAZIN-4-IL)IMIDAZO[1,2-b]-PIRIDAZINA, SU PREPARACION Y SU APLICACION EN TERAPEUTICA
AR050365A1 (es) Compuestos inhibidores de multi- quinasa pirrolopirimidina aril- amino sustituidos.
AR046186A1 (es) Compuestos derivados de 1,3,8-triaza-espiro[4.5]decan-4-ona
ATE487715T1 (de) Triazolderivate als modulatoren von dopamin-d3- rezeptoren
DE602006006850D1 (de) Als modulatoren von dopamin-d3-rezeptoren geeignete azabicyclo-(3,1,0)-hexan-derivate
NO20063747L (no) Substituerte kinoliner og deres anvendelse som mykobakterielle inhibitorer
AR035795A1 (es) Derivados de glutaramida sustituida con n-fenpropilciclopentilo como inhibidores de la enzima endopeptidasa neutra, uso de los mismos, procedimientos e intermediarios para su preparación y composiciones que contienen dichos inhibidores
PE20090435A1 (es) Inhibidores de tetrahidropiranocromeno de gamma secretasa