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MX2016016488A - Derivados de azetidina sustituidos como ligandos de receptores asociados a aminas en trazas (taar). - Google Patents

Derivados de azetidina sustituidos como ligandos de receptores asociados a aminas en trazas (taar).

Info

Publication number
MX2016016488A
MX2016016488A MX2016016488A MX2016016488A MX2016016488A MX 2016016488 A MX2016016488 A MX 2016016488A MX 2016016488 A MX2016016488 A MX 2016016488A MX 2016016488 A MX2016016488 A MX 2016016488A MX 2016016488 A MX2016016488 A MX 2016016488A
Authority
MX
Mexico
Prior art keywords
disorders
halogen
hydrogen
substituted
lower alkyl
Prior art date
Application number
MX2016016488A
Other languages
English (en)
Inventor
Galley Guido
Norcross Roger
Pflieger Philippe
Cecere Giuseppe
RAUBER Etienne
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 MX2016016488A publication Critical patent/MX2016016488A/es

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    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D403/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00
    • C07D403/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings
    • C07D403/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, not provided for by group C07D401/00 containing two hetero rings linked by a chain containing hetero atoms as chain links
    • 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
    • A61K31/397—Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having four-membered rings, e.g. azetidine
    • 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
    • A61P25/08—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
    • 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
    • A61P25/20—Hypnotics; Sedatives
    • 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
    • A61P25/00—Drugs for disorders of the nervous system
    • A61P25/30—Drugs for disorders of the nervous system for treating abuse or dependence
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/04—Anorexiants; Antiobesity agents
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/06—Antihyperlipidemics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P3/00—Drugs for disorders of the metabolism
    • A61P3/08—Drugs for disorders of the metabolism for glucose homeostasis
    • A61P3/10—Drugs for disorders of the metabolism for glucose homeostasis for hyperglycaemia, e.g. antidiabetics
    • A—HUMAN NECESSITIES
    • A61—MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61P—SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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
    • 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
    • A61P9/06—Antiarrhythmics
    • 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
    • A61P9/12—Antihypertensives
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D205/00—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom
    • C07D205/02—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings
    • C07D205/04—Heterocyclic compounds containing four-membered rings with one nitrogen atom as the only ring hetero atom not condensed with other rings having no double bonds between ring members or between ring members and non-ring members
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D401/00—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom
    • C07D401/02—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings
    • C07D401/12—Heterocyclic compounds containing two or more hetero rings, having nitrogen atoms as the only ring hetero atoms, at least one ring being a six-membered ring with only one nitrogen atom containing two hetero rings linked by a chain containing hetero atoms as chain links

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • General Health & Medical Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • Medicinal Chemistry (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Neurology (AREA)
  • Biomedical Technology (AREA)
  • Diabetes (AREA)
  • Psychiatry (AREA)
  • Hematology (AREA)
  • Heart & Thoracic Surgery (AREA)
  • Cardiology (AREA)
  • Obesity (AREA)
  • Psychology (AREA)
  • Pain & Pain Management (AREA)
  • Epidemiology (AREA)
  • Anesthesiology (AREA)
  • Hospice & Palliative Care (AREA)
  • Child & Adolescent Psychology (AREA)
  • Endocrinology (AREA)
  • Addiction (AREA)
  • Emergency Medicine (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Plural Heterocyclic Compounds (AREA)

Abstract

La presente invención se refiere a los compuestos de la fórmula I en donde R1 es hidrógeno, metoxi o fluoro, R2/R2' son independientemente uno del otro hidrógeno, metoxi o fluoro; R3/R4 son independientemente uno del otro hidrógeno o halógeno; R es hidrógeno o fluoro; L1 es -CH2-, -NR'-, -O-, -S- o CF2-, o -HC=; R' es hidrógeno o alquilo inferior; L2 es un enlace, -C(O)NH-, -NH-, -CH2NHC(O)-, -NHC(O)- o -NHC(O)NH-; R es hidrógeno, halógeno, alcoxi inferior, ciano o es fenilo opcionalmente sustituido con uno o más sustituyentes, seleccionados de halógeno, alquilo inferior sustituido con halógeno o alcoxi inferior, o es un heteroarilo de cinco o seis miembros, seleccionado de piridinilo, pirimidinilo, pirazinilo, piridazinilo o pirazolilo, cuyos heteroarilos están opcionalmente sustituidos con uno o más sustituyentes, seleccionados de halógeno, alquilo inferior, alcoxi inferior, ciano, cicloalquilo, alquilo inferior sustituido con halógeno, alcoxi inferior sustituido con halógeno o por fenilo sustituido con halógeno; N es un átomo de nitrógeno en el anillo en la posición 1 o 2; o a una sal por adición de ácido farmacéuticamente adecuada de los mismos. Los compuestos de las fórmulas I tienen una buena afinidad hacia los receptores asociados a las aminas en trazas (TAARs), especialmente para TAAR1 y pueden ser utilizados para el tratamiento de la depresión, trastornos de ansiedad, trastorno bipolar, trastorno de hiperactividad con déficit de atención (ADHD), trastornos relacionados al estrés, trastornos psicóticos tales como esquizofrenia, trastornos neurológicos tales como enfermedad de Parkinson, trastornos neurodegenerativos tales como la enfermedad de Alzheimer, epilepsia, migraña, hipertensión, abuso de sustancias y trastornos metabólicos tales como trastornos de la alimentación, diabetes, complicaciones diabéticas, obesidad, dislipidemia, trastornos del consumo y asimilación de energía, trastornos y mal funcionamiento de la homeostasis de la temperatura corporal, trastornos del sueño y del ritmo circadiano, y trastornos cardiovasculares.
MX2016016488A 2014-08-27 2015-08-24 Derivados de azetidina sustituidos como ligandos de receptores asociados a aminas en trazas (taar). MX2016016488A (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP14182445 2014-08-27
PCT/EP2015/069315 WO2016030310A1 (en) 2014-08-27 2015-08-24 Substituted azetidine derivatives as taar ligands

Publications (1)

Publication Number Publication Date
MX2016016488A true MX2016016488A (es) 2017-03-30

Family

ID=51398565

Family Applications (1)

Application Number Title Priority Date Filing Date
MX2016016488A MX2016016488A (es) 2014-08-27 2015-08-24 Derivados de azetidina sustituidos como ligandos de receptores asociados a aminas en trazas (taar).

Country Status (10)

Country Link
US (1) US10023559B2 (es)
EP (1) EP3186224B1 (es)
JP (1) JP6539724B2 (es)
KR (1) KR101894681B1 (es)
CN (1) CN107001259B (es)
BR (1) BR112017000160A2 (es)
CA (1) CA2954098A1 (es)
MX (1) MX2016016488A (es)
RU (1) RU2017107521A (es)
WO (1) WO2016030310A1 (es)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
NZ737451A (en) * 2015-05-20 2022-01-28 Integrative Res Laboratories Sweden Ab Novel azetidine derivatives useful as modulators of cortical catecholaminergic neurotransmission
CR20180443A (es) 2016-03-17 2018-11-21 Hoffmann La Roche Derivado de morfolina
FI3541784T3 (fi) 2016-11-18 2023-10-02 Integrative Res Laboratories Sweden Ab Uudet atsetidiinijohdannaiset, jotka ovat hyödyllisiä kortikaalisen katekoliamiini-neurotransmission modulaattoreina
WO2018124001A1 (ja) 2016-12-27 2018-07-05 国立研究開発法人理化学研究所 Ｂｍｐシグナル阻害化合物
CN110437205B (zh) 2018-08-24 2022-07-08 广东东阳光药业有限公司 吡啶烯基哌啶衍生物及其用途
WO2021067215A1 (en) 2019-09-30 2021-04-08 Agios Pharmaceuticals, Inc. Piperidine compounds as menin inhibitors
US11091447B2 (en) 2020-01-03 2021-08-17 Berg Llc UBE2K modulators and methods for their use
EP4417602A1 (en) 2023-02-16 2024-08-21 Bayer AG Substituted pyrazole carboxamides, salts thereof and their use as herbicidally active substances

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GB2085427B (en) * 1980-10-08 1984-12-05 Robins Co Inc A H 3-phenoxyazetidines
US5130309A (en) * 1991-04-12 1992-07-14 A. H. Robins Company, Incorporated Aryloxy and aryloxyalklazetidines as antiarrhythmic and anticonvulsant agents
GB9425211D0 (en) 1994-12-14 1995-02-15 Ucb Sa Substituted 1H-imidazoles
GB9520150D0 (en) 1995-10-03 1995-12-06 Orion Yhtymae Oy New imidazole derivatives
US6841684B2 (en) 1997-12-04 2005-01-11 Allergan, Inc. Imidiazoles having reduced side effects
GB0007884D0 (en) * 2000-03-31 2000-05-17 Pfizer Ltd Diphenyl ether compounds useful in therapy
DE102004061748A1 (de) * 2004-12-22 2006-07-06 Bayer Healthcare Ag Azetidin-substituierte Pyrazoline
CN101616902B (zh) 2007-02-15 2013-03-27 弗·哈夫曼-拉罗切有限公司 作为taar1配体的2-氨基*唑啉类化合物
JP2010527980A (ja) * 2007-05-22 2010-08-19 プロシディオン・リミテッド 代謝障害を治療するための二環状アリールおよびヘテロアリール化合物
BRPI0813837A2 (pt) * 2007-07-27 2015-01-06 Hoffmann La Roche 2-azetidinametanoaminas e 2-pirrolidinametanoaminas como ligantes de taar
US8575364B2 (en) * 2008-10-30 2013-11-05 Janssen Pharmaceutica Nv Modulators of serotonin receptor
US20120165304A1 (en) * 2008-11-27 2012-06-28 Boehringer Ingelheim International Gmbh 6,7,8,9-Tetrahydro-5H-1,4,7,10a-tetraaza-cyclohept[f]indene derivatives, pharmaceutical compositions containing these compounds, their use and processes for preparing them
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WO2013170072A2 (en) * 2012-05-09 2013-11-14 Neurop, Inc. Compounds for the treatment of neurological disorders

Also Published As

Publication number Publication date
JP6539724B2 (ja) 2019-07-03
EP3186224A1 (en) 2017-07-05
KR20170031763A (ko) 2017-03-21
JP2017526661A (ja) 2017-09-14
KR101894681B1 (ko) 2018-09-04
BR112017000160A2 (pt) 2017-10-31
CA2954098A1 (en) 2016-03-03
CN107001259B (zh) 2019-12-06
RU2017107521A3 (es) 2019-01-22
US10023559B2 (en) 2018-07-17
EP3186224B1 (en) 2021-04-21
CN107001259A (zh) 2017-08-01
WO2016030310A1 (en) 2016-03-03
US20170144994A1 (en) 2017-05-25
RU2017107521A (ru) 2018-10-01

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