ES2721286T3 - Derivados heterociclialquinos y su uso como moduladores de los receptores mGluR5 - Google Patents

Derivados heterociclialquinos y su uso como moduladores de los receptores mGluR5 Download PDF

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Publication number
ES2721286T3
ES2721286T3 ES15822958T ES15822958T ES2721286T3 ES 2721286 T3 ES2721286 T3 ES 2721286T3 ES 15822958 T ES15822958 T ES 15822958T ES 15822958 T ES15822958 T ES 15822958T ES 2721286 T3 ES2721286 T3 ES 2721286T3
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Spain
Prior art keywords
group
optionally substituted
alkyl
modulators
formula
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ES15822958T
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English (en)
Inventor
Carlo Riva
Patrizia Angelico
Elena Poggessi
Toma Carlo De
Davide Graziani
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Recordati Ireland Ltd
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Recordati Ireland Ltd
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    • 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
    • A61K31/41Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having five-membered rings with two or more ring hetero atoms, at least one of which being nitrogen, e.g. tetrazole
    • A61K31/42Oxazoles
    • A61K31/424Oxazoles condensed with heterocyclic ring systems, e.g. clavulanic acid
    • 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
    • A61K31/435Heterocyclic compounds having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins having six-membered rings with one nitrogen as the only ring hetero atom
    • A61K31/44Non condensed pyridines; Hydrogenated derivatives thereof
    • A61K31/445Non condensed piperidines, e.g. piperocaine
    • A61K31/4523Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems
    • A61K31/454Non condensed piperidines, e.g. piperocaine containing further heterocyclic ring systems containing a five-membered ring with nitrogen as a ring hetero atom, e.g. pimozide, domperidone
    • 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
    • A61K31/53771,4-Oxazines, e.g. morpholine not condensed and containing further heterocyclic rings, e.g. timolol
    • 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
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/28Drugs 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
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P25/00Drugs for disorders of the nervous system
    • A61P25/30Drugs for disorders of the nervous system for treating abuse or dependence
    • AHUMAN NECESSITIES
    • A61MEDICAL OR VETERINARY SCIENCE; HYGIENE
    • A61PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
    • A61P43/00Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • 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

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  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Veterinary Medicine (AREA)
  • Public Health (AREA)
  • Medicinal Chemistry (AREA)
  • Animal Behavior & Ethology (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • Engineering & Computer Science (AREA)
  • Epidemiology (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • General Chemical & Material Sciences (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Biomedical Technology (AREA)
  • Neurology (AREA)
  • Neurosurgery (AREA)
  • Psychiatry (AREA)
  • Addiction (AREA)
  • Hospice & Palliative Care (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

Un compuesto de fórmula I **Fórmula** o un enantiómero, diastereómero o una sal farmacéuticamente aceptable del mismo en el que: R1 es un grupo CO opcionalmente sustituido por uno o más grupos o sustituyentes R2; R2 está ausente o es un grupo heterocíclico C1-C9 mono o bicíclico opcionalmente sustituido que contiene de 1 a 3 heteroátomos seleccionados entre nitrógeno, oxígeno y azufre, un grupo arilo C6-C14 mono, bi o tricíclico opcionalmente sustituido, o un grupo opcionalmente sustituido escogido entre alquilo, cicloalquilo, alcoxi, cicloalcoxi, ariloxi, heteroariloxi, alquiltio, amino, N-alquilamino, N,N-dialquilamino o N-alquil-N-alcoxiamino; R3 es un grupo fenilo o piridilo opcionalmente sustituido, seleccionándose dichos sustituyentes opcionales de un grupo haluro o de un grupo alquilo C1-C10, y siendo n igual a 1.
ES15822958T 2014-12-29 2015-12-29 Derivados heterociclialquinos y su uso como moduladores de los receptores mGluR5 Active ES2721286T3 (es)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US201462097482P 2014-12-29 2014-12-29
PCT/EP2015/081337 WO2016107865A1 (en) 2014-12-29 2015-12-29 Heterocyclylalkyne derivatives and their use as modulators of mglur5 receptors

Publications (1)

Publication Number Publication Date
ES2721286T3 true ES2721286T3 (es) 2019-07-30

Family

ID=55080108

Family Applications (1)

Application Number Title Priority Date Filing Date
ES15822958T Active ES2721286T3 (es) 2014-12-29 2015-12-29 Derivados heterociclialquinos y su uso como moduladores de los receptores mGluR5

Country Status (16)

Country Link
US (2) US9593127B2 (es)
EP (1) EP3240792B1 (es)
JP (1) JP6691127B2 (es)
KR (1) KR20170100656A (es)
CN (1) CN107406461B (es)
AU (1) AU2015373392B2 (es)
BR (1) BR112017014226A2 (es)
CA (1) CA2972668A1 (es)
EA (1) EA035237B1 (es)
ES (1) ES2721286T3 (es)
IL (1) IL253227A0 (es)
MX (1) MX2017008639A (es)
PH (1) PH12017501209A1 (es)
SG (1) SG11201705355VA (es)
WO (1) WO2016107865A1 (es)
ZA (1) ZA201704416B (es)

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
PL202623B1 (pl) 2000-06-28 2009-07-31 Smithkline Beecham Plc Sposób wytwarzania drobno zmielonego preparatu substancji leczniczej, drobno zmielona substancja lecznicza wytworzona tym sposobem i zawierająca ją kompozycja farmaceutyczna
GB0413605D0 (en) * 2004-06-17 2004-07-21 Addex Pharmaceuticals Sa Novel compounds
EP2414340A1 (en) * 2009-04-03 2012-02-08 Dainippon Sumitomo Pharma Co., Ltd. Compounds for treating disorders mediated by metabotropic glutamate receptor 5, and methods of use thereof
TW201116532A (en) * 2009-08-05 2011-05-16 Merz Pharma Gmbh & Co Kgaa Metabotropic glutamate receptor modulators
KR101862626B1 (ko) * 2010-07-09 2018-05-31 레코르다티 아일랜드 리미티드 Mglu5 대항체로서의 신 스피로헤테로사이클릭 화합물
CA2806103A1 (en) * 2010-08-31 2012-03-08 Vanderbilt University Bicyclic oxazole and thiazole compounds and their use as allosteric modulators of mglur5 receptors

Also Published As

Publication number Publication date
KR20170100656A (ko) 2017-09-04
PH12017501209A1 (en) 2017-10-18
ZA201704416B (en) 2019-06-26
AU2015373392A1 (en) 2017-08-17
US20160185798A1 (en) 2016-06-30
EP3240792B1 (en) 2019-01-23
EA201791439A1 (ru) 2018-02-28
MX2017008639A (es) 2018-05-28
US9889121B2 (en) 2018-02-13
IL253227A0 (en) 2017-08-31
WO2016107865A1 (en) 2016-07-07
EA035237B1 (ru) 2020-05-19
CA2972668A1 (en) 2016-07-07
NZ734071A (en) 2018-08-31
CN107406461B (zh) 2020-03-13
US9593127B2 (en) 2017-03-14
JP2018500371A (ja) 2018-01-11
CN107406461A (zh) 2017-11-28
SG11201705355VA (en) 2017-08-30
EP3240792A1 (en) 2017-11-08
JP6691127B2 (ja) 2020-04-28
US20170182011A1 (en) 2017-06-29
BR112017014226A2 (pt) 2018-03-06
AU2015373392B2 (en) 2020-05-14

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