MA38012B1 - Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 - Google Patents

Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5

Info

Publication number
MA38012B1
MA38012B1 MA38012A MA38012A MA38012B1 MA 38012 B1 MA38012 B1 MA 38012B1 MA 38012 A MA38012 A MA 38012A MA 38012 A MA38012 A MA 38012A MA 38012 B1 MA38012 B1 MA 38012B1
Authority
MA
Morocco
Prior art keywords
modulators
ethynyl derivatives
receptor activity
mglur5 receptor
disease
Prior art date
Application number
MA38012A
Other languages
English (en)
Other versions
MA38012A1 (fr
Inventor
Heinz Stadler
Eric Vieira
Georg Jaeschke
Lothar Lindemann
Antonio Ricci
Daniel Rueher
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 MA38012A1 publication Critical patent/MA38012A1/fr
Publication of MA38012B1 publication Critical patent/MA38012B1/fr

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D413/00—Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D413/02—Heterocyclic 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
    • C07D413/06—Heterocyclic 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 carbon chain containing only aliphatic carbon atoms
    • 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
    • A61P1/04—Drugs for disorders of the alimentary tract or the digestive system for ulcers, gastritis or reflux esophagitis, e.g. antacids, inhibitors of acid secretion, mucosal protectants
    • 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
    • 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
    • A61P25/04—Centrally acting analgesics, e.g. opioids
    • 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
    • A61P25/22—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
    • A61P43/00—Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D213/00—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members
    • C07D213/02—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members
    • C07D213/04—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D213/60—Heterocyclic compounds containing six-membered rings, not condensed with other rings, with one nitrogen atom as the only ring hetero atom and three or more double bonds between ring members or between ring members and non-ring members having three double bonds between ring members or between ring members and non-ring members having no bond between the ring nitrogen atom and a non-ring member or having only hydrogen or carbon atoms directly attached to the ring nitrogen atom with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
    • C07D213/78—Carbon atoms having three bonds to hetero atoms, with at the most one bond to halogen, e.g. ester or nitrile radicals
    • C07D213/81—Amides; Imides

Abstract

La présente invention concerne des dérivés d'éthynyle de formule (i) dans laquelle y est un groupe n ou ch, r1 est un groupe fluoro ou chloro, r2 est un groupe hydrogène ou méthyle ou leur sel d'addition aux acides pharmaceutiquement acceptable, leur mélange racémique, ou leur énantiomère et/ou isomère optique et/ou stéréoisomère correspondant. Il a été découvert avec surprise que les composés de formule générale i sont des antagonistes des récepteurs métabotropes au glutamate (modulateurs allostériques négatifs) destinés à être utilisés dans le traitement de l'anxiété et de la douleur, de la dépression, du syndrome de l'x fragile, des troubles du spectre autistique, de la maladie de parkinson et de la maladie du reflux gastro-oesophagien).
MA38012A 2012-10-18 2015-04-17 Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5 MA38012B1 (fr)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
EP12188940 2012-10-18
PCT/EP2013/071500 WO2014060398A1 (fr) 2012-10-18 2013-10-15 Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5

Publications (2)

Publication Number Publication Date
MA38012A1 MA38012A1 (fr) 2016-05-31
MA38012B1 true MA38012B1 (fr) 2016-12-30

Family

ID=47049067

Family Applications (1)

Application Number Title Priority Date Filing Date
MA38012A MA38012B1 (fr) 2012-10-18 2015-04-17 Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5

Country Status (27)

Country Link
US (1) US9227959B2 (fr)
EP (1) EP2909180B1 (fr)
JP (1) JP5989250B2 (fr)
KR (1) KR101684816B1 (fr)
CN (1) CN104718192B (fr)
AR (1) AR093042A1 (fr)
AU (1) AU2013333988B2 (fr)
BR (1) BR112015006454A8 (fr)
CA (1) CA2882520A1 (fr)
CL (1) CL2015000891A1 (fr)
CO (1) CO7200248A2 (fr)
CR (1) CR20150144A (fr)
EA (1) EA025667B1 (fr)
ES (1) ES2599553T3 (fr)
HK (1) HK1207639A1 (fr)
IL (1) IL237380A (fr)
MA (1) MA38012B1 (fr)
MX (1) MX2015004898A (fr)
MY (1) MY168937A (fr)
NZ (1) NZ705144A (fr)
PE (1) PE20150629A1 (fr)
PH (1) PH12015500398A1 (fr)
SG (1) SG11201501392TA (fr)
TW (1) TWI490208B (fr)
UA (1) UA114529C2 (fr)
WO (1) WO2014060398A1 (fr)
ZA (1) ZA201500856B (fr)

Families Citing this family (8)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
EA026941B1 (ru) * 2012-10-18 2017-06-30 Ф. Хоффманн-Ля Рош Аг ПРОИЗВОДНЫЕ ЭТИНИЛА В КАЧЕСТВЕ МОДУЛЯТОРОВ АКТИВНОСТИ РЕЦЕПТОРА mGluR5
PE20180358A1 (es) 2015-06-03 2018-02-21 Hoffmann La Roche Derivados de etinilo
WO2017053769A1 (fr) * 2015-09-25 2017-03-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Utilisation de dérivés de triazole comme antagonistes du récepteur p2y14
US10849907B2 (en) 2017-12-08 2020-12-01 Boehringer Ingelheim International Gmbh Imidazopyridine derivatives and the use thereof as medicament
CN112867508B (zh) 2018-10-17 2023-09-15 勃林格殷格翰国际有限公司 4-吡啶基甲基-吗啉衍生物及其作为药物的用途
CN112888684B (zh) * 2018-10-17 2023-10-10 勃林格殷格翰国际有限公司 4-嘧啶-5-基甲基-吗啉衍生物及其作为药物的用途
PE20211278A1 (es) * 2018-10-17 2021-07-19 Boehringer Ingelheim Int Derivados de 4-pirazin-2-ilmetil-morfolina y su uso como medicamento
CN113950478B (zh) 2019-06-04 2024-02-02 勃林格殷格翰国际有限公司 作为nr2b负向调节剂的嘌呤衍生物及其作为药物的用途，特别是用于治疗抑郁病症

Family Cites Families (6)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
TW544448B (en) * 1997-07-11 2003-08-01 Novartis Ag Pyridine derivatives
UA80888C2 (en) * 2003-06-05 2007-11-12 Hoffmann La Roche Imidazole derivatives as glutmate receptor antagonists
MX2009013169A (es) * 2007-06-03 2010-04-30 Univ Vanderbilt Moduladores alostericos positivos del mglur5 benzamida y metodos de elaboracion y uso de los mismos.
US8853392B2 (en) * 2007-06-03 2014-10-07 Vanderbilt University Benzamide mGluR5 positive allosteric modulators and methods of making and using same
US8389536B2 (en) * 2009-10-27 2013-03-05 Hoffmann-La Roche Inc. Positive allosteric modulators (PAM)
WO2013049255A1 (fr) * 2011-09-26 2013-04-04 Vanderbilt University Analogues de 5-(prop-1-yn-1-yl)picolinamide substitué comme modulateurs allostériques des récepteurs de mglur5

Also Published As

Publication number Publication date
CA2882520A1 (fr) 2014-04-24
AU2013333988B2 (en) 2017-03-09
MX2015004898A (es) 2015-07-21
CR20150144A (es) 2015-04-30
NZ705144A (en) 2018-09-28
EA025667B1 (ru) 2017-01-30
JP5989250B2 (ja) 2016-09-07
MY168937A (en) 2019-01-10
ES2599553T3 (es) 2017-02-02
WO2014060398A1 (fr) 2014-04-24
AR093042A1 (es) 2015-05-13
TW201420571A (zh) 2014-06-01
BR112015006454A8 (pt) 2019-08-20
IL237380A (en) 2017-02-28
CL2015000891A1 (es) 2015-09-11
US9227959B2 (en) 2016-01-05
KR20150055044A (ko) 2015-05-20
PH12015500398B1 (en) 2015-04-27
CN104718192B (zh) 2016-08-31
PH12015500398A1 (en) 2015-04-27
MA38012A1 (fr) 2016-05-31
EP2909180A1 (fr) 2015-08-26
JP2015531392A (ja) 2015-11-02
SG11201501392TA (en) 2015-05-28
BR112015006454A2 (pt) 2017-07-04
IL237380A0 (en) 2015-04-30
AU2013333988A1 (en) 2015-02-26
HK1207639A1 (zh) 2016-02-05
US20150225385A1 (en) 2015-08-13
UA114529C2 (uk) 2017-06-26
PE20150629A1 (es) 2015-05-11
KR101684816B1 (ko) 2016-12-20
CN104718192A (zh) 2015-06-17
EP2909180B1 (fr) 2016-10-05
CO7200248A2 (es) 2015-02-27
ZA201500856B (en) 2016-08-31
TWI490208B (zh) 2015-07-01
EA201590699A1 (ru) 2015-07-30

Similar Documents

Publication Publication Date Title
MA38012B1 (fr) Dérivés d'éthynyle comme modulateurs de l'activité des récepteurs mglur5
MA42442A (fr) Dérivés d'éthynyle comme modulateurs du récepteur métabotropique au glutamate
MA35133B1 (fr) Dérivés d'éthynyle comme modulateurs allostériques positifs de mglur5
KR101725696B1 (ko) 신규한 이환형 피리딘온
MA35062B1 (fr) Dérivés d'amines hétérocycliques
MA35192B1 (fr) Derives de pyrazole
EA201070535A1 (ru) Новые агонисты глюкокортикоидных рецепторов
MA38272A1 (fr) Peptides en tant qu'agonistes de l'oxytocine
MA38885A1 (fr) Dérivés d'éthynyle modulateurs allosteriques positifs (pam) du recepteur metabotropique du glutamate 4 (mglu4)
MA38659B1 (fr) Dérivés éthynyle comme antagonistes du récepteur métabotrope du glutamate
US20190382354A1 (en) PHENYL AND PYRIDINYL SUBSTITUTED IMIDAZOLES AS MODULATORS OF RORyT
MA35113B1 (fr) 5-(phényl/pyridinyl-éthinyl)-2-pyridine/2 pyrimidine-carboxamides comme modulateur de mglur5
MA38011B1 (fr) Dérivés d'éthynyle comme modulateurs de l'activité du récepteur mglur5
MA29809B1 (fr) N-[1,3,4]-thiadiazol-2-yl-benzenesulfonamides,procedes pour leur preparation et leur utilisation en tant que produits pharmaceutiques
PH12015500346A1 (en) Ethynyl derivatives as modulators of mglur5 receptor activity
WO2018098128A1 (fr) Traitement de troubles du spectre autistique, de troubles obsessivo-compulsifs et de troubles de l'anxiété
MA37895A1 (fr) Dérivés d'aryléthynylpyrimidine substitués modulateurs allostériques du récepteur métabotrope 5 de glutamate, utiles pour le traitement, par ex. Schizophrénie, maladies cognitives, syndrome x fragile, autisme, psychose et obésité
MA38229B1 (fr) Derives d'aminocyclobutane, leur procede de preparation et leur utilisation a titre de medicaments
RU2008152764A (ru) Биарилкарбоксиариламиды как модуляторы ванилоидного рецептора типа 1
MA42508B1 (fr) Dérivés d'éthynyle
WO2012084873A1 (fr) Esters d'acides 4-(hétéro)aryl-éthynyl-octahydro-indole-1-carboxyliques
MA34251B1 (fr) Derives amido-tropane