PE20150629A1 - Derivados de etinilo como moduladores de la actividad del receptor de mglur5 - Google Patents

Derivados de etinilo como moduladores de la actividad del receptor de mglur5

Info

Publication number
PE20150629A1
PE20150629A1 PE2015000396A PE2015000396A PE20150629A1 PE 20150629 A1 PE20150629 A1 PE 20150629A1 PE 2015000396 A PE2015000396 A PE 2015000396A PE 2015000396 A PE2015000396 A PE 2015000396A PE 20150629 A1 PE20150629 A1 PE 20150629A1
Authority
PE
Peru
Prior art keywords
disease
modulators
receptor activity
phenyletinyl
methanone
Prior art date
Application number
PE2015000396A
Other languages
English (en)
Inventor
Georg Jaeschke
Lothar Lindemann
Antonio Ricci
Daniel Rueher
Heinz Stadler
Eric Vieira
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 PE20150629A1 publication Critical patent/PE20150629A1/es

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

SE REFIERE A DERIVADOS DE ETINILO DE FORMULA (I) DONDE Y ES N O CH; R1 ES F O Cl; R2 ES H O METILO, O UNA SAL DE ADICION DE ACIDO FARMACEUTICAMENTE ACEPTABLE. SON COMPUESTOS PREFERIDOS: (3,3-DIMETIL-MORFOLIN-4-IL)-[5-(3-CLORO-FENILETINIL)-PIRIMIDIN-2-IL]-METANONA; [5-(3-CLORO-FENILETINIL)-PIRIDIN-2-IL]-MORFOLIN-4-IL-METANONA; ENTRE OTROS. TAMBIEN SE REFIERE A UN PROCEDIMIENTO DE PREPARACION Y A UNA COMPOSICION FARMACEUTICA. DICHOS COMPUESTOS SON ANTAGONISTAS DEL RECEPTOR DE GLUTAMATO METABOTROPICO (MODULADORES ALOSTERICOS NEGATIVOS) SIENDO UTILES PARA EL TRATAMIENTO DE LA ANSIEDAD Y EL DOLOR, LA DEPRESION, TRASTORNOS DEL ESPECTRO AUTISTA, LA ENFERMEDAD DE PARKINSON, Y LA ENFERMEDAD DEL REFLUJO GASTROESOFAGICO (GERD)
PE2015000396A 2012-10-18 2013-10-15 Derivados de etinilo como moduladores de la actividad del receptor de mglur5 PE20150629A1 (es)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
EP12188940 2012-10-18

Publications (1)

Publication Number Publication Date
PE20150629A1 true PE20150629A1 (es) 2015-05-11

Family

ID=47049067

Family Applications (1)

Application Number Title Priority Date Filing Date
PE2015000396A PE20150629A1 (es) 2012-10-18 2013-10-15 Derivados de etinilo como moduladores de la actividad del receptor de mglur5

Country Status (27)

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

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 (en) * 2015-09-25 2017-03-30 The United States Of America, As Represented By The Secretary, Department Of Health And Human Services Triazole derivatives as p2y14 receptor antagonists
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 (en) * 2011-09-26 2013-04-04 Vanderbilt University Substitued 5-(prop-1-yn-1-yl)picolinamide analogs as allosteric modulators of mglur5 receptors

Also Published As

Publication number Publication date
CA2882520A1 (en) 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 (en) 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 (en) 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
MA38012B1 (fr) 2016-12-30
UA114529C2 (uk) 2017-06-26
KR101684816B1 (ko) 2016-12-20
CN104718192A (zh) 2015-06-17
EP2909180B1 (en) 2016-10-05
CO7200248A2 (es) 2015-02-27
ZA201500856B (en) 2016-08-31
TWI490208B (zh) 2015-07-01
EA201590699A1 (ru) 2015-07-30

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