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AR078172A1 - PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLUR - Google Patents

PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLUR

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Publication number
AR078172A1
AR078172A1ARP100103338AARP100103338AAR078172A1AR 078172 A1AR078172 A1AR 078172A1AR P100103338 AARP100103338 AAR P100103338AAR P100103338 AARP100103338 AAR P100103338AAR 078172 A1AR078172 A1AR 078172A1
Authority
AR
Argentina
Prior art keywords
fluoroethyl
ethyl
hydrogen
group
mglur
Prior art date
Application number
ARP100103338A
Other languages
Spanish (es)
Original Assignee
Sanofi Aventis
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 Sanofi AventisfiledCriticalSanofi Aventis
Publication of AR078172A1publicationCriticalpatent/AR078172A1/en

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Abstract

Translated fromSpanish

Estos compuestos son moduladores de receptores metabotropicos de glutamato (mGluR), particularmente, el receptor mGluR2. Por tanto, son utiles como agentes farmacéuticos, especialmente en el tratamiento y/o prevencion de una diversidad de trastornos del sistema nervioso central (SNC), que incluyendo, pero sin limitacion, afecciones neurodegenerativas agudas y cronicas, psicosis, trastornos de déficit cognitivo, convulsiones, ansiedad, depresion, migrana, dolor, trastornos del sueno y emesis. Reivindicacion 1: Un compuesto de la formula (1): en donde: R1 está seleccionado del grupo consistente en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo, propilo, hidroxietilo, 2-(tetrahidro-piran-2-iloxi)-etilo; R2 está seleccionado del grupo consistente en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo, propilo, metoximetilo, etoximetilo, 2-fluoroetoximetilo, etoxi-1-fluoroetilo, isopropoximetilo, -COOH, fenilo, bencilo, 2-, 3-, 4-, o 5-fluorofenilo, 2-, 3-, 4-, o 5-fluorobencilo, 2,4-difluorofenilo, 2,4-difluoro-bencilo, fenoxi, benciloxi, 2-, 3-, 4-, o 5-fluorofenoxi, 2-, 3-, 4-, o 5-fluorobenciloxi, 2,4-difluorofenoxi, 2,4-difluorobenciloxi, hidroximetilo, hidroxietilo, morfolinilmetilo, pirrolidinilmetilo, piperidinilmetilo, tetrahidrofuranilmetoximetilo, fenilo, ciclopropilo, ciclopropilmetilo y ciclopentiloximetilo; y R3, R4 y R5 son iguales o diferentes y, de manera independiente entre sí, están seleccionados del grupo consistente en hidrogeno, halogeno, CF3, alquilo(C1-6), alcoxi(C1-6), ciclohexilo, 1-metilciclohexilo, 4-metoxi-ciclohexilo, 4,4'-difluorociclohexilo, ciclohexenilo, 4-fluoro-ciclohexenilo, biciclo[3.3.1]nonilo, biciclo[3.3.1]noniletilo, 1,1',1'',3,3',3ö-hexafluoro-2-hidroxi-propilo; o bien dos de R3, R4 y R5 están en carbonos adyacentes y tomados junto con los carbonos a los cuales están unidos forman un anillo de cinco o seis miembros; o una de sus sales, o uno de sus solvatos o uno de sus hidratos.These compounds are modulators of metabotropic glutamate receptors (mGluR), particularly the mGluR2 receptor. Therefore, they are useful as pharmaceutical agents, especially in the treatment and / or prevention of a variety of central nervous system (CNS) disorders, which including, but not limited to, acute and chronic neurodegenerative conditions, psychosis, cognitive deficit disorders, seizures, anxiety, depression, migraine, pain, sleep disorders and emesis. Claim 1: A compound of the formula (1): wherein: R1 is selected from the group consisting of hydrogen, methyl, fluoromethyl, ethyl, 2-fluoroethyl, propyl, hydroxyethyl, 2- (tetrahydro-pyran-2-yloxy) - ethyl; R2 is selected from the group consisting of hydrogen, methyl, fluoromethyl, ethyl, 2-fluoroethyl, propyl, methoxymethyl, ethoxymethyl, 2-fluoroethoxymethyl, ethoxy-1-fluoroethyl, isopropoxymethyl, -COOH, phenyl, benzyl, 2-, 3-, 4-, or 5-fluorophenyl, 2-, 3-, 4-, or 5-fluorobenzyl, 2,4-difluorophenyl, 2,4-difluoro-benzyl, phenoxy, benzyloxy, 2-, 3-, 4-, or 5-fluorophenoxy, 2-, 3-, 4-, or 5-fluorobenzyloxy, 2,4-difluorophenoxy, 2,4-difluorobenzyloxy, hydroxymethyl, hydroxyethyl, morpholinylmethyl, pyrrolidinylmethyl, piperidinylmethyl, tetrahydrofuranylmethoxymethyl, phenyl, cyclopropyl, cyclopropyl, cyclopropylmethyl and R3, R4 and R5 are the same or different and, independently of each other, are selected from the group consisting of hydrogen, halogen, CF3, (C1-6) alkyl, (C1-6) alkoxy, cyclohexyl, 1-methylcyclohexyl, 4-methoxy-cyclohexyl, 4,4'-difluorocyclohexyl, cyclohexenyl, 4-fluoro-cyclohexenyl, bicyclo [3.3.1] nonyl, bicyclo [3.3.1] nonylethyl, 1,1 ', 1' ', 3,3' , 3ö-hexafluoro-2-hydroxypropyl; or two of R3, R4 and R5 are in adjacent carbons and taken together with the carbons to which they are attached form a ring of five or six members; or one of its salts, or one of its solvates or one of its hydrates.

ARP100103338A2009-09-152010-09-13 PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLURAR078172A1 (en)

Applications Claiming Priority (2)

Application NumberPriority DateFiling DateTitle
US24258909P2009-09-152009-09-15
FR10558082010-07-16

Publications (1)

Publication NumberPublication Date
AR078172A1true AR078172A1 (en)2011-10-19

Family

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Family Applications (1)

Application NumberTitlePriority DateFiling Date
ARP100103338AAR078172A1 (en)2009-09-152010-09-13 PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLUR

Country Status (3)

CountryLink
AR (1)AR078172A1 (en)
TW (1)TW201124421A (en)
WO (1)WO2011034832A1 (en)

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TWI417095B (en)2006-03-152013-12-01Janssen Pharmaceuticals Inc1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mglur2-receptors
TW200845978A (en)2007-03-072008-12-01Janssen Pharmaceutica Nv3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en)2007-03-072009-01-01Janssen Pharmaceutica Nv3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200927731A (en)2007-09-142009-07-01Ortho Mcneil Janssen Pharm1,3-disubstituted-4-phenyl-1H-pyridin-2-ones
WO2009033704A1 (en)2007-09-142009-03-19Ortho-Mcneil-Janssen Pharmaceuticals, Inc.1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1, 4'] bipyridinyl-2'-ones
CA2735764C (en)2008-09-022016-06-14Ortho-Mcneil-Janssen Pharmaceuticals, Inc.3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
MX2011003691A (en)2008-10-162011-09-06Ortho Mcneil Janssen PharmIndole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors.
WO2010060589A1 (en)2008-11-282010-06-03Ortho-Mcneil-Janssen Pharmaceuticals, Inc.Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
MY153913A (en)2009-05-122015-04-15Janssen Pharmaceuticals Inc7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
EA020671B1 (en)2009-05-122014-12-30Янссен Фармасьютикалз, Инк.1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF mGluR2 RECEPTORS
SG176021A1 (en)2009-05-122011-12-29Janssen Pharmaceuticals Inc1,2,4-triazolo [4,3-a] pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
AR078171A1 (en)*2009-09-152011-10-19Sanofi Aventis DIHYDROBENZOCICLOALQUILOXIMETIL-OXAZOLOPIRIMIDINONES REPLACED, PREPARATION AND USE OF THE SAME
ES2552879T3 (en)2010-11-082015-12-02Janssen Pharmaceuticals, Inc. 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
EP2643320B1 (en)2010-11-082015-03-04Janssen Pharmaceuticals, Inc.1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
US9271967B2 (en)2010-11-082016-03-01Janssen Pharmaceuticals, Inc.1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
JP2015006994A (en)*2011-10-282015-01-15大正製薬株式会社Dihydroimidazooxazole derivative
JO3368B1 (en)2013-06-042019-03-13Janssen Pharmaceutica Nv 6, 7- dihydropyrazolu [5,1-a] pyrazine-4 (5 hands) -on compounds and their use as negative excretory regulators of Miglore 2 receptors.
JO3367B1 (en)2013-09-062019-03-13Janssen Pharmaceutica Nv1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
LT3431106T (en)2014-01-212021-02-10Janssen Pharmaceutica NvCombinations comprising positive allosteric modulators of metabotropic glutamatergic receptor subtype 2 and their use
AU2015208233B2 (en)2014-01-212019-08-29Janssen Pharmaceutica NvCombinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
TWI713497B (en)*2015-02-262020-12-21南韓商愛思開生物製藥股份有限公司Imidazopyrimidine and imidazotriazine derivative, and pharmaceutical composition comprising the same
CA3049800A1 (en)*2017-01-102018-07-19Owen-Barry Pharmaceuticals Inc.Anticonvulsant compounds

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EP2137193B1 (en)2007-03-092017-08-09SanofiSubstituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof

Also Published As

Publication numberPublication date
TW201124421A (en)2011-07-16
WO2011034832A1 (en)2011-03-24

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