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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

Info

Publication number
AR078172A1
AR078172A1 ARP100103338A ARP100103338A AR078172A1 AR 078172 A1 AR078172 A1 AR 078172A1 AR P100103338 A ARP100103338 A AR P100103338A AR P100103338 A ARP100103338 A AR P100103338A AR 078172 A1 AR078172 A1 AR 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 Aventis filed Critical Sanofi Aventis
Publication of AR078172A1 publication Critical patent/AR078172A1/en

Links

Classifications

    • C—CHEMISTRY; METALLURGY
    • C07—ORGANIC CHEMISTRY
    • C07D—HETEROCYCLIC COMPOUNDS
    • C07D498/00—Heterocyclic compounds containing in the condensed system at least one hetero ring having nitrogen and oxygen atoms as the only ring hetero atoms
    • C07D498/02—Heterocyclic 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
    • C07D498/04—Ortho-condensed systems
    • 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
    • A61P25/06—Antimigraine agents
    • 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
    • A61P25/18—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
    • A61P25/24—Antidepressants

Landscapes

  • Health & Medical Sciences (AREA)
  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Engineering & Computer Science (AREA)
  • Bioinformatics & Cheminformatics (AREA)
  • General Chemical & Material Sciences (AREA)
  • Nuclear Medicine, Radiotherapy & Molecular Imaging (AREA)
  • Neurosurgery (AREA)
  • Biomedical Technology (AREA)
  • Chemical Kinetics & Catalysis (AREA)
  • Veterinary Medicine (AREA)
  • Medicinal Chemistry (AREA)
  • Neurology (AREA)
  • Public Health (AREA)
  • Pharmacology & Pharmacy (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Animal Behavior & Ethology (AREA)
  • General Health & Medical Sciences (AREA)
  • Pain & Pain Management (AREA)
  • Psychiatry (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)

Abstract

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.

ARP100103338A 2009-09-15 2010-09-13 PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLUR AR078172A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24258909P 2009-09-15 2009-09-15
FR1055808 2010-07-16

Publications (1)

Publication Number Publication Date
AR078172A1 true AR078172A1 (en) 2011-10-19

Family

ID=43014314

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103338A AR078172A1 (en) 2009-09-15 2010-09-13 PHENOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED AND USE OF THE SAME AS MODULATORS OF METABOTROPIC RECEPTORS OF MGLUR

Country Status (3)

Country Link
AR (1) AR078172A1 (en)
TW (1) TW201124421A (en)
WO (1) WO2011034832A1 (en)

Families Citing this family (22)

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TWI417095B (en) 2006-03-15 2013-12-01 Janssen Pharmaceuticals Inc 1,4-disubstituted 3-cyano-pyridone derivatives and their use as positive allosteric modulators of mglur2-receptors
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
AU2008297877C1 (en) 2007-09-14 2013-11-07 Addex Pharma S.A. 1,3-disubstituted-4-phenyl-1 H-pyridin-2-ones
ES2356032T3 (en) 2007-09-14 2011-04-04 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. 4-PHENYL-3,4,5,6-TETRAHIDRO-2H, 1'H- [1,4 '] BIPIRIDINIL-2'-ONAS 1,3'-DISUSTITUTED.
JP5547194B2 (en) 2008-09-02 2014-07-09 ジャンセン ファーマシューティカルズ， インコーポレイテッド． 3-Azabicyclo [3.1.0] hexyl derivatives as modulators of metabotropic glutamate receptors
RU2517181C2 (en) 2008-10-16 2014-05-27 Орто-Макнейл-Янссен Фармасьютикалз, Инк. Indole and benzomorpholine derivatives as modulator of metabotropic glutamate receptors
CN102232074B (en) 2008-11-28 2014-12-03 奥梅-杨森制药有限公司 Indole and benzoxazine derivatives as modulators of metabotropic glutamate receptors
BRPI1010831A2 (en) 2009-05-12 2016-04-05 Addex Pharmaceuticals Sa 1,2,4-triazolo [4,3-a] pyridine derivatives and their as positive allosteric modulators of mglur2 receptors
MY153913A (en) 2009-05-12 2015-04-15 Janssen Pharmaceuticals Inc 7-aryl-1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors
MY161325A (en) 2009-05-12 2017-04-14 Janssen Pharmaceuticals Inc 1, 2, 4-triazolo[4,3-a]pyridine derivatives and their use for the treatment or prevention of neurological and psychiatric disorders
AR078171A1 (en) * 2009-09-15 2011-10-19 Sanofi Aventis DIHYDROBENZOCICLOALQUILOXIMETIL-OXAZOLOPIRIMIDINONES REPLACED, PREPARATION AND USE OF THE SAME
WO2012062751A1 (en) 2010-11-08 2012-05-18 Janssen Pharmaceuticals, Inc. 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
ES2552455T3 (en) 2010-11-08 2015-11-30 Janssen Pharmaceuticals, Inc. 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
ES2552879T3 (en) 2010-11-08 2015-12-02 Janssen Pharmaceuticals, Inc. 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
JP2015006994A (en) * 2011-10-28 2015-01-15 大正製薬株式会社 Dihydroimidazooxazole derivative
JO3368B1 (en) 2013-06-04 2019-03-13 Janssen Pharmaceutica Nv 6,7-DIHYDROPYRAZOLO[1,5-a]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
JO3367B1 (en) 2013-09-06 2019-03-13 Janssen Pharmaceutica Nv 1,2,4-TRIAZOLO[4,3-a]PYRIDINE COMPOUNDS AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS
KR20200126026A (en) 2014-01-21 2020-11-05 얀센 파마슈티카 엔.브이. Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
EP3431106B1 (en) 2014-01-21 2020-12-30 Janssen Pharmaceutica NV Combinations comprising positive allosteric modulators of metabotropic glutamatergic receptor subtype 2 and their use
TWI713497B (en) * 2015-02-26 2020-12-21 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
KR102672910B1 (en) * 2017-01-10 2024-06-07 오웬-배리 파머소티컬즈 인코포레이티드 anticonvulsant compounds

Family Cites Families (1)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
KR101547573B1 (en) 2007-03-09 2015-08-26 사노피 Substituted dihydro and tetrahydro oxazolopyrimidinones preparation and use thereof

Also Published As

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

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