AR078173A1 - BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USE - Google Patents

BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USE

Info

Publication number
AR078173A1
AR078173A1 ARP100103339A ARP100103339A AR078173A1 AR 078173 A1 AR078173 A1 AR 078173A1 AR P100103339 A ARP100103339 A AR P100103339A AR P100103339 A ARP100103339 A AR P100103339A AR 078173 A1 AR078173 A1 AR 078173A1
Authority
AR
Argentina
Prior art keywords
ring
fluoroethyl
hydrogen
group
disorders
Prior art date
Application number
ARP100103339A
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 AR078173A1 publication Critical patent/AR078173A1/en

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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
    • A61P25/14—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

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

Abstract

Los compuestos de la presente son moduladores alostéricos de receptores de glutamato metabotropico (mGluR), particularmente, el receptor mGluR2. Por lo tanto, los compuestos de ésta son utiles como agentes farmacéuticos, especialmente en el tratamiento y/o prevencion de una diversidad de trastornos del sistema nervioso central (SNC), incluyendo, pero sin limitacion, afecciones neurodegenerativas agudas y cronicas, psicosis, trastornos de déficit de la cognicion, convulsiones, ansiedad, depresion, migrana, dolor, trastornos del sueno y emesis. Reivindicacion 1: Un compuesto de la formula (1), donde: R1 está seleccionado del grupo que consiste en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo y propilo; R2 está seleccionado del grupo que consiste en hidrogeno, metilo, fluorometilo, etilo, 2-fluoroetilo, propilo, 1,1-difluoropropilo, metoximetilo, etoximetilo, 2-fluoroetoximetilo, etoxi-1-fluoroetilo, isopropoximetilo, fenilo, hidroximetilo, hidroxietilo, morfolinilmetilo, pirrolidinilmetilo, tetrahidrofuranilmetoximetilo, ciclopropilo y ciclopentiloximetilo; y R3, R4, R5, R6, R7 y R8 son iguales o diferentes y de forma independiente entre sí, están seleccionados del grupo que consiste en hidrogeno, halogeno, CF3, alquilo C1-4, cicloalquilo C3-6, alcoxi C1-4; o dos de R6, R7 y R8 están en carbonos adyacentes y tomados juntos con el anillo fenilo forman un anillo naftaleno; o dos de R6, R7 y R8 están en carbonos adyacentes y tomados junto con los carbonos a los que están unidos forman un anillo de cinco o seis miembros; o uno de R6, R7 y R8 se une con el anillo fenilo adyacente para formar un anillo fluorenilo; o una sal del mismo.The compounds herein are allosteric modulators of metabotropic glutamate (mGluR) receptors, particularly, the mGluR2 receptor. Therefore, its compounds are useful as pharmaceutical agents, especially in the treatment and / or prevention of a variety of disorders of the central nervous system (CNS), including, but not limited to, acute and chronic neurodegenerative conditions, psychosis, disorders of deficit of cognition, 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 and propyl; R2 is selected from the group consisting of hydrogen, methyl, fluoromethyl, ethyl, 2-fluoroethyl, propyl, 1,1-difluoropropyl, methoxymethyl, ethoxymethyl, 2-fluoroethoxymethyl, ethoxy-1-fluoroethyl, isopropoxymethyl, phenyl, hydroxymethyl, hydroxyethyl, morpholinylmethyl, pyrrolidinylmethyl, tetrahydrofuranylmethoxymethyl, cyclopropyl and cyclopentyloxymethyl; and R3, R4, R5, R6, R7 and R8 are the same or different and independently of each other, are selected from the group consisting of hydrogen, halogen, CF3, C1-4 alkyl, C3-6 cycloalkyl, C1-4 alkoxy ; or two of R6, R7 and R8 are in adjacent carbons and taken together with the phenyl ring form a naphthalene ring; or two of R6, R7 and R8 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 R6, R7 and R8 binds with the adjacent phenyl ring to form a fluorenyl ring; or a salt thereof.

ARP100103339A 2009-09-15 2010-09-13 BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USE AR078173A1 (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
US24258309P 2009-09-15 2009-09-15
FR1056266 2010-07-29

Publications (1)

Publication Number Publication Date
AR078173A1 true AR078173A1 (en) 2011-10-19

Family

ID=42988485

Family Applications (1)

Application Number Title Priority Date Filing Date
ARP100103339A AR078173A1 (en) 2009-09-15 2010-09-13 BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USE

Country Status (3)

Country Link
AR (1) AR078173A1 (en)
TW (1) TW201121978A (en)
WO (1) WO2011034828A1 (en)

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TW200845978A (en) 2007-03-07 2008-12-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-tetrahydropyran-phenyl)-pyridin-2-one derivatives
TW200900065A (en) 2007-03-07 2009-01-01 Janssen Pharmaceutica Nv 3-cyano-4-(4-pyridinyloxy-phenyl)-pyridin-2-one derivatives
BRPI0816767B8 (en) 2007-09-14 2021-05-25 Addex Pharmaceuticals Sa compound 4-phenyl-3,4,5,6-tetrahydro-2h,1'h-[1,4']bipyridinyl-2'-disubstituted 1',3'-ones, pharmaceutical composition and use of same
CN101801930B (en) 2007-09-14 2013-01-30 奥梅-杨森制药有限公司 1,3-disubstituted-4-phenyl-1 h-pyridin-2-ones
CN102143955B (en) 2008-09-02 2013-08-14 Omj制药公司 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors
JP5656848B2 (en) 2008-10-16 2015-01-21 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． Indole and benzomorpholine derivatives as metabotropic glutamate receptor modulators
CA2744138C (en) 2008-11-28 2015-08-11 Ortho-Mcneil-Janssen Pharmaceuticals, Inc. Indole and benzoxazine derivatives as modulators of metabotropic glutamate 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
RS53075B (en) 2009-05-12 2014-04-30 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
US8946205B2 (en) 2009-05-12 2015-02-03 Janssen Pharmaceuticals, Inc. 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mGluR2 receptors
AR078171A1 (en) * 2009-09-15 2011-10-19 Sanofi Aventis DIHYDROBENZOCICLOALQUILOXIMETIL-OXAZOLOPIRIMIDINONES REPLACED, PREPARATION AND USE OF THE SAME
WO2012062750A1 (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
US9012448B2 (en) 2010-11-08 2015-04-21 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
US9580653B2 (en) * 2012-12-12 2017-02-28 Merck Patent Gmbh Liquid-crystalline medium
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
WO2015050871A2 (en) 2013-10-04 2015-04-09 Novartis Ag Organic compounds to treat hepatitis b virus
CA2925129C (en) 2013-10-04 2023-04-04 Novartis Ag 3' end caps for rnai agents for use in rna interference
KR20220039824A (en) 2014-01-21 2022-03-29 얀센 파마슈티카 엔.브이. Combinations comprising positive allosteric modulators or orthosteric agonists of metabotropic glutamatergic receptor subtype 2 and their use
LT3431106T (en) 2014-01-21 2021-02-10 Janssen Pharmaceutica Nv Combinations comprising positive allosteric modulators of metabotropic glutamatergic receptor subtype 2 and their use
KR102103898B1 (en) * 2017-01-23 2020-04-24 주식회사 엘지화학 Additive for nonaqueous electrolyte, nonaqueous electrolyte for lithium secondary battery comprising the same, and lithium secondary battery
CN112724157B (en) * 2021-01-23 2022-04-19 中国科学院新疆理化技术研究所 Dihydrooxazolo [5,4-d ] pyrrolo [1,2-a ] pyrimidin-9 (5H) -one derivatives and use thereof
WO2023129667A1 (en) 2021-12-30 2023-07-06 Biomea Fusion, Inc. Pyrazine compounds as inhibitors of flt3

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EP2137193B1 (en) 2007-03-09 2017-08-09 Sanofi Substituted dihydro and tetrahydro oxazolopyrimidinones, preparation and use thereof

Also Published As

Publication number Publication date
WO2011034828A1 (en) 2011-03-24
TW201121978A (en) 2011-07-01

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