AR078173A1 - BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USE - Google Patents
BIFENYLOXIMETHYL DIHIDRO OXAZOLOPIRIMIDINONES REPLACED, ITS PREPARATION AND USEInfo
- 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
Links
Classifications
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- 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
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.
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) |
Families Citing this family (26)
Publication number | Priority date | Publication date | Assignee | Title |
---|---|---|---|---|
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 |
TWI445532B (en) | 2007-09-14 | 2014-07-21 | Janssen Pharmaceuticals Inc | 1',3'-disubstituted-4-phenyl-3,4,5,6-tetrahydro-2h, 1'h-[1,4'] bipyridinyl-2'-ones |
JP5433579B2 (en) | 2007-09-14 | 2014-03-05 | 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. | 1,3-disubstituted-4-phenyl-1H-pyridin-2-one |
CA2735764C (en) | 2008-09-02 | 2016-06-14 | Ortho-Mcneil-Janssen Pharmaceuticals, Inc. | 3-azabicyclo[3.1.0]hexyl derivatives as modulators of metabotropic glutamate receptors |
ES2466341T3 (en) | 2008-10-16 | 2014-06-10 | Janssen Pharmaceuticals, Inc. | Indole and benzomorpholine derivatives as modulators of metabotropic glutamate receptors |
WO2010060589A1 (en) | 2008-11-28 | 2010-06-03 | 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 |
SG176018A1 (en) | 2009-05-12 | 2011-12-29 | Janssen Pharmaceuticals Inc | 1,2,4-triazolo[4,3-a]pyridine derivatives and their use as positive allosteric modulators of mglur2 receptors |
MX2011011964A (en) | 2009-05-12 | 2012-02-23 | 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 |
JP5852666B2 (en) | 2010-11-08 | 2016-02-03 | ジヤンセン・フアーマシユーチカルズ・インコーポレーテツド | 1,2,4-Triazolo [4,3-a] pyridine derivatives and their use as positive allosteric modulators of the mGluR2 receptor |
PL2649069T3 (en) | 2010-11-08 | 2016-01-29 | Janssen Pharmaceuticals Inc | 1,2,4-TRIAZOLO[4,3-a]PYRIDINE DERIVATIVES AND THEIR USE AS POSITIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS |
ES2536433T3 (en) | 2010-11-08 | 2015-05-25 | 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 |
WO2014090362A1 (en) * | 2012-12-12 | 2014-06-19 | 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 |
CA3188691A1 (en) | 2013-10-04 | 2015-04-09 | Novartis Ag | 3'end caps for rnai agents for use in rna interference |
DK3096790T3 (en) | 2014-01-21 | 2019-10-07 | Janssen Pharmaceutica Nv | COMBINATIONS INCLUDING POSITIVE ALLOSTERIC MODULATORS OR ORTHOSTERIC AGONISTS OF METABOTROP GLUTAMATERG SUBTYPE 2 RECEPTOR AND APPLICATION OF THESE |
UA127921C2 (en) | 2014-01-21 | 2024-02-14 | Янссен Фармацевтика Нв | Combinations containing positive allosteric modulators or orthosteric agonists 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 |
US11945785B2 (en) | 2021-12-30 | 2024-04-02 | Biomea Fusion, Inc. | Pyrazine compounds as inhibitors of FLT3 |
Family Cites Families (1)
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 |
-
2010
- 2010-09-13 AR ARP100103339A patent/AR078173A1/en unknown
- 2010-09-14 WO PCT/US2010/048687 patent/WO2011034828A1/en active Application Filing
- 2010-09-14 TW TW099130957A patent/TW201121978A/en unknown
Also Published As
Publication number | Publication date |
---|---|
WO2011034828A1 (en) | 2011-03-24 |
TW201121978A (en) | 2011-07-01 |
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