- pyrrole logical sequence handkerchief nai intermediate preparation method (by machine translation)
-
The invention relates to a simple operation, raw materials are easy, and the production cost is low, the quality of the product is good and is suitable for the industrial production of the intermediate pyrrole logical sequence handkerchief nai 5 - (pyridine - 2 - yl) - 2 (1H) - pyridone of the preparation method. (by machine translation)
- -
-
-
- PROCESS FOR THE PREPARATION OF PERAMPANEL
-
The present invention relates to processes for the preparation of perampanel and its intermediates.
- -
-
Paragraph 0057-0058
(2016/04/26)
-
- Development of Novel PET Probes for Central 2-Amino-3-(3-hydroxy-5-methyl-4-isoxazolyl)propionic Acid Receptors
-
We document the development of PET probes for central AMPA receptors and their application to in vivo animal imaging. An initial screening of perampanel derivatives was performed to identify probe candidates. Despite the high autoradiographic contrast yie
- Oi, Norihito,Tokunaga, Masaki,Suzuki, Michiyuki,Nagai, Yuji,Nakatani, Yosuke,Yamamoto, Noboru,Maeda, Jun,Minamimoto, Takafumi,Zhang, Ming-Rong,Suhara, Tetsuya,Higuchi, Makoto
-
p. 8444 - 8462
(2015/11/24)
-
- PYRIDAZINE DERIVATIVES AS EAAT2 ACTIVATORS
-
Pyridazine derivatives that activate the excitatory amino acid transporter 2 (EAAT2), and methods of use thereof for treating or preventing diseases, disorders, and conditions associated with glutamate excitotoxicity.
- -
-
Page/Page column 34; 35
(2013/03/26)
-
- METHODS FOR PREPARING INTERMEDIATES OF PERAMPANEL
-
Methods for the synthesis of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula I or salts thereof are provided.
- -
-
Paragraph 0087
(2013/05/09)
-
- Process for the preparation of 2-alkoxy-5-(pyridin-2-yl)pyridine, an intermediate of perampanel
-
The present invention relates to a process for synthesising 2-alkoxy-5-(pyridin-2-yl)pyridine which is an intermediate of the synthesis of the active substance Perampenel.
- -
-
Paragraph 0064
(2013/05/09)
-
- Discovery of 2-(2-Oxo-1-phenyl-5-pyridin-2-yl-1,2-dihydropyridin-3-yl) benzonitrile (Perampanel): A novel, noncompetitive α-amino-3-hydroxy-5- methyl-4-isoxazolepropanoic acid (AMPA) receptor antagonist
-
Dysfunction of glutamatergic neurotransmission has been implicated in the pathogenesis of epilepsy and numerous other neurological diseases. Here we describe the discovery of a series of 1,3,5-triaryl-1H-pyridin-2-one derivatives as noncompetitive antagonists of AMPA-type ionotropic glutamate receptors. The structure-activity relationships for this series of compounds were investigated by manipulating individual aromatic rings located at positions 1, 3, and 5 of the pyridone ring. This culminated in the discovery of 2-(2-oxo-1-phenyl-5- pyridin-2-yl-1,2-dihydropyridin-3-yl)benzonitrile (perampanel, 6), a novel, noncompetitive AMPA receptor antagonist that showed potent activity in an in vitro AMPA-induced Ca2+ influx assay (IC50 = 60 nM) and in an in vivo AMPA-induced seizure model (minimum effective dose of 2 mg/kg po). Perampanel is currently in regulatory submission for partial-onset seizures associated with epilepsy.
- Hibi, Shigeki,Ueno, Koshi,Nagato, Satoshi,Kawano, Koki,Ito, Koichi,Norimine, Yoshihiko,Takenaka, Osamu,Hanada, Takahisa,Yonaga, Masahiro
-
p. 10584 - 10600
(2013/02/23)
-
- A practical, laboratory-scale synthesis of Perampanel
-
The orally active, noncompetitive, selective AMPA receptor antagonist Perampanel, 2-[1,6-dihydro-6-oxo-1-phenyl-(2,3-bipyridin)-5-yl]benzonitrile, has been prepared from readily available, relatively inexpensive starting materials. The synthesis was carried out on a laboratory scale with no specialized equipment, and involved only two chromatographic purifications. Georg Thieme Verlag Stuttgart. New York.
- McElhinny Jr., Charles J.,Carroll,Lewin, Anita H.
-
-
- Structure-activity relationship study of pyridazine derivatives as glutamate transporter EAAT2 activators
-
Excitatory amino acid transporter 2 (EAAT2) is the major glutamate transporter and functions to remove glutamate from synapses. A thiopyridazine derivative has been found to increase EAAT2 protein levels in astrocytes. A structure-activity relationship study revealed that several components of the molecule were required for activity, such as the thioether and pyridazine. Modification of the benzylthioether resulted in several derivatives (7-13, 7-15 and 7-17) that enhanced EAAT2 levels by >6-fold at concentrations 50 of 0.5 μM.
- Xing, Xuechao,Chang, Ling-Chu,Kong, Qiongman,Colton, Craig K.,Lai, Liching,Glicksman, Marcie A.,Lin, Chien-Liang Glenn,Cuny, Gregory D.
-
scheme or table
p. 5774 - 5777
(2011/10/18)
-
- PRODUCTION PROCESS OF 2,3'-BIPYRIDYL-6'-ONE
-
A production process where 2,3′-bipyridyl-6′-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3′-bipyridyl-6′-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
- -
-
Page/Page column 11
(2010/02/17)
-
- PROCESS FOR PRODUCTION OF 2,3'-BIPYRIDYL-6'-ONE
-
A production process where 2,3'-bipyridyl-6'-one can be produced in high purity at low cost on an industrial scale without using an expensive catalyst or special equipment is provided. A process for producing 2,3'-bipyridyl-6'-one comprises reacting an acetylpyridine derivative with at least one of compounds represented by formulae (II) to (V) to synthesize a bipyridine derivative and hydrolyzing the bipyridine derivative by one-pot preparation. In formulae (II) to (V), each of R2 to R8, X and Y represents a given group.
- -
-
Page/Page column 17
(2009/12/07)
-
- PROCESS FOR PRODUCING 5-(2 -PYRIDYL)-2-PYRIDONE DERIVATIVE
-
The present invention provides a method of industrially and advantageously producing a 5-(2'-pyridyl)-2-pyridone derivative. The present invention relates to a production method of a 5-(2'-pyridyl)-2-pyridone derivative represented by the formula (VI), which includes reacting a pyridine derivative of the formula (I) with a brominating agent to give a 5-bromopyridine derivative of the formula (II), reacting the obtained 5-bromopyridine derivative with a metallizing agent to give an organometallic compound of the formula (III), reacting the obtained organometallic compound with a 2-sulfonylpyridine derivative of the formula (IV) to give a 6-alkoxy-3,2'-bipyridine derivative of the formula (V) and hydrolyzing the obtained 6-alkoxy-3,2'-bipyridine derivative: wherein each symbol is as defined in the Description.
- -
-
Page/Page column 8
(2008/06/13)
-
- 1,2-DIHYDROPYRIDINE COMPOUNDS, PROCESS FOR PREPARATION OF THE SAME AND USE THEREOF
-
The present invention provides a novel compound having an excellent AMPA receptor inhibitory action and/or kainate inhibitory action. A compound represented by the following formula, a salt thereof or hydrates thereof. In the formula, Q indicates NH, O or S; and R1, R2, R3, R4 and R5 are the same as or different from each other and each indicates hydrogen atom, a halogen atom, a C1-6 alkyl group or a group represented by the formula -X-A (wherein X indicates a single bond, an optionally sbutituted C1-6 alkylene group etc.; and A indicates an optionally substituted C6-14 aromatic hydrocarbocyclic group or 5- to 14-membered aromatic heterocyclic group etc.).
- -
-
-