21717-96-4Relevant articles and documents
Simple 2-amino-5-halogenated pyridine preparation method
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Paragraph 0037-0040, (2019/10/01)
The invention provides a 2-amino-5-halogenated pyridine preparation method, which comprises: carrying out an addition reaction on 4-cyano-1-butyne and a halogen element X2 in a solvent under the catalysis of an acidic catalyst to obtain 4,4,5,5-tetrahalogenated n-valeronitrile, and carrying out cyclization on the 4,4,5,5-tetrahalogenated n-valeronitrile and ammonia through pyridine to obtain 2-amino-5-halogenated pyridine. According to the present invention, the preparation method has advantages of mild preparation condition, safety, environmental protection, low cost, high selectivity, less by-products and high product yield, and is suitable for industrial production.
NOVEL TRICYCLIC COMPOUNDS AS INHIBITORS OF MUTANT IDH ENZYMES
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Page/Page column 44; 45, (2017/05/17)
The present invention is directed to tricyclic compounds of formula (I), (Ia) or (Ib) which are inhibitors of one or more mutant IDH enzymes. The present invention is also directed to uses of these tricyclic compounds in the potential treatment or prevention of cancers in which one or more mutant IDH enzymes are involved. The present invention is also directed to compositions comprising these compounds. The present invention is also directed to uses of these compositions in the potential prevention or treatment of such cancers.
Synthesis and pharmacological evaluation of a second generation of pyridothiadiazine 1,1-dioxides acting as AMPA potentiators
Francotte, Pierre,Tullio, Pascal de,Podona, Tchao,Diouf, Ousmane,Fraikin, Pierre,Lestage, Pierre,Danober, Laurence,Thomas, Jean-Yves,Caignard, Daniel-Henri,Pirotte, Bernard
scheme or table, p. 9948 - 9956 (2009/04/05)
Taking into account structure-activity relationships obtained with our previous series, new diversely substituted 1,2,4-pyridothiadiazine 1,1-dioxides were designed to obtain novel AMPA potentiators. The aim of this work was focused on the improvement of lipophilicity, which is well known as a critical parameter to obtain in vivo active central nervous system agents. For this purpose, two positions on the pyridine ring were privileged to insert selected groups. Among the synthesized compounds emerged 7-chloro-4-ethyl-3,4-dihydro-2H-pyrido[2,3-e]-[1,2,4]-thiadiazine 1,1-dioxide (12d), which was evaluated in two memory tests in Wistar rats and showed cognition enhancing effects after intraperitoneal injection at doses as low as 0.3 mg/kg.