112190-09-7Relevant articles and documents
Preparation method and application of 5-aminobenzene[b][1,8]naphthyridine compound
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Paragraph 0016-0017, (2019/10/17)
The invention belongs to the field of pharmaceutical chemistry, and specifically provides a preparation method and application of a 5-aminobenzene[b][1,8]naphthyridine compound. The preparation methodis a route for synthesis of the 5-aminobenzene [b][1,8] naphthalidine compound by intramolecular cyclization of a molecule of a 4,6-2-disubstituted-2-Naryl-3nitrile compound catalyzed by trifluoro-methanesulfonic acid, more 5-aminobenzene[b][1,8]naphthalidine compounds can be prepared, and the prepared compounds show good antitumor activity in vitro.
Synthesis of a new series of pyridine and fused pyridine derivatives
Al-Issa, Siham Abdulrahman
, p. 10902 - 10915 (2012/11/07)
The reaction of 4-methyl-2-phenyL-1,2-dihydro-6-oxo-5-pyridine- carbonitrile (1) with arylidene malononitrile afforded isoquinoline derivatives 2a,b. 6-Chloro-4- methyl-2-phenyl-5-pyridinecarbonitile (3) obtained by chlorination of compound 1 with phosphoryl chloride was converted into 6-amino-4-methyl-2-phenyl-5-pyridinecarbonitrile (4) and 6-hydrazido-4-methyl-2- phenyl-5-pyridinecarbonitrile (5) in good yield, through reactions with ammonium acetate and hydrazine hydrate, respectively. Treatment of 4 with ethyl acetoacetate, acetic anhydride, formic acid, urea and thiourea gave the corresponding pyrido [2,3-d] pyrimidine derivatives 7-10a,b. A new series of 6-substituted-4-methyl-2- phenyl-5-pyridine carbonitriles 11-13 has been synthesized via reaction of 4 with phenyl isothiocyanate, benzenesulphonyl chloride and acetic anhydride. Treatment of 4 with malononitrile gave 1,8-naphthyridine derivative 14. The reactivity of hydrazide 5 towards acetic acid, phenylisothiocyanate and methylacrylate to give pyrazolo-[3,4-b]-pyridine derivatives 15-17 was studied. Treatment of 5 with acetic anhydride, phthalic anhydride and carbon disulphide gave pyridine derivatives 18,19 and 1,2,4-triazolo-[3,4-a]-pyridine derivative 20.
EPHA4 RTK INHIBITORS FOR TREATMENT OF NEUROLOGICAL AND NEURODEGENERATIVE DISORDERS AND CANCER
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Page/Page column 20, (2010/05/13)
The present invention is directed to compounds of generic formula (I) which are inhibitors of ephrin A4. The invention is also directed to pharmaceutical compositions comprising the compounds, and to the use of the compounds and compositions in the treatm
Design and synthesis of 6-phenylnicotinamide derivatives as antagonists of TRPV1
Westaway, Susan M.,Thompson, Mervyn,Rami, Harshad K.,Stemp, Geoffrey,Trouw, Leontine S.,Mitchell, Darren J.,Seal, Jon T.,Medhurst, Stephen J.,Lappin, Sarah C.,Biggs, James,Wright, James,Arpino, Sandra,Jerman, Jeffrey C.,Cryan, Jennifer E.,Holland, Vicky,Winborn, Kim Y.,Coleman, Tanya,Stevens, Alexander J.,Davis, John B.,Gunthorpe, Martin J.
scheme or table, p. 5609 - 5613 (2009/06/18)
6-Phenylnicotinamide (2) was previously identified as a potent TRPV1 antagonist with activity in an in vivo model of inflammatory pain. Optimization of this lead through modification of both the biaryl and heteroaryl components has resulted in the discovery of 6-(4-fluorophenyl)-2-methyl-N-(2-methylbenzothiazol-5-yl)nicotinamide (32; SB-782443) which possesses an excellent overall profile and has been progressed into pre-clinical development.
NOVEL PYRIDINE DERIVATIVES, A PROCESS FOR THEIR PREPARATION AND A PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 55, (2008/06/13)
This invention relates to novel pyridine derivatives having an inhibitory effect on production of cytokines, which are involved in inflammatory responses, thus suggesting its usefulness as therapeutic agents for treating diseases related to inflammation, immune, chronic inflammation as well as an agent having an anti-inflammatory and analgesic effect. Further, this invention relates to a method of manufacturing the same and a pharmaceutical composition containing the same.