68302-09-0Relevant academic research and scientific papers
Tricyclic aminocyanopyridine inhibitors of mitogen activated protein kinase-activated protein kinase-2
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, (2008/06/13)
Aminocyanopyridine compounds are described which are capable of inhibiting mitogen activated protein kinase-activated protein kinase-2. Pharmaceutical compositions and kits are also described, which include an anminocyanopyridine MK-2 inhibiting compound.
Studies on antianaphylactic agents. 7. Synthesis of antiallergic 5-oxo-5H-[1]benzopyrano[2,3-b]pyridines
Nohara,Ishiguro,Ukawa,Sugihara,Maki,Sanno
, p. 559 - 586 (2007/10/02)
5-Oxo-5H-[1]benzopyrano[2,3-b]pyridine-3-carboxylic acids 23 and their tetrazole analogues 24 were synthesized from 4-oxo-4H-1-benzopyran-3-carbonitriles or 2-amino-4-oxo-4H-1-benzopyran-3-carboxaldehydes. When administered intravenously, they exhibited antiallergic activity in a reaginic PCA test in rats. In the carboxylic acid series, the activity was influenced by the substituents at the 2-position and increased substantially in the following order: Me, OMe 2 OH, H NHOMe. On the other hand, in the tetrazole series, 2-unsubsitituted derivatives showed the highest activity. Regardless of the kinds of substituents at positions 2 and 3, compounds bearing an alkyl group, especially an isopropyl group at the 7-position, were superior in activity to the corresponding unsubstituted compounds. Among these alkyl derivatives, 3-carboxylic acid derivatives, i.e., 23c (7-ethyl), 23g (2-amino-7-isopropyl), 23r [2-(methoxyamino)-7-isopropyl], and a 3-tetrazole derivative 24c (7-isopropyl), were 41-184 times as potent as disodium cromoglycate. They also exhibited remarkable activity when administered orally; clinical studies on 23g (AA-673) are in progress.
SYNTHESIS OF 3-SUBSTITUTED-5-OXO-5H-BENZOPYRANOPYRIDINE DERIVATIVES
Ishiguro, Toshihiro,Ukawa, Kiyoshi,Sugihara, Hirosada,Nohara, Akira
, p. 733 - 740 (2007/10/02)
3-Cyano-. 3-alkoxycarbonyl-, and 3-formyl-5-oxo-5H-benzopyranopyridine dervatives were prepared by reactions of 2-amino-4-oxo-4H-1-benzopyran-3-carboxaldehydes 1 with acetylene derivatives (methods A-C) or with reactive methylene compounds (methods D-E) and also by catalytic hydrogenation of 2-chloro-5-oxo-5H-benzopyranopyridine-3-carbonitriles 12 (method F).
1-Azaxanthone-3-carboxylic acids
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, (2008/06/13)
The present invention relates to novel 1-azaxanthone-3-carboxylic acid and its derivatives usable for effective medicines for the treatment of allergic diseases, which are shown by the following formula (I) STR1 wherein R1 is hydrogen, alkyl, phenyl, carboxyl, hydroxyl, alkoxy or amino group which may be unsubstituted or substituted by one alkyl, m is 0, 1 or 2 and R2 is alkyl, alkoxy, halogen, nitro, hydroxy, carboxyl, butadienylene (--CH=CH--CH=CH--) which forms a benzene ring with any adjacent carbon atoms or amino group which may be unsubstituted or substituted by at least one alkyl, and their physiologically acceptable salts.
