59207-24-8Relevant academic research and scientific papers
Design and synthesis of piperazinylpyridine derivatives as novel 5-HT 1A agonists/5-HT3 antagonists for the treatment of irritable bowel syndrome (IBS)
Asagarasu, Akira,Matsui, Teruaki,Hayashi, Hiroyuki,Tamaoki, Satoru,Yamauchi, Yukinao,Sato, Michitaka
experimental part, p. 34 - 42 (2009/07/18)
We have prepared a series of piperazinylpyridine derivatives for the treatment of irritable bowel syndrome (IBS). These compounds, which were designed by pharmacophore analysis, bind to both serotonin subtype 1A (5-HT 1A) and subtype 3 (5-HT3) receptors. The nitrogen atom of the isoquinoline, a methoxy group and piper-azine were essential to the pharmacophore for binding to these receptors. We also synthesized furo- and thienopyridine derivatives according to structure-activity relationship analyses. Compound 17c (TZB-20810) had high affinities to these receptors and exhibited 5-HT1A agonistic activity and 5-HT3 antagonistic activity concurrently, and is a promising drug for further development in the treatment of IBS.
Sulfonic acid sulfonylamino n-(heteroaralkyl)-azaheterocyclylamide compounds
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, (2008/06/13)
The compounds of formula I herein exhibit useful pharmacological activity and accordingly are incorporated into pharmaceutical compositions and used in the treatment of patients suffering from certain medical disorders. More specifically, they are inhibitors of the activity of Factor Xa. The present invention is directed to compounds of formula I, compositions containing compounds of formula I, and their use, for treating a patient suffering from, or subject to, a physiological condition which can be ameliorated by the administration of an inhibitor of the activity of Factor Xa.
1-SUBSTITUTED AMINO-3-THIENO-[3,2-c]PYRIDINYLOXY-2-PROPANOLS
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, (2008/06/13)
This invention provides new compounds of formula I, STR1 wherein X is sulphur or oxygen,R is alkyl of 3 to 7 carbon atoms or cycloalkyl of 3 to 7 carbon atoms, cycloalkyl of 3 to 7 carbon atoms monosubstituted by alkyl of 1 to 4 carbon atoms, α-dialkylpropinyl of 5 to 9 carbon atoms or α-dialkyl-allyl of 5 to 9 carbon atoms, hydroxyalkyl of 2 to 7 carbon atoms or phenoxyalkyl of 8 to 11 carbon atoms, the oxygen atom of the last two radicals being separated by at least two carbon atoms from the nitrogen atom to which R is bound, R 1 isI. hydrogen or alkyl of 1 to 4 carbon atoms in the 2,3,6 or 7 position, orIi. chlorine or bromine, in the 2, 3 or 7 position,Iii. nitro or--NHA wherein A is alkanoyl of 1 to 4 carbon atoms, in the 2, 3 or 7 position, orIv. fluorine, cyano or COOB, wherein B is alkyl of 1 to 4 carbon atoms, in the 2 or 3 position, andR 2 isI. hydrogen or alkyl of 1 to 4 carbon atoms in the 2, 3, 6 or 7 position,Ii. chlorine or bromine, in the 2, 3 or 7 position, orIii. fluorine in the 2 or 3 position,Useful in the treatment of heart diseases.
