112913-95-8Relevant articles and documents
AMIDE DERIVATIVE AND PHARMACEUTICAL COMPOSITION CONTAINING THE SAME
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Page/Page column 26-27, (2010/10/19)
Disclosed is a compound having a strong affinity to serotonin-4 receptors, which is useful as an enterokinesis-promoting agent or a digestive tract function-improving agent. Specifically, disclosed is a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. Also specifically disclosed is a pharmaceutical composition containing a compound represented by Formula (1) or a pharmaceutically acceptable salt thereof. [In Formula (1), Ar represents a group represented by Formula (Ar-1) or Formula (Ar-2).]
Indolobenzazepine HCV NS5B inhibitors
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Page/Page column 239-240, (2008/06/13)
The invention encompasses compounds and salts of Formulas I, II, III, and IV as well as compositions and methods of using the compounds. The compounds have activity against hepatitis C virus (HCV) and are useful in treating those infected with HCV.
Pyrimidine derivatives
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, (2008/06/13)
Pyrimidine derivatives useful as a gastrointestinal prokinetic agent, represented by formula STR1 wherein X is O or NR5, Y is O, S or NR5 wherein R5 is a hydrogen atom, a C1 -C6 alkyl group or the like; R1 and R2 may be the same or different and each is a hydrogen atom, a C1 -C6 alkyl group or the like; R3 is CN, or COOR6 wherein R6 is a C1 -C6 alkyl group, a C3 -C6 cycloalkyl group, an aryl group or the like; R4 is --SR7 or --NR8 R9 wherein R7 is a C1 -C6 alkyl group; R8 is a C1 -C6 alkyl group or the like; R9 is a hydrogen atom, a C1 -C6 alkyl group or the like, or R8 and R9 may represent, together with the nitrogen atom to which they are attached, an N-substituted piperazine ring of formula (X) STR2 wherein R10 represents a C1 -C6 alkyl group or the like or a pharmacologically acceptable salt thereof. The above-mentioned compounds are useful as a gastrointestinal prokinetic agent used for the therapy of digestive tract diseases.
Quinolone antimicrobial agents substituted with morpholines at the 7- position. Syntheses and structure-activity relationships
Araki,Kuroda,Uemori,Moriguchi,Ikeda,Hirayama,Yokoyama,Iwao,Yakushiji
, p. 1356 - 1363 (2007/10/02)
A series of novel 7-substituted 1-cyclopropyl-6,8-difluoro-1,4-dihydro-4- oxo-3-quinolinecarboxylic acids have been prepared and tested for antibacterial activities and for convulsive activities in combination with nonsteroidal antiinflammatory drug. Stru
Novel benzamides as selective and potent gastrokinetic agents. III. Synthesis and structure-activity relationships of 4-amino-5-chloro-2-methoxy- and 2-ethoxy-N-[(4-substituted 2-morpholinyl)methyl]-benzamides
Kato,Morie,Harada,Yoshida,Matsumoto
, p. 652 - 660 (2007/10/02)
A series of 4-amino-5-chloro-2-methoxy- and 2-ethoxy-N-[(4-substituted 2-morpholinyl)methyl]benzamides (11-44) were prepared and evaluated for gastrokinetic activity by determining their effects on the gastric emptying of phenol red semisolid meal in rats. The N-4 substituent includes alkyl, phenoxyalkyl, (4-fluorobenzoyl)alkyl, and heteroarylmethyl groups. The benzamide derivatives, having an isopropyl, isoamyl, neopentyl, 3-(4-chlorophenoxy)propyl, or pyridylmethyl group at N-4, showed potent in vivo gastric emptying activity. In particular, 4-amino-5-chloro-2-ethoxy-N-[[4-(3-pyridylmethyl)-2-morpholinyl]methyl ]benzamide (57b) was equipotent to the 4-fluorobenzyl analogue 1b (AS-4370 as its citrate) in the gastrokinetic activity on phenol red semisolid meal in rats and mice, and on resin pellet solid meal in rats. Moreover, compound 57b was free from dopamine D2 receptor antagonistic activity in both in vitro ([3H]spiperone binding) and in vivo (apomorphine-induced emesis in dogs) tests. Structure-activity relationships of compounds with various substituents at N-4 are also discussed.
Substituted benzamide derivatives, for enhancing gastrointestinal motility
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, (2008/06/13)
Compounds of the formula: STR1 wherein R is hydrogen, alkoxycarbonyl, benzyloxycarbonyl, heteroarylalkyl, phenylalkenyl, or --T--(Y)p --R6 (wherein T is single bond or alkylene, Y is oxygen, sulfur or carbonyl, R6 is phenyl, substituted phenyl, naphthyl, or diphenylmethyl, and p is 0 or 1, provided that when T is single bond, p is 0); R1 is halogen, hydroxy, alkoxy, cycloalkyloxy, alkenyloxy, alkynyloxy, alkoxy interrupted by oxygen or carbonyl, alkylthio, amino, monosubstituted amino, or a substituted alkoxy; R2 is hydrogen; R3 is hydrogen, halogen, amino, alkylamino, dialkylamino, alkanoylamino, or nitro; R4 is hydrogen, halogen, nitro, sulfamoyl, alkylsulfamoyl, or dialkylsulfamoyl; or any two adjacent groups of the R1, R2, R3 and R4 may combine to form alkylenedioxy, and the remaining two groups are each hydrogen; R5 is hydrogen or alkyl; X is alkylene; m and n are each 1 or 2; provided that at least one of the groups R2, R3 and R4 is other than hydrogen, and acid addition salts, quaternary ammonium salts and N-oxide derivatives thereof, processes for preparation thereof, and pharmaceutical composition containing the same. Said compounds, salts and N-oxide derivatives thereof show excellent gastrointestinal motility enhancing activity.