114432-29-0Relevant academic research and scientific papers
A Novel Class of Calcium-Entry Blockers: The 1-sulfonyl>indolizines
Gubin, Jean,Lucchetti, Jean,Mahaux, Jean,Nisato, Dino,Rosseels, Gilbert,et al.
, p. 981 - 988 (2007/10/02)
The synthesis and initial biological evaluation of a series of 1-sulfonylindolizines is described.These compounds have been shown to be representatives of a novel class of potent, slow-channel calcium antagonists.All compounds were found to be at least as active as the reference calcium antagonists verapamil and cis-(+)-diltiazem.Structure-activity relationship studies have shown that all compounds possessing an aralkyl group in the amine moiety and an isopropyl or cyclopropyl group at the 2 position of the indolizine are among the most potent calcium antagonists know n outside the 1,4-dihydropyridine series.The IC50 value for the inhibition of nitrendipine binding vary between o.19 and 4.5 nM whereas the IC50 value for nifedipine is 2.5 nM.One of the compounds in this group (9ab) has now been selected for clinical development.
Aminoalkoxyphenyl derivatives, process of preparation and compositions containing the same
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, (2008/06/13)
Aminoalkoxyphenyl derivatives useful in the treatment of certain pathological syndromes of the cardiovascular system of formula: STR1 in which: B represents a --S, --SO--, or --SO2 -- group, R1 and R2, which are identical or different, each denote hydrogen, a methyl or ethyl radical or a halogen such as chlorine, bromine or iodine, A denotes a straight- or branched-alkylene radical having from 2 to 5 carbon atoms or a 2-hydroxypropylene radical in which the hydroxy is optionally substituted by a lower alkyl radical, Ar represents a group STR2 R4 denotes hydrogen or an alkyl radical and Cy represents a cyclic group.
Use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure
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, (2008/06/13)
The present invention is directed to the use of aminoalkoxyphenyl derivatives for reducing and/or controlling excessive intraocular pressure and compositions suitable for this case.
