40912-71-8Relevant academic research and scientific papers
SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
-
Page/Page column 239, (2009/01/24)
The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
Enzymatically activated cycloSal-d4T-monophosphates: The third generation of cycloSal-pronucleotides
Gisch, Nicolas,Balzarini, Jan,Meier, Chris
, p. 1658 - 1667 (2008/01/27)
The third generation of cycloSal-pronucleotides, 5-diacetoxymethyl- cycloSal-d4T-monophosphates (5-di-AM-cycloSal-d4TMPs), is reported as a new class of "lock-in"-modified cycloSal-pronucleotides. These compounds bear an esterase-cleavable geminal dicarboxylate (acylal) attached to the aromatic ring of the saligenyl unit. The conversion into a strong acceptor group (aldehyde) leads to a strong decrease in hydrolytic stability. As a consequence, a fast release of a nucleoside monophosphate (i.e., d4TMP) follows. The concept of this enzymatic activation is proven by hydrolysis studies in phosphate buffer, cell extracts, and human serum. These investigations showed the conversion of the acylal group into a polar aldehyde by enzymatic cleavage. Besides, antiviral activities against HIV are presented.
Medicaments having psychotropic properties (antitussives)
-
, (2008/06/13)
5-Bromo-N-(N1 -pyrrolidino-alkyl)-ortho-cresotamides having 2 to 5 carbon atoms in the alkyl moiety and therapeutically acceptable salts thereof, compositions containing such compounds useful as antitussives, and a method of suppressing of a cough in a host by administering an effective amount of such a compound with a pharmaceutically acceptable excipient. 5-Bromo-ortho-cresotamide may also be named 5-bromo-2-hydroxy-3-methyl-benzamide.
