355399-89-2Relevant academic research and scientific papers
6-sulphamoyl -3-quinolyphosphonic acid compounds
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, (2008/06/13)
The invention relates to a compound of formula (I): wherein: X represents chlorine or fluorine or CF3, R represents hydrogen or a group and methods for using the same.
Novel quinolinone-phosphonic acid AMPA antagonists devoid of nephrotoxicity.
Cordi, Alex A,Desos, Patrice,Ruano, Elisabeth,Al-Badri, Hashim,Fugier, Claude,Chapman, Astrid G,Meldrum, Brian S,Thomas, Jean-Yves,Roger, Anita,Lestage, Pierre
, p. 787 - 802 (2007/10/03)
We reported previously the synthesis and structure-activity relationships (SAR) in a series of 2-(1H)-oxoquinolines bearing different acidic functions in the 3-position. Exploiting these SAR, we were able to identify 6,7-dichloro-2-(1H)-oxoquinoline-3-phosphonic acid compound 3 (S 17625) as a potent, in vivo active AMPA antagonist. Unfortunately, during the course of the development, nephrotoxicity was manifest at therapeutically effective doses. Considering that some similitude exists between S 17625 and probenecid, a compound known to protect against the nephrotoxicity and/or slow the clearance of different drugs, we decided to synthesise some new analogues of S 17625 incorporating some of the salient features of probenecid. Replacement of the chlorine in position 6 by a sulfonylamine led to very potent AMPA antagonists endowed with good in vivo activity and lacking nephrotoxicity potential. Amongst the compounds evaluated, derivatives 7a and 7s appear to be the most promising and are currently evaluated in therapeutically relevant stroke models.
Aryl or heteroaryl quinolylphosphonic acid compounds
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, (2008/06/13)
The invention relates to a compound of formula (I): wherein: R1represents halogen or a group CF3, R2represents aryl or heteroaryl, R3and R4are as defined in the description and methods for using the s
6-amino- or 6-hydrazino-sulphonyl-3-quinolynyl-phosphonic acid compounds
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, (2008/06/13)
The invention relates to a compound of formula (I): wherein: R1 represents halogen or a group CF3, R2 represents hydrogen or alkyl or cycloalkyl, R3 is as defined in the description, R4 and R5 /
