Carbonic anhydrase inhibitory properties of novel sulfonamide derivatives of aminoindanes and aminotetralins
摘要:
Six sulfonamides derived from indanes and tetralines were synthesized. The human carbonic anhydrase isozymes hCA I and hCA II inhibition effects of the synthesized sulfonamides were determined. From these compounds, while N-(5,6-dimethoxy-2,3-dihydro-1H-inden-2-yl) methane sulfonamide showed the most potent inhibitory effect against hCA I (K-i = 46 +/- 5.4 mu M, r(2) = 0.978), N-(1,2,3,4-tetrahydronaphthalene-2-yl) methanesulfonamide was found to have the best inhibitory effect against hCA II (K-i = 94 +/- 7.6 mu M, r(2) = 0.982).
Preventives/remedies for voiding disturbance containing a compound having both of an acetylcholinesterase inhibitory action and an α1 antagonistic action which exhibits an excellent effect of improving the urinary function of the bladder (i.e., effects of improving urine flow rate and voiding efficiency) without affecting the urinary pressure or the blood pressure.
DERIVES D'ACYLAMINOTHIAZOLE ET LEUR APPLICATION COMME INHIBITEURS DE BETA-AMYLOIDE
申请人:Sanofi-Aventis
公开号:EP1709018B1
公开(公告)日:2011-07-20
ACYLAMINOTHIAZOLE DERIVATIVES AND USE THEREOF AS BETA-AMYLOID INHIBITORS
申请人:BALTZER Sylvie
公开号:US20080176911A1
公开(公告)日:2008-07-24
Compounds of formula (I) as defined herein:
inhibit the formation of the β-amyloid peptide (β-A4) and are, therefore, useful in the treatment of pathologies in which a β-amyloid peptide (β-A4) formation inhibitor provides a therapeutic benefit. Particular such pathologies are senile dementia, Alzheimer's disease, Down's syndrome, Parkinson's disease, amyloid angiopathy, cerebrovascular disorders, frontotemporal dementias and Pick's disease, post-traumatic dementias, pathologies linked to neuroinflammatory processes, Huntington's disease and Korsakov's syndrome.