[EN] PYRIDAZINONE-BASED BROAD SPECTRUM ANTI-INFLUENZA INHIBITORS<br/>[FR] INHIBITEURS ANTIGRIPPAUX À LARGE SPECTRE À BASE DE PYRIDAZINONE
申请人:HOFFMANN LA ROCHE
公开号:WO2018001948A1
公开(公告)日:2018-01-04
The present invention relates to compounds of formula (I): (I) or pharmaceutically acceptable salts thereof, as well as processes for their manufacture, pharmaceutical compositions comprising them, and their use as medicaments.
A novel and efficient method for the oxidation of 2-arylindoles to synthesize 2-arylbenzoxazinones utilizing oxone as the sole oxidant has been developed. The reaction tolerates a wide range of functional groups and allows quick and atom-economical assembly of a variety of valuable 2-arylbenzoxazinones in high yields.
7-(Ethoxycarbonyl)-6,8-dimethyl-2-phenyl-1(2H)-phthalazinone derivatives and several analogues were synthesized and their inhibitory effects on platelet aggregation were evaluated. Structure-activity relationships are discussed. All synthesized compounds showed no appreciable effect on platelet aggregation induced by adenosine diphosphate, but most of them inhibited effectively the arachidonic acid
5-aryl-1H-1,2,4-triazole compounds as inhibitors of cyclooxygenase-2 and pharmaceutical compositions containing them
申请人:LABORATOIRE THERAMEX S.A.
公开号:EP1099695A1
公开(公告)日:2001-05-16
The invention relates to 5-aryl-1H-1,2,4-triazole compounds of the formula :
in which R1, R2, R3 and R4 are as defined in the specification.
These compounds are potent and selective COX-2 inhibitors.
The invention also relates to pharmaceutical compositions comprising these compounds.
The present invention relates to compounds, pharmaceutical compositions and methods of using compounds of formula (I) in the treatment and/or prevention of certain diseases or conditions. In formula (I), A is chosen from ortho substituted aryl or heteroaryl species, X is chosen from --OH, --SH, NHR and R.sup.1 or R.sup.2 is chosen from --(CH.sub.2).sub.n L wherein L may be selected from a variety of substituents including aryl, heteroaryl and heterocyclic groups. The compounds are useful in treating and/or preventing neurological disorders associated with excitatory amino acids. ##STR1##