[EN] 6,7-DIHYDROPYRAZOLO[1,5-A]PYRAZIN-4(5H)-ONE COMPOUNDS AND THEIR USE AS NEGATIVE ALLOSTERIC MODULATORS OF MGLUR2 RECEPTORS<br/>[FR] COMPOSÉS 6,7-DIHYDROPYRAZOLO[1,5-A] PYRAZIN-4(5H)-ONE ET LEUR UTILISATION COMME MODULATEURS ALLOSTÉRIQUES NÉGATIFS DES RÉCEPTEURS MGLUR2
申请人:JANSSEN PHARMACEUTICA NV
公开号:WO2016016395A1
公开(公告)日:2016-02-04
The present invention relates to novel 6,7-dihydropyrazolo[1,5-a]pyrazin-4(5H)-one derivatives as negative allosteric modulators (NAMs) of the metabotropic glutamate receptor subtype 2 ("mGluR2"). The invention is also directed to pharmaceutical compositions comprising such compounds, to processes for preparing such compounds and compositions, and to the use of such compounds and compositions for the prevention or treatment of disorders in which the mGluR2 subtype of metabotropic receptors is involved.
The present invention aims to provide an iminopyridine derivative compound having an α
1D
adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like.
The present invention provides a compound represented by the formula
wherein each symbol is as defined in the specification, or a salt thereof.
Provided are an iminopyridine derivative having a selective α1D adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α1D adrenergic receptor antagonistic action. An α1D adrenergic receptor antagonist containing a compound represented by the formula:
wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α1D adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
Provided are an iminopyridine derivative having a selective α
1D
adrenergic receptor antagonistic action and useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like, and a screening method for a compound having an α
1D
adrenergic receptor antagonistic action. An α
1D
adrenergic receptor antagonist containing a compound represented by the formula:
wherein each symbol is as defined in the specification, or a salt thereof, and a method of screening for an agent having an α
1D
adrenergic receptor antagonistic action for the prophylaxis or treatment of a lower urinary tract disease, which includes measuring the bladder smooth muscle tension of rats with bladder outlet obstruction.
The present invention aims to provide an iminopyridine derivative compound having an α1D adrenergic receptor antagonistic action, which is useful as an agent for the prophylaxis or treatment of a lower urinary tract disease and the like. The present invention provides a compound represented by the formula
wherein each symbol is as defined in the specification, or a salt thereof.