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Status:
Investigational
Source:
NCT00362024: Phase 2 Interventional Terminated Alzheimer's Disease
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Piprofurol is a benzofuran chalcon derivative. It is a calcium channel blocker. Piprofurol inhibited in a concentration-dependent manner the calcium-induced contractions in isolated potassium depolarized preparations of rat aorta and relaxed the K+-induced contraction of the dog coronary artery and the rabbit basilar artery. Piprofurol also inhibited noradrenaline-induced vascular smooth muscle contractions but the antagonism was clearly noncompetitive and the contractions induced were altered by concentrations two orders of magnitude higher than the concentration inhibiting calcium-induced contractions. Piprofurol exerts a negative inotropic effect on guinea-pig papillary muscle. These effects suggested a potentially anti-ischemic activity. This is confirmed in anaesthetized dogs, where piprofurol reduced the epicardial ST-segment elevation following coronary artery occlusion, and in isolated heart preparations, where it decreased the leakage of LDH during periods of anoxia and reoxygenation. Piprofurol is a coronary vasodilator and antihypertensive agent.
Class (Stereo):
CHEMICAL (ACHIRAL)
Zinoconazole, an imidazole derivative that was used as an antifungal agent. Information about the current use of this compound is not available.
Class (Stereo):
CHEMICAL (ACHIRAL)
Zapizolam was studied as a sedative and anxiolytic agent that has never been marketed.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Pixefole is the 1,2,4-oxadiazole derivative. It has a similar profile of muscle-relaxant activity in animals to that of chlorzoxazone. In rats, pifexole is reported to be seven times more potent than chlorzoxazone in inhibition of strychnine-induced convulsions.
Status:
Investigational
Source:
INN:pidolacetamol [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pidolacetamol is an analgesic and antipyretic agent.
Status:
Investigational
Source:
NCT00248404: Phase 1/Phase 2 Interventional Completed Tumors
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00886067: Phase 1 Interventional Completed Healthy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT02115282: Phase 3 Interventional Active, not recruiting Anatomic Stage III Breast Cancer AJCC v8
(2014)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Entinostat (MS-275) is an orally active, highly selective, small-molecule histone deacetylase inhibitor (HDACi) derived from benzamide. Entinostat preferentially inhibited HDAC1 versus HDAC3 and had no inhibitory activity toward HDAC8. The time to maximum plasma concentration (tmax) of entinostat ranged from 0.5 to 60h (median of 2h). Elimination of the drug was bi-exponential, with a terminal half-life of 30-80h. Entinostat is a well-tolerated that demonstrates promising therapeutic potential in both solid and hematologic malignancies. Its efficacy does not appear directly dose-related, and as such, more relevant biomarkers are needed to adequately assess its activity.