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Restrict the search for
m nalidixic acid
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Dezinamide is a potential antiepileptic drug that binds to the voltage-sensitive sodium channel. It is a metabolite of fluzinamide. It was active in preventing maximal seizures induced in mice or rats by electroshock and threshold seizures induced in mice by metrazol, bicuculline, and picrotoxin. It was predominantly active against tonic-clonic seizures. Adverse experiences included headache, ataxia, blurred vision, diplopia, dizziness, lightheadedness, and mild confusion. Dezinamide development was discontinued because of toxicity problems not observed with the metabolite.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Libenzapril is a long-acting, small polar angiotensin-converting enzyme (ACE) inhibitor with antihypertensive activity. Libenzapril competitively binds to and inhibits ACE, thereby blocking the conversion of angiotensin I to angiotensin II. This prevents the potent vasoconstrictive actions of angiotensin II and results in vasodilation. Libenzapril also decreases angiotensin II-induced aldosterone secretion by the adrenal cortex, which leads to an increase in sodium excretion and subsequently increases water outflow. Both libenzapril and water transport was found to be significantly higher (about two- to five-fold) in six of the seven different brain regions in hypertensive rats as compared to the normotensive controls.
Status:
Investigational
Source:
NCT00683436: Phase 2 Interventional Terminated Primary Insomnia
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Adipiplon is an oral, partial agonist of the GABAA alpha-3 (α3) receptor that was being developed by Neurogen Corporation for the treatment of insomnia, anxiety disorders and schizophrenia. Adipiplon has been tested in Phase 1 and 2 studies in over 600 subjects for the treatment of insomnia, demonstrating statistical significance compared to placebo on primary endpoints for sleep initiation and maintenance in patients with chronic insomnia. Adipiplon has also demonstrated statistical significance compared to placebo for self-reported quality of sleep in all completed Phase 2 studies to date. Additionally, in studies completed to date it has been well tolerated at all doses tested. Development of adipiplon was discontinued during 2008.
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Zoniporide hydrochloride is a novel, potent and selective NHE-1 inhibitor (IC50 = 14 nM). Reduces infarct size in the isolated heart (EC50 = 0.25 nM). Attenuates post-ischemic cardiac contractile dysfunction and ischemia-reperfusion-induced ventricular fibrillation in vivo. Zoniporide hydrochloride represents a novel class of potent and selective human NHE-1 inhibitors with potential utility for providing cardioprotection in a clinical setting.
Status:
Investigational
Source:
NCT00100347: Phase 1 Interventional Terminated Non-Hodgkin's Lymphoma,
(2004)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
PPI-2458 is a synthetic derivative of fumagillin with antineoplastic and cytotoxic properties. PPI-2458 irreversibly inhibits the enzyme methionine aminopeptidase type 2 (MetAP2), thereby preventing abnormal cell growth and angiogenesis. PPI-2458 is reported to have a better toxicity profile compared to other agents of its class. In a phase 1 clinical study, PPI-2458 was administered to patients with non-Hodgkin lymphoma. The data confirm the participation of active metabolites in the in vivo efficacy of PPI-2458. In in vitro studies, osteoclast formation and activity were inhibited by PPI-2458, a mechanism not previously attributed to MetAP-2 inhibition. PPI-2458 treatment reduced synovial and osteochondral angiogenesis, synovial inflammation, joint damage, and pain behavior. PPI-2458 exerts disease-modifying activity in experimental arthritis through its direct inhibition of several pathophysiologic processes of this disease. These results provide a rationale for assessing the potential of PPI-2458 as a novel rheumatoid arthritis therapy.
Status:
Investigational
Source:
USAN:PIROXICAM CINNAMATE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Piroxicam cinnamate (Cinnoxicam) is the anti-inflammatory agent. It is a cyclooxygenase inhibitor. Cinnoxicam was used in patients with inflammatory-degenerative osteoarticular diseases. The treatment brought about a significant improvement in the clinical variables considered (spontaneous pain at rest and on movement and functional limitation), which was observed within a few days of starting therapy. Tolerance was good, only a few slight side-effects having been reported. Cinnoxicam is a safe and reliable therapeutic option for men with oligoasthenospermia associated with a grade III varicocele, but surgery is better for those with grade II, IV and V. Piroxicam cinnamate as a long-acting prodrug is marketed by SPA in Italy for the treatment of rheumatic disorders.
Class (Stereo):
CHEMICAL (ACHIRAL)
Belfosdil (or SR-7037) is an antihypertensive calcium channel blocker.
Class (Stereo):
CHEMICAL (RACEMIC)
Class (Stereo):
CHEMICAL (ACHIRAL)
FLOSATIDIL is an antihypertensive drug discontinued in Phase II for angina pectoris.
Class (Stereo):
CHEMICAL (RACEMIC)
Prazitone (also known as AGN-511) is a barbiturate derivative patented by Aspro-Nicholas Ltd. as a non-sedating anxiolytic and antidepressant
