U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 2561 - 2570 of 141793 results

Linifanib (ABT-869) is a structurally novel, receptor tyrosine kinase (RTK) inhibitor that is a potent inhibitor of members of the vascular endothelial growth factor (VEGF) and platelet-derived growth factor (PDGF) receptor families, but has much less activity against unrelated RTKs, soluble tyrosine kinases, or serine/threonine kinases. Linifanib (ABT-869) does not have a general antiproliferative effect due to its high dose requirement. However, it may exhibit potent antiproliferative and apoptotic effects on tumor cells whose proliferation is dependent on mutant kinases, such as FMS-related tyrosine kinase receptor-3 (FLT3). Linifanib (ABT-869) was in phase III clinical trial for the treatment of hepatocellular carcinoma, but the study failed to meet the primary end point.
Status:
Investigational
Source:
INN:carbocloral [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Carbocloral is a carbamate ester derivative used as sedative and hypnotic drug. Carbocloral is as effective as chloral hydrate in producing sedation, hypnosis, and general anesthesia, and more effective in inducing relaxation of skeletal muscles. Carbocloral was also more effective as an anticonvulsant and less toxic than chloral hydrate.
Status:
Investigational
Source:
INN:florifenine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


FLORIFENINE is an anti-inflammatory agent. It inhibits the cyclooxygenase pathway and, in addition, it inhibits migration and decreases in vitro the release of neutrophil elastase.
Status:
Investigational
Source:
INN:sulfogaiacol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Potassium guaiacolsulfonate also known as sulfoguaiacolum is a salt of GUAIACOLSULFONIC ACID, which is used as an expectorant, to relieve symptoms of cough and mucus in the chest due to respiratory infections, asthma, colds, or hay fever. It works by thinning mucus (phlegm) in the lungs, making it less sticky and easier to cough up. This reduces chest congestion by making coughs more productive.
Status:
Investigational
Source:
INN:olpadronic acid
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Olpadronate, a nitrogenated bisphosphonate that can inhibit bone resorption. Although it shares the therapeutic and pharmacological properties of pamidronate and alendronate, it has a greater dosage amplitude, more predictable effects, and greater digestive tolerability than other bisphosphates. Clinical trials have shown that the oral olpadronate was well tolerated and effective in the treatment of Paget's disease. In addition, the drug is ongoing in phase II clinical trials in the Netherlands. This clinical trial has to assess the efficacy of the intravenous drug in decreasing the average back pain intensity from baseline.
Status:
Investigational
Source:
INN:triletide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Triletide is a tripeptide derivative which shows cytoprotective and antiulcerogenic activity. It is a thromboxane synthase inhibitor. Analysis of both individual and pooled data indicated that triletide was well absorbed after oral administration, with a lag time of 0.3 hours and the blood peak was reached after about 1.1 to 1.3 hours. Metabolization to desmethyl, desacetyl, desmethyl-desacetyl and hydroxylated derivatives plays a major role in the biotransformation of the drug and thus in its disappearance from blood, the distribution half-life being about 1 hour. A greater proportion of patients given the combination cimetidine and triletide was found to be endoscopically healed after treatment in comparison with those who had cimetidine alone (53% vs 40%). Intensity of symptoms decreased significantly faster and to a significantly greater extent in the same patients, as did antacid intake. Triletide appears to be equally well tolerated as, but significantly more effective than, aluminium hydroxide and magnesium hydroxide in relieving symptoms and promoting healing in patients with mild to moderate duodenal ulcer. There were no complaints of possible side-effects with either triletide treatment and no evidence of any significant changes in blood pressure, heart rate or routine haematology and haematochemistry investigations.
Status:
Investigational
Source:
INN:flunidazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Flunidazole (also known as MK-915) is a 5-nitroimidazole derivative used as an antiparasitic treatment. It has been shown to have both trichomonacidal and amebicidal properties. Flunidazole has been used for the treatment of Trichomonas vaginalis vaginitis, Blastocystis hominis, Entamoeba histolytica and Giardia intestinalis.
Status:
Investigational
Source:
INN:altanserin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

Altanserin is a potent and selective 5-HT2A receptor antagonist. Serotonin (5-HT) system functioning have been proposed for a variety of psychiatric disorders, but a direct method quantitatively assessing 5-HT release capacity in the living human brain is still lacking. It was suggested that the combination of a dexfenfluramine-induced 5-HT release and subsequent assessment of 5-HT(2A) receptor availability with [(18)F]altanserin by positron emission tomography (PET) was suitable to measure cortical 5-HT release capacity in the human brain. Besides human neuroimaging studies altanserin has also been used in the study of rats.
Status:
Investigational
Source:
INN:orbofiban
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Orbofiban was developed as an orally active glycoprotein IIb/IIIa antagonist. By 2001, this drug had progressed to phase III clinical trials. Unfortunately, was found that orbofiban induced thrombocytopenia and thrombosis. In addition, despite no significant excess risk of intracranial hemorrhage, orbofiban was not effective in preventing ischemic stroke or transient ischemic attack. Besides, the use of this drug had led to an increase in mortality. Based on all these results further development of this drug was discontinued.
Status:
Investigational
Source:
INN:glisindamide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Glisindamide is a hypoglycemic agent and part of the second-generation sulfonamide derivatives, used as medication to control blood sugar levels in patients with diabetes mellitus type 2. Glisindamide exerts greater binding affinity to sulfonylurea receptor type 1 (SUR1) than the first-generation compounds. It also exerts greater binding affinity for peroxisome proliferator-activated receptor gamma (PPARgamma) agonistic activity.

Showing 2561 - 2570 of 141793 results