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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Fostedil (KB-944) is a phosphonic acid derivative with potent vasodilator activity. KB-944 has been demonstrated to produce long lasting coronary vasodilator and hypotensive effects in conscious and anesthetized dogs; increase coronary blood flow in isolated, blood perfused heart preparations of dogs; and reduce systemic pressure in conscious normotensive and hypertensive rats. Slow channel calcium entry blockade is thought to contribute to the vasodilator activity of KB-944. Fostedil is longer acting in hypertensive animals than either nifedipine or diltiazem suggesting a potential clinical advantage for this compound. Unexpectedly, fostedil was shown to produce atrial fibrillation in 3 of 10 hypertensive patients in a placebo controlled study. Fostedil had been in phase II clinical trials for the treatment of angina pectoris. However, this research has been discontinued.
Status:
Investigational
Source:
NCT04172532: Phase 1/Phase 2 Interventional Recruiting Locally Advanced Pancreatic Adenocarcinoma
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Status:
Investigational
Source:
NCT00992563: Phase 2 Interventional Completed Age Related Macular Degeneration
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
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.
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.
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.
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.
Status:
Investigational
Source:
INN:cevoglitazar [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cevoglitazar is a dual agonist for the peroxisome proliferator-activated receptor (PPAR)-alpha and -gamma subtypes. Cevoglitazar was as effective as pioglitazone at improving glucose tolerance, normalizes intramyocellular lipids and reduces body weight gain and adiposity, independent of food intake. Metabolic profiling showed that in the muscle cevoglitazar improves the lipid profile via both PPARα‐ and PPARγ‐mediated mechanisms. Cevoglitazar only induced small changes to the lipid composition of visceral fat. In subcutaneous fat, however, cevoglitazar induced changes similar to those observed with fenofibrate suggesting export of fatty acids from this depot.
Status:
Investigational
Source:
NCT00336713: Phase 3 Interventional Completed Depressive Disorder
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Sanofi aventis developed saredutant (also known as SR 48968C) as a tachykinin neurokinin-2 (NK2) receptor antagonist for the treatment of depressive disorders and generalized anxiety disorder. This drug participated in phase III clinical trials in patients with a generalized anxiety disorder and as Combination Treatment for major depressive disorder, however, the drug failed to meet efficacy endpoints. It is known that NK-2 receptor mediates airway obstruction that is why saredutant was studied as a potential treatment of asthma. However, all studies of the drug were discontinued.
Status:
Investigational
Source:
INN:narmafotinib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04110054: Phase 2 Interventional Completed Chronic Cough
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
