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

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Showing 2631 - 2640 of 34988 results

Status:
Investigational
Source:
USAN:CYPOTHRIN [USAN]
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Cypothrin is a synthetic pyrethroid insecticide, developed by American Cyanamide for the control of ticks and marketed under the tradename Panecto. The compound exhibited systemic insecticidal activity in the model of flies infestation in mice and ixodicidal activity in against larvae of Boophilus microplus.
Status:
Investigational
Source:
INN:viprostol
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Viprostol (also known as CL115,347), a prostaglandin E2 congener that was studied as an antihypertensive agent. Viprostol has a potent and prolonged blood pressure lowering effect in many models of hypertension. In clinical studies, viprostol has been demonstrated to lower arterial blood pressure significantly in man following transdermal and/or intravenous administration. The antihypertensive action of viprostol has been suggested to be the result of peripheral vasodilatation. In addition, the drug participated in a clinical trial in normal subjects and in patients with Raynaud's phenomenon. It was found the optimal dosage was 1000 ug; the effect could last for 84 hours; higher dosage may be associated with a "steal" phenomenon.
Status:
Investigational
Source:
INN:levomequitazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Levomequitazine is the L-enantiomer of mequitazine. The antihistaminergic activity mainly resides in the S-enantiomer, L-mequitazine, whereas the anticholinergic activity mainly resides in the D-enantiomer. It was shown, that L-enantiomer of mequitazine is less potent antagonist of human M3 muscarinic acetylcholine receptors than D-enantiomer. In vitro binding studies have shown that the affinity of L-mequitazine for H1 receptors is approximately ten times higher and to muscarinic receptors ten times lower, compared to d-mequitazine. Memory impairment was observed after administration of L-mequitazine 10 mg alone on delayed recall. This could be due to indirect effects of H1 receptor blockade. L-mequitazine 10 mg produced mild driving impairment, whereas L-mequitazine 2.5 and 5.0 mg show no effects on driving. Levomequitazine had been in phase III clinical trials by Pierre Fabre for the treatment of perennial allergic rhinitis and seasonal allergic rhinitis.
Status:
Investigational
Source:
NCT01313572: Phase 3 Interventional Terminated Coronary Artery Disease
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Apadenoson (BMS-068645) is a selective adenosine 2A agonist that contains a methyl ester group which undergoes esterase hydrolysis to its acid metabolite. Apadenoson had been in phase III clinical trials by Forest (now a part of Allergan) for the treatment of coronary artery disease. However, this study has been terminated.
Status:
Investigational
Source:
INN:dazolicine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dazolicine is an anti-arrhythmic compound, developed by the German company Roechlingsche Eisen & Stahl. In patients with various types of arrhythmia, after i.v. injection the drug proved to have very strong antiarrhythmic potency and rather a low incidence of side effects. After oral treatment, ectopic beats were eliminated in only 4 of 10 patients.
Status:
Investigational
Source:
INN:moxicoumone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Moxicoumone is orally available coumarin derivative patented by Francesco, Vismara, Societa per Azioni for capillary fragility treatment
Bardoxolone methyl, the C-28 methyl ester of 2-cyano-3,12-dioxoolean-1,9-dien-28-oic acid (CDDO) known as CDDO-Me or RTA 402, is one of the derivatives of synthetic triterpenoids. Bardoxolone methyl directly blocks IKKbeta activity and thereby the NF-kappaB pathway by interacting with Cys-179 in the IKKbeta activation loop. Binding of bardoxolone methyl to Kelch-like erythroid cell-derived protein with CNC homology-associated protein 1 (Keap1) disrupts its critical cysteine residues, leading to the release of the nuclear factor erythroid 2-related factor 2 (Nrf2), which hinders its ubiquitination and finally leads to its stabilization and nuclear translocation. In the nucleus, Nrf2 activates the transcription of phase 2 response genes, leading to a coordinated antioxidant and anti-inflammatory response. In addition, it acts as an antagonist of the peroxisome proliferator-activated receptor gamma. Through Keap1/Nrf2 and nuclear factor-κB pathways, this agent can modulate the activities of a number of important proteins that regulate inflammation, redox balance, cell proliferation and programmed cell death. This agent is generally well tolerated, but it may increase adverse cardiovascular events. Presently, it is being further tested for the treatment of patients with chronic kidney disease, cancer, and pulmonary arterial hypertension.
Status:
Investigational
Source:
NCT01556607: Phase 1 Interventional Completed Drug Safety
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


VP-14637 (also known as MDT 637) was developed as an inhibitor of respiratory syncytial virus (RSV). RSV is the leading cause of respiratory tract infections in humans. VP-14637 participated in phase I clinical trial to evaluate the safety and pharmacokinetic profile of the drug in healthy human volunteers. However, further study was discontinued because of the strategic decision.
Apilimod is a small molecule inhibitor of interleukin-12 and interleukin-23 synthesis thereby preventing IL-12/IL-23 mediated immune responses. Apilimod is also observed to inhibit the nuclear accumulation of NF-kappB protein family, and viral infections dependent on phosphatidylinositol-3-phosphate 5-kinase (PIKfyve). Apilimod has been investigated as a potential treatment for a number of autoimmune conditions.
Status:
Investigational
Source:
NCT00373516: Phase 2 Interventional Completed Psoriasis
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Becocalcidiol is a vitamin D analog participated in phase II clinical trials as a topical treatment for psoriasis. Therapy was safe and well tolerated, however further studies were discontinued.

Showing 2631 - 2640 of 34988 results