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

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Showing 931 - 940 of 14117 results

Status:
Investigational
Source:
INN:picumeterol
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Picumeterol (GR114297A) is a potent and highly selective beta2-adrenoceptor agonist with a longer duration of action than salbutamol, but shorter than salmeterol. Picumeterol is the (R)-isomer of the racemic entity GR63411B, and picumeterol has been shown to be about 40 times more potent than the (S)-isomer (GR114744A) in various in vitro pharmacological models of beta2-agonist activity. Picumeterol is of potential value in the treatment of asthma and related diseases in man following inhalation administration. In the clinical studies, the bronchodilator potencies of picumeterol and GR 63411B were similar. However, both drugs were short-acting, which is at odds with their activity in vitro. These compounds display dissociation between bronchodilator activity and protection against methacholine-induced bronchoconstriction.
Status:
Investigational
Source:
NCT00752011: Phase 1 Interventional Completed Cancer
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


3'-C-ethynylcytidine (Ethynylcytidine, TAS-106) is a synthetic cytidine nucleoside containing a covalently bound ethynyl group with potential antineoplastic and radiosensitizing activities. 3'-C-ethynylcytidine is metabolized in tumor cells to ethynylcytidine triphosphate (ECTP), which inhibits RNA synthesis by competitive inhibition of RNA polymerases I, II and III; subsequently, RNase L is activated, resulting in apoptosis. RNase L is a potent antiviral and antiproliferative endoribonuclease that cleaves singled stranded RNA, causes 28s rRNA fragmentation, and activates Janus Kinase (JAK), a mitochondrial-dependent apoptosis signaling molecule. Development of a cytosine derivative of 3'-ethynyl ribonucleoside, TAS-106, as an intravenously administered treatment for solid tumours was discontinued. A phase II trial in patients with head and neck cancer was terminated in the US.
Status:
Investigational
Source:
INN:loreclezole [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Loreclezole was found to be active in all animal models of seizures, whether a genetic model of reflex epilepsy was used or models where seizures were elicited by chemical or electrical stimulation. In addition, loreclezole was active against both TON and CLON seizures and increased the threshold for behavioral as well as EEG seizures. Loreclezole has a very rapid onset of action and a duration of the activity, which in certain tests last for more than 24 hr. Chronic administration for 5-7 days did not lead to tolerance to the anticonvulsant action of loreclezole. Loreclezole potentiates gamma-aminobutyric acid (GABA) type A receptor function, by interacting with a specific allosteric modulatory site on receptor beta-subunits. It also acts as a negative modulator at a novel regulatory site, enhancing GABAA receptor sensitization. Inhibits homomeric ρ1 GABAC receptors.
Status:
Investigational
Source:
INN:nantradol [INN]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Status:
Investigational
Source:
INN:ceftioxide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Ceftioxide is broad-spectrum , beta-lactam antibiotic patented by German pharmaceutical company Hoechst A.-G.
Status:
Investigational
Source:
USAN:CEFUROXIME PIVOXETIL [USAN]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Cefuroxime Pivoxetil is an ester prodrug of cefuroxime, a semisynthetic, broad-spectrum, beta-lactamase-resistant, second-generation cephalosporin with antibacterial activity. Cefuroxime binds to and inactivates penicillin-binding proteins (PBPs) located on the inner membrane of the bacterial cell wall. PBPs are enzymes involved in the terminal stages of assembling the bacterial cell wall and in reshaping the cell wall during growth and division. Inactivation of PBPs interferes with the cross-linkage of peptidoglycan chains necessary for bacterial cell wall strength and rigidity. This results in the weakening of the bacterial cell wall and causes cell lysis.
Status:
Investigational
Source:
INN:amelometasone
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Conditions:

TS-410 (Amelometasone), is a topical anti-inflammatory steroid. Amelometasone lotion - external steroid preparation - is marketed in Japan.
Status:
Investigational
Source:
INN:dimepregnen
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dimepregnen is an antiestrogen agent.
Status:
Investigational
Source:
NCT00430300: Phase 2 Interventional Terminated Pulmonary Disease, Chronic Obstructive
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



UK-432097 is a selective adenosine A2a agonist which was in development with Pfizer as an inhaled treatment for asthma and chronic obstructive pulmonary disease. UK-432097 had been in phase II clinical trials by Pfizer for the treatment of chronic obstructive pulmonary disease (COPD). However, this study was terminated prematurely due to futility based on results of interim analysis.
Status:
Investigational
Source:
INN:primidolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Primidolol (also known as UK-11,443) is an imidazolidinone derivative patented by American pharmaceutical corporation Pfizer Corp as a specific β-adrenergic blocker. In clinical trials, Primidolol shows some antihypertensive activity but the overall change in the cardiovascular parameters failed to demonstrate a significant difference compared to placebo.