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

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Showing 141 - 150 of 2243 results

Status:
Investigational
Source:
INN:narlaprevir [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Narlaprevir (formerly SCH 900518), a NS3 protease inhibitor is being developed by R-Pharm for the treatment of a chronic hepatitis C (genotype 1). Narlaprevir is a potent inhibitor of hepatitis C virus (HCV) NS3 protease with a Ki of 7 ± 1 nM and a 90% inhibitory concentration (IC90) of ∼28 ng/ml for HCV genotype 1 replicon in vitro. Narlaprevir successfully passed extensive pre-clinical and clinical trials in Schering-Plough Research Institute (USA) and in a variety of clinical centers of Europe, USA and Russia. Based on clinical findings R-Pharm obtained a registration certificate for Arlansa (Narlaprevir) ЛП-003622 dd 12.05.2016 issued by Ministry of Healthcare of the Russian Federation.
Status:
Investigational
Source:
NCT02124447: Not Applicable Interventional Withdrawn Patients Undergoing Screening or Surveillance Colonoscopy
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

N-Acetylsulfanilyl chloride is a benzenesulfonyl chloride derivative used as intermediate in the synthesis of various pharmaceuticals and organic compounds. N-Acetylsulfanilyl chloride is also used in the synthesis of N,N-dimethylsulfanilamide as the internal standard in the reaction. The reaction is used to determine tramadol and its O-demethylated metabolite in blood plasma.
Status:
Investigational
Source:
NCT00504790: Phase 1 Interventional Completed Cancer
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

GSK-923295 is a small-molecule inhibitor of the mitotic kinesin centromere-associated protein E (CENP-E), and the third novel drug candidate to arise from Cytokinetics' broad strategic alliance with GlaxoSmithKline (GSK). GSK-923295 demonstrated a broad spectrum of activity against a range of human tumor xenografts grown in nude mice, including models of colon, breast, ovarian, lung and other tumors. GSK-923295 is the first drug candidate to enter human clinical trials that specifically targets CENP-E and is currently in Phase I human clinical trials being conducted by GSK. GSK-923295 inhibited release of inorganic phosphate and stabilized CENP-E motor domain interaction with microtubules. Inhibition of CENP-E motor activity in cultured cells and tumor xenografts caused failure of metaphase chromosome alignment and induced mitotic arrest, indicating that tight binding of CENP-E to microtubules is insufficient to satisfy the mitotic checkpoint. Consistent with genetic studies in mice suggesting that decreased CENP-E function can have a tumor-suppressive effect, inhibition of CENP-E induced tumor cell apoptosis and tumor regression.
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:dacisteine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Dacisteine is a derivative of a N-acetylcysteine, where a second acetyl group is attached to a sulfur atom. Dacisteine is marketed in France under tradename Mucothiol for the treatment of disorders of bronchial secretion, acute bronchitis and acute episode of chronic bronchopneumopathies. Dacisteine exerts its action on the gel phase of the mucus, presumably by breaking the disulfide bonds of the glycoproteins, and thus promotes the expectoration.
Status:
Investigational
Source:
INN:cartasteine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cartasteine is thioether derivative patented by Beijing Beipeng Technology Co. for resisting platelet aggregation and preventing or treating cardiovascular and cerebrovascular diseases
Status:
Investigational
Source:
INN:eflumast
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Eflumast (RP42068; N-(2-hydroxy-3-acetyl-5-fluorophenyl)-5-carboxamido-1H tetrazole) is an antiallergic agent. It was under development as an orally active antiasthmatic.
Status:
Investigational
Source:
INN:telenzepine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Telenzepine is a selective muscarinic M1 receptor antagonist that was studied for selective inhibition of gastric acid secretion. Telenzepine was used in clinical trials in patients with acute duodenal ulcer, where was found that once daily administration of 3 mg in the evening must be regarded as the optimal dosage regimen of telenzepine. However, the preregistration for peptic ulcer in Germany was discontinued. In addition, the drug was studied in patients with nocturnal asthma. It was shown that telenzepine via the oral route at a dose of up to 5 mg was not effective in preventing nocturnal asthma.
Status:
Investigational
Source:
NCT00352313: Phase 1/Phase 2 Interventional Completed Brain and Central Nervous System Tumors
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Status:
Investigational
Source:
INN:molracetam
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Information in the literature related to the biological and/or pharmacological properties of molracetam is absent.