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

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Showing 1531 - 1540 of 3134 results

Status:
Possibly Marketed Outside US
Source:
Wien Med Wochenschr. 1995;145(1):18-21.: Phase 4 Human clinical trial Completed N/A
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Medrogestone is a progesterone derivative used for the treatment of progesterone deficiency, especially those observed in the premenopausal period, haemorrhages and menorrhagia of fibroids, endometriosis, menstrual cycle disorders, etc. The drug acts by binding and activating progesterone receptors. In Europe, medrogestone is available under the name Colprone, however it is no longer marketed in the USA, Germany and Austria.
Tenidap ([Z]-5-chloro-2,3-dihydro-3-[hydroxy-2-thienylmethylene]-2-oxo-1H-indole-1-carboxamide) is an oxindole derivative, a COX/5-LOX inhibitor and cytokine-modulating anti-inflammatory drug candidate that was under development by Pfizer as a promising potential treatment for rheumatoid arthritis. Tenidap shows potent inhibition of cyclooxygenase in vitro, that is of several magnitudes greater than 5-lipoxygenase inhibition. Lipoxygenase inhibition, however, has been difficult to document in vivo because Tenidap is highly protein bound and free drug concentrations are below those necessary for 5-lipoxygenase inhibition. However, several in-vitro activities distinguish Tenidap from conventional cyclooxygenase inhibitors. As shown with stimulated human neutrophils, tenidap inhibits activation of collagenase, lysosomal enzyme secretion, and superoxide generation, as well as aggregation and adhesion to endothelium. Furthermore, unlike Non-steroidal anti-inflammatory drugs (NSAIDs), it lowers circulating C-reactive protein (CRP) concentrations by a magnitude equivalent to hydroxychloroquine and auranofin. This result suggests an effect on the synthesis and/or release of the cytokines known to induce the acute-phase protein response-namely, IL-1, IL-6, and TNF-alpha. Tenidap, like existing second-line drugs, lowers serum IL-6 concentrations, a property not shared by NSAIDs The cytokine inhibitory effect also includes reduced in-vitro concentrations of TNF-alpha and IL-1 from both RA synovium and peripheral blood mononuclear cells. There is no immunosuppressive effect of Tenidap in either animal or clinical studies. In clinical studies. The comparisons between tenidap and other second-line agents show that Tenidap produced a faster reduction in CRP than Auranofin. The rate of withdrawal because of inefficacy was similar (18-20%) in Auranofin and Tenidap groups. The quality of life using the arthritis impact measurement scales has also been assessed Scores were better with tenidap than with NSAID monotherapy, but equivalent to the second line plus NSAID combinations. Tenidap is registered in the United States, Netherlands, and Italy but is not marketed because marketing approval was rejected by the FDA in 1996 due to liver and kidney toxicity, which was attributed to metabolites of the drug with a thiophene moiety that caused oxidative damage.

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Morinamide is a second line anti-tuberculous agent. In vitro morinamide demonstrated clear dose-dependent bacteriostatic and bactericidal activities. The anti-mycobacterial effect of morinamide was the same as pyrazinamide and was dependent on the acidity of medium (pH 5.6). Liver function test abnormalities following morinamide therapy are usually mild, and onset of jaundice is extremely uncommon. It has been given orally as the hydrochloride in the treatment of tuberculosis.
Status:
Possibly Marketed Outside US
Source:
Tiacob by Sanofi-Synthelabo
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tiapride is a drug that selectively blocks D2 and D3 dopamine receptors in the brain. It is used to treat a variety of neurological and psychiatric disorders including dyskinesia, alcohol withdrawal syndrome, negative symptoms of psychosis, and agitation and aggression in the elderly. A derivative of benzamide, tiapride is chemically and functionally similar to other benzamide antipsychotics such as sulpiride and amisulpride known for their dopamine antagonist effects. Tiapride is marketed under various trade names and is widely available outside of the United States. The most common trade name for tiapride is Tiapridal, which is used throughout Europe, Russia, as well as parts of South America, the Middle East, and North Africa. It is also sold under different names in Italy (Italprid, Sereprile), Japan (Tialaread, Tiaryl, Tiaprim, Tiaprizal), Chile (Sereprid), Germany (Tiaprid, Tiapridex), and China (Tiapride).
Status:
Possibly Marketed Outside US
Source:
NCT02107144: Phase 4 Interventional Completed Coronary Artery Disease
(2014)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Trimetazidine is a medicine, which is used for the treatment of angina pectoris. The drug mechanism of action is explained by its ability to selectively inhibit long-chain 3-ketoacyl coenzyme A thiolase, an enzyme responsible for mitochondrial beta-oxidation of long chain fatty acids. Trimetazidine also increases pyruvate dehydrogenase activity, binds to the mitochondrial membrane, directly inhibits cardiac fibrosis and improves mechanical resistance of the sarcolemma.
Status:
Possibly Marketed Outside US
Source:
GLITISOL by Sterling Winthrop
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Thiamphenicol is a broad-spectrum antibiotic, which is active against gram-positive and gram-negative organisms. The drug is marketed in Asia and Latin America for the treatment of various infections, including sexually transmitted diseases. As many phenicols, thiamphenicol inhibits the protein synthesis in bacterias by binding to 23S ribosomal subunit. In Europe and USA the drug is used in a veterinary practice.
Status:
Possibly Marketed Outside US
Source:
Japan:Cefozopran Hydrochloride
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Cefozopran hydrochloride is a third-generation cephalosporin that was launched for the treatment of severe infections in immunocompromised patients caused by staphylococci and enterococci. While it shows a very broad antibacterial spectrum against Gram-positive and Gram-negative organisms, it is particularly potent against S. aureus, Enterococcus faecalis, P. aeruginosa, and Citrobacter freundii. It is resistant to hydrolysis by most chromosomal and plasmid mediated β-lactamases and is reported to be active against respiratory, urinary tract, obstetrical, gynecological, soft tissue, and surgical infections. Similar to β-lactams, cephalosporins interfere with PBP (penicillin binding protein) activity involved in the final phase of peptidoglycan synthesis. PBP’s are enzymes which catalyze a pentaglycine crosslink between alanine and lysine residues providing additional strength to the cell wall. Without a pentaglycine crosslink, the integrity of the cell wall is severely compromised and ultimately leads to cell lysis and death. Resistance to cephalosporins is commonly due to cells containing plasmid encoded β-lactamases.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)



Nitroscanate (trade name Lopatol) is a medium-spectrum anthelmintic used on dogs and cats. It is available in the form of tablets for oral administration. It is not used on livestock. Nitroscanate is effective against the major gastrointestinal roundworms (nematodes) of dogs and cats (e.g.Toxocara canis, Toxocara cati, Ancylostoma spp, Uncinaria stenocephala) and tapeworms (e.g. Dipylidium caninum, Echinococcus granulosus, Taenia spp, etc.). The molecular mode of action of nitroscanate has not been elucidated. It is assumed that it acts as an uncoupler of the oxidative phosphorylation in the cell mitochondria, which disturbs the production of ATP, the cellular "fuel". This impairs the parasites motility and probably other processes as well.
Status:
Possibly Marketed Outside US
Source:
NCT02807922: Phase 4 Interventional Completed Sleep
(2016)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Conditions:

Zopiclone (brand names Zimovane and Imovane) is a nonbenzodiazepine hypnotic agent used in the treatment of insomnia. The therapeutic pharmacological properties of zopiclone include hypnotic, anxiolytic, anticonvulsant, and myorelaxant properties. Zopiclone and benzodiazepines bind to different sites on GABAA-containing receptors, causing an enhancement of the actions of GABA to produce the therapeutic and adverse effects of zopiclone. The metabolite of zopiclone called desmethylzopiclone is also pharmacologically active, although it has predominately anxiolytic properties. One study found some slight selectivity for zopiclone on α1 and α5 subunits, although it is regarded as being unselective in its binding to α1, α2, α3, and α5 GABAA benzodiazepine receptor complexes. Desmethylzopiclone has been found to have partial agonist properties, unlike the parent drug zopiclone, which is a full agonist. The mechanism of action of zopiclone is similar to benzodiazepines, with similar effects on locomotor activity and on dopamine and serotonin turnover. A meta-analysis of randomised controlled clinical trials that compared benzodiazepines to zopiclone or other Z drugs such as zolpidem and zaleplon has found few clear and consistent differences between zopiclone and the benzodiazepines in sleep onset latency, total sleep duration, number of awakenings, quality of sleep, adverse events, tolerance, rebound insomnia, and daytime alertness. After oral administration, zopiclone is rapidly absorbed, with a bioavailability around 75–80%. Time to peak plasma concentration is 1–2 hours. High-fat meal preceding zopiclone administration does not change absorption (as measured by AUC), but reduces peak plasma levels and delays its occurrence, thus may delay the onset of therapeutic effects. The pharmacokinetics of zopiclone in humans are stereoselective. After oral administration of the racemic mixture, Cmax (time to maximum plasma concentration), area under the plasma time-concentration curve (AUC) and terminal elimination half-life values are higher for the dextrorotatory enantiomers, owing to the slower total clearance and smaller volume of distribution (corrected by the bioavailability), compared with the levorotatory enantiomer. In urine, the concentrations of the dextrorotatory enantiomers of the N-dimethyl and N-oxide metabolites are higher than those of the respective antipodes. Zopiclone is sometimes used as a method of suicide. It has a similar fatality index to that of benzodiazepine drugs, apart from temazepam, which is particularly toxic in overdose.
Status:
Possibly Marketed Outside US

Class (Stereo):
CHEMICAL (ACHIRAL)

Imolamine is a coronary vasodilator, which is used in the treatment of angina pectoris and as a local anesthetic. Imolamine has been shown to produce in animals coronary vasodilation, local anaesthesia, analgesia and a papaverine like action in duodenal preparations. Imolamine increased the tone of uterus and ileum and this was accompanied by a reduction in amplitude of contraction. The response of the stomach tissue to imolamine was similar to that of butalamine and aminophylline, i.e. a relaxant action on smooth muscle. Imolamine has a variable action on tone, producing an increase in ileum and uterus and a decrease in stomach. Imolamine is able to cause severe cytolytic hepatitis.

Showing 1531 - 1540 of 3134 results