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

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Showing 2791 - 2800 of 34988 results

Status:
Investigational
Source:
NCT02569827: Phase 1/Phase 2 Interventional Withdrawn Dengue Fever
(2018)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Modipafant is a dihydropyridine derivative patented by American multinational pharmaceutical corporation Pfizer Ltd. as platelet-activating factor antagonist for bronchoconstriction and asthma treatment. Platelet-activating factor, proposed as an important inflammatory mediator in asthma, reproduces several of the features of asthma, such as microvascular leakage, mucus secretion, bronchoconstriction, and possibly increased airway responsiveness. Unfortunately, in clinical trials, Modipafant failed to demonstrate superior efficacy compared to placebo.
Status:
Investigational
Source:
INN:metiprenaline
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Metiprenaline was developed as a bronchodilator. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:pirdonium bromide
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Pirdonium is an antihistamine agent. It is the hydrophilic Histamine H1 receptor antagonist.
Status:
Investigational
Source:
NCT00957788: Phase 1 Interventional Terminated Tinnitus
(2009)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Gacyclidine (GK11) is a derivative of phencyclidine with neuroprotective properties. Tritiated gacyclidine and its enantiomers bind to NMDA receptors with binding parameters similar to those of other non‐competitive NMDA receptor antagonists. Beneficial effects of gacyclidine include reduction of lesion size and improvement of functional parameters after injury. In traumatic brain injury models, gacyclidine also improves behavioral parameters and neuronal survival. In an animal model of Amyotrophic lateral sclerosis (ALS), functional alteration of locomotor activity was evident and improved the survival of mice, suggesting that chronic administration of gacyclidine beginning at early symptomatic stage may be beneficial for patients with ALS. Gacyclidine has also been associated with altered mental status and end organ damage in patients.
Status:
Investigational
Source:
INN:quazinone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quazinone (also known as Ro 13-6438 ) is a cardiotonic and vasodilator drug which was developed and marketed in the 1980s for the treatment of heart disease. The positive inotropic response to Quazinone of the isolated guinea pig papillary muscle was accompanied by inhibition of myocardial phosphodiesterase (PDE) activity and elevation of intracellular cyclic AMP (cAMP) levels Quazinone had no effect on Na+, K+-stimulated or Ca2+-stimulated ATPase activity and did not influence the rate of calcium uptake in cardiac membrane vesicles. Quazinone caused a concentration-dependent increase in the upstroke velocity, overshoot, and duration of slow action potentials evoked in partially depolarized papillary muscles. Pretreatment of guinea pigs with reserpine did not prevent the effects of Quazinone on slow action potentials but slightly decreased its positive inotropic activity. In clinical trials, Quazinone induces dose-dependent hemodynamic changes, an increase in cardiac index combined with decreases in pulmonary capillary wedge pressure and systemic and pulmonary arterial pressures.
Status:
Investigational
Source:
INN:broquinaldol
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Broquinaldol is a halogenated derivative of quinoline and a member of the class of compounds known as halogenated phenazines. Broquinaldol and related compounds have demonstrated efficacy against antibiotic-tolerant bacterial biofilms and Mycobacterium tuberculosis. Against several bacterial strains, broquinaldol had a minimum inhibitory concentration of 0.78 microM. Broquinaldol was also identified as having antiproliferative activity against thyroid cancer cells in vitro.
GDC-0152 binds to the XIAP BIR3 domain, the BIR domain of ML-IAP, and the BIR3 domains of cIAP1 and cIAP2. GDC-0152 promotes degradation of cIAP1, induce activation of caspase-3/7, and lead to decreased viability of breast cancer cells. GDC-0152 improves outcome in breast cancer and glioma xenografted mouse. GDC 0512 was in phase I development in the US for the treatment of cancer; however, Roche announced in their 2009 results presentation, that development of the agent has been discontinued.
Status:
Investigational
Source:
NCT00479427: Phase 2 Interventional Completed Osteoarthritis
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GW842166 is a pyrimidine cannabinoid 2 (CB2) receptor agonist that was being developed by GlaxoSmithKline for the treatment of inflammatory pain. It has potent analgesic, anti-inflammatory and anti-hyperalgesic actions in animal models, but without cannabis-like behavioural effects due to its extremely low affinity for the CB1 receptor. GW842166 shows similar potency and efficacy for rat and human recombinant CB2 receptors with EC50 of 91 nM and 63nM, respectively. GW842166 is in Phase 2 trial.
Status:
Investigational
Source:
NCT01466088: Phase 2 Interventional Completed Alzheimer's Disease
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


ISPRONICLINE is a partial agonist at the a4b2 subtype of nicotinic acetylcholine receptors (nAChRs) without interaction with other nAChRs or other receptor systems. It has antidepressant, nootropic, and neuroprotective effects. It progressed to phase II clinical trials for the treatment of dementia and Alzheimer's disease but is no longer under development.
Status:
Investigational
Source:
INN:lemildipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Lemildipine is a 1,4-dihydropyridine calcium channel blocker which is under phase III development by Banyu (Merck and Co), in Japan, for its potential to treat hypertension and cerebrovascular ischemia. In one study, involving five patients with essential hypertension accompanied by cerebrovascular disorder, lemildipine, administered orally at doses of 5 to 20 mg/day, significantly lowered blood pressure and increased cerebral blood flow. Another study in 31 patients with essential hypertension demonstrated that lemildipine has significant pressure lowering effects without affecting serum lipids. Worldwide rights to market the drug have been assigned to Kowa in Japan.

Showing 2791 - 2800 of 34988 results