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

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Showing 271 - 280 of 13993 results

Status:
Investigational
Source:
NCT00506012: Phase 2 Interventional Terminated Myoclonus
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

T-2000 is an oxopyrimidine derivative patented by Taro Pharmaceutical Industries Ltd. as a tranquilizing agent. T-2000 acts as a modulator of GABA A receptor with well-documented anticonvulsant activity and little sedation in animal models. In vitro, equimolar concentrations of T-2000 and phenobarbital produce equivalent enhancement of GABA-evoked chloride currents. Unfortunately, in clinical trials T-2000 failed to demonstrate efficacy in older patients with essential tremor. Moreover, daily administration of T2000 resulted in higher total blood barbiturate levels, likely accounting for the poor tolerability.
Status:
Investigational
Source:
NCT00485394: Phase 2 Interventional Unknown status Age-Related Macular Degeneration
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Othera Pharmaceuticals developed OT-551 as an antioxidant and anti-inflammatory agent. OT-551 downregulates the overexpression of the protein complex nuclear factor (NF)-kappa B. It is known that NF-kappa B is highly activated when oxidative stress, inflammation, and angiogenesis occurs. OT-551 was studied in phase II clinical trial for the treatment of age-related macular degeneration. In addition, the drug was studied for the treatment of cataracts and dry eyes; however, these studies were discontinued. Besides, phase II clinical trial for the treatment of geographic atrophy has shown that OT-551 might have limited or no benefit as a treatment for this disease.
Status:
Investigational
Source:
NCT00379990: Phase 2 Interventional Completed Arthritis, Rheumatoid
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

GW 274150 was developed by GlaxoSmithKline as a selective inhibitor of inducible nitric oxide synthase (iNOS; also known as NOS2). Nitric oxide synthase (NOS) is an important chemical involved in the production of NO. Reduction of NOS, and therefore NO, may be an effective technique for the treatment of migraine headache. GW 274150 offered the potential of anti-inflammatory activity in migraine through a novel mechanism of action. The drug has completed phase II of the clinical trials for patients with rheumatoid arthritis and migraine disorders. In addition, GW 274150 was involved in phase I clinical trial for patients with mild asthma. However, all these studied were discontinued.
Status:
Investigational
Source:
NCT00519376: Phase 2 Interventional Completed Pulmonary Disease, Chronic Obstructive
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

VILANTEROL α-PHENYL CINNAMATE (GW642444H), originally developed by GlaxoSmithKline, is a long-acting β2 adrenoceptor agonist for once daily treatment of COPD and asthma. Phase III clinical trials are ongoing. GW642444H is Vilanterol a-phenylcinnimate salt. In clinical studies the study drug may been given as a dry powder in the form of either the ‘H’ salt (with the excipient lactose), or in the form of the ‘M’ salt (with the excipients lactose and cellobiose octaacetate). Its pharmacological effect is attributable to stimulation of intracellular adenylyl cyclase which catalyzes the conversion of adenosine triphosphate (ATP) to cyclic-3',5'-adenosine monophosphate (cAMP). Increases in cyclic AMP are associated with relaxation of bronchial smooth muscle and inhibition of release of hypersensitivity mediators from mast cells in the lungs.
Status:
Investigational
Source:
NCT00972504: Phase 2 Interventional Completed Rhinitis, Allergic, Seasonal
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

GSK-1004723 is a dual histamine H(1) and H(3) receptor antagonist with a long duration of action that has been investigated for the treatment of allergic rhinitis. GSK-1004723 was designed for intranasal administration as a suspension or solution. Clinical trials (phase 1 and 2) showed that GSK-1004723 is well tolerated and demonstrates clinically significant attenuation of symptoms (tested in an environmental allergen challenge chamber). However, attenuation of symptoms was less than seen for treatment with cetirizine (a commonly used over-the-counter antihistamine).
NGX267 is a partial muscarinic receptor agonist with functionally specific M1 and M3 receptor activity, developed by Torrey Pines Therapeutics(TPTX) for the treatment of Xerostomia, Alzheimer’s disease and cognitive deficits in schizophrenia. NGX-267 had been in phase II clinical trials for the treatment of Xerostomia, however, all researchers on this drug candidate were discontinued.
Status:
Investigational
Source:
NCT00861549: Phase 1 Interventional Completed Healthy
(2008)
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Phencynonate (PHH) is a novel anticholinergic compound. It is structurally similar to scopolamine, possesses both muscarinic and nicotinic antagonistic properties as well as anti-NMDA properties. It has been developed as a safe and effective drug for the prevention of motion sickness in tablet form, it also demonstrates clear anticonvulsant effectiveness after soman poisoning in a rat model. S-isomer was more effective against motion sickness and had not anxiogenic action at therapeutic doses. S-isomer has the higher affinity and activity for mAChR in cerebral cortex and acted as a competitive mAChR antagonist. PHH was able to suppress chronic unpredictable mild stress (CUMS)-induced oxidative stress and enhance the antioxidant capacity and antioxidant proteins activity, such as superoxide dismutase 2 (SOD2) and peroxiredoxin 6 (Prdx6). PHH ameliorated CUMS-induced depressive phenotypes by up-regulating SIRT6 deacetylation activity. PHH-mediating SIRT6 pathway is required for antidepressant response and PHH can be used as a novel therapeutic to effectively treat depression. Phencynonate is in phase III clinical trials for the treatment of vertigo.
Status:
Investigational
Source:
NCT00345774: Phase 2 Interventional Completed Pulmonary Hypertension
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



5-((4-(6-Chlorothieno[2,3-d]pyrimidin-4-ylamino)piperidin-1-yl)methyl)-2-fluorobenzonitrile monofumarate (PRX-08066) is a selective 5-hydroxytryptamine receptor 2B (5-HT2BR) antagonist that causes selective vasodilation of pulmonary arteries. This drug was discovered and developed by Predix (later Epix) Pharmaceuticals and is being researched for the treatment of pulmonary arterial hypertension. In animal studies, PRX-08066 has been found to reduce several key indicators of pulmonary arterial hypertension and improved cardiac output, with similar efficacy to established drugs for this condition such as bosentan, sildenafil, beraprost and iloprost.
Status:
Investigational
Source:
NCT00993421: Phase 2 Interventional Terminated Obesity
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


LY377604 is a human β3-adrenergic receptor agonist and β1- and β2-adrenergic receptor antagonist with no sympathomimetic activity at the β1- and β2-adrenergic receptors. Combination of LY377604 and a norepinephrine-serotonin uptake inhibitor (sibutramine) was studied in the treatment of obesity. LY377604 would ameliorate side effect of sibutramine treatment (increase in blood pressure and heart rate due to activation of the sympathetic nervous system).
Status:
Investigational
Source:
NCT00412620: Phase 2 Interventional Terminated Schizophrenia
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Abbott Laboratories was developing the selective dopamine D3 receptor antagonist, ABT-925 (formerly A 437203), for the treatment of schizophrenia. ABT-925 is a selective dopamine D₃ receptor antagonist with an approximately 100-fold higher in vitro affinity for dopamine D₃ versus D₂ receptors. ABT 925 was undergoing phase II clinical development for the treatment of schizophrenia. However, development was discontinued in December 2007.