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

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Showing 4371 - 4380 of 6957 results

Status:
Investigational
Source:
NCT00992667: Phase 1 Bronchial Asthma
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Apocynin, also known as acetovanillone, is a natural organic compound related to vanillin. It has been isolated from a variety of plant sources. Metabolites of apocynin are able to block the activity of NADPH oxidase, thus giving apocynin antioxidant and anti-inflammatory capabilities. Effects of apocynin on the concentration of reactive oxygen and nitrogen species in patients with asthma and chronic obstructive pulmonary disease were investigated in phase I clinical trials. In preclinical models, it was found that apocynin provides neuroprotective effects in models of stroke and Parkinson's disease.
Status:
Investigational
Source:
NCT03127124: Phase 1/Phase 2 Pancreatic Adenocarcinoma Metastatic
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



3-Phenylpropionic acid (hydrocinnamic acid, HA) is an end-product of the bacterial degradation of unabsorbed phenylalanine in the intestinal lumen. HA is used in ice cream, drinks, and candy manufacture field as a flavoring agent. In recent years, HA is widely used in the pharmaceutical industry. Hydrocinnamic Acid inhibits the currents of WT and SQT3 syndrome-related mutants of Kir2.1 channel.
Status:
Investigational
Source:
INN:FORMETOREX [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Status:
Investigational
Source:
NCT02783794: Phase 2 Stage IV Breast Cancer
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Phenyl sodium is organometallic compound. It is used to carry exchange reactions to produce phenylmalonic acid.
Status:
Investigational
Source:
INN:DROXINAVIR [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00014547: Phase 2 Lung Cancer
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT00014690: Phase 2 Primary Peritoneal Cavity Cancer
(2001)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
NCT01963208: Phase 3 Drug Resistant Partial Onset Seizure
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Ganaxolone (3alpha-hydroxy-3beta-methyl-5alpha-pregnan-20-one) (GNX) is the 3beta-methylated synthetic analog of allopregnanolone; it belongs to a class of compounds referred to as neurosteroids. GNX is an allosteric modulator of GABA(A) receptors acting through binding sites which are distinct from the benzodiazepine binding site. It has activity in a broad range of animal models of epilepsy. GNX has been shown to be well tolerated in adults and children. In early phase II studies, GNX has been shown to have activity in adult patients with partial-onset seizures and epileptic children with history of infantile spasms. It is currently undergoing further development in infants with newly diagnosed infantile spasms, in women with catamenial epilepsy, and in adults with refractory partial-onset seizures. Ganaxolone is a CNS-selective GABAA modulator being developed in three different dose forms (IV, capsule, and liquid) intended to maximize therapeutic reach to adult and pediatric patients in both acute and chronic care settings.Ganaxolone is a synthetic analog of endogenous allopregnanolone, which has been shown to be an effective anticonvulsant by restoring electrical balance to the seizing brain. While allopregnanolone’s anticonvulsant and anti-anxiety activities are well documented, allopregnanolone has the potential to convert back to its metabolic precursor progesterone, which could lead to hormonal side effects. Ganaxolone has been designed with an added methyl group that prevents back conversion to an active steroid which unlocks ganaxolone’s potential for chronic use. In preclinical studies, ganaxolone exhibited potency and efficacy comparable to allopregnanolone. Both ganaxolone and allopregnanolone bind to GABAA at the synaptic and extrasynaptic binding sites. Activity with extrasynaptic GABAA receptors are of particular importance for treating patients who developed tolerance to benzodiazepines and barbiturates. Ganaxolone binds to the GABAA receptors, which opens the pore to allow chloride ions to move into the postsynaptic neuron, leading to the inhibition of neurotransmission.

Showing 4371 - 4380 of 6957 results