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

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Showing 221 - 230 of 11247 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
INN:itriglumide
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


ITRIGLUMIDE, an anthranilic acid derivative, is a cholecystokinin B receptor antagonist.
Status:
Investigational
Source:
INN:meturedepa [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Meturedepa (also known as AB-132), an alkylating agent that was developed as an antineoplastic drug. Meturedepa was studied to treat lymphomas and leukemias. The drug also participated in the Eastern clinical drug evaluation program for 233 patients with advanced cancer. Information about the current use of this compound is not available.
Status:
Investigational
Source:
NCT00621270: Phase 2 Interventional Completed Major Depressive Disorder
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Coluracetam (code name BCI-540; formerly MKC-231) is a nootropic agent of the racetam family. It was initially developed and tested by the Mitsubishi Tanabe Pharma Corporation for Alzheimer's disease. After the drug failed to reach endpoints in its clinical trials it was in-licensed by BrainCells Inc for investigations into major depressive disorder (MDD). Like most racetam compounds, Coluracetam increases choline uptake, but it also increases uptake in damaged neurons. Specifically, Coluracetam interacts with the HACU process, which is responsible for absorbing choline into the neurons. This increased uptake occurs during the Acetylcholine synthesis process. Since Coluracetam improves choline preservation during this process, a larger amount is converted into Acetylcholine. This results in increased memory, attention and alertness. It is important to note here, that these benefits were only seen in subjects with previously impaired neurons, not in subjects with normally functioning neurons. Coluracetam is also shown to improve AMPA potentiation, which is a process that triggers cognitive function and alertness. Although Coluracetam interacts with choline transporters as well, there isn’t enough evidence to explain why or how this interaction occurs, or what occurs after the interaction. Coluracetam has been in phase II clinical trials for the treatment of major depression and anxiety. However, this research has been discontinued.
Status:
Investigational
Source:
INN:dazepinil [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Dazepinil (HRP 543) is a 1,3-benzodiazepine antidepressant, developed by Hoerscht in the early 1980s. In mouse tests, dazepinil inhibited tetrabenazine-induced ptosis and potentiated yohimbine toxicity. In vitro, dazepinil inhibited norepinephrine and serotonin uptake into rat brain synaptosomes and lacked anticholinergic activity.
Status:
Investigational
Source:
NCT00113893: Phase 2 Interventional Completed Bone Marrow Diseases
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Talmapimod is a p38 MAPK kinase inhibitor that inhibits p38 alpha with IC50 value of 9 nM which is 10-times lower then IC50 for p38 beta. Talmapimod was under clinical development for the treatment of Myelodysplastic Syndromes, Multiple Myeloma and Rheumatoid Arthritis (phase II), however, it seems to be discontinued as no longer presents in Janssen's pipeline.
Status:
Investigational
Source:
INN:rafigrelide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Rafigrelide is an imidazoquinazoline derivative patented by pharmaceutical company Shire LLC as platelet-lowering agent for the treatment of myeloproliferative diseases. Rafigrelide is a chemical analog of anagrelide, which is used to reduce platelet counts in myeloproliferative disorders. Compared with anagrelide, Rafigrelide has reduced potency against phosphodiesterase III, which may help to reduce potential side effects. The concentration of Rafigrelide that produces 50% of the maximum inhibition (IC50) of PDE III is 164 nM, making it an approximately 200-fold less potent inhibitor of phosphodiesterase III than 3-hydroxy anagrelide. In the clinical trial, Rafigrelide showed antithrombotic properties during a two-week treatment period in healthy male volunteers. The reductions in thrombus formation were seen in surrogate models of both high and low shear rates suggesting drug efficacy in different arterial conditions.