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

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Showing 471 - 480 of 4716 results

Status:
Investigational
Source:
INN:ciclafrine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Ciclafrine is azaspiroalkane derivative patented by pharmaceutical company Goedecke A.-G. for the low blood pressure treatment
Status:
Investigational
Source:
NCT02860000: Phase 2 Interventional Active, not recruiting Estrogen Receptor Status
(2017)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Alisertib (MLN8237) is an orally available selective aurora A kinase inhibitor developed by Takeda. Alisertib inhibited AAK over ABK with a selectivity of more than 200-fold in cells and produced a dose-dependent decrease in bipolar and aligned chromosomes in the HCT-116 xenograft model, a phenotype consistent with AAK inhibition. Alisertib inhibited proliferation of human tumor cell lines in vitro and produced tumor growth inhibition in solid tumor xenograft models and regressions in in vivo lymphoma models. It is currently in phase II clinical trials for acute myeloid leukaemia; B cell lymphoma; brain cancer; mesothelioma; prostate cancer; small cell lung cancer.
Status:
Investigational
Source:
INN:pranidipine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)


Pranidipine is the calcium channel blocker. Pranidipine did not affect the sensitivity of the contractile proteins to calcium. Pranidipine also did not alter cyclic GMP-induced relaxation in alpha-toxin-skinned vascular preparations. Pranidipine also prolonged glyceryl trinitrate-induced relaxation in the endothelium denuded rat aorta. Pranidipine enhances cyclic GMP-independent NO-induced relaxation of smooth muscle by a mechanism other than through NO-induced hyperpolarization. These effects were in direct contrast to amlodipine, another new 1,4-dihydropyridine calcium antagonist. Pranidipine increased blood velocity and probably blood flow in the optic nerve head, choroid, and retina of rabbits. Pranidipine was not detrimental to global cardiac function in animals with dilated cardiomyopathy. Pranidipine enhances relaxation produced by endothelium-derived relaxing factor in carotid artery. Pranidipine was investigated as pharmacological agent for the treatment of angina pectoris and hypertension.
Status:
Investigational
Source:
NCT00937937: Phase 2 Interventional Active, not recruiting Acral Lentiginous Melanoma
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Dinaciclib (SCH 727965) is a small molecule inhibitor of cyclin-dependent kinases. Dinaciclib demostrates potent and selective inhibition of CDK2, CDK5, CDK1, and CDK9 activity. Dinaciclib inhibits cell cycle progression and proliferation in various tumor cell lines in vitro. Dinaciclib is a product of a drug discovery collaboration between Pharmacopeia (later Ligand Pharmaceuticals) and Schering-Plough (later Merck & Co.) that began in 1998. Dinaciclib showed promising effect in treating haematological malignancies and solid tumors.
Status:
Investigational
Source:
INN:rioprostil
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Rioprostil is a methylprostaglandin E1 analog. Rioprostil inhibits gastric acid secretion and enhances the gastric mucus-bicarbonate barrier. In peptic ulcer cases, it facilitates the healing process and the elimination of pain. Rioprostil can also be used to prevent recurrence of duodenal ulcers. However, its development has been discontinued in 2000.
Status:
Investigational
Source:
NCT00597662: Phase 1 Interventional Completed Adhesions
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fostriecin, an antitumor antibiotic produced by Streptomyces pulveraceus, is a strong inhibitor of serine/threonine protein phosphatases type 2A and type 4, and inhibits the catalytic activity of partially purified Topo II (type II topoisomerase) in a non-competitive manner.
Status:
Investigational
Source:
INN:cronidipine
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Cronidipine (LF 2.0254) is a calcium channel blocker. LF 2.0254 inhibited in a time-dependent fashion K(+)- and Ca2(+)-induced contractions of rabbit aorta with respective IC50 of 2.7 nM and 1.7 nM. Cronidipine had a long-lasting antihypertensive action in spontaneously hypertensive rats and was able to decrease blood pressure and increase heart rate and plasma renin activity in hypertensive dogs.
Status:
Investigational
Source:
INN:fluzinamide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Fluzinamide (AHR-8559), an anticonvulsant agent that was studied in patients with refractory partial seizures. However, information about the further development of this drug is not available.
Status:
Investigational
Source:
NCT01800838: Phase 1 Interventional Completed Recurrent Cutaneous T-cell Non-Hodgkin Lymphoma
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)