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

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Showing 821 - 830 of 13311 results

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

Class (Stereo):
CHEMICAL (ABSOLUTE)

Rolicyprine (EX-4883) is an antidepressant. This compound is a potent inhibitor of monoamine oxidase in vivo. One study found that rolicyprine must be biotransformed before it is a pharmacologically active compound. Once it is activated, Rolicyprine appears to have a pharmacology like that of the antidepressant tranylcypromine. It was suggested that the products of this biotransformation are tranylcypromine and pyrrolidone carboxylic acid. No information on current use of rolicyprine is available.
Status:
Investigational
Source:
NCT00023387: Not Applicable Interventional Completed Tuberculosis
(2000)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Status:
Investigational
Source:
NCT00605787: Phase 2 Interventional Completed Type 2 Diabetes Mellitus
(2002)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Tetradecylthioacetic acid (TTA) is a hypolipidemic antioxidant with immunomodulating properties involving activation of peroxisome proliferator-activated receptors (PPARs). TTA exerts both hypolipidemic and anti-inflammatory effects in psoriasis patients - TTA can be of therapeutic benefit for a subgroup of psoriatic patients. TTA may improve myocardial function in heart failure, potentially involving its ability to decrease the availability of free fatty acids in plasma and increase the myocardial proportion of n-3 polyunsaturated fatty acids. TTA attenuates dyslipidemia in patients with type 2 diabetes mellitus. These effects may occur through mechanisms involving PPAR-alpha and PPAR-delta activation, resulting in increased mitochondrial fatty acid oxidation.
Status:
Investigational
Source:
NCT03088670: Phase 3 Interventional Completed Diabetes Mellitus, Type 2
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Gosogliptin (PF-734200) is a compound developed for treatment of type II diabetes and has been approved for use in Russia. It is a selective dipeptidyl peptidase 4 (DPP-4) inhibitor, with hypoglycemic activity. The drug is safe and well tolerated at all doses tested when added to metformin (a diabetes drug), and safely and effectively lowered HbA (1c) in subjects receiving metformin. A phase 3 study to study the safety and efficacy of gosogliptin has been completed. Gosogliptin has also been studied as potential drug for the treatment of renal insufficiency.
Status:
Investigational
Source:
Eur J Cancer Clin Oncol. May 1986;22(5):601-5.: Phase 2 Human clinical trial Completed Breast Neoplasms
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Carubicin (also known as Carminomycin) is an anthracycline antineoplastic antibiotic isolated from the bacterium Actinomadura carminata. Carubicin intercalates into DNA and interacts with topoisomerase II, thereby inhibiting DNA replication and repair and RNA and protein synthesis. The drug is active against a variety of experimental tumors. Pharmacology studies in animals revealed that the drug bound largely to serum proteins and that it was widely distributed. In clinical trials The main toxic effect was myelosuppression but gastrointestinal intolerance and alopecia were also reported. Objective partial responses were seen in two of seven previously untreated patients with non-small cell lung cancer and one of three patients with squamous cell carcinoma of the head and neck previously untreated with chemotherapy.
Status:
Investigational
Source:
NCT01139151: Phase 1 Interventional Completed Leukemia
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Thiarabine (also known as OSI-7836) is a new-generation deoxycytidine nucleoside analog with potent anticancer activity. As with other nucleoside analogs, Thiarabine is a prodrug and requires intracellular phosphorylation by deoxycytidine kinase to the active form (Thiarabine-triphosphate), which then competes with deoxycytidine for incorporation into DNA resulting in cell death. In xenograft studies using lung, colon, pancreatic, breast, and melanoma models, Thiarabine shows superior antitumor activity in most of these tumors, particularly in lung and pancreatic models, compared with gemcitabine, cisplatin, and paclitaxel. Thiarabine seems to be less schedule dependent than gemcitabine, showing antitumor activity with a variety of schedules in preclinical studies. In clinical trials, Thiarabine administration was associated with excessive fatigue, and despite changes in its schedule and duration of administration.
Status:
Investigational
Source:
INN:flovagatran [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

FLOVAGATRAN is a potent, reversible, low-molecular-weight, highly selective synthetic direct thrombin inhibitor that has demonstrated promising pharmacokinetic properties and biological activity in preclinical studies. However, its development for thrombosis was discontinued in Phase II.
Status:
Investigational
Source:
NCT00842335: Phase 1/Phase 2 Interventional Completed Advanced Solid Tumors
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


CGI-1842 (also known as JI-101) is an oral multi-kinase inhibitor that targets vascular endothelial growth factor receptor type 2 (VEGFR-2), platelet derived growth factor receptor β (PDGFR-β), and ephrin type-B receptor 4 that has been used in trials studying the treatment of Cancer, Colon Cancer, Neuroendocrine, Ovarian Cancer, and Advanced Solid Tumors. By targeting multiple angiogenesis signaling pathways in tumor vessel beds, CGI-1842 has the potential to inhibit multiple stages of tumor angiogenesis and thus enhance anti-tumor efficacy. In preclinical models, CGI-1842 induced concentration-dependent blocking of both EphB4- and VEGF-stimulated signaling pathways and has shown excellent antitumor activity. CGI-1842 is well tolerated in cancer patients and has shown impressive activity in Phase I clinical trials.
Status:
Investigational
Source:
NCT01766622: Phase 2 Interventional Withdrawn Ovarian Neoplasms
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

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.