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

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Showing 2051 - 2060 of 39119 results

Status:
Investigational
Source:
INN:maleylsulfathiazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Maleylsulfathiazole is a sulphonamide antibacterial. It was used in the treatment of diarrhea.
Status:
Investigational
Source:
INN:sodelglitazar [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sodelglitazar is an oral insulin sensitiser, a peroxisome proliferator-activated receptor (PPAR) pan agonist that was under development with GlaxoSmithKline for the treatment of hyperlipidaemia, type 2 diabetes mellitus and metabolic syndrome. Sodelglitazar exerts higher binding affinity for the delta subtype as compared to gamma and alpha subtypes. Sodelglitazar was being investigated in Phase II clinical trials for the treatment of T2DM and its complications, but this research has been discontinued.
Status:
Investigational
Source:
INN:nitraquazone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Nitraquazone (TVX 2706) is an phosphodiesterase inhibitor with antiinflammatory action. It strongly enhances the increase in intracellular levels of cyclic AMP caused by appropriate effectors in all systems tested so far. EC50 values are in the submicromolar range. The effect is apparently neither due to an increased responsiveness of the hybrid cells for an effector like prostaglandin E1 nor to an increased activity of adenylate cyclase, but to an inhibition of both low and high affinity cyclic AMP phosphodiesterases. Half-maximal inhibition of enzyme activity is obtained at 10 uM TVX 2706. TVX 2706 does not interfere with the calmodulin activation of phosphodiesterase. Nitraquazone affected cytokine production by PHA-stimulated human blood cells. Nitraquazone was active in reducing the production of IL-5 (IC50 = 0.8 uM), while its potency against IL-2, GM-CSF and IFN-gamma was 3-6 times lower.
Status:
Investigational
Source:
NCT00000763: Phase 1 Interventional Completed Sarcoma, Kaposi
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



TNP-470 (AGM-1470, (3R,4S,5S,6R)-5-methoxy-4- [(2R,3R)-2-methyl-3-(3-methyl-2-butenyl) -oxiranyl]-1-oxaspiro[2,5]oct-6-yl(chloroacetyl) carbamate) is an anti-angiogenic, semisynthetic analogue of fumagillin, a known antibiotic secreted by the fungus Aspergillus fumigatus fresenius, which is under clinical development for the treatment of cancer by Takeda Chemical Industries Ltd. in Japan and TAP Pharmaceuticals, Inc. in the United States. TNP-470 binds to and irreversibly inactivates methionine aminopeptidase-2 (MetAP2), resulting in endothelial cell cycle arrest late in the G1 phase and inhibition of tumor angiogenesis. This agent may also induce the p53 pathway, thereby stimulating the production of cyclin-dependent kinase inhibitor p21 and inhibiting angiogenesis. In early clinical reports, TNP-470 is tolerated up to 177 mg/m(2) with neurotoxic effects (fatigue, vertigo, ataxia, and loss of concentration) being the principal dose-limiting toxicity (DLT). TNP-470 is being evaluated in Phase I-II trials in the US in patients with Kaposi’s sarcoma, cervical cancer, breast cancer, brain cancer, prostate cancer and renal cell carcinoma.
Status:
Investigational
Source:
INN:quilostigmine
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Quilostigmine (also known as NXX-066) is an isoquinolinecarboxylate patented by Hoechst-Roussel Pharmaceuticals Inc as a memory enhancer. Quilostigmine acts as acetylcholinesterase inhibitor and studies as a potential drug for treating Alzheimer’s disease. Quilostigmine is well absorbed from the gastrointestinal tract, but the oral bioavailability poor to moderate in rats and dogs because of pre-systemic metabolism. In preclinical studies has demonstrated activity in animal models of memory function. In clinical trials, Quilostigmine was well tolerated in healthy subjects up to a single dose of 64 mg and multiple doses of 60 mg QD for seven days
Status:
Investigational
Source:
NCT00346502: Phase 1/Phase 2 Interventional Withdrawn Dysplastic Nevus Syndrome
(2006)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Betulinic acid (BA) is a plant-derived pentacyclic triterpenoid that exerts potent anti-cancer effects in vitro and in vivo. It`s anticancer property is linked to its ability to induce apoptotic cell death in cancer cells by triggering the mitochondrial pathway of apoptosis. In contrast to the cytotoxicity of betulinic acid against a variety of cancer types, normal cells and tissue are relatively resistant to betulinic acid, pointing to a therapeutic window. Compounds that exert a direct action on mitochondria present promising experimental cancer therapeutics, since they may trigger cell death under circumstances in which standard chemotherapeutics fail. Thus, mitochondrion-targeted agents such as betulinic acid hold great promise as a novel therapeutic strategy in the treatment of human cancers. Betulinic acid has antiretroviral, antimalarial, and anti-inflammatory properties. Betulinic acid exerts its inhibitory effect by preventing topoisomerase I-DNA interaction as a result of which the 'cleavable complex' is not formed. In consequence, it also acts as an antagonist to camptothecin-mediated cleavage. The antitumor pharmacological effects of BA consist of triggering apoptosis via the mitochondrial pathway, regulating the cell cycle and the angiogenic pathway via factors, including specificity protein transcription factors, cyclin D1 and epidermal growth factor receptor, inhibiting the signal transducer and activator of transcription 3 and nuclear factor‑κB signaling pathways, preventing the invasion and metastasis of tumor cells, and affecting the expression of topoisomerase I, p53 and lamin B1. Betulinic Acid has also been used in trials studying the treatment of Dysplastic Nevus Syndrome. Betulinic acid acts as anti-melanoma agent through inhibiting aminopeptidase N activity with IC50 of 7.3 uM. Betulinic acid is an inhibitor of HIV-1 with EC50 of 1.4 uM.
Status:
Investigational
Source:
INN:diclonixin
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Diclonixin is the analgesic and anti-inflammatory agent.
Status:
Investigational
Source:
INN:dicresulene [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Dicresulene is the antiseptic agent. It was used as a hemostatic drug for the control of persistent bleeding.
Status:
Investigational
Source:
INN:cinfenoac
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Cinfenoac is a chalcone derivative patented by a pharmaceutical company Biorex Laboratories from the UK. The compound is claimed for the treatment of inflammatory and allergic conditions, as well as for the treatment of the ulcerous condition of the gastrointestinal tract.
Status:
Investigational
Source:
INN:properidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Properidine is an isopropyl analog of pethidine that acts as opioid analgesic.

Showing 2051 - 2060 of 39119 results