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

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Showing 5491 - 5500 of 167129 results

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

Class (Stereo):
CHEMICAL (RACEMIC)

Gloxazone is a drug tested against anaplasmosis and cowdriosis, both tick-borne diseases. It was found to cause toxicity in the kidneys of rats and also had unacceptably high toxic levels in lactating cattle.
Status:
Investigational
Source:
INN:freselestat
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)



Freselestat (ONO-6818) is reversible, nonpeptide high affinity and selective human neutrophil elastase inhibitor, which was under development by Ono for the potential treatment of inflammatory conditions, such as rheumatoid arthritis, inflammatory bowel disease and chronic obstructive pulmonary disease (COPD). Freselestat mediated neutrophil elastase inhibition, leads to the reduction of interleukin 8 production and the reduction of the complement membrane attack complex formation. Freselestat competitively inhibits neutrophil elastase in humans, rats, and hamsters, but does not inhibit other proteases such as pancreatic elastase, trypsin, proteinase 3, cathepsin G, or matrix metalloproteinases. Freselestat inhibits acute lung injury induced by neutrophil elastase in rats, minimizing lung hemorrhage, the accumulation of neutrophils in the lung and suppresses leukocyte levels in an in vivo model of COPD. Freselestat was in phase I studies for COPD in Japan and the US. However, due to abnormal variations in liver function, the development of Freselestat was terminated.
Status:
Investigational
Source:
INN:pazinaclone
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Isoindoline pazinaclone (also known as DN-2327), a partial agonist at GABAA benzodiazepine receptors, produced anxiolytic, taming and anti-convulsive effects. This neuropsychiatric drug was involved in phase II clinical trial for patients with generalized anxiety disorder. However, this study was discontinued.
Status:
Investigational
Source:
NCT03897036: Phase 1 Interventional Active, not recruiting Carcinoma, Basal Cell
(2019)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Silmitasertib (CX-4945) is a potent and selective orally bioavailable small molecule inhibitor of Casein kinase II (CK2). The antiproliferative activity of CX-4945 against cancer cells correlated with expression levels of the CK2α catalytic subunit. CX-4945 caused cell-cycle arrest and selectively induced apoptosis in cancer cells relative to normal cells. When administered orally in murine xenograft models, CX-4945 was well tolerated and demonstrated robust antitumor activity. Senhwa Biosciences is developing silmitasertib for the treatment of cholangiocarcinoma, other solid tumours, Castleman's disease (giant lymph node hyperplasia) and multiple myeloma. The compound was originally developed by Cylene Pharmaceuticals. Phase Ib/II development is underway in the US and South Korea for the treatment of cholangiocarcinoma, and development in the remaining indications is at the phase I stage. As at July 2016, no recent reports of development had been identified for phase-I development in Giant-lymph-node-hyperplasia in USA (PO, Capsule), phase-I development in Multiple-myeloma in USA (PO, Capsule), phase-I development in Solid-tumours (Late-stage disease) in USA (PO, Capsule).
Status:
Investigational
Source:
NCT00230581: Phase 2 Interventional Completed Irritable Bowel Syndrome
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

DDP-225 (also known as MCI-225), a thienopyrimidine analog, is a selective noradrenaline reuptake inhibitor with serotonin receptor antagonism. It shows antidepressant-like properties in animal models. MCI-225 could be useful in the treatment of attentional deficits and related cognitive dysfunctions in psychiatric disorders.
Status:
Investigational
Source:
Int J Radiat Oncol Biol Phys. Apr 2014;88(5):1025-31.: Phase 1 Human clinical trial Completed Liver Neoplasms/radiotherapy
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Yttrium is a soft, silvery metal. Yttrium is often used as an additive in alloys. It increases the strength of aluminium and magnesium alloys. It is also used in the making of microwave filters for radar and has been used as a catalyst in ethene polymerisation. Yttrium-aluminium garnet (YAG) is used in lasers that can cut through metals. It is also used in white LED lights. Yttrium oxide is added to the glass used to make camera lenses to make them heat and shock resistant. It is also used to make superconductors. Yttrium oxysulfide used to be widely used to produce red phosphors for old-style colour television tubes. Radioactive isotope yttrium-90 is used in targeted tumor radiotherapy and nuclear medicine imaging of yttrium-90 radioactivity with bremsstrahlung imaging and positron emission tomography.
Status:
Investigational
Source:
NCT00081172: Phase 2 Interventional Completed Prostate Cancer
(2004)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Lutetium is a silvery-white, hard, dense metal. Lutetium is little used outside research. One of its few commercial uses is as a catalyst for cracking hydrocarbons in oil refineries. Lutetium-177 radionuclide is used in radiopharmaceutical therapy. FDA approved Lutetium-177 dotatate for the treatment of somatostatin receptor-positive gastroenteropancreatic neuroendocrine tumors (GEP-NETs).
Status:
Investigational
Source:
INN:serazapine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Serazapine (CGS15040) is an anxiolytic agent. It is structurally novel 5-HT2 receptor antagonist. Preliminary preclinical findings indicated an anticonflict effect in a behavioral suppression test, and two preliminary investigations in volunteers also suggested anxiolytic potential. In the first of these studies serazapine resembled diazepam, a reference anxiolytic drug, electroencephalographically. Additionally, in a test of psychogenic stress in volunteers it reduced cardiac output.
Status:
Investigational
Source:
INN:bidisomide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Bidisomide (previously known as SC 40230) was developed as a sodium channel antagonist with class I antiarrhythmic properties. Bidisomide participated in clinical trials for patients with arrhythmia. However, the development was discontinued due to a lack of demonstrable efficacy.
Status:
Investigational
Source:
INN:spiriprostil
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Spiriprostil (IBI-P-01028 or R,S-cis-6-(6'-carboxyhexyl)-7-trans-n-hexyl-1,3-diazaspiro-[4-4]-nona n-2,4- dione) is a cytoprotective agent. It is an anti-ulcer agent.

Showing 5491 - 5500 of 167129 results