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

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Showing 81 - 90 of 4773 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Ethoxazene (2,4-diamino-4-ethoxyazobenzene) is an analgesic compound. It may be used as an indicator of acidity in an examination of gastric function.
Status:
Investigational
Source:
INN:indorenate [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Indorenate (TR3369, INDO) is a serotonin-like compound with high affinity for 5- HT1A receptors and a lower affinity for 5-HT1C and 5-HT1B receptors. Indorenate possesses antihypertensive and anxiolytic activity in animal behaviour tests. Similar to other serotonin receptor agonists, Indorenate also has anorectic activity; this effect was blocked by the administration of the 5-HT2A/2C receptor antagonists cinanserin, cyproheptadine, metergoline and methysergide. A unpublished clinical trial confirmed its antihypertensive activity in men.
Status:
Investigational
Source:
INN:imisopasem manganese [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Imisopasem Manganese is a manganese-based non-peptidyl mimetic of the human mitochondrial manganese superoxide dismutase (MnSOD), with potential antioxidant and radioprotective activities. Metaphore Pharmaceuticals Inc. is developing Imisopasem Manganese for the potential treatment of pain, dermatological disease and inflammation. Upon administration, imisopasem manganese mimics the activity of MnSOD and scavenges reactive oxygen species (ROS), such as superoxide anion, which prevents oxygen free radical damage to macromolecules such as DNA. This reduces ROS-mediated lipid peroxidation, prevents apoptosis and protects against oxygen free radical-induced toxicity in normal tissues.
Status:
Investigational
Source:
INN:girisopam [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Girisopam (GYKI 51189), a 2,3-benzodiazepine, is a compound with anxiolytic and antipsychotic action. It has shown these effects in several animal models. Girisopam differs from the traditional 1,4-benzodiazepines because of its selective anxiolytic action without muscle relaxant and anticonvulsive activity, and because it does not have affinity for 1,4-benzodiazepine receptors. Antidepressant activity of girisopam was also reported. The binding site of girisopam in neuronal cells in the central nervous system is located exclusively to the basal ganglia. Because the danger of tolerance and dependence is lower for 2,3-benzodiazepine than 1,4-benzodiazepines, girisopam may potentially be used in treatment of addiction and affective disorders. No clinical trials were conducted in the US.
Status:
Investigational
Source:
INN:melizame [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Melizame is a sugar substitute for sweetening caloric or noncaloric materials.
Status:
Investigational
Source:
INN:betacetylmethadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Betacetylmethadol is a synthetic narcotic analgesic under international control according to the UN Single Convention 1961.
Status:
Investigational
Source:
INN:evobrutinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Evobrutinib is a highly selective, irreversible inhibitor of Bruton's tyrosine kinase (BTK). It potently inhibits BCR- and Fc receptor-mediated signaling and, thus, subsequent activation and function of B cells and innate immune cells such as monocytes and basophils. Evobrutinib demonstrated effectivity in autoimmune disease preclinical models. Evobrutinib is being developed by Merck Serono for the treatment of various autoimmune disorders.
Sonolisib (PX-866) is a small-molecule inhibitor of the alpha, gamma, and delta isoforms of phosphoinositide 3-kinase (PI3K) with potential antineoplastic activity. Sonolisib inhibits the production of the secondary messenger phosphatidylinositol-3,4,5-trisphosphate (PIP3) and activation of the PI3K/Akt signaling pathway, which may result in inhibition of tumor cell growth and survival in susceptible tumor cell populations. Inhibition of the PI3K pathway with Sonolisib leads to inhibition of cell growth and decreased activation of downstream targets in GBM, both in vitro and in vivo, using U87–tumor-bearing mice, including Akt, S6, and mTOR. Sonolisib was in phase II clinical trials by Oncothyreon for the treatment of glioblastoma multiforme and castration-resistant prostate cancer (CRPC). It was in phase I/II clinical trials for the treatment of malignant melanoma, non-small cell lung cancer and Head and neck cancer. In clinical trials, Sonolisib was well tolerated, with common side effects being diarrhea, nausea, vomiting, and elevated liver enzymes. However, no recent development has been reported.
Status:
Investigational
Source:
INN:aranotin
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Aranotin, a metabolite of Arachniotus aureus, possesses the antiviral and antibiotic properties. It inhibits viral RNA synthesis against strains of rhino-, coxsackie, polio- and parainfluenza viruses.
Status:
Investigational
Source:
JAN:EMITEFUR [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Emitefur or BOF-A2 is a fluorinated pyrimidine antimetabolite exerting antineoplastic properties. It is a compound composed of 5-fluorouracil (5-FU) and 3-cyano-2,6-dihydroxypyridine (CNDP), an inhibitor of 5-FU degradation by dihydrouracil dehydrogenase in order to prolong the blood 5-FU level as well as increase selective toxicity to a tumor. Emitefur demonstrated clinical activity in preliminary studies in Japan. Emitefur development for the treatment of solid tumors has been discontinued.