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

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Showing 1831 - 1840 of 132111 results

Status:
Investigational
Source:
INN:pirtenidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirtenidine is the antimicrobial agent. Pirtenidine was found to be highly efficacious against oral plaque-forming microorganisms. Adherence of Candida spp. to buccal epithelial cells in vitro was significantly reduced after both short- and long-term periods of yeast exposure to sub-inhibitory concentrations of pirtenidine. The drug was shown to cause extensive leakage of cytoplasmic contents from the Candida albicans cells which was correlated with morphological and ultrastructural changes in the yeast. Pirtenidine affects the lipids and sterol composition of C. albicans.
Status:
Investigational
Source:
INN:taltrimide [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Taltrimide, a taurine derivative that was developed as an anticonvulsive agent. Taltrimide strongly inhibits the sodium-independent binding of taurine to synaptic membranes of the brain and it does not appear to bind to GABAA and benzodiazepine receptor. The drug was studied in phase II clinical trial Finland as an anticonvulsant agent to treat epilepsy. However, the further development of this drug was discontinued.
Status:
Investigational
Source:
INN:octabenzone [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Conditions:

Octabenzone is a UV absorber/screener. It is used to protect polymers (e.g., polyethylene, polypropylene, polyvinylchloride) against damage by UV light.
Status:
Investigational
Source:
INN:libecillide
Source URL:

Class (Stereo):
CHEMICAL (UNKNOWN)

Libecillide is a specific monovalent penicilloyl hapten inhibitor of allergic reactions to penicillin. A depression of skin hypersensitivity to PPL and/or penicillin and penicillin derivatives sometimes persisting for weeks and months was obvious in numerous allergic patients submitted to combined libecillide-penicillin treatment. A depressing effect on antipenicillin antibody titers detected by passive hemaglutination was also manifest in some patients. The overall tolerance of libecillide in allergic patients has been very good. Nevertheless, the major obstacle to a wider general use of libecillide at the present time appears to be the occurrence of positive skin reactions to that compound in approximately 5 percent of patients allergic to penicillin.
Status:
Investigational
Source:
INN:ladostigil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

LADOSTIGIL, a rasagiline derivative, is a reversible acetylcholinesterase and butyrylcholinesterase inhibitor with neuroprotective properties. It also acts as an irreversible brain monoamine oxidases inhibitor. It is under development for the treatment of neurodegenerative disorders like dementia and Alzheimer's disease.
Bimosiamose, discovered by Encysive Pharmaceutical and presently being developed by Revotar Biopharmaceuticals, is an 863 g/mol molecular weight dimer with minimal carbohydrate content and is, to date, the leading selectin inhibitor in clinical development. It was developed as anti-inflammatory drug fir the treatment of acute chronic inflammatory disorders including COPD. This compound has shown promise in a phase IIa 'proof of concept' trial in patients with asthma, reducing airway recruitment of eosinophils after intravenous administration. In acute lung injury, neutrophils (a type of white blood cells, thus belonging to the group of cells of the body’s defence system-the immune system) are drawn to the small lung bloodvessels and migrate into the air sacs (alveoli). There they release substances, which cause the inflammation leading to further destruction of the lung tissue. Bimosiamose disodium is expected to hinder the migration of these neutrophils into the alveoli.
Status:
Investigational
Source:
INN:bisbendazole
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Bisbendazole was developed as an anthelmintic agent.
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.
Dacinostat (also known as LAQ824), is a hydroxamate histone deacetylase inhibitor with potential anticancer activity. Dacinostat inhibits histone deacetylase enzymatic activities in vitro and transcriptionally activated the p21 promoter in reporter gene assays. Tumor cells treated with Dacinostat caused acetylation of HSP90 and degradation of its cargo oncoproteins. Flow cytometry studies revealed that both tumor cell lines and normal diploid fibroblasts arrested in the G2/M phase of the cell cycle after Dacinostat treatment. However, an increased sub-G1 population at 48 h (reminiscent of apoptotic cells) was only observed in the cancer cell lines treated with Dacinostat. Dacinostat exhibited antitumor effects in a xenograft animal models. In phase I trials, Dacinostat was well tolerated at doses that induced accumulation of histone acetylation, with higher doses inducing changes consistent with HSP90 inhibition. In another phase 1 in patients with advanced solid tumors, grade 3 or 4 toxicities were observed. Dacinostat had been in phase II clinical trials by Novartis for the treatment of solid tumors but further studies were discontinued.
Status:
Investigational
Source:
INN:cinperene [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Cinperene is an investigational compound proposed for clinical use as a strong and long-acting peripheral central anticholinergic. In animal models, cinperene inhibited mydriasis, pilocarpine-induced salivation, and lacrimation, scratching, hunching and other symptoms.

Showing 1831 - 1840 of 132111 results