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Restrict the search for
m nalidixic acid
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Iosulamide is triiodobenzoic acid derivative patented by Sterling Drug Inc as an X-ray contrast agent. Iosulamide shows clear advantages in animal tests over meglumine iodipamide. The intravenous toxicity of Iosulamide meglumine is considerably lower than that of iodipamide (Cholografin) in the mouse and rat. Studies of biliary and urinary excretion patterns indicate Iosulamide is rapidly excreted compared to iodipamide, while at the same time providing equal concentrations in bile. More efficient blood to bile clearance rate and a shorter blood half-life for Iosulamide may account for the lower circulating blood levels and rapid total excretion compared to iodipamide. Iosulamide's rapid blood-bile clearance coupled with its extremely low toxicity may allow rapid administration of high doses, affording superior visualization and safety compared to iodipamide.
Class (Stereo):
CHEMICAL (RACEMIC)
Carbenzide is hydrazine derivative with the high antidepressant activity and low toxicity patented by pharmaceutical company Warner-Lambert Pharmaceutical Co. Carbenzide acts via monoamine oxidase (MAO) inhibition and increase the level of brain serotonin.
Status:
Investigational
Source:
INN:recoflavone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Recoflavone (DA-6034) is a synthetic derivative of eupatillen (flavone derivative). It has antioxidant properties, and anti-inflammatory effects in inflammatory bowel disease (IBD). Although the exact mechanism is still unknown, recoflavone may decrease intestinal permeability in an indomethacin-induced intestinal injury model via the extracellular signal-regulated kinase pathway. In a phase I clinical trial, recoflavone was well tolerated and minimally absorbed in healthy volunteers. In other (phase II and III) clinical trials, the drug has been evaluated for use in treatment of gastritis (phase III), dry eyes, and Crohn’s disease (discontinued).
Status:
Investigational
Source:
NCT00741442: Phase 2 Interventional Completed Hyperuricemia
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Buthalital is a barbiturate derivative which was under development as a short-acting anesthetic. However, development was discontinued, perhaps due to its extremely rapid elimination rate] and buthalital sodium was never marketed.
Status:
Investigational
Source:
NCT01038440: Not Applicable Interventional Completed Sudden Cardiac Death
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
INN:silmitasertib [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
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).
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
Class (Stereo):
CHEMICAL (RACEMIC)
Lodelaben (SC-39026) is a human neutrophil elastase inhibitor. Its inhibition of elastase is reversible and noncompetitive at low concentrations. Inhibition is "mixed" at higher inhibitor concentrations. SC-39026 is inactive against hog pancreatic elastase, bovine alpha-chymotrypsin and Pseudomonas aeruginosa elastase, but does inhibit human neutrophil cathepsin G. Lodelaben was developed as antiarthritic agent and tested as adjunct to emphysema therapy. Monocrotaline-injected rats given SC-39026 had significantly lower mean pulmonary artery pressure than those given vehicle, and this correlated with a significant reduction in the number of abnormally muscularized arteries at alveolar wall level. SC-39026 did not significantly reduce monocrotaline-induced medial hypertrophy of muscular arteries, endothelial injury, and associated subendothelial edema. Lodelaben reduces endotoxin-induced lung dysfunction in awake sheep.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
ISALMADOL is an analgesic agent.
