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Restrict the search for
methylene blue
to a specific field?
Status:
Investigational
Source:
NCT01588548: Phase 1 Interventional Completed Advanced Solid Malignancies
(2012)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
AZD-1208 is an orally available, potent and highly selective Pim inhibitor that effectively inhibits all three isoforms. AZD-1208 inhibits the growth of several AML cell lines and sensitivity correlates with the level of Pim-1 expression, STAT5 activation and presence of protein tyrosine kinase mutation. AZD-1208 causes cell cycle arrest and apoptosis in MOLM-16 cells in culture. This is accompanied by a dose-dependent reduction in phosphorylation of BAD, 4EBP1 and p70S6K. In addition, AZD-1208 leads to potent inhibition of colony growth of primary AML cells from bone marrow aspirates and downregulates phosphorylation of Pim targets. AZD-1208 was in Phase 1 trials to evaluate the safety and tolerability profile and to determine the maximum tolerated dose (MTD). There were two trials where AZD-1208 had been administered orally in AML and solid tumour (of all types) patients. The studies had being discontinued due to safety reasons.
Status:
Investigational
Source:
INN:clodanolene [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Clodanolene is a skeletal muscle contraction antagonist, closely related to dantrolene sodium. The drug has no measurable direct effect on the peripheral or central nervous systems. In a mouse of muscle spasticity (Straub-tail mouse), clodanolene induced skeletal muscle relaxation more effectively than neuromuscular blocking agents, local anesthetics, or centrally-acting muscle relaxants. Indirect evidence indicates clodanolene acts on caffeine-sensitive calcium stores in the muscle cells.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Tigemonam is a dialkylazetidinone derivative patented by E. R. Squibb and Sons, Inc. as a beta-lactam agent useful for the treatment of bacterial infections. Of the orally active beta-lactams, tigemonam is one of the most potent, with a spectrum of activity similar to that of aztreonam and highly resistant to hydrolysis by the beta-lactamase enzymes. Tigemonam inhibits 90% of Escherichia coli, Klebsiella spp., Proteus spp., Salmonella spp., Haemophilus influenzae and Branhamella catarrhalis tested. In localized infections, tigemonam also demonstrated excellent in vivo activity. In acute pyelonephritis in mice caused by Escherichia coli or Proteus sp., tigemonam was very effective. In a rat lung model with Klebsiella pneumoniae, tigemonam was active with a median effective dose of 46 mg/kg compared with 160 mg/kg for cefaclor and over 200 mg/kg for amoxicillin.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Azaspirium was studied as a spasmolytic and antihypertensive agent.
Status:
Investigational
Source:
INN:darbufelone [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Darbufelone mesylate is a dual inhibitor of cellular prostaglandin and leukotriene production. Darbufelone potently inhibits PGHS-2 (IC50 = 0.19 uM) but is much less potent with PGHS-1 (IC50= 20 uM). Darbufelone is a dual inhibitor of cellular PGF2R and LTB4 production. Darbufelone is orally active and nonulcerogenic in animal models of inflammation and arthritis. Darbufelone mesylate was in phase III clinical trials by Pfizer and Zhuhai United Laboratories for the treatment of rheumatoid arthritis.
Class (Stereo):
CHEMICAL (RACEMIC)
Pirazmonam is a potent anti-gram-negative monobactam that is differentiated from aztreonam by its high intrinsic activity against Ps. aeruginosa and good activity against Pseudomonas species. Pirazmonam has generally poor activity against gram-positive aerobic bacteria and anaerobic bacteria. Pirazmonam is a Trojan Horse molecule containing a b-lactam antibiotic that has been developed based on bacterial iron uptake systems. It features high structural similarity to aztreonam attached to a 3-hydroxy-4-pyridinone iron chelating group. Pirazmonam exhibited strong affinity to penicillin-binding protein 3 (PBP3) of Escherichia coli and moderate to negligible affinity to the other E. coli PBPs.
Status:
Investigational
Source:
NCT00909688: Phase 1 Interventional Completed Healthy
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
BLI 489 was developed by Wyeth as a 6-methylidene-penem β-lactamase inhibitor for the treatment of bacterial infections and urinary tract infections. BLI-489 has shown the promising clinical data, however, development of this drug, was discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Xorphanol (also known as TR5379M) is a full κ-opioid receptor agonist and is a partial agonist at μ opioid receptor. Clinically, xorphanol was studied as an orally active analgesic that provided effective pain relief but showed low physical dependence liability. Further development of this drug was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Bendacalol (also known as CGS 10078B) is an alpha- and beta-adrenergic receptor inhibitor with calcium entry blocking effect was studied for the treatment of hypertension. Animal experiments have sown some positive results. However, information about further studies is not available.
Status:
Investigational
Source:
NCT00275197: Phase 2 Interventional Completed Depressive Disorder, Major
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Elzasonan (CP 448187) is a serotonin 1B/1D receptor antagonist. Elzasonan was primarily metabolized via oxidative N‐demethylation, N‐oxidation, and aryl hydroxylation. Pfizer was developing elzasonan for the treatment of anxiety and affective disorders however development has been discontinued.
