{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
{{facet.count}}
Status:
Investigational
Source:
USAN:UNDECANOATE [USAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Undecanoic acid (UDA) is a fatty acid with significant antimycotic activity. Undecanoic acid is a straight-chain, eleven-carbon saturated medium-chain fatty acid found in body fluids; the most fungitoxic of the C7:0 - C18:0 fatty acid series. It has a role as a human metabolite and an antifungal agent. It is a straight-chain saturated fatty acid and a medium-chain fatty acid. It is a conjugate acid of an undecanoate. It derives from a hydride of an undecane. Undecanoic acid inhibited the production of exocellular lipase and keratinase but stimulated the production of exocellular phospholipase A in T. rubrum undecanoic acid-resistant mutant (udar). At its minimum inhibitory concentration, undecanoic acid inhibits biosynthesis of phosphatidyl serine, phosphatidyl ethanolamine and polyphosphoinositol but does not inhibit the synthesis of phosphatidyl glycerol, phosphatidyl choline, phosphatidyl inositol and phosphatidic acid in Trichophyton rubrum. At higher concentration, however UDA inhibits biosynthesis of all phosphatides present in this dermatophyte. UDA also affects catabolism of these phosphatides. This inhibitory effect of UDA may be partially responsible for its toxic action on T. rubrum.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Maridomycin is a macrolide antibiotic. Sreptomyces sp. No. B-5050 was found to produce maridomycin. Maridomycin was found to be composed of six components, maridomycins I, II, III, IV, V and VI. Their structures are different from each other in acyl moieties at C3 and C4" positions. Maridomycins I, II, III, IV, V and VI showed similar antibacterial spectra against Gram-positive bacteria including acid-fast bacteria. Maridomycin has bacteriostatic activity rather than bactericidal activity. Prominent therapeutic effect was observed against certain Gram-positive bacterial infection in mice.
Class (Stereo):
CHEMICAL (MIXED)
Sulfinalol is a hydroxyphenylalkanolamine derivative patented by Sterling Drug Inc. as the antiarrhythmic, antihypertensive, vasodilating, and adrenergic agent. Oral administration of sulfinalol reduces the pressure of conscious spontaneously hypertensive rats. Antihypertensive action of sulfinalol was inhibited by propranolol pretreatment. Sulfinalol demonstrates effective beta-adrenergic blockade at the antihypertensive dose tested as judged by inhibition of the chronotropic responses to sympathetic stimulation and isoproterenol in pithed rats. In the renal hypertensive dog. sulfinalol lowered both systolic and diastolic blood pressure to normal values with an only slight change in heart rate.
Status:
Investigational
Source:
NCT01294202: Phase 2 Interventional Completed Gastrointestinal Stromal Tumor (GIST)
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Onalespib (AT13387; (2,4-dihydroxy-5-isopropyl-phenyl)-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindol-2-yl] methanone, l-lactic acid salt), is wholly owned by Astex, a novel, high-affinity HSP90 inhibitor, which is currently being clinically tested, has shown activity against a wide array of tumor cell lines, including lung cancer cell lines. As a targeted inhibitor of Hsp90, onalespib has the potential to control the proliferation of multiple solid tumors and hematological malignancies where uncontrolled cell growth is dependent on the interaction between Hsp90 and its client proteins. Astex is pursuing an approach based on the observation that addition of onalespib to a molecularly targeted agent may delay the emergence of resistance to the agent, and hence prolong the window of therapeutic benefit. Onalespib is currently being evaluated via a CRADA with the National Cancer Institute (NCI) in various tumor types, and in a Phase 1/2 clinical study in combination with AT7519, Astex CDK inhibitor.
Status:
Investigational
Source:
NCT03070132: Phase 3 Interventional Withdrawn Trigeminal Neuralgia
(2023)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Raxatrigine also known as GSK1014802 and CNV-1014802, is a novel analgesic under development by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN). It is a novel state dependent small molecule sodium channel blocker that preferentially inhibits the Nav 1.7 ion channel, a therapeutic target implicated by genetics in human pain conditions. Raxatrigine is thought to penetrate the central nervous system and block Nav channels in a novel manner. CNV1014802 was granted orphan drug designation in 2013 by the US Food and Drug Administration (FDA) for the treatment of trigeminal neuralgia.
Status:
Investigational
Source:
JAN:SEPIMOSTAT MESILATE [JAN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT02585934: Phase 3 Interventional Completed Alzheimer's Disease
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Intepirdine, also known as SB-742457, RVT-101, was originally developed by GlaxoSmithKline (GSK) as an antagonist of the serotonin receptor 6 (5-HT6). GSK sold the rights for further study of this drug to Axovant Sciences in 2014. Intepirdine is in phase 3 clinical trial for Alzheimer's and in a phase 2 trial for dementia with Lewy bodies.
Status:
Investigational
Source:
NCT01137526: Phase 2 Interventional Completed Alzheimer's Disease
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT01529736: Not Applicable Interventional Completed Partial Edentulism
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00604916: Early Phase 1 Interventional Completed Pneumonia
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Tebufenozide, a non-steroidal insect growth regulator, is extensively used to control pests. It is considered an environmentally friendly pesticide due to its specificity on target insects. However, some studies have found that tebufenozide is cytotoxic to man, although the exact mechanism is unknown. Experiments with human cells have shown that tebufenozide induced DNA damage in HeLa cells. This effect was achieved by inducing the cell cycle arrest and by apoptosis through activating the p53 protein in a Bax- and Bcl-2-triggered mitochondrial pathway.