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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Moxazocine is a benzomorphan derivative patented by Bristol-Myers Co. as potent opioid analgesic. Moxazocine acts as a partial agonist or mixed agonist/antagonist of the opioid receptors and binds preferentially to the κ-opioid receptor. In clinical studies, Moxazocine demonstrated superior efficacy compared morphine, but was never marketed.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Dilopetine is a racemic mixture of (+)-E-6006 citrate (E-6101) and (-)-E6006 citrate (E-6102) enantiomers being developed as a potential antidepressant. Initial experiments indicate that dilopetine exhibits an antidepressant profile in tests with mice and rats. Dilopetine has been observed to normalize the increased substance P levels in the periaqueductal gray of rats during stressor exposure (Hamon, personal communication), suggesting that the drug may function by inhibiting substance P release. Treatment with dilopetine reduced the vocalizing of isolated guinea pig pups in a dose-dependent fashion.
Status:
Investigational
Source:
NCT00394628: Phase 1/Phase 2 Interventional Unknown status Glioblastoma Multiforme
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Banoxantrone (formally known as AQ4N), a bioreductive drug that is irreversibly converted to AQ4, a stable DNA affinic cytotoxic compound. Banoxantrone is activated by haem-containing reductases such as inducible nitric oxide synthase (iNOS). In hypoxic cells, AQ4N is reduced to the topoisomerase II inhibitor AQ4. By inhibition of topoisomerase II within these hypoxic areas, AQ4N has been shown to sensitize tumors to existing chemo- and radiotherapy treatments. Novacea, the company which was responsible for clinical trials for banoxantrone had decided to scale back on its clinical development, including discontinuing the clinical trial in acute lymphoblastic leukemia and delaying the planned clinical trial in B-cell lymphoma. The company decided to continue enrollment in an ongoing Phase 1b/2a clinical trial in patients with glioblastoma multiforme. However, further information about these clinical trials are not available. Some recent experiments have shown that targeting hypoxic tumors with high levels of iNOS with a combination of AQ4N and radiotherapy could be a useful clinical therapeutic strategy.
Status:
Investigational
Source:
NCT04669028: Phase 3 Interventional Completed Alzheimer Disease
(2021)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
HE3286, a synthetic derivative of androst-5-ene-3β,7β,17β-triol (AET), a non-glucocorticoid anti-inflammatory metabolite of the adrenal steroid, dehydroepiandrosterone is under development by Harbor BioSciences as an anti-inflammatory; antiepileptic drugs; antihyperglycemic agent. HE3286 was studied in phase I clinical trials in Obese Adult Subjects, in Patients With Rheumatoid Arthritis in Patients With Active, Mild-to-Moderate Ulcerative Colitis, and in Patients With Type 2 Diabetes Mellitus. In all these studies were determined safety, tolerance, pharmacokinetics, and activity of HE3286. In addition, was shown that HE3286 acted via binding, regulation and/or activation of MAPK or ERK, or through modulation of NFκB. Experiments on animals have shown that the drug could have a neuroprotective influence in glaucoma, as well as other chronic neurodegenerations.
Status:
Class (Stereo):
CHEMICAL (MIXED)
Hexopyrronium is an antihistaminic agent. Its gastric antisecretory action was studied in human. Information about the current use of this drug is not available.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conorphone (TR5109) is an opioid of mixed agonist-antagonist analgesic class. In animal models, conorphone demonstrated an analgesic activity in the same range as morphine, and lack of addiction liability. Conoprphone was evaluated in a clinical trial for postoperative pain in the oral surgery model and in patients with postepisiotomy pain. The 40 mg dose of conorphone resulted in a significant incidence of side effects such as drowsiness, dizziness, nausea, and vomiting.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Quiflapon Sodium (MK-0591; (3-[1-(4-chlorobenzyl)-3-(t-butylthio)-5-(quinolin-2-yl-methoxy)- indol-2-yl]-2,2-dimethyl propanoic acid, previously L-686,708) had been in phase II clinical studies for the treatment of inflammatory bowel disease, but the study was discontinued later, because in spite of MK-591 markedly inhibited Leukotrienes (LT) biosynthesis, it did not differ significantly from placebo in clinical efficacy. Also was discovered, that MK-0591 may modify the airway changes associated with bronchial hyper responsiveness, as well as offer symptomatic relief in asthma. MK-0591 is a selective and specific 5-Lipoxygenase-activating protein (FLAP) inhibitor with an IC50 value of 1.6 nM in a FLAP binding assay. In additional, recently was discovered, that MK591 possesses all major attributes of a standard anti-metastatic agent with significant cancer-selective effect, and suggest that MK591 may turn out to be an effective agent for therapy of castration-resistant, bone-metastatic prostate cancer. Though details of the molecular underpinnings of the anti-metastatic action of MK591 are unknown at this time, this finding gives an opportunity for further exploration to better understand the signaling mechanisms involved by in vitro and in vivo experiments.
Status:
Investigational
Source:
INN:pemaglitazar [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Pemaglitazar was developed as a dual peroxisome proliferator-activated receptors alpha and gamma (PPAR- α,γ) agonist. Information about the further development of this drug is not available.
Status:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Methyldihydromorphine is a synthetic narcotic analgesic related to the morphine. This compound has no pharmaceutical value in the US.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Algestone is a progesterone like female hormone. Algestone is a C21-steroid that is pregn-4-ene substituted by oxo groups at position 3 and 20 and hydroxy groups at positions 16 and 17. It has a role as a progestin. It is a 20-oxo steroid, a 16alpha-hydroxy steroid, a 17-hydroxy steroid, a C21-steroid, a 3-oxo-Delta(4) steroid and a tertiary alpha-hydroxy ketone. It derives from a hydride of a pregnane. Algestone is used as anti-inflammatory drug (topical) and combination with enanthate as injectable contraceptive.
