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Restrict the search for
alpha-tocopherol acetate
to a specific field?
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lirexapride serotonin 5-HT4 receptor and dopamine D2 receptor agonists. It had been in phase II clinical trials for the treatment of irritable bowel syndrome. However, this research has been discontinued.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lexacalcitol (KH1060) is over 100 times more active than 1alpha,25-dihydroxyvitamin D3 and is of potential interest in the treatment of psoriasis and other diseases characterized by accelerated cell growth and T lymphocyte activation, which was studied in the clinical trial. KH1060 also prevents type I diabetes in the preclinical investigation without significant effects on calcium or bone metabolism. In addition also was shown that neuroblastoma (NB) cell lines were more susceptible to growth inhibition by KH1060, suggesting its possible use in NB to potentiate the action of retinoids, which are in clinical use for this disease. The underlying biochemical reasons for the increased biological activity of KH1060 are unknown, but it can include 1) metabolic considerations in addition to explanations based upon 2) enhanced stability of KH1060-liganded transcriptional complexes.
Status:
Investigational
Source:
INN:fenmetozole [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Fenmetozole is an alpha-2 adrenergic receptor antagonist which was developed for the treatment of schizophrenic and/or depressed patients, however never reached the market. It was also shown that the drug may reduce symptoms of minimal brain dysfunction in children and antagonize the effect of barbiturates and ethanol.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Lobuprofen is an ester type analgesic, in which the acid moiety (ibuprofen) has peripheral analgesic activity and the alcohol moiety (mCPPol) has central analgesic activity.
Status:
Investigational
Source:
NCT02251197: Phase 2 Interventional Completed Stroke
(2001)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Clobenetine is benzomorphan derivative developed by Boehringer-Ingelheim. Clobenetine acts as a sodium channel blocker and displaces radioligand from neurotoxin receptor site 2 of the Na(+) channel in rat brain synaptosomes with IC50 of 49 nM. The IC50 value for the inactivated Na(+) channels was much lower than for Na(+) channels in the resting state. In animal models, clobenetine reduced lesion size in mice and rats when administered 5 min after permanent focal cerebral ischemia at doses that did not impair motor coordination. Clobenetine produced significant analgesic and anti-hyperalgesic effects in the rat model of arthritis, induced by complete Freund's adjuvant. In the early 2000s, the compound was investigated in phase II clinical trial for the treatment of thromboembolic stroke, but no results were reported.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Clocinizine is an antihistamine derivative of diphenylmethylpiperazine. Clocinizine is a competitive and reversible H1 receptor antagonist. The drug is marketed in Spain under tradename Senioral in combination with phenylpropanolamine for temporary relief of nasal congestion in colds, rhinitis, and sinusitis.
Status:
Investigational
Source:
NCT01362400: Phase 2 Interventional Completed Non Small Cell Lung Cancer
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Retaspimycin (IPI-504) was previously under development by manufacturer Infinity Pharmaceuticals in conjunction with MedImmune, a part of AstraZeneca. Retaspimycin is a small-molecule inhibitor of heat shock protein 90 (HSP90) with antiproliferative and antineoplastic activities. Retaspimycin binds to and inhibits the cytosolic chaperone functions of HSP90, which maintains the stability and functional shape of many oncogenic signaling proteins and may be overexpressed or overactive in tumor cells. Retaspimycin-mediated inhibition of HSP90 promotes the proteasomal degradation of oncogenic signaling proteins in susceptible tumor cell populations, which may result in the induction of apoptosis. Orphan drug designation was assigned to the compound by the FDA for the treatment of gastrointestinal stromal cancer (GIST). Infinity Pharmaceuticals has discontinued the development of retaspimycin (IPI-504) an inhibitor of the HSP-90) complex, for the treatment of cancer due to lack of efficacy in 1913.
Status:
Investigational
Source:
NCT00327002: Phase 2 Interventional Completed Metabolic Syndrome X
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
LY-518674 is a highly potent and selective proliferator-activated receptor (PPAR)-alpha agonist. LY-518674 produced a much greater increase in serum high-density lipoprotein-cholesterol (HDL-c) than the known fibrate drugs. The increase in HDL-c was associated with de novo synthesis of apolipoprotein A-1. It was being developed for the treatment of dyslipidemias with atherogenic potential.
Status:
Investigational
Source:
NCT00555919: Phase 2 Interventional Completed Metastatic Breast Cancer
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Lonaprisan is an orally bioavailable pentafluoroethyl derivative of a mifepristone-related steroid with antiprogestagenic activity. Lonaprisan is a pure, highly receptor-selective progesterone receptor (PR) antagonist (both PR isoforms PR-A and PR-B); binding of this agent to PRs inhibits PR activation and the associated proliferative effects. Lonaprisan showed limited efficacy as second-line endocrine therapy in postmenopausal women with PR-positive metastatic breast cancer. Lonaprisan had been in phase II clinical trials by Bayer for the treatment of breast cancer and dysmenorrhea. However, this research has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Napamezole [WIN 51181] is a potent alpha-2 adrenergic receptor antagonist and a selective inhibitor of 5-hydroxytryptamine re-uptake in vitro. Napamezole was at the phase I stage of development with Sanofi Winthrop (formerly known as Sterling Drug before it was purchased by Sanofi) in the USA as a treatment for depression. The alpha adrenergic antagonist activity of napamezole was determined in vitro in rat brain receptor binding assay using [3H]clonidine and [3H]prazosin for alpha-2 and alpha-1 receptors, respectively. The Ki values for napamezole were 28 nM (alpha-2) and 93 nM (alpha-1).
