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Restrict the search for
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Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Investigational
Source:
INN:dimethylthiambutene [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Dimethylthiambutene is the synthetic narcotic analgesic agent. It has analgesic effect similar to those of meperidine. The (+)-enantiomer of dimethylthiambutene is more active than the (-)-isomer. Dimethylthiambutene clinically compared with meperidine (pethidine), but maintains the dependence-producing capability of morphine. It has had illicit use in Japan in the past. Dimethylthiambutene is under international control according to the UN Single Convention 1961 and its amendments, Schedule I.
Status:
Investigational
Source:
NCT00244322: Phase 2 Interventional Completed Alzheimer's Disease
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Semagacestat (LY-450139) was a gamma secretase inhibitor being developed as a treatment for Alzheimer's disease by Eli Lilly. It was hoped that the drug would help to delay the onset of severe Alzheimer's disease, and thereby help preserve cognitive and executive functioning and in turn improve patient quality of life. Semagacestat (LY-450139) is designed to inhibit gamma secretase, an enzyme that is involved in the cleavage of APP to beta-amyloid. By decreasing production of beta-amyloid, it is hoped that gamma secretase inhibitors will exert a disease-modifying effect in Alzheimer's disease and thus slow or halt the destruction of nerve cells – the final stage in the amyloid cascade hypothesis. In March 2008 semagacestat (LY-450139) advanced to Phase III development, where it was evaluated in the IDENTITY (Interrupting Alzheimer's Dementia by EvaluatiNg Treatment of AmyloId PaThologY) trial, the first Phase III trial for this new anti-dementia drug. In August 2010, Eli Lilly announced its decision to halt the development of Semagacestat. The decision was taken after analysing the preliminary results of the second Phase III clinical trial of the drug, which indicated that semagacestat failed to slow disease progression. The drug, in fact, worsened cognition and the ability to perform day-to-day activities.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Cicaprost is a prostacyclin receptor (IP) agonist and orally active prostacyclin analog with potent systemic and pulmonary vasodilatation and anti-inflammatory activity. In preclinical models, Cicaprost treatment largely prevented the hypercholesterolemia-related impairment of coronary vasodilation and nitric oxide release in Isolated Langendorff-hearts. Cicaprost inhibits proinflammatory chemokines production not only from lipopolysaccharides (LPS) or (tumor necrosis factor-alpha) induced primary human monocyte-derived macrophages but also from LPS-stimulated monocyte-derived dendritic cells. Besides that Cicapost strongly inhibits lymph node and organ metastases of spontaneously metastasizing mammary tumors with a mode of action different from cytostatic or antihormonal drugs. In animal models, Cicaprost prevents metastasis if given continuously from the day of tumor implantation, and is effective in reducing metastasis if treatment is begun following surgical removal of the primary tumor when micrometastases are already present. Clinical trials of Cicaprost in healthy male volunteers demonstrate significant anti-platelet and vasodilatory effects.
Status:
Investigational
Source:
INN:clociguanil [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Clociguanil (BRL 50216, WR 38839) is an antimalarial compound, a derivative of N-benzyloxydihydrotriazine, developed by Beecham Pharmaceuticals. Mode of action studies indicated that clociguanil is a dihydrofolate reductase inhibitor of Plasmodium and is capable of marked potentiation with a selected sulphonamide against both the sensitive N strain and the cycloguanil-resistant B line of P. berghei. A combination of clociguanil and sulphadiazine prevented the development of parasitemia caused by P. falciparum in humans. The subsequent development of clociguanil was discontinued because of a relatively short half-life in man and lack of suppression of pre-erythrocytic schizogony of a strain of P. falciparum resistant to chloroquine, pyrimethamine, and proguanil.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Motapizone is a pyridazinone derivative patented by pharmaceutical company Nattermann, A., und Cie. G.m.b.H. as an antithrombotic and hypotensive agent. Motapizone ats as a potent inhibitor of the isoenzyme phophodiesterase type III. In preclinical studies potent antithrombotic and hypotensive properties of motapizone has been shown in rats, cats, and dogs. In normal human volunteers, single oral doses of motapizone up to 10 mg produced significant inhibition of platelet aggregation measured by the ex vivo method. These effects were dependent upon the dose of motapizone and associated with an increase in heart rate and a reduction in diastolic blood pressure.
Status:
Investigational
Source:
NCT00285025: Phase 2 Interventional Completed Alzheimer Disease
(2005)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Paliroden is an orally active drug that activates the synthesis of endogenous neurotrophins or nerve growth factors. Paliroden was investigated in phase II clinical trial in patients with Alzheimer's disease and to evaluate its effect on 18F-Dopa PET imaging in patients with Parkinson's disease. The further development of paliroden was discontinued due to its insufficient efficacy.
Status:
Investigational
Source:
NCT01320553: Phase 2 Interventional Completed Allergic Conjunctivitis
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00483704: Phase 3 Interventional Completed Migraines
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Telcagepant (MK-0974) is a calcitonin gene-related peptide receptor antagonist. Merck & Co was developing telcagepant for the treatment of pain. Telcagepant is an extremely potent CGRP antagonist with a Ki = 0.77 (0.07 nM). Telcagepant showed efficacy against acute migraines; however, different patient populations may show more beneficial effects with telcagepant versus triptans. In the acute treatment of migraine, Telcagepant was found to have equal potency to rizatriptan and zolmitriptan in two Phase III clinical trials. Merck & Co has now terminated development of the drug.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Cimaterol is a chemically stable nonselective agonist β1-, β2-, and β3-adrenoceptors. Cimaterol is used in sport as a stimulant and a fat burner that assists bodybuilders and strength athletes to get rid of body fats. Aside from shedding off fats, another benefit for using cimaterol for athletes is a boost in strength as well as an increase in muscle size or lean body mass. The increase in muscle size has been seen in previous animal studies when cimaterol is used. However, the reason behind the muscle gain is not identified yet, but the body has a very different response compared from taking in anabolic steroids. Experts in the field are saying that the increased nitrogen retention, that is known to cause by cimaterol, maybe the reason behind the muscle gain. Another great thing about Cimaterol is that, it can improve blood flow.
