U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 821 - 830 of 24423 results

Status:
Investigational
Source:
INN:diethylthiambutene [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Diethylthiambutene is an analgesic agent with an effect like that of morphine. Diethylthiambutene mainly used in veterinary. It is highly toxic to cats. Can cause convulsions if injected intravenously. Diethylthiambutene is a synthetic opioid drug. It is under international control according to the UN Single Convention 1961 and its amendments, schedule I.
Status:
Investigational
Source:
INN:ruzadolane
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Ruzadolane (previously known as UP 26-91) is a serotonin receptor antagonist that was developed as a non-narcotic, centrally acting analgesic agent for the treatment of anxiety disorder and pain. However, these studies were discontinued.
Status:
Investigational
Source:
NCT00631657: Phase 3 Interventional Completed Sleep Initiation and Maintenance Disorders
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Esmirtazapine (S-(+)mirtazapine or ORG-50081) is an enantiomer of mirtazapine (REMERON®), a high-affinity antagonist at 5-HT2/5-HT3 and H1 receptors, used in the treatment of depression. Esmirtazapine has a shorter plasma half-life than the R(−) enantiomer. Esmirtazapine is preferentially metabolized into an 8-hydroxy glucuronide. Organon was developing esmirtazapine for the treatment of hot flushes (vasomotor symptoms) associated with the menopause and insomnia.
Status:
Investigational
Source:
NCT00596258: Phase 2 Interventional Completed Cervical Intraepithelial Neoplasia
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Sivifene (also known as A-007), a triaryl hydrazone that produced objective responses when applied topically. During preclinical studies, sivifene was observed to upregulate both cutaneous and systemic T-lymphocytes, in particular, CD4/8+ lymphocyte subtypes. The current mechanism of action for the drug is unknown however is assumed that it can show its immunomodulating properties through the upregulation of the CD45 T lymphocyte cell surface receptor. Sivifene was being evaluated for its anticancer activities in melanoma, breast cancer, Kaposi's sarcoma, and lymphoproliferative disorders. The drug as a 0.25% gel is confirmed as an effective palliative treatment option for cutaneous metastases from cancers. Skin reactions were minimal, tolerated, and no cessation of treatment was required. However, the further development of this drug apparently has been discontinued.
Status:
Investigational
Source:
NCT00794430: Phase 2 Interventional Completed Diabetic Peripheral Neuropathic Pain
(2008)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Indantadol (previously known as CHF-3381) is an oral and noncompetitive N-methyl-D-aspartate (NMDA) receptor antagonist and reversible monoamine oxidase-A (MAO-A) inhibitor that is being developed by Vernalis plc, under license from Chiesi Farmaceutici SpA, for the potential treatment of neuropathic pain. In preclinical studies, indantadol exhibited neuroprotective effects after kainate-induced seizures and displayed anticonvulsant and antihyperalgesic activity. Indantadol also caused a dose-dependent decrease in exploratory motility. In a human heat-capsaicin-induced pain model, indantadol at a dose of 500 mg effectively reduced the area of secondary hyperalgesia. The tolerability profile of the drug at single doses up to 600 mg and twice-daily doses up to 400 mg in clinical trials was significantly more favorable than for other NMDA antagonists. Most side effects have been observed to be mild, and include dizziness and asthenia. Indantadol was in phase II clinical trials for the treatment of chronic cough and neuropathic pain. However, these studies had been discontinued.
Status:
Investigational
Source:
INN:parogrelil [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



NT-702 (parogrelil hydrochloride) is a novel phosphodiesterase 3 (PDE) inhibitor, and being developed for the treatment of intermittent claudication (IC) in patients with peripheral arterial disease. In Japan, Phase 2 studies are being conducted for intermittent claudication caused by arteriosclerosis obliterans, intermittent claudication caused by spinal canal stenosis, and asthma. In the USA, a Phase 2 study for intermittent claudication caused by arteriosclerosis obliterans has been successfully completed. Also was shown, that NT-702 has an anti-inflammatory effect as well as a bronchodilating effect and might be useful as a novel potent therapeutic agent with both a bronchodilating and an anti-inflammatory effect.
Status:
Investigational
Source:
NCT00481325: Phase 2/Phase 3 Interventional Completed Generalized Anxiety Disorder
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pexacerfont is a highly potent and selective CRF1 receptor antagonist that displays no agonist properties. It is specific for CRF1 receptors and has more than 1,000- fold less affinity for CRF2 receptors, and more than 100- fold less affinity for the CRF-binding protein. In extensive preclinical studies, pexacerfont has been shown to inhibit specific binding of CRF to rat, dog, monkey, and human CRF1 receptors. The functional anxiolytic effects of CRF1 receptor occupancy were demonstrated in two rodent models of anxiety, situational anxiety and elevated plus maze paradigms. Pexacerfont did not demonstrate efficacy compared to placebo for the treatment of generalized anxiety disorder in human. The bogus taste tests suggested some protective effect of pexacerfont against eating after a laboratory stressor. Pexacerfont had been in phase II clinical trials for the treatment of irritable bowel syndrome and depression depression.
Status:
Investigational
Source:
NCT00924989: Phase 3 Interventional Completed Adrenocortical Carcinoma
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Linsitinib is an inhibitor of the insulin receptor and the insulin-like growth factor 1 receptor, which may result in the inhibition of tumor cell proliferation and the induction of tumor cell apoptosis. Linsitinib is in phase II clinical trials for the treatment of metastatic prostate carcinoma, gastrointestinal stromal tumors and other cancers. Common adverse events included fatigue, nausea hyperglycaemia and anorexia.
Status:
Investigational
Source:
INN:levopropicillin [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Levopropylcillin – is a penicillin derivative, L-enantiomer of antibiotic Propicillin. Levopropylcillin properties are similar to benzylpenicillin particularly used in streptococcal infections, not resistant to penicillinase. Levopropylcillin is acid resistant and can be used orally as the potassium salt.
Status:
Investigational
Source:
INN:rocbrutinib [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)