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Restrict the search for
icosapent ethyl
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Conditions:
There is no much available information related to the biological and pharmacological application of imidoline, but this compound has been found to be as potent as chlorpromazine in increasing striatal DOPA accumulation and prolactin secretion in vivo. Imidoline exhibited only weak inhibitory activity towards dopamine-sensitive adenylate cyclase and 3H-spiroperidol binding to striatal membranes in vitro. A proposed active conformation involves intramolecular hydrogen bonding between the protonated dimethylamino group and the oxygen of the imidazolidinone ring. The spatial relationship between the amine nitrogen and phenyl ring in this conformation allows proper fit of imidoline with key dimensions described for the dopamine receptor.
Status:
Class (Stereo):
CHEMICAL (ACHIRAL)
Carcainium is phenylcarbamoylmethyl derivative with local anesthetic and potent anti-tussive activity. In preclinical studies Carcainium significantly reduced the spontaneous and histamine-evoked discharges in Aδ-fibres originating from airway, rapidly adapting stretch receptors (RARs) without affecting histamine-evoked bronchoconstriction. Acute pre-treatment of guinea-pigs with aerosols of Carcainium prevent of capsaicin-evoked and citric acid-induced coughs.
Status:
Investigational
Source:
INN:benzindopyrine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Benzindopyrine belongs to anticholinergic agents. It was studied as an antipsychotic drug.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Fedotozine [(1R)-1-phenyl-1-[(3,4,5-trimethoxy) benzyloxymethyl]-N,N- dimethyl-n-propylamine, (2S,3S-tartrate], derived from the arylacetamide series, is an opioid drug which acts as a selective agonist for kappa(1a)-opioid receptor. Pharmacological studies have shown that fedotozine exerts a peripheral antinociceptive action, comparable with that of other kappa-agonists. Results of Phase III trials of fedotozine against irritable bowel syndrome and dyspepsia have ultimately been disappointing and was lack of efficacy in subsequent studies.
Class (Stereo):
CHEMICAL (RACEMIC)
Merafloxacin (CI 934) is a quinolone antibacterial. It is an inhibitor of Type II DNA topoisomerase. It demonstrated excellent activity against gram-positive organisms, including Corynebacterium sp. In addition, although the activity of merafloxacin against gram-negative bacilli was less than that reported for similar agents, it was comparable to that of aminoglycosidic aminocyclitol antibiotics. Merafloxacin development has been discontinued.
Status:
Investigational
Source:
NCT00296257: Phase 2 Interventional Terminated Rheumatoid Arthritis (RA)
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Rimacalib (SMP 114) is a prostaglandin E2 antagonist that has been evaluated for use in rheumatoid arthritis. This orally bioavailable compound is a CaMKII inhibitor developed for human use. A phase II clinical trial to compare the effects of rimacalib to placebo in patients with rheumatoid arthritis has been terminated in 2009. Rimacalib also reduces SR Ca2+ leak and was therefore suggested as a candidate drug to treat proarrhythmogenic events in human atrial cardiomyocytes and cardiomyocytes from patients with heart failure.
Status:
Investigational
Source:
NCT00780663: Phase 2 Interventional Completed Neuroendocrine Tumors
(2008)
Source URL:
Class (Stereo):
CHEMICAL (EPIMERIC)
Quarfloxin (also known as CX-3543) is a fluoroquinolone derivative patented by Cyclene Pharmaceuticals, Inc. as an antitumor agent. Quarfloxin selectively disrupts nucleolin/rDNA G-quadruplex complexes in the nucleolus, thereby inhibiting DNA polymerase I transcription and inducing apoptosis in cancer cells. CX-3543 was evaluated in phase II clinical studies for the treatment of low or intermediate grade neuroendocrine carcinoma, including carcinoid and islet cell cancer. In 2008, a trial for the treatment of chronic lymphocytic leukemia (CLL) was withdrawn prior to patient enrollment. In 2010, phase I clinical studies for the treatment of solid tumors and for the treatment of lymphoma were terminated upon the observation that the modified dose schedule presented no advantage over previously studies schedule solid tumors/ Cylene discontinued development of quarfloxin in 2010.
Status:
Investigational
Source:
NCT00495885: Phase 3 Interventional Completed Sleep Initiation and Maintenance Disorders
(2007)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Volinanserin (MDL-100,907) is a highly selective 5-HT2A receptor antagonist. It is widely used in
scientific research to investigate the function of the 5-HT2A receptor. Volinanserin is also being trialed as a
potential antipsychotic, antidepressant and treatment for insomnia. Volinanserin (M-100907) was in
phase III trials for chronic schizophrenia. In August 1999, development was discontinued for acute
schizophrenia (schizoaffective disorder) on the basis of poor results. M-100907 is also active in animal
models involving blockade of NMDA glutamatergic channel receptors, an effect known to resemble some
behavioral symptoms of schizophrenia in man. M-100907 is also claimed in other patents for the
treatment of thromboembolic disorders, for the treatment of various developmental neurological
disorders such as autism and attention deficit hyperactivity disorder.
Status:
Investigational
Source:
NCT02276027: Phase 2 Interventional Completed Adenocarcinoma Lung Cancer; Squamous Cell Lung Carcinoma
(2015)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT00676910: Phase 1 Interventional Completed Neoplasms
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
JNJ-26854165 (Serdemetan), a novel tryptamine derivative, was developed as an activator of p53, and its initially proposed mechanism of action involved preventing the association of HDM2 with the proteasome and thereby stabilizing HDM2 substrates such as p53. Consistent with this proposed mechanism, Serdemetan induced apoptosis in acute myeloid and lymphoid leukemia cell lines and in primary acute leukemia isolates. Serdemetan is currently being evaluated in Phase I clinical trials in patients with non-small cell lung cancer; prostate cancer; solid tumours.
