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Restrict the search for
phenyl aminosalicylate
to a specific field?
Status:
Investigational
Source:
NCT01294202: Phase 2 Interventional Completed Gastrointestinal Stromal Tumor (GIST)
(2011)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Onalespib (AT13387; (2,4-dihydroxy-5-isopropyl-phenyl)-[5-(4-methyl-piperazin-1-ylmethyl)-1,3-dihydro-isoindol-2-yl] methanone, l-lactic acid salt), is wholly owned by Astex, a novel, high-affinity HSP90 inhibitor, which is currently being clinically tested, has shown activity against a wide array of tumor cell lines, including lung cancer cell lines. As a targeted inhibitor of Hsp90, onalespib has the potential to control the proliferation of multiple solid tumors and hematological malignancies where uncontrolled cell growth is dependent on the interaction between Hsp90 and its client proteins. Astex is pursuing an approach based on the observation that addition of onalespib to a molecularly targeted agent may delay the emergence of resistance to the agent, and hence prolong the window of therapeutic benefit. Onalespib is currently being evaluated via a CRADA with the National Cancer Institute (NCI) in various tumor types, and in a Phase 1/2 clinical study in combination with AT7519, Astex CDK inhibitor.
Status:
Investigational
Source:
NCT00741910: Phase 2 Interventional Completed Crohn's Disease
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Conditions:
Semapimod (CNI-1493) is a cytokine inhibitor and synthetic guanylhydrazone mitogen-activated protein kinase blocker, is being developed by Cytokine PharmaSciences as a potential treatment for Crohn's disease and other inflammatory conditions. As of December 2001, a phase I study demonstrating the safety of the compound had been completed and phase II trials for psoriasis and Crohn's disease were ongoing. In April 2003, preclinical and early clinical studies were underway for a variety of indications, including congestive heart failure and pancreatitis. Semapimod inhibits activation of p38 MAPK and NF-κB and induction of cyclooxygenase-2 by TLR ligands, but not by IL-1β or stresses. Semapimod inhibits TLR4 signaling (IC50 ≈0.3 umol) and acts by desensitizing cells to LPS; it fails to block responses to LPS concentrations of ≥5 ug/ml. Semapimod had been in phase II clinical trials by Ferring Pharmaceuticals for the treatment of Crohn's disease. However, this research has been discontinued. Semapimod is in phase I clinical trials for the treatment of autoimmune disorders and inflammation.
Class (Stereo):
CHEMICAL (ACHIRAL)
Senazodan (previously known as MCI 154), a positive inotropic agent that inhibits phosphodiesterase III and possesses a vasodilating property. Senazodan was studied in the phase II clinical trial in Japan in patients with acute heart failure. However, this study was discontinued.
Status:
Investigational
Source:
NCT03070132: Phase 3 Interventional Withdrawn Trigeminal Neuralgia
(2023)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Raxatrigine also known as GSK1014802 and CNV-1014802, is a novel analgesic under development by Convergence Pharmaceuticals for the treatment of lumbosacral radiculopathy (sciatica) and trigeminal neuralgia (TGN). It is a novel state dependent small molecule sodium channel blocker that preferentially inhibits the Nav 1.7 ion channel, a therapeutic target implicated by genetics in human pain conditions. Raxatrigine is thought to penetrate the central nervous system and block Nav channels in a novel manner. CNV1014802 was granted orphan drug designation in 2013 by the US Food and Drug Administration (FDA) for the treatment of trigeminal neuralgia.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Thiazesim (also known as ) is a benzothiazepine derivative patented by Olin Mathieson Chemical Corp. as an oral anti-depressant and tranquilizer useful in the treatment of Parkinsonism. Thiazesim is chemically related to the tranquilizing drugs chlordiazepoxide and diazepam but possesses a unique action on the limbic system, namely a selective depression of the lateral amygdaloid nucleus in experimental animals. Thiazesim shows potent anti-depressant activity in clinical trials.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Pobilukast is the Leukotriene D4 receptor antagonist. Pobilukast significantly attenuated the Salmonella enteritidis endotoxin-induced thrombocytopenia but had no effect on either the endotoxin-induced early leukopenia or late leukocytosis. Additionally, Pobilukast significantly reduced the endotoxin-induced hemoconcentration and improved survival to 30% at 48 hr. Pobilukast dose-dependently inhibited the immediate hemodynamic changes after leukotriene D4 (LTD4) injections. Pobilukast also attenuated the increase in vascular permeability and the prolonged decrease in CO, suggesting that the observed cardiac and vascular effects of LTs were mediated by stimulation of LT receptors. A shift toward the right of the dose-response curves to histamine with pobilukast compared to that with placebo in three subjects was demonstrated, whereas the active compound did not exhibit any protective effect against histamine in the remaining nine subjects. It was concluded that there is a leukotriene component to the bronchial responses to histamine in some, but not all, subjects. Pobilukast had been in phase II clinical trial for the treatment of asthma. However, this development was discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Oxamisole (previously known as PR 879-317A), a selective immunomodulatory agent that was studied for the treatment of viral infections. Experiments on mice have shown that antiviral properties of oxamisole were mediated through the immunomodulatory effects of this compound on the immune system. However, further development of this drug was discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Tioperidone is tranquilizer. This antidepressant agent reverses P-glycoprotein-mediated multidrug resistance.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Tubulozole is a stereospecific microtubule inhibitor. Structurally it is related to the benzimidazole carbamates by its carbamate moiety, which is essential for the activity of both types of compounds. The compound exists as a cis-isomer called tubulozole-C (R 46 846) and as a trans-isomer called tubulozole-T. The cis-isomer appears to be a potent and specific microtubule inhibitor, the trans-isomer being inactive at 100 times higher concentrations. At low concentrations, both isomers of tubulozole (C, T) inhibit Plasmodium falciparum but only tubulozole C inhibits mammalian cells. Since tubulozole C prevents polymerization of mammalian tubulin whereas tubulozole T does not, the antimalarial action of tubulozoles may not involve microtubules. Tubulozole-C, a new synthetic anticancer drug, interfered with the structure and function of microtubules in both interphase and mitotic cells. The activity of Tubulozole-C in experimental tumor systems can be explained partly by a direct antimitotic effect and partly by the disintegration of the normal subcellular organization of the nondividing cells. At concentrations which affect the microtubule system, tubulozole-C arrested directional migration of transformed cells and malignant invasion in a three-dimensional organ culture system. Investigations in vivo show that malignant L1210 leukemia cells are more susceptible to the antimicrotubular effect of tubulozole-C than are the normal leukocytes of the host. The trans-isomer of tubulozole (tubulozole-T, R 48 265), which has no antitumor activity in vivo, did not affect the microtubule system of cells in vitro or their capacity for directional migration or for malignant invasion.
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Clodazon (AW 142446) is an antidepressant drug investigated in Germany in the 1960s. In animal models, clodazon inhibits the catalepsy induced by tetrabenazine and it potentiates the effect of catecholamines, both effects being of the order experienced with imipramine. In clinical trials, about 2/3 of the patients showed a positive antidepressive effect with few side effects.
