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Restrict the search for
phenyl aminosalicylate
to a specific field?
Class (Stereo):
CHEMICAL (UNKNOWN)
Targets:
Igmesine is a sigma-1 receptor agonist. It was assayed in clinical trials targeting major depressive disorder. Igmesine is the only antisecretory agent that we have tested to date that inhibits both cholera toxin and the E. coli enterotoxins. Sigma receptors are known to be present on nerves in the enteric nervous system and this would seem to be a potentially useful class of drugs to pursue for the treatment of secretory diarrhoea in humans. It was shown that when Alzheimer's disease rats were submitted to the conditioned fear stress test, igmesine can significantly reduce the stress-induced motor suppression, indicating exogenous σ-1 receptor agonists may alleviate Alzheimer's disease-associated depressive symptoms.
Class (Stereo):
CHEMICAL (ACHIRAL)
Brovanexine is a derivative of bromhexine used as an adjunct to antibacterials in preparations for the treatment of respiratory-tract infections. Oral administration of brovanexine hydrochloride (BR-222) caused a significant increase in the output volume of respiratory tract fluid. Brovanexine at 10 and 20 mg/kg showed a tendency to reduce the viscosity of respiratory tract fluid in anesthetized dogs. Brovanexine also showed a tendency to reduce the viscosity of sputum obtained from the SO2-exposed rabbits.
Status:
Investigational
Source:
NCT01905540: Phase 1 Interventional Completed Healthy
(2013)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Deferitazole is an iron chelator, developed by the FerroKin BioSciences (later acquired by Shire, and then by Takeda). Deferitazole is a member of the desazadesferrithiocin class of siderophore-related tridentate chelators. It binds Fe(III) with very high affinity and selectivity over Fe(II) and other biologically important metals. Deferitazole was investigated in phase 2 clinical trials in patients with iron overload due to repeated red blood cell transfusion and beta-thalassemia, however, the development of the drug was discontinued. In preclinical models, deferitazole demonstrated efficacy for the treatment and prevention of malaria.
Status:
Investigational
Source:
NCT00280631: Phase 1/Phase 2 Interventional Completed Myelodysplastic Syndrome (MDS)
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Ezatiostat (TLK199) [γ-glutamyl-S-(benzyl)cysteinyl-R-phenyl glycine diethyl ester] is an inhibitor of Glutathione S-transferase P1–1 (GSTπ). The drug is a peptidomimetic of GSH (glutathione), esterified to enhance cellular uptake and designed to bind to the “G-site” of GSTP1–1. Independent of catalysis inhibition, TLK199 also disrupts the protein:protein interaction site(s) between GSTP1–1 and JNK1. Telik Inc was developing TLK-199 for the potential prevention of myelosuppression in blood diseases, namely myelodysplastic syndrome.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Adaprolol is a beta-adrenergic antagonist that is being developed as a topical agent to treat glaucoma. Adaprolol demonstrated a safer cardiovascular profile, especially in the population over 70 years old. It was in Phase II clinical trials for the treatment of glaucoma. This research has been discontinued.
Status:
Investigational
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Conditions:
Talopram (Lu 3-010) is a selective inhibitor norepinephrine transporter belonging to the antidepressants of the thymoleptic group.
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.
Status:
Investigational
Source:
NCT00751231: Phase 2 Interventional Completed Percutaneous Coronary Intervention
(2008)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Elinogrel, previously known as PRT060128 or PRT128, is a direct-acting, reversible P2Y12 inhibitor for both intravenous and oral administration. Elinogrel has been tested in 2 phase II studies for the treatment of acute coronary syndrome, myocardial infarction and prevention of secondary thrombotic events. Elinogrel therapy was associated with an increased incidence of dyspnea and incidence of elevated liver transaminases. The development of the drug was terminated in January 2012 by Novartis.
Status:
Investigational
Source:
NCT00803933: Phase 2 Interventional Completed African Trypanosomiasis
(2003)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Pafuramidine or DB289, [2,5-bis-(4-amidinophenyl)furan bis-O-methylamidoxime] is a pro-drug of DB75, [2,5-bis(4-amidinophenyl)furan] also known as furamidine. The biotransformation process of DB289 to DB75 in the human liver consists of three O-demethylation reactions
catalyzed by the Cyp4F enzyme subfamily and three N-dehydroxylation reactions catalyzed by cytrochrome b5 and NADH-cytochrome b5 reductase. DB289 was studied for therapeutic treatment against human African trypanosomiasis, Pneumocystis pneumonia and malaria. In November 2006, Immtech Pharmaceuticals, Inc. announced that the U.S. Food and Drug Administration (FDA) had granted orphan drug designation for pafuramidine (DB289) to treat Pneumocystis jiroveci pneumonia (PCP), a common life-threatening opportunistic infection in HIV/AIDS and other immunosuppressed patients. Despite the high efficacy of DB289 in patients, the mechanism of action of DB75 is unknown. The mechanism of antimicrobial activity of diamidine compounds is incompletely understood. They undergo active uptake by purine transporter systems in trypanosomes and their mechanism of action may involve interference with DNA-associated enzymes inhibition of heme crystallization11 or/and collapse of the transmitochondrial membrane potential.
Class (Stereo):
CHEMICAL (RACEMIC)
Targets:
Telupidine (GR53992B), a dihydropyridine derivative is a calcium channel blocker. This is an antihypertensive and cardiovascular agent. Information about the current use of this compound is not available.
