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Restrict the search for
dimethyl fumarate
to a specific field?
Class (Stereo):
CHEMICAL (ACHIRAL)
Sulfatroxazole is a sulfamide derivative patented by Swiss multinational healthcare company F. Hoffmann-La Roche & Co., A.-G. as an antibacterial agent and bacteriostatic antibiotic. Sulfatroxazole competitively inhibits dihydropteroate synthase preventing the formation of dihydropteroic acid, a precursor of folic acid which is required for bacterial growth. Sulfatroxazole is a component present in various veterinary drugs.
Status:
Investigational
Source:
INN:dexniguldipine [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
Dexniguldipine (B8509-035, (-)-(R)-niguldipine) is a new dihydropyridine derivative, that exerts selective antiproliferative activity in a variety of tumor models and, in addition, has a high potency in overcoming multidrug resistance. Dexniguldipine is ( - )-(R)-enantiomer of niguldipine, of which the ( )-(S)-enantiomer shows pronounced cardiovascular hypotensive activity due to its high affinity for the voltage-dependent Ca2 channel. As compared with the (S)-enantiomer, the (R)-enantiomer has a 40-fold lower affinity for the Ca 2 channel and, accordingly, only minimal hypotensive activity in animal pharmacology models. Dexniguldipine have shown antiproliferative activity in several tumor cell lines, but the concentrations necessary to inhibit growth have varied by several orders of magnitude between cell lines. Initial results of preclinical investigations for the evaluation of the mechanism of its antiproliferative activity demonstrate that dexniguldipine interferes with intracellular signal transduction by affecting phosphoinositol pathways, protein kinase C expression, and intracellular Ca 2 metabolism. In a series of human tumor xenografts in vitro, dexniguldipine demonstrated selective antiproliferative activity against several tumor types, e.g., melanoma and renal-cell carcinoma. Striking results were obtained in a hamster model, in which neuroendocrine lung tumors could be completely eradicated by 20 weeks of oral treatment with 32.5mg/kg dexniguldipine, whereas Clara-cell-type lung tumors were not affected. In in vitro studies, dexniguldipine has been found to bind to P-glycoprotein (P-gp) and to enhance the cytotoxicity of chemotherapeutic agents such as doxorubicin and etoposide in several cell lines The synergistic effect may well be associated with the reversal of multidrug resistance (MDR) related to the activity of P-gp. In the clinical therapy of cancer, resistance to many cytostatic drugs is a major cause of treatment failure. However, the high potency of dexniguldipine (about 10-fold as compared with that of verapamil in vitro) and its low cardiovascular activity provide the opportunity to achieve blood or tumor concentrations that might be high enough to overcome Mdr 1 resistance in patients without producing dose-limiting cardiovascular effects.
Status:
Investigational
Source:
NCT03317587: Not Applicable Interventional Completed Obesity
(2017)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Class (Stereo):
CHEMICAL (ABSOLUTE)
Metergotamine (MY-25 or 1-methyl-ergotamine-bitartrate) is a derivative of ergotamine and belongs to peptide alkaloids. It exerts a dampening effect on vessels, in that relaxation is brought about in contracted vessels, whereas contraction is brought in dilated vessels. Metergotamine was being studied in migraine prophylaxis.
Status:
Investigational
Source:
NCT01770548: Not Applicable Interventional Completed Autism
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Status:
Investigational
Source:
NCT04649216: Phase 1 Interventional Completed Healthy Volunteers
(2020)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Chugai Pharmaceutical is developing a parathyroid 1 receptor agonist called as PCO371. It is known that parathyroid hormone (PTH) is essential for calcium homeostasis and its action is mediated by the PTH type 1 receptor. PCO371 can provide a new treatment option for PTH-related disorders, including hypoparathyroidism. This drug participated in phase I clinical trial in healthy volunteers. However, Chugai Pharmaceutical has terminated this study. No recent reports of the development of PCO371are available.
Status:
Investigational
Source:
INN:guaifylline [INN]
Source URL:
Class (Stereo):
CHEMICAL (RACEMIC)
Guaithylline (or Guaifylline), a xanthine derivative that was studied as a bronchodilator and expectorant, however, has never been marketed.
Status:
Class (Stereo):
CHEMICAL (RACEMIC)
Status:
Investigational
Source:
Vet Res Commun. Jan 2008;32(1):75-92.: Not Applicable Veterinary clinical trial Completed N/A
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
(E)-Tetrachlorovinphos is an (E)- isomer of Tetrachlorovinphos. Tetrachlorovinphos is an organophosphate cholinesterase inhibitor that is used as an insecticide. Tetrachlorvinphos was introduced and first used commercially in 1966 in the USA. Tetrachlorvinphos was originally registered for use on various food crops, livestock, pet animals. Tetrachlorvinphos is applied dermally to livestock to control flies and mites. It is used as an oral larvicide in cattle, hog, goats and horses; in cattle ear tags to control flies; in cattle feedlots; in poultry dust boxes to control poultry mites; and in poultry houses. Tetrachlorvinphos also is used in pet sleeping areas and pet flea collars and to control flies around refuse sites, recreational areas, and for general outdoor treatment. Tetrachlorvinphos can cause cholinesterase inhibition in humans; that is, it can overstimulate the nervous system causing nausea, dizziness, confusion, and at very high exposures (e.g., accidents or major spills), respiratory paralysis and death. In 2014, the Natural Resources Defense Council (NRDC) filed a lawsuit against the United States Environmental Protection Agency (EPA) seeking EPA to respond to NRDC’s 2009 petition to ban tetrachlorvinphos in common pet flea treatment products. Tetrachlorvinphos is reportedly registered for use in Canada, South Africa, and Australia.
Status:
Investigational
Source:
NCT02249403: Phase 2 Interventional Completed Alzheimer Disease
(1999)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Talsaclidine (WAL-2014) is a selective full agonist of M1 muscarinic receptor, having partial agonist activity on the M2 and M3 subtypes (with no in vivo consequences). The general receptor profile of talsaclidine demonstrates a nearly specific interaction with muscarinic receptors, having only weak binding affinity for alpha1- and nicotinic receptors. The drug is being tested in phase III of clinical trials for the treatment of Alzheimer's disease.
