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Restrict the search for
beta carotene
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Class (Stereo):
CHEMICAL (ABSOLUTE)
Ceftiolene (42980RP) is a new cephalosporin with a broad antibacterial spectrum similar to cefotaxime or ceftriaxone. The affinities of ceftiolene for penicillin-binding proteins are very comparable with those of ceftriaxone and cefotaxime for Escherichia coli, and generally greater than those of latamoxef (moxalactam) for the higher molecular weight PBPs of E. coli. Enterobacter cloacae. The affinity of ceftiolene for PBP1 of Staphylococcus aureus is greater than those of cefotaxime or latamoxef but comparable with these antibiotics for PBP3. The bacteriolytic activity of ceftiolene at defined concentrations against Gram-negative organisms is similar to that of ceftriaxone and significantly better than that of the other third-generation cephalosporins tested.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Caprindolol, also known as SDZ 21009, is a beta-adrenoceptor blocker with affinity for serotonin (5-HT1A and 5-HT1B receptors.
Class (Stereo):
CHEMICAL (RACEMIC)
Bometolol is a cardiospecific beta-adrenergic blocking drug that was never marketed.
Status:
Investigational
Source:
NCT00304525: Phase 1/Phase 2 Interventional Completed Metastatic Melanoma
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
CHIR-265 (RAF265) is a potent selective orally active small molecule Raf-kinase inhibitor with anti‐angiogenic activity through inhibition of vascular endothelial growth factor type 2 (VEGFR‐2) in preclinical models. CHIR-265 effectively block phosphorylation of Raf's downstream substrates MEK and ERK in cells and also kill melanoma and colorectal cancer cell lines harboring B-Raf mutations independent of PTEN mutation status. Raf kinase inhibition by CHIR-265 in mutant B-Raf melanoma cell lines causes cell cycle arrest and induces apoptosis, mimicking the effect of Raf RNAi in these cells. CHIR-265 also potently inhibits the phosphorylation of VEGFR2 and proliferation of VEGF-stimulated hMVEC.
Status:
Investigational
Source:
INN:dexefaroxan [INN]
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Dexefaroxan is a selective alpha 2-adrenergic receptor antagonist. Вexefaroxan improved TgCRND8 (protein-transgenic mouse model of Alzheimer's disease) behavioral phenotypes and increased BDNF mRNA expression without affecting amyloid-β peptide levels. Dexefaroxan treatment also enhanced the number and complexity of the dendritic arborizations of polysialated neural cell adhesion molecule-positive neurons. The trophic effects of dexefaroxan on newborn cells might involve an increase in brain-derived neurotrophic factor, which was upregulated in afferent noradrenergic fiber projection areas and in neurons in the granule cell layer. By promoting the survival of new endogenously formed neurons, dexefaroxan treatment represents a potential therapeutic strategy for maintaining adult neurogenesis in neurodegenerative conditions, such as Alzheimer's disease, that affect the hippocampus. Dexefaroxan increases neuron survival in the olfactory bulb of the adult rat in vivo, putatively as a result of reducing the apoptotic fate of telencephalic stem cell progenies.
Status:
Investigational
Source:
NCT00332202: Phase 3 Interventional Completed Non Hodgkin Lymphoma
(2006)
Source URL:
Class (Stereo):
CHEMICAL (ACHIRAL)
Targets:
Enzastaurin is a serine/threonine kinase inhibitor that showed antiangiogenic, antiproliferative, and proapoptotic properties in vitro and antitumor activity in vivo in a xenograft Waldenström macroglobulinemia (WM) model. Enzastaurin (LY317615) is a potent PKCβ selective inhibitor. Enzastaurin suppresses angiogenesis and was advanced for clinical development based upon this antiangiogenic activity. Enzastaurin suppresses tumor growth through multiple mechanisms: direct suppression of tumor cell proliferation and the induction of tumor cell death coupled to the indirect effect of suppressing tumor-induced angiogenesis. Enzastaurin is an orally administered drug that was intended for the treatment of solid and haematological cancers. Enzastaurin had shown encouraging preclinical results for the prevention of angiogenesis, inhibition of proliferation and induction of apoptosis as well as showing limited cytotoxicity within phase I clinical trials. However, during its assessment in phase II and III clinical trials the efficacy of enzastaurin was poor both in combination with other drugs and as a single agent. Eli Lilly discontinued development of enzastaurin after top-line data from the double-blind, international Phase III PRELUDE trial in 758 DLBCL patients showed that enzastaurin missed the primary endpoint of improving DFS vs. placebo.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Epervudine (5-isopropyl-2'-deoxyuridine) is an antiviral compound. The antiviral effect of epervudine on herpes viruses (HSV-1 and HSV-2) is based on the sensitivity of virus DNA to nucleases due to epervudine incorporation into the virus DNA and the resulting change in DNA conformation. Virus selectivity is based on virus induced thymidine kinase activity and on HSV induction of polymerase enzymes catalyzing the incorporation. Epervudine (HEVIZOS) ointment is used to treat herpetic skin infections.
Class (Stereo):
CHEMICAL (MIXED)
Dioxadilol is benzodioxane derivative. It has beta-adrenolytic activity. Dioxadilol is antihypertensive, antianginal and antiarrhythmic agent but less potent than propranolol.
Status:
Investigational
Source:
INN:levometiomeprazine [INN]
Source URL:
Class (Stereo):
CHEMICAL (UNKNOWN)
Levometiomeprazine is antiemetic, neuroleptic agent.
Class (Stereo):
CHEMICAL (RACEMIC)
Conditions:
Moguisteine is a non-narcotic antitussive compound. Moguisteine demonstrated inhibitory effect on rapidly adapting irritant receptors that could account for the antitussigenic effect of this compound. Furthermore, it is possible that ATP-sensitive K(+) channels may be involved in the anti-tussive effect of peripherally acting non-narcotic moguisteine. The drug did not show any toxic effect on the dams and their fetuses, nor did it have any teratogenic effect in either of the tested species. Finally, moguisteine had no adverse effects, either on parturition or on peri-and postnatal survival and/or development of the offspring. It was reported that moguisteine to be effective in reducing cough frequency in chronic cough of bronchitis and COPD. It was recommended for the short-term symptomatic relief of coughing. Preregistration of moguisteine in Italy is discontinued.
