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Restrict the search for
dimethyl fumarate
to a specific field?
Status:
Investigational
Class (Stereo):
CHEMICAL (ACHIRAL)
Indimilast is dioxodihydropyridopyrimidine derivative patented by global pharmaceutical company AstraZeneca as phosphodiesterase IV inhibitor. Indimilast modulates lung inflammation and causes bronchodilation by increasing intracellular cyclic adenosine 3', 5'-monophosphate in airway smooth muscle and inflammatory cells. Indimilast is potentially useful in chronic obstructive pulmonary disease but its activity was never evaluated in clinical trials.
Status:
Investigational
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
HU-308 ([(1R,2R,5R)-2-[2,6-dimethoxy-4-(2-methyloctan-2-yl)phenyl]-7,7-dimethyl-4-bicyclo[3.1.1]hept-3-enyl]methanol) is a potent, selective agonist for the CB2 receptor. The synthesis and characterization took place in the laboratory of Prof. Mechoulam at the Hebrew University of Jerusalem in the late 1990s. It has analgesic effects, promotes proliferation of neural stem cells,[3] and protects both liver and blood vessel tissues against oxidative stress via inhibition of TNF-α. In vivo, HU-308 has hypotensive, analgesic, and anti-inflammatory activities in mice that can be reversed by the CB2 receptor antagonist SR 144528 but not the CB1 receptor antagonist rimonabant. Pretreatment of mice with HU-308 decreases the I/R-induced tissue damage, inflammatory cell infiltration, tissue, and serum TNF-α, MIP-1, and MIP-2 levels, tissue lipid peroxidation, and apoptosis. HU-308 increases proliferation of HT29 colon cancer cells and growth of tumors in an HT29 mouse xenograft model. The physiological and toxicological properties of this compound have not been evaluated in humans.
Class (Stereo):
CHEMICAL (RACEMIC)
IPRAVACAINE is a long-acting local anesthetic which anesthetic potency is similar to that of bupivacaine. It blocks the open state of human cardiac K+ channels.
Status:
Investigational
Source:
NCT01270438: Phase 2 Interventional Withdrawn Adenocarcinoma of the Colon
(2010)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Targets:
Conditions:
RO4929097 (R-4733) is a small-molecule inhibitor of gamma-secretase (γ-secretase) with high oral bioavailability leading to the blockade of Notch signaling in tumor cells. This compound was co-developed by Roche and National Cancer Institute (NCI). RO4929097 had been in phase II clinical trials for the treatment of melanoma, colorectal cancer, and pancreatic cancer. However, these researches has been discontinued. Combination of RO4929097 and bevacizumab was well tolerated in phase I of clinical trial and can be considered in patients with recurrent malignant glioma.
Class (Stereo):
CHEMICAL (ACHIRAL)
Mipitroban (previously known as UP 11677), a thromboxane A2 receptor antagonist that was investigated to treat thrombosis. However, further studies were apparently discontinued.
Class (Stereo):
CHEMICAL (ACHIRAL)
Foropafant is a platelet-activating factor (PAF) antagonist which was developed by Sanofi. It was in clinical development for the treatment of asthma, thrombosis and ulcerative colitis. The development of the drug was discontinued due to lack of efficacy.
Class (Stereo):
CHEMICAL (ACHIRAL)
FENPRINAST is a cromotyn-like bronchodilator used for the treatment of allergy and exercise-induced asthma.
Class (Stereo):
CHEMICAL (ABSOLUTE)
Levosemotiadil is an S-enantiomer of semotiadil. It is an antiarrhythmic drug with sodium and calcium channel blocking action, as well as potassium blocking activity. Levosemotiadil is bound strongly and enantioselectively to human serum albumin and human alpha1-acid glycoprotein. Since levosemotiadil is hydrophobic basic drug, it is likely that this drug is also bound to lipoprotein in human plasma. Levosemotiadil might be effective in prevention of lethal arrhythmias. It was shown, that levosemotiadil prevented ventricular fibrillation in 64% of the high-risk animals. Heart rate responses to myocardial ischemia and to graded doses of isoproterenol were blunted by the high dose of levosemotiadil. Levosemotiadil had been in phase II clinical trials by Santen Pharmaceutical for the treatment of arrhythmias. However, this study was discontinued.
Status:
Investigational
Source:
NCT00987337: Phase 2 Interventional Completed Hepatitis
(2009)
Source URL:
Class (Stereo):
CHEMICAL (ABSOLUTE)
Conditions:
Filibuvir (PF-868554), being developed by Pfizer, is an orally administered, non-nucleoside inhibitor of the HCV NS5B RNA-dependent RNA polymerase for the potential treatment of chronic hepatitis C (HCV) infection. Filibuvir is a potent and specific inhibitor of the virally encoded NS5B polymerase, and inhibited genotype 1 sub genomic HCV replication in the cell-based replicon system. In phase I and a IIa clinical trial in treatment-naïve patients infected with genotype 1 HCV, filibuvir monotherapy or in combination with pegylated IFNα2a/ribavirin (the standard of care [SoC] for HCV infection) for up to 4 weeks significantly reduced HCV RNA levels compared with placebo or SoC alone. However, company stopped development of the drug and the decision to halt development of the non-nucleoside polymerase inhibitor, which was in mid-stage testing, was not related to any safety issues.
Class (Stereo):
CHEMICAL (RACEMIC)
Pretiadil is a thiadiazepine dioxide derivative patented by American pharmaceutical company Bristol-Myers Co. as a coronary vasodilating compound.
