U.S. Department of Health & Human Services Divider Arrow National Institutes of Health Divider Arrow NCATS

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Showing 9421 - 9430 of 10822 results

Status:
Investigational
Source:
INN:diproqualone [INN]
Source URL:

Class (Stereo):
CHEMICAL (EPIMERIC)

Diproqualone was used primarily for the treatment of inflammatory pain associated with osteoarthritis. The analgesic activity of diproqualoneis synergistic with that of noramidopyrine. It also display anti-inflammatory action in the rat, inhibiting plantar edema with dextran or serotonin, atopic edema from ovalbumin, etc. It has spasmolytic, anticholinergic and antihistaminic action in higher doses. It is not hypnotic and has no anticonvulsant effects. The therapeutic symptoms for diproqualone are all types of pain: postoperative, posttraumatic, dental, neuritis, anti-inflammatory arthritis, etc.
Status:
Investigational
Source:
Avian Pathol. Feb 2008;37(1):45-50.: Not Applicable Veterinary clinical trial Completed Protozoan Infections, Animal/parasitology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dimetridazole is an anti-fungal and anti-protozoal drug traditionally used in veterinary for the prevention and treatment of histomoniasis in turkeys, genital trichomoniasis in cattle and hemorrhagic enteritis in pigs. Results from the in vitro and in vivo tests suggested, that dimetridazole was not genotoxic compound, but its use is legally limited, although this compound is still can be found in eggs.
Status:
Investigational
Source:
INN:pentopril
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Pentopril (CGS 13945) is a member of a series of l-glutarylindoline-2(S)-carboxylic acid derivatives. Pentopril was evaluated as an inhibitor of a cell-free preparation of angiotensin-converting enzyme (ACE) isolated from rabbit lung. Intravenous administration of incremental doses of pentopril to anesthetized normotensive rats produced a dose-related inhibition of angiotensin I (AI) pressor responses. The onset of inhibition of the A1 pressor response was rapid, and substantial inhibition occurred at 5 min after administration of the ACE inhibitors. Pentopril hydrolyzed in vivo to the biologically active free-acid form of CGS 13934. It was well tolerated in normal volunteers and hypertensive patients. Pentopril was developed for the treatment of both hypertension and congestive heart failure. Pentopril produced little clinical improvement and no biochemical improvement in a patients with rheumatoid arthritis.
Status:
Investigational
Source:
NCT01984294: Phase 2 Interventional Completed Chronic HCV Infection
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Radalbuvir (also known as GS-9669 ) is a Hepatitis C virus NS 5 protein inhibitor for the treatment of hepatitis C virus (HCV) infection developed by Gilead Sciences. Radalbuvir is a highly optimized thumb site II nonnucleoside inhibitor, with a binding affinity of 1.35 nM for the genotype (GT) 1b protein. It is a selective inhibitor of HCV RNA replication, with a mean 50% effective concentration of ≤ 11 nM in genotype 1 and 5 replicon assays, but lacks useful activity against genotypes 2 to 4. In preclinical Radalbuvir exhibited at least additive activity in combination with agents encompassing four other direct modes of action (NS3 protease, NS5A, NS5B via an alternative allosteric binding site, and NS5B nucleotide) as well as with alpha interferon or ribavirin in replicon assays. It exhibited high metabolic stability in vitro human liver microsomal assays, which, in combination with its pharmacokinetic profiles in rat, dog, and two monkey species, is predictive of good human pharmacokinetics. In clinical trials, Radalbuvir shows highly effective inhibition of wild-type HCV.
Status:
Investigational
Source:
NCT00195325: Phase 1 Interventional Terminated Tumors
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Targets:


Cevipabulin is a synthetic, water-soluble tubulin-binding agent with potential antineoplastic activity. Cevipabulin appears to bind at the vinca-binding site on tubulin but seems to act more similar to taxane-site binding agents in that it enhances tubulin polymerization and does not induce tubulin depolymerization. The disruption in microtubule dynamics may eventually inhibit cell division and reduce cellular growth.
Status:
Investigational
Source:
INN:temiverine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
Status:
Investigational
Source:
INN:temiverine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
Status:
Investigational
Source:
Avian Pathol. Feb 2008;37(1):45-50.: Not Applicable Veterinary clinical trial Completed Protozoan Infections, Animal/parasitology
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Dimetridazole is an anti-fungal and anti-protozoal drug traditionally used in veterinary for the prevention and treatment of histomoniasis in turkeys, genital trichomoniasis in cattle and hemorrhagic enteritis in pigs. Results from the in vitro and in vivo tests suggested, that dimetridazole was not genotoxic compound, but its use is legally limited, although this compound is still can be found in eggs.
Status:
Investigational
Source:
INN:temiverine
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Temiverine was developed as an antimuscarinic and calcium-antagonist agent for the treatment of overactive bladder. Temiverine participated in clinical trials; however, the development of the drug was discontinued on the pre-registration stage.
Status:
Investigational
Source:
NCT01730768: Phase 2 Interventional Completed Schizophrenia
(2012)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Showing 9421 - 9430 of 10822 results