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

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Showing 49971 - 49980 of 55039 results

Status:
Investigational
Source:
INN:bemarinone
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Bemarinone (ORF 16600) is a positive inotropic and vasodilator agent with potential clinical utility in the management of congestive heart failure. The compound selectively and competitively inhibited cyclic AMP phosphodiesterase fraction III. However, further studies were discontinued
Status:
Investigational
Source:
INN:naflocort
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Naflocort (SQ 26,490) is a topical anti-inflammatory adrenocortical steroid. It was a moderately potent inhibitor of edema formation in the rat. After extended topical application, SQ 26,490 totally inhibited edema formation without appreciable production of skin atrophy, measured under identical conditions. SQ 26,490 possesses the property for a greater separation of anti-inflammatory and atrophogenic activities than comparative corticoids.
Status:
Investigational
Source:
INN:sibenadet [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

AstraZeneca R&D Charnwood (formerly Astra Charnwood, a subsidiary of AstraZeneca) was developing sibenadet (Viozan, AR-C68397AA) for the potential treatment of chronic obstructive pulmonary disease and asthma. Sibenadet is a dual D2 dopamine receptor, beta2-adrenoceptor agonist that combines bronchodilator activity with the sensory afferent modulating effects associated with D2-receptor agonism. Development of sibenadet has been discontinued due to disappointing efficacy findings.
Status:
Investigational
Source:
INN:fluparoxan
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Fluparoxan (GR50360A) is a potent α2-adrenergic receptor antagonist used in the treatment of central neurodegenerative diseases, depression, the improvement of cognitive dysfunction in schizophrenia and in models of Alzheimer's disease. Fluparoxan was undergoing phase III trials as an antidepressant, but this development was also discontinued because of poor efficacy.
Status:
Investigational
Source:
NCT01285414: Phase 2 Interventional Completed Glioblastoma Multiforme
(2010)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Veribulin is a novel microtubule destabilizer that both functions as a potent cytotoxin and acts as a vascular disrupting agent (VDA). It binds to the same (or nearby) sites on β-tubulin as colchicine. It is capable of evading multidrug resistance pumps and, thus, achieves high CNS concentrations. It is efficacious in multiple xenograft models without CNS toxicity. Veribulin had previously demonstrated pre-clinical and clinical activity in multiple tumor types. Veribulin is in phase II clinical trial for the treatment of Glioblastoma and Malignant melanoma.
Status:
Investigational
Source:
INN:bunolol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Bunolol is non-selective beta-adrenoreceptor antagonist with significant antihypertensive, antiarrhythmic and local anesthetic activities. Bunolol is a racemic mixture and Levobunolol is greater than 60 times more potent than its dextro isomer in its beta-blocking activity. Bunolol is 3 times as potent as propranolol by i.v. administration in anesthetized dogs in antagonizing the cardiovascular actions of isoproterenol and the response to cardioaccelerans nerve stimulation. When oral doses were given to unanesthetized dogs with subsequent induction of anesthesia, Bunolol was 20 times as potent as propranolol. The β-adrenergic blocking activity of Bunolol appeared to be competitive, and the activity was largely restricted to the l-isomer. Bunolol is extensively metabolized by both oxidative and reductive routes.
Status:
Investigational
Source:
INN:spirazine [INN]
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Spirotriazine is a dihydrotriazine derivative patented by Burroughs Wellcome & Co. (U.S.A.) Inc. as the anthelmintic agent. In preclinical models, Spirotriazine shows potent activity against intestinal parasites and negligible microbiological activity.
Status:
Investigational
Source:
NCT00400296: Phase 1 Interventional Completed Neoplasms
(2005)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

A diaminopyrimidine compound R547 is a small molecule selective ATP-competitive inhibitor of cyclin-dependent kinases CDK1, CDK2 and CDK4 and has excellent in vitro cellular potency, inhibiting the growth of various human tumor cell lines. In vivo, R547 showed antitumor activity in all of the models tested to date, including six human tumor xenografts and an orthotopic syngeneic rat model. R547 was being developed by Roche for the treatment of solid tumours. The compound was undergoing clinical development in the US. However, no recent development has been reported and it is assumed to have been discontinued.
Status:
Investigational
Source:
INN:zinoconazole
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Zinoconazole, an imidazole derivative that was used as an antifungal agent. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:trantelinium bromide
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Trantelinium bromide is an anticholinergic and spasmolytic drug, used for the treatment of gastric ulcers.

Showing 49971 - 49980 of 55039 results