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

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Showing 791 - 800 of 24164 results

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

Class (Stereo):
CHEMICAL (ACHIRAL)

Danitracen (WA 335) is an antidepressant compound developed in the 1970s. Danitracen acts by blocking central and peripheral 5-HT receptors: it potentiates testosterone-induced sexual behavior in rats and abolishes the 5-hydroxytryptophan (5-HTP) induced hypermotility in mice. In amphetamine-treated rats, administration of danitracen lowered whole brain serotonin and norepinephrine levels. Danitracen investigated in clinical trials in depressed patients. At 3 mg/day, danitracen was equipotent to 150 mg/day amitriptyline.
Status:
Investigational
Source:
NCT00824421: Phase 2 Interventional Completed HIV-1
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Lersivirine (UK-453,061) is a novel second-generation non-nucleoside reverse transcriptase inhibitor (NNRTI). It binds reverse transcriptase in a distinct way leading to a unique resistance profile. Lersivirine is a second-line NNRTI, which was investigated in a Phase IIb clinical trial. Lersivirine has shown encouraging virologic efficacy in a Phase IIa monotherapy study in NNRTI-naive patients. In a Phase IIb clinical trial in ART naive patients, clinical efficacy of lersivirine was compared with efavirenz, each administered together with tenofovir disoproxil fumarate/emtricitabine. After 48 weeks, lersivirine exhibited a slightly lower virologic response but similar immunologic efficacy. However, the trial was not powered for formal hypothesis testing of noninferiority of lersivirine. The development of lersivirine was recently stopped because the developing company determined that the compound would not provide an improvement over existing NNRTIs.
Status:
Investigational
Source:
INN:tiafibrate
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiafibrate is a dithiahexadecanediol derivative patented by Juste S. A. Quimico-Farmaceutica as a hypocholesteremic agent. In rats, Tiafibrate at 125 mg/kg day orally for 14 days gave a 38.8% decrease in blood lipids and a 33.7% decrease in blood cholesterol.
Status:
Investigational
Source:
NCT01704196: Phase 2 Interventional Completed Cocaine Dependence
(2013)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Nepicastat (SYN-117) is a potent and selective inhibitor of dopamine-β-hydroxylase. This compound in Phase 2 of clinical trial for the treatment cocaine addiction and posttraumatic stress disorder.
Status:
Investigational
Source:
INN:tilozepine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tilozepine is a thienobenzazepine derivative patented Wander A.-G. as hypnotic, sedative, antipsychotic, and muscle relaxant. Tilozepine acts as a non-selective antagonist of dopamine receptors and shows neuroleptic activity in animal models.
Status:
Investigational
Source:
INN:soraprazan [INN]
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Soraprazan (remofuscin), a potassium-competitive acid blocker (P-CAB; formerly called an acid pump antagonist [APA]), is being developed by Katairo GmbH for the treatment of Stargardt's disease and dry age-related macular degeneration (AMD). Clinical development is underway for Stargardt's disease and dry age-related macular degeneration in the Netherlands and Germany. On 13 November 2013, orphan designation was granted by the European Commission to Katairo GmbH, Germany, for soraprazan for the treatment of Stargardt’s disease. Soraprazan is a a highly potent reversible, and fast-acting inhibitor of gastric H,K-ATPase. Soraprazan shows immediate inhibition of acid secretion in various in vitro models and in vivo and was found to be more than 2000-fold selective for H,K-ATPase over Na,K- and Ca-ATPases.
Status:
Investigational
Source:
NCT00548925: Phase 2 Interventional Completed Diabetic Neuropathic Pain
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Sofinicline is a selective agonist of the a4b2 subtype of nAChR. It is under development by Abbott Laboratories in collaboration with NeuroSearch. It is produced as a capsule in doses of 1, 2 or 4 mg. Sofinicline is a full agonist of the a4b2 nAChR. It has high binding affinity, ~ 0.1 nM, for this receptor. Sofinicline is orally active and is metabolized hepatically. Sofinicline has been used in trials studying the treatment of ADHD, neuralgia, diabetic neuropathies, diabetic polyneuropathy, and diabetic neuropathic pain, among others.
Status:
Investigational
Source:
INN:furethidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Furethidine, a pethidine analog was studied as an analgesic agent. This compound is not currently used in medicine and is listed in schedules of the single convention on narcotic drugs of 1961 as amended by the 1972 protocol.
Status:
Investigational
Source:
INN:cefetrizole
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Cefetrizole is aminocephalosporanic acid derivative with broad antibacterial activity against penicillin-resistant strains patented by Spanish pharmaceutical company Ferrer Internacional S. A.
Status:
Investigational
Source:
INN:tiamenidine
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tiamenidine (also known as HOE 440) is a diazacycloalkene derivative patented by Farbwerke Hoechst A.-G. as 2 alpha-sympathomimetic antihypertensive agents. In preclinical models, tiamenidine induces hypotension and bradycardia in renal hypertensive cats and rats and in normal rats and dogs. Furthermore, Tiamenidine inhibits the liberation of norepinephrine from nerves leading to the heart and suppress sympathetic circulatory reflexes in dogs. In clinical trials, Tiamenidine exerts favor influences on systolic and diastolic blood pressure, and reduces plasma noradrenaline and adrenaline levels and suppresses plasma renin activity. Unfortunately, during the withdrawal of Tiamenidine, there is a rebound of blood pressure and plasma noradrenaline and adrenaline, overshooting baseline levels.