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

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Showing 6311 - 6320 of 13501 results

Status:
Investigational
Source:
NCT00540657: Phase 2 Interventional Completed Celiac Disease
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Vercirnon (GSK-1605786, CCX-282, nTraficet-EN) is a selective, and potent antagonist of human CCR9. Vercirnon binds to the intracellular side of the receptor, exerting allosteric antagonism and preventing G-protein coupling. CCR9 is a tissue-specific lymphocyte trafficking molecule that selectively attracts both B- and T-cells to the small gut. Inhibition of CCR9 by GSK-1605786 may inhibit B- and T-cell entry to the small gut and ameliorate inflammation while leaving immune function at other anatomical sites unaffected. Vercirnon is an orally bioavailable, anti-inflammatory agent that is being developed by ChemoCentryx for treatment of inflammatory bowel disease with an initial focus in Crohn's disease. A pivotal phase III programme of vercirnon was initiated in patients with moderate-to-severe Crohn's disease, however, the programme was suspended when the first pivotal trial failed to meet its primary endpoint. Phase II trials for ulcerative colitis and celiac disease were conducted, however investigations for ulcerative colitis were suspended while no further development has been reported for celiac disease.
Status:
Investigational
Source:
NCT02452008: Phase 2 Interventional Active, not recruiting Prostate Cancer
(2016)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Galunisertib is a potent inhibitor of TGF beta type 1 receptor. The drug is under clinical development for the treatment of different cancers: pancreatic, hepatocellular, breast, rectal, prostate etc. and reached phase 2/3 in patients with myelodysplastic syndromes.
Status:
Investigational
Source:
NCT00490516: Phase 2 Interventional Completed Schizophrenia
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)


Conditions:

ACP-104 or N-Desmethylclozapine (NDMC), or norclozapine is a major metabolite of clozapine, which was developed like a small molecule drug candidate by ACADIA for treatment schizophrenia. ACP-104 combines M1 muscarinic agonist, 5-HT2A inverse agonist, and D2 and D3 dopamine partial agonist in a single compound and, therefore, uniquely addresses what ACADIA believed are the three most promising target mechanisms for treating schizophrenia. Then drug was discontinued, because the study did not meet its primary endpoint of antipsychotic efficacy or any of the secondary endpoints. Neither dose of ACP-104 demonstrated improved efficacy as compared to placebo. The most common adverse events in the treatment arms relative to placebo were increased salivation, tachycardia, and dyspepsia, which were noted to be dose-related. There was no clinically significant decrease in neutrophil counts in the study drug arms.
Status:
Investigational
Source:
INN:tienocarbine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Tienocarbine is a thienopyridoindole derivative patented by Troponwerke G.m.b.H. und Co. K.-G. as antidepressant. Tienocarbine acts as a mixed dopamine agonist-antagonist
Status:
Investigational
Source:
INN:tidembersat
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Tidembersat is a benzopyran derivative patented by SmithKline Beecham PLC for treating and preventing a variety of CNS disorders, such as Huntington's chorea, schizophrenia and traumatic brain injury
Status:
Investigational
Source:
INN:tienoxolol
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tienoxolol is a benzoic acid derivative patented by Centre d'Activite et de Recherche Pharmaceutique Industrielle Biologique et Medicale as β-sympatholytic and diuretic. Tienoxolol acts as a beta-adrenergic receptor antagonist shows potent diuretic and natriuretic activity and, besides that anti-hypertension activity in preclinical models. In clinical trials, Tienoxolol significantly and dose-dependently reduced exercise-induced tachycardia. This effect started 1 h after drug administration, peaked between 4 h and 6 h and lasted at least 12 h.
Status:
Investigational
Source:
INN:zolasartan
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Zolasartan (previously known as GR 117289) is an angiotensin II (AT1) receptor antagonist that was studied for the treatment of hypertension. It was undergoing phase II clinical trials with Glaxo Wellcome in the United Kingdom before the study was discontinued.
Status:
Investigational
Source:
INN:zoficonazole
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Zoficonazole was developed as an antibacterial and an antifungal agent. Information about the current use of this compound is not available.
Status:
Investigational
Source:
INN:toprilidine [INN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Toprilidine is an active peripheral vasodilator and sedative agent. 1 to 1.5 ug given intraarterially augmented the blood flow in the Arteria femoralis of dogs by 100%. Five microg/kg i.v. increased the blood flow in the Arteria femoralis in six dogs on an average by 32%.
Status:
Investigational
Source:
INN:tomoglumide
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

Tomoglumide (CR 1392) is the glutaramic acid-derivative. It is a cholecystokinin (CCK) receptor antagonist. The CR 1392 had an inhibitory effect on both CCK-octapeptide (CCK-8)-stimulated immunoreactive insulin (IRI) release and exocrine secretion in the isolated perfused rat pancreas. The concentration of CR 1392 that caused half-maximal inhibition of CCK-8-stimulated IRI release was 300 times lower than that of exocrine secretion. CR 1392 was also effective in reducing the elevated serum amylase activity, pancreatic weight, and histologic alterations even when administered after the pancreatitis had been induced.

Showing 6311 - 6320 of 13501 results