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

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Showing 1041 - 1050 of 13240 results

Status:
Investigational
Source:
NCT01235520: Phase 3 Interventional Completed Schizophrenia
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)


Conditions:

Bitopertin is a Glycine transporter type 1 inhibitor which was developed by Hoffmann-La Roche for the treatment of patients with schizophrenia. The drug was shown to be potent in vitro, however it failed to meet primary endpoints in phase III. Bitopertin was also tested for the treatment of obsessive-compulsive disorder, but the development stopped in phase II.
Status:
Investigational
Source:
NCT01435226: Phase 2 Interventional Completed Hepatitis C, Chronic
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



GS-9190 (Tegobuvir) a novel nonnucleoside inhibitor of hepatitis C virus NS5B polymerase was investigated for treatment Hepatitis C, Chronic, but on the clinical trial II was discontinued.
Status:
Investigational
Source:
NCT00810147: Phase 2 Interventional Completed Alzheimer's Disease
(2009)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)



Avagacestat (BMS-708163) is an oral gamma secretase inhibitor designed for selective inhibition of amyloid beta (Aβ) synthesis. Avagacestat was in development by Bristol-Myers Squibb for the treatment of Alzheimer's disease (AD). Avagacestat is a potent, selective, orally bioavailable γ-secretase inhibitor of Aβ40 and Aβ42 with IC50 of 0.3 nM and 0.27 nM, demonstrating a 193-fold selectivity against Notch. In November 2012, Bristol-Myers Squibb terminated clinical trials of the drug and announced its decision to end further development of avagacestat
Status:
Investigational
Source:
NCT01168882: Phase 1 Interventional Withdrawn Hematological Malignancies
(2011)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



RGB-286638 is a multi-targeted protein kinase inhibitor currently in Phase 1 clinical testing. In vitro cell-free kinase assays indicated that RGB-286638 inhibits CDK1, 2, 3, 4, 5, and 9 and is less active against CDK6 and 7. The RGB-286638 compound has been shown to inhibit the processes controlling cell division in cancer cells by targeting multiple cyclin-dependent kinase proteins involved in regulating the cell cycle. RGB-286638 has also been shown to induce apoptosis (programmed cell death) and to inhibit other important protein kinases involved in the proliferation of cancer cells. RGB-286638 treatment results in tumor regression and increased survival in a number of pre-clinical models of solid and hematological tumors.
Status:
Investigational
Source:
NCT00619164: Phase 2 Interventional Completed Acute Coronary Syndrome
(2007)
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)



Atopaxar, also known as E 5555 is a novel reversible protease-activated receptor-1 (PAR-1) thrombin receptor antagonist. The inhibition of thrombin-mediated platelet activation by means of protease-activated receptor-1 inhibitors represents an attractive therapeutic option for patients with atherothrombotic disease processes. In preclinical studies, atopaxar demonstrated inhibition of thrombin receptor-activating peptides (TRAP)- and thrombin-induced platelet aggregation. Atopaxar was being developed by Eisai for acute coronary syndromes (ACS) and coronary disorders, including atherothrombosis, unstable angina pectoris and myocardial infarction. Atopaxar was in phase II clinical development in the US, EU and Japan. However, development was discontinued in May 2012.
Status:
Investigational
Source:
NCT04719273: Phase 2 Interventional Active, not recruiting Refractory Endometrial Adenocarcinoma
(2021)
Source URL:

Class (Stereo):
CHEMICAL (ABSOLUTE)

Onapristone is a type I progesterone receptor (PR) antagonist that prevents PR- mediated DNA transcription and was studied as an antitumor agent. This drug possessed activity in breast cancer and is participating in phase II clinical trials to test any good and bad effect for the treatment of endometrial cancer, ovarian cancer, peritoneal cancer, and prostate cancer.
Status:
Investigational
Source:
INN:prodilidine
Source URL:

Class (Stereo):
CHEMICAL (MIXED)

Prodilidine is an arylpyrrolidine derivative patented by Mead Johnson & Co.as moderately potent analgesic. By comparison with other drugs, including morphine, Prodilidine has a prompt and unusually sustained antinociceptive action in rodents by all routes. Prodilidine substantially lacks antipyretic, anti-inflammatory, antitussive, constipating, respiratory depressant, and cardiovascular effects. Prodilidine resembles meperidine in excitatory properties and body-temperature lowering action at high dosage. The d-isomer is about twice as potent and toxic as the l-isomer parenterally; by the gastric route, the difference is markedly less.
Status:
Investigational
Source:
JAN:HYDRAMETHYLNON [JAN]
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Status:
Investigational
Source:
INN:pirogliride
Source URL:

Class (Stereo):
CHEMICAL (ACHIRAL)

Pirogliride is the antidiabetic agent. It has been found to produce a hypoglycemic effect in nondiabetic rats, dogs, mice, and monkeys. To being three to four times more potent than tolbutamide, pirogliride also differs from the sulfonylureas in lowering blood glucose concentrations of streptozotocin-diabetic rats and db/db mice, and, moreover, oral administration to normal fasted dogs did not produce the characteristic rise in insulin concentrations observed with tolbutamide. Pirogliride potentiates glucose-induced insulin secretion from isolated islets. This effect is accompanied by a facilitated glucose metabolism. Pirogliride partially prevents the known inhibitory effects of mannoheptulose on glucose-induced secretion and utilization. Pirogliride was found to produce a concentration-dependent inhibition of gluconeogenesis in rat kidney cortex slices. hepatocytes and perfused liver. Pirogliride was metabolized in man to a small extent by oxidation of the 4-position of the phenyl ring.
Status:
Investigational
Source:
INN:isalmadol [INN]
Source URL:

Class (Stereo):
CHEMICAL (RACEMIC)

ISALMADOL is an analgesic agent.

Showing 1041 - 1050 of 13240 results